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Summary Objectives The chief objective of the present research was to reduce local side effects by reducing the dose, controlling the release, and improving the stability by developing and optimizing tretinoin (TRT)-loaded topical emulgel formulation. Methods TRT emulgel (TE) was prepared and optimized at varying ratios of excipients and using 32 optimal response surface design (ORSD). The TRT emulgel was optimized based on TRT content and in vitro release profile of TRT from formulated emulgel batches. The optimized TRT was characterized for physical properties, pH, viscosity, spreadability, extrudability, photomicroscopy, in vitro anti-acne, in vivo skin irritation, in vivo anti-inflammatory activity, and stability study. Results The FTIR and DSC analysis revealed the compatibility between TRT and formulation excipients of emulgel. The batch F5 of emulgel formulation displayed maximum drug content (98.69 ± 1.26%), and controlled TRT release (78.27 ± 0.69%). Thus, batch F5 was selected as an optimized batch for further characterization. The photomicroscopic analysis of optimized TE exhibited the presence of spherical globules. The pH and viscosity of optimized TE were found to be 6.20 ± 0.12 and 3240cP respectively. Besides, the optimized TE showed good spreadability and extrudability. The in vitro anti-acne activity against Propionibacterium acne (P. acne) of optimized TE (diameter of zone of inhibition 34.54 ± 0.26 mm) was found to be the comparatively same as that of marketed Sotret® gel (diameter of zone of inhibition 36.13 ± 0.43 mm). Moreover, no sign of irritation was observed in rats treated with optimized TE indicating the safety of TE. Furthermore, the optimized TE displayed significant (p Conclusion Thus, the emulgel could be a promising approach for the topical delivery of TRT with improved performance and reduced side effects.

Polymeric materials from plants continue to be of interest to pharmaceutical scientists as potential binders in immediate release tablets due to availability, sustainability, and constant supply to feed local pharmaceutical industries. Paracetamol tablet formulations were utilized in investigating the potential binding characteristics of pectin harnessed from various okra genotypes (PC1-PC5) in Ghana. The pectin yields from the different genotypes ranged from 6.12 to 18.84%w/w. The pH of extracted pectin ranged from 6.39 to 6.92, and it had good swelling indices and a low moisture content. Pectin extracted from all genotypes were evaluated as binders (10, 15, and 20%w/v) and compared to tragacanth BP. All formulated tablets (F1-F18) passed the weight uniformity, drug content, hardness, and friability tests. Based on their crushing strength, tablets prepared with pectin from the various genotypes were relatively harder ( P ≤ 0.05 ) than tablets prepared with tragacanth BP. Tablets prepared with pectins as binders at 10%w/v and 15%w/v passed the disintegration and dissolution tests with the exception of PC4 at 15%w/v. Incorporation of pectin from all genotypes (excluding PC5) as a binder at concentrations above 15%w/v (F13, F16, F14, and F15) produced tablets which failed the disintegration test and showed poor dissolution profiles. Thus, pectin from these genotypes can be industrially commodified as binders in immediate release tablets using varying concentrations.

The present work is to formulation and evaluation of Ofloxacin of microencapsulated suspension by using solvent evaporation method. The Preparation contains six formulations of suspensions with 2 different polymers with different concentrations as Ofloxacin resinate + HPMC, Ofloxacin resinate + Carbopol 934. The prepared batches of Ofloxacin microencapsulated suspension were evaluated for the pH, viscosity, sedimentation volume; density, drug content and antibacterial activity of all the six formulations were performed. Formulations F-3, F-6 gave better sustained release and antibacterial activity. Comparative study of F-3, F-6 with marketed product reveal the F-3 is best fitted formulation for preparation of microencapsulated suspension.

