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Risk control for nitrosamine impurities in drug products is currently a major challenge in the industry. Nitrosamines can form during drug product manufacturing and storage through the reaction of nitrites with amine-containing APIs or impurities. The level of nitrites in excipients and the rate of reaction often control the build-up of nitrosamine. Although the variability in nitrite levels across excipient types and suppliers is well recognized, the impact of excipient selection on the level of nitrosamine formed has not been systematically studied. This gap of knowledge is addressed in the current work. We present theoretical case studies of formulations where microcrystalline cellulose (MCC), or lactose supplier, or superdisintegrant type are changed in pursuit of lower levels of nitrite. The impact of the average, maximum, and minimum levels of nitrites in each excipient on nitrosamine formation in the dosage form is calculated. The input data for this calculation are the formulation composition, nitrosamine molecular weight (MW), percentage of conversion, and nitrite levels per excipient. The percentage of conversion (based on the formulation and manufacturing variables) and nitrite levels were taken from the recent literature. We show that changing the supplier of a single excipient, or of the three most critical excipients, can reduce nitrosamine formation by up to −59% and −89%, respectively. We also show that high-risk formulations, e.g., high MW nitrosamines, high dosage weights, and high percentages of conversion (e.g., wet granulation), can often be de-risked below regulatory acceptable daily intake via careful excipient selection. Finally, we provide an open-access tool that enables users to calculate the theoretical formation of nitrosamines in their specific formulations. This calculation template can be used for (i) the preliminary screening of the risk of nitrosamine formation in drug products and (ii) the preliminary assessment of the impact of excipient selection for risk mitigation. [ABSTRACT FROM AUTHOR]

Carbamazepine is a medicine used to manage epilepsy and partial or tonic-clonic seizures. This study aimed at formulating and obtaining carbamazepine orodispersible tablets for paediatric use at a 50 mg dose, with a diameter not greater than 6 mm and a tablet weight of 80 mg, through a direct compression process. The SeDeM pre-formulation/formulation method was used to define the characteristics of both carbamazepine and the selected excipients for direct compression. This study succeeded in formulating and obtaining the proposed tablets. Following the application of the SeDeM method, the tablets met the mass uniformity test and showed appropriate hardness values for orodispersible tablets. The tablets also met the United States Pharmacopeia (USP) test specifications at t = 60 min. The orodispersible tablets obtained may improve compliance with paediatric treatment with carbamazepine, ensuring the safety and effectiveness of the medicine.

Telmisartan (Tel) is a potent antihypertensive drug with a very poor aqueous solubility, especially in pH ranging from 3 to 9 (i.e., biological fluids) that results in poor bioavailability. Our aim was to improve Tel solubility and dissolution rates without the need for expensive multistep procedures, and without inclusion of alkalinizers. This study adopted the use of surface solid dispersions (SSDs) employing superdisintegrants, hydrophilic polymers and combined carriers including a superdisintegrant with a hydrophilic polymer. Tel-SSDs were formulated using thesolvent evaporation method. Compatibility between Tel and different carriers was examined via FT-IR. Tel-SSDs were evaluated optically and thermally to reveal a complete loss of the crystalline nature of the drug. Both drug content and percentage yield were calculated to judge the efficiency of the preparation technique used. Saturation, aqueous solubility, and dissolutions rates were determined. Dissolution profiles were studied using model dependent and independent approaches and were subjected to the pair-wise procedure using the DDsolver software program. Effect of aging was studied by comparing the drug content and dissolution profiles of freshly prepared SSDs with aged samples. All Tel-SSDs showed acceptable physical properties. Tel-SSDs showed pertinent enhancement related to the carrier used. Combined surface solid dispersions employing superdisintegrant croscarmellose sodium with either hydrophilic polymer PEG 4000 or Poloxamer 407 gave remarkable enhancement in solubility and dissolution rates of Tel where more than 90% of the drug was released within 20 min. The effect of aging results proved a non-significant difference in the drug content and dissolution profiles between fresh and aged samples. Formulation of Tel SSDs using combined carriers proved to be effective in enhancing the aqueous solubility and dissolution rates of Tel, as well as showing good stability upon aging. [ABSTRACT FROM AUTHOR]

