替硝唑结肠定位肠溶片在家犬的药代动力学研究

目的　研究家犬口服替硝唑结肠定位肠溶片的药代动力学特征。方法　实验家犬随机分成两组 ,分别服用受试制剂和参比制剂 ,采用RP HPLC法测定血浆和肠道中药物浓度。结果　受试制剂和参比制剂的Tmax分别为 (6 3±1 2 )h和 (2 4± 1 1)h ,Cmax分别为 (46 2 3± 8 93 )mg·L-1和 (5 8 0 8± 14 65 )mg·L-1,用梯形法计算所得的AUC0 -t分别为 (42 3 2 1± 93 0 8)mg·h·L-1和 (45 8 2 2±112 0 7)mg·h·L-1。与参比制剂相比 ,受试制剂的相对生物利用度为 92 9%± 6 6%。家犬服用替硝唑结肠定位肠溶片 6 5h后结肠中替硝唑的量较多 ,而小肠中则几乎未检测到替硝唑。结论　家犬服用替硝唑结肠定位肠溶片后药物吸收出现明显的滞后 ,替硝唑结肠定位肠溶片在胃和小肠中稳定 ,几乎不释放出药物 ,而在结肠处释放出大量药物 ,具有良好的结肠定位释放效果

The pharmacokinetics of colon-specific tinidazole tablets in dogs

AIM To study the pharmacokinetic characters following oral administration of colon specific tinidazole tablets in healthy dogs METHOD The plasma and intestine content concentration of tinidazole was determined by RP HPLC method following a single oral dose of 500 mg of two formulations given to each dogs in an open randomized two way crossover design RESULT The main pharmacokinetic parameters of test and reference tablets were as follow: T max : (6 3±1 2) h and (2 4±1 1) h; C max : (46 23±8 93) mg·L -1 and (58 08±14 65) mg·L -1 ; AUC 0-t : (423 21±93 08) mg·h·L -1 and (458 22±112 07) mg·h·L -1 The relative bioavailability of tinidazole colon specific enteric tablets was 92 9%±6 6%. 6 5 h after intake of colon specific tablets, there were a great deal of tinidazole in dogs colon but almost no tinidazole in small intestine CONCLUSION The result demonstrated that the colon tropic effect of the tablets is significant in dogs