Profiling of the Compounds Absorbed in Human Plasma and Urine after Oral Administration of a Traditional Japanese (Kampo) Medicine, Daikenchuto
Profiling of the Compounds Absorbed in Human Plasma and Urine after Oral Administration of a Traditional Japanese (Kampo) Medicine, Daikenchuto
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DOI：
10.1124/dmd.110.033589
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发表时间：
2010-11-01
影响因子：
3.9
通讯作者：
Hanazaki, Kazuhiro
中科院分区：
文献类型：
--
作者：
Iwabu, Jun;Watanabe, Junko;Hanazaki, Kazuhiro
大kenchuto （DKT）是一种医药级的日本传统（汉布）药物，广泛用于治疗包括术后肠梗阻在内的各种胃肠道疾病，已作为处方药纳入日本现代医疗保健体系。DKT是一种由日本辣椒（花椒果实）、加工姜、人参和麦芽糖作为添加剂组成的综合草药。尽管对DKT及其成分的药理活性进行了大量的研究，但缺乏对DKT的吸收、分布、代谢和排泄的研究，这使得很难获得其作用机制的一致图景。在本研究中，我们构建了一个由液相色谱和质谱分析7个条件组成的分析程序，对DKT成分类药材的44种成分进行了鉴定。我们对4名健康志愿者口服15.0 g DKT后0.5 ~ 8 h的血浆和尿液进行了研究。结果表明：1)辣椒和姜的血浆中羟基- α -三酚和[6]-shogaol分别在0.5 h出现显著峰，之后随着采样时间的延长逐渐降低；2)人参皂苷Rb-1是人参中一个突出的峰，在采样期间逐渐升高；3)在血浆和尿液中检测到葡萄糖醛酸偶联物羟基酚、酚和姜辣酚；4)两名男性个体和两名女性个体的样本之间没有明显差异。这些结果为DKT的药代动力学和药理学的进一步研究提供了强有力的基础。
Daikenchuto (DKT), a pharmaceutical-grade traditional Japanese (Kampo) medicine, has been widely used for the treatment of various gastrointestinal disorders including postoperative ileus and has been integrated into the modern medical care system in Japan as a prescription drug. DKT is a multiherbal medicine consisting of Japanese pepper (zanthoxylum fruit), processed ginger, and ginseng with maltose as an additive. Despite substantial research on the pharmacological activities of DKT and its ingredients, the lack of studies on absorption, distribution, metabolism, and excretion of DKT has made it difficult to obtain a consistent picture of its mechanism of action. In the present study, we constructed an analysis procedure consisting of seven conditions of liquid chromatography and mass spectrometric analysis, which enabled the identification of 44 ingredients of DKT component herbs. We investigated the plasma and urine profiles of these ingredients 0.5 to 8 h after oral administration of 15.0 g of DKT in four healthy volunteers. The results indicated that 1) hydroxy-alpha-sanshool and [6]-shogaol, the prominent peaks in plasma derived from Japanese pepper and ginger, respectively, were detected at 0.5 h and thereafter decreased throughout the sampling period; 2) ginsenoside Rb-1, a prominent peak derived from ginseng, increased gradually during the sampling period; 3) glucuronide conjugates of hydroxy-sanshools, shogaols, and gingerols were detected in plasma and urine; and 4) no obvious differences between samples from the two male and the two female individuals were observed. These results provide a strong basis for future studies on pharmacokinetics and pharmacology of DKT.