文章摘要
杨 洁,张银娣,胡 刚,卓海通,沈建平.盐酸二甲双胍缓释片人体药代动力学和相对生物利用度研究[J].南京医科大学学报,2007,(9):920~923
盐酸二甲双胍缓释片人体药代动力学和相对生物利用度研究
Pharmacokinetics and relative bioavailability of metformin hydrochloride sustained release tablet in healthy volunteers
投稿时间:2007-03-19  
DOI:10.7655
中文关键词: 二甲双胍  缓释  药代动力学  生物利用度
英文关键词: metformin  sustained release  pharmacokinetics  bioavailability
基金项目:
作者单位
杨 洁 南京医科大学临床药理研究所,江苏 南京 210029 
张银娣  
胡 刚  
卓海通  
沈建平  
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中文摘要:
      目的:研究盐酸二甲双胍缓释片(受试制剂)和普通片(参比制剂)在健康受试者体内的药代动力学过程和相对生物利用度?方法:20名男性志愿者随机自身交叉口服受试制剂和参比制剂,单剂量两制剂各服用1 000 mg,多剂量受试制剂服用1 000 mg × 1次/天,参比制剂服用500 mg × 2次/天?血浆中二甲双胍浓度使用HPLC-UV法测定?采用二房室模型进行血药浓度-时间数据分析,并计算药动学参数和相对生物利用度?结果:受试制剂和参比制剂单剂量口服后二甲双胍的Cmax分别为(1.61 ± 0.37)μg/ml和(2.47 ± 0.74)μg/ml;Tmax分别为(3.1 ± 0.6)h和(1.5 ± 0.7)h;T1/2分别为(5.1 ± 1.9)h和(2.7 ± 0.3)h;AUC0→t分别为(11.08 ± 2.88)h·μg/ml和(12.03 ± 2.63)h·μg/ml;受试制剂相对于参比制剂的生物利用度F为(92.6 ± 14.7)%?受试制剂和参比制剂多剂量口服后二甲双胍的Cmax分别为(1.60 ± 0.25)mg/ml和(1.57 ± 0.40)μg/ml ;Tmax分别为(3.2 ± 0.4)h和(1.1 ± 0.5)h;T1/2分别为(5.5 ± 3.1)h和(3.0 ± 0.6)h;AUCss分别为(13.24 ± 3.08)h·μg/ml和(6.99 ± 1.50)h·μg/ml?受试制剂的相对生物利用度F为(95.3 ± 17.5)%?结论:受试制剂和参比制剂生物等效,且具有缓释特性?
英文摘要:
      Objective:To compare pharmacokinetics and relative bioavailability of metformin hydrochloride sustained release tablet(the test preparation) with metformin common tablet(the reference preparation). Methods:Twenty male healthy volunteers were enrolled in a randomized two-way crossover design with a single-oral dose study(1 000 mg once per day for each preparation) and a multi-oral dose study(1 000 mg once per day for the test preparation and 500 mg twice per day for the reference preparation). The plasma concentrations of metformin were determined by high performance liquid chromatography(HPLC). A two-compartment model was adopted in metformin plasma concentration-time data analysis. Pharmacokinetics parameters were also calculated and bioequivalent was analyzed. Results:The main pharmacokinetic parameters of the test preparation and the reference preparation were as following:In single-dose group,Cmax was(1.61 ± 0.37) and (2.47 ± 0.74)μg/ml;Tmax(3.1 ± 0.6) and (1.5 ± 0.7)h;T1/2(5.1 ± 1.9) and(2.7 ± 0.3)h;AUC0→t(11.08 ± 2.88) and(12.03 ± 2.63)h·μg/ml and the relative bioavailability of the test preparation was(92.6 ± 14.7)%. In Multi-dose group:Cmax was(1.60 ± 0.25) and (1.57 ± 0.40)μg/ml;Tmax(3.2 ± 0.4) and (1.1 ± 0.5)h;T1/2(5.5 ± 3.1) and (3.0 ± 0.6)h;AUCss(13.24 ± 3.08) and (6.99 ± 1.50)h·μg/ml,and the relative bioavailability of the test preparation was(95.3 ± 17.5)%. Conclusion:The test preparation was bioequivalent to the reference common tablet,and showed the characteristics of sustained release.
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