ABSTRACT

A reverse phase liquid chromatographic analytical method was developed for the simultaneous determination of Dapivirine and DS003 content in tablet dosage form. The chromatographic separation was achieved by using a C 18 column with mobile phase containing a gradient mixture of 0.05% v/v trifluoroacetic acid in water as mobile phase A and acetonitrile as mobile phase B at a flow rate of 0.5 ml/min. Both of the analytes were quantified with a UV detector at 245 nm. Dapivirine and DS003 were subjected to the stress conditions of oxidation, acid and base hydrolysis and thermolysis. The analytes were found to be stable under acidic and thermal conditions. Dapivirine was not significantly affected by base hydrolysis but was severely affected by oxidative conditions. DS003 was significantly affected by both oxidation and base hydrolysis. The stability-indicating capability of this method was demonstrated by adequate separation of the degradation peaks from those of the actives in the stress degraded samples. The method was validated for linearity, specificity, system suitability, precision and accuracy in accordance with ICH guidelines. The proposed method was applied to quantitate Dapivirine and DS003 in drug-excipient compatibility studies, assay of the tablets and stability studies of Dapivirine and DS003 tablets.

Sensitive and reproducible methods to assess in vitro release rates from semisolid products can provide significant value during drug development. The purpose of the present study was to develop and validate an in vitro release test (IVRT) for a topical gel formulation of an HIV microbicide. The method was developed using a vertical diffusion cell system, commercially available synthetic membranes, and HPLC with UV detection. The IVRT method was robust, reproducible, and sensitive to some of the formulation parameters evaluated. The method was applied to evaluate release rates of the active pharmaceutical ingredient from formulations during stability studies.