畜牧兽医学报 ›› 2007, Vol. 38 ›› Issue (7): 718-722.doi:

• 基础兽医 • 上一篇    下一篇

磺胺间甲氧嘧啶混悬注射液在猪体内的药动学研究

吴俊伟;饶勇;姜波   

  1. 1.西南大学荣昌校区动物医学系,重庆 402460;2.西南大学药学院,重庆400715;3.重庆方通动物药业有限公司,重庆402460
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2007-07-25 发布日期:2007-07-25

Study on the Pharmacokinetic of Sulfamonomethoxine Suspension Injection in Pigs

WU Jun-wei;RAO Yong;JIANG Bo   

  1. 1. Department of Animal Medical Science, Rongchang Campus, Southwest University,Chongqing 402460, China; 2.College of Pharmacy, Southwest University, Chongqing 400715, China; 3.Chongqing Fangtong Animal Pharmaceutical CO., LTD, Chongqing 402460, China
  • Received:1900-01-01 Revised:1900-01-01 Online:2007-07-25 Published:2007-07-25

摘要: 本文比较了磺胺间甲氧嘧啶(SMM)和SMM-Na两种混悬注射液与SMM-Na注射液在猪体内的药物代谢动力学特征,旨在为SMM混悬注射液的开发和注册提供依据。将18头猪随机分成SMM混悬注射液、SMM-Na混悬注射液和SMM-Na注射液3个试验组,按100 mg/kg BW单次肌注给药。 HPLC分析血浆中的药物浓度,用MCPKP程序计算动力学参数。3种制剂在猪体内的动力学过程都符合一级吸收二室模型,主要药动学参数如下,SMM混悬注射液:t1/2α (2.86±0.85) h,t1/2β (45.57±8.06) h,AUC (712.04±108.20) mg·L-1·h,Cmax (12.16± 0.52) mg/L;SMM-Na混悬注射液:t1/2α (7.90±1.21) h, t1/2β (24.87±12.92) h,AUC (1 489.78±164.63) mg·L-1·h,Cmax (97.86±10.24) mg/L;SMM-Na注射液:t1/2α(0.10±0.04) h, t1/2β(6.20±0.57) h,AUC (1 080.83± 93.78) mg·L-1·h,Cmax (84.30±4.26) mg/L。SMM混悬注射液虽然消除缓慢,但血药浓度低,有效血药浓度时间短,很难达到临床治疗的要求;SMMNa混悬注射液血药浓度高,有效血药浓度时间长,是一种较理想的缓释制剂。

Abstract: The aim was to obtain the basic data for development and registration the sulfamonomethoxine (SMM) suspension preparation.The pharmacokinetics of SMM and SMM-Na suspension injections and SMMNa injection were studied in healthy pigs. 18 pigs of 3 groups were administered muscularly with SMM at 100 mg/kg body weight in single.The SMM concentrations in plasma were analyzed by high performance liquid chromatography (HPLC).The pharmacokinetic parameters were calculated by MCPKP program. The pharmacokinetic processes of 3 preparations were all fitted to twocompartment open model with first-order absorption. The main pharmacokinetic parameters were as follows: t1/2α (2.86±0.85) h,t1/2β (45.57±8.06) h,AUC (712.04±108.20) mg·L-1·h,Cmax (12.16±0.52) μg/mL for the SMM suspension; t1/2α (7.90±1.21) h, t1/2β (24.87±12.92) h, AUC (1 489.78±164.63) mg·L-1·h, Cmax (97.86±10.24) μg/mL for the SMM-Na suspension; t1/2α (0.10±0.04) h, t1/2β(6.20±0.57) h,AUC (1 080.83±93.78) mg·L-1·h,Cmax (84.30±4.26) mg/L for the SMM-Na injection. Though SMM suspension injection was eliminated very slowly, its plasma-drug concentrations were low with a short effective plasma-drug concentration time, and were difficult to meet the clinic treatment requirement. SMM-Na suspension injection showed a long effective plasma drugconcentration time with high plasma-drug concentrations and it was an excellent delayed-release preparation.