国产司帕沙星两种制剂的生物等效性研究

Bioequivalent study of two formulations of domestic sparfloxacin

12例健康男性志愿受试者采用随机交叉给药方案 ,分别单剂口服国产司帕沙星颗粒剂和胶囊剂40 0 mg,进行生物等效性研究。用 RP- HPL C法测定血清中司帕沙星浓度 ,试验结果表明 :血药浓度 -时间数据经 3p97程序自动拟合 ,符合一室模型。颗粒剂和胶囊剂的达峰时间分别为 (4 .79± 0 .40 )和 (4 .79± 0 .33) h,峰浓度分别为 (1.5 5± 0 .35 )和 (1.5 4± 0 .46 ) mg/L,AUC0 - 96 分别为 (5 5 .31± 11.89)和 (5 2 .5 2± 13.6 0 ) (mg·h) /L。以上药代动力学参数经方差分析无显著性差异 (P>0 .0 5 )和双单侧 t检验 (P<0 .0 5 ) ,两种制剂具有生物等效性。司帕沙星颗粒剂对胶囊剂的相对生物利用度为 10 6 .7%。

The pharmacokinetics of sparfloxacin granule and capsule were determined following a single oral dose of 400mg given to 12 healthy volunteers in an open randomized crossover study. The sparfloxacin concentrations in serum were measured by RP HPLC. The pharmacokinetic parameters were calculated on the basis of one compartment model by using 3P97 program. T max of domestic sparfloxacin granule and capsule were (4.79±0.40) and (4.79±0.33)h; C max were (1.55±0.35) and (1.54±0.46)mg/L; AUC 0-96 were (55.31±11.89) and (52.52±13.60)(mg·h)/L respectively. The pharmacokinetic parameters obtained from our studies showed no significant differences between two products. The relative bioavailability of sparfloxacin granule to capsule was 106.7%, so it demonstrated that both formulations were bioequivalent.