中国临床药理学与治疗学2007，Vol.12Issue(2)：214-218,5.
组胺H1受体拮抗剂盐酸依匹斯汀片人体药动学与生物等效性研究
Pharmacokinetics and bioequivalence of epinastine hydrochloride,a histamine H1 receptor antagonist, in healthy Chinese volunteers
师少军 1李忠芳 2陈华庭 1曾繁典3
作者信息
- 1. 华中科技大学同济医学院附属协和医院药剂科,武汉,430022,湖北
- 2. 华中科技大学同济医学院附属协和医院妇产科,武汉,430022,湖北
- 3. 华中科技大学同济医学院临床药理研究所,武汉,430030,湖北
- 折叠
摘要
Abstract
To determine the pharmacokinetics and bioequivalence of epinastine (EPN) hydrochloride, a promising histamine H1 receptor antagonist, in healthy Chinese volunteers under fasting conditions. METHODS: EPN hydrochloride test and reference tablets were administered as a single dose on two treatment days separated by a 1-week washout period. After dosing, serial blood samples were collected for a period of 36 h, and plasma EPN hydrochloride concentrations were determined by a validated reversed-phase HPLC method and pharmacokinetic parameters were calculated with DAS software. RESULTS: Plasma concentration-time profiles were adequately described by a two-compartment open model. The compound was rapidly absorbed and cleared slowly from plasma with a half-life of approximately 10 h. The main pharmacokinetic parameters of EPN hydrochloride test and reference tablets were as follow: tmax were (2.2±0.5) and (2.0±0.4)h, Cmax were (66±16)and (68±13)μg/L, t1/2 were(10.1±1.3) and (10.4±2.4)h, AUC0-36 were (592±88) and (601±94)μg·h·L-1, respectively. The relative bioavailability of test tablets was (99±13)%. CONCLUSION: The results indicate that the two formulations of EPN hydrochloride tablets are bioequivalent in the rate and extent of absorption.关键词
盐酸依匹斯汀/高效液相色谱法/药动学/生物等效性Key words
epinastine hydrochloride/HPLC/pharmacokinetics/bioequivalence分类
医药卫生引用本文复制引用
师少军,李忠芳,陈华庭,曾繁典..组胺H1受体拮抗剂盐酸依匹斯汀片人体药动学与生物等效性研究[J].中国临床药理学与治疗学,2007,12(2):214-218,5.