The increasing number of multisource pharmaceuticals has necessitated the need for continuous quality assessment of products available for atients’ consumption. Promethazine is an anti-histamine used in cases of nausea, vomiting, motion sickness etc. The study was to examine the in vitro quality parameters for ten brands of promethazine hydrochloride tablets sold in retail pharmacies in Edo State, Nigeria. The parameters determined were identification, weight variation, friability, hardness, disintegration, dissolution rate and assay. All samples were evaluated for conformity with British Pharmacopoeia (BP) 2017 standards. Results obtained showed tablet weight ranging from 0.08 g ± 1.77 % to 0.255 g ± 3.557 %, hardness from 4.36 ± 0.58 to 8.33 ± 3.21 kg/cm2, friability of < 1 %, disintegration time of 2.47 ± 0.90 to 69.66 ± 7.23 min and assay of 61.32 ± 2.04 to 183.19 ± 0.11%. The ten batches but one released more than 80 % of their drug content within 30 min. Analysis of similarity factor revealed other samples but PR-7 can be interchangeable with PR-1 based on dissolution profile. The results showed that not all samples examined passed all the pharmacopoeia tests for satisfactory quality. Thus, they all cannot be used interchangeably in clinical practice. Keywords: Promethazine; Quality Control; Dissolution; Pharmacopoeial specifications

Aims: This study investigated whether locally marketed rosuvastatin calcium tablets in Bangladesh have comparable physical and chemical attributes, including in vitro bioequivalence profiles, to the proprietary brand. Methodology: Nine generic products (G1-G9) containing 10 mg of rosuvastatin calcium were compared to the proprietary brand Crestor® (R1) and an FDA approved generic rosuvastatin calcium tablet (R2). Weight variation, diameter, thickness, friability, drug content, disintegration time and dissolution profiles were tested according to United States Pharmacopeia (USP) guidelines. In vitro bioequivalence requirements were assessed by calculating difference (f1) and similarity (f2) factors. Results: The generic products complied with the pharmacopeial requirements for weight variation, disintegration time and friability. All the tablets had drug ranging between 92%-105% and released more than 80% of rosuvastatin within first 15-30 minutes. However, for brands G5, G7 and G8 the f1 values were 15.7%, 15.82% and 25.21% respectively and their f2 values were 41.8, 41.6 and 32.6 respectively whereas for G9 the f2 value was 43.4. These brands have thus failed to meet in vitro bioequivalence requirements. Conclusion: We conclude that few substandard generics of rosuvastatin calcium has somehow found its way to the market and further studies are required to ascertain their noncompliance.

The poor solubility and low stability of rifampicin limited its therapeutic efficacy. One of the common strategies is to form an inclusion complex to address the problems. In this study, acyclic cucurbit[n]uril was used for encapsulation of rifampicin to form an inclusion complex. The inclusion complex was prepared by the kneading method and characterized by DSC, SEM, FT-IR, NMR, PXRD, and UV-Vis spectroscopy. The results confirmed the formation of 1:1 inclusion complex. The drug content was calculated to be 27.35 ± 0.54%. The aqueous solubility of rifampicin was increased 20-fold by complexation with acyclic cucurbit[n]uril. Moreover, the thermo-stability and photo-stability of free rifampicin and inclusion complex were investigated by HPLC. Rifampicin was stabilized by encapsulating the piperazine ring in the cavity of acyclic cucurbit[n]uril. In addition, the MIC of free RIF and RIF‧ACB were determined by using in vitro experiments. It was found that rifampicin complexed by acyclic cucurbit[n]uril exhibited similar antibacterial activities against strain H37Rv to rifampicin alone.

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.

The present research was aimed to formulate and evaluate Lansoprazole delayed release multiple unit pellets in capsules. Lansoprazole degrades in the acidic environment of the stomach. It is also unstable under conditions of high temperature and high humidity which leads to therapeutic inefficiency. Hence it is important to bypass the acidic pH of the stomach. Protection of drug from acidic environment is done by coating the drug with enteric polymer. In the present study, successive layers of drug layer, barrier layer and enteric layer was coated on the inert sugar spheres by using solution/suspension layering technique in Fluidized bed processor (FBP). The prepared drug layered and barrier layered pellets were evaluated for % yield. The prepared lubricated pellets were evaluated for flow properties i.e., bulk density, tapped density, compressibility index and hausner’s ratio. Lubricated pellets filled into size ‘1’ capsules and evaluated for drug content, drug content resisted in acid, invitro drug release studies and compared with the marketed product. The dissimilarity and similarity factors for the optimized and marketed formulations were found to be 84.29. Accelerated Stability Testing (AST) was performed as per the ICH guidelines at 40±5°C/75±5% RH for 6 months and found satisfactory.

