198 results on '"LACTOSE MONOHYDRATE"'
Search Results
2. Design of Experiments (DoE)-based approach for improvement of dry mixing processes in the production of low-dose Alprazolam tablets using Raman spectroscopy for content uniformity monitoring
- Author
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Makraduli Liljana, Makreski Petre, Makraduli Filip, Slaveska-Spirevska Irena, Bakovska-Stoimenova Tanja, Lazarevska-Todevska Elena, Piponski Marjan, Anevska Maja, Glavas-Dodov Marija, Simonoska-Crcarevska Maja, Mladenovska Kristina, Goracinova Katerina, and Geskovski Nikola
- Subjects
alprazolam ,content uniformity ,lactose monohydrate ,response surface factorial experimental design ,raman spectroscopy ,Pharmacy and materia medica ,RS1-441 - Abstract
A low-dose tablet formulation, containing a potent Benzodiazepine derivative Alprazolam was developed, considering the achievement of appropriate content uniformity of the active substance in powder blends and tablets as a major challenge. Two different types of lactose monohydrate (Tablettose 80 and Granulac 200) and two different types of dry mixing processes (high-shear mixing and "in bulk" mixing) were employed. To evaluate the influence of the variables (mixing speed, mixing time, filling level of the high-shear and cube mixer, lactose monohydrate type) and their interactions upon the response (content uniformity of Alprazolam in the powder blends), a Factorial 2 4 design (with 4 factors at 2 levels in 1 block) was generated for each type of mixer. For high-shear dry mixing the Response Surface, D-optimal Factorial 2 4 design (with 2 replications and 31 experiments) was used, while for the "in bulk" dry mixing the Response Surface, Central Composite Factorial 2 4 design (with 34 experiments) was used. The process parameters for the high-shear mixer were varied within the following ranges: filling level of 70-100%, impeller mixing speed of 50-300 rpm and mixing time of 2-10 minutes. For the cube mixer the following process parameter ranges were employed: filling level of 30-60%, mixing speed of 20-390 rpm and mixing time of 2-10 minutes. Raman spectroscopy in conjunction with a validated Partial Least Square (PLS) regression model was used as a Process Analytical Technology (PAT) tool for Alprazolam content determination and content uniformity monitoring. The DoE model was further employed to optimize the powder blending process in regard to the achievement of appropriate Alprazolam content uniformity using high-shear mixing and Tabletosse 80 as filler. The desirability function revealed that the following process parameters: a mixing time of 2 minutes, a mixing speed of 300 rpm and a 70% filling level of the mixer would produce powder blends with the lowest variability in Alprazolam content. The three independent lab batches of low-dose Alprazolam tablets, produced with high-shear mixing using these process parameters, conformed to the requirements of the European Pharmacopoeia for content (assay) of Alprazolam and uniformity of the dosage units.
- Published
- 2023
3. Mechanical relaxation of process-induced structural disorder of α-lactose monohydrate upon particle comminution
- Author
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Bansal, Harsimran, Price, Robert, and Fotaki, Nikoletta
- Subjects
Mechanical Relaxation ,Process Induced Structural Disorder ,a-Lactose Monohydrate ,Lactose Monohydrate ,Particle Comminution ,Comminution ,water activity ,physical properties ,stability ,Conditioning ,Micronised Lactose ,fine particle fraction ,micronized ,Inhalation ,Cohesive interface ,material characteristics ,Characterisation ,FPF ,MMAD ,FPM ,mass median aerodynamic diameter ,aerodynamic diameter ,APSD ,DSC ,Degradation ,Furfural ,humidity and temperature influence ,Water absorption ,Water content ,CAB ,cohesive adhesive balance - Abstract
The physical and chemical properties of orally inhaled powders in capsule-based dry powder inhalers (DPI) are crucial in maintaining a stable and functioning product during its shelf-life. The process history of a material has been known to directly influence formulation structure, performance, thermodynamic stability and shelf-life of a DPI product. It is also well-known that size-reduction processes, such as air-jet micronisation, activate an otherwise stable crystalline form of a material due to the high energy attrition the materials are subjected to. Process-induced structural defects upon particle comminution, which appear almost exclusively at the surface of a processed material, inevitably lead to an unstable, activated state. This energetic state will undergo mechanical relaxation post-micronisation. Relaxation is a thermodynamically driven and a time-dependant process where a material is driven to revert to a more stable form. Certain materials, including micronised lactose monohydrate, may succumb to degradation in the presence of a partial water vapour pressure, and can be rendered unusable during this period of relaxation. It is, therefore, crucial to understand the underlying processes dictating relaxation to achieve better control and a quality-led design of an orally inhaled drug product. This study focused on characterising the inherent disorder associated with micronised α-lactose monohydrate, and identifying methods and mechanisms by which material stability can be restored. An array of physical and chemical characterisation techniques were used to assess the material properties of micronised lactose before and upon conditioning using well-defined conditions of relative humidity and liquefied propellants. These studies indicated that air-jet micronisation can introduce profound changes to the distribution of crystal-bound water within micronised lactose monohydrate. The laagering effects of freshly micronised lactose monohydrate under ambient conditions were also investigated, and suggested an apparent but insignificant amount of dissipation of the energy associated with the mechanical activation process. Studies using controlled environmental conditioning to stabilise micronised lactose monohydrate showed no significant changes in the material's physical properties. However, results showed an unprecedented thermal behaviour in the material. Drastic changes in the distribution of freely-bound water and in the material's lattice were observed. In another study, a novel technique assessing the degradation of freshly micronised and conditioned lactose was undertaken over a six-month period under stressed stability conditions. A volatile degradation molecule was suppressed upon conditioning, suggesting a more stable form of micronised lactose monohydrate may have formed. A study was also undertaken to understand the effect of intense ball milling for size-reduction of primary crystals of lactose monohydrate. With a lower energy input during comminution, ball milling did not induce similar thermal changes observed for micronised lactose whilst its physical character was comparable. In establishing that freely available water under ambient conditions is a major issue for controlling metastable pharmaceutical powders, investigations into the stability and conditioning of commercially available capsule-based DPI products was commenced using water activity measurements. A novel method developed to assess the influence of water activity and equilibrium relative humidity in the headspace surrounding hermetically sealed capsule-based products, suggested that pre-equilibration appears to play a defining role in the successful shelf-life of capsule-based inhaler products. Finally, a study on the stability of a tiotropium formulation was investigated at elevated temperatures across a wide range of relative humidities with time. Results indicated that a relationship between the formulation and the material properties of the capsule may readily degrade the formulation and severely affect shelf-life and product performance.
- Published
- 2018
4. An Investigation into Improvement of Stability and Efficacy of Intravesical BCG Formulations Using Freeze-Drying Technique
- Author
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Hamidreza Hozouri, Dariush Norouzian, and Reza Aboofazeli
- Subjects
bacillus calmette–guérin ,cryoprotectant ,freeze drying ,intravesical bcg ,lactose monohydrate ,mycobacterium bovis ,Medicine ,Biology (General) ,QH301-705.5 - Abstract
Bacillus Calmette–Guérin (BCG) has been used as an intravesical product for the treatment of intermediate and high risk, non-muscle-invasive bladder cancer (NMIBC). Freeze drying technique is highly recommended for product development, however, the microorganism sensitivity to freezing and drying processes is a major chalenge which may lead to poor survival. To overcome this problem, the use of cryoprotectants in intravesical BCG formulation is required. This study was, therefre, planned to design a new formulation, using an attenuated strain of Mycobacterium bovis, which could be produced by freeze drying technique with the aim of prolonging its storage stability and increasing its efficacy as well as the ease of administration. For this purpose, sodium L-glutamate monohydrate (a commonly used stabilizer in domestic BCG suspension formulations) was replaced by lactose monohydrate. New intravesical BCG formulations, both in lyophilized and liquid forms, were eventually evaluated by moisture content assay, viable count assay, bacterial and fungal contamination, safety test and determination of bacterial concentration and O2 consumption. The results were compared with the data obtained for the conventional lyophilized and liquid products. Maximum survival rate was achieved in the presence of 10 % w/v lactose monohydrate for both liquid and lyophilized formulations when stored at less than -10 and 2-8C, respectively. In summary, the freeze-dried formulations developed with lactose monohydrate met the requirements of intravesical BCG in high viability and stability during storage. HIGHLIGHTS • Lyophilization technique and lactose monohydrate as a protecting sugar were used to improve the stability, storage conditions, shelf-life and effcicay of intravesical BCG product. • Maximum survival rate was attained for both liquid and lyophilized lactose-based formulations prepared with 10 %w/v lactose monohydrate and stored at less than -10 and 2-8°C, respectively. • Freeze-dried products possessed higher stability and efficacy in comparison with corresponding liquid preparations.
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- 2021
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5. Lactose: Use, measurement, and expression of results.
- Author
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Portnoy, Matilde and Barbano, David M.
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LACTOSE , *DAIRY processing , *DAIRY products , *CATTLE breeds , *CATTLE breeding , *DAIRY cattle , *MILK yield - Abstract
Lactose has different uses in the dairy, food, and pharmaceutical industries. Being aware of the different forms of lactose and their concentrations can be very helpful in managing dairy product quality, properties, and manufacturing efficiency. Correct measurement and reporting of lactose concentration in milk and other dairy products will be of increased importance in the future as more value-added uses of lactose are developed and as milk lactose data are used in farm management decision making. Lactose should be reported as anhydrous lactose because lactose data will be used to make increasingly important decisions in dairy processing, dairy product labeling, and milk production in the future. Lactose also plays an important role in milk synthesis within a cow. Milk production factors and dairy cattle breed selection influence the amount of high value fat and protein produced per unit of lactose. If the off-farm value of lactose remains low, more attention may be focused on using ultrafiltration to process milk and leave 50 to 60% of the lactose and water from milk at the farm to recover the energy value of the lactose as feed and reduce the hauling cost of the high value components of milk to a dairy product manufacturing factory. Many methods exist to determine lactose concentration, but the most important methods are enzymatic assays, HPLC, and mid-infrared analysis. New, value-added uses for lactose need to be developed. Consistent and accurate methods of lactose measurement and consistent expression of lactose results will support this development process. Starting in January 2017, the USDA Federal Milk Market Laboratories began reporting lactose content of milk as anhydrous lactose and discontinued the reporting of lactose by difference. [ABSTRACT FROM AUTHOR]
- Published
- 2021
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6. Improving Tableting Performance of Lactose Monohydrate by Fluid-Bed Melt Granulation Co-Processing
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Djordje Medarević, Jelena Djuriš, Mirjana Krkobabić, and Svetlana Ibrić
- Subjects
co-processing ,direct compression ,lactose monohydrate ,fluid-bed melt granulation ,self-lubricating excipients ,tableting behaviour ,Pharmacy and materia medica ,RS1-441 - Abstract
Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression.
