摘要
用健康家兔经口服给药(剂量为30mg/kg),研究甲砜霉素及HP-β-CD甲砜霉素的药动学规律。以RP-HPLC法测定血浆中甲砜霉素的浓度,药物浓度-时间数据用3P97药动学程序软件处理。家兔单剂量口服给药甲砜霉素和HP-β-CD甲砜霉素血药浓度-时间数据均符合一级吸收一室开放模型。甲砜霉素主要动力学参数为:Lagtime(0.05±0.02)h,t1/2ka(0.83±0.02)h,t1/2ke(2.27±0.31)h,T(peak)(1.84±0.12)h,C(max)(6.98±0.95)mg/L,AUC(34.98±0.68)mg(/L·h),F(110.74±0.02)%。HP-β-CD甲砜霉素主要动力学参数为:Lagtime(0.02±0.01)h,t1/2ka(0.91±0.16)h,t1/2ke(0.86±0.15)h,T(peak)(0.96±0.07)h,C(max)(8.59±0.55)mg/L,AUC(43.02±0.87)mg(/L·h),F(142.07±0.02)%。HP-β-CD甲砜霉素在家兔体内的药动学特征表现为分布广泛,消除迅速;口服给药吸收迅速且完全,生物利用度高。
The pharmacokinetic regulations of thiamphenicol and HP-β-CD thiamphenicol were investigated by taken oral administration at a dosage of 30 mg/kg to healthy rabbits. The concentration of thiamphenicol in plasma was determined by RP-HPLC, and the data of concentration-time were analyzed by pharmacokinetic-eompartment analysis soft (3P97). The data of eoncentration-time after oral administration of thiamphenieol and HP-β-CD thiamphenicol were all fitted to a one-compartment open model with first-order absorption. The main pharmacokinetie parameters of thiamphenieol were as follows: Lagtime (0. 05 ±0. 02) h, t1/2ka (0. 83 ±0. 02) h, t1/2ke (2.27 ±0. 31 ) h, T (peak) (1. 84 ±0. 12) h, C (max) (6. 98 ±0. 95) mg/L, AUC (34. 98 ±0. 68) mg/ (L·h) and F (110. 74 ±0. 02) %. The main pharmacokinetic parameters of HP-β-CD thiamphenicol were as follows: Lagtime (0. 02 ±0. 01) h, t1/2ka (0. 91 ±0. 16) h, t1/2ke (0.86 ±0. 15) h, T(peak) (0.96 ±0. 07) h, C (max) (8.59 ±0. 55) mg/L, AUC (43.02 ±0. 87) mg/(L ·h), F (142.07 ±0. 02) %. The pharmaeokinetic characteristics of HP-β-CD thiamphenicol in healthy rabbits manifested the rapid and complete absorption, wide distribution, rapid elimination and the high bioavailability by the oral routes.
出处
《湖南农业科学》
2009年第12期11-14,共4页
Hunan Agricultural Sciences
基金
江苏畜牧兽医职业技术学院基金项目(200717)