FORMULATION AND EVALUATION OF ESOMEPRAZOLE FAST DISSOLVING BUCCAL FILMS

Objective: The present study deals with the formulation and evaluation of fast dissolving buccal films for effective treatment option in the gastroesophageal reflux disease.Methods: Esomeprazole fast dissolving buccal films are a convenient formulation of which can be taken with or without water. In the present investigation, polyvinyl alcohol and polyvinylpyrrolidone were used as film-forming agents and polyethylene glycol 400 is taken as plasticizer. Solvent evaporation method was used for the preparation of fast dissolving buccal films.Results: The films were prepared and evaluated for film thickness, folding endurance, dispersion test, drug content, and dissolution. The in vitro dissolution studies were carried out using simulated salivary fluid (pH 6.8 phosphate buffer).Conclusion: Among all the formulations, Formulation E7 was released up to 99.6% of the drug from the film within 5 min of time which exhibits faster absorption and also shows desirable characteristics of the film. The drug-excipient interaction studies WERE carried out by Fourier-transform infrared studies, differential scanning calorimetry analysis-X-diffraction studies, and scanning electron microscopic studies and the results revealed that there were no major interactions between the drugs and excipients used for the preparation of films

SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING SOLUPLUS AS CARRIER

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Ezetimibe solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as a disintegrant in pellets. Ezetimibe pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in 1% SLS using USP apparatus II. FTIR and SEM analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation ED5 showed better dissolution rate to the extent of 1.07 folds and 1.95 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation EP5 containing 1:5 ratio of ezetimibe to soluplus showed an improved dissolution rate to the extent of 1.173 folds and 2.136 folds when compared to the marketed formulation and the pure drug, respectively. FTIR analysis revealed that there was no major interaction between the drug and the excipients.  Conclusion: From the present study, it was observed that the solubility of ezetimibe was enhanced by soluplus in pellet formulations when compared to solid dispersions

DEVELOPMENT AND EVALUATION OF OSMOTIC CONTROLLED RELEASE MATRIX TABLETS FOR LOSARTAN POTASSIUM

Osmotically controlled oral drug delivery systems utilize osmotic pressure as energy source for the controlled delivery of drugs, independent of pH and hydrodynamic conditions of gastro intestinal tract (GIT). The present study was aimed to develop osmotic controlled extended release formulations of Losartan potassium an angiotensin II receptor antagonist with anti- hypertensive activity. Losartan potassium matrix tablets were prepared by direct compression process using HPMC K 15M as polymeric material and mannitol as osmogen at varied concentrations. The matrix tablets were further coated with different compositions of ethylcellulose7cps and PEG-4000 by pan coating method. Physical parameters such as weight uniformity, drug content, hardness and friability were evaluated for uncoated tablets and were found to be within I.P limits. The coating thickness and percentage of coating applied for various tablets were also evaluated. The optimized coated tablets were further subjected to micro drilling on the upper face to get 0.5µm orifice diameter. All the tablets were further subjected to dissolution studies by using USP apparatus II with distilled water as medium. These studies indicated that all the tablets were found to release the drug up to 12 hours, while coated tablets with orifice found to release the drug at zero order rate, which was in good agreement with peppas n values >0.9