Itharat Arunporn, Kanokkangsadal Puritat, Khemawoot Phisit, Wanichsetakul Preecha, Davies Neal M
Department of Applied Thai Traditional Medicine, Faculty of Medicine, Thammasat University, Pathumtani, Thailand, 12120.
Center of Excellence in Applied Thai Traditional Medicine Research, Thammasat University, Pathumtani, Thailand, 12120.
Res Pharm Sci. 2020 Oct 19;15(5):410-417. doi: 10.4103/1735-5362.297843. eCollection 2020 Oct.
To investigate the pharmacokinetics of piperine after single oral doses of capsules containing Sahastara (SHT) remedy dried ethanolic extracts in healthy Thai volunteers.
Twenty-four healthy volunteers were divided into two dosage groups. They received a single oral dose of SHT remedy extract capsules of 100 or 200 mg. Blood was collected at time intervals of 0, 0.5, 1, 2, 4, 6, 8, 12, 24, and 48 h. Acute clinical safety was monitored by complete physical examination and laboratory tests during the study period. Piperine concentration in blood and urine was determined by liquid chromatography tandem-mass spectrometry.
FINDINGS/RESULTS: No serious adverse events were detected, only one volunteer had abdominal pain that was self-limiting. The pharmacokinetics of piperine following SHT remedy extract capsule administration demonstrated a mean peak concentration (C) of piperine of 3.77 μg/mL and 6.59 μg/mL after dosing with 100 and 200 mg, respectively. Interestingly, a secondary maximum concentration of piperine was observed in this study, which might be related to enterohepatic recirculation. Negligible amounts of unchanged piperine were detected in urine.
The systemic exposure of piperine after SHT remedy ethanolic extract demonstrated dose proportionality after single oral dosing of 100-200 mg. Piperine was detectable in plasma for at least 48 h with evidence of enterohepatic recirculation. Metabolism and excretion profiles of piperine after administration of SHT remedy extract capsule need to be further explored for phytopharmaceutical product development.
研究在健康泰国志愿者单次口服含有萨哈斯塔拉（SHT）疗法干燥乙醇提取物的胶囊后胡椒碱的药代动力学。
24名健康志愿者分为两个剂量组。他们单次口服100或200毫克的SHT疗法提取物胶囊。在0、0.5、1、2、4、6、8、12、24和48小时的时间间隔采集血液。在研究期间通过全面体格检查和实验室检测监测急性临床安全性。采用液相色谱串联质谱法测定血液和尿液中胡椒碱的浓度。
未检测到严重不良事件，只有一名志愿者出现自限性腹痛。服用SHT疗法提取物胶囊后胡椒碱的药代动力学显示，服用100毫克和200毫克后胡椒碱的平均峰浓度（Cmax）分别为3.77微克/毫升和6.59微克/毫升。有趣的是，本研究中观察到胡椒碱有二次最大浓度，这可能与肠肝循环有关。尿液中检测到的未变化胡椒碱量可忽略不计。
单次口服100 - 200毫克SHT疗法乙醇提取物后，胡椒碱的全身暴露呈现剂量比例关系。血浆中胡椒碱至少在48小时内可检测到，有肠肝循环的证据。对于植物药产品开发，需要进一步探索服用SHT疗法提取物胶囊后胡椒碱的代谢和排泄情况。