- Published
- 2021
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7. Development of Four Certified Reference Materials for Water Content in Solids.
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Zhi, X., Wang, H., Wu, Z., and Li, J.
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REFERENCE sources , *KARL Fischer technique , *METHANE hydrates , *DISTRIBUTION isotherms (Chromatography) , *RAW materials , *WATER - Abstract
Water content in solid materials is usually measured by loss on drying and Karl Fischer titration (KFT) methods. The validation of KFT methods requires the certified reference materials (CRMs) for the water content in solids, especially those with lower water content. In the present study, two mixtures of sodium tartrate dihydrate and 4-methoxybenzoic acid were prepared using the gravimetric method and then used as candidates of CRMs with water content of 10.0 and 1.0 mg·g−1, respectively. Furthermore, the CRM of lactose monohydrate and that of 4-methoxybenzoic acid were also developed. The stability against the humidity of the raw materials was characterized using water sorption isotherms. The thermal stability of the raw materials was characterized by the thermogravimetric analyzer. These four CRMs for water content were certified using Karl Fischer coulometric and volumetric titration. To make the water content traceable, both KFT methods were calibrated using a home-made water content standard prepared by the gravimetric method. The average value of the two methods was used as the certified value. The certified water contents and their expanded uncertainties (U, k = 2) of four CRMs were (50.7 ± 0.6) mg·g−1, (9.90 ± 0.2) mg·g−1, (0.878 ± 0.044) mg·g−1 and (0.142 ± 0.013) mg·g−1, respectively. This series of CRMs were suitable for the validation of KFT methods for the water contents in solids. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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8. Caking of anhydrous lactose powder owing to phase transition and solid-state hydration under humid conditions: From microscopic to bulk behavior.
- Author
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Afrassiabian, Zahra and Saleh, Khashayar
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LACTOSE , *PHASE transitions , *HYDRATION , *POWDERS , *CRYSTALLIZATION kinetics , *ACTIVATION energy , *PROTON conductivity - Abstract
This work deals with the phase transition of anhydrous lactose in solid-state due to moisturizing and subsequent crystallization and caking. It was found that anhydrous lactose is converted to lactose monohydrate when exposed to ambient moisture. The conversion rate and the kinetics of transformation were investigated at various temperatures and RH (15 to 40 °C and 70% to 95% RH). The results showed that the kinetic rate and the conversion increase with RH and T. The limiting step was the crystallization of anhydrous β-lactose. A simple kinetic law for the global rate of transformation was developed. The rate constants and the activation energy were calculated by comparison between the experimental data and the model. The effect of storage conditions on the caking behavior and kinetics of anhydrous lactose was also investigated. The results highlighted that the caking of powders was directly related to the fractional conversion of anhydrous lactose. Unlabelled Image • Caking of anhydrous lactose powders at RH > 70% occurs by crystallization. • Cakes strength is related to the extent of anhydrous to monohydrate conversion. • An apparent kinetics law for crystallization was established experimentally. • Hard cakes are obtained for conversion rates higher than 8%. • Soft cakes appears from almost 4% conversion. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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9. Somatic Cell Count and Milk Yield Losses in Goats
- Author
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Oto Hanuš, Petr Roubal, Josef Kučera, Marcela Klimešová, Radoslava Jedelská, and Jaroslav Kopecký
- Subjects
individual goat milk ,lactation ,fat ,crude protein ,lactose monohydrate ,milk secretion disorders ,Agriculture ,Biology (General) ,QH301-705.5 - Abstract
This work is aimed at prediction and quantification of goat milk yield (MY, kg) losses by the somatic cell count (SCC, 103.ml−1) in milk recording. The goal is to support the prevention of milk secretion disorders, milk yield and quality. During two years there were evaluated composition and properties of individual milk samples (n = 1 173). There were included animals of brown short‑haired (BSH) breed and BSH × white short‑haired in one flock. The linear and nonlinear regression, interpolation, extrapolation, approximation and qualified estimation were used for milk losses prediction along the SCC. The relevant values of the SCC arithmetic and geometric mean and median and MY arithmetic mean were: 1,400 103.ml−1 (with high variability of 128 %), 745 and 747 103.ml−1; 2.94 kg/ day. The relationship between fat and crude protein had a correlation coefficient of 0.395, P < 0.001. There were stated the correlations between SCC and: lactose −0.416, P < 0.001; solids non fat −0.25, P < 0.001; MY −0.135, P < 0.01. The relationship between SCC and MY was negative along months, 6 cases out of 7 and significant in March and May (P < 0.05 and P < 0.01). For instance predicted MY for SCC intervals 1–1.999, 2–2.999, 3–3.999, 4–4.999, 5–5.999, 6–6.999 and ≥ 7 thousands 103.ml−1 may be 3.99, 3.77, 3.6 , 3.46, 3.33, 3.23 and 3.13 kg in 3rd month etc. The corresponding MY losses by SCC are evident from this trend. The result use is focused on the original dairy goat farm and use elsewhere is possible in farms with similar SCC, goat milk yield and rearing system.
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- 2017
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10. Stability behaviour of antiretroviral drugs and their combinations. 9: Identification of incompatible excipients.
- Author
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Kurmi, Moolchand, Sahu, Archana, Ladumor, Mayurbhai Kathadbhai, Kumar Bansal, Arvind, and Singh, Saranjit
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- *
ANTIRETROVIRAL agents , *ABACAVIR , *LACTOSE , *SODIUM dodecyl sulfate , *TENOFOVIR - Abstract
Graphical abstract Highlights • Antiretroviral drugs-excipient compatibility studies were performed. • Abacavir formed two interaction products with lactose monohydrate. • Sodium lauryl sulphate enhanced the degradation of tenofovir disoproxil fumarate. • Interaction products were identified and characterized through LC-MS/TOF and NMR. • In-silico toxicity and ADMET properties were evaluated for identified interaction products. Abstract Incompatibility studies of antiretroviral drugs, viz., lamivudine (3TC), emtricitabine (FTC), abacavir sulfate (ABC), tenofovir disoproxil fumarate (TDF), zidovudine (ZDV), efavirenz (EFV) and nevirapine (NVP) were carried out in the presence of ten selected excipients, i.e., microcrystalline cellulose, lactose monohydrate, starch, magnesium stearate, sodium lauryl sulfate, sodium starch glycolate, croscarmellose sodium, colloidal silica, povidone K-30 and hydroxypropyl cellulose. Among all, ABC showed reaction with lactose monohydrate, resulting in the formation of two interaction products, while sodium lauryl sulphate enhanced the degradation of TDF. The interaction products of ABC-Lactose were separated by high performance liquid chromatography (HPLC) and subjected to liquid chromatography-high resolution mass spectrometry (LC-HRMS) studies for their characterization. One of the products was also isolated and subjected to 1D and 2D nuclear magnetic resonance (NMR) studies for structural confirmation. The toxicity of both was predicted using TOPKAT and ADMET™ software and compared to the drug. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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11. Modelling the Mechanical Behaviour of a Pharmaceutical Tablet Using PDEs
- Author
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Ahmat, Norhayati, Ugail, Hassan, Castro, Gabriela González, Günther, Michael, editor, Bartel, Andreas, editor, Brunk, Markus, editor, Schöps, Sebastian, editor, and Striebel, Michael, editor
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- 2012
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12. High-Resolution THz Spectroscopy to Measure Strong THz Absorption Signatures of si-RNA in Solution
- Author
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Brown, E. R., Mendoza, E. A., Kuznetsova, Y., Neumann, A., Brueck, S. R. J., Pereira, Mauro F., editor, and Shulika, Oleksiy, editor
- Published
- 2011
- Full Text
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13. Quantitative and qualitative use of thermal analysis for the investigation of the properties of granules during fluid bed melt granulation.
- Author
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Regdon, Géza and Korteby, Yasmine
- Subjects
- *
THERMAL analysis , *GRANULATION , *REACTION mechanisms (Chemistry) , *AGGLOMERATION (Materials) , *VISCOSITY - Abstract
This study describes a novel approach for the use of thermal analysis to study the aftermath of the fluid bed melt granulation process and to depict the growth mechanism of the granules by quantifying the enthalpies of the granules at every physicochemical change using DSC and their mass loss through TG coupled to MS for a qualitative determination of the composition and amount of the evolved gases for the corresponding fragment ion. The experiments were made in situ with lactose monohydrate and two viscosity grades of PEG (2000 and 6000) as meltable binders with different contents and size fractions. DSC showed the presence of a beta lactose endotherm peak after the melting of alpha lactose and a proportional increase in its intensity with the increase in the particle size and the content of the binder, which suggested a relation with the agglomeration growth. Interestingly, TG and MS showed a larger reduction in the water content from lactose with the increase in the binder particle size, making it possible to evaluate the dehydration during the melt granulation. Indeed, during the distribution mechanism the low binder particle size and viscosity exposed lactose to a high heat transfer from the fluidizing air. However, a high binder particle size results in lactose immersed in the PEG particles, causing water to be trapped inside the granules and hence a larger reduction in water mass loss indicating the immersion mechanism. Therefore, thermal analysis is a promising tool for granulation growth control. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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14. Crystal engineering of lactose using electrospray technology: carrier for pulmonary drug delivery.
