盐酸川芎嗪经皮给药系统的制备及体外释放和透皮研究

Preparation,in vitro Release and Percutaneous Penetration of Ligustrazine Hydrochloride Transdermal Delivery System

用盐酸川芎嗪作为模型药物,将阿拉伯胶与聚丙烯酸酯压敏胶共混,制备了一种微观非均相、宏观均相的经皮给药系统,并考察了非均相结构对药物体外释放及透皮速率的影响。结果表明,阿拉伯胶含量为15%时可抑制载药量为5%的贴片中药物析晶,同时增加盐酸川芎嗪的体外释放与裸鼠皮肤的透过量,且阿拉伯胶的加入量对于贴片的黏附性无明显影响。

A novel microheterogeneous and macrohomogeneous transdermal delivery system loaded with ligustrazine hydrochloride was prepared by blending acrylic pressure-sensitive adhesive （PSA） with gum arabic （GA）. The effect of the structure of microheterogeneous matrix on the in vitro release and permeation profiles of the drug through the hairless mice skin were investigated. The results showed that 15 % GA could inhibit the drug to crystallize out in the patches containing 5 % ligustrazine hydrochloride, and increase the in vitro release and permeation amount. There was no significant effect of amount of GA on adhesive property of the patches.