高效液相色谱法研究人体内盐酸二甲双胍药动学和生物等效性  

Pharmacokinetics and bioequivalence of metformin hydrochloride tablets in health volunteers

作　　者：袭荣刚[1] 王晓波[1] 石焱[1] 李忠亮[1] 隋淼[1] 宋晓楠[1] 

机构地区：[1]解放军第210医院国家药物临床试验机构,大连116021

出　　处：《中国新药杂志》2009年第3期230-233,共4页Chinese Journal of New Drugs

摘　　要：目的：研究健康人口服盐酸二甲双胍片后的药动学和生物等效性。方法：20个健康受试者采用随机分组自身交叉对照试验设计，口服盐酸二甲双胍片0．5g后用HPLC法测定血浆中盐酸二甲双胍浓度，以DAS软件计算其药动学参数和评价生物等效性。结果：在选定的色谱条件下盐酸二甲双胍与内标及血浆杂质分离良好，在24～2000ng·mL^-1范围内线性良好。相对回收率大于91．31％，日内和日间RSD小于9．29％。盐酸二甲双胍片受试制剂和参比制剂的主要药动学参数：Tmax分别为（2．25±0．53）和（2．30±0．44）h，Cmax分别为（1498．9±207．9）和（1540．1±209．3）ng·mL；t1／2分别为（3．82±1．40）和（3．90±1．16）h；AUC0-t分别为（8202±1624）和（7979±1650）ng·h·mL^-1；用面积法（AUC0～t）估算的盐酸二甲双胍片相对生物利用度为（103．2±9．7）％。结论：用HPLC法测定血浆中盐酸二甲双胍浓度，杂质无干扰，定量限低，重复性好，准确度高。2制剂生物等效。Objective： To study the pharmacokinetics and bioequivalence of mefformin hydrochloride tablets in health volunteers. Methods： In 20 volunteers, mefformin hydrochloride tablets were orally administered in a 2-way crossover design. The concentration of mefformin hydrochloride in plasma was determined by HPLC; the pharmacokinetie parameters were calculated using DAS software. Results： The calibration curve was linear in the range from 24 to 2 000 ng-mL^-1. The relative recovery was more than 91.31%. The intra- and inter-day RSDs were less than 9.29%. The main pharmaeokinetic parameters T1/2, C T and AUC0-t for the test tablet were （3.82±1.40） h, （1498.9±207.9） ng·mL^-1, （2.25±0.53） hand （8202±1 624） ng·h·mL^-1, respectively. Those for the reference tablet were （3.90±1.16） h, （1540.1±209.3） ng·mL^-1, （2.30±0.44） h and （7 979 ± 1 650） ng·h·mL^-1, respectively. The relative bioavailability of the test tablet was （103.2% ±9.7）%. Conclusion ： The HPLC method is sensitive, accurate and convenient for determination of mettbrmin hydrochloride in plasma. The reference and test tablets are bioequivalent.

关 键 词：盐酸二甲双胍片 高效液相色谱 药动学 生物等效性 

分 类 号：R969.1[医药卫生—药理学] R977.15[医药卫生—药学]