复方盐酸二甲双胍片的相对生物利用度与药动学研究  

Relative bioavailability of a complex Metformin plus glibenclaminde formulation in male volunteers

作　　者：刘晓颖 陈铁锋 杨敏 余细勇 林曙光 

机构地区：[1]Research Center of Medical Sciences, Guangdong Provincial People's Hospital

出　　处：《中国临床药理学与治疗学》2007年第10期1186-1187,共2页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：AIM: To investigate the relative bioavailability of the test complex Metformin hydrochloride formulations (1.25 mg glibenclaminde and 250 mg metformin hydrochloride per pellet) and evaluate its bioequivalence of the complex compared with individual drug adminstration. METHODS: A randomized, self-control, two-way crossover studies were conducted in 20 healthy volunteers[(24±4) years, (62±7) kg, weight index (21.0±1.9)]. One pellet of fest drug or two pellets of reference (commercially available, 1.25 mg glibenclaminde per pellet and 250 mg Metformin hydrochloride per pellet respectively) were orally administrated and the alternative ones were administrated after a washout time of one week. Serum samples were collected before and after administration within 24 hours. Metformin and glibenclaminde concentrations in serum were measured by HPLC. Pharmacokinetic parameters were analyzed by 3P97 computer program. Cmax, tmax were calculated by raw data, AUC(0-last) was also calculated by the trapezoidal summation method. T-test was applied for the all pharmacokinetic parameters of the test and reference drug, the bioequivalence of Cmax, tmax and AUC(0-last) was analyzed by DAS 1.0 computer program package. RESULTS: The tmax, Cmax, t1/2Ka, t1/2Ke of glibenclaminde were as follows(test vs reference): (2.9±0.6) vs (2.8±0.6) h, (112±26) vs (117±28) μg/L, (1.6±0.4) vs (1.5±0.5) h, (1.6±0.4) vs (1.5±0.5) h, and AUC(0-last), AUC0-∝ were (607±109) vs (608±124) μg·L-1·h, (663±124) vs (655±127) mg·L-1·h, respectively. All parameters of mertiform were: tmax (2.0±0.8) vs (2.0±1.2) h, Cmax (1.7±0.4) vs (1.7±0.5) μg/L, t1/2Ka (0.5±0.5) vs (0.6±0.5) h, t1/2Ke (3.2±1.5) vs (2.8±0.9) h, respectively, and AUC(0-last) (8.4±2.4) vs (8.8±2.6), AUC0-∝ (8.9±2.4) vs (9.3±2.7) mg·L-1·h, respectively. There was no significant difference of all parameters between the test drug and the reference (P>0.05) which indicated the pharmacokinetic property of these two were similar. The relative bioavailability of gliAIM： To investigate the relative bioavailability of the test complex Metformin hydrochloride formulations （1.25 mg glibenclaminde and 250 mg metformin hydrochloride per pellet） and evaluate its bioequivalenee of the complex compared with individual drug adminstration. METHODS： A randomized, self-control, two-way crossover studies were conducted in 20 healthy vohmteers [ （24 ±4） years, （62±7） kg, weight index （21.0± 1.9）]. One pellet of lest drug or two pellets of reference （commercially available, 1.25 mg glibenclaminde per pellet and 250 mg Metformin hydrochloride per pellet respectively） were orally administrated and the alternative ones were administrated after a washout time of one week. Serum samples were collated before and after administration within 24 hours. Metformin and glibenclaminde concentrations in serum were measured by HPLC. Pharmacokinetic parameters were analyzed by 3P97 computer program. Cmax, tmax were calculated by raw data, AUC（0-last） was also calculated by the trapezoidal summation method. T- test was applied for the all pharmacokinetic parameters of the test and reference drug, the bioequivalence of Cmax, tmax and AUC（0-last） was analyzed by DAS 1.0 computer program package.

关 键 词：复方盐酸二甲双胍片 相对生物利用度 药物代谢动力学 男性 

分 类 号：R969.1[医药卫生—药理学]