Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada.
J Pharm Pharm Sci. 2010;13(1):43-55. doi: 10.18433/j3zp42.
Oseltamivir is a prodrug that requires metabolic activation but there is little information on whether natural health products interact to prevent the biotransformation by the carboxylesterase.
HPLC-DAD-ESI-MSD and fluorometric assays were used to determine if 50-pooled mixed gender human liver microsomes can mediate the formation of the active carboxylate metabolite and then if this reaction is affected by natural health products.
Extracts from 6 traditional Cree botanicals, a commercially available Echinacea product, Goldenseal and a traditional Chinese medicine reduced the formation of the active drug. In addition to oseltamivir carboxylate we report the detection of two new metabolites which are derivatives of oseltamivir carboxylate, one of which is a metabonate formed as a result of methanol.
In vitro studies would suggest that there is the potential for some natural health products used by patients in response to pandemic A/H1N1 to reduce drug efficacy. Further studies are required to determine if these potential interactions could be clinically significant.
奥司他韦是一种前药，需要代谢激活，但关于天然保健品是否会相互作用以阻止羧酸酯酶的生物转化，知之甚少。
采用 HPLC-DAD-ESI-MSD 和荧光检测法，确定 50 例混合性别人类肝微粒体是否可以介导活性羧酸代谢物的形成，然后确定该反应是否受天然保健品的影响。
6 种传统克里族植物、一种市售的紫锥菊产品、白毛茛和一种中药提取物均可减少活性药物的形成。除奥司他韦羧酸酯外，我们还报告了两种新代谢物的检测，它们均为奥司他韦羧酸酯的衍生物，其中一种是甲氧基形成的甲氧基羧酸酯，是甲醇的代谢产物。
体外研究表明，用于应对大流行性 A/H1N1 的一些患者使用的天然保健品有可能降低药物疗效。需要进一步研究以确定这些潜在的相互作用是否具有临床意义。