- Author
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Patil, Sharvil, Mahadik, Abhijeet, Nalawade, Pradeep, and More, Priyesh
- Subjects
LACTOSE ,DRUG delivery systems ,PHARMACEUTICAL powders ,ELECTROSPRAY ionization mass spectrometry ,AEROSOL therapy - Abstract
Context:Dry powder inhalers (DPIs) consisting of a powder mixture containing coarse carrier particles (generally lactose) and micronized drug particles are used for lung drug delivery. The effective drug delivery to the lungs depends on size and shape of carrier particles. Thus, various methods have been proposed for engineering lactose particles to enhance drug delivery to lungs. Objective:The objective of current work was to assess suitability of electrospray technology toward crystal engineering of lactose. Further, utility of the prepared lactose particles as a carrier in DPI was evaluated. Materials and methods:Saturated lactose solutions were electrosprayed to obtain electrosprayed lactose (EL) particles. The polymorphic form of EL was determined using Fourier transform infrared spectroscopy, powder X-ray diffractometry, and differential scanning calorimetry. In addition, morphological, surface textural, and flow properties of EL were determined using scanning electron microscopy and Carr’s index, respectively. The aerosolization properties of EL were determined using twin-stage impinger and compared with commercial lactose particles [Respitose®(SV003, Goch, Germany)] used in DPI formulations. Results and discussion:EL was found to contain both isomers (α and β) of lactose having flow properties comparable to Respitose®(SV003). In addition, the aerosolization properties of EL were found to be significantly improved when compared to Respitose®(SV003) which could be attributed to morphological (high elongation ratio) and surface characteristic (smooth surface) alterations induced by electrospray technology. Conclusion:Electrospray technology can serve as an alternative technique for continuous manufacturing of engineered lactose particles which can be used as a carrier in DPI formulations. [ABSTRACT FROM PUBLISHER]
- Published
- 2017
- Full Text
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15. Industrial application of QbD and NIR chemometric models in quality improvement of immediate release tablets
- Author
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Mohamed Abdallah, Ahmed M. Ramadan, and Emad B. Basalious
- Subjects
Near Infrared Spectroscopy (NIRS) ,NIR, Near Infra-red ,Quality management ,PCA, Principal Component Analysis ,QbD, Quality by Design ,Pharmaceutical Science ,RM1-950 ,02 engineering and technology ,PC, Principal Component ,SEM, Structural Equation Modelling ,030226 pharmacology & pharmacy ,Quality by Design ,Chemometrics ,PLS, Partial Least Square ,03 medical and health sciences ,0302 clinical medicine ,Artificial Intelligence ,Sodium Starch Glycolate ,Immediate release ,Content Uniformity ,Process engineering ,Dissolution ,Mathematics ,Quality by Design (QbD) ,Pharmacology ,business.industry ,021001 nanoscience & nanotechnology ,RMSEP, Root Mean Square Error of Prediction ,LACTOSE MONOHYDRATE ,PAT, Process Analytical Technology ,Formulation ,Original Article ,Therapeutics. Pharmacology ,0210 nano-technology ,business ,Design space - Abstract
Quality by Design (QbD) and chemometric models are different sides of the same coin. While QbD models utilize experimentally designed settings for optimization of some quality attributes, these settings can also be utilized for chemometric prediction of the same attributes. We aimed to synchronize optimization of comparative dissolution results of carvedilol immediate release tablets with chemometric prediction of dissolution profile and content uniformity of the product. As an industrial application, selection of variables for optimization was done by performing risk assessment utilizing the archived product records at the pharmaceutical site. Experimental tablets were produced with 20 different settings with the variables being contents of sucrose, sodium starch glycolate, lactose monohydrate, and avicel Ph 101. Contents of the excipients were modelled with F1 dissimilarity factor and F2 similarity factor in HCL, acetate, and USP dissolution media to determine the design space. We initiatively utilized Partial Least Square based Structural Equation Modelling (PLS-SEM) to explore how the excipients and their NIR records explained dissolution of the product. Finally, the optimized formula was utilized with varied content of carvedilol for chemometric prediction of the content uniformity.
- Published
- 2021
16. The influence of porosity on tablet subdivision
- Author
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Mariana Landin, Izabel Cristina Rodrigues da Silva, Livia L. Sa-Barreto, Ricardo Neves Marreto, Marcilio Cunha-Filho, Guilherme M. Gelfuso, Maíra T. Teixeira, and Tais Gratieri
- Subjects
Materials science ,business.industry ,General Chemical Engineering ,02 engineering and technology ,Mechanical resistance ,021001 nanoscience & nanotechnology ,Friability ,Microstructure ,Diluent ,LACTOSE MONOHYDRATE ,Microcrystalline cellulose ,chemistry.chemical_compound ,020401 chemical engineering ,chemistry ,General Materials Science ,0204 chemical engineering ,Composite material ,0210 nano-technology ,business ,Porosity ,Subdivision - Abstract
A tablet microstructure, especially the porosity, is a crucial parameter that influences the mechanical properties. Herein, tablet subdivisions were studied as a function of tablet porosity. The tablets were manufactured in the presence of different diluents, namely microcrystalline cellulose, Ludipress®, or lactose monohydrate. Furthermore, the addition of Camphor was investigated, which was thereafter sublimated with a view of obtaining tablets having varying degrees of porosity. Microstructural assays were correlated to the subdivision performance. The increase in porosity reduced the hardness and increased the tablet friability, adversely impacting the subdivision. For all the excipients, an increase in relative porosity >90% represented the threshold level from which an inadequate subdivision occurred. The increase in tablet porosity led to a reduction in mechanical resistance, which, combined with a heterogeneous and discontinuous distribution of pores within the matrix, resulted in poor subdivision results. Controlling tablet porosity is an important consideration when designing tablets having a subdivision purpose.
- Published
- 2020
17. SOMATIC CELL COUNT AND MILK YIELD LOSSES IN GOATS.
- Author
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HANUŠ, OTO, ROUBAL, PETR, KUČERA, JOSEF, KLIMEŠOVÁ, MARCELA, JEDELSKÁ, RADOSLAVA, and KOPECKÝ, JAROSLAV
- Subjects
- *
DAIRY mixes , *DAIRY products , *SOMATIC cells , *GOATS , *LIVESTOCK - Abstract
This work is aimed at prediction and quantification of goat milk yield (MY, kg) losses by the somatic cell count (SCC, 103.ml-1) in milk recording. The goal is to support the prevention of milk secretion disorders, milk yield and quality. During two years there were evaluated composition and properties of individual milk samples (n = 1 173). There were included animals of brown short-haired (BSH) breed and BSH x white short-haired in one flock. The linear and nonlinear regression, interpolation, extrapolation, approximation and qualified estimation were used for milk losses prediction along the SCC. The relevant values of the SCC arithmetic and geometric mean and median and MY arithmetic mean were: 1,400 103.ml-1 (with high variability of 128 %), 745 and 747 103.ml-1; 2.94 kg/ day. The relationship between fat and crude protein had a correlation coefficient of 0.395, P < 0.001. There were stated the correlations between SCC and: lactose -0.416, P < 0.001; solids non fat -0.25, P < 0.001; MY -0.135, P < 0.01. The relationship between SCC and MY was negative along months, 6 cases out of 7 and significant in March and May (P < 0.05 and P < 0.01). For instance predicted MY for SCC intervals 1--1.999, 2--2.999, 3--3.999, 4--4.999, 5--5.999, 6--6.999 and ≥ 7 thousands 103.ml-1 may be 3.99, 3.77, 3.6 , 3.46, 3.33, 3.23 and 3.13 kg in 3rd month etc. The corresponding MY losses by SCC are evident from this trend. The result use is focused on the original dairy goat farm and use elsewhere is possible in farms with similar SCC, goat milk yield and rearing system. [ABSTRACT FROM AUTHOR]
- Published
- 2017
- Full Text
- View/download PDF
18. Influence of the Glidant on Diluent Flow Characterization Using Shear Cell Method
- Author
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Paulo Costa, José Eduardo Silva, Mafalda Machado, PJ Salústio, and Telmo Nunes
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Materials science ,Flow (psychology) ,Analytical chemistry ,Pharmaceutical Science ,Fraction (chemistry) ,Diluent ,LACTOSE MONOHYDRATE ,Shear cell ,chemistry.chemical_compound ,Caking ,Glidant ,chemistry ,Drug Discovery ,medicine ,Lactose ,medicine.drug - Abstract
The aim of this study was to compare the bulk lactose flow behavior with a defined fraction with smaller particles obtained by sieving from the bulk lactose and to evaluate the effect of a glidant addition on both samples. These powders showed, in a previous work, similar flow indexes (ffc) that motivated the addition of colloidal silicon dioxide in order to observe if there were any changes in their flow behaviors. To evaluate this effect on the diluent flow behavior, the methods described in the European Pharmacopeia were used. The results obtained from conventional methods and shear cell methods (using the Powder Flow Tester) were compared, and they showed evident differences in the bulk and tapped densities values and flow classifications. The lactose monohydrate (FTotal) and lactose with particles smaller than 63 μm (F
- Published
- 2020
19. A Simplex Centroid Design to Quantify Triboelectric Charging in Pharmaceutical Mixtures
- Author
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Shivangi Naik, Raj Mukherjee, Sameera Sansare, Bodhisattwa Chaudhuri, and Aritra Halder
- Subjects
Materials science ,Statistical design ,food and beverages ,Pharmaceutical Science ,Centroid ,Lactose ,02 engineering and technology ,021001 nanoscience & nanotechnology ,Methacrylate ,030226 pharmacology & pharmacy ,Wall material ,LACTOSE MONOHYDRATE ,Excipients ,Microcrystalline cellulose ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Theophylline ,chemistry ,Chemical engineering ,Powders ,0210 nano-technology ,Ternary operation ,Triboelectric effect ,Tablets - Abstract
The present study focuses on the implementation of a modified simplex centroid statistical design to predict the triboelectrification phenomenon in pharmaceutical mixtures. Two drugs (Ibuprofen and Theophylline), 2 excipients (lactose monohydrate and microcrystalline cellulose/MCC), and 2 blender wall materials (aluminum and poly-methyl methacrylate) were studied to identify the trends in charge transfer in pharmaceutical blends. The statistical model confirmed the excipient-drug interactions, irrespective of the blender wall materials, as the most significant factor leading to reduced charging. Also, lactose monohydrate was able to explain the charge variability more consistently compared with MCC powders when used as secondary material. The ratio of the individual components in the blends explained almost 80% of the bulk charging for Ibuprofen mixtures and 70% for Theophylline mixtures. The study also explored the potential lack of efficacy of lactose-MCC as a combination in ternary systems when compared with binary mixtures, for impacts on charge variability in pharmaceutical blends.
