Suppr超能文献

胡椒碱对姜黄素在动物和人类志愿者体内药代动力学的影响。

Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers.

作者信息

Shoba G, Joy D, Joseph T, Majeed M, Rajendran R, Srinivas P S

机构信息

Department of Pharmacology, St. John's Medical College, Bangalore, India.

出版信息

Planta Med. 1998 May;64(4):353-6. doi: 10.1055/s-2006-957450.

Abstract

The medicinal properties of curcumin obtained from Curcuma longa L. cannot be utilised because of poor bioavailability due to its rapid metabolism in the liver and intestinal wall. In this study, the effect of combining piperine, a known inhibitor of hepatic and intestinal glucuronidation, was evaluated on the bioavailability of curcumin in rats and healthy human volunteers. When curcumin was given alone, in the dose 2 g/kg to rats, moderate serum concentrations were achieved over a period of 4 h. Concomitant administration of piperine 20 mg/kg increased the serum concentration of curcumin for a short period of 1-2 h post drug. Time to maximum was significantly increased (P < 0.02) while elimination half life and clearance significantly decreased (P < 0.02), and the bioavailability was increased by 154%. On the other hand in humans after a dose of 2 g curcumin alone, serum levels were either undetectable or very low. Concomitant administration of piperine 20 mg produced much higher concentrations from 0.25 to 1 h post drug (P < 0.01 at 0.25 and 0.5 h; P < 0.001 at 1 h), the increase in bioavailability was 2000%. The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in both rats and humans with no adverse effects.

摘要

由于姜黄素在肝脏和肠壁中快速代谢,生物利用度较差,因此从姜黄中提取的姜黄素的药用特性无法得到利用。在本研究中,评估了已知的肝脏和肠道葡萄糖醛酸化抑制剂胡椒碱对大鼠和健康人类志愿者体内姜黄素生物利用度的影响。当单独给大鼠服用2 g/kg剂量的姜黄素时,在4小时内可达到中等血清浓度。同时给予20 mg/kg的胡椒碱可使给药后1-2小时内姜黄素的血清浓度短暂升高。达到最大浓度的时间显著延长(P < 0.02),而消除半衰期和清除率显著降低(P < 0.02),生物利用度提高了154%。另一方面,在人类中,单独服用2 g姜黄素后,血清水平要么检测不到,要么非常低。同时服用20 mg胡椒碱可使给药后0.25至1小时产生更高的浓度(0.25和0.5小时时P < 0.01;1小时时P < 0.001),生物利用度提高了2000%。该研究表明,在所使用的剂量下,胡椒碱可提高大鼠和人类体内姜黄素的血清浓度、吸收程度和生物利用度,且无不良反应。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验