注射用哌拉西林钠/舒巴坦钠(8∶1)在比格犬体内的药代动力学  

Pharmacokinetics of injective piperacillin sodium /sulbactam sodium( 8∶ 1) in beagle dogs

作　　者：王利杰[1] 金鑫[1] 王鹏[1] 

机构地区：[1]沈阳华泰药物研究有限公司,沈阳110015

出　　处：《中国临床药理学杂志》2013年第10期770-773,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究注射用哌拉西林钠/舒巴坦钠(8∶1)中哌拉西林钠及舒巴坦钠在比格犬体内的药代动力学。方法三周期交叉试验设计,6只比格犬静脉滴注给予受试和参比药物(按哌拉西林钠计143 mg·kg-1,按舒巴坦钠计为18mg·kg-1)后,用HPLC-MS法同时测定血浆中哌拉西林和舒巴坦的浓度,用DAS2.0软件计算药代动力学参数。结果静脉滴注给药后血浆中受试和参比药物的哌拉西林的c max分别为(710.28±148.44),(743.70±212.02)μg·mL-1;t1/2分别为(0.60±0.23),(0.62±0.22)h;AUC0-t分别为(360.01±28.19),(377.64±107.36)μg·h·mL-1;以AUC0-t计算,哌拉西林的相对生物利用度平均为(99.6±18.0)%;血浆中的舒巴坦的c max分别为(70.95±14.59),(88.34±16.31)μg·mL-1;t1/2分别为(0.84±0.27),(0.71±0.09)h;AUC0-t分别为(59.59±4.52),(55.68±7.57)μg·h·mL-1;以AUC0-t计算,舒巴坦的相对生物利用度平均为(108.4±14.2)%。结论本方法准确可靠,操作简便,适用于药代动力学研究。Objective To study pharmacokinetics of injective piperacillin sodium/sulbactam sodium（8：1 ） in beagle dogs. Methods In this experiment, three period crossover design. A single intravenous at a dose of piperacillin sodium 143 mg·kg^-1 and sulbactam sodium 18 mg·kg^-1 was given to 6 healthy beagle dogs in order to study pharmacokinetics of injective piperacillin sodium/sulbactam sodium （8：1 ） in plasma. Concentration was determined by HPLC -MS method. DAS 2. 0 software was used for pharmacokinetic parameters. Results The main pharmacokinetic parameters of test and referent piperacillin sodium were as followings： Cmax were （710.28 ± 148.44）, （743.70 ± 212.02）μg·mL^-1; t1/2 were （0.60±0.23）, （0.62±0.22） h; AUC0-t, were （360.01 ±28.19）, （377.64 ± 107.36） μg·h·mL^-1; the relative bioavailability of Piperacillin sodium is （99. 6 ± 18） %. The main pharmacokinetic parameters of sulbactam sodium were as followings： Cmax were （70. 95 ± 14. 59 ）, （88.34±16.31）μg·mL^-1; t1/2 were （0.84±0.27）, （0.71 ±0.09） h; AUC0-t were （59. 59 ±4. 52）, （55. 68 ±7. 57）μg·h·mL^-1 ; the relative bioavailability of Sulbactam sodium is（ 108. 4 ± 14. 2） %. Conclusion This HPLC - MS method is simple, sensitive and accurate. It is suitable for pharmacokinetic study of the drugs.

关 键 词：哌拉西林钠 舒巴坦钠 高效液相色谱-质谱 药代动力学 

分 类 号：R978.11[医药卫生—药品] R969.1[医药卫生—药学]