[皮肤角质层和真皮对通过皮肤贴片递送的氟尿嘧啶经皮吸收的影响]
[Influence of the stratum corneum and dermis of the skin on the percutaneous absorption of fluorouracil delivered through skin patch].
作者信息
Li Guo-feng, Chen Jian-hai, Kamiyama Fumio, Yamamoto Akira, Chen Zhi-liang
机构信息
Department of Pharmacy, Nanfang Hospital, First Military Medical University, Guangzhou 510515, China.
出版信息
Di Yi Jun Yi Da Xue Xue Bao. 2002 Sep;22(9):800-2.
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 (K(p)) 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. K(p) of 5-FU in various conditions was calculated.
RESULTS
The K(p) of 5-FU via SC -stripped skin was 2.3 times that via intact skin, and in the presence of IPM, K(p) 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 K(p) of 5-FU via SC-stripped skin.
目的
研究皮肤各层，特别是角质层（SC）和活性层，以及吸收促进剂肉豆蔻酸异丙酯（IPM）对药物渗透性（K(p)）的各自影响。
方法
制备用氟尿嘧啶（5-FU）作为受试药物饱和的贴剂。通过不同大鼠皮肤层进行Franz扩散实验，并采用高效液相色谱（HPLC）或气相色谱（GC）测定5-FU和IPM的含量。计算不同条件下5-FU的K(p)。
结果
5-FU透过去角质层皮肤的K(p)是透过完整皮肤的2.3倍，在存在IPM的情况下，K(p)是透过完整皮肤的1.8倍，是透过去角质层皮肤的2.4倍。
结论
去除角质层后5-FU的渗透性增强，IPM可克服完整皮肤中角质层的屏障以促进5-FU吸收，但不能提高5-FU透过去角质层皮肤的K(p)。
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