Carbamazepine is a medicine used to manage epilepsy and partial or tonic-clonic seizures. This study aimed at formulating and obtaining carbamazepine orodispersible tablets for paediatric use at a 50 mg dose, with a diameter not greater than 6 mm and a tablet weight of 80 mg, through a direct compression process. The SeDeM pre-formulation/formulation method was used to define the characteristics of both carbamazepine and the selected excipients for direct compression. This study succeeded in formulating and obtaining the proposed tablets. Following the application of the SeDeM method, the tablets met the mass uniformity test and showed appropriate hardness values for orodispersible tablets. The tablets also met the United States Pharmacopeia (USP) test specifications at t = 60 min. The orodispersible tablets obtained may improve compliance with paediatric treatment with carbamazepine, ensuring the safety and effectiveness of the medicine. [ABSTRACT FROM AUTHOR]

Swelling‐based disintegration is considered important for drug release from tablets and can be modified with excipients called tablet disintegrants. Swelling of tablets occurs axially and radially, and most researchers have observed both these events separately using 2D images. In the current work, we have studied these events simultaneously instead of separately under a stereozoom microscope for tablet compacts composed of high proportions of disintegrants (sodium starch glycolate, SSG and croscarmellose sodium, CCS), using water as the disintegrating medium. A hypothesis is proposed for the measurements of radial and axial swellings from a single 2D image, as horizontal lengths based on trigonometric functions for a right‐angle triangle. All predicted axial and radial lengths (as per proposed hypothesis) are found validated with respect to vernier calliper measurements for dry‐tablet compacts with a minute error of 3.809%. The axial swelling is approximately fivefolds more than that of radial swelling on the basis of normalised lengths. No particular trend can be spotted exclusively in favour of a superdisintegrant; however, the CCS‐based tablets have shown higher swelling as compared to SSG‐based tablets. From the current studies, it is evident that both axial and radial dimensions are obtainable from single 2D stereozoom images and can be successfully implemented for swelling studies of tablets. [ABSTRACT FROM AUTHOR]

The present study aimed to investigate if the manufacturer variability of croscarmellose sodium, a superdisintegrant, could have an impact on the dissolution of sitagliptin phosphate (a highly water-soluble drug) and escitalopram oxalate (a sparingly soluble drug) from their tablets. Some of the physicochemical properties of croscarmellose sodium (CCS) powders obtained from four different manufacturers were studied. Tablets containing 25 mg sitagliptin phosphate and 10 mg escitalopram oxalate were prepared, and the effects of the source and varying concentration of CCS (0, 1, 3, and 5%w/w) on the disintegration time and dissolution rate of the mentioned drugs were investigated. The results of the following tests: degree of substitution, residue on ignition, loss on drying, content of water-soluble material, and pH, carried out according to the USP/NF CCS monograph, were within the acceptance criteria for all four products. However, considerable differences were found in the swelling behavior of CCS samples, differentiating them into two groups of highly swelling and low-swelling products. The disintegration times of the tablets containing different quantities of the various CCS samples were similar, which confirms the indiscriminatory nature of this test. However, the highly swelling CCSs resulted in tablets with superior dissolution profiles. While with the highly water-soluble drug, increasing the concentration of low-swelling CCSs to 3 or 5% could improve the dissolution profiles; in the case of sparingly soluble drug, this was not possible. Therefore, functional differences between CCSs produced by various manufacturers are affected by the drug solubility and the ratio of the disintegrant used in the formulations. [ABSTRACT FROM AUTHOR]

