环丙沙星的临床药物动力学研究

Clinical pharmacokinetic study on ciprofloxacin

研究健康志愿者口眼和静脉滴注环丙沙星的药物动力学，并比较不同剂量、空腹与进餐、单剂与多剂给药的体内过程。单剂空腹口服环丙沙星５００ｍｇ后，Ｃｍａｘ为３．４８ｍｇ·Ｌ－１、为３．０１ｈ、ＡＵＣ为１４．１４ｈ．ｍｇ·Ｌ－１，静脉滴注环丙沙星２００ｍｇ后Ｃｍａｘ为６．５６ｍｇ·Ｌ－１、为３．７３ｈ，口服环丙沙星绝对生物利用度为６８．８９％。单剂空腹口服２５０、５００和１０００ｍｇ环丙沙星后，Ｃｍａｘ为１．８２～７．７２ｍｇ·Ｌ－１，为２．４７～３．１５ｎ，ＡＵＣ与剂量呈比例增加，进餐与空腹口服环丙沙星５００ｍｇ后的体内过程显示进食可使该药的吸收轻度减少。与单剂口服５００ｍｇ相比，５００ｍｇ日２次×７ｄ多剂给药后的Ｃｍａｘ和ＡＵＣ均较单剂者略增高，草剂口服２５０、５００、１０００和５００ｍｇ多剂量后２４ｈ尿排出率为给药量的４７％～５５％，静滴２００ｍｇ者为７１．０６％，基于上述药动学资料，拟订了环丙沙星对各种感染的治疗方案。

A pharmacokinetic study on ciprofloxacin was carried out in normal volunteers The pharmacokinetic parameters of different dosages,fasting and non fasting state,single dose and multiple doses were compared.After a single oral dose of 500mg,mean Peak serum level was 3.48 mg·L-1.Serum ciprofloxacin half-life was 3.01h and the AUC was 14.14 h·mg· L-1.The peak serum ciprofloxacin concentration was 6.56 mg·L-1and the serum ciprofloxacin elimination half-life 3.73 h after iv infusion of 200mg.The absolute bioavail ability of oral ciprofloxacin was 68.89%.After oral dose of 250 mg,500 mg and 1000 mg,mean peak serum levels ranged from 1.82 mg·L-1 to 7.72 mg ·L-1.The elimination half lives were from2. 47 to 3.15 h,and AUC were also proportional to dose.Compared with fasting state,the absorption of ciprofloxacin was slightly decreased after meal.Comared with the single dose of ciprofloxacin 500 mg,multiple doses of the drug 500mg twice daily for 7 days produced slightly increases in the Cmax and AUC.The percentage of ciprofloxacin urinary recovery within 24 hours after single dose of 250,500,1000mg and multiple doses of 500 mg was from 47%～55%,and 71.06% of the drug was collected after ciprofloxacli 200 mg iv infusion.Based on the pharmacokinetic data obtained,a therapeutic regimen of ciprofloxacin was proposed for the treatment of various infections.