Formulation and Evaluation of Taste Masked Oro-dispersible Tablets of an Anti-HIV Drug

摘要

Tenofovir disoproxil fumarate is a fumaric acid salt of bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir. Tenofovirexhibits activity against HIV-1 reverse transcriptase. Tenofovir disoproxil fumarate is the water soluble (BCS class – III drug) diesterprodrug of the active ingredient tenofovir. The oral bioavailability in fasted patients is approximately 25%. The drug is incompletelyabsorbed from gastrointestinal tract. Formulation of tenofovir disoproxil fumarate into an oro-dispersible dosage form can providefast relief with greater bioavailability. The bitter taste of drug should be masked in order to formulate it in a palatable form. In thecurrent research work, an attempt was made to mask the bitter taste of tenofovir by complexation technique, with a formulationinto oro-dispersible tablets, using superdisintegrants sodium starch glycolate (SSG), crospovidone (CP) and croscarmellose sodium(CCS) in different concentrations. The complexes of tenofovir disoproxil fumarate with β-cyclodextrin were prepared byco-grounding method in various drug: complex ratios. The prepared solid inclusion complexes were analysed for taste masking andcharacterized by FT-IR. Using the optimized drug: β-cyclodextrin complex (1:1 molar ratio), oro-dispersible tablets were preparedand evaluated for thickness, weight variation, hardness, friability, drug content, wetting time, water absorption ratio, in vitrodispersion time, in vitro disintegration time and in vitro dissolution rate. The maximum drug release of 99.85% was obtained fromthe formulation F6 containing the highest concentration of CP and therefore formulation F6 was considered as the optimizedformulation.