Abstract

The aim of the present research was to enhance the dissolution rate of poorly water soluble drug, bicalutamide by adsorption process. Bicalutamide is an antiandrogen agent used in the treatment of prostate cancer. To improve the dissolution rate of the drug, hydrophilic carrier like povidone K30 and adsorbent like magnesium aluminum silicate were used as dissolution rate enhancers. Granules of bicalutamide were prepared by wet granulation technique by using magnesium aluminum silicate and povidone K 30 either alone or in combination at different concentrations. The granules were evaluated for packing and compression properties. The granules were compressed into tablets, and different tableting parameters were investigated. The dissolution profile of the tablets was also evaluated and compared with the marketed product. From the dissolution profile, it was observed that the carrier ratio of 3:1 of magnesium aluminum silicate to povidone K 30 exhibited higher dissolution rate than the other formulations.   Key words: Bicalutamide, magnesium aluminum silicate, adsorption, povidone K 30.

Highlights

  • Product development scientists working in the areas of drug discovery, preformulation and formulation studies are using various solubilization techniques for solving solubility problems related to the drug in their daily work

  • The results showed that the granules were compressible by tapping

  • The results showed that the dissolution rate of the drug was greatly influenced by the amount of adsorbate concentration present

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Summary

Introduction

Product development scientists working in the areas of drug discovery, preformulation and formulation studies are using various solubilization techniques for solving solubility problems related to the drug in their daily work. (Vippagunta et al, 2002; Chiou and Riegalman, 1971; Leuner and Dressman, 2005; Kinoshita et al, 2002; Toshiro, 2006). The solubility and dissolution rate of poorly water soluble drug can be altered in many ways, such as modification of drug crystal forms, addition of co-solvents, micronisation, solubilisation by surfactants, addition of adsorbents, solid dispersion, complexation with cyclodextrins (CD), etc. Some of these techniques make use of organic solvents which are expensive and hazardous to our environment. The two reasons suggested for the rapid release of drugs from the surface of clays are the weak

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