地克珠利肠溶微囊在家兔体内的药代动力学研究  

Pharmacokinetics of diclazuril intestines dissolving microcapsules in rabbits

作　　者：舒刚[1] 叶连娟 杨乐 张伟[1] 张莉 符华林[1] 

机构地区：[1]四川农业大学动物医学院动物疫病与人类健康四川省重点实验室,四川雅安625014

出　　处：《中国兽医科学》2013年第6期639-644,共6页Chinese Veterinary Science

基　　金：教育部"长江学者和创新团队发展计划"创新团队项目(IRT0848)

摘　　要：将8只家兔分为2组,分别单次经口灌服地克珠利原药和微囊(以地克珠利计为20mg/kg),于设定的时间点采血,经高效液相色谱法测定血药浓度,采用DAS2.0药代动力学软件进行处理,求出药代动力学参数,研究了家兔口服地克珠利肠溶微囊后的药代动力学特征。结果表明,原药与微囊的药代动力学行为均符合二室模型,Cmax分别为(58.541±0.021)和(76.738±0.073)μg/mL;T1/2Ka分别为(3.451±0.089)和(11.957±0.375)h;T1/2β分别为(26.088±0.177)和(29.523±0.219)h;AUC(0-∞)分别为(4 129.138±13.546)和(6 017.061±16.872)(μg/mL).h;MRT(0-∞)分别为(64.011±0.44)和(75.904±0.623)h。证实地克珠利微囊化后,达峰时间明显推迟,且达峰浓度升高,同时药物在兔体内平均滞留时间明显长于原药,生物利用度有了显著提高。Eight rabbits were divided into two groups,and after single oral gavage diclazuril and diclazuril microcapsule(equivalent to diclazuril 20 mg/kg),blood was collected in the set time points and determined by HPLC.The pharmacokinetic parameters were calculated by DAS2.0 pharmacokinetic software.Pharmacokinetics of diclazuril intestines dissolving microcapsules was studied in the rabbit plasma after single oral gavage.The results showed that the mean concentration-time curves of diclazuril and reference preparation were fitted to the two-compartment model with the main pharmacokinetic parameters as follows:Cmax were(58.541±0.021) μg/mL and(76.738±0.073) μg/mL respectively;T1/2Ka were(3.451±0.089) h and(11.957±0.375) h respectively;T1/2β were(26.088±0.177) h and(29.523±0.219) h respectively;AUC(0-∞) were(4 129.138±13.546)(μg/mL)·h and(6 017.061±16.872)(μg/mL)·h respectively,MRT(0-∞) were(64.011±0.44) h and(75.904±0.623) h respectively.Compared with the original drug solution,the peak time of microcapsules was significantly delayed,and the peak concentration increased,while the mean residence time of drugs in rabbits was longer than that of original drug.After diclazuril microencapsulation,the effect was longer than that of original drug,and bioavailability was significantly improved.

关 键 词：地克珠利 兔 微囊 药代动力学 

分 类 号：S859.795[农业科学—临床兽医学]