The present work aimed to produce Curcumin based nanoliposomes that nanoliposome can target the site via the brain in a controlled manner. Nanoliposomes are important in controlling the carriage; Curcumin which is an active constituent of curcuminoids thus also provides an effective treatment for the central nervous system and plays a crucial role. The interaction of the drug was ruled out by FT-IR studies and no incompatibility and lipids and surfactant. To optimize the formulation, factors affecting the physical appearance of Nanoliposomes were investigated. Curcumin-loaded Nanoliposomes were formulated using cholesterol by physical dispersion method and characterized for particle size, drug content, stability, production yield. Prepared nanoliposomes gave the better physical, morphological concerning the concentration of the lipids, surfactant, and ratio of lipid and surfactant. Six different formulations of Nanoliposomes F1-F6 were formulated to obtain the optimized formulation. The TEM (Transmission Electron Microscopy) of Nanoliposomes showed that they were rounded in shape and porous in texture. In-vitro drug release of formulation indicates that formulation F6 was selected as an optimized formulation for incorporation into the nanoliposomes among all the six formulations and liposome showed drug release in a controlled manner at the end of 10 hours. Keywords: Curcumin, Nanoliposomes, Physical Dispersion Method, Brain Targeting, Blood-Brain Barrier, Cholesterol, Bioavailability, In vitro Release.

Background: The concept of formulating ODT containing montelukast sodium offers an appropriate, practical approach to accomplish fast release of the drug. Absorption of these tablets takes place directly into the systemic circulation which bipass the hepatic first-pass metabolism of montelukast sodium which ultimately results in the improvement in the bioavailability. Method: In the present study ODT tablets of montelukast sodium were prepared by using different Superdisintegrants like natural and synthetic (tulasi, hibiscus, orange peel powder, Ispaghula, banana peel powder, Crospovidone). Thirteen formulations were designed, using a two level of Superdisintegrants (minimum and maximum concentration) and employing two Superdisintegrants at a time by using the co-processed technique. Results: No significant drug and excipients interaction was observed. The prepared tablets were evaluated by weight variation, thickness, hardness, friability, drug content uniformity, disintegration time, wetting time, in-vitro dissolution studies. A formulation containing 6mg of natural and synthetic Superdisintegrants was offered the relatively rapid release of montelukast sodium when compared with other concentrations employed in this investigation. Conclusion: Montelukast sodium formulation were prepared by Crospovidone and ispaghula combination of Superdisintegrants were releases 98.91% drug in 30 min.

Nanotechnology has been actively integrated as drug carriers over the last few years to treat various cancers. The main hurdle in the clinical management of cancer is the development of multidrug resistance against chemotherapeutic agents. To overcome the limitations of chemotherapy, the researchers have been developing technological advances for significant progress in the oncotherapy by enabling the delivery of chemotherapeutic agents at increased drug content levels to the targeted spots. Several nano-drug delivery systems designed for tumor-targeting are evaluated in preclinical and clinical trials and showed promising outcomes in cancerous tumors’ clinical management. This review describes nanocarrier’s importance in managing different types of cancers and emphasizing nanocarriers for drug delivery and cancer nanotherapeutics. It also highlights the recent advances in nanocarriers-based delivery systems, including polymeric nanocarriers, micelles, nanotubes, dendrimers, magnetic nanoparticles, solid lipid nanoparticles, and quantum dots (QDs). The nanocarrier-based composites are discussed in terms of their structure, characteristics, and therapeutic applications in oncology. To conclude, the challenges and future exploration opportunities of nanocarriers in chemotherapeutics are also presented.

