花椒毒素在人体皮肤及角质层中的渗透动力学探讨  

Penetration kinetics of xanthotoxin across human skin and stratum corneum

作　　者：王来友[1] Jelle Millet 黄芳芳[1] 杨得坡[1] 

机构地区：[1]中山大学药学院,广东广州510080 [2]弗朗什-孔泰大学药学院

出　　处：《药学学报》2006年第9期878-881,共4页Acta Pharmaceutica Sinica

基　　金：广州市科技局对外国际合作资助项目[穗条科字(2003)51号]

摘　　要：目的探讨花椒毒素在人体完整皮肤及其角质层中的渗透动力学特性。方法采用人体离体皮肤及从完整皮肤中分离出的角质层,在Franz-cell扩散池中进行不同浓度的花椒毒素乙醇溶液(0.1,0.5,2.5和5.0 mg.mL-1)的渗透实验,均采用1.4%的人血清溶液作为接收液,用HPLC法测定各接收液的药物量和皮肤中的贮存药物量。结果花椒毒素乙醇溶液单位面积透过完整人皮肤速率随着浓度增加而增加,2.5 mg.mL-1以上的浓度对其速率几乎无影响。在角质层中也存在同样的现象,但其单位面积透皮速率最大值提前了约6 h。而且随着给药浓度的增加,24 h后完整皮肤和角质层的药物贮存量也相应增加,但达到一定浓度后存在饱和现象。且花椒毒素乙醇溶液在完整皮肤中的透皮时滞(0.82 h)明显大于在角质层中的透皮时滞(0.47 h)。结论该结果对开发花椒毒素外用制剂时浓度的选择提供了依据,并对其外用药物后照射长波段紫外光(UVA)的时间提供了参考。Aim To investigate the penetration kinetics of xanthotoxin in human skin and stratum corneum. Methods The penetration experiments were accomplished by the deposit of ethanolic xanthotoxin solution onto human skin and stratum corneum mounted on Franz cells. The diffused xanthotoxin in the receptor solution （1.4% human serum albumin） and the retained amount in the skin and in the stratum corneum after 24 h exposure were quantified by using high performance liquid chromatography. Results Xanthotoxin flux was increased with the concentration deposited onto the human skin, and when the concentration is above 2.5 mg ·mL^-1 , there is no influence on the xanthotoxin flux. Similar results were obtained from the stratum corneum. And the peak time for the flux in the stratum corneum was preceded about 6 h earlier than that of the whole human skin. The retained xanthotoxin amount after 24 h exposure in the skin and in the stratum corneum increased according to the concentration deposited and has the tendency to saturate. The lag time of ethanolic xanthotoxin solution in the whole human skin is significantly higher than that in the stratum corneum （ P 〈 0.05 ）. Conclusion The characteristics of penetration kinetics of xanthotoxin will provide the information for concentration choice of topical formulation and give a reference for ultra violet A （UVA） irradiation time confirmation.

关 键 词：花椒毒素 透皮吸收 角质层 补骨脂素疗法 

分 类 号：R969.1[医药卫生—药理学]