Rivastigmine凝膠化微乳劑經皮輸送系統之研究

Study of Rivastigmine-loaded Microemulsion-Based Gel for Transdermal Drug Delivery

蔡姈君(Ling-Chun Tsai)

指導教授 ： 吳寶珠

高雄醫學大學/藥學院/藥學系碩士班/碩士(2017年)

摘要

Rivastgimine是一種乙醯膽鹼抑制劑，用於治療輕至中度阿茲海默症所造成之癡呆症。Rivastigmine可經由口服吸收，但受到肝臟首渡代謝影響，導致生體可用率低下，且易造成噁心嘔吐等腸胃道不適副作用，若改使用經皮投予途徑將可避開首渡代謝，也因不經過腸胃道而能減少副作用的發生。
本篇研究主要目的為發展之凝膠化微乳劑作為藥物載體，用於提升Rivastigmine經皮投予的穿透性與便利性。凝膠化微乳劑不僅具有微乳劑特性如熱穩定、提升穿透力與增加溶解度，且製作過程簡便，另外因黏稠度的增加，使劑型附著於皮膚的時間增長，進而提高藥物的使用範圍。
結果顯示在微乳劑配方中以藥物穿透量最多的F8為最佳配方；以Carbopol 934製成之凝膠化微乳劑，能順利成形且最為安定，並具有相對高的藥物穿透量，因此，使用此劑型為藥物載體以經皮輸送系統投予，可提升Rivastigmine的穿透能力與皮膚附著力，並使之有更廣泛的應用。

關鍵字

Rivastigmine ； 微乳劑 ； 凝膠化微乳劑 ； 經皮吸收

並列摘要

Rivastigmine is a reversible cholinesterase inhibitor which is used to treat mild to moderate dementia of Alzheimer’s disease and Parkinson’s disease. However, Rivastigmine may cause some gastrointestinal adverse effects like vomiting and nausea by oral administration. Hence, transdermal administration route is a suitable way to reduce the side effects. Microemulsions have been widely used for their advantages such as easily preparation, enhancement of penetration and thermodynamically stable. Previous studies also have mentioned that microemulsions can improve the bioavailability of drugs. Microemulsion-based gel can be prepared by adding thickening agent, in order to increase the viscosity and improve the ability of remaining on skin. The aim of this study was to develop and evaluate microemulsion-based gel for transdermal delivery of Rivastigmine.
In this study, different kind of oil, surfactant and cosurfactant were used to prepare drug-loaded microemulsions. Microemulsion with different ratio of components were prepared and evaluated to find the best formulation. The results showed that F8 had the highest skin permeation capacity. After adding Carbopol 934, F8 microemulsion-gel was stable. When containing 3 % Rivastigmine, the formulation had higher penetrative amount compared to commercial product. These results showed that F8 microemulsion-gel is a promising carrier for transdermal administration of Rivastigime.

並列關鍵字

Rivastigmine ； Microemulsion ； Microemulsion based-gel ； Drug transdermal delivery system

參考文獻

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