Sediment delivery model (SeDeM) system is innovative tool to correlate micromeritic properties of powders with compressibility. It involves computation of indices which facilitate direct compressibility of solids and enable corrective measures through particle engineering. Study had multiple objectives, viz, (i) to enhance solubility of BCS class II, nevirapine using solid dispersions; (ii) SeDeM analyses of excipients and solid dispersions to analyze direct compressibility; and (iii) prepare orodispersible tablets (ODT). Solid dispersions were prepared by solvent evaporation. Superdisintegrants and solid dispersions were analyzed for primary indices of dimension, compressibility, flowability, stability, and disgregability derived from micromeritic properties. Radar diagrams were constructed to provide visual clues to deficient properties for direct compressibility. ODTs were prepared using excipients which passed criteria for direct compressibility and evaluated for tablet properties. Solid dispersions with Eudragit S100 revealed 6 to 10 fold increase in solubility in various dissolution media including biorelevant media in comparison with plain drug. Solubility was found to be pH dependent. SeDeM analyses facilitated identification of superdisintegrants and excipients with unfavorable compressibility. Radar diagrams provided a clear pictorial evidence of lacunae in powder properties. Based on SeDeM results, tablets were formulated by direct compression using crosspovidone, croscarmellose sodium, and mannitol. All batches showed 40% release in first minute in simulated salivary fluid. [ABSTRACT FROM AUTHOR]

Oral disintegrating tablets are a new trend in novel drug delivery systems that have seen a surge in popularity in recent decades. To improve the efficacy of solid dosage forms, super disintegrants are used. This is accomplished by reducing the disintegration time, which improves the rate of drug dissolution. Disintegrants are substances or combination of substances added to a drug formulation to aid in the breaking up or disintegration of tablet or capsule content into smaller fragments that dissolve more quickly than without them. Several newer agents known as 'Superdisintegrants' have been developed in recent years. Superdisintegrants classified as synthetic, semi-synthetic, natural, and co-processed blends have been used to create effective mouth dissolving tablets and overcome the limitations of traditional tablet dosage form. In the solid dosage form, superdisintegrants are typically used at a low level typically (1-10%) relative to the total weight of the dosage unit. In present studies, includes all the information about Superdisintegrants, such as their types, advantage, selection criteria, incorporation methods, ideal properties and mechanism, which are used in the formulation to provide safer, more effective drug delivery while maintaining patient conformity. [ABSTRACT FROM AUTHOR]

Purpose: The present study was aimed to formulate and evaluate fast-disintegrating tablets (FDTs) having Flurbiprofen (FP) and Metoclopramide HCl (MHCl) in combination. Method: Direct compression was used to formulate FDTs of FP and MHCl as a combination regimen in six formulations. FDTs are defined as solid oral dosage form that disintegrates rapidly within seconds when placed in the oral cavity. FDT-1, FDT-2, FDT-3, FDT-4, FDT-5, and FDT-6 were formulated using crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants each in two formulations. Several pre-compression tests (angle of repose, bulk density, tapped density, Hausner's ratio, and compressibility index), post-compression evaluation (weight variation, friability, hardness, disintegration time, wetting time, assay, in vitro dissolution study, release kinetics study, statistical analysis, and stability study), and drug compatibility study were done for all six formulations. Results: Pre-compression evaluation showed good flow properties of powder blend. Drug compatibility study showed no interactions between active drugs and excipients. Disintegration and wetting time of all the formulations were in seconds indicating immediate release of drug. Optimized formulation (FDT-6) containing sodium starch glycolate in 15 mg gave 100% release in 15 min for MHCl and in 20 min for FP. Optimized formulation was found stable after being placed at accelerated stability conditions for 6 months. Release kinetics study showed that all formulations followed Korsmeyer-Peppas model indicating drug release from modified release dosage form. Statistical analysis revealed no significant difference statistically (p > 0.05) between drug release rate of all prepared formulations. Conclusion: FDTs improved the release rate that assured that this tactic may be beneficial to increase the dissolution rate of FP and MHCl in order to increase patient compliance. [ABSTRACT FROM AUTHOR]

