【摘要】 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。更多还原

【Abstract】 The pharmacokinetics and bioavailability of ofloxacin after intravenous infusion and an oral dose of 3 different preparations in man were studied. A dose of 200mg ofloxacin was administered intravenously according to cross- over randomly design in the drip rate of 3. 3 and 6.7mg per min,(ie 1. 0h and0. 5h infusion)to the same 10 healthy male voluntcers. The concentration-time curves fitted to two compartment open model. The mean peak concentrations after iv infusion were 4. 68 ± 0. 98 and 5.72±0. 98mg/l, respectively(P<0. 05). The peak concentrations were in accordance with the drip rate. No signifieant difference was found in other main pharmacokinetic parameters. An oral dose of 200 mg of foreign tablets, domestic tablets or domestic capsules were given in the self-controlled, randomized, three-way cross-over study to another 10 healthy male volunteers. The C-T curves fitted to one-compartment open model. The pharmacokinetic parameters between three preparations were not significantly different. The vaiucs of T1/2(β)and AUC between intravenous and oral dosing were not significantly different, either.The bioavailability of three oral preparations of ofloxacin were 100.4, 88. 5 and 95. 1%, respectively. These results indicate that the absorption of oral dosing was excellent and a higher concentration was achieved after intravenous infusion than oral dosing. The plasma concentrations were detected by bioassay.更多还原