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目的:制备齐墩果酸膜修饰脂质体,并对其体内药动学行为进行研究。方法:以合成的高荷电密度的N-三甲基壳聚糖(TMC)为脂质体膜修饰材料,通过FT-IR、1 H-NMR对合成产物进行结构确证;采用乙醇注入法制备TMC修饰的齐墩果酸脂质体(OA-TCL),采用微柱离心、透射电镜、粒径Zeta电位测定仪考察OA-TCL的理化性质,并对OA-TCL口服给药后在大鼠体内药动学行为进行研究。结果:脂质体呈球形或类球形,平均粒径(164±4.24)nm,Zeta电位为(23.8±0.2)mV,包封率可达(96.8±1.76)%;药动学参数显示OA-TCL药-时曲线下面积分别为齐墩果酸混悬液组、齐墩果酸未修饰脂质体组的2.51,2.33倍。结论:该研究为进一步研究OA-TCL在急慢性肝损伤治疗中的应用提供了基础,为难溶性中药成分口服给药系统的设计提供了新思路。
OBJECTIVE: To prepare oleanolic acid membrane modified liposomes and study its pharmacokinetics in vivo. Methods: The synthetic high charge density N-trimethyl chitosan (TMC) was used to modify the liposome membrane. The structure of the synthesized product was confirmed by FT-IR and 1 H-NMR. Ethanol injection TMC-modified oleanolic acid liposomes (OA-TCL). The physical and chemical properties of OA-TCL were investigated by microcolumn centrifugation, transmission electron microscopy and particle size Zeta potential meter. After oral administration of OA-TCL, In vivo pharmacokinetic behavior research. Results: The liposomes were spherical or spheroidal with an average particle size of (164 ± 4.24) nm and a Zeta potential of (23.8 ± 0.2) mV and an encapsulation efficiency of 96.8 ± 1.76%. The pharmacokinetic parameters of OA- TCL drug - time curve area were oleanolic acid suspension group, oleanolic acid unmodified liposomes 2.51,2.33 times. Conclusion: This study provides the basis for the further study of the application of OA-TCL in the treatment of acute and chronic liver injury and provides a new idea for the design of oral administration system of traditional Chinese medicine.