O controle da qualidade de sólidos por meio de ensaios físico-químicos apresenta grande importância na garantia da qualidade de medicamentos. Diante disto, este estudo teve como objetivo comparar a qualidade de comprimidos de nimesulida com β-ciclodextrina (Maxsulid®) e sem β-ciclodextrina (Nisulid®) como forma de investigar se os testes vigentes se aplicam às formas farmacêuticas que contenham complexos de inclusão com ciclodextrinas em sua composição. Para tal, foram realizados ensaios físico-químicos descritos na Farmacopeia Brasileira 6ª edição para comprimidos de nimesulida. Frente ao exposto, ambos os medicamentos obtiveram resultados satisfatórios na maioria dos testes de caracterização físico-química. Os testes de doseamento e dissolução foram realizados por meio de determinações quantitativas utilizando a Cromatografia Líquida de Alta Eficiência. Os resultados do doseamento mostraram que a metodologia aplicada não está adequada para extrair o fármaco do complexo de inclusão e assim doseá-lo de maneira eficiente. No teste de dissolução, os dois medicamentos foram aprovados de acordo com os critérios estabelecidos na Farmacopeia Brasileira. Porém, Maxsulid® foi o único a obter sua totalidade dissolvida em 120 minutos. Dessa forma, fica clara a importância da implementação de protocolos analíticos adequados às novas tecnologias aplicadas na produção de medicamentos.

Dextromethorphan (DXM) is exceptionally bitter, yet the most widely used antitussive agents worldwide. It belongs to BCS class-II of pharmaceutical agents because of its poor water solubility; this is why it is only available in its hydrobromide salt form either in liquid or in solid formulations in the market. This water-soluble salt of the drug releases its content to a greater extent in salivary pH, which increases bitterness perception. This study aimed at designing a more palatable chocolate formulation of DXM, which releases the minimum drug in salivary pH. DXM nano-emulsion prepared using lecithin and Tween-80 was dried and incorporated in placebo chocolates, poured into silicon molds, and refrigerated to have medicated chocolates. Medicated chocolates had an average weight of 1.757 ± 0.006 g, a thickness of 7.606 ± 0.0175 mm, and hardness of 2.007 ± 0.0102 Kp. The average drug content was 98.707 ± 0.012%. The average particle size of optimized nano-emulsion was 101.145 ± 2.906 nm with an encapsulation efficiency of 75.866 ± 0.543%. Scanning electron microscopy (SEM) revealed the spherical structure of nanoparticles. Fourier transform infrared (FTIR) spectra and differential scanning calorimetry (DSC) thermograms showed no drug-excipient interaction, and X-ray diffraction (XRD) analysis confirmed the amorphous form of the drug in nano-emulsion. The minimal drug was released at salivary pH from chocolate formulation compared to the standard. The Human Panel taste evaluation confirmed better palatability of chocolate than marketed syrup and tablet formulations of DXM. The novel medicated chocolate of DXM was proven to have a better palatability profile than its marketed formulations.

Thiols play critical roles in regulating biological functions and have wide applications in pharmaceutical and biomedical industries. However, we still lack a general approach for the simultaneous detection of various thiols, especially in complex systems. Herein, we establish a 19F NMR platform where thiols are selectively fused into a novelly designed fluorinated receptor that has two sets of environmentally different 19F atoms with fast kinetics (k2 = 0.73 mM−1 min−1), allowing us to generate unique two-dimensional codes for about 20 thiols. We demonstrate the feasibility of the approach by reliably quantifying thiol drug content in tablets, discriminating thiols in living cells, and for the first time monitoring the thiol related metabolism pathway at the atomic level. Moreover, the method can be easily extended to detect the activity of thiol related enzymes such as γ-glutamyl transpeptidase. We envision that the versatile platform will be a useful tool for detecting thiols and elucidating thiol-related processes in complex systems., A 19F NMR platform, capable of discriminating various small molecule thiols, was designed for in-cell thiol differentiation and monitoring, and further detection of the γ-GT activity, demonstrating the wide applications in thiol-related processes.