- Published
- 2020
20. Expedited Investigation of Powder Caking Aided by Rapid 3D Prototyping of Testing Devices
- Author
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Jens Risbo, Jukka Rantanen, Cosima Hirschberg, Changquan Calvin Sun, and Johan Boetker
- Subjects
Rapid prototyping ,Cylindrical geometry ,Time Factors ,Materials science ,Sample geometry ,Pharmaceutical Science ,Lactose ,Equipment Design ,Talc ,LACTOSE MONOHYDRATE ,High-Throughput Screening Assays ,Workflow ,Excipients ,Caking ,Key factors ,Materials Testing ,Printing, Three-Dimensional ,Anticaking agent ,medicine ,Technology, Pharmaceutical ,Powders ,Composite material ,medicine.drug - Abstract
Powder caking can dramatically affect powder handling and downstream production processes. Understanding the key factors that contribute to bulk powder caking is crucial. This article introduces the Hirschberg caking device (HCD), which is a 3D-printed device allowing for parallel testing of powder caking in a cylindrical geometry. In the HCD setup, the powder sample is stored in controlled conditions in the sample holder. On removal of the sample holder, the caked powder will remain in the shape determined by the sample geometry while the remaining powder will fall down. Caking indices can be calculated based on image analysis and weight measurement. The results obtained for the caking of lactose monohydrate with the HCD were in good agreement with the results obtained by a ring shear tester. In addition, a strain tester was used to measure the strength of the formed cakes. Using this approach, critical storage conditions and the required concentration of a given anticaking agent (talc) for lactose monohydrate could be identified. This work demonstrates the potential of rapid prototyping in powder characterization by introducing a fast and affordable approach for exploring and trouble-shooting powder caking.
- Published
- 2020
21. Испитивање утицаја величине честица везивног средства на својства копроцесованих ексципијенаса добијених поступком гранулације топљењем
- Author
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Karajanev, Kristina, Petrović, Nađa, Aleksić, Ivana, and Glišić, Teodora
- Subjects
Precirol® ,paracetamol ,co-processed excipient ,lactose monohydrate ,melt granulation - Abstract
Потреба за новим ексципијенсима унапређених карактеристика, довела је до развоја копроцесованих ексципијенаса, који представљају комбинацију конвенционалних ексципијенаса обрађених различитим технолошким поступцима, а у односу на физичке имају унапређене физичко-механичке карактеристике. A need for new excipients with improved characteristics has led to development of co-processed excipients, representing a combination of conventional excipients prepared by different technological processes, which have improved physicomechanical characteristicsin comparison with simplephysical mixtures.
- Published
- 2022
22. Experimental procedures — Estimation of major food constituents
- Author
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James, C. S. and James, C. S.
- Published
- 1995
- Full Text
- View/download PDF
23. Solution properties and taste behavior of lactose monohydrate in aqueous ascorbic acid solutions at different temperatures: Volumetric and rheological approach.
- Author
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Sarkar, Abhijit and Sinha, Biswajit
- Subjects
- *
LACTOSE , *TASTE testing of food , *VITAMIN C , *AQUEOUS solutions , *RHEOLOGY , *SOLVATION , *VISCOSITY - Abstract
The densities and viscosities of lactose monohydrate in aqueous ascorbic acid solutions with several molal concentrations m = (0.00–0.08) mol kg −1 of ascorbic acid were determined at T = (298.15–318.15) K and pressure p = 101 kPa. Using experimental data apparent molar volume ( ϕ V ), standard partial molar volume ( ϕ V 0 ), the slope ( S V ∗ ), apparent specific volumes ( ϕ Vsp ), standard isobaric partial molar expansibility ( ϕ E 0 ) and its temperature dependence ( ∂ ϕ E 0 / ∂ T ) P , the viscosity B -coefficient and solvation number ( S n ) were determined. Viscosity B -coefficients were further employed to obtain the free energies of activation of viscous flow per mole of the solvents ( Δ μ 1 0 ≠ ) and of the solute ( Δ μ 2 0 ≠ ). Effects of molality, solute structure and temperature and taste behavior were analyzed in terms of solute-solute and solute-solvent interactions; results revealed that the solutions are characterized predominantly by solute-solvent interactions and lactose monohydrate behaves as a long-range structure maker. [ABSTRACT FROM AUTHOR]
- Published
- 2016
- Full Text
- View/download PDF
24. Improving tableting performance of lactose monohydrate by fluid-bed melt granulation co-processing
- Author
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Medarević, Đorđe, Medarević, Đorđe, Đuriš, Jelena, Krkobabić, Mirjana, Ibrić, Svetlana, Medarević, Đorđe, Medarević, Đorđe, Đuriš, Jelena, Krkobabić, Mirjana, and Ibrić, Svetlana
- Abstract
Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression.
- Published
- 2021
25. Determination of microbial recovery for some pharmaceutical raw materials and passive monitoring at production area and microbiology laboratory at Egyptian pharmaceutical company
- Author
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Mohamed Mohamed, Salah Abdelbary, Mohammed Mohammed Azab, Saad El-Din Hassan, and Amr Fouda
- Subjects
Plate method ,Production area ,business.industry ,Environmental science ,Microbiological quality ,Contamination ,Raw material ,business ,LACTOSE MONOHYDRATE ,Control methods ,Microbiology ,Pharmaceutical industry - Abstract
Objective: This study aims to evaluate the validity of pharmaceutical raw materials obtained from an Egyptian pharmaceutical factory to ensure the accuracy of the examination findings before they are used in the manufacturing process. On the other hand, it also aims to determine the environmental microbial count at the microbiology laboratory and production areas to prevent microbial contamination during production and during microbiological analysis. Methods: Assessment of microbiological quality control according to pharmacopeia as plate method by using TSB media with a concentration of 0.1% tween 80, for passive monitoring using settled plate (TSA) media. Results: the percentage of microbial recovery for lactose monohydrate was 89%, 85%, 94%, 92%, 91%, and 91%, while Croscarmellose recorded 81%, 85%, 85%, 85%, and 88%, Mannitol recorded 86%, 85%, 91%, 83%, 86%, and 88%, Magnesium stearate recorded 91%, 85%, 94%, 89%, and 91%, and finally, Talc Powder recorded 94%, 85%, 94%, 91%, 87% and 85% for Pseudomonas aeruginosa, Salmonella enterica, Staphylococcus aureus, Candida albicans, Bacillus subtilis and Escherichia coli respectively for each pharmaceutical raw material. Methods of analysis recorded under acceptance criteria in the selected pharmaceutical factory according to pharmacopeia. On the other hand, the microbial quality of air for the production area selected by an Egyptian pharmaceutical company was under acceptance limits. Conclusion: All quality control methods and assessments of pharmaceutical raw materials, laboratories, and production areas must be performed to measure and control microbial contamination in the pharmaceutical industry and then produce high-quality pharmaceutical products free of microbial contamination, and methods of analysis must be recorded under acceptance criteria in the selected pharmaceutical factory according to pharmacopeia. On the other hand, the microbial quality of the air for the production area and microbiology laboratory that was selected by an Egyptian pharmaceutical company was under accepted limits. All quality control methods and assessments of pharmaceutical raw materials, laboratories, and production areas must be performed to measure and control microbial contamination in the pharmaceutical industry and then produce high-quality pharmaceutical products free of microbial contamination.
- Published
- 2021
26. Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions
- Author
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Hisham Al-Obaidi, Thomas Hibbard, Amy Granger, and Sefinat Opesanwo
- Subjects
Drug ,Lung deposition ,media_common.quotation_subject ,Inhaled drug ,Pharmaceutical Science ,Nanotechnology ,02 engineering and technology ,Review ,030226 pharmacology & pharmacy ,03 medical and health sciences ,0302 clinical medicine ,Pharmacy and materia medica ,coamorphous ,Medicine ,cocrystals ,media_common ,Inhalation ,business.industry ,solubility ,dry powder inhalers ,021001 nanoscience & nanotechnology ,Antimicrobial ,LACTOSE MONOHYDRATE ,RS1-441 ,Drug delivery ,pulmonary drug delivery ,0210 nano-technology ,business ,Flow properties - Abstract
It is well established that currently available inhaled drug formulations are associated with extremely low lung deposition. Currently available technologies alleviate this low deposition problem via mixing the drug with inert larger particles, such as lactose monohydrate. Those inert particles are retained in the inhalation device or impacted in the throat and swallowed, allowing the smaller drug particles to continue their journey towards the lungs. While this seems like a practical approach, in some formulations, the ratio between the carrier to drug particles can be as much as 30 to 1. This limitation becomes more critical when treating lung conditions that inherently require large doses of the drug, such as antibiotics and antivirals that treat lung infections and anticancer drugs. The focus of this review article is to review the recent advancements in carrier free technologies that are based on coamorphous solid dispersions and cocrystals that can improve flow properties, and help with delivering larger doses of the drug to the lungs.
