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目的比较分别用不饱和磷脂和饱和磷脂为膜材,不同溶剂制得的秋水仙碱醇质体理化特性的差别。方法采用注入法制备秋水仙碱醇质体,正交设计法筛选处方。比较不饱和磷脂与饱和磷脂对其形态学、包封率、稳定性和经皮渗透的累积透过量的影响。结果制备的两种醇质体形状呈圆球形或类圆形,结构完整。含不饱和磷脂醇质体平均粒径为100 nm,粒径分布较窄,包封率达58%;含饱和磷脂醇质体平均粒径为50 nm,粒径分布较宽,包封率达63%;含饱和磷脂醇质体的稳定性受高温和光照的影响都要明显小于含不饱和磷脂醇质体。含饱和磷脂醇质体的药物单位面积累计透过量和药物在皮肤中的滞留量也明显高于含不饱和磷脂醇质体的透过量和滞留量。结论经初步评价,用氢化磷脂、乙醇和Tween 80所制备的秋水仙碱醇质体在包封率、稳定性和经皮渗透的累积透过量方面明显优于用大豆磷脂和异丙醇所制备的秋水仙碱醇质体。
Objective To compare the physical and chemical characteristics of colchicine made from different solvents with unsaturated phospholipid and saturated phospholipid respectively. Methods The colchicine alkaloids were prepared by injection method, and the prescriptions were selected by orthogonal design. The effect of unsaturated phospholipid and saturated phospholipid on the morphological, entrapment efficiency, stability and cumulative permeation of transdermal permeation was compared. Results The prepared two kinds of ethosomes were spherical or almost circular in shape and were structurally intact. The average particle size of the unsaturated phospholipid-containing ethosomes was 100 nm, the particle size distribution was narrow and the entrapment efficiency was 58%. The average particle size of the saturated phospholipid-containing ethosomes was 50 nm with wide particle size distribution and the entrapment efficiency 63%; the stability of saturated phosphatidylethanolamine was significantly lower than that of unsaturated phosphatidylinositol by high temperature and light. The cumulative permeation per unit area of the drug containing saturated phosphatidylserine and the retention of the drug in the skin were also significantly higher than those of the unsaturated phosphatidylserine containing body. CONCLUSIONS: Preliminary evaluation of colchicine alkaloids prepared with hydrogenated phospholipids, ethanol, and Tween 80 was significantly superior to that with soy lecithin and isopropanol in terms of encapsulation efficiency, stability, and cumulative permeation of transdermal permeation Colchicine Alkaloids.