甲砜霉素及HP-β-CD甲砜霉素在家兔体内的药代动力学比较研究

用健康家兔经口服给药(剂量为30 mg/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 Comparison between Thiamphenicol and HP-β-CD Thiamphenicol in Rabbit

The pharmaeokinetic regulations of thiamphenicol and HP-β-CD thiamphenieol 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 pharmaeokinetic-compartment analysis soft(3P97).The data of concentration-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 pharmacokinetic parameters of thiamphenicol 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 pharmaeokinetic parameters of HP-β-CD thiamphenieol 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 pharmacokinetic characteristics of HP-β-CD thiamphenieol in healthy rabbits manifested the rapid and complete absorption,wide distribution,rapid elimination and the high bioavailability by the oral routes.