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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Systemic availability and pharmacokinetics of thymol in humans.
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Systemic availability and pharmacokinetics of thymol in humans.

机译：百里香酚在人体内的系统可用性和药代动力学。

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摘要

Essential oil compounds such as found in thyme extract are established for the therapy of chronic and acute bronchitis. Various pharmacodynamic activities for thyme extract and the essential thyme oil, respectively, have been demonstrated in vitro, but availability of these compounds in the respective target organs has not been proven. Thus, investigation of absorption, distribution, metabolism, and excretion are necessary to provide the link between in vitro effects and in vivo studies. To determine the systemic availability and the pharmacokinetics of thymol after oral application to humans, a clinical trial was carried out in 12 healthy volunteers. Each subject received a single dose of a Bronchipret TP tablet, which is equivalent to 1.08 mg thymol. No thymol could be detected in plasma or urine. However, the metabolites thymol sulfate and thymol glucuronide were found in urine and identified by LC-MS/MS. Plasma and urine samples were analyzed after enzymatic hydrolysis of the metabolites by headspace solid-phase microextraction prior to GC analysis and flame ionization detection. Thymol sulfate, but not thymol glucuronide, was detectable in plasma. Peak plasma concentrations were 93.1+/-24.5 ng ml(-1) and were reached after 2.0+/-0.8 hours. The mean terminal elimination half-life was 10.2 hours. Thymol sulfate was detectable up to 41 hours after administration. Urinary excretion could be followed over 24 hours. The amount of both thymol sulfate and glucuronide excreted in 24-hour urine was 16.2%+/-4.5% of the dose.
机译：建立了在百里香提取物中发现的精油化合物，用于治疗慢性和急性支气管炎。在体外已分别证明了百里香提取物和百里香精油的各种药效学活性，但是尚未证明这些化合物在各自的靶器官中的可用性。因此，必须进行吸收，分布，代谢和排泄的研究，以提供体外作用与体内研究之间的联系。为了确定百里酚对人口服后的全身可用性和百里酚的药代动力学，在12名健康志愿者中进行了一项临床试验。每个受试者接受单剂量的Bronchipret TP片剂，相当于1.08 mg百里酚。在血浆或尿液中未检测到百里酚。然而，尿液中发现了硫酸百里酚和百里香葡糖苷酸代谢产物，并通过LC-MS / MS进行了鉴定。在通过GC分析和火焰离子化检测之前，通过顶空固相微萃取对代谢产物进行酶水解后，对血浆和尿液样品进行了分析。在血浆中可检测到硫酸百里酚，而不是百里香葡糖醛酸。血浆峰值浓度为93.1 +/- 24.5 ng ml（-1），在2.0 +/- 0.8小时后达到峰值。平均终末消除半衰期为10.2小时。给药后最多41小时即可检测到硫酸百里酚。排尿可以持续24小时以上。硫酸百里酚硫酸盐和葡糖醛酸化物在24小时尿液中排泄的量为剂量的16.2％+ /-4.5％。

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