Department of Gastroenterological Surgery, Gastroenterological Center, Cancer Institute Hospital, Japanese Foundation for Cancer Research, Tokyo, Japan.
Clin Pharmacol Ther. 2011 Aug;90(2):221-8. doi: 10.1038/clpt.2011.110. Epub 2011 May 4.
Peppermint oil has been shown to relax gastrointestinal smooth muscle. In this randomized, placebo-controlled study, an L-menthol preparation, NPO-11, was assessed for tolerability and pharmacokinetics (PK) during gastrointestinal endoscopy. Single doses of NPO-11, as high as 320 mg, were well tolerated. NPO-11 was rapidly absorbed, with peak concentrations reached within 1 h after administration. Approximately 70% of the administered L-menthol and its metabolites were excreted in the urine, and this amount fluctuated with no change in the dose. The principal metabolite identified in plasma and urine was menthol glucuronide. The other metabolites include mono- or di-hydroxylated menthol derivatives, most of which are excreted, in part, as glucuronic acid conjugates. The pharmacokinetic data indicated that when NPO-11 is sprayed directly onto the gastric mucosa, it is rapidly metabolized to glucuronic acid conjugates that are excreted in urine. The findings from this study provide new data on the safety and PK of NPO-11 and support further trials.
薄荷油已被证明可使胃肠道平滑肌松弛。在这项随机、安慰剂对照的研究中，对 L-薄荷醇制剂 NPO-11 的耐受性和药代动力学（PK）进行了评估，该研究用于胃肠道内镜检查。高达 320mg 的单剂量 NPO-11 具有良好的耐受性。NPO-11 吸收迅速，给药后 1 小时内达到峰值浓度。大约 70%的给予的 L-薄荷醇及其代谢物在尿液中排泄，并且该量随剂量的变化而波动。在血浆和尿液中鉴定出的主要代谢物是薄荷醇葡萄糖醛酸苷。其他代谢物包括单或二羟基化的薄荷醇衍生物，其中大多数以葡萄糖醛酸缀合物的形式部分排泄。药代动力学数据表明，当 NPO-11 直接喷洒到胃黏膜上时，它会迅速代谢为葡萄糖醛酸缀合物，然后从尿液中排泄。这项研究的结果提供了 NPO-11 的安全性和 PK 的新数据，并支持进一步的试验。
