Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 102, Issue 6, Pages 1859-1868Publisher
WILEY-BLACKWELL
DOI: 10.1002/jps.23528
Keywords
tenofovir; HIV; AIDS; antiretroviral; vaginal tablet; microbicide; hardness; particle size; preformulation; powder technology
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Tenofovir is a nucleoside reverse-transcriptase inhibitor that is currently being investigated as a potential HIV microbicide candidate, with a recent phase IIb study of a 1% (w/w) tenofovir gel reducing HIV acquisition by 39% in sexually active women. However, not only does a HIV microbicidal product need to be safe and effective, it also needs to be cheap and easy to manufacture. In this study, we report the development of a tenofovir-loaded tablet, manufactured using a single sustained-release polymer, which has an acceptable hardness, friability and tenofovir release rate. Furthermore, by varying both the type and molecular weight of the sustained-release polymer, as well as the particle size of both tenofovir and the sustained-release polymer, we can vary the release rate of tenofovir from the tablets. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:18591868, 2013
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