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目的:比较罗格列酮钠肠溶制剂与罗格列酮钠普通制剂在犬体内的药动学特征及其生物等效性。方法:将6只犬均分为2组,分别单次灌服罗格列酮钠肠溶胶囊或罗格列酮钠普通胶囊4mg,于给药前及给药后450min内后腿静脉取血,给药7d后,相同剂量自身交叉给药,于上述相同时间点取血,用高效液相色谱法测定血浆中罗格列酮浓度;经DAS2.0软件处理,计算药动学参数。结果:在相同剂量下,罗格列酮钠肠溶胶囊与其普通胶囊的药动学参数分别为AUC0～∞:(119.662±8.451)、(118.493±15.325)mg.min.L-1,t1/2Ka:(101.548±6.526)、(39.702±26.293)min,cmax:(0.359±0.035)、(0.807±0.208)mg.L-1;与普通胶囊比较,肠溶胶囊的AUC0～∞无显著性差异,t1/2Ka明显延长、cmax明显降低(P<0.05或P<0.01)。结论:与普通胶囊比较,罗格列酮钠肠溶制剂与其生物等效且具有明显的缓释特征。
OBJECTIVE: To compare the pharmacokinetics and bioequivalence of rosiglitazone sodium enteric-coated and rosiglitazone sodium common in dogs. Methods: All the 6 dogs were divided into 2 groups. The rats were administrated with 4 mg of rosiglitazone sodium enteric-coated capsules or normal sodium rosiglitazone capsules respectively. Blood samples were collected from the hind leg vein before administration and within 450 minutes after administration After the administration for 7 days, the same dose was administered to the patients at the same time, blood was taken at the same time and the plasma concentration of rosiglitazone was determined by HPLC. The pharmacokinetic parameters were calculated by DAS2.0 software. Results: The pharmacokinetic parameters of rosiglitazone sodium enteric-coated capsules and ordinary capsules at the same dose were AUC0 ~ ∞ (119.662 ± 8.451), (118.493 ± 15.325) mg.min.L-1, t1 / 2Ka: (101.548 ± 6.526), (39.702 ± 26.293) min, cmax: (0.359 ± 0.035), (0.807 ± 0.208) mg.L-1, respectively. There was no significant difference in the AUC0 ~ ∞ of enteric capsules , t1 / 2Ka significantly prolonged, cmax decreased significantly (P <0.05 or P <0.01). CONCLUSIONS: Sodium rosiglitazone enteric-coated formulations are bioequivalent to conventional capsules and have a sustained-release profile.