The buccal delivery is an attractive route to improve the clinical efficacy of ropinirole hydrochloride (RH) for the treatment of Parkinson and restless syndrome since this drug undergoes extensive first-pass effect, which has only 50% bioavailability after oral administration. The purpose of this study was to develop and optimize the formulation of fast disintegrating buccal effervescent tablets of RH using four types of superdisintegrants. The direct compression method was used to develop four different formulas containing RH using Kyron T-314, crospovidone, croscarmellose sodium, and sodium starch glycolate separately as a superdisintegrant. Sodium bicarbonate and citric acid were added to the formulations to produce effervescence, while sodium carbonate was used as a pH adjusting agent. All the prepared formulas were evaluated, in terms of weight variation, friability, content dose uniformity, hardness, disintegration, and dissolution test. The best formulation was selected for the subsequent study. The obtained results from pre-compression studies were in acceptable range according to British Pharmacopoeia. All formulas passed through the quality control test and significant difference (P < 0.05) was observed for the formula four compared to other formulas, due to the presence of Kyron T-314 as a superdisintegrant in formulation number 4. RH cloud be prepared as a buccal effervescent tablet and superdisintegrant provide fast disintegration of the tablet to exert rapid action.

The main objective of this study was to prepare quick dispersible tablets of drug sumatriptan succinate, which can rapidly disintegrate in the saliva using three different superdisintegrants that is, sodium starch glycolate, crospovidone, and croscarmallose sodium with taste masking polymer beta-cyclodextrin and aspartame as a sweetener. The taste masking of the drug was done by mixing it with the polymer beta-cyclodextrin using solvent evaporation method and then mixing optimized quantity of aspartame to it. The quick dispersible tablets were prepared by direct compression technique using taste masked drug and other formulation excipients. The effect of various super disintegrants in three different concentrations has been studied. The prepared tablets were evaluated for wetting time, in-vitro disintegration time, strength, and in-vitro dissolution time. As per the results obtained, it was found that the formulation batch no. 4 was found to be the best formulation, as the data’s obtained by it was found to be in the required range of mouth dissolving tablets.

Since orally disintegrating tablets (ODTs) of tramadol hydrochloride are not available in the market, so an attempt has been taken to formulate and evaluate ODT preparation of tramadol hydrochloride. In this present work, direct compression was the technique used for preparing ODT using superdisintegrants like croscarmellose sodium, sodium starch glycolate and crospovidone at different concentrations. Prepared formulations were evaluated for various quality parameters-angle of repose, Carr's index, Hausner ratio, weight variation, friability, hardness, drug content, dispersion time, wetting time and invitro dissolution. The angle of repose data indicated that the flow property of all the formulations was good to excellent. Comparing with the specifications, the results of Carr's index (%) and Hausner's ratio indicated that the flowability of all the formulations blend was significantly good. Prepared formulations showed average wetting time ranging from 40-45 seconds, average dispersion time with 3-6 minutes. In-vitro dissolution profile indicated the cumulative % drug release between 30-80% for most of the cases. [ABSTRACT FROM AUTHOR]

Background: In the current investigation, a strive became finished to synthesis a novel polymer, starch tartrate by treating potato starch with tartaric acid and utilize it as superdisintegrant for designing candesartan cilexetil (CC) fast-dissolving tablets. Starch tartrate was synthesized from potato starch and evaluated for phytochemical tests, physicochemical properties, and acute toxicity studies. CC tablets have been prepared by usage of a direct compression approach. Results: Acute toxicity studies on novel polymer indicated that there are no physiological changes in the rat behavior and were healthy. Formulated CC tablets were gone through precompression parameters, post-compression parameters, and stability studies. All the parameters were observed to be within the pharmacopeia detailed limits. It was found that the formulation of starch tartrate dissolute the drug at a faster rate when compared to other formulations (P < 0.05). Optimized formulation was evaluated for FTIR and DSC analysis revealed that there had been no most important incompatibilities between the active molecule and excipients. Stability research on the optimized formula confirmed the stability of the formulation. Conclusion: It was concluded that the novel polymer, starch tartrate synthesized from potato starch was endow to be appropriate for fast dissolving tablet preparation. The optimized formulation obtained was with decent chemical and physical properties having accelerated disintegration and onset of action. [ABSTRACT FROM AUTHOR]

