中国药物警戒 ›› 2011, Vol. 8 ›› Issue (7): 385-387.

• 基础及临床研究 •    下一篇

三种左奥硝唑制剂在健康人体的生物利用度与生物等效性分析

王晓娟1, 袁洪2, 宋敏2, 谭鸿毅2, 黄志军2, 刘畅2, 黄原原2, 付志敏2, 阳国平2   

  1. 1.湖南食品药品职业学院,湖南 长沙 410000;
    2.中南大学湘雅三医院,湖南 长沙 410000
  • 收稿日期:2011-02-21 出版日期:2011-07-10 发布日期:2015-07-13
  • 作者简介:王晓娟,女,高级讲师,药品相关专业知识教学以及剂型与疗效的研究。

The Bioavailability and Bioequivalence Analysis of Three Levornidazole Preparations in Healthy Volunteers

WANG XIAO-juan1, YUAN Hong2, SONG Min2, TAN Hong-yi2, HUANG Zhi-jun2, LIU Chang2, HUANG Yuan-yuan2, FU Zhi-min2, YANG Guo-ping2   

  1. 1.HuNan Food and Drug Vocational College, Hunan Changsha, 410000, China;
    2.The Third Xiangya Hospital of Central South University, Hunan Changsha 410000, China
  • Received:2011-02-21 Online:2011-07-10 Published:2015-07-13

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摘要： 目的 比较3种国产左奥硝唑制剂在健康人体内的药代动力学,并评价3种制剂的生物等效性。方法 24名健康男性志愿者三交叉单剂量口服受试制剂左奥硝唑分散片、胶囊和参比制剂左奥硝唑片500mg后,用HPLC-UV法测定血药浓度,用DAS Ver 2.1计算其药代动力学参数并评价三者的生物等效性。结果 受试制剂左奥硝唑分散片、胶囊和参比制剂左奥硝唑片的主要药代动力学参数：Cmax分别为（10.6±3.5）、（10.4±3.7）和（11.1±3.3）mg·L-1;tmax分别为（0.76±0.70）、（1.35±0.80）和（0.92±0.84）h;t1/2分别为（13.2±1.4）、（12.9±1.7）和（12.3±1.9）h;AUC0→48分别为（140.7 31.3）、（149.5±28.5）和（143.2±37.2）mg·L-1·h;AUC0→∞分别为（152.6±33.4）、（162.0±31.8）和（153.7±30.1）mg·L-1·h。以AUC0→48、AUC0→∞作为评价依据,受试制剂对参比制剂的相对生物利用度F分别为（98.3±12.0）%、（99.5 12.1）%和（104.9±9.5）%、（106.0±10.5）%。结论 左奥硝唑分散片、胶囊和参比制剂左奥硝唑片三种制剂生物等效。

关键词: 左奥硝唑, 药代动力学, 生物等效性, 高效液相色谱-紫外检测器

Abstract: Objective To study the pharmacokinetics and bioequivalence of three Levornidazole preparations in healthy volunteers. Methods The study was conducted in twenty-four healthy male volunteers. After receiving a single dose of 500 mg Levornidazole dispersible tablet, Levornidazole capsule and Levornidazole tablet(Reference) in three crossed way, the drug concentrations in plasma were determined by HPLC-UV method, the pharmacokinetic parameters and the statistical analysis of bioequivalence were obtained by DAS Ver 2.1. Results The pharmacokinetic parameters for Levornidazole dispersible tablet, Levornidazole capsule and the reference Levornidazole tablet were as follows: Cmax were (10.6±3.5), (10.4±3.7) and (11.1±3.3)mg·L-1, tmax were(0.76±0.70), (1.35±0.80) and (0.92±0.84)h, t1/2 were(13.2±1.4), (12.9±1.7) and (12.3±1.9)h, AUC0→48 were(140.7±31.3 ), (149.5±28.5) and (143.2±37.2)mg·L-1·h, AUC0→∞ were (152.6±33.4), (162.0±31.8) and (153.7±30.1)mg·L-1·h. By evaluating AUC0→48 and AUC0→∞, the relative bioavailability of Levornidazole dispersible tablet and capsule to the reference were (98.3±12.0)%, (99.5±12.1)% and (104.9±9.5)%, (106.0±10.5)% respectively. Conclusion Levornidazole dispersible tablet, capsule and the reference tablets were bioequivalent.

Key words: Levornidazole, pharmacokinetics, bioequivalence, HPLC-UV

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