四种前体脂质体制剂的包封率比较及小肠吸收研究

目的:采用一种新型前体脂质体制备方法将4种不同极性的药物分别制成前体脂质体,考察此种制备方法对不同药物的适用性。方法:比较齐墩果酸、水飞蓟素、替加氟、肉苁蓉总苷4种前体脂质体制剂水合后所形成脂质体的包封率,选用齐墩果酸前体脂质体、水飞蓟素前体脂质体水合后进行离体小肠吸收实验,以考察所形成脂质体的吸收情况,从而对体内吸收情况进行预测。结果:4种前体脂质体制剂中,包封率为齐墩果酸>水飞蓟素>替加氟>肉苁蓉总苷;离体小肠吸收实验结果显示:齐墩果酸脂质体、水飞蓟素脂质体与其对照溶液相比,药时曲线下面积增大。结论:前体脂质体制备方法尤其适用于弱极性药物如齐墩果酸,制成的脂质体制剂与对照相比,明显促进了药物的吸收。

The trap efficiency and the absorption of four kinds of proliposomes

Objective: A new proliposomal technology was used to trap several drugs, such as tegafur, silymarin, cistanosides, oleanolic acid, and then the suitability of the preparation method were studied. Methods: These proliposomes formed liposomes after mixing with water. And then the trap efficiencies of every kinds of the liposomes were determined and compared. Furthermore, the absorption in vitro of two kinds of liposomes was investigated. Results: The trap efficiency changed with the partition coefficient. When the partition coefficient increased, the trap efficiency increased. And the absorption of the drug could be improved than the drug solution after the drug was made into the liposome. Conclusion: This kind of liposomal technology trapped the drugs efficiently, and the lipophilic drugs were trapped more easily. Furthermore, this absorption of the drug could be improved.