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目的 :研究来氟米特在离体皮肤中的渗透代谢行为 ,为其经皮给药制剂的研制提供依据。方法 :采用Valia -Chien扩散池 ,以体外昆明种小鼠和SD大鼠皮肤为屏障进行渗透代谢实验 ,适时取样 ,HPLC法测定来氟米特和A77172 6的浓度。结果 :来氟米特在不同皮肤中的渗透代谢特性明显不同 ,来氟米特和A77172 6的累积量均随时间延长而呈线性增加 ,而来氟米特本身渗透速率低时分解产物的水平反而高。结论 :A77172 6是在来氟米特透皮过程中分解产生的 ,但皮肤的代谢屏障对于来氟米特的渗透总速率影响较小
OBJECTIVE: To study the infiltration and metabolism of leflunomide in exfoliated skin, and to provide a basis for the preparation of its transdermal preparation. Methods: ValiaChien diffusion cells were used to infiltrate the skin of Kunming mice and SD rats in vitro. The samples were collected in time and the concentrations of leflunomide and A77172 6 were determined by HPLC. RESULTS: The levofloxacin significantly differed in the osmotic and metabolic properties of different skins. The cumulative amount of leflunomide and A77172 6 increased linearly with time, whereas the level of leflunomide when leflunomide itself had a low permeation rate But high. Conclusions: A77172 6 is decomposed during leflunomide transdermal skin release, but the skin’s metabolic barrier has less effect on the overall rate of infiltration of leflunomide