Does a kampo medicine containing schisandra fruit affect pharmacokinetics of nifedipine like grapefruit juice?
Does a kampo medicine containing schisandra fruit affect pharmacokinetics of nifedipine like grapefruit juice?
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DOI：
10.1248/bpb.29.2065
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发表时间：
2006-10-01
影响因子：
2
通讯作者：
Mizukami, Hajime
中科院分区：
文献类型：
--
作者：
Makino, Toshiaki;Mizuno, Fumika;Mizukami, Hajime
近年来，中药相互作用作为一个重要的医学课题引起了人们的广泛关注。然而，药物信息有时令人困惑。已有的体外研究表明五味子对CYP 3A 4有较强的抑制作用，并认为五味子具有药-药相互作用的可能性。在本研究中，我们评估了五味子和shoseiryuto，在日本传统汉方医学包含8个草药，包括五味子，在体外对大鼠CYP 3A活性的草药配方的抑制作用，和shoseiryuto对硝苯地平在大鼠体内的药代动力学的影响，与葡萄柚汁，一个良好的特性的天然CYP 3A抑制剂。Shoseiryuto及其草药成分，五味子，紫菀和肉桂皮表现出体外抑制CYP 3A的作用。虽然Shoseiryuto在体外抑制大鼠CYP 3A活性的程度与葡萄柚汁相当，Shoseiryuto没有显着影响硝苯地平在大鼠的血浆浓度曲线葡萄柚汁。这些结果表明，使用与患者服用的相同剂型制备的草药提取物的体内实验是必要的，以提供有关草药-药物相互作用的适当信息。
Herb-drug interaction has attracted attention as medicinal topics recently. However, the drug information is sometimes confusing. Previous in vitro studies revealed that schisandra fruit had strong inhibitory effect on CYP3A4 and claimed the possibilities of its herb-drug interaction. In the present study, we evaluated the inhibitory effects of schisandra fruit and shoseiryuto, an herbal formula in Japanese traditional kampo medicine containing eight herbal medicines including schisandra fruit, on rat CYP3A activity in vitro, and the effect of shoseiryuto on pharmacokinetics of nifedipine in rats, in comparison with those of grapefruit juice, a well-characterized natural CYP3A inhibitor. Shoseiryuto and its herbal constituents, schisandra fruit, ephedra herb and cinnamon bark exhibited in vitro inhibitory effect of CYP3A. Although shoseiryuto inhibited rat CYP3A activity in vitro with a degree comparable to grapefruit juice, shoseiryuto did not significantly affect a plasma concentration profile of nifedipine in rats as grapefruit juice did. These results indicate that in vivo experiments using the extract of herbal medicine prepared with the same dosage form as patients take are necessary to provide proper information about herb-drug interaction.