黄豆苷元自微乳化半固体骨架胶囊制备及大鼠体内药动学研究

Preparation of self-microemulsifying semi-solid matrix hard capsules of daidzein and its pharmacokinetics in rats

目的:制备黄豆苷元自微乳化半固体骨架胶囊,并考察其在大鼠体内药动学行为。方法:制备药物的过饱和溶液以测定药物在各种油、表面活性剂及助表面活性剂中的溶解度,采用伪三元相图法筛选表面活性剂与助表面活性剂的比例;通过正交设计优化处方并考察了大鼠经灌胃后体内药动学情况。结果:优化后的处方各组分比为DA(1.5)∶LM1944CS(10)∶聚山梨酯(Tween-80)/Transcutol(4∶1)(50)∶S-40(20)。黄豆苷元自微乳化半固体骨架胶囊与市售胶囊的相对生物利用度为(256.0±26.0)%。结论:按优化后处方制得黄豆苷元自微乳化半固体骨架释药系统可显著提高其生物利用度。

Objective： To prepare daidzein self-microemulsifying hard capsules drug delivery system and to investigate its pharmacokinetic profiles in SD rats.Methods： The optimum formulations of daidzein self-microemulsifying hard capsules were screened by solubility experiments,pseudo-ternary phase diagrams and orthogonal design.Pharmacokinetic profiles after oral administration were investigated in SD rats.Results： The optimum daidzein self-microemulsifying hard capsules were composed of daidzein（1.5）∶LM1944CS（10）∶Tween-80/Transcutol（4∶1）（50）∶S-40（20）.The relative bioavailability between DA-SMEDDS and DA capsule was（256.0±26.0）%.Conclusion： Daidzein self-microemulsifying hard capsules can be prepared according to the optimum formulations and the bioavailability is dramatically increased.