氧氟沙星缓释胶囊家犬体内药动学及相对生物利用度

Pharmacokinetics and relative bioavailability of ofloxacin sustained-release capsules in dogs

目的:检测氧氟沙星缓释胶囊T1,T2(受试制剂)与泰利必妥片(参比制剂)在家犬体内的生物利用度。方法:采用RP-HPLC法检测狗血浆中氧氟沙星浓度。样品处理采用乙腈沉淀蛋白。绘制出血药浓度-时间曲线,并计算主要药动学参数。结果:受试制剂T1,T2及参比制剂的Cmax分别为(12．66±2．50),(7．84±2．42)和(35．22±2．49)mg·L-1;Tmax为(8．00±1．26),(10．17±1．60)和(2．50±0．55)h;MRT为(11．46±0．42),(12．23±1．00)和(6．57±0．61)h。T1和参比片剂的AUC无显著性差异,相对生物利用度为(95．91±11．38)％。T2和参比片剂的AUC有显著性差异,相对生物利用度为(59．37±20．80％)。结论:经统计学检验,受试制剂T1具有明显的缓释特征,和参比片剂具有生物等效性,氧氟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。

Objective：To investigate the relative bioavailability of ofloxacin sus capsules T1 and T2 （test） versus common ofloxacin tablets （reference） dogs. Methods tained-release ： The concentrations of ofloxacin in dogs＇ plasma were determined by the RP-HPLC. The acetonitrile was used to remove the plasma protein. Results：The major pharmacokinetic parameters of the test （T1 and T2） and reference samples were Cmax （ 12.66 ± 2.50）, （7.84 ±2.42） vs. （35.22 ± 2.49 ） mg·L^-1 ; Tmax （ 8.00 ± 1.26）, （10.17±1.60） vs. （2.50±0.55）h; MRT（11.46 ±0.42）, （12.23±1.00） vs. （6.57± 0.61 ）h, respectively. The T1 capsules showed no statistical difference of AUC value from the reference tablets. The T2 capsules had a significant difference of AUC value from the reference tablets. The relative bioavailability of the test （T1 and T2） capsules to the reference tablets was （95.91 ± 11.38 ） % and （59.37 ±20.80% ）, respectively. Conclusion： The ofloxaein sustained-release capsules （T1） are bioequivalent to the ofloxaein tablets, featuring sustained release.