- Published
- 2021
27. Nanostructured Valsartan Microparticles with Enhanced Bioavailability Produced by High-Throughput Electrohydrodynamic Room-Temperature Atomization
- Author
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Julia Hrakovsky, Maria Pardo-Figuerez, Cristina Prieto, Jose M. Lagaron, Zoran Evtoski, Ministerio de Ciencia, Innovación y Universidades (España), Generalitat Valenciana, European Commission, and Programa Iberoamericano de Ciencia y Tecnología para el Desarrollo
- Subjects
Materials science ,Chemistry, Pharmaceutical ,Drug Compounding ,Pharmaceutical Science ,Nanoparticle ,Biological Availability ,02 engineering and technology ,030226 pharmacology & pharmacy ,Article ,Excipients ,03 medical and health sciences ,Crystallinity ,Surface-Active Agents ,0302 clinical medicine ,Differential scanning calorimetry ,Hypromellose Derivatives ,Nanonization ,Pulmonary surfactant ,Dynamic light scattering ,Enhanced bioavailability ,HPMC ,Drug Discovery ,medicine ,Humans ,Particle Size ,Antihypertensive Agents ,Hexoses ,Drug Carriers ,BCS II drug, valsartan, nanonization, HPMC, lactose monohydrate, enhanced bioavailability ,Temperature ,Lactose monohydrate ,021001 nanoscience & nanotechnology ,BCS II drug ,Drug Liberation ,Chemical engineering ,Valsartan ,Solubility ,Permeability (electromagnetism) ,Molecular Medicine ,Nanoparticles ,Particle size ,Caco-2 Cells ,0210 nano-technology ,Crystallization ,medicine.drug - Abstract
The high-throughput drying and encapsulation technique called electrospraying assisted by pressurized gas (EAPG) was used for the first time to produce nanostructured valsartan within microparticles of excipients. Valsartan, a poorly absorbed and lipid-soluble drug, was selected since it is considered a good model for BCS class II drugs. Two different polymeric matrices were selected as excipients, i.e., hydroxypropyl methylcellulose (HPMC) and lactose monohydrate, while Span 20 was used as a surfactant. The produced 80% valsartan loading formulations were characterized in terms of morphology, crystallinity, in vitro release, in vitro Caco-2 cells’ permeability, and in vivo pharmacokinetic study. Spherical microparticles of ca. 4 μm were obtained within which valsartan nanoparticles were seen to range from 150 to 650 nm. Wide-angle X-ray scattering and differential scanning calorimetry confirmed that valsartan had a lower and/or more ill-defined crystallinity than the commercial source, and photon correlation spectroscopy and transmission electron microscopy proved that it was dispersed and distributed in the form of nanoparticles of controlled size. In vitro dissolution tests showed that the HPMC formulation with the lowest API particle size, i.e., 150 nm, dissolved 2.5-fold faster than the commercial valsartan in the first 10 min. This formulation also showed a 4-fold faster in vitro permeability than the commercial valsartan and a 3-fold higher systemic exposure than the commercial sample. The results proved the potential of the EAPG processing technique for the production of safe-to-handle microparticles containing high quantities of a highly dispersed and distributed nanonized BCS class II model drug with enhanced bioavailability., This research was funded by the Spanish Ministry of Science and Universities (project RTI-2018-097249-B-C1), the Valencian Innovation Agency BIOENCAP project (reference no. INNCAD00-18-31), the H2020 EU projects FODIAC (reference no. 778388), the CAPSULTEK (reference no. 873827), and the CYTED thematic network (reference no. 319RT0576).
- Published
- 2021
28. Continuous Antisolvent Crystallization of α-Lactose Monohydrate: Impact of Process Parameters, Kinetic Estimation, and Dynamic Analysis
- Author
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Shailesh Agrawal, Nitin Pawar, and Ravi Methekar
- Subjects
Materials science ,010405 organic chemistry ,Organic Chemistry ,010402 general chemistry ,Kinetic energy ,01 natural sciences ,LACTOSE MONOHYDRATE ,0104 chemical sciences ,law.invention ,Chemical engineering ,law ,Continuous crystallization ,Scientific method ,Physical and Theoretical Chemistry ,Crystallization - Abstract
Continuous crystallization has recently gained attention in industrial crystallization. This paper summarizes the study of continuous antisolvent crystallization of α-lactose monohydrate using etha...
- Published
- 2019
29. Физико-химические и технологические характеристики зюзника европейского травы экстракта сухого и композиции на его основе
- Subjects
Synthetic drugs ,chemistry.chemical_compound ,Traditional medicine ,chemistry ,biology ,Magnesium stearate ,Medicinal plants ,biology.organism_classification ,LACTOSE MONOHYDRATE ,Lycopus europaeus - Abstract
Today, mainly synthetic drugs are used for the prevention and treatment of thyroid diseases. Along with this, the development of drugs based on dry extracts of medicinal plants of special interest. The article reports on the physicochemical and technological properties of a dry extract from Lycopus europaeus L. herbs as well as on the selection of auxiliary substances and the study of technological characteristics of the experimental samples containing this dry extract. For the drug preparation in capsules, a method of stepwise mixing of medicinal and auxiliary substances is proposed. The results of research showed that the optimum technological characteristics are offered by a composition including lactose monohydrate, Aerosil A380, and magnesium stearate of plant origin as auxiliary substances.
- Published
- 2019
30. Comparison between the next generation impactor and the twin glass impinge as model pulmonary drug delivery devices
- Author
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Huner K. Omer, Hewa Abdulla Hamadameen, and Nozad Rashid Husein
- Subjects
Chromatography ,business.industry ,Constant flow ,Inhaler ,animal diseases ,lcsh:R ,lcsh:Medicine ,02 engineering and technology ,Salbutamol Sulphate ,021001 nanoscience & nanotechnology ,030226 pharmacology & pharmacy ,Two stages ,LACTOSE MONOHYDRATE ,Dry-powder inhaler ,03 medical and health sciences ,Dry powder inhaler ,0302 clinical medicine ,Drug delivery ,Medicine ,Next generation impactor ,0210 nano-technology ,business ,Twin glass impinge - Abstract
Background and objective: The British Pharmacopoeia contains four apparatus for testing inhalers. Two of these are the next generation impactor, and the twin glass impinge which differs in their use. The next generation impactor apparatus should ideally have at least five stages; even though the twin glass impinge has only two stages, it is still listed in the British Pharmacopoeia. The next generation impactor is more accurate, reliable and sophisticated than the twin glass impinger. This study gives a detailed comparison of the two pieces of equipment. Methods: Carriers including mannitol, lactose monohydrate, trehalose and sucrose with active pharmaceutical ingredient; salbutamol sulphate were delivered by dry powder inhaler using the next generation impactor and twin glass impinger at a constant flow rate of 60L/min. Results: The twin glass impinge respirable fractions of the powders were higher than the next generation impactor for each carrier. As expected, mannitol powder had the lowest percentage remaining in the capsule compared to lactose monohydrate, trehalose and sucrose had the greatest percentage remaining for both inhaler devices. Conclusion: Even though both apparatus are important for in-vitro studies of drug delivery into the lungs using inhaler devices, the next generation impactor is better suited when a specific size range is required. The twin glass impinger is useful for simple inhaler testing, and the inclusion within the British Pharmacopoeia is justified.
- Published
- 2019
31. Effect of lignin on the release rate of acetylsalicylic acid tablets
- Author
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Maurice N. Collins, Gavin Walker, Javed Iqbal, Mahboubeh Pishnamazi, and Saeed Shirazian
- Subjects
Chemistry, Pharmaceutical ,Drug Compounding ,Lactose ,02 engineering and technology ,Lignin ,Biochemistry ,03 medical and health sciences ,chemistry.chemical_compound ,Tableting ,Hardness ,Structural Biology ,Humans ,Dissolution testing ,Cellulose ,Molecular Biology ,Dissolution ,030304 developmental biology ,Active ingredient ,0303 health sciences ,Chromatography ,Aspirin ,Chemistry ,General Medicine ,021001 nanoscience & nanotechnology ,LACTOSE MONOHYDRATE ,Microcrystalline cellulose ,Drug Liberation ,Solubility ,Drug release ,0210 nano-technology ,Tablets - Abstract
The main focus of this paper is on the improvement of formulations utilising non-conventional bio-based excipients to improve tablet release rates. Two different formulations were considered. The first formulation contains Alcell lignin, lactose monohydrate and microcrystalline cellulose as excipients and acetylsalicylic acid (aspirin) as active pharmaceutical ingredient (API). The second formulation contains lactose monohydrate and microcrystalline cellulose as excipients and aspirin as API. The prepared formulations were roller compacted followed by milling, sieving, and tableting. The tablets were then characterised in terms of dissolution rate in order to compare the release rates. Results indicated that tablets containing Alcell lignin have quicker release, faster disintegration times and higher tablet hardness for all samples with differing process parameters. Higher API dissolution has been attributed to the amorphous structure of lignin and its interaction with aspirin, which increases dissolution of the API.
- Published
- 2019
32. In vitro and in vivo evaluation of the taste-masking efficiency of Amberlite IRP88 as drug carries in chewable tablets
- Author
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Xiaopeng Han, Shan Zhang, Lei Yang, Zhuodong Chai, Chao Qin, Lifang Yin, Wei He, and Yangyun Dong
- Subjects
Drug ,Taste ,Chromatography ,Chemistry ,Batch method ,media_common.quotation_subject ,Pharmaceutical Science ,02 engineering and technology ,Amberlite ,021001 nanoscience & nanotechnology ,Bitter taste ,030226 pharmacology & pharmacy ,LACTOSE MONOHYDRATE ,respiratory tract diseases ,03 medical and health sciences ,0302 clinical medicine ,In vivo ,cardiovascular system ,Taste masking ,0210 nano-technology ,media_common - Abstract
The objective of this research is to study the taste masking efficiency of Amberlite IRP88 in sildenafil citrate chewable tablets. Amberlite IPR88 was complexed with sildenafil citrate using the batch method. Formulation with sildenafil citrate/Amberlite IPR88 in a ratio of 2:1 by weight showed higher Drug complexation efficiency and drug-loaded, and furthermore the results from SEM, DSC, XRD, and FT-IR of selected complex indicated that the salt bridge between sildenafil and citrate was replaced by salt bridge between NH groups of sildenafil and the sulfonate group of the resin. Different chewable tablets containing the complex were prepared with various ingredients as well. Then, dissolution tests, in vivo performance assessment as well as palatability evaluation of chewable tablets were performed. The dissolution behaviors, in vivo performances and taste profiles of the prepared chewable tablets with lactose monohydrate, CMC-Na were similar to those of Nipatra Chewable Tablets, which was one of selling sildenafil citrate chewable tablet. Overall, the pH-dependent process of ion exchange by weak cationic resins opens a promising approach to mask the bitter taste of cationic drug for oral fast disintegrating formulation such as sildenafil citrate.
