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ENZYME KINETICS OF NICARDIPINE METABOLISM IN HUMAN LIVER MICROSOMES
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 12
- DOI:
- 10.3321/j.issn:0513-4870.2001.12.003
- Key Word:
- 尼卡地平;微粒体;药代动力学
Abstract： 目的体外研究人肝微粒体中尼卡地平代谢的酶动力学及选择性的CYP酶抑制剂对其代谢的影响.方法用人肝微粒体研究尼卡地平代谢的酶动力学,探讨CYP酶的选择性抑制剂对其代谢的影响及参与其脱氢代谢的CYP酶.结果结果表明CYP3A的抑制剂酮康唑可以显著地抑制尼卡地平的脱氢代谢,使尼卡地平的代谢速率下降.CYP2E1的抑制剂DDC仅在高浓度时抑制尼卡地平二氢吡啶环脱氢代谢,而其他CYP特异性抑制剂对尼卡地平二氢吡啶环脱氢代谢没有明显的影响.结论 CYP3A参与了尼卡地平的代谢,CYP3A的抑制剂可能会与尼卡地平发生代谢相互作用,从而降低尼卡地平的代谢速率.
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