甲磺酸帕珠沙星的人体药动学  

Pharmacokinetic study of pazufloxacin mesylate in Chinese healthy volunteers

作　　者：沈建平[1] 张银娣[1] 卓海通[1] 余俊先[1] 

机构地区：[1]南京医科大学临床药理研究所,江苏南京210029

出　　处：《中国医院药学杂志》2007年第7期880-883,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究甲磺酸帕珠沙星在健康人体内的药动学特征。方法:12名健康志愿者(男女各6名)单剂量和多剂量静脉滴注甲磺酸帕珠沙星氯化钠注射液300mg,滴注时间30min。血浆用20%高氯酸水溶液沉淀蛋白,上清液直接用高效液相色谱-荧光检测血浆中帕珠沙星药物浓度。结果:最小检测限小于0.028mg.L-1,提取回收率大于90%,日内、日间变异(RSD小于10%)。静脉滴注甲磺酸帕珠沙星在健康人体内的药动学特征用3P97程序拟合为二房室模型,其主要药动力学参数单剂量时和多剂量时的Cmax,t1/2β,AUC0-t,AUC0-∞,Vc和CL分别为(7.2±0.8)mg.L-1和(7.3±0.8)mg.L-1,(2.04±0.17)h和(2.24±0.23)h,(14.0±1.5)mg.L.h-1和(14.3±1.5)mg.L.h-1,(13.1±1.5)mg.L.h-1和(13.3±1.2)mg.L.h-1,(27.2±4.6)L和(25.3±8.8)L,(22.1±2.6)L.h-1和(23.7±2.1)L.h-1。单剂量时和多剂量间的药动学参数,除了t1/2β和MRT有性别差异外,其余无明显差异。结论:静脉滴注甲磺酸帕珠沙星后无论单剂量和多剂量的药动学参数基本一致,说明连续300mg,bid,静脉滴注5d体内无明显累积,药动学参数如t1/2β,MRT可能存在性别差异,其原因尚不清。OBJECTIVE To investigate the pharmacokinetics of pazufloxacin mesylate in Chinese healthy volunteers. METHODS Twelve healthy volunteers were received a single dose （300 mg）, then multi-doses （300 mg bid） within 30 min intravenous infusion of pazufloxacin mesylate in an open randomized cross-over study. The plasma concentration of pazufloxacin were determined by HPLC-fluorescence. RESULTS The quantitation limit was 0.028 mg·L^-1 The relative standard deviations for within-day and between-day were all 〈5%, And the recoveris were 〉90%. A good linearity was obtained from 0.028 to 14. 50 mg·L^-1. The results showed that the plasma concentration-time curve conformed to two eompatment model. Pharmaeokinetie profiles were fitted to an open two-compartment model analyzed by using 3P97. The mean pharmaeokinetic parameters of singldose and multi dose were： Cmax （7. 2 ±0. 8）mg·L^-1 and （7. 3 ± 0. 8）mg · L^-1 ;t1/2 （2. 04 ± 0. 17）h and （2. 24 ± 0. 23 ）h; AUC0-t （14.0±l.5）mg·h·L^-1 and （13.1±l.5）mg·h·L^-1;Vc（27.2±4.6）L and （25.3±8.8）L;CL （22.1±2.6）L·h^-1 and （23.7± 2. 1）L·h^-1 ,respectively. No significant diference existed between a single dose and multiple doses, but significant diffences of T1/2 and MRT occurred within man and fimale whether by a single dose or multiple doses. CONCLUSION Pazufloxacin mesylate is tolerant with a single dose or multi-doses, by intravenous infusion in Chinese healthy volunteers. No accumulation in the body was observed after 5 days administration. Significant diference in pharmacokinetic parameters such as t1/2 and MRT may be due to sex differenc.

关 键 词：甲磺酸帕珠沙星 药动学 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学]