Summary Background & aims Wernicke's encephalopathy is associated mainly with malnourishment in alcohol-dependent patients but can be caused also by cancer, Crohn's disease, gastrointestinal surgery or prolonged parenteral nutrition (PN) without adequate supplementation of vitamins. The disorder, with a significant mortality rate of up to 20%, is often associated with the underlying disease and intensifies after administration of non-supplemented PN. Thus, it seems justified to add thiamine to PN admixtures prepared for parenterally fed patients. Due to the lack of data on the stability of thiamine in PN admixtures at concentrations exceeding 60 mg/L, we decided to determine the possibility of adding a high dose of thiamine (800 mg per bag, 320 mg/L) to PN admixtures in order to treat Wernicke's encephalopathy in malnourished patients. Methods The study aimed to assess the stability of the physical properties of PN admixtures (pH, zeta potential, particle size) and to determine thiamine content using an HPLC method. Results Thiamine was found to degrade regardless of the PN admixture composition and storage conditions. The highest decrease in thiamine content was observed at room temperature without light protection whereas the lowest at a temperature of 4 ± 1 °C with light protection. Conclusions The treatment of Wernicke's encephalopathy in parenterally fed patients is possible with the use of high thiamine doses (800 mg) added to PN admixtures without a decrease in the drug content above 10% within the first 24 h. It should be emphasized that thiamine as a photosensitive drug must be stored and administered under conditions ensuring light protection.

Background Overdose deaths related to illegal drugs in North American markets are now dominated by potent synthetic opioids such as fentanyl, a circumstance foreshadowed by often-overlooked events in Estonia since the turn of the century. Market transitions generate important and far-reaching implications for drug policy. Argument and analysis The supplier-driven introduction of illegally manufactured synthetic opioids into street opioids is elevating the risk of fatal overdose. Using the most recent overdose mortality and drug seizure data in North America, we find that overdose deaths and seizures involving synthetic opioids are geographically concentrated, but this might be changing. Examination here suggests that in some places fentanyl and its analogues have virtually displaced traditional opioids, such as heroin. The concealing of synthetic opioids in powders sold as heroin or pressed into counterfeit medications substantially increases harms. The nature and scale of the challenge posed by synthetic opioids is unprecedented in recent drug policy history. Conclusions There is urgent need for policy and technological innovation to meet the challenges posed by illegally produced synthetic opioids. Novel interventions worth examining include supervising drug use, proactively deterring on-line distribution and new technologies aimed at improving transparency, such as point-of-use drug content testing. Continuing to approach this problem only with existing policies and available methods, such as naloxone, is unlikely to be enough and will result in many premature deaths.

Background The objective of present research work is to design and characterize camptothecin gel using Carbopol-934 for the treatment of epidermoid carcinoma. Optimized herbal gel formulations were evaluated for homogeneity and appearance, viscosity, extrudability, spreadability, drug content, drug release, pH, and in vitro skin cancer activity on A431 cell lines. Results Mass and Infrared Spectra respectively conforms molecular weight and functional groups present in camptothecin. All the formulations F1 to F5 showed good homogeneity, pH from 6.68 to 6.90, spreadability in the range of 15.81–23.37 gm.cm/s, extrudability 85.51–90.45% w/w, drug content 89.12–96.64%, and in vitro diffusion 88.36–98.40%, respectively. The drug release study showed that all the formulations followed a diffusion-controlled, zero-order release mechanism. Anticancer activity results indicate that camptothecin gel induce cell death in A-439 cells having IC50 48.03 μg and % apoptosis 54.67 ± 4.58. Conclusion Topical delivery of camptothecin alleviates the side effects caused by systemic chemotherapy; hence, the developed herbal gel formulation can be effectively useful to deliver camptothecin in the treatment of epidermoid carcinoma on A-431 cells.

The aim of this study was to a choice most exceptional technique for the development of antidiabetic nanoparticles encompass natural polymer particles using the Analytic Hierarchy Process (AHP). In our method of selection may be lead to waste of time, loss of products and financial resources. Based on the above reasons, AHP has employed to discover the appropriate method. In the AHP, a special hierarchy was built with a goal for alternatives. After constructing the AHP, the expert select software was used to calculate the overall priority of criteria, sub-criteria and options. The best alternative selected was founded on the highest priority. Based on the Nanoscale to formulate and evaluate antidiabetic nanoparticles encompasses natural polymer particles, and it shows the particle size Polydispersity Index and zeta potential were within acceptable limits. Drug content and entrapment efficiencies were 94.16% and 86.14%, respectively. Our study concludes that AHP was the feasible and real tool for choosing the most suitable method for the formulation and evaluation of antidiabetic nanoparticles.

