咪达那新凝胶的制备及其体外经皮透过性

Preparation and in vitro transdermal penetration of imidafenacin gels

目的制备咪达那新凝胶,考察药物的体外经皮透过性,探讨咪达那新经皮给药的可行性。方法制备了以羟丙纤维素为胶凝剂的咪达那新水-醇凝胶。采用水平扩散池,以大鼠腹部全皮为渗透膜,筛选经皮通透促进剂;采用Franz扩散池,分别用微孔滤膜和大鼠腹部全皮为渗透膜,研究咪达那新凝胶剂的药物释放和体外经皮通透性。结果 Azone、油酸和肉豆蔻酸异丙酯等对咪达那新的经皮通透性有较好的促进效果。咪达那新凝胶中,乙醇、1,2-丙二醇和Transcutol P在一定浓度范围内对药物累积经皮通透量无显著影响,促渗剂azone能显著增加药物的累积经皮通透量。结论 Azone作为渗透促进剂加入咪达纳新凝胶剂中,可显著增加药物的经皮透过性,咪达那新经皮给药制剂的研发具有可行性。

Objective To prepare imidafenacin gel, investigate the penetration of imidafenacin through rat skin in vitro, and discuss the potential of transdermal delivery of imidafenacin. Method The imidafenacin hydro-alcoholic gels were prepared using HPC as the gelling agent, and horizontal diffusion cell method was used to screen the permeation enhancer through full-thickness rat skin; The in vivo drug release and transdermal penetration of imidafenacin were investigated with Franz diffusion cells using microporous membrane and rat skin as the permeation membrane, respectively. Results The Azone and oleic oil showed the optimum enhancement in penetration. The contents of ethanol, PG and Transcutol P in the gels had little influence on the permeation of imidafenacin, while Azone, as an enhancer, could promote the accumulated penetration remarkably. Conclusion Of the penetration enhancers investigated, Azone was found to improve notably the transdermal penetration of imidafenacin, and our studies indicated potential of transdermal delivery of imidafenacin.