口服给药后药-时曲线双峰现象研究进展

中国临床药理学与治疗学 ›› 2014, Vol. 19 ›› Issue (3): 341-345.

口服给药后药-时曲线双峰现象研究进展

王艳^1,2, 阳国平², 郭成贤², 裴奇³, 章冉冉^1,2, 黄路^1,2

¹中南大学药学院,长沙 410013,湖南;
²中南大学湘雅三医院临床药理中心,长沙 410013,湖南;
³中南大学湘雅三医院药剂科,长沙 410013,湖南

收稿日期:2013-10-08 修回日期:2014-02-25 出版日期:2014-03-26 发布日期:2014-04-10
通讯作者: 阳国平,男,教授,硕士生导师,主要从事临床药理学与药代动力学研究。Tel: 0731-88618339 E-mail: ygp9880@163.com
作者简介:王艳,女,硕士研究生,主要从事临床药学与药代动力学研究。Tel: 14789952453 E-mail: xiangyaxixi@163.com
基金资助:
重大疾病新药临床评价研究综合技术平台建设(2012ZX09303014-001);国家“重大新药创制”科技重大专项;国家自然科学基金(81302851);湖南省科学技术厅科技计划一般项目(2012WK3044);湖南省卫生厅科研基金课题(132013-028)

Plasma Double-peak Phenomenon Following Oral Administration

WANG Yan^1,2, YANG Guo-ping², GUO Cheng-xian³, PEI Qi², ZHANG Ran-ran^1,2, HUANG Lu^1,2

¹Pharmaceutical College of Central South University, Changsha 410013, Hunan,China;
²Pharmaceutical Preparation Section of Xiangya Third Hospital of Central South University, Changsha 410013, Hunan,China;
³Clinical Pharmacology Center of Xiangya Third Hospital of Central South University, Changsha 410013,Hunan,China

Received:2013-10-08 Revised:2014-02-25 Online:2014-03-26 Published:2014-04-10

摘要/Abstract

摘要： 许多药物在口服后血药浓度-时间曲线常表现出特殊的双峰甚至多峰现象。药物受崩解释放不均一及其脂溶性等的影响,是目前已知的产生双峰现象的常见药物因素。而从生理学角度分析,以往多认为肠肝循环、胃内pH等因素是从生理学角度分析产生双峰的主要原因,最新报道的产生双峰现象的机制有多种且一直存在争议,主要包括:胃动力因素的影响、胃肠道存在多吸收位点以及P-糖蛋白在肠道分布不均等重要机制。本文对口服给药后非药物制剂因素导致的药-时曲线双峰现象的机制研究概况进行综述,为药物体内过程研究及更好的指导临床安全用药提供参考。

关键词: 双峰现象, 肠肝循环, P-糖蛋白, 胃排空延迟, 胃肠蠕动

Abstract: The plasma concentration-time curves of many drugs often show a double-peak or mutiple-peak phenomenon after oral administration. The non-uniformly rate of drug disintegrate and release from the dosage form and lipid solubility may be the common causes of this matter. Enterohepatic circulation and gastric pH were thought to be the two main factors for the double-peak phenomenon from Physiology Perspective. According to the lasted report,there were multiple mechanism of double-peak phenomenon and the greater part of them have been controversial, mainly include that gastricmotility, multiple gastrointestinal tract absorption site, uneven distribution of P-glycoprotein in gut and so on. The main purpose of the article is summarizing the research situation of the mechanism of this phenomenon to provide reference for clinical safe drug use.

Key words: double-peak phenomenon, enterohepatic circulation, P-glycoprotein, delayed gastric emptying, gastrointestinal motility

中图分类号:

R969.1

王艳, 阳国平, 郭成贤, 裴奇, 章冉冉, 黄路. 口服给药后药-时曲线双峰现象研究进展[J]. 中国临床药理学与治疗学, 2014, 19(3): 341-345.

WANG Yan, YANG Guo-ping, GUO Cheng-xian, PEI Qi, ZHANG Ran-ran, HUANG Lu. Plasma Double-peak Phenomenon Following Oral Administration[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(3): 341-345.

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