经皮给药用热熔压敏胶的制备及其体外评价

 目的 制备供经皮给药用的热熔压敏胶,考察其贴剂的体外释放药物和透皮的性能。方法 以异戊二烯-苯乙烯-异戊二烯三嵌段共聚物（SIS）、C5加氢石油树脂、羊毛脂、液体石蜡、邻苯二甲酸二丁酯、2,6-二叔丁基对甲酚为材料,按正交法设计实验,以黏性、熔融温度、水蒸气透过率为指标,筛选经皮给药用热熔压敏胶的配方;以α-细辛醚为模型药物,考察所制备的热熔压敏胶贴剂的体外释放和透皮性能。结果 最佳的热熔压敏胶处方为异戊二烯-苯乙烯-异戊二烯三嵌段共聚物：C5加氢石油树脂-羊毛脂-液体石蜡-邻苯二甲酸二丁酯-2,6-二叔丁基对甲酚=100∶140∶20∶40∶20∶2。所得的热熔压敏胶体外释放α-细辛醚的速率高于普通热熔压敏胶。其透皮速率为（4.75±0.84）μg·cm^-2·h^-1,均高于普通热熔压敏胶和丙烯酸酯压敏胶。结论 本研究制备的热熔压敏胶性能优良,是制备经皮给药贴剂的良好材料。

Development of Hot Melt Pressure Sensitive Adhesive For Transdermal Use and in Vitro Evaluation

Objective To develop hot melt pressure sensitive adhesive (HMPSA) for transdermal use,and to investigate the in vitro drug release and permeation property of HMPSA based patches. METHODS HMPSA was prepared using styrene-isoprene-styrene triblock copolymer (SIS),C5 petroleum resin hydrogenate,lanoline,liquid paraffin,dibutyl phthalate,2,6-ditertbutyl-cresol as material under orthogonal design. The formulation of HMPSA was screened using stickiness,melt temperature and vapor permeation rate as index. The in vitro drug release behavior and transdermal property of the optimized HMPSA were evaluated using α-asarone as model drug. RESULTS The optimized formulation of HMPSA (HMPSA-OP) was followed as: SIS: C5 petroleum resin hydrogenate: lanoline: liquid paraffin: dibutylphthalate: 2,6-ditertbutyl-cresol=100:140:20:40:20:2. HMPSA-OP had shown more rapid drug release than ordinary HMPSA. And the in vitro transdermal flux of HMPSA-OP was （4.75±0.84）μg·cm^-2·h^-1,higher than that of ordinary HMPSA and acrylate PSA. CONCLUSION The HMPSA-OP shows good property and was suitable to prepare transdermal patch.