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目的：研究来氟米特在新生ＳＤ大鼠皮肤匀浆中的代谢作用，为来氟米特经皮给药制剂的研究提供实验依据。方法：取新生 ＳＤ大鼠腹部皮肤于生理盐水中匀浆，制备高、中、低 ３组浓度来氟米特的皮肤匀浆液， ３２℃保温，适时取样，以ＨＰＬＣ法测定来氟米特和其活性代谢物Ａ７７ １７２６的浓度。结果：除对照组（不含皮肤匀浆）中来氟米特浓度保持不变外，其他各组中来氟米特浓度均随保温时间的延长而降低，活性代谢物Ａ７７ １７２６的浓度随保温时间的延长而增加。结论：来氟米特在新生ＳＤ大鼠皮肤匀浆上清中具有较明显的代谢作用。
OBJECTIVE: To study the metabolism of leflunomide in the skin homogenate of neonatal SD rats, and to provide experimental evidence for the study of percutaneous delivery of leflunomide. Methods: The skin of abdomen of SD rats was homogenized in normal saline, and the skin homogenates of leflunomide with high, medium and low concentrations were prepared and incubated at 32 ℃. Samples were taken at appropriate time, and leflunomide and Its active metabolite A77 1726 concentration. RESULTS: Leflunomide concentration remained unchanged in all the groups except leflunomide in the control group (without skin homogenate), and the concentrations of the active metabolite A77 1726 decreased with incubation time The increase of time. Conclusion: Leflunomide has more obvious metabolism in the supernatant of SD skin of rats.