100g/kg磷酸替米考星可溶性粉和100g/L替米考星溶液在鸡体内的比较药动学

Comparative pharmacokinetics of 100g/kg tilmicosin phosphate powder and 100g/L tilmicosin solution by oral administration in chicken

采用单剂量平行随机对照试验设计,将24只健康肉用商品鸡随机分成2组,每组公母各半。分别单剂量(12mg/kg,根据体重以替米考星计)经口内服100g/kg磷酸替米考星可溶性粉和100g/L替米考星溶液(对照品)。给药后按预定时间采集血样,血浆中替米考星的质量浓度采用HPLC紫外检测器进行定量分析。对实测的血药浓度-时间数据采用Winnonlin5.2药动学分析软件计算药代动力学参数,对100g/kg磷酸替米考星可溶性粉和100g/L替米考星溶液在鸡体内的药动学参数进行比较研究。结果显示,100g/L替米考星溶液对照品单剂量内服后,平均消除半衰期(t1/2β)为17.316h,达峰时间(tmax)和峰值浓度(Cmax)分别为1.083h和0.399μg/mL,平均药时曲线下面积(AUC)为1.891h·μg/mL,平均滞留时间(MRT)为8.286h;100g/kg磷酸替米考星可溶性粉单剂量内服后,t1/2β为13.207h,tmax和Cmax分别为1.333h和0.372μg/mL,AUC为1.813h·μg/mL,MRT为7.612h。结果表明,100g/kg磷酸替米考星可溶性粉和100g/L替米考星溶液口服给药在鸡胃肠道内吸收迅速,消除较慢。两者经口给药的主要药动学参数之间均无显著差异(P>0.05)。

A single dose of parallel test design was used.Twenty-four healthy broiler chickens with consistent weight were randomly divided into two equal groups,half of male and half of female in each group.The pharmacokinetics of the test substance 100g/kg tilmicosin phosphate powder and the reference substance 100g/L tilmicosin solution were studied in chickens by oral route(12mg/kg according to body weight).The plasma concentrations of tilmicosin were determined by high-performance liquid chromatographic methods,and pharmacokinetic parameters were calculated by kinetic program Winnonlin 5.2.The means of t1/2β,tmax,Cmax,AUCand MRT of the 100g/L tilmicosin solution were 17.316 h,1.083 h,0.399μg/mL,1.891h·μg/mL and 8.286 h,respectively.And the means of t1/2β,tmax,Cmax,AUCand MRTof 100g/kg tilmicosin phosphate powder were 13.207 h,1.333 h,0.372μg/mL,1.813h·μg/mL and 7.612 h,respectively.Compared with the reference substance,there is no difference in the test substance on AUC,tmax,MRT,t1/2βand Cmax(P>0.05).