两种长效曲普瑞林注射剂在Beagle犬体内的药动学研究  

Studies on pharmacokinetics of two long-acting triptorelin injections in Beagle dogs

作　　者：李周[1] 丁存刚[1] 周臻[1] 葛庆华[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《世界临床药物》2013年第4期212-216,共5页World Clinical Drug

摘　　要：目的研究两种长效曲普瑞林注射剂(达必佳3.75 mg及达菲林3.75 mg)在Beagle犬体内的药动学参数。方法 10条健康雄性Beagle犬随机分成2组,肌注达必佳或达菲林,采用经验证的LC-MS/MS法测定Beagle犬血浆中曲普瑞林浓度。使用DAS 3.2.2软件计算药动学参数。结果达必佳和达菲林主要药动学参数Cmax为(11.95±2.127)与(27.93±8.752)ng/mL、Tmax为(1.2±0.4)与(0.7±0.3)h、T1/2为(244.7±99.25)与(239.6±87.50)h、AUC(0-t)为(758.8±111.9)与(492.3±125.9)ng h mL-1、AUC(0-)为(778.9±101.3)与(515.6±125.3)ng h mL-1。结论可采用LC-MS/MS法检测达必佳和达菲林的Beagle犬体内药动学参数。两药在Cmax、AUC(0-t)与AUC(0-)有差异,但两者血药浓度维持在最低定量限(LLOQ)以上的时间均达到28 d以上。Objective To study pharmacokinetics of two long-acting triptorelin injections(Decapeptyl 3.75 mg and Diphereline 3.75 mg) in male Beagle dogs.Methods A tatal of 10 healthy male Beagle dogs were randomly divided into two groups.The plasma concentration of triptorelin was determained by a validated LC-MS/MS method after intramuscular injection of the two injections.The pharmacokinetic parameters were calculated by DAS 3.2.2.Results The mean pharmacokinetic parameters were as follows: Cmax(11.95±2.127) and(27.93±8.752) ng/mL,Tmax(1.2±0.4) and(0.7 ±0.3) h,T1/2(244.7±99.25) and(239.6±87.50) h,AUC(0-t)(758.8±111.9) and(492.3±125.9)ng h mL-1,AUC(0-)(778.9± 101.3)and(515.6±125.3) ng h mL-1,respectively for Decapeptyl and Diphereline.Conclusion The Cmax、AUC(0-) and AUC(0-t)of Diphereline and Decapeptyl in Beagle dogs were different significantly.These two injections could keep the plasma concentration above the LLOQ for more than 28 days.

关 键 词：曲普瑞林 达必佳 达菲林 微球 微囊 长效注射剂 药动学 

分 类 号：R977.1+2[医药卫生—药品] R965[医药卫生—药学]