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[摘要]
目的 制备白芷香豆素储库型贴剂,考察其体外释药特性和离体皮肤渗透性,筛选有效的透皮吸收促进剂,提高白芷香豆素的透皮吸收速率。方法 选取羟丙甲纤维素为储库介质,以乙烯-醋酸乙烯共聚物膜为控释膜,制备白芷香豆素储库型透皮贴剂。用Franz扩散池进行乳猪离体皮肤渗透实验,用HPLC测定欧前胡素量,考察凝胶用量、药物用量、促渗剂对药物透皮速率的影响,并对优选的贴剂进行体外释放研究。结果 最佳处方为1%羟丙基甲基纤维素(HPMC)、1%白芷香豆素、3%肉豆蔻酸异丙酯、3%氮酮;由该处方制得的贴剂稳态透皮速率(Js)达到0.713 μg/(cm2∙;h),体外释放速率接近零级。结论 储库型白芷香豆素贴剂有较高的经皮渗透速率,体外释药完全,有望成为新型的透皮制剂。
[Key word]
[Abstract]
Objective To prepare the reservoir patch of coumarins in Angelicae Dahuricae Radix and investigate its release and transdermal absorption characteristics in vitro. The efficient enhancers were chosen to improve the drug's permeation rate. Methods The reservoir patch was prepared using hydroxypropyl methylcellulose (HPMC) as medium and ethylene vinyl acetate (EVA) membrane to control the release of drug. The Franz diffusion cells were used and HPLC was used to determine imperatorin content and permeation rate. The content of imperatorin was determined by HPMC. The effect of the gel consumption, the content of coumarins and penetration enhancer on the transdermal flux were investigated by selecting porcine skin as model. The release of the selected patch in vitro was investigated. Results 1% HPMC, 1% coumarins in Angelicae Dahuricae Radix, 1% Isopropyl Myristate (IPM) and 3% Azone were the best permeation of the patch. The permeation rate reached 0.713 μg/(cm2·h). The release mechanisms of the patch in vitro coincided with zero-order kinetic. Conclusion The reservoir patch of coumarins in Angelicae Dahuricae Radix had high transdermal rate and complete in vitro release. It was indicated that the patch could be expected to be an effective transdermal drug delivery system.
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[基金项目]
浙江省杭州市卫生科技计划项目(2013A47)