替硝唑果胶骨架型结肠定位缓释片在犬体内药动学研究

目的 研究替硝唑果胶骨架型结肠定位缓释片在犬体内药动学.方法 采用双周期交叉试验设计,6只健康Beagle犬分别服用受试制剂或参比制剂,用HPLC法测定Beagle犬血浆中药物浓度.结果 受试、参比制剂在犬体内的血药浓度变化符合二室模型,其主要药动学参数：Tmax分别为（7.0±0.92）和（2.0±0.31）h;Cmax分别为（66.97±5.9）和（112.2±7.4）μg/L;AUC0-t分别为（1243.88±25.67）和（1523.84±27.89）mg·h/L;AUC0-∞分别为（1277.18±30.58）和（1548.67±20.89）mg·h/L,受试制剂的相对生物利用度为82.47%.结论 本法准确、灵敏,适用于替硝唑果胶骨架型结肠定位缓释片的药动学研究.

The pharmacokinetics study of tinidazole pectin matrics colon-specific sustained-release tablets in dogs

Objective To develop a method to study the pharmacokinetics of tinidazole pectin matrics colon-specific sustainedrelease tablets in dogs. Methods The plasma concentrations were determined by HPLC. Two-period cross over self-control trail was con- ducted to 6 Beagle dogs which were administrated a single dose of the oral test tablets and reference tablets. Results The pharmacokinetics of two preparations fitted to two-compartment model. The main pharmacokinetic parameters ： Tmax were （ 7.0 ±0. 92 ） and （ 2.0 ±0. 31） h;Cmax were （66.97±5.9）and（112.2 ±7.4） μg./L;AUC0-t were （1 243.88 ±25.67）and（1 523.84 ±27.89） mg · h/L;AUC0-∞were （1 277.18 ± 30.58）and（ 1 548.67 ± 20.89） mg · h/L and test tablets showed a relative bioavailability of 82.47%. Conclusion The method was accurate and sensitive which was suitable for Tinidazole pectin matrics pharmacokinetics study.