家犬单剂量口服氢溴酸加兰他敏缓释微丸胶囊的生物利用度研究

目的:研究氢溴酸加兰他敏缓释微丸胶囊在家犬体内单剂量的生物利用度。方法:采用双周期交叉试验,取家犬6只随机分成2组,分别灌胃给予氢溴酸加兰他敏缓释微丸胶囊和氢溴酸加兰他敏胶囊进行双周期交叉试验,于给药后不同时点取血样,采用高效液相色谱法测定血药浓度及计算相关药动学参数。结果:单剂量给药后,缓释微丸胶囊和胶囊的AUC分别为(1867.24±321.05)、(1604.60±289.17)ng·h·mL-1,tmax分别为(5.42±2.24)、(0.73±0.62)h,Cmax分别为(89.62±11.23)、(162.82±15.35)ng·mL-1,t1/2分别为(8.93±1.82)、(7.58±1.21)h;缓释微丸胶囊的相对生物利用度为116.36%。结论:氢溴酸加兰他敏缓释微丸胶囊具有明显的缓释性,与氢溴酸加兰他敏胶囊具有生物等效性。

Bioavailability of Single Oral Dose of Galanthamine Hydrobromide Extended - release Pellet Capsule in Dogs

OBJECTIVE： To study the bioavailability of single oral dose of galanthamine hydrobromide（GH） sustained- release pellet capsule （GHSRPC） in healthy dogs. METHODS： By a two-cycle crossover trial, 6 dogs were randomly assigned to receive GHSRPC or GH capsules respectively by ig. Blood samples were taken at different time and the plasma concentrations of GHSRPC and GH capsules were determined by HPLC, meanwhile their pharmacokinetic parameters were computed. RESULTS： After a single dose administration of GHSRPC and GH capsules, the pharmacokinetic parameters were as follows： AUC were （1 867.24±321.05） and （1 604.60±289.17） ng·h·mL^-1, were （5.42±2.24） and （0.73±0.62） h; C were （89.62± 11.23） and （162.82± 15.35） ng · mL^-1 t 1/2 were （8.93± 1.82） and （7.58± 1.21） h, respectively. The relative bioavailability of the GHSRPC was 116.36%. CONCLUSION： The results showed significant sustained release characteristics of the GHSRPC, It＇s bioequivalent with GH capsule.