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ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF CARVEDILOL BY SOLID DISPERSION TECHNIQUE USING ROTA-EVAPORATION AND LYOPHILIZATION METHODS

Abstract

Shivangi Madhok* and Akankasha Madhok

Despite significant advancements in the science of drug delivery, solubilization of poorly aqueous soluble drugs still remains a challenging task for formulation. The purpose of the study was to improve the physicochemical properties of poorly aqueous soluble drug carvedilol (CAR) like solubility, dissolution properties and stability of poorly soluble drug by forming dispersion with skimmed milk powder as carrier. CAR was formulated by solid dispersions using rota-evaporation method and lyophilization method in different ratios 1:1, 1:3, 1:5, and 1:7 of drug and carrier (skimmed milk powder). The formulations were evaluated for various in vitro parameters (Drug content, Drug release, phase solubility studies, dissolution efficiency, DSC, SEM, XRD) as well as changes in the physical state during storage under different humidity conditions. Good uniformity of drug content was observed with all formulations and lies between 96.29 % to 99.13 %. All the solid dispersions showed dissolution improvement compare to pure drug. The solubility was also increased from 23.28 μg/ml in case of carvedilol pure drug to 224.68 μg/ml and 205.31 μg/ml in case of these solid dispersions. The DE60 was also increased from 36.83% to 56.31% and 54.92 %. The dispersion with skimmed milk powder (1:7) by Rota evaporation Method and Lyophilization Method (1:5) showed faster dissolution rate (96.1 % and 94.88 % respectively). The tablets were formulated from the final and stable solid dispersions. These solid dispersions were selected to prepare tablets using Ac-dosol as superdisintegrant and Avicel PH102 as diluents. Tablets were characterized for hardness, friability, disintegration time, percent drug release studies. Tablet T2 showed highest dissolution rate and best dissolution efficiency at (DE 60) minutes. The similarity factor was calculated for comparison of the dissolution profile before and after stability studies. The f2 value was found to be more than 50 (~ 94.00) thereby indicating a close similarity between both the dissolution profiles. 

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