PVA-g-mPEG接枝聚合物的制备及其防药物滥用性能

Preparation and anti-drug abuse performance of PVA-g-mPEG graft polymer

阿片类药物的滥用问题日益严重,目前防滥用制剂局限在以往已有的技术,在开发新材料方向却少有报道,为此本文通过分子设计提出以接枝改性的方法制备一种具有防滥用性能的新型PVA-g-mPEG接枝聚合物。以聚乙烯醇(PVA)、单甲氧基聚乙二醇(mPEG)和环氧氯丙烷(ECH)为原料,采用两步反应合成法制备聚乙烯醇/单甲氧基聚乙二醇的接枝聚合物(PVA-g-mPEG),研究了反应温度对接枝率的影响。通过傅里叶红外光谱、核磁共振氢谱、差示扫描量热法以及X射线衍射法对产物进行表征。另外,以盐酸二甲双胍为模型药物,制备了接枝聚合物骨架片,考察了材料的防滥用性能。结果表明:随着接枝率的升高(43.44%,81.23%,120.48%),在水中20min时分别有28.3%、20.8%和12.9%的药物被提取,表明接枝聚合物具有一定的防滥用效果,对开发新的防滥用药的药用辅料具有较好的指导作用。

The abuse of opioids is becoming more and more serious.The abuse deterrent formulations are limited to the existing technologies,but there are few reports on the development of new materials at present.Therefore,a novel PVA-g-mPEG graft polymer with anti-abuse performance was prepared by grafting modification through molecular design.Polyvinyl alcohol/mono-methoxypolyethylene glycol graft polymer(PVA-g-mPEG)was prepared with polyvinyl alcohol(PVA),mono-methoxypolyethylene glycol(mPEG)and epichlorohydrin(ECH)by a two-step reaction method.The effect of reaction temperature on the grafting rate was studied.The graft polymer was characterized by FTIR,1H NMR,DSC and XRD.In addition,using metformin hydrochloride as model drug,the graft polymer matrix tablets were prepared,and the anti-abuse performance of the materials was investigated.The results showed that with the increase of grafting ratio(43.44%,81.23%,120.48%),28.3%,20.8%and 12.9%of drugs were extracted from water in 20min,respectively,which indicates that the graft polymer had a certain anti-abuse effect and good guiding effect on the development of new anti-abuse pharmaceutic adjuvant materials.