人血浆中氧氟沙星的HPLC测定及其相对生物利用度

Determination of ofloxacin and its relative bioavailability in human plasma by HPLC

目的 建立人血浆中氧氟沙星测定含量的HPLC法,评价氧氟沙星片在健康人体内的药动学及生物等效性。方法 采用改进的HPLC法,测定2 0名健康受试者单剂量交叉口服4 0 0mg氧氟沙星供试片或参比片后不同时间点的血药浓度,计算其药动学参数和相对生物利用度,评价2制剂的生物等效性。结果 氧氟沙星供试片与参比片的主要药动学参数分别为:AUC0→2 4(2 7. 16 1±4 . 0 86 )、(2 5 . 32 2±3 2. 96 )mg·h·L-1;cmax(3 4.12±0 . 6 4 2 )、(3 331±0 . 6 17)mg·L-1;tmax(1 2 .93±0 . 4 6 4 )、(1 .14 3±0 . 5 72 )h;T1/ 2ke(7 .12 0±0 . 4 86 )、(7 .184±0 . 5 16 )h。2制剂主要药动学参数AUC0→2 4、cmax经对数转换后进行等效性分析,其90 %置信区间分别为10 2 . 1%～112 . 0 %、93 2 %～112. 2 %。结论 2制剂具有生物等效性。

AIM To establish a HPLC method for determination of ofloxacin and to study pharmacokinetics and bioequivalence of ofloxacin in human. METHODS The ofloxacin concentration in plasma was determined by an improved HPLC method following a single oral dose of 400 mg of tested ofloxacin tablet and reference ofloxacin tablet given respectively to 20 healthy male volunteers in an open randomized crossover design. The pharmacokinetic parameters and relative bioavailability were calculated to evaluate the bioequivalence of 2 preparations. RESULTS AUC 0-24 of tested ofloxacin tablet and reference ofloxacin tablet were(27.161±4.086)and(25.322±3.296)mg·h·L -1, c max were(3.412±0.642)and(3.331±0.617)mg·L -1,t max were(1.293±0.464)and(1.143±0.572)h,T 1/2 were(7.120±0.486)and(7.184±0.516)h,respectively. These main pharmacokinetic parameters obtained showed no statistically significant difference between 2 products.CONCLUSION:Both preparations are bioequivalent.