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角质层与真皮层对氟尿嘧啶贴剂经皮吸收的影响

Influence of the stratum corneum and dermis of the skin on the percutaneous absorption of fluorouracil delivered through skin patch

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【作者】 李国锋陈建海陈志良神山文男山本昌

【Author】 LI Guo-feng, CHEN Jian-hai, Kamiyama Fumio, Yamamoto Akira, CHEN Zhi-liang’Department of Pharmacy, Nanfang Hospital, First Military Medical University, Guangzhou 510515, China; Pharma-ceutical Department, Kyoto Pharmaceutical University, Kyoto 607-844, Ja

【机构】 第一军医大学南方医院药学部京都药科大学药剂学教室京都药科大学药剂学教室 广东 广州510515广东 广州510515日本 京都607-8414日本 京都607-8414

【摘要】 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。

【Abstract】 Objective To investigate the respective influence of skin layers, specifically the stratum corneum (SC) and the viable layer, and isopropyl myristate (IPM), an absorption enhancer, on the permeability (Kp) of drug. Methods Patches saturated with fluorouracil (5-FU), which was used as a test drug, were prepared. The Franz diffusion experiment via different rat skin layers was carried out, and high-performance liquid chromatography (HPLC) or gas chromatography (GC) was employed to determine the contents of 5-FU and IPM. Kp of 5-FU in various conditions was calculated. Results The Kp of 5-FU via SC -stripped skin was 2.3 times that via intact skin, and in the presence of IPM, Kp was 1.8 times that via intact skin and 2.4 times that via SC-stripped skin. Conclusion The permeability of 5-FU is enhanced after the SC is stripped, and IPM can overcome the barrier of SC in intact skin to facilitate 5-FU absorption, but can not enhance the Kp of 5-FU via SC-stripped skin.

  • 【文献出处】 第一军医大学学报 ,Journal of First Military Medical University , 编辑部邮箱 ,2002年09期
  • 【分类号】R944.2
  • 【被引频次】6
  • 【下载频次】175
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