Purpose: Sertraline HCl (SRT) is a selective serotonin reuptake inhibitor (SSRI) that is used to treat depression and anxiety disorders. SRT is characterized by limited water solubility and suffers from low bioavailability due to first-pass effect. Therefore, this study aims to formulate SRT-Cyclodextrin (CD) orodispersible tablet (ODT) using direct compression technique to avoid SRT drawbacks. Methods: A 22 × 3 full factorial design was adopted using three factors, namely, CD type (βCD and HPβCD), SRT-CD mixing type (physical and solid dispersion), and type of diluent/superdisintegrant (xylitol/polyvinylpyrrolidone, maltitol/polyvinylpyrrolidone, and maltitol/co-processed mixture of polyvinylpyrrolidone and Ac-Di-Sol). Precompression studies were carried out on each formulation blend followed by the characterization of the prepared ODTs. All the ODTs were assessed for weight variation, hardness, friability, content uniformity, in vitro disintegration time, wetting time, water absorption ratio, in vitro dispersion time, and in vitro dissolution study. Accelerated and long-term stability studies were executed on the selected formulation. A pharmacokinetic study of the selected SRT ODT was accomplished through sublingual administration using LC/MS/MS assay in comparison to the conventional oral tablet Lustral®. Results: ODT prepared with SRT-βCD solid dispersion with maltitol/polyvinylpyrrolidone (F4) led to reducing the disintegration time (9 ± 1.41 sec) and enhancing the dissolution efficiency (84 ± 2.5%). It showed a significant decrease of Tmax to 4 h instead of 8 h for Lustral® and increased the extent of drug absorption with a relative bioavailability of 117%. Conclusion: SRT orodispersible sublingual tablet can be considered as a promising delivery system for the treatment of depression. SRT sublingual ODT can avoid first-pass effect of SRT and hence improve its bioavailability due to the enhancement of SRT dissolution and rapid absorption through the oral mucosa. [ABSTRACT FROM AUTHOR]

The paper aimed to progress an ideal gastro retentive drug delivery system intended for directing Losartan and Hydrochlorothiazide as a fixed-dose combination for anti-hypertensive therapy. The bilayer tablets were primed through direct compression method. Losartan was formulated by means of a floating layer expending hydrophilic swellable polymer Hydroxy Propyl Methyl Cellulose K4M, ethyl cellulose (4cps) as a buoyancy enhancer, sodium bicarbonate as a gas spawning agent. The amount of polymer blends remains optimized using 23 full factorial designs. The clout of experimental factors such as swelling agent concentration, buoyancy enhancer and gas generating agent on floating lag time, total floating time, T50% and % drug release remain investigated to get optimized formulation. The responses remain analyzed using Analysis of variance, and polynomial equation stood created for every retort using Multiple linear regression analysis. Entirely preparations floated for more than 12 h. The release pattern of losartan stood fitted to diverse models based on the coefficient of correlation (r). All the formulations, except F2, showed the Korsemeyer-Peppas model as the best fit model. Formulation F2 showed the zero-order model. Diffusion exponents (n) remained indomitable designed for entirely formulations (0.45–0.89), accordingly the chief drug discharge mechanism was non-fickian (anamolous) transport. Formulation F4 containing 20% w/w Hydroxy Propyl Methyl Cellulose K4M, 15% Sodium bicarbonate and 5% ethyl cellulose (4cps) was the best formulation as per the range of drug release remain institute to be more than 95 % in 12h and floating lag time was 20.15 s. The immediate-release layer stood optimized using crospovidone and Indion 414 as a super disintegrant. Formulation A8 containing 2% Indion 414 was considered as optimized formulation as it released 99% drug within 35 min and possessed less disintegration time. Optimized formulation F4 from the controlled-release layer and A8 from immediate-release layer was used to formulate bilayer tablet. The optimized formulation was imperilled to stability reading for three months at 40○C/75% relative humidity. The stability revision exhibited no substantial alteration in the appearance of tablets, floating characteristics, drug content and in-vitro drug dissolution. Consequently, a biphasic drug release design was effectively accomplished over the formulation of floating bilayer tablets.

