PMID: 8592677Nov 1, 1995Paper

Proton-cotransport of pravastatin across intestinal brush-border membrane

Pharmaceutical Research
I TamaiA Tsuji

Abstract

The purpose of the present study is to clarify the intestinal brush-border transport mechanism of a weak organic acid, pravastatin, an HMG-CoA reductase inhibitor. The transport of pravastatin was studied by using intestinal brush-border membrane vesicles prepared from rabbit jejunum, and uptake by the membrane vesicles was measured using rapid filtration technique. The initial uptake of [14C]pravastatin was markedly increased with decreases in extravesicular pH and showed a clear overshoot phenomenon in the presence of a proton gradient (pHin/out = 7.5/5.5). A protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, significantly reduced the uptake of [14C]pravastatin. In addition, an ionophore for sodium, potassium and proton, nigericin, stimulated the uptake of [14C]pravastatin in the presence of a potassium gradient ([K+]in/[K+]out = 0/145 mM). On the other hand, neither the imposition of an inwardly directed sodium gradient nor an outwardly directed bicarbonate gradient stimulated the uptake of [14C]pravastatin. In the presence of a proton gradient (pHin/out = 7.5/5.5), the initial uptake of pravastatin was saturable with the apparent Kt of 15.2 +/- 3.2 mM and Jmax of 10.6 +/- 1.21 nmol/mg protein/10 sec. The uptak...Continue Reading

Citations

Jan 4, 2003·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Akira Tsuji
Jul 19, 2003·Pharmacological Reviews·Naomi MizunoYuichi Sugiyama
Dec 25, 2004·Drug Metabolism and Pharmacokinetics·Toshiya Katsura, Ken-Ichi Inui
Aug 18, 2005·The Journal of Pharmacy and Pharmacology·Jun-Shik ChoiHyo-Kyung Han
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