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目的 比较皮肤角质层和真皮层及促透剂对药物经皮吸收的影响。方法 制备氟尿嘧啶(5-FU)贴剂为模型药剂,以肉豆蔻酸异丙酯(TPM)为促透剂,采用Franz扩散池法,用高效液相色谱法和气相色谱法分别检测5-FU和IPM浓度,计算5-FU在各种皮肤状态下的透皮能力(Kp)。结果剥离角质层后,5-FU的Kp是经完整皮肤的2.3倍;在IPM作用下5-FU的Kp为原来的1.8倍(经完整皮肤)和2.4倍(经剥离角质层皮肤)。结论剥离角质层能增加5-FU的吸收;IPM主要降低角质层对5-FU的屏障作用,在剥离角质层后其对5-FU的吸收也没有增加作用。
Objective To compare the effects of cutaneous stratum corneum, dermal layer and transdermal enhancers on transdermal drug absorption. Methods Fluorouracil (5-FU) patch was used as a model drug. The permeation rate of TPM was determined by Franz diffusion cell method. The effects of 5-FU And IPM concentration, the transdermal ability (Kp) of 5-FU under various skin conditions was calculated. Results Kp of 5-FU was 2.3-fold that of intact skin after stripping of the stratum corneum; Kp of 5-FU under IPM was 1.8-fold (intact skin) and 2.4-fold (by stripping of the stratum corneum skin) of original. Conclusions Peeling stratum corneum can increase the absorption of 5-FU. IPM mainly reduces the barrier function of stratum corneum to 5-FU, and does not increase the absorption of 5-FU after stratum corneum stratum stripping.