阿魏酸环糊精包合物的制备及体外经皮通透性的评价

采用饱和水溶液法分别制备阿魏酸的α-、β-和γ-环糊精包合物,并计算3种包合物的相稳定常数.经X-射线衍射确证后,用离体大鼠腹部皮肤进行3种包合物水溶液的体外经皮渗透试验.结果表明,3种包合物中阿魏酸-γ-环糊精包合物的包合率和相稳定常数均最大;阿魏酸包合物水溶液的透过量均小于阿魏酸原药水溶液的透过量,说明包合起到了缓释作用,更适于局部用药.

Preparation and in vitro Permeation of Inclusion Compounds of Ferulic Acid with Cyclodextrins

The inclusion compounds of ferulic acid with three cyclodextrins(α-CD,β-CD and γ-CD)were prepared by saturated solution-stirring method,respectively.The phase stability constants of the three inclusion compounds were determined and their formation was confirmed with X-ray diffractometry.The in vitro permeation and skin retention of the inclusion compounds though the excised rat skin were investigated.The results showed that the inclusion ratio and phase stability constant of the γ-cyclodextrin inclusion were the highest among the three compounds.The permeation of the three inclusion compounds was lower than that of ferulic acid solution,indicating that the inclusion compounds were more suitable for preparing a sustained-release dosage form for local application.