罗红霉素缓释胶囊在家犬体内的药动学及相对生物利用度

Relative bioavailability and pharmacokinetics of sustained-release roxithromycin capsules in dogs

目的评价罗红霉素缓释胶囊在家犬体内的药动学、相对生物利用度及体内外相关性。方法6条家犬随机交叉口服罗红霉素普通片和罗红霉素缓释胶囊 3 0 0mg后 ,利用HPLC法测定血药浓度并对其进行药动学和生物利用度研究。结果罗红霉素缓释胶囊和普通片的tmax分别为 (6 40±1 67)h和 (1 60± 0 5 5 )h ,cmax分别为 (6 5 2± 1 44)mg·L-1和 (1 5 5 1± 4 3 8)mg·L-1,AUC0 -52 分别为 (1 5 2 99± 3 3 5 2 )mg·h·L-1和 (1 70 86± 446 43 )mg·h·L-1,MRT0 -52 分别为 (2 0 42± 1 1 5 )h和 (1 3 0 3± 2 80 )h ,相对生物利用度为 90 76% ;其体内吸收与体外释药相关性显著 (r =0 9788)。

Objective To study the pharmacokinetics and relative bioavailability of sustained-release roxithromycin capsules in dogs.Methods A single oral dose of 300 mg of conventional roxithromycin tablets and sustained-release roxithromycin capsules were given to 6 dogs in a randomized crossover design. The drug concentrations in plasma were determined by the HPLC method. The pharmacokinetic parameters and the relative bioavailability were measured. Results The pharmacokinetic parameters of roxithromycin in conventional roxithromycin tablets and sustained-release roxithromycin capsules were t max(6.40±1.67 )h and (1.60±0.55)h, c max(6.52±1.44)mg·L -1 and (15.51±4.38)mg·L -1,AUC 0-52 (152.99±33.52)h·mg·L -1 and (170.86±446.43)h·mg·L -1,MRT 0-52(20.42±1.15)h and(13.03±2.80)h, respectively. The relative bioavailability of the sustained-release roxithromycin capsules was 90.76%. This was well relative in the relationship between absorption percent in vivo and dissolution percent in vitro. Conclusion An obvious characteristic of sustained-release capsules is shown in the concentration-time curves of roxithromycin in sustained-release capsules in dogs.