苯磺酸氨氯地平乳剂凝胶的制备及其体外透皮吸收的考察

Preparation of amlodipine besylate emulgels for transdermal administration and its percutaneous permeability in vitro

目的:制备苯磺酸氨氯地平乳剂凝胶,考察不同透皮吸收促进剂对其体外透皮吸收的影响。方法:选择4种不同基质制备苯磺酸氨氯地平乳剂凝胶,优化处方;采用立式改良Franz扩散池,优选接受介质,研究卵磷脂、萜烯类化合物、氮酮3类促进剂对苯磺酸氨氯地平乳剂凝胶体外小鼠模型透皮释放的影响。结果:最佳凝胶基质为25%泊洛沙姆F127,最佳透皮吸收促进剂为2.5%卵磷脂,苯磺酸氨氯地平乳剂凝胶的累积渗透量Q24h达到(148.69±39.92)μg·cm-2,JS为(6.19±1.66)μg·cm-2·h-1。结论:2.5%卵磷脂作为苯磺酸氨氯地平乳剂凝胶渗透效果良好,为今后开发经皮给药制剂提供理论基础。

Objective： To prepare a suitable emulgel formulation of amlodipine besylate and investigate its percutaneous permeation using rat skin and diffusion cell technique. Methods： Emulgels of amlodipine besylate were prepared by four types gelling agents. The effects of three types of penetration enhancers including lecithin,terpenes and azone on transdermal permeation of the drug were evaluated. Results： The formulation prepared using Pluronic F127 showed desirable characteristics and appearance. Amlodipine besylate emulgels using lecithin as the enhancer showed highest cumulative amount（ Q24h） of（ 148. 69 ± 39. 92） μg·cm- 2and fluxrate of（ 6. 19 ± 1. 66）μg·cm- 2·h- 1. Conclusion： The prepared amlodipine besylate emulgels have a good potential for transdermal delivery.