SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE PROTEASE INHIBITOR

There are more than 40% of drugs which are poorly soluble and 90% of the drugs from the pipeline are from BCS class II and IV. Application of techniques like computers, robotics, high-throughput screening, combinatorial chemistry have resulted in database of huge drug-like molecules which are generally derived solely based on the affinity of the molecule with the target physiological bodies viz. enzymes, receptors etc. These new chemical entities or drug-like substances having poor biopharmaceutical properties exhibiting poor pharmacological properties. Poor biopharmaceutical properties like poor solubility poses many difficulties and delay in drug development process as the these molecules show satisfactory performance in-vitro or in-silico but in-vivo they fail to exhibit pharmacological response thereby have low bioavailability. Drug dissolution is rate limiting step in majority of the cases hence increasing solubility leads to increased dissolution rate and thereby likely to increase the bioavailability. By doing so the drug is available in a solubilized form at site of action and is efficacious at lower doses. In the present work dissolution rate of poorly soluble protease inhibitor have been attempted using various methods. Using simple method of preparation formulations were prepared and it was observed that solid dispersion of the given drug exhibited better release than other methods viz. beta-Cyclodextrin and adsorption on an inert carrier.