Supramolecular modification of selected antiretroviral drugs

Master Thesis

2011

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University of Cape Town

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A number of antiretroviral drugs that are currently in use for anti-HIV therapy have extremely poor aqueous solubility. This, along with the fact that many of these pharmaceutical compounds possess potential hydrogen bond donor and acceptor functionalities, makes them ideal candidates for attempted supramolecular derivatisation. The primary objective of this study was to carry out cocrystal screening and attempt cyclodextrin complexation with nevirapine, efavirenz, lamivudine and zidovudine, with a view to identifying and isolating new solid forms of these drugs. Any new forms were to be characterised by a variety of analytical techniques, including thermal, spectroscopic and X-ray analysis and, where possible, such derivatives would be tested for any enhancements of drug solubility.
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