Simple, rapid, precise, accurate and specific UV-spectrophotometric method has been developed for atorvastatin calcium determination in bulk and in tablets dosage form. The method was based on using sodium citrate 0.01M as hydrotropic agent. Measurements of the UV absorbance were performed at 241 nm, and the developed method was validated as per ICH guidelines. The method obeyed Beer’s law (R2 = 0.999) in a concentration range of 2 – 20 μg/mL. The limits of detection (LOD) and quantification (LOQ) were 0.64 and 1.9 μg/mL, respectively. At all levels of precision, RSD% values were below 2%. Accuracy of the proposed method was ascertained by standard addition method and the percentage recovery (n = 3) was within 100 – 100.43%. The method was applied to analysis of three atorvastatin tablet brands each claimed to contain 20 mg atorvastatin, and the percentage drug content was found to be 101.42 ± 1.56%, 99.04 ± 0.33%, and 97.71 ± 0.98%.

Amlodipine is a calcium channel blocker that is widely used to treat hypertension, which is a chronic health condition characterized by persistent elevated pressure of blood in the arteries. Hypertension is a predisposing factor to stroke, kidney failure, heart diseases and vision loss. The large demand for amlodipine makes it a good candidate for fakers. Consumption of substandard and/or fake amlodipine tablets will have a negative impact on the management of hypertension. This justifies continuous monitoring of amlodipine preparations in the marketplace and the provision of simple and cost-effective assay method that could be routinely utilised for their assay. Ten different brands of amlodipine tablets were qualitatively assessed for uniformity of weight, friability, hardness, disintegration and dissolution rate using standard physical methods. Quantitative assay was carried out using spectrophotometric method. The spectrophotometric measurement was done at a wavelength of 240 nm. Seven brands met the official requirements for uniformity of weight; eight passed the friability test and the hardness tests. All the brands tested passed the disintegration test and nine brands passed the dissolution test. The spectrophotometric assay showed that all the brands passed the United States Pharmacopoeia (USP) requirement for percentage drug content. The assay method used in this study is reliable, simple and cost- effective and can be routinely used to assay amlodipine tablets. Keywords: Amlodipine, qualitative, quantitative, assay, ultraviolet spectrophotometry

Objective: The main focus of the study was to investigate the marketed formulations of cinnarizine and it is marketed analogous. Methods: The study involved the analysis of basic pre-formulation studies, namely, physical properties, melting point, Fourier-transform infrared, loss on drying, assay of cinnarizine, standard curve, and partition co-efficient of various marketed tablets of cinnarizine. Results: Cinnarizine is an H1-receptor antagonist drug which is widely used for the treatment of dynamical sickness, vomiting, and vertigo. In this study, five known marketed formulations of cinnarizine were evaluated for weight variation, hardness, drug content, friability, disintegration time, and in vitro dissolution as well as the drug release kinetics of the tablets. As per the study, the drugs show low disintegration time and good hardness, also in vitro dissolution studies have shown near about 90% drug release at the end of the first 10 min and then cumulative drug release of not less than 92% in the nearby 10 min. Hence, these formulations show lower friability, acceptable taste, and shorter disintegration time which make them suitable to be accepted. Thus, the tablets are good for the use, so allow them to be marketed for the wellbeing of humans. Conclusion: It had been found that all the tablets show acceptable limits for various parameters of analysis, in a sustained manner. Thus, all the tablets are effective for usage under standard conditions.