Purpose: To develop fast dissolving oral film to address vomiting and nausea in pediatric population. Methods: Oral films of Dimenhydrinate were prepared by solvent casting method by using hydroxypropylmethyl cellulose E5 (HPMC E5), polyethylene glycol 400 (PEG 400) and croscarmellose sodium. Solubility of dimenhydrinate was enhanced by ethanol as a co-solvent. To make dimenhydrinate palatable sodium saccharin and peppermint oil were used. All films were evaluated for mechanical parameters, surface pH, morphology, disintegration time and percent dissolution. Results: Films were smooth, acceptable and white in colour. For optimized batch, drug content (99.106%), disintegration time (25 sec), dissolution (99.10% in 210 sec), surface pH (6.81) were acceptable. Conclusion: Optimized batch, due to its potential to deliver through fast dissolving film, can be developed for clinical use.

The purpose of this research work is to formulate and evaluate the Orodispersible tablet of Fluvastatin Sodium to enhance the bioavailability and effectiveness of the drug. The objectives of the drug work were to formulate and evaluate Orodispersible tablets of Fluvastatin Sodium, having adequate mechanical strength, rapid disintegration, and fast action. Precompression parameters like angle of repose, bulk density, tapped density, compressibility index & post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration, and in-vitro dispersion time were studied. The hardness, friability, and drug content of all the formulations were found to be within the limits. The best formulation PK09 has shown good disintegration time, dissolution time, and dispersion time. The optimized formulation of batch PK9 gave the best in-vitro release of 99.60% in 3min in phosphate buffer pH 6.8. The release of the drug followed the matrix diffusion mechanism as compared to the commercial formulation. Formulation PK9 gives quick disintegration and better drug release. Hence it can be concluded that the formulation of PK9 is stable and effective for quick action and it is an alternative to the conventional tablets. [ABSTRACT FROM AUTHOR]

Due to more versatility and comfort, mouth dissolving tablets are the most advanced type of oral solid dosage forms. Compared to conventional tablets, it increases the effectiveness of APIs by dissolving within a minute in the oral cavity after contact with less saliva, without chewing and without the need for water for administration. Mouth Dissolving Tablets of Ketorolac tromethamine were prepared by direct compression method using various superdisintegrants like crospovidone, Croscarmellose sodium, and Sodium starch glycolate in different concentrations. Prepared tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time and in vitro drug release. Results of pre-compression and post-compression studies of all formulations were found within the standard limits. The tablets of all the batches were found to release more than 80% of drug in 5 minutes, which is the desired quality of mouth dissolving tablets that helps in faster absorption of the drug and quick onset of therapeutic effect. The the order of dissolution of various disintegrants was found to be Crospovidone> SSG> CCS. There was no significant variation in drug content of drug during stability studies for selected batch F3 in accelerated conditions over three months. It was concluded from the study that fast release of Ketorolac tromethamine from formulation F3 may reduce onset of drug action with better patient compliance. [ABSTRACT FROM AUTHOR]

Furazolidone is a nitro furan antimicrobial agent used in the treatment of diarrhea or enteritis caused by bacteria or protozoan infections. Furazolidone is also active in treating typhoid fever, cholera and salmonella infections. In present research work an attempt has been made to prepare inclusion complex tablets of Furazolidone with increased rate of dissolution may leads to increase bioavailability. Formulation of inclusion complex tablet of poorly soluble Furazolidone by β Cyclodextrin and Hydroxypropyl β cyclodextrin by different ratio (1:1), (1:2), (1:3) using kneading method. The papered inclusion complex evaluated by phase solubility study optimized inclusion complex Furazolidone: Hydroxypropyl β Cyclodextrin (1:2) ratio give enhanced solubility. After optimization of inclusion complex of Furazolidone: Hydroxypropyl β Cyclodextrin inclusion complex were prepared by direct compression method. Sodium starches Glycolate, croscarmellose sodium, crospovidone are used as a superdisintegrants. Drug polymer interactions were investigated using Fourier transform infrared spectroscopy. The prepared formulation were evaluated for various parameters like weight variation, hardness, friability, drug content, disintegration time, wetting time, in vitro drug release, Batch D5was optimized formulation containing 5% Crospovidone showed less disintegration time 20 sec and more than 99.54% drug release at 30 mint. Stability studies were carried out at 40 ± 2°C/75 ± 5% RH for formulation D5 for 1 month Stability studies on the best formulation indicated that there was no significant change found in hardness, disintegration time, wetting time and drug release of tablets. [ABSTRACT FROM AUTHOR]

