β-环糊精和促透剂对辣椒碱经皮透过特性的影响

Effect of β-cyclodextrin and penetration enhancers on in vitro permeation of capsaicin through rat skin

【目的】研究不同浓度β-环糊精及促透剂对辣椒碱体外经皮渗透的影响。【方法】采用改良的Franz扩散池法,以离体鼠皮为透皮屏障,用高效液相色谱法测定接受液中辣椒碱的含量,计算药物的累积透过量,采用滞留时间法求算经皮渗透参数,考察不同浓度β-环糊精以及不同浓度十二烷基硫酸钠(sodium dodecyl sulfate,SDS)、尿素与辣椒碱-β-环糊精包合物对辣椒碱的促透作用。【结果】β-环糊精与辣椒碱形成包合物后透皮速率提高;添加SDS或尿素的辣椒碱-β-环糊精包合物透皮速率进一步增高,其中0.1%SDS的促透效果最为明显,而不同浓度的尿素促透效果相近。【结论】β-环糊精包合的辣椒碱经皮透过量增加,选择10 g/Lβ-环糊精制备辣椒碱β-环糊精包合物较适宜,SDS或尿素可进一步促进包合物中辣椒碱的透皮吸收。

[Objective] To study the in vitro effects of β -cyclodextrin and 2 kinds of penetration enhancers on the percutaneous absorption of capsaicin through isolated rat skin. [ Methods] A modified Franz diffusion apparatus was used in this experiment. HPLC method was established to determine the content of capsaicin in receivers at specified time points. All the percutaneous parameters like amount permeated （Q）, diffusivity （Dapp）, permeability coefficient （Pm）, partition coefficient （Kapp） and release rate constant （J） were calculated statistically. [ Results] β-cyclodextrin enhanced the percutaneous absorption of capsaicin. Release rate constant increased more when urea or SDS was added into capsaicin-13 -cyclodextrin inclusion compound. 0.1% SDS was more effective for transdermal permeability of capsaicin in rats. [Conclusions] β-cyclodextrin can be used as transdermal permeation enhancer in topical preparation of capsaicin. The optimal concentration of β-cyclodextrin is 10 g/L. The coapplication of SDS and urea can enhance absorption more significantly.