Analysis chemical-pharmaceutical of Darunavir tablets and its inclusion complex

Abstract

Darunavir is a protease inhibitor used in the treatment of HIV infection. It is a synthetic non-peptide analogue of amprenavir which became commercially available in 2006. It is a pillar of the therapy cocktail for patients with the virus. On the market are found Darunavir ethanolate tablets of 75, 300, 400 and 600 mg. This is the most stable form. This drug has low solubility in water and poor bioavailability therefore require administration in relatively high doses for a successful therapeutic effect. The complexation of drugs by using cyclodextrin is welcome in this point because improve the solubility and consequently increase the dissolution rate of poorly soluble drugs. This project aims to achieve (I) investigation of polymorphism, (II) perform and study the complexation of Darunavir with ²-cyclodextrin, (III) develop and validate analytical methods for Darunavir and the inclusion complex, including capillary electrophoresis, spectroscopy in the infrared region and chromatographic analysis, (IV) dissolution study to compare the dissolution rate of Darunavir with their inclusion complex, (V) carrying out study the long term stability as well as providing (VI) techniques for the qualitative identification to the pharmaceutical form and standard. This research includes a current issue, innovative and extremely important for both the area of quality control of drugs and for the pharmaceutical technology, being a multidisciplinary work. (AU)