环丙沙星在猪体内的生物利用度及药物动力学

Bioavailability and Pharmacokinetics of Ciprofloxacin in Pigs

18 头健康长白×大白×杜洛克杂交猪,分3 组,每组6 头,按5 m g/kg 的剂量进行了静注、肌注及内服环丙沙星的药动学研究。高效液相色谱法测定血浆中药物的质量浓度,MCPKP药代动力学程序处理药时数据。静注给药时,环丙沙星体内分布快且广泛,消除较慢,t1/2α为(0.35±0.19) h,t1/2β为(3.15±0.57) h,Vd(area)为(3.24±0.51) L/kg,ClB 为(0.73±0.15) L/(kg·h- 1 )。肌注和内服给药时,环丙沙星均吸收较快,但内服吸收速度和程度均不及肌注给药,t1/2ka 分别为(0.23±0.15)、(0.38±0 .21) h,tm ax 分别为(0.63±0.31)、(1.39±0.39) h,Cm ax 分别为(1.31±0.34)、(0.60±0.14) m g/L,生物利用度(F)分别为(77.96±5.89)% 、(51.58±5.69)% 。本研究发现,环丙沙星肌注和内服给药的消除半衰期与静注给药相似,分别为(3.45±0.66)、(3.32±0.96) h,与在其他哺乳动物的动力学特征有所不同。

The pharmacokinetics of ciprofloxacin following intravenous(IV), intramuscular(IM) and oral(PO) administration of 5.0 mg/kg body weight have been investigated in healthy pigs. The plasma concentrations were determined by HPLC. Following IV administration, ciprofloxacin was well distributed and slowly eliminated. The main pharmacokinetic parameters were as follows: t 1/2α , (0.35±0.19) h; t 1/2β , (3.15±0.57) h; V d(area) , (3.24±0.51) L/kg; Cl B , (0.73±0.15) L/(kg·h -1 ). Ciprofloxacin was rapidly and well absorbed after IM administration, with t 1/2ka of (0.23± 0.15 ) h, t max of (0.63±0.31) h, C max of (1.31±0.34) mg/L. The bioavailability(F) was (77.96± 5.89 )%. For PO administration, the absorption of ciprofloxacin in pigs was also fast, with t 1/2ka of ( 0.38 ± 0.21 ) h, t max of (1.39±0.39) h, C max of (0.60±0.14) mg/L and F was (51.58±5.69)%. Mean elimination half life was (3.45±0.66) h for IM administration and (3.32±0.96) h for PO administration, which showed no difference with that after IV administration.