Takigawa T, Tainaka H, Mihara K, Ogata H
Department of Biopharmaceutics, Meiji College of Pharmacy, Tokyo, Japan.
Biol Pharm Bull. 1998 May;21(5):541-3. doi: 10.1248/bpb.21.541.
We studied the inhibition of S-warfarin metabolism by nonsteroidal antiinflammatory drugs (NSAIDs) in human liver microsomes in vitro. After screening for potential inhibitors among ten NSAIDs using human recombinant cytochrome P450, inhibition kinetic parameters were estimated using human liver microsomes. Phenylbutazone and bucolome were suggested to increase the unbound steady-state level of S-warfarin about four- and five-fold, respectively, as estimated from these metabolic parameters.
我们在体外人肝微粒体中研究了非甾体抗炎药（NSAIDs）对S-华法林代谢的抑制作用。使用人重组细胞色素P450在10种NSAIDs中筛选潜在抑制剂后，用人肝微粒体估算抑制动力学参数。根据这些代谢参数估算，保泰松和布可隆分别可使S-华法林的游离稳态水平提高约4倍和5倍。