Oral disintegrating tablets are a novel attractive dosage form in which the tablet disintegrates or dissolves in the buccal cavity within seconds without the use of water. The major drawback in designing this dosage form is unpleasant taste and low solubility of active entity. Valsartan is an antihypertension drug used in treatment of high blood pressure, congestive heart failure (CHF) and post-myocardial infarction (MI). It is characterized by its bitter taste, which effects the patient's compliance. Despite this, it belong to the BCS II Classification in which drugs have low solubility and high permeability. The aim of the present research work was to formulate orally disintegrating tablets of valsartan using natural and synthetic superdisintegrants. The drug was characterized according to different compendia methods, on the basis of identification by UV spectroscopy, pH, organoleptic properties and other tests. Drugpolymer compatibility was carried out by FTIR. The values of pre-compression parameters assessed were within specified limits and showed good free flowing properties. The data on post-compression parameters such as weight variation, hardness, friability, wetting time, water absorption ratio, content uniformity, disintegration time and dissolution was found to be within the prescribed limits. Batch F9 with disintegration time 24 sec was selected as the optimized formulation. Batch F9 was also subjected to stability studies for three months and was tested for its appearance, average weight, hardness, disintegration time, percent friability and its release rate, which were in prescribed ranges and satisfactory. [ABSTRACT FROM AUTHOR]

Oral fast dissolving midodrine hydrochloride films prepared by solvent casting method, PEG 400 was the selected plasticizers, incorporating superdisintegrants such as croscarmellose sodium (CCS) and sodium starch glycolate (SSG) to achieve the goal. Drug content, weight variability, film thickness, disintegration time, endurance, percentage of moisture content, and in vitro dissolution tests were analyzed for the prepared films. In all formulations, the tensile strength value was found from 0.965±0.045 and 1.256±0.032 and the folding capacity was over 100. The assay values ranged from 97.98±0.25 to 99.89±0.36 percent for all formulations. The disintegration time was ranging between 55±9 to 120±6 sec, the minimum time for disintegration was found in formulation F5 (55±9). The prepared F5 formulation shows greater release of the drug (99.25±0.41 percent) within 15 min relative to other formulations. As the drug having low solubility, fast disintegration may leads to more drug availability for dissolution, resulting in faster absorption in systemic circulation increased systemic availability of drug leads to quick onset of action which is prerequisite for hypertension. [ABSTRACT FROM AUTHOR]

Background: In the present investigation, an attempt was made to isolate starch from jackfruit seed powder and utilize it as a superdisintegrant to design fast dissolving tablets of irbesartan. Methods: Starch was isolated from jackfruit seeds via aqueous and alkali extraction processes and evaluated for its physicochemical properties, for phytochemical tests, and for acute toxicity studies. Irbesartan fast dissolving formulations were prepared using the wet granulation technique. Results: Acute toxicity studies for the extract indicated that all rats were healthy with no physiological changes in their behavior. The prepared irbesartan tablet formulations were found to be stable according to the Indian Pharmacopoeia-specified limits for postcompression parameters. From in vitro dissolution studies, it was observed that formulations F5 and F8 containing 5% w/w of alkali extracted starch and 5% w/w of croscarmellose sodium showed faster disintegration and improved dissolution rate compared with the other formulations. Fourier transfer infrared spectroscopic and differential scanning colorimetric analysis performed on optimized formulations indicated that there were no major interactions between the drug and excipients. Accelerated stability studies carried out on optimized formulations showed all tablets to be stable. Conclusion: The tablets prepared from jackfruit seed starch as superdisintegrant were found to be suitable for preparation of fast dissolving tablets.

