薄荷油和评价ascorbyl棕榈酸酯作为细胞色素抑制剂P4503A4活动在体外和体内。

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梳妆台g·瓦希V,黄,黄HT,贝利DG

薄荷油和评价ascorbyl棕榈酸酯作为细胞色素抑制剂P4503A4活动在体外和体内。

中国新药杂志。2002年9月,72 (3):247 - 55。doi: 10.1067 / mcp.2002.126409。

PubMed ID

12235445 (在PubMed

]

文摘

目的:我们的研究旨在确定薄荷油的效果和ascorbyl棕榈酸酯对细胞色素P4503A4 (CYP3A4)活动在人类非洛地平的体外和口服生物利用度。方法:可逆和硝苯地平氧化机理压抑人类肝脏微粒体进行了研究。非洛地平口服药物动力学及其dehydrofelodipine代谢物测定12个健康志愿者管理非洛地平后,10毫克延长释放的平板电脑,与葡萄柚汁(300毫升),薄荷油(600毫克),ascorbyl棕榈酸酯(500毫克),或水在随机4路交叉研究。结果:薄荷油(抑制常数(K (i)) = 35.9 + / - 3.3 microg / mL,意思是+ / - SEM)和2成分、薄荷醇(K (i) = 87.0 + / - 7.0 micromol / L),和薄荷基乙酸(K (i) = 124.0 + / - 7.0 micromol / L),产生可逆抑制硝苯地平氧化。Ascorbyl棕榈酸酯是更有效(K (i) = 12.3 + / - 0.5 micromol / L)。这些物质系统抑制剂。葡萄柚汁,薄荷油增加曲线下的面积(AUC)值的非洛地平(173%,94%,-280%;范围(P < . 01), 140%, 77% -262%;分别P < . 05),与水。他们增强血浆浓度峰值非洛地平(C (max))和AUC和C (max) dehydrofelodipine但没有改变半衰期(t(1/2))的物质。 Grapefruit juice decreased the dehydrofelodipine/felodipine AUC ratio, but peppermint oil did not. Ascorbyl palmitate did not change the pharmacokinetics of felodipine or dehydrofelodipine compared with water. CONCLUSIONS: Peppermint oil, menthol, menthyl acetate, and ascorbyl palmitate were moderately potent reversible inhibitors of in vitro CYP3A4 activity. Grapefruit juice increased the oral bioavailability of felodipine by inhibition of CYP3A4-mediated presystemic drug metabolism. Peppermint oil may also have acted by this mechanism. However, this requires further investigation. Ascorbyl palmitate did not inhibit CYP3A4 activity in vivo.

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药物酶

药物	酶	类	生物	药理作用	行动
薄荷油	细胞色素P450 3 a4	蛋白质	人类	未知的	抑制剂	细节