环丙沙星的人体药代动力学研究

PHARMACOKINETICS OF CIPROFLOXACIN IN HEALTHY ADULT VOLUNTEERS

健康志愿者8名,静脉恒速滴注乳酸环丙沙星200mg(30min)后,其体内过程符合二室开放模型,主要药动学参数分别为:滴注完时浓度Co为4.14±0.82μg/ml,消除相半衰期t1/2为3.35± 0.30h,AUC为7.225±0.814μg·h/ml。另外8名志愿者分别口服500mg盐酸环丙沙星胶囊或片剂后,其体内过程符合一室模型,主要药动学参数分别为;C_(max)为2.47± 0.33及2.28±0.30μg/ml;t1/2为3.13±0.44及3.51±0.35h,Tp为1.53±0.36及1.28±0.31h;AUC为17.08±2.17及15.91±2.01μg·h/ml。绝对生物利用度为78.8％及72.7％。血浆药物浓度采用微生物法测定。

A 200mg dose of ciprofloxacin (CPF) was given as a 30 minute intravenous infusion to each of eight healthy volunteers. The plasma course of CPF could be best discribed by an open two-compartment model. Its main parameters were as follows:Co = 4.14± 0.82μg/ml; t_(1/2)(β) = 3.35±0.30h, AUC = 7.225 ± 0.814μg·h/ml. 500mg dose of CPF capsules or tablets were randomly cross-over given to another group of 8 healthy volunteers. The concentrationtime curve of CPF fitted in with an one-compartment model, and the main parameters of the two preparations were as follows. Cmax were 2.47 ± 0.33 and 2.28±0.30μg/ml; t_(1/2) were 3.13±0.44 and 3.5±0.35h; Tp were 1.53 ± 0.36 and 1.28±0.3lh; AUC were 17.08±2.17 and 15.91±2.01μg·h/ml; F(compared with intravenous infusion)were 78.8% and 72.7%, respectively. The plasma levels were detected with a bioassay.