CONTROLLED RELEASE FORMULATIONS OF ANTIRETROVIRAL (ARV) DRUGS USING POLYMETHACRYLATE POLYMERS
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Date
2010-09-26
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Ahmadu Bello University Zaria
Abstract
To improve patient compliance and ensure better success in the
management of HIV, spansule technology was employed to formulate
controlled release dosage drug. Generic forms of seven of the most
commonly used Anti-retro viral (ARV) drugs (didanosine, indinavir,
lamivudine, nelfinavir, nevirapine, stavudine and zidovudine) and their
clinically approved combinations were used in this study. Calculated
daily dose was divided into one loading and four maintainace doses.
Granules of the drugs, prepared using wet granulation method, were
divided into five batches and spray coated with various grades of
polymethacrylate polymers (Eudragit brand). Using different
combinations/ratios, each ARV drug and their combinations were filled
into capsules of sizes 00 to 000. Parameters such as solubility,
disintegration, coating thickness and dissolution were determined. In-
vitro testing for drug release was conducted to mimic various pH
conditions of the G.I.T using disodium hydrogen orthophosphate and
potassium dihydrogen phosphate buffers. Spectrophotometric method
was used to determine drug release. To serve as control, conventional
forms of the seven ARVs obtained from a major manufacturer were tested for drug release.