- Published
- 2019
33. Liquid crystalline phase as a probe for crystal engineering of lactose: Carrier for pulmonary drug delivery.
- Author
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Patil, Sharvil S., Mahadik, Kakasaheb R., and Paradkar, Anant R.
- Subjects
- *
LIQUID crystal states , *CRYSTALS , *MOLECULAR probes , *CHEMICAL engineering , *LACTOSE , *DRUG delivery systems , *INHALATION administration - Abstract
The current work was undertaken to assess suitability of liquid crystalline phase for engineering of lactose crystals and their utility as a carrier in dry powder inhalation formulations. Saturated lactose solution was poured in molten glyceryl monooleate which subsequently transformed into gel. The gel microstructure was analyzed by PPL microscopy and SAXS. Lactose particles recovered from gels after 48 h were analyzed for polymorphism using techniques such as FTIR, XRD, DSC and TGA. Particle size, morphology and aerosolisation properties of prepared lactose were analyzed using Anderson cascade impactor. In situ seeding followed by growth of lactose crystals took place in gels with cubic microstructure as revealed by PPL microscopy and SAXS. Elongated (size ∼ 71 μm) lactose particles with smooth surface containing mixture of α and β-lactose was recovered from gel, however percentage of α-lactose was more as compared to β-lactose. The aerosolisation parameters such as RD, ED, %FPF and % recovery of lactose recovered from gel (LPL) were found to be comparable to Respitose® ML001. Thus LC phase (cubic) can be used for engineering of lactose crystals so as to obtain particles with smooth surface, high elongation ratio and further they can be used as carrier in DPI formulations. [ABSTRACT FROM AUTHOR]
- Published
- 2015
- Full Text
- View/download PDF
34. Influence of filler selection on twin screw foam granulation.
- Author
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Rocca, K. E., Weatherley, S., Sheskey, P. J., and Thompson, M. R.
- Subjects
FOAM ,EXCIPIENTS ,GRANULATION ,NUCLEATION ,ABSORPTION ,WETTING agents ,BINDING agents - Abstract
The influence of filler selection in wet granulation was studied for the novel case where the binder is delivered as an unstable, semi-rigid aqueous foam to an extrusion process. The work primarily examined the impact of differing concentrations of microcrystalline cellulose (Avicel PH® 101) in a formulation with spray-dried α-lactose monohydrate (Flowlac® 100) in regards to wetting and granule nucleation for this relatively new technique known as continuous foam granulation. Foam stability was varied within the work to change its drainage and coarsening behavior atop these powder excipients, by use of different foamable binding agents (METHOCEL™ F4 PLV and METHOCEL™ Premium VLV) as well as by adjusting the foam quality. A static bed penetration test was first used to study the foam behavior in wetting these powders without the processing constraints of an extruder which limit possible liquid-to-solids ratios as well as introduce shear which may complicate interpretation of the mechanism. The test found that the penetration time to saturate these powders decreased as their water absorption capacity increased which in turn decreased the size of the formed nuclei. Differences in the stability of the foamed binder had minimal influence on these attributes of wetting despite its high spread-to-soak behavior. The size of granules produced by extrusion similarly demonstrated sensitivity to the increasing water absorption capacity of the filler and little dependency on foam properties. The different liquid-to-solids ratios required to granulate these different formulations inside the extruder highlighted an evolving concept of powder lubricity for continuous foam granulation. [ABSTRACT FROM AUTHOR]
- Published
- 2015
- Full Text
- View/download PDF
35. Understanding the Effect of Energy Density and Formulation Factors on the Printability and Characteristics of SLS Irbesartan Tablets-Application of the Decision Tree Model
- Author
-
Đorđe Medarević, Stefan Pavlović, Marijana Madžarević, Jelena Đuriš, Branka Ivković, and Svetlana Ibrić
- Subjects
tailoring drug release ,Materials science ,printability ,Pharmaceutical Science ,02 engineering and technology ,030226 pharmacology & pharmacy ,laser speed ,Article ,law.invention ,03 medical and health sciences ,0302 clinical medicine ,Irbesartan ,Pharmacy and materia medica ,law ,decision tree ,medicine ,Composite material ,021001 nanoscience & nanotechnology ,LACTOSE MONOHYDRATE ,RS1-441 ,Selective laser sintering ,Energy density ,Drug release ,0210 nano-technology ,energy density ,Decision tree model ,medicine.drug - Abstract
Selective laser sintering (SLS) is a rapid prototyping technique for the production of three-dimensional objects through selectively sintering powder-based layer materials. The aim of the study was to investigate the effect of energy density (ED) and formulation factors on the printability and characteristics of SLS irbesartan tablets. The correlation between formulation factors, ED, and printability was obtained using a decision tree model with an accuracy of 80%. FT-IR results revealed that there was no interaction between irbesartan and the applied excipients. DSC results indicated that irbesartan was present in an amorphous form in printed tablets. ED had a significant influence on tablets’ physical, mechanical, and morphological characteristics. Adding lactose monohydrate enabled faster drug release while reducing the possibility for printing with different laser speeds. However, formulations with crospovidone were printable with a wider range of laser speeds. The adjustment of formulation and process parameters enabled the production of SLS tablets with hydroxypropyl methylcellulose with complete release in less than 30 min. The results suggest that a decision tree could be a useful tool for predicting the printability of pharmaceutical formulations. Tailoring the characteristics of SLS irbesartan tablets by ED is possible, however, it needs to be governed by the composition of the whole formulation.
- Published
- 2021
36. Understanding the Effect of Dispersion Corrections on the Calculated Spectra of $\alpha$-Lactose Monohydrate
- Author
-
Calum N. A. Towler, John Kendrick, and Andrew D. Burnett
- Subjects
Materials science ,Dispersion (optics) ,Crystallite ,LACTOSE MONOHYDRATE ,Molecular physics ,Spectral line - Abstract
THz spectra were recorded for a polycrystalline $\alpha$ -lactose monohydrate sample at 4 K. Solid-state DFT was then used to aid the interpretation of the spectrum. In particular, we investigate how the inclusion of a number of empirical dispersion corrections to the DFT calculations influences the correlation between calculation and experiment.
- Published
- 2020
37. Classification of polymorphic forms of fluconazole in pharmaceuticals by FT-IR and FT-NIR spectroscopy
- Author
-
Mourad Kharbach, Abdelaziz Bouklouze, Philippe Hubert, Mohammed Alaoui Mansouri, Roland Djang’eing’a Marini, Yahia Cherrah, Issam Barra, Pierre-Yves Sacre, and Eric Ziemons
- Subjects
Itraconazole ,Clinical Biochemistry ,Pharmaceutical Science ,Infrared spectroscopy ,Excipient ,01 natural sciences ,Analytical Chemistry ,Excipients ,Drug Discovery ,Spectroscopy, Fourier Transform Infrared ,medicine ,Fourier transform infrared spectroscopy ,Least-Squares Analysis ,Fluconazole ,Spectroscopy ,Chromatography ,Spectroscopy, Near-Infrared ,010405 organic chemistry ,Manufacturing process ,Chemistry ,010401 analytical chemistry ,LACTOSE MONOHYDRATE ,0104 chemical sciences ,Miconazole ,medicine.drug - Abstract
The main goal of this work was to test the ability of vibrational spectroscopy techniques to differentiate between different polymorphic forms of fluconazole in pharmaceutical products. These are mostly manufactured with fluconazole as polymorphic form II and form III. These crystalline forms may undergo polymorphic transition during the manufacturing process or storage conditions. Therefore, it is important to have a method to monitor these changes to ensure the stability and efficacy of the drug. Each of FT-IR or FT-NIR spectra were associated to partial least squares-discriminant analysis (PLS-DA) for building classification models to distinguish between form II, form III and monohydrate form. The results has shown that combining either FT-IR or FT-NIR to PLS-DA has a high efficiency to classify various fluconazole polymorphs, with a high sensitivity and specificity. Finally, the selectivity of the PLS-DA models was tested by analyzing separately each of three following samples by FT-IR and FT-NIR: lactose monohydrate, which is an excipient mostly used for manufacturing fluconazole pharmaceutical products, itraconazole and miconazole. These two last compounds mimic potential contaminants and belong to the same class as fluconazole. Based on the plots of Hotelling’s T² vs Q residuals, pure compounds of miconazole and itraconazole, that were analyzed separately, were significantly considered outliers and rejected. Furthermore, binary mixtures consist of fluconazole form-II and monohydrate form with different ratios were used to test the suitability of each technique FT-IR and FT-NIR with PLS-DA to detect minimum contaminant or polymorphic conversion from a polymorphic form to another using also the plots of Hotelling’s T² vs Q residuals.
