盐酸环丙沙星缓释胶囊家犬体内生物利用度研究

Bioavailability study of ciprofloxacin hydrochloride sustained-release capsules in dogs

目的检测盐酸环丙沙星缓释胶囊与普通片在家犬体内的生物利用度。方法样品用乙腈沉淀蛋白 ,然后用氯仿除去杂质。采用反相高效液相色谱法测定家犬体内的盐酸环丙沙星血药浓度。结果受试制剂及参比制剂的cmax分别为 (9 2 0± 2 0 2 )mol·L-1和 (2 2 5 1± 7 2 4)mol·L-1;tmax分别为 (6 0 0± 0 0 )h和 (2 5 0± 0 5 5 )h ;平均滞留时间 (tMR)分别为 (1 2 2 3± 2 92 )h和 (5 66±1 7)h ,2种制剂的AUC无显著性差异 ,相对生物利用度为 (97 1 0± 9 61 ) %。结论经统计学检验 ,受试制剂具有明显的缓释特征 ,2种制剂具有生物等效性 ,盐酸环丙沙星缓释胶囊体内吸收百分数与体外累积释放百分数相关性分析结果表明两者具有显著的相关性 (P <0 0 1 )。

Objective To study on the pharmacokinetics and bioavailability of ciprofloxacin hydrochloride sustained-release capsules on comparison with that of the conventional tablets.Methods Acetonitrile was added to the plasma to sediment the protein and then chloroform was added to remove the impurity and the part of acetonitrile. The concentration of ciprofloxacin hydrochloride in dogs′ plasma was determined by RP-HPLC method.The plasma concentration-time curves were plotted.The main pharmacokinetic parameters of the two preparations and the relative bioavailability of the sustained-release capsules were obtained.Results The c _ max of the two preparations were (9.20±2.02)mol·L -1 and (22.51±7.24)mol·L -1 respectively; t _ max if that was(6.00±0.0)h and (2.50±0.55)h and t _ MR were (12.23±2.92)h,(5.66±1.7)h respectively.There was no significant difference between the AUC value of the two formulations.The oral relative bioavailability of the sustained-release capsules to the conventional tablets was (97.10±9.61)%.Conclusion By the statistical analysis,the ciprofloxacin hydrochloride sustained-release capsule possessed good sustained-release characeteristics and the test and reference formulations were of bioequivalence.Significant correlation between in vitro dissolution and in vivo absorption of ciprofloxacin hydrochloride sustained-release capsules was found.