Inhibitory effect of valsartan on the intestinal absorption and renal excretion of bestatin in rats

Journal of Pharmaceutical Sciences
Xiaokui HuoKexin Liu

Abstract

Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically understood. Herein, the effect and mechanism of sartans on the intestinal absorption and renal excretion of the dipeptide-like drug bestatin were investigated. Following oral combination with valsartan, the plasma concentration and area under the plasma concentration-time curve of bestatin in rats decreased significantly. Bestatin absorption in rat-everted intestinal sacs was dramatically reduced by valsartan. Sartans exhibited concentration-dependent inhibition on the uptake of bestatin in human PEPT1 (hPEPT1)-HeLa cells. The cumulative urinary excretion and renal clearance of the two drugs in rats decreased after intravenous coadministration. Moreover, decreased uptake of the two drugs was observed in rats' kidney slices and human organic anion transporter (hOAT)1/hOAT3-transfected cells when coadministered. The results suggest that the intestinal absorption and renal excretion of bestatin in rats were inhibited by coa...Continue Reading

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Citations

Jul 13, 2014·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Li WangKexin Liu
Jan 7, 2016·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Chaojun XueKexin Liu
Oct 18, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yuan FengKexin Liu
Feb 18, 2017·Clinical Pharmacokinetics·Anton IvanyukThierry Buclin

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