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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。
OBJECTIVE: To study the applicability of this preparation method to different drugs by using a new method of preparation of precursor liposomes to make four different polarity drugs into precursor liposomes respectively. METHODS: The entrapment efficiency of liposomes formed by hydration of oleanolic acid, silymarin, tegafur and cistanche glycosides was compared. Liposomes of oleanolic acid precursor, silymarin After in vitro hydration of liposomes, small intestine absorption experiments were carried out to investigate the absorption of liposomes formed, and to predict the absorption in the body. Results: The entrapment efficiency of oleanolic acid, silymarin, tegafur and glycosides of cistanche in the four liposome preparations was as follows: liposomes of oleanolic acid, silymarin Compared with its control solution, the area under the curve of drug increased. CONCLUSION: The preparation of liposomes is especially suitable for the preparation of lipophilic drugs such as oleanolic acid. Compared with the control, the prepared liposomes obviously promote the absorption of drugs.