热熔压敏胶中药物释放性能的研究

Release Characterization of Drugs in Hot-melt Pressure Sensitive Adhesive

目的考察不同性质药物在苯乙烯-异戊二烯-苯乙烯(SIS)热熔压敏胶中的释放性能,研究热熔压敏胶的适用药物范围。方法以SIS热熔压敏胶为基质,分别制备隐丹参酮、α-细辛醚、咖啡因、槲皮素、黄芩苷、氢溴酸高乌甲素、盐酸青藤碱的胶黏分散型贴剂,以60%乙醇溶液为释放介质,于单室扩散池中测定各种药物的释放;使用差示扫描量热法(DSC)分析隐丹参酮、黄芩苷与热熔压敏胶的相容性。结果SIS热熔压敏胶贴剂的药物释放行为符合Higuchi方程;药物在热熔压敏胶中释放的速率与药物的亲脂性有关,高亲脂性药物释放快;热熔压敏胶与高亲脂性的隐丹参酮相容性良好,与低亲脂性的黄芩苷不相容。结论SIS热熔压敏胶适于制备高亲脂性药物的胶黏分散型贴剂。

OBJECTIVE To investigate the release behavior of drugs with different physico-chemical properties in styrene-isoprene-styrene （SIS） hot-melt pressure sensitive adhesive （HMPSA）, and to evaluate the applicability of HMPSA in dermal patches. METHODS Adhesive dispersion-type patches which containing cryptotanshinone, α-asarone, caffeine, quercetin, baicalin, sinomenine hydrochloride, lappaconitine hydrobromide were prepared using SIS HMPSA, respectively. The release experiments was carried on single chamber diffusion cell using 60% ethanol solution as release media. The effects of the type of adhesive and the content of drugs on release rate were evaluated. The compatibility of HMPSA with cryptotanshinone and baicalin was also studied by differential scanning calorimetry （DSC）. RESULTS The drug release behavior of HMPSA patches followed Higuchi equation. The release rate of patches was related with the drug properties. High lipophilic drugs were showed higher release rates. The HMPSA had good compatibility with high lipophilic cryptotanshinone, while low lipophilic baicalin was incompatibility. CONCLUSION The SIS HMPSA is a suitable and compatible pressure sensitive adhesive for the development of transdermal drug delivery systems for high lipophilic drugs.