两种介孔硅材料对布洛芬控制释放的比较研究

发布时间：2018-04-27 00:05

本文选题：布洛芬 + 控制释放　；参考：《南华大学》2015年硕士论文

【摘要】：布洛芬是世界普遍公认的非甾体解热镇痛药,而控制释放系统可以最大限度地发挥其在人体内的药物活性,并减少给药剂量。早期合成的介孔材料孔道不规则,孔径分布不均匀,使其在药物控制释放方面的应用受到了很大程度地限制。采用凝胶-溶胶法合成的MCM-41介孔硅材料具有更多的孔洞特性和微粒形态,其孔内可以负载药物分子,表面可以通过改性组装功能性分子;并通过不同的外来刺激影响其表面理化性质以控制功能分子对二氧化硅孔洞的打开和闭合,进而实现控制释放孔洞中药物分子的目的。本文采用凝胶-溶胶法并添加有机扩孔剂,制备了MCM-41与MCM-41-Epoxy两种介孔二氧化硅材料,以制得的介孔二氧化硅为载体,进行介孔二氧化硅对布洛芬控制释放的比较研究。具体研究内容如下:(1)介孔二氧化硅材料的合成与表征。碱性条件下,用CTAB(十六烷基三甲基溴化铵)作为模板剂与TEOS(正硅酸乙酯)发生反应,加入1,3,5-三甲苯扩孔,反应完成后采用酸洗法去除模板,制备了具有较大孔径的MCM-41介孔硅材料。在此基础上,将制得的MCM-41环氧基功能化。以无水甲苯为反应介质,将MCM-41与硅烷偶联剂KH560(γ-缩水甘油醚氧丙基三甲氧基硅烷)高温反应,制备了环氧基功能化的MCM-41-Epoxy材料。将两种材料进行红外、扫描电镜、X射线粉末衍射、氮气吸附脱附等一系列表征,结果表明,环氧基的特征峰在910cm-1附近,MCM-41材料比表面积(SBET)、孔容V/(cm3.g-1)以及孔径(D/nm)、XRD的衍射峰值均大于MCM-41-Epoxy。(2)负载布洛芬及其控制释放的研究。将两种材料放入高浓度的布洛芬溶液中充分吸附,直至溶液的紫外吸收吸光度不再发生变化。计算出MCM-41与MCM-41-Epoxy两种介孔材料对布洛芬的负载率,分别为18.92%和27.36%。通过模拟两种人体体液p H环境对MCM-41-Epoxy-IBU中布洛芬释放率的研究,最终选择p H为7.4的PBS缓冲溶液作为应激物,构建控释系统。经比较研究,MCM-41对布洛芬的释放速度较快,经约9h释放量达到80%以上。而MCM-41-Epoxy释放较缓慢,24h后达到65%左右的释放量。
[Abstract]:Ibuprofen is widely recognized as a nonsteroidal antipyretic analgesics, and the controlled release system can maximize its drug activity in human body and reduce the dosage of the drug. The irregular pore channels and uneven pore size distribution of the early synthesized mesoporous materials limited their application in drug controlled release to a large extent. The MCM-41 mesoporous silicon materials synthesized by gel-sol method have more pore characteristics and particle morphology, which can be loaded with drug molecules in their pores, and functional molecules can be assembled on the surface by modification. In order to control the opening and closing of Sio _ 2 pores by different external stimuli, the surface physicochemical properties can be controlled, and the aim of controlling the release of drug molecules in the pores can be achieved. In this paper, two kinds of mesoporous silica materials, MCM-41 and MCM-41-Epoxy, were prepared by gel-sol method and organic reaming agent. The controlled release of ibuprofen from mesoporous silica was studied by using mesoporous silica as carrier. The main contents are as follows: 1) Synthesis and characterization of mesoporous silica. In alkaline condition, CTAB (cetyltrimethylammonium bromide) was used as template agent to react with TEOS (ethyl orthosilicate), adding 1k3ttrimethylbenzene to dilatate the pores. After the reaction was finished, the template was removed by acid washing method. MCM-41 mesoporous silicon with large pore size was prepared. On this basis, the MCM-41 epoxy group was functionalized. Epoxy functional MCM-41-Epoxy materials were prepared by high temperature reaction of MCM-41 with silane coupling agent KH 560 (纬 -glycidyl propyl trimethoxysilane) in anhydrous toluene as reaction medium. Two kinds of materials were characterized by IR, SEM X-ray powder diffraction, nitrogen adsorption and desorption. The specific surface area of MCM-41 material near 910cm-1, the pore volume V / P cm3.g-1) and the peak diffraction peak of the pore size D / N ~ (-1) are all larger than those of MCM-41-Epoxy.P-2) loaded ibuprofen and their controlled release. The two materials were fully adsorbed in a high concentration ibuprofen solution until the UV absorbance of the solution was no longer changed. The loading rates of two mesoporous materials, MCM-41 and MCM-41-Epoxy, for ibuprofen were 18.92% and 27.36, respectively. The release rate of ibuprofen in MCM-41-Epoxy-IBU was studied by simulating two kinds of human body fluid pH environment. Finally, PBS buffer solution with pH 7.4 was selected as stress substance to construct controlled release system. The release rate of ibuprofen by MCM-41 was faster than that of MCM-41, and the release rate of ibuprofen reached more than 80% after about 9 hours. However, the release of MCM-41-Epoxy was about 65% after 24 hours of release.
【学位授予单位】：南华大学
【学位级别】：硕士
【学位授予年份】：2015
【分类号】：TQ460.1;TQ127.2

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