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中药浸膏贴片用环氧化SIS热熔压敏胶的制备及其性能研究
Study on the Preparation and Performance of Epoxidized SIS HMPSA for Chinese Medical Extract Patch
【作者】 高轶;
【导师】 张军营;
【作者基本信息】 北京化工大学 , 化学, 2011, 硕士
【摘要】 针对目前透皮吸收制剂辅料的缺乏以及传统制剂在使用性能上的不完善,本文以环氧化SIS为基体树脂制备医用热熔压敏胶,利用基体分子橡胶段中双键转化成环氧基后分子极性的增加,提高压敏胶的力学性能,药物相容性和生物相容性,将其应用于中药浸膏贴片领域,提高了贴片的粘附性、载药量和透气性,具有重要的使用价值和应用前景。主要工作如下:以ESIS为基体树脂,环氧大豆油为增塑剂和高度氢化松香为增粘树脂,制备出一种ESIS热熔压敏胶。采用正交实验法和载药量试验法优选出制备中药贴片用ESIS热熔压敏胶的最佳配方。结果表明:当m(ESIS):m(环氧大豆油):m(高度氢化松香):m(抗氧剂1010)=100:80:100:1.4时,ESIS热熔压敏胶的综合性能满足中药贴片的使用要求,并且其最大载药量(34%)和水蒸气透过率[1.297g/(m2·d)]均高于同类产品(SIS医用压敏胶和传统天然橡胶膏)。研究了ESIS的环氧值、苯乙烯含量、助剂用量以及载药量对ESIS热熔压敏胶及贴片力学性能的影响。结果表明:在实验范围内,环氧值的增加,提高了嵌段共聚物橡胶相溶度参数,分子间作用力和分子极性的提高有助于其力学性能的提高;苯乙烯含量大的ESIS压敏胶力学性能较高;压敏胶的初粘力和剥离强度随着增粘树脂或增塑剂用量的不断增加均出现先增大后减小现象;载药量的增加使贴片剥离强度和持粘力呈下降趋势。对基体树脂ESIS与助剂共混物的相态结构和ESIS热熔压敏胶的热氧稳定性进行了研究,积累了丰富的实验数据,对其进一步的实际应用具有一定的指导意义。
【Abstract】 For the lack of the adjuncts of transdermal drug delivery system currently and the imperfect use performance of traditional preparation, in this paper, using epoxidized styrene-isoprene-styrene block copolymer as the matrix resin for the preparation of hot-melt pressure-sensitive medical adhesives, the polarity of substrate molecule increased with the double bonds of rubber segment in substrate molecule being oxidized, improving the mechanical properties, drug compatibility and biocompatibility of the pressure-sensitive adhesive. Being applied in the field of Chinese medical extract patch, enhanced the adhesion of the patch, the drug loading and the permeability, and had significant value in use and application prospects.The main tasks were as follows:Using ESIS as the matrix resin, epoxy soybean oil as the plasticizer, highly hydrogenated rosin as the tackifier, synthesized a ESIS based hot-melt pressure-sensitive adhesives(HMPSA). The best formula of preparing ESIS based hot-melt pressure-sensitive adhesives used in Chinese medical extract patch was optimized by Orthogonal design and drug-loading experiment. The Experimental results showed that when ESIS:epoxy soybean oil:highly hydrogenated rosin:antioxidant 1010 was 100:80:100:1.4(mass fraction),the comprehensive properties of the ESIS based hot-melt pressure-sensitive adhesives could satisfied on the need of Chinese medical extract patch. Both the drug load content (34%) and the water vapor permeability [1.297 g/(m2·d)] were higher than similar products(SIS based hot-melt pressure-sensitive adhesives and traditional natural rubber plaster).The influence of the content of epoxy group of ESIS, styrene content, assistant content and the drug loading rate on the mechanical properties of the ESIS based hot-melt pressure-sensitive adhesives were investigated. The results indicated that as the increase of the content of epoxy group, the solubility parameter of the rubber in block copolymers became bigger.Inter-molecular forces and molecular polarity of the experimental product increased,and helped enhancing its mechanical properties. High styrene content also improved the mechanical properties. Both the initial adhesive strength and peel strength of the pressure-sensitive adhesive increased first, and then decreased with the increasing of the amount of tackifier and plasticizer. Peel strength and holding power descended with the amount of Chinese medical extract increasing. The micro phasal structure of the blends with matrix resin ESIS and the assistant was studied as well as the thermal oxidation stability of ESIS based hot-melt pressure-sensitive adhesives, accumulating rich experimental data, determinately guiding the technicalinnovation and application in this domain.