药物化学

Tablet Formulation and Enhancement of Aqueous Solubility of Efavirenz by Solvent Evaporation Co-Crystal Technique

Abstract

Vikas G Rajurkar, Nagare Amit Sunil and Vilas Ghawate

Improvement in the aqueous solubility,physicochemical and micromeritics property of insoluble and slightly soluble drugs is of major concern in pharmaceutical formulations. It is commonly observed in the drug industry that on average more than 35% of newly discovered drugs are poorly water-soluble. Poor “drug like” properties of lead compounds led to ineffective absorptionfrom the site of administration, less bioavailability which has been designated as an important part of the high clinical failure. In the present work, Efavirenz, nonnucleoside reverse transcriptase inhibitors (NNRTIs) in first-line antiretroviral therapy (ART) belongs to BCS class II drug (highly permeable and low soluble). A simultaneous DSC, FT-IR, SEM, XRPD micro spectroscopy, dissolution study and micromeritics properties studies was used to quickly investigate the co-crystal. Tablet formulation was developed by direct compression method and there evaluation was performed.