One of the factors causes dental caries is salivary state. Drug addicts may have different salivary pH due to the drug content that is commonly consumed. The purpose of this study was to determine the relationship of salivary pH to the DMFT index in the Methadone Maintenance Therapy group in the city of Yogyakarta. This type of observational analytic study is Case control design. A sample of 64 subjects, divided into 2 case and control groups. Case groups are people who are members of the Methadone Maintenance Therapy Program at the Gedongtengen Health Center in Yogyakarta. Saliva pH measuring instrument is a pH strip. Test the relationship between salivary pH and DMFT using the Spearman rank test. The results showed that the average DMF-T in the case group was 8.4, higher than the control group 2.1 while the saliva pH of the PTRM group in the acid category (5.8) was lower than the control group with a neutral pH category (6.6). There is a significant relationship between salivary pH and DMF-T index in the Methadone Maintenance Therapy group in Yogyakarta City.

espanolSe prepararon y liofilizaron particulas (Ps) polimericas mucoadhesivas a base de Gantrez®, cargadas con farmaco, mediante el metodo de desplazamiento de disolvente modificado, para administracion intranasal de metoclopramida HCl (MCP). Las Ps obtenidas se caracterizaron midiendo tamano (368,0 ± 79,6), indice de polidispersion (0,294 ± 0,014) y potencial Z (-47,3 ± 4,4) (Nanosizer, Malvern, ZS90). La carga de farmaco (%CF= 12,86 ± 0,7) y la eficiencia de encapsulamiento (%EE= 77,14 ± 3,9) se determinaron por un metodo espectrofotometrico UV, previamente validado. Se hizo un estudio de liberacion in vitro, bajo condiciones sink, usando membranas de dialisis y un agitador orbital. Las particulas obtenidas poseen caracteristicas tecnologicas adecuadas en cuanto a tamano, contenido de farmaco y perfil de liberacion, por lo que se consideran potencialmente adecuadas para la administracion nasal de metoclopramida. EnglishUsing the modified solvent displacement method, drug-loaded mucoadhesive polymeric particles (Ps) based on Gantrez ®, were prepared and freeze-dried, intended for intranasal delivery of metoclopramide HCl (MCP). Ps characterization was performed by measuring their size (368,0 ± 79,6), the polydispersity index (0,294 ± 0,014) and the Zeta potential (-47,3 ± 4,4) (Nanosizer, Malvern, ZS90). Drug loading (%DL= 12,86) and encapsulation efficiency (%EE= 77,14) were determined by a UV spectrophotometric method (previously validated). In vitro release studies were carried out under sink conditions, using dialysis tubes and orbital shaker. The obtained particles possess attractive technological characteristics in terms of size, drug content and delivering profile, being potentially suitable for nasal administration of metoclopramide.

The main problems to humans include the infection caused in the respiratory tract and urinary tract, namely respiratory tract infection (RTI) and urinary tract infection (UTI). Cefpodoxime Proxetil drug is available in the market that has a problem with drug release profile and flows property. To overcome this problem, the compacted powder form made into a micro-ionized form for its better flow property and drug release by using a direct compression technique. The study was based on the aim to evaluate and formulate oro-dispersible tablets as an effective approach via orally for the treatment of RTI & UTI prepared by direct compression technique. FTIR and DSC showed no incompatibility between drugs and excipients. The pure drug Cefpodoxime Proxetil and the excipients were blended using an octagonal blender. The Pre-formulation study was performed for this blend and pure drug. Further, the blend was made compressed into a tablet by direct compression technique. Two factorial design was implemented. Prepared tablets were evaluated for drug content, hardness, thickness, uniformity in the weight, friability, disintegration test, dispersion time, in-vitro studies, release kinetics, and also stability studies. The optimized formulation A6 found to have good flow property. The evaluation results of optimized formula A6 showed 99.60% drug content, 390mg average weight, 0.91% weight uniformity, 3.80 kg/cm2 hardness, 0.67%, friability, 23.70sec, disintegration time, 16 sec dispersion time and 95.5% drug release than the other formulation batch. The current study showed that the optimized formula A6 exhibited good disintegration time, drug release, and friability than marketed product X and other batches.

