UIC/NIH Center for Botanical Dietary Supplements Research, University of Illinois College of Pharmacy, Department of Medicinal Chemistry and Pharmacognosy, Chicago, Illinois, USA.
Clin Pharmacol Ther. 2010 Feb;87(2):219-25. doi: 10.1038/clpt.2009.251. Epub 2009 Dec 23.
Dietary supplements containing black cohosh are alternatives to conventional hormone replacement therapy in menopause. This study investigates the maximum tolerated dose of a 75% ethanol extract of black cohosh and determines the pharmacokinetics of one of its most abundant triterpene glycosides, 23-epi-26-deoxyactein. Single doses of black cohosh extract containing 1.4, 2.8, or 5.6 mg of 23-epi-26-deoxyactein were administered to 15 healthy, menopausal women. Serial blood samples and 24-h urine samples were obtained; blood chemistry, hormonal levels, and 23-epi-26-deoxyactein levels were determined. No acute toxicity or estrogenic hormone effects were observed. Pharmacokinetic analyses of 23-epi-26-deoxyactein in sera indicated that the maximum concentration and area under the curve increased proportionately with dosage, and that the half-life was ~2 h for all dosages. Less than 0.01% of the 23-epi-26-deoxyactein was recovered in urine 24 h after administration. No phase I or phase II metabolites were observed either in clinical specimens or in vitro.
含黑升麻的膳食补充剂是绝经后替代传统激素替代疗法的选择。本研究调查了黑升麻 75%乙醇提取物的最大耐受剂量，并确定了其最丰富的三萜糖苷之一 23-表-26-去氧乙酰的药代动力学。给 15 名健康绝经后妇女单次服用含有 1.4、2.8 或 5.6 毫克 23-表-26-去氧乙酰的黑升麻提取物。采集了一系列血样和 24 小时尿样；测定了血液化学、激素水平和 23-表-26-去氧乙酰的水平。未观察到急性毒性或雌激素样激素作用。23-表-26-去氧乙酰在血清中的药代动力学分析表明，最大浓度和曲线下面积与剂量成比例增加，半衰期在所有剂量下均约为 2 小时。给药后 24 小时，尿液中回收的 23-表-26-去氧乙酰不到 0.01%。无论是在临床标本还是在体外，均未观察到 I 期或 II 期代谢物。
