甲磺酸加替沙星片在健康志愿者体内的药动学

Pharmacokinetics of gatifloxacin mesylate tablets in healthy volunteers

目的 :研究健康志愿者口服甲磺酸加替沙星片后的药动学特征 ,为临床安全、合理用药提供参考依据。方法 :18名健康男性单剂量口服甲磺酸加替沙星片 4 0 0mg ,以高效液相色谱法测定服药后 2 4h内的血药浓度 ,计算其药动学参数。结果 :甲磺酸加替沙星片在健康人体内的处置符合一级吸收的一室代谢模型 ,主要药动学参数Tmax,Cmax,T12 β,AUC( 0 2 4 ) 分别为 :(1.5±s 0 .4 )h ,(3.4± 1.0 )mg·L- 1,(6 .6± 1.0 )h ,(33± 10 )mg·h·L- 1。结论 :甲磺酸加替沙星在人体内的药动学特征与文献报道的盐酸加替沙星相似 ,口服吸收快 ,生物利用度高、体内平均滞留时间长 ,且存在个体差异。

AIM: To study the pharmocokinetics characteristics of gatifloxacin mesylate tablets in healthy volunteers in order to providing the verification of clinical safety and reasonable application of them. METHODS: Eighteen male subjects received a single oral dose of 400 mg of gatifloxacin mesylate. The plasma concentration of gatifloxacin mesylate was determined by HPLC method. RESULTS: The main pharmacokinetics parameters of gatifloxacin mesylate were as follows: T_ max, C_ max, T__ 12β, AUC_ (0-24) were (1.5±s 0.4) h, (3.4±1.0) mg·L -1,(6.6±1.0) h, (33±10) mg·h·L -1, respectively. CONCLUSION: The pharmacokinetics of gatifloxacin mesylate tablets are similar to those of gatifloxacin hydrochloride. It has advantage of quick absorption, high bioavailability and long mean retention time and inter-individual variability.