Objectives The objective of this study was to develop a method for the preparation and characterization of paroxetine (PRX) tablets, obtained by coupling hot-melt extrusion and fused deposition modelling (FDM)-based three-dimensional printing (3DP) technology. The impact of the printing process parameters on the drug stability and on the tablets performance was assessed. Methods Tablets were obtained by FDM of hot-melt extruded PRX-loaded filaments. Physicochemical, thermal, spectroscopic, diffractometric analysis and in-vitro dissolution tests of the intermediate products and the finished dosage forms were performed. Key findings The characterization of printed tablets evidenced mass and dimensions uniformity, and consistency of drug content and dissolution profile. The formation of amorphous solid dispersions and interaction of formulation components throughout the manufacturing process were demonstrated. Layer thickness, printing temperature, printing and travelling speeds, and infill were the most impacting process parameters on both the physicochemical properties and the in-vitro performance of the 3D-printed tablets. Conclusions PRX tablets, meeting compendial limits, were manufactured by 3DP, envisaging their clinical use as individually designed dosage forms. The assessment of the impact of processing parameters on the printed tablets provided insights, which will ultimately allow streamlining of the 3D process set-up for quicker and easier production of patient-centric medicines.

Synergistic delivery of two drugs is a desirable choice to overcome drug resistance. Resveratrol (RES) and xanthohumol (XAN) which are both new drugs originated from plants exhibit great potential in the treatment of cancer, but there are few studies on combining them in a delivery system. In this work, a new core/shell fiber mesh containing RES and XAN was designed out via coaxial electrospinning, and the effect of drug content on the medicated fibers was discovered. RES/polyethylene oxide (PEO) could be well combined with XAN/Poly(lactide-glycolide) (PLGA) to make core/shell fibers, but fibrous morphology worsened with increasing drug content of the core or shell to some extent. The core/shell was amorphous nature, and changing drug content had little influence on the wetability of the core/shell fibers. The release accelerated with drug content increasing in the fibers, and RES and XAN showed gradient release, which the release rate of RES was slower than XAN. These two drugs could sustain release for 350 h. When the blend ratios of RES/PEO and XAN/PLGA were 50/50 and 10/90 in the fibers, the fiber mesh showed the best mechanical properties, of which the tensile strength and elongation at break were 2.85 ± 0.10 MPa and 55.23 ± 2.53%, respectively. The medicated fibers presented good characteristics of inhibiting breast cancer cell activity.

Content uniformity (CU) of the active pharmaceutical ingredient is a critical quality attribute of tablets as a dosage form, ensuring reproducible drug potency. Failure to meet the accepted uniformity in the final product may be caused either by suboptimal mixing and insufficient initial blend homogeneity, or may result from further particle segregation during storage, transfer or the compression process itself. This review presents the most relevant powder segregation mechanisms in tablet manufacturing and summarizes the currently available, up-to-date research on segregation and uniformity loss at the various stages of production process—the blend transfer from the bulk container to the tablet press, filling and discharge from the feeding hopper, as well as die filling. Formulation and processing factors affecting the occurrence of segregation and tablets’ CU are reviewed and recommendations for minimizing the risk of content uniformity failure in tablets are considered herein, including the perspective of continuous manufacturing.

A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets.

Quetiapine fumarate (QF) is an atypical antipsychotic used off-label for the treatment of delirium in critically-ill infants and children. For the treatment of pediatric populations or patient populations with trouble swallowing tablets, an oral suspension would be an ideal dosage formulation. However, there are no liquid formulations of QF commercially available. Therefore, a compounded oral suspension prepared from the commercial QF tablets is widely used in clinical settings. The extemporaneous preparation of QF compounded oral suspension changes the formulation from a solid form to a liquid form. Thus, the stability of QF compounded oral suspension should be critically evaluated to guide pharmacists for administration and storage of QF compounded oral suspensions. However, the stability of the nonaqueous oral QF suspension was not measured. The objective of this study was to develop QF compounded oral suspensions at 10 mg/mL by using commercial QF tablets in two readily available aqueous vehicles (Ora-Sweet and Ora-Blend) and measure their stability at both room temperature and under refrigeration. Physical stability of the QF compounded suspensions were evaluated by appearance and odor. Chemical stability of the QF compounded suspensions were evaluated based on pH, degradation, drug content and the amount of the drug dissolved in the vehicles. An HPLC method was validated and used to evaluate QF compounded suspensions over 60 days. In addition to the total drug in the suspensions, the dissolved drug in the vehicles was also measured during the stability testing and evaluated as a stability parameter. Overall, QF suspension prepared in Ora-Blend was preferable, demonstrating a superior 60-day stability at both room temperature and refrigerated storage.