2种司帕沙星胶囊人体生物利用度与生物等效性研究

目的:比较2种司帕沙星胶囊的人体药动学参数、生物利用度,评价二者的生物等效性。方法:22名男性健康志愿者随机交叉单剂量口服200mg受试制剂或参比制剂后,应用高效液相色谱法测定血浆中司帕沙星浓度,并利用3p97程序计算药动学参数及评价二者生物等效性。结果:受试制剂与参比制剂体内药-时曲线符合二室模型,Cm ax分别为(0.85±0.23)、(0.90±0.27)μg.mL-1,tm ax分别为(5.59±2.28)、(4.95±1.17)h,AUC0~120分别为(27.92±6.09)、(29.65±8.49)μg.h.mL-1,AUC0~∞分别为(29.95±6.51)、(31.74±9.38)μg.h.mL-1。受试制剂相对生物利用度为(97.47±18.32)%。结论:受试制剂与参比制剂具有生物等效性。

Bioavailability and Bioequivalence of 2 Kinds of Sparfloxacin Capsules in Healthy Subjects

OBJECTIVE: To compare the pharmacokinetics and bioavailability between two kinds of sparfloxacin capsules and to evaluate the bioequivalence of the two preparations.METHODS: A single dose of 200mg test capsule or reference capsule of sparfloxacin was administered by randomized crossover way in 22 healthy male volunteers and the plasma concentrations of the sparfloxacin were determined by HPLC.The pharmacokinetic parameters were calculated with 3P97 pharmacokinetic program and the bioavailability was evaluated.RESULTS: The concentration-time curves of two preparations fitted two compartment model.The pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows: Cmax:(0.85± 0.23) μ g· mL-1 vs.(0.90± 0.27) μ g· mL-1;tmax:(5.59± 2.28) h and(4.95± 1.17) h;AUC0～ 120:(27.92± 6.09) μ g· h· mL-1 vs.(29.65± 8.49) μ g· h· mL-1;AUC0～ ∞ :(29.95± 6.51) μ g· h· mL-1 vs.(31.74± 9.38) μ g· h· mL-1.The relative bioavailability of test sparfloxacin capsule was(97.47± 18.32) %.CONCLUISION: The test sparfloxacin and the reference one are bioequivalent.