- Published
- 2020
38. Lactose monohydrate (C12H22O11 · H2O) mediated synthesis and spectral analysis of nanocrystalline Ni0.5Cu0.5Fe2O4
- Author
-
Vibhu T. Sivanandan and Arun S. Prasad
- Subjects
010302 applied physics ,Materials science ,Metals and Alloys ,02 engineering and technology ,021001 nanoscience & nanotechnology ,Condensed Matter Physics ,01 natural sciences ,LACTOSE MONOHYDRATE ,Nanocrystalline material ,Spinel ferrite ,0103 physical sciences ,Materials Chemistry ,Chemical preparation ,Spectral analysis ,Physical and Theoretical Chemistry ,0210 nano-technology ,Nuclear chemistry - Abstract
Ni0.5Cu0.5Fe2O4 nanocrystalline spinel ferrite was synthesized through a lactose monohydrate (C12H22O11 · H2O) mediated chemical preparation technique (post annealed at 600 °C for 4 h). Va...
- Published
- 2020
39. Lactose: Use, measurement, and expression of results
- Author
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Matilde Portnoy and David M. Barbano
- Subjects
Farms ,Ultrafiltration ,Lactose ,Enzymatic Assays ,03 medical and health sciences ,chemistry.chemical_compound ,Genetics ,Animals ,Food science ,Manufacturing efficiency ,Dairy cattle ,030304 developmental biology ,Mathematics ,0303 health sciences ,0402 animal and dairy science ,food and beverages ,04 agricultural and veterinary sciences ,Milk production ,040201 dairy & animal science ,LACTOSE MONOHYDRATE ,Lactose measurement ,Dairying ,Milk ,chemistry ,Animal Science and Zoology ,Cattle ,Female ,Food Science - Abstract
Lactose has different uses in the dairy, food, and pharmaceutical industries. Being aware of the different forms of lactose and their concentrations can be very helpful in managing dairy product quality, properties, and manufacturing efficiency. Correct measurement and reporting of lactose concentration in milk and other dairy products will be of increased importance in the future as more value-added uses of lactose are developed and as milk lactose data are used in farm management decision making. Lactose should be reported as anhydrous lactose because lactose data will be used to make increasingly important decisions in dairy processing, dairy product labeling, and milk production in the future. Lactose also plays an important role in milk synthesis within a cow. Milk production factors and dairy cattle breed selection influence the amount of high value fat and protein produced per unit of lactose. If the off-farm value of lactose remains low, more attention may be focused on using ultrafiltration to process milk and leave 50 to 60% of the lactose and water from milk at the farm to recover the energy value of the lactose as feed and reduce the hauling cost of the high value components of milk to a dairy product manufacturing factory. Many methods exist to determine lactose concentration, but the most important methods are enzymatic assays, HPLC, and mid-infrared analysis. New, value-added uses for lactose need to be developed. Consistent and accurate methods of lactose measurement and consistent expression of lactose results will support this development process. Starting in January 2017, the USDA Federal Milk Market Laboratories began reporting lactose content of milk as anhydrous lactose and discontinued the reporting of lactose by difference.
- Published
- 2020
40. Evaluation of excipients effects on the impurity profile of lyophilized hydroxocobalamin formulation
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Sercan Semiz, Suleyman Ozakin, Muge Guleli, Ibrahim Karabacak, Sevki Kizilok, Mahmut Ozbek, and Gökay Gün
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Chromatography ,Chemistry ,Farmakoloji ve Eczacılık ,Pharmaceutical Science ,Excipient ,Pharmacy ,Raw material ,Pharmaceutical formulation ,Hydroxocobalamin ,LACTOSE MONOHYDRATE ,Drug formulation,excipient,lyophilization,hydroxocobalamin,stability ,Impurity ,Health Care Sciences and Services ,medicine ,Mannitol ,Sağlık Bilimleri ve Hizmetleri ,Pharmacology and Pharmacy ,Parenteral solutions ,medicine.drug - Abstract
Background and Aims: The aim of the research work was to compare excipient effects and develop a stable pharmaceutical product in the form of lyophilized powder. Mannitol, lactose monohydrate, EDTA and glycine are widely used in pharmaceutical formulations and food products. Methods: The production method consists of mainly four parts: raw material weighing process, preparation of bulk solutions, lyophilization and analytical determination. A total of five formulations were prepared and lyophilized to the stability study. To improve the stability of hydroxocobalamin formulations (F1-F5), they were evaluated with different excipients (mannitol, lactose monohydrate, EDTA and glycine) during the stability period. Stability studies were performed to check impurity and assay of hydroxocobalamin. Results: The rate of impurity and assay results were compared to F1-F5 formulations. As a result of impurity and assay analysis for F3 and F4, the formulations were found to be within limit. Both of them were determined to the best formulations for impurity of hydroxocobalamin. Conclusion: The research proposes a new stable formulation and proper storage conditions for lyophilized hydroxocobalamin parenteral solutions. The impurity problem of lyophilized hydroxocobalamin formulation was optimized with lactose monohydrate and lactose monohydrate + EDTA combination.
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- 2020
41. Modified release of furosemide from Eudragits® and poly(ethylene oxide)-based matrices and dry-coated tablets
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Marilena Vlachou, Angeliki Siamidi, and Efthymia Geraniou
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matrix tablets ,compression coated tablets ,furosemide ,Eudragit® ,poly(ethylene oxide) ,polyvinylpyrrolidone ,Chemistry, Pharmaceutical ,Drug Compounding ,Oxide ,Pharmaceutical Science ,Lactose ,02 engineering and technology ,macromolecular substances ,eudragit® ,030226 pharmacology & pharmacy ,Polyethylene Glycols ,Excipients ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Polymethacrylic Acids ,Furosemide ,medicine ,Diuretics ,Dissolution ,Pharmaceutical industry ,Poly ethylene ,Pharmacology ,Polyvinylpyrrolidone ,Ethylene oxide ,technology, industry, and agriculture ,Povidone ,General Medicine ,Hydrogen-Ion Concentration ,021001 nanoscience & nanotechnology ,Coated tablets ,LACTOSE MONOHYDRATE ,Molecular Weight ,Drug Liberation ,chemistry ,Delayed-Action Preparations ,HD9665-9675 ,0210 nano-technology ,medicine.drug ,Nuclear chemistry ,Tablets - Abstract
Modified release of furosemide from tablet formulations is preferred by patients, because of physiological problems, acute diuresis being the most serious, compared to the forms designed for immediate release. With this in view, we aimed at achieving furosemide’s longer gastric retention and waste minimization by preparing matrix and compression coated tablets incorporating different grades of Eudragit® and poly(ethylene oxide) (PEO), polyvinylpyrrolidone (PVP) and lactose monohydrate. Dissolution profiles of the new formulations were compared with that of the main stream drug Lasix®, 40 mg tablets. The results indicate that the use of Eudragit® in conjunction with either PVP or lactose monohydrate led to a slower release rate in the intestinal fluids compared to Lasix®. Moreover, furosemide release in the intestinal pH from matrix tablets and compression coated tablets was not noticeably different. Formulations incorporating PEO led to sustained release, in intestinal fluids, which depended on the molecular weight of PEO.
- Published
- 2020
42. Development of an in-line Raman spectroscopic method for continuous API quantification during twin-screw wet granulation
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Julia Harting and Peter Kleinebudde
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Diclofenac ,Materials science ,Chromatography ,Chemistry, Pharmaceutical ,Process analytical technology ,Pharmaceutical Science ,Ibuprofen ,02 engineering and technology ,General Medicine ,Spectrum Analysis, Raman ,bacterial infections and mycoses ,equipment and supplies ,021001 nanoscience & nanotechnology ,030226 pharmacology & pharmacy ,LACTOSE MONOHYDRATE ,Screw speed ,03 medical and health sciences ,symbols.namesake ,Granulation ,0302 clinical medicine ,symbols ,0210 nano-technology ,Raman spectroscopy ,Spectroscopy ,Biotechnology - Abstract
Raman spectroscopy was evaluated as a process analytical technology (PAT) tool for continuous API quantification during twin-screw wet granulation. Therefore, a Raman probe was implemented in front of the granulator barrel. This setup enabled the collection of Raman spectra upon a constant granule flow. To develop an in-line PLS calibration model, eight binary mixtures of the API and lactose monohydrate with API contents between 5 and 50% were pre-blended and granulated in a twin-screw granulator with a screw speed of 150 rpm and a powder feed rate of 40 g/min. Water was used as a granulation liquid with different liquid to solid ratios depending on the API content. Ibuprofen and diclofenac sodium were chosen as model drugs and separated PLS models were built for each API. The predictive performance of the developed PLS models was determined by granulating and monitoring new test samples containing different API concentrations. This evaluation showed that the models were able to predict the API concentration with an RMSEP of 0.59% for ibuprofen and 1.5% for diclofenac sodium. In a second part, the developed in-line Raman spectroscopic method was used to determine the API concentration during a split feeding process. Therefore, the API and lactose monohydrate were added by two independently adjustable feeders into the twin-screw granulator barrel. The in-line spectroscopy analysis which was verified by UV-analysis indicated that the mixing ability of the twin-screw granulator was good for the used settings and all adjusted API concentrations.
