Gastrointestinal permeability studies using combinations of rifampicin and nucleoside analogue reverse transcriptase inhibitors in rats
Objectives: To investigate the gastrointestinal tract (GIT) permeability of five nucleoside analogue reverse transcriptase inhibitors (NRTIs), viz., zidovudine, stavudine, abacavir sulphate, lamivudine and didanosine, individually and in the presence of rifampicin in rats by ligated-loop technique....
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Published in | Indian journal of pharmacology Vol. 39; no. 6 |
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Main Authors | , |
Format | Journal Article |
Published |
India
Medknow Publications on behalf of Indian Pharmacological Society
14.03.2008
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Subjects | |
Online Access | Get full text |
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Summary: | Objectives: To investigate the gastrointestinal tract (GIT)
permeability of five nucleoside analogue reverse transcriptase
inhibitors (NRTIs), viz., zidovudine, stavudine, abacavir sulphate,
lamivudine and didanosine, individually and in the presence of
rifampicin in rats by ligated-loop technique. Materials and Methods:
The permeability studies were carried out on Sprague-Dawley rats in the
weight range of 240-260 g. The drug contents were estimated by a
validated gradient HPLC method. Degradation and solubility studies were
also carried out on the drugs, alone and in combination, to correlate
with the results of in situ experiments. Results: The results showed
that rifampicin was better absorbed from stomach and duodenum;
zidovudine was moderately absorbed throughout GIT; stavudine and
lamivudine were absorbed better through the intestine; abacavir was
well absorbed through duodenum; and didanosine completely disappeared
through stomach and was absorbed moderately from proximal parts of the
intestine. In drug combinations, NRTIs did not influence
permeability/absorption of rifampicin and vice versa. The disappearance
of didanosine through stomach could be ascribed to decomposition of the
drug at pH 2. Conclusion: The study reaffirms that rifampicin and
NRTIs do not influence gastrointestinal permeability of each other. |
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ISSN: | 0253-7613 1998-3751 |