格列齐特片的人体药代动力学及其相对生物利用度研究  

Pharmacokinetic and Relative Bioavailability of Gliclazide Tablets After a Single Oral Administration in Healthy Subjects

作　　者：孙建国[1] 高凌[1] 王广基[1] 吴子梅[1] 霍朝阳 闫亚新 

机构地区：[1]中国药科大学新中新药研究开发中心

出　　处：《中国药科大学学报》1998年第3期217-220,共4页Journal of China Pharmaceutical University

摘　　要：建立了ＨＰＬＣ方法测定人血浆中格列齐特的药物浓度。采用反相柱和乙腈甲醇水（１５∶４５∶４０）（ｐＨ３．５）作为流动相，格列吡嗪作为内标，检测波长为λ２２８ｎｍ。研究了１０名健康受试者随机交叉口服某药厂研制的格列齐特片剂和标准参比制剂格列齐特片８０ｍｇ后，用ＨＰＬＣ法测定血浆中药物浓度。估算某药厂研制的格列齐特片和标准参比制剂的生物半衰期分别为９．９２±３．５２ｈ和９．９７±３．４５ｈ，达峰时间分别为３．５０±０．７１ｈ和３．８５±２．２６ｈ，峰浓度分别为５．７８±０．９５μｇ／ｍｌ和６．１４±１．５６μｇ／ｍｌ。以标准参比制剂为对照，用面积法估算的某药厂研制的格列齐特片剂的相对生物利用度为１．０１±０１１。经方差分析和双单侧检验两制剂的ＡＵＣ０４８和ＡＵＣ０∞及Ｃｍａｘ，结果表明两制剂生物等效。A method was reported for the determination of gliclazide in plasma. HPLC is performed on a reversedphase column with a mobile phase of acetonitrilemehtyanolwater (pH 3.5) (15∶45∶40), at λ228 nm, using glipizide as internal standard 10 healthy subjects randomly received the gliclazide (GZ) tablets (80 mg×1) overcross. The pharmacokinetic parameters of reference and test tablets were: t1/2k 9.92±3.52 h and 9.97±3.45 h; tmax 3.50±0.71 h and 3.85±2.26 h; Cmax 5.78±0.95 μg/ml, 6.14±1.56 μg/ml respectively. The relative bioavailability of test tablet is 1.01±0.11. Pharmacokinetic parameters from comparative bioavailability trial were analyzed by ANOVA and two onesided test procedures. Results showed that the two tablets were bioequivalent.

关 键 词：格列齐特 药代动力学 生物利用度 降血糖药 

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