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目的研究银杏酮酯自微乳化给药系统(GBE50-SMEDDS)的药物代谢动力学与生物利用度。方法以杏灵颗粒剂为对照,桑色素为内标,槲皮素、山奈素、异鼠李素为对照品,计算总黄酮醇苷含量,进行大鼠灌胃给药体内血药浓度测定。结果血药浓度-时间曲线和药物动力学参数显示,GBE50-SMEDDS的Cmax比参比对照颗粒剂提高了0.3 mg/L,Tmax提前了2.7 h,消除速率减小,消除半衰期延长了7.4 h,分布速率增大,分布半衰期提前了2.2 h,AUC(0-∞)提高了13.8 mg.h.L-1,AUC(0-∞)是参比对照颗粒剂的152.47%,提高了52.47%。结论 GBE50-SMEDDS新制剂比现有市场剂型杏灵颗粒剂生物利用度高,为临床疗效的提高提供了实验基础。
Objective To study the pharmacokinetics and bioavailability of ginkgo ketal ester self-microemulsifying drug delivery system (GBE50-SMEDDS). Methods Xinglin granules as a control, morin as an internal standard, quercetin, kaempferol, isorhamnetin for the reference substance, calculate the total flavonol glycoside content of rat gavage administered blood concentration determination. Results The plasma concentration-time curve and pharmacokinetic parameters of GBE50-SMEDDS showed that the Cmax of GBE50-SMEDDS was increased by 0.3 mg / L, Tmax was 2.7 h, the elimination rate was reduced, the elimination half-life was prolonged by 7.4 h, The distribution half-life increased by 2.2 h, the AUC (0-∞) increased by 13.8 mg.hL-1, and the AUC (0-∞) increased by 52.47% compared with 152.47% of the reference granules. Conclusion The new formulation of GBE50-SMEDDS has higher bioavailability than the existing market Xingling granules, which provides the experimental basis for the improvement of clinical efficacy.