注射用头孢曲松钠动物体内药代动力学和相对生物利用度研究  

Study on the pharmacokinetics of ceftriaxone sodium for injection and its relative bioavailability in SD rat and cynomolgus monkey

作　　者：臧卫军[1] 高颖慧[1] 向志雄[1] 张乐多[1] 

机构地区：[1]上海医药集团股份有限公司中央研究院,上海201203

出　　处：《上海医药》2016年第21期70-75,共6页Shanghai Medical & Pharmaceutical Journal

摘　　要：目的:对比上海新亚药业与罗氏制药生产的两种注射用头孢曲松钠产品(简称为新亚和罗氏芬)在SD大鼠和食蟹猴的药代动力学性质差异。方法:实验动物在静脉注射和肌肉注射后,采用UPLC-MS/MS测定血浆中头孢曲松浓度,通过Kinetica 5.1计算药代动力学参数。结果:静脉注射后,新亚和罗氏芬在SD大鼠体内的AUC0-t分别为483.4±179.5μg·h/ml、542.4±166.0μg·h/ml、在食蟹猴体内分别为1 703.6±564.4μg·h/ml、1 811.7±601.7μg·h/ml。肌肉注射后,新亚和罗氏芬在SD大鼠体内的AUC0-t分别为412.6±153.4μg·h/ml、451.7±147.1μg·h/ml、在食蟹猴体内分别为1 454.9±592.9μg·h/ml、1 367.3±772.0μg·h/ml。相对于罗氏芬,新亚在SD大鼠体内静脉和肌肉注射的相对生物利用度分别为(89.1±98.6)%、(91.3±55.4)%、在食蟹猴体内分别为(94.0±9.6)%、(106.4±103.0)%。结论:两种制剂在大鼠和食蟹猴上的药代动力学特点类似,未见显著差异。Objective： To compare pharmacokinetic properties of two kinds ofceflriaxone sodium which were produced by Shanghai New Asia pharmaceutical and Roche pharmaceuticals （New Asia and Rocephin for short）. Methods： SD rats and cynomolgus monkeys were intravenously or intramuscularly injected with one of the two preparations, respectively. Their concentrations in plasma were determined by UPLC-MS/MS. The pharmacokinetic parameters were calculated by Kinetica 5.1. Results： The areas under the curve （AUC0.,） of New Asia and Rocephin were 483.4±179.5 and 542.4±166.0μg·h/ml in SD rats and 1 703.6±564.4 and 1 811.7±601.7μg·h/ml in cynomolgus monkeys via intravenous injection and 412.6±153.4 and 451.7±147.1μg·h/ml in SD rats and 1 454.9±592.9 and 1 367.3±772.0μg·h/ml in cynomolgus monkeys via intramuscular injection, respectively. The relative bioavailability of New Asia was （89.1±98.6）% and （94.0±9.6）% in SD rat and cynomolgns monkeys via intravenous injection and （91.3±55.4）% and （106.4±103.0）% in SD rat and cynomolgus monkeys via intramuscular injection, respectively. Conclusion： The pharmacokinetic properties of both preparations in SD rats and cynomolgns monkeys are similar and the significant differences are not found.

关 键 词：注射用头孢曲松钠 药代动力学 相对生物利用度 

分 类 号：R965[医药卫生—药理学]