HPLC法测定盐酸二甲双胍肠溶胶囊及片剂的人体药代动力学及其生物利用度  

BIOAVAILABILITY OF METFORMIN HYDROCHLORIDE IN ENTERIC-SOLUBLECAPSULE FORM USING A NEW REVERSE - PHASE HIGH - PERFORMANCELIQUID CHROMATOGRAPHY ASSAY METHOD

作　　者：刘京[1] 申竹芳[1] 谢明智[1] 

机构地区：[1]中国医学科学院药物研究所,北京100050

出　　处：《中国临床药理学杂志》1994年第3期165-170,共6页The Chinese Journal of Clinical Pharmacology

摘　　要：11例健康男性志愿者,随机分为两组,分别交叉口服盐酸二甲双胍肠溶胶囊和片剂,用反相高效液相色谱法测定血浆样品,进行生物利用度研究.结果表明,口服两种剂型后药物均能很快吸收,口服1000mg盐酸二甲双胍肠溶胶囊和片剂的达峰时间(Tpeak)分别为2.28±0.38h和2.03±0.40h;峰浓度(Cmax)为2.52±0.90mg/l和2.38±0.74mg/l;口服两种剂型的吸收迟滞时间(Tlag)分别为0.47±0.11和0.35±0.32h;二者的药时曲线下面积(AUC)分别为12.74士4.28mg·h^(-1)·L^(-1)和12.70±5.03mg·h^(-1)·L^(-1);消除半衰期(T_(1/2))分别为1.74±0.49h和1.98土0.76h ;经t检验,两种剂型的药代动力学参数无显著性差异,口服盐酸二甲双肌肠溶胶囊对其片剂的相对生物利用度为100.3%.To study the bioavailability of metformin enteric - soluble capsule, a new rapid andsensitive HPLC method was established. Eleven young healthy volunteers received a single dose of metformin hydrochloride 1000 mg in enteric - soluble capsule and tablet forms. Plasma concentrations were determined by HPLC in samples collected prior to and 0.33,0.67,1,1. 5,2,3,4,6,8 and 10 hours after dosing. Experimental results showed that the concentration-time curve of two dosage forms were both fitted to one compartment model. T1/2 α of enteric - soluble casule and tablet were 0. 97±0. 28 and 0. 83±0. 37 h, T1/2 were 1.74±0.49 and 1.98±0.76h, Tpeak were 2. 28± 0. 38 and 2. 03±0. 40 h, Cmax were 2.52 ± 0.90 and 2. 38±0. 74 mg /l and AUC were 12. 74± 4. 28 and 12. 70 ±5. 03 mg · h-1 · L-1. Pharmacokinetic parameters indicated no significant differece between enteric - soluble capsule and tablet forms. The bioavailability of the two dosage forms was similar.

关 键 词：盐酸二甲双胍 肠溶胶囊 生物利用度 药代动力学 

分 类 号：R977.15[医药卫生—药品]