【摘要】 采用乙醇注入超声法制备长春西汀醇质体。以醇质体的包封率和渗透速率为指标,经正交试验筛得最佳处方为:长春西汀用量0.45%,乙醇用量45%,磷脂用量3%,超声3 min。优化后醇质体的包封率为(79.5±1.8)%,药物含量为(3.52±0.03)mg/ml,经皮渗透速率为(8.15±0.05)?g·cm-2·h-1。为提高醇质体的生物黏附性,进一步将醇质体制成凝胶。以SD大鼠离体皮肤为屏障,对比了长春西汀醇质体及其凝胶、长春西汀饱和溶液及其凝胶的体外经皮渗透行为。结果后三者的体外经皮渗透速率分别为(3.56±0.13)、(1.15±0.14)和(0.53±0.03)ug·cm-2·h-1。更多还原

【Abstract】 The vinpocetine(1) ethosomes were prepared by ethanol injection-sonication method. The formulation was optimized by orthogonal test with encapsulation effi ciency and permeation rate of the ethosomes as the indexes. The encapsulation effi ciency, drug content and permeation rate of the optimal ethosomes contained 0.45% 1, 45% ethanol, 3% lecithin and sonication for 3 min were(79.5±1.8)%,(3.52±0.03)mg/ml and(8.15±0.05)ug·cm-2·h-1, respectively. Then the optimal formulation was processed to hydrogel to improve the bioadhesion of ethosomes. The stable penetration rates(Jss) of 1 ethosomes and its gel as well as 1 saturated solution and its gel were investigated and compared with the excised rat skin as the barrier. The results of the latter three products were(3.56±0.13),(1.15±0.14)and(0.53±0.03)ug·cm-2·h-1, respectively.更多还原