Division of Pharmacology and Therapeutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto, Japan.
J Pharm Pharmacol. 2012 May;64(5):670-6. doi: 10.1111/j.2042-7158.2011.01443.x. Epub 2012 Feb 7.
Many patients use herbal medicines to relieve menopausal symptoms. Keishi-bukuryo-gan contains five herbal components, and has been used for treating hypermenorrhoea, dysmenorrhoea and menopausal symptoms in Asian countries. In this study, we investigated the potential herb-drug interactions of keishi-bukuryo-gan in healthy female subjects.
Thirty-one healthy females (20-27 years) were studied to evaluate their baseline activity of cytochrome P450 (CYP) 1A2, CYP2D6, CYP3A, xanthine oxidase (XO) and N-acetyltransferase 2 (NAT2) based on the urinary metabolic indices of an 8-h urine sample collected after a 150-mg dose of caffeine and a 30-mg dose of dextromethorphan, and also the urinary excretion ratio of 6β-hydroxycortisol to cortisol. Thereafter, the subjects received 3.75g of keishi-bukuryo-gan twice daily for seven days, and underwent the same tests on post-dose day 7.
The geometric mean phenotypic index for CYP1A2 significantly decreased by 16% on day 7 compared with the baseline (P=0.026). Keishi-bukuryo-gan did not alter the indices for CYP2D6, CYP3A, XO and NAT2.
Keishi-bukuryo-gan may inhibit the activity of CYP1A2, which is predominantly involved in oestrogen metabolism. However, TJ-25 is unlikely to participate in herb-drug interactions involving medications predominantly metabolized by CYP2D6, CYP3A, XO and NAT2. K
许多患者使用草药来缓解更年期症状。克氏柴胡根包含五种草药成分，已在亚洲国家用于治疗月经过多、痛经和更年期症状。在这项研究中，我们调查了克氏柴胡根在健康女性中的潜在药物相互作用。
31 名健康女性（20-27 岁）接受研究，以评估她们在服用 150mg 咖啡因和 30mg 右美沙芬后 8 小时尿液样本的代谢物指标基础上，细胞色素 P450（CYP）1A2、CYP2D6、CYP3A、黄嘌呤氧化酶（XO）和 N-乙酰转移酶 2（NAT2）的基础活性，以及 6β-羟基皮质醇与皮质醇的尿排泄比值。此后，受试者每天两次服用 3.75 克克氏柴胡根，持续 7 天，并在第 7 天进行相同的测试。
与基线相比，第 7 天 CYP1A2 的几何平均表型指数显著下降 16%（P=0.026）。克氏柴胡根不改变 CYP2D6、CYP3A、XO 和 NAT2 的指数。
克氏柴胡根可能抑制 CYP1A2 的活性，CYP1A2 主要参与雌激素代谢。然而，TJ-25 不太可能参与主要由 CYP2D6、CYP3A、XO 和 NAT2 代谢的药物的药物相互作用。
