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经皮给药压敏胶和水凝胶材料的制备与性能

Synthesis and Properties of Press Sensitive Adhesives and Hydrogel for Transdermal Drug Delivery Systems

【作者】 张斌

【导师】 董岸杰;

【作者基本信息】 天津大学 , 材料学, 2007, 硕士

【摘要】 经皮给药具有诸多优点,是现代给药制剂一大发展方向,但目前我国经皮给药制剂所用辅料严重缺乏,极大限制了该剂型的发展,本论文对适于皮肤用的亲水性非离子聚氨酯压敏胶及两类聚乙烯醇(PVA)凝胶基质进行了研究,期望制得新型经皮给药制剂的适宜基质。非离子聚氨酯压敏胶是由二异氰酸酯与多元醇的混合物进行反应,生成预聚体,再经扩链制得。论文考察了异氰酸酯的种类、反应温度、时间及原料配比等因素的影响,确定了工艺稳定、产品性能优良的亲水性聚氨酯压敏胶的配方及制备工艺。采用斜坡滚球停止法、180°剥离、持粘力测试等方法对一些影响压敏胶力学性能的因素进行了考察。采用Franz扩散池对载药压敏胶贴剂的经皮药物释放行为进行了体外考察。结果表明,该聚氨酯压敏胶贴剂具有良好的力学性能及药物控释能力,适用于经皮给药系统。本论文分别采用硼砂和正硅酸乙酯为交联剂,制备出了Ⅰ型和Ⅱ型PVA凝胶。考察了两类凝胶的力学性能与溶胀性能和各影响因素;对两类凝胶进行了透皮释放实验,研究了它们与药物的相容性及经皮给药性能。结果表明,Ⅱ型PVA凝胶在力学性能(如强度、韧性等方面)和溶胀性能上优于Ⅰ型PVA凝胶,其药物释放速率略低于Ⅰ型PVA凝胶。

【Abstract】 Transdermal drug delivery system (TDDs) has received much attention in drug release because of several advantages. The serious lack of polymer materials used in TDDs is a big bottle-neck problem embarrassing the development of TDDs. In this paper the skin compatible hydrophilic polyurethane pressure sensitive adhesives (PSAs) and two types of polyvinyl alcohol (PVA) hydrogel were studied in order to developed new materials for TDDs.The hydrophilic polyurethane PSAs were synthesized by polyaddition of polymer glycol, diisocyanate and extender. The effects, such as the kinds of the diisocyanates, the temperature, the reaction time and the ratios of the materials on the productions, were studied carefully in this work. The methods of rolling boll at a slope, peeling at 180°angle and cohesion test were used to evaluate the mechanical properties of PSAs. The transdermal drug delivery properties of the prepared PSAs were evaluated invitro by Franze diffuse method. The study results indicated that the hydrophilic polyurethane PSAs prepared in this paper show good mechanical and drug delivery properties, which suit for the TDDs application.Two types of PVA hydrogels, PVA-Ⅰand PVA-Ⅱ, were prepared by using borax and tetraethoxysilanes (TEOS) as crosslinkers. The mechanics and swelling behavior of the two gels, as well as their influence factors, were investigated. The transdermal release experiments were also performed in order to evaluate the drug compatibility and control drug release problem. The study results show that PVA-Ⅱhydrogel presents better performance in mechanics and swelling properties than PVA-Ⅰ, while PVA-Ⅰshows lightly higher drug release rate.

  • 【网络出版投稿人】 天津大学
  • 【网络出版年期】2009年 04期
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