复方盐酸特比萘芬贴剂的制备与体外透皮性能研究

Preparation of compound terbinafine hydrochloride patch and its in vitro percutaneous permeability

目的制备复方盐酸特比萘芬压敏胶贴剂,并对其体外透皮性能进行研究。方法采用改良Franz扩散池,以离体大鼠皮肤为屏障进行经皮渗透试验,高效液相色谱法测定盐酸特比萘芬和酮康唑不同时间点、不同接收液中的体外皮肤透过量,并对药物在不同时间的皮肤局部贮药量进行测定。结果 24 h内盐酸特比萘酚的体外皮肤透过率低于0.05%,酮康唑的皮肤透过率低于2%,盐酸特比萘芬皮肤贮药量24 h为8.763μg/cm2,酮康唑为20.86μg/cm2,且在72 h内皮肤贮药量呈增加趋势。结论所制得的复方盐酸特比萘芬贴剂可发挥局部长效的治疗作用,有望开发为长效经皮给药制剂。

Objective To prepare terbinafine hydrochloride and ketoconazole drug-in-adhesive patches and evaluate its in vitro percutaneous permeability. Methods The permeation characteristics was evaluated by using modified Franz diffusion cell fitted with mouse skin. The content of terbinafine hydrochloride and ketoconazole in different receiving solution at different time was determined by HPLC. The dermal loading quantity of terbinafine hydrochloride and ketoconazole at different time was also determined. Results The transdermal amount of terbinafine hydrochloride was below 0. 05% and the transdermal amount of ketoconazole was below 2% in 24 h. The dermal loading quantity of terbinafine hydrochloride and ketoconazole was 8. 763 μg / cm2 and 20. 86 μg / cm2 in 24 h. The dermal loading quantity increased in 72 h. Conclusion The prepared compound terbinafine hydrochloride patches can play a role in the region effect,and it has good potential for long-time transdermal delivery.