长春西汀透皮贴剂的研制及体外释药机理的探讨

Preparation of vinpocetine transdermal therapeutic system and study on in vitro permeation mechanism

目的 :制备长春西汀透皮贴剂 ,研究其体外释药机理。方法 :在单层贴剂优化处方的基础上制备了单层、双层和三层贴剂 ,比较不同类型贴剂经不同皮肤的体外渗透速率 ,对三层贴剂进行了质量考察并研究了其释药机理。结果 :三层贴剂和双层贴剂的经皮渗透量大于单层贴剂。去除角质层的皮肤对药物经皮渗透的屏障作用明显小于完整皮肤。结论 :长春西汀贴剂质量可控 ,刺激性小 ,药物经皮吸收的主要屏障为角质层 ,在经皮渗透中有较微弱的储库效应 ,其渗透行为主要是零级释药模式。

OBJECTIVE To prepare the matrix-type vinpocetine transdermal therapeutic system and study the permeation mechanism. METHODS Basing on the optimized formulation of single-layered patch, single-layered,double-layered and triple-layered patch were developed. In vitro permeation studies using franz diffusion cell were carried out to compare the transdermal delivery of vinpocetine from different types of patch. Quality of triple-layered patch was examined and the permeation mechanism of vinpocetine by changing the skin condition was also studied. RESULTS The permeated amounts of vinpocetine from triple-layered patch and double-layered patch were higher than those from single-layered patch. The barrier effect of stripped stratum corneum was highly less than that of whole skin. CONCLUSION The patch of vinpocetine is well qualified without skin irritation. The transdermal barrier of vinpocetine is mainly in the stratum corneum and the deposit functionis not obvious. In vitro skin permeation of vinpocetine conforms to the zero-order behavior.