- Published
- 2018
43. Milling induced amorphisation and recrystallization of α-lactose monohydrate
- Author
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Samaneh Pazesh, Michael Schuleit, Anna Millqvist-Fureby, Göran Alderborn, Niklas Nordgren, Maria Badal Tejedor, and Mark W. Rutland
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Recrystallization (geology) ,Materials science ,Surface Properties ,Pharmaceutical Science ,Lactose ,02 engineering and technology ,030226 pharmacology & pharmacy ,law.invention ,03 medical and health sciences ,chemistry.chemical_compound ,Tableting ,0302 clinical medicine ,Differential scanning calorimetry ,law ,Particle Size ,Crystallization ,Calorimetry, Differential Scanning ,Water ,021001 nanoscience & nanotechnology ,LACTOSE MONOHYDRATE ,Chemical engineering ,chemistry ,Particle size ,Powders ,0210 nano-technology ,Material properties - Abstract
Preprocessing of pharmaceutical powders is a common procedure to condition the materials for a better manufacturing performance. However, such operations may induce undesired material properties modifications when conditioning particle size through milling, for example. Modification of both surface and bulk material structure will change the material properties, thus affecting the processability of the powder. Hence it is essential to control the material transformations that occur during milling. Topographical and mechanical changes in surface properties can be a preliminary indication of further material transformations. Therefore a surface evaluation of the α-lactose monohydrate after short and prolonged milling times has been performed. Unprocessed α-lactose monohydrate and spray dried lactose were evaluated in parallel to the milled samples as reference examples of the crystalline and amorphous lactose structure. Morphological differences between unprocessed α-lactose, 1 h and 20 h milled lactose and spray dried lactose were detected from SEM and AFM images. Additionally, AFM was used to simultaneously characterize particle surface amorphicity by measuring energy dissipation. Extensive surface amorphicity was detected after 1 h of milling while prolonged milling times showed only a moderate particle surface amorphisation. Bulk material characterization performed with DSC indicated a partial amorphicity for the 1 h milled lactose and a fully amorphous thermal profile for the 20 h milled lactose. The temperature profiles however, were shifted somewhat in the comparison to the amorphous reference, particularly after extended milling, suggesting a different amorphous state compared to the spray-dried material. Water loss during milling was measured with TGA, showing lower water content for the lactose amorphized through milling compared to spray dried amorphous lactose. The combined results suggest a surface-bulk propagation of the amorphicity during milling in combination with a different amorphous structural conformation to that of the amorphous spray dried lactose. The hardened surface may be due to either surface crystallization of lactose or to formation of a low-water glass transition.
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- 2018
44. Physicochemical and Technological Characteristics of Lycopus Europaeus L. Dry Herbal Extract and Related Compositions
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M. A. Dzhavakhyan, A. S. Khomik, O. A. Semkina, and V. I. Zvereva
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Pharmacology ,chemistry.chemical_compound ,Chromatography ,biology ,Chemistry ,Drug Discovery ,Pharmacology toxicology ,Magnesium stearate ,biology.organism_classification ,LACTOSE MONOHYDRATE ,Lycopus europaeus - Abstract
The physicochemical and technological properties of Lycopus europaeus dry herbal extract were studied. Excipients were also selected. The technological characteristics of experimental samples containing L. europaeus dry herbal extract were studied. Stepwise mixing of drugs and excipients was proposed to prepare capsules. The results showed that a formulation in which lactose monohydrate, AEROSIL® A380, and vegetable magnesium stearate were used as excipients had the optimal technological characteristics.
- Published
- 2019
45. Evaluation of Functional Characteristics of Lactose by Inverse Gas Chromatography.
- Author
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Patera, J., Zamostny, P., Litva, D., Berova, Z., and Belohlav, Z.
- Abstract
Abstract: The work was focused on the analysis of different batches of the common pharmaceutical excipient lactose using inverse gas chromatography (IGC). Several batches of amorphous (spray dried) and crystalline form of lactose were studied. Surface properties represented by the surface energy and specific (acid-base) interactions between probes and analyzed samples shows batch variations and significant differences between manufacturers and technological processes. The second part of this work was focused on effect of relative humidity and temperature on stability of lactose. The variations of surface energy and specific interactions over time were studied. The changes in surface properties of two batches of lactose-amorphous and crystalline caused by higher relative humidity were measured by IGC. From measured values are obvious different chemical and physical properties of both lactose forms. Negative effect of higher temperature and air humidity lead to changes in surface energy and mainly rapid changes of electron–acceptor and electron-donor surface sites. Lactose monohydrate shows dramatic decrease in the surface energy and in the strength of electron-accepting sites on the contrary of spray dried where the acidity of surface increased. [Copyright &y& Elsevier]
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- 2012
- Full Text
- View/download PDF
46. Moisture Monitoring in Fluid-Bed Granulation by Multi-Resonance Microwave Sensor: Applicability on Crystal-Water Containing Donepezil Granules
- Author
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Peters, Johanna, Taute, Wolfgang, Döscher, Claas, Höft, Michael, Knöchel, Reinhard, and Breitkreutz, Jörg
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- 2019
- Full Text
- View/download PDF
47. The impact of material attributes and process parameters on the micronisation of lactose monohydrate
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Shariare, M.H., de Matas, M., York, P., and Shao, Q.
- Subjects
- *
LACTOSE , *PHARMACEUTICAL powders , *PARTICLE size distribution , *DRUG delivery devices , *ORAL drug administration , *EXPERIMENTAL design , *INVERSE gas chromatography - Abstract
Abstract: Dry powder inhalers (DPIs), which are important medicines for drug delivery to the lungs, require drug particles in the respirable size range of 1–6μm for optimal lung deposition. Drugs administered by the oral route also derive benefit from particles in this size range owing to their large surface area to volume ratio, which provides potential for rapid dissolution. Micronisation used in the production of particles, however often leads to heterogeneous product containing mechanically activated surfaces with amorphous content. This study was therefore carried out to evaluate the effect of particle properties of three grades of lactose monohydrate, with sizes above and below the brittle–ductile transition (dcrit) and their interaction with process variables on the quality of micronised material. Following an experimental design, the impact of three factors (grinding pressure, injector pressure and feed rate) on the particulate attributes of micronised powders produced from the different size grades was assessed. Processing conditions were shown to be important determinants of powder properties only for the coarsest starting material. Ultrafine material was achieved by processing finer grade feed stock below dcrit. However the resultant product was more crystalline and transformed on heating to the anhydrous state with markedly reduced onset temperature with lower energy surfaces than powders produced from larger sized starting material. Thus the propensity for micronisation of lactose monohydrate can be altered through control of starting materials and optimal settings for process variables. [Copyright &y& Elsevier]
- Published
- 2011
- Full Text
- View/download PDF
48. Improving powder flow properties of a cohesive lactose monohydrate powder by intensive mechanical dry coating.
- Author
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Qi Zhou, Armstrong, Brian, Larson, Ian, Stewart, Peter J., and Morton, David A. V.
- Subjects
- *
LACTOSE products , *PHARMACEUTICAL powders , *STEARATES , *SILICA - Abstract
The objective of this study was to improve the cohesive lactose powder flowability. A cohesive lactose monohydrate powder was processed in either a tumbling blender or an intensive mechanical processor with either magnesium stearate or fumed silica. No substantial changes in particle size were detected by laser diffraction following either treatment. The untreated lactose sample exhibited very poor powder flow. Only limited improvements in powder flowability were indicated after the tumbling blending, intensive mechanical processing with the fumed silica or without additives. However, the intensive mechanical processing of the lactose sample with magnesium stearate demonstrated exceptionally large increases in both poured and tapped density as well as notable improvements in all powder flowability indicators examined. Our findings support the use of intensive mechanical processing technique as an effective method to coat cohesive pharmaceutical powders with selected additives, modify the surface nature of the particles, reduce the interparticle cohesive forces and hence improve powder flowability. The subtle differences in powder flow behaviour of lactose samples between the untreated and tumbling blended powders with magnesium stearate were only detected by the powder rheometer using its dynamic mode, indicating its potential advantages over traditional powder flow characterisation approaches. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:969–981, 2010 [ABSTRACT FROM AUTHOR]
- Published
- 2010
- Full Text
- View/download PDF
49. Study of the effect of lactose on the structure of sodium alginate films
- Author
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Bajdik, János, Makai, Zsolt, Berkesi, Ottó, Süvegh, Károly, Marek, Tamás, Erős, István, and Pintye-Hódi, Klára
- Subjects
- *
LACTOSE , *ALGINATES , *SODIUM alginate , *THIN films , *CHEMICAL structure , *FOURIER transform infrared spectroscopy , *HYDRATES - Abstract
Abstract: The aim of this study was to evaluate the interaction between the film-forming sodium alginate and lactose monohydrate. This combination is used in the co-spray-drying technique for microencapsulation, but no respect on the structure of the film formed has not been published previously. From mechanical tests, positronium lifetime measurements and FT-IR studies on free films containing different ratios of film-former and lactose, we concluded that the mechanical strength of the sodium alginate film decreased with the increasing proportion of lactose. The free volume in the polymer matrix decreased to a minimum as the lactose content was progressively increased to 40%, but subsequently increased at higher lactose contents. The explanation of this phenomenon is the filling of the holes with the sugar. As lactose became predominant component, the structure of the polymer network weakened. These conclusions were supported by the FT-IR findings. The present results permit a clear explanation of the previously reported favourable effects of this film-forming combination on the dissolution of the active agent from the microcapsules. [Copyright &y& Elsevier]
- Published
- 2009
- Full Text
- View/download PDF
50. Effective Modification of Particle Surface Properties Using Ultrasonic Water Mist.
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Genina, Natalja, Räikkönen, Heikki, Heinämäki, Jyrki, Antikainen, Osmo, Siiriä, Simo, Veski, Peep, and Yliruusi, Jouko
- Abstract
The goal of the present study was to design a new technique to modify particle surface properties and, through that, to improve flowability of poorly flowing drug thiamine hydrochloride and pharmaceutical sugar lactose monohydrate of two different grades. The powdered particles were supplied by a vibratory feeder and exposed to an instantaneous effect of water mist generated from an ultrasound nebulizer. The processed and original powders were evaluated with respect to morphology (scanning electron microscopy, atomic force microscopy, and spatial filtering technique), flow, and solid state properties. It was found that rapid exposition of pharmaceutical materials by water mist resulted in the improvement of powder technical properties. The evident changes in flowability of coarser lactose were obviously due to smoothing of particle surface and decreasing in the level of fines with very slight increment in particle size. The changes in thiamine powder flow were mainly due to narrowing in particle size distribution where the tendency for better flow of finer lactose was related to surface and size modifications. The aqueous mist application did not cause any alteration of the crystal structures of the studied materials. The proposed water mist treatment technique appears to be a robust, rapid, and promising tool for the improvement of the technological properties of pharmaceutical powders. [ABSTRACT FROM AUTHOR]
- Published
- 2009
- Full Text
- View/download PDF
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