盐酸乙哌立松片在健康人体内的药代动力学及生物等效性  

Pharmacokinetics and bioequivalence of eperisone hydrochloride tablet in healthy subjects

作　　者：魏欣[1] 丁黎[1] 高家敏[1] 李君[1] 张胜强[1] 沈建平[2] 张银娣[2] 

机构地区：[1]中国药科大学药物分析教研室,江苏南京210009 [2]南京医科大学基础医学院临床药理研究所,江苏南京210029

出　　处：《药学学报》2004年第4期309-311,共3页Acta Pharmaceutica Sinica

摘　　要：AimTo develop a HPLC-ESI-MS assay for determination of eperisone hydrochloride in human plasma and investigate the pharmacokinetics and bioequivalence of two epe risone hydrochloride tablets in human. MethodsBuflomedil hydrochloride was used as the internal standard. After alkalized with saturated sodium bicarbonate solution, plasma was extracted with diethylether- cyclohexane (1∶1) and separated using HPLC on a reversed-phase C 18 colum n with a mobile phase of 10 mmol·L -1 ammonium acetate buffer solution (adjusted to pH 3 88 with acetic acid)-methanol (20∶80). HPLC-ESI-MS was p erformed in the selected ion monitoring (SIM) mode using target ions at m/z 260 for eperisone and m/z 308 for the internal standard. A randomiz ed crossover design was performed in 20 healthy volunteers. In the two study per iods, a single 100 mg dose of each tablet was administered to each volunteer. ResultsCalibration curve was linear over the range of 0 02-20 μg·L -1 . The limit of quantification for eperisone hydrochloride in plasma was 0 02 μg·L -1 . The main pharmacokinetics parameters T 1/2 , T max and C max were (2 7±0 4) h, (1 1±0 5) h and (2 8±2 8) μg·L -1 for the reference tablet; (2 8±0 5) h, (1 1±0 4) h and (3±4) μg·L -1 for the test tablet, respectively. The relative bioavalabilit y of the test tablet was (101±13)%. ConclusionThe assay was proved to be sensitive, accurate and convenient. The two formulati ons were bioequivalent.AimTo develop a HPLC-ESI-MS assay for determination of eperisone hydrochloride in human plasma and investigate the pharmacokinetics and bioequivalence of two epe risone hydrochloride tablets in human. MethodsBuflomedil hydrochloride was used as the internal standard. After alkalized with saturated sodium bicarbonate solution, plasma was extracted with diethylether- cyclohexane (1∶1) and separated using HPLC on a reversed-phase C 18 colum n with a mobile phase of 10 mmol·L -1 ammonium acetate buffer solution (adjusted to pH 3 88 with acetic acid)-methanol (20∶80). HPLC-ESI-MS was p erformed in the selected ion monitoring (SIM) mode using target ions at m/z 260 for eperisone and m/z 308 for the internal standard. A randomiz ed crossover design was performed in 20 healthy volunteers. In the two study per iods, a single 100 mg dose of each tablet was administered to each volunteer. ResultsCalibration curve was linear over the range of 0 02-20 μg·L -1 . The limit of quantification for eperisone hydrochloride in plasma was 0 02 μg·L -1 . The main pharmacokinetics parameters T 1/2 , T max and C max were (2 7±0 4) h, (1 1±0 5) h and (2 8±2 8) μg·L -1 for the reference tablet; (2 8±0 5) h, (1 1±0 4) h and (3±4) μg·L -1 for the test tablet, respectively. The relative bioavalabilit y of the test tablet was (101±13)%. ConclusionThe assay was proved to be sensitive, accurate and convenient. The two formulati ons were bioequivalent.

关 键 词：盐酸乙哌立松片 健康人体 药代动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]