论文部分内容阅读
本文报道氧氟沙星人体不同速度恒速静滴及不同制剂口服的药代动力学及绝对生物利用度数据。10名受试者自身对照法以3.3及6.7mg/min速度静滴氧氟沙星200mg,其体内过程均符合二房室模型特征,静滴结束时最高浓度(C(max))分别为4.68±0.98及5.72±0.98mg/l(p<0.05)。其余药代动力学参数差异无显著性。表明滴速不同主要影响体内最高血浓度。另10名受试者以拉丁方次序先后口服氧氟沙星进口、国产片剂及国产胶囊200mg,其体内过程符合一室模型特征,不同制剂口服后各药代动力学参数差异无显著性。静滴与口服比较:静滴后Cmax较各制剂口服后Cmax高(P<0.01),T1/2,AUC值差异无显著性,三制剂口服绝对生物利用度分别为100.4,88.5及95.1%。结果表明口服生物利用度高,而静滴较口服达更高的血浓度。血药浓度用微生物法测定。
This article reports the pharmacokinetics and absolute bioavailability data of ofloxacin at different rates of constant velocity intravenous infusion and different preparations. 10 subjects were self-controlled by intravenous infusion of ofloxacin 200 mg at 3.3 and 6.7 mg / min. The in vivo processes were in accordance with the characteristics of two-compartment model. The highest concentration (C (max)) at the end of intravenous infusion 4.68 ± 0.98 and 5.72 ± 0.98 mg / l (p <0.05). The remaining pharmacokinetic parameters were not significantly different. Indicating that different dripping speed mainly affects the highest blood concentration in the body. The other 10 subjects in the order of the Latin side oral ofloxacin, domestic tablets and domestic capsules 200mg, in vivo process in line with the characteristics of one-compartment model, different formulations after oral pharmacokinetic parameters were no significant difference. Compared with oral administration, the Cmax after intravenous infusion was significantly higher than that after oral administration (P <0.01), but there was no significant difference between T1 / 2 and AUC. The absolute oral bioavailability of three preparations was 100.4 and 88 .5 and 95.1%. The results show that oral bioavailability is high, while intravenous infusion of higher blood concentrations. Blood concentration was determined by microbiological method.