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目的制备秋水仙碱醇质体并考察醇质体作为秋水仙碱经皮给药载体的可行性。方法采用注入法制备秋水仙碱醇质体,紫外法测定其包封率,并以包封率为指标,利用正交试验法优化处方和制备工艺;采用TYJ-6A型透皮扩散实验仪,用小鼠腹部皮肤进行体外经皮渗透实验;比较不同给药形式对秋水仙碱经皮渗透的影响。结果最佳处方为乙醇3.3mL,豆磷脂0.25g和秋水仙碱0.025g,用注入法注入4min即可,包封率达57.0%。秋水仙碱醇质体的经皮渗透速率(6.54μg·cm-2·h-1)是水溶液的5.59倍,是普通脂质体的3.14倍,是体积分数为30%乙醇溶液的1.24倍。10h后皮肤中药物的滞留量大小顺序为:醇质体>体积分数为30%乙醇溶液>普通脂质体>饱和水溶液。结论醇质体能提高秋水仙碱的透皮速率,增加药物在皮肤中的滞留量。
OBJECTIVE To prepare colchicine alkaloids and investigate the feasibility of using ethosomes as colchicine transdermal drug delivery vehicles. Methods The colchicine alcohol was prepared by injection method. The entrapment efficiency was determined by ultraviolet spectrophotometry. The entrapment efficiency was used as an index to optimize the formulation and preparation process by orthogonal test. Using TYJ-6A transdermal diffusion apparatus, In vitro transdermal skin permeation test was performed on the abdominal skin of mice. The effects of different administration forms on the transdermal permeation of colchicine were compared. Results The best prescription for the ethanol 3.3mL, 0.25g soybean lecithin and colchicine 0.025g, by injection injection 4min, encapsulation efficiency of 57.0%. The transdermal permeation rate (6.54 μg · cm-2 · h-1) of colchicine was 5.59 times that of the aqueous solution, 3.14 times that of the ordinary liposome, and 1.24 times of the volume fraction of the 30% ethanol solution. 10h after the skin retention of drugs in the order of size: alcohol volume> 30% ethanol solution> ordinary liposome> saturated aqueous solution. CONCLUSION Ethosomes can improve the dermal penetration rate of colchicine and increase the drug retention in the skin.