Objective: Oral dispersible isoniazid 50 mg/pyridoxine 6.25 mg fixed-dose combination (FDC) tablets were formulated for Isoniazid Preventive Therapy in pediatrics weighing less than 5 kg. Significance: The Kenyan clinical market lacks age-appropriate isoniazid/pyridoxine formulations for pediatrics whose dose requirements are catered extemporaneously. The proposed oral dispersible FDC tablets would improve the treatment outcomes of the drug combination by ensuring accurate dosing, reduce pill burden, prolonged shelf life, and circumvent individual drug stock-outs. Method: Nine batches of isoniazid/pyridoxine FDC tablets with an average weight of 125 mg differing in the composition of three superdisintegrants were formulated. Pre-formulation studies were done on the powder blend using Fourier transform infra-red spectroscopy before the blend was directly compressed. Pharmaceutical parameters of the tablets were assessed against compendial specifications. Results: Pre-formulation studies showed no predictable incompatibilities between the drugs and excipients. All batches complied with compendial specifications for weight uniformity, hardness and disintegration, while three batches complied with the friability test. Only Batch Nine tablets containing croscarmellose and sodium starch glycolate superdisintegrants in the ratio of 3:5 complied with the assay specification. Batch Nine tablets contained 96% of isoniazid and 95% of pyridoxine complying with the United States Pharmacopeia (USP) monograph limits of 90–110% and 95–115% of the labelled isoniazid and pyridoxine, respectively. In the in-vitro dissolution studies, 88.7% and 105.3% of isoniazid and pyridoxine contained in Batch Nine tablets dissolved within 30 min complying with the USP specifications for dissolution test. Conclusion: The isoniazid/pyridoxine FDC incorporating croscarmellose sodium and sodium starch glycolate superdisintegrants was the most successful formulation since the formulated tablets complied with all the evaluated compendial specifications implying potential clinical utility of the formulation.

Orally disintegrating tablet (ODT) has number of advantages like faster onset of action, ease of administration, rapid disintegration and dissolution etc. A novel attempt has been made to develop orally disintegrating tablets of Ondansetron by using two approaches, one is soluble hydrophilic matrix by superdisintegrant and other is effect of sweetener on the formulation. Direct compression method was employed for making orally disintegrating tablets. The formulated orally disintegrating tablets have rapid disintegration property for better patient compliance. Formulated tablets were evaluated for physical parameters along with wetting time, disintegration time, drug content and “in vitro” dissolution. In first approach it was found that batch F7 containing Crospovidone (Polyplasdone XL 10) 10 mg showed minimum disintegration time (i.e. approx. 7.00 seconds) with maximum drug release. Wetting time for batch F7 was found to be minimum (i.e. 12 seconds). In second approach of selection of sweetener batch F 10 containing Sodium saccharin was found better in terms of Impurity study (Relative Substances study).Impurity was found within the specified limit compared to other two sweeteners. Stability study was carried out on optimized formulation. Overall batch containing 10 mg Crospovidone (Polyplasdone XL 10) along with Sodium Saccharin was found stable both physically and chemically.

SeDeM design expert technique used to evaluate the risks of poor flow of pharmaceutical powders under preformulation studies which reveals direct compression suitability and prepare robust composition of active pharmaceutical ingredient (API) and excipient in tablets formulation. The purpose of this study was to develop oral disintegrating tablets of Furosemide using different concentration of natural and synthetic superdisintegrants by means of SeDeM design technique. Oral disintegrating tablets (ODT) of Furosemide were prepared by direct compression technique using isolated banana powder and croscarmellose sodium (Ac-di-sol) together with microcrystalline cellulose as superdisintegrants. SeDeM design was performed to check suitability and deficient of excipients and drug for optimized composition derived based on IPP value. These tablets were evaluated for hardness, friability, drug content, weight variation, wetting time and in-vitro dissolution. All the formulations showed low weight variation with dispersion time less than 173.5±0.70 seconds and rapid in-vitro dissolution. The drug content of all the formulations was within the acceptable limits. Lubricated blend composition of F4 found average radius value 5.24, 0.66 and 5.509 for IGC, IP and IPP respectively, compressed tablet shown good physical properties. The optimized formulation F4 showed good release profile with 99.25 percentage drug release compared to other trial batches. It was concluded that natural superdisintegrant (banana powder) showed better disintegrating property than synthetic super disintegrant (Ac-di-sol) in the formulations of ODTs. [ABSTRACT FROM AUTHOR]