Intestinal permeability of Lamivudine using single pass intestinal perfusion

采用单次肠灌注法测定拉米夫定的肠道通透性

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Abstract

The intestinal transport of lamivudine, a nucleotide reverse transcriptase inhibitor, was investigated using the single pass intestinal perfusion technique in male Wistar rats. Single pass intestinal perfusion was performed in small intestine at a flow rate of 0.20 ml/min. Lamivudine exhibits a high intestinal permeability over the length of the small intestine indicative of compounds that are well absorbed. The P eff of lamivudine is in the range of drugs with high intestinal permeability and high fraction of dose absorbed indicating that lamivudine readily crosses the intestine. This also suggests that lamivudine belongs to biopharmaceutics classification system class I and is a good candidate for biopharmaceutics classification system based biowaiver. The permeability values obtained from this study may be useful in models of exposure assessment.

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