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. MethodsBuflomedi...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.展开更多
目的 探讨盐酸乙哌立松治疗痉挛性脑瘫患儿的临床效果。方法 选取84例痉挛性脑瘫患儿作为研究对象,按照随机数字表法分为Ⅰ组(盐酸乙哌立松治疗组)、Ⅱ组(盐酸苯海索治疗组)、Ⅲ组(氯硝西泮治疗组),对比各组治疗效果、肌张力缓解情况以...目的 探讨盐酸乙哌立松治疗痉挛性脑瘫患儿的临床效果。方法 选取84例痉挛性脑瘫患儿作为研究对象,按照随机数字表法分为Ⅰ组(盐酸乙哌立松治疗组)、Ⅱ组(盐酸苯海索治疗组)、Ⅲ组(氯硝西泮治疗组),对比各组治疗效果、肌张力缓解情况以及药物不良反应发生率。结果 Ⅰ组治疗效果显著优于Ⅱ组和Ⅲ组( P <0.05);治疗前, 3组肌张力水平无显著差异( P >0.05),治疗后, 3组患儿肌张力均有所好转,但Ⅰ组和Ⅲ组的肌张力评分显著低于Ⅱ组( P <0.05);治疗期间,Ⅲ组不良反应发生率最高,Ⅰ组不良反应发生率最低,组间差异显著( P <0.05)。结论 采用盐酸乙哌立松治疗小儿痉挛性脑性瘫痪效果佳,不仅能有效改善患儿肌张力障碍,而且具有较高的安全性。展开更多
文摘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.
文摘目的 探讨盐酸乙哌立松治疗痉挛性脑瘫患儿的临床效果。方法 选取84例痉挛性脑瘫患儿作为研究对象,按照随机数字表法分为Ⅰ组(盐酸乙哌立松治疗组)、Ⅱ组(盐酸苯海索治疗组)、Ⅲ组(氯硝西泮治疗组),对比各组治疗效果、肌张力缓解情况以及药物不良反应发生率。结果 Ⅰ组治疗效果显著优于Ⅱ组和Ⅲ组( P <0.05);治疗前, 3组肌张力水平无显著差异( P >0.05),治疗后, 3组患儿肌张力均有所好转,但Ⅰ组和Ⅲ组的肌张力评分显著低于Ⅱ组( P <0.05);治疗期间,Ⅲ组不良反应发生率最高,Ⅰ组不良反应发生率最低,组间差异显著( P <0.05)。结论 采用盐酸乙哌立松治疗小儿痉挛性脑性瘫痪效果佳,不仅能有效改善患儿肌张力障碍,而且具有较高的安全性。
