疏水缔合水溶性聚合物P(DMDAAC-NVP-IOA)与萘普生相互作用及释药性  

Interactions of Hydrophobically Associating Poly(DMDAAC-NVP-IOA) with Naproxen and Its Drug Release Characteristics

作　　者：王新龙[1] 张跃军[1] 

机构地区：[1]南京理工大学化工学院,南京210094

出　　处：《应用化学》2008年第12期1393-1398,共6页Chinese Journal of Applied Chemistry

基　　金：国家科技攻关项目(2003BA327C)

摘　　要：以水为介质，采用自由基胶束聚合制备了二甲基二烯丙基氯化铵（DMDAAC）、N-乙烯基吡咯烷酮（NVP）和丙烯酸异辛酯（IOA）三元共聚疏水缔合水溶性聚合物P（DMDAAC-NVP-IOA），测定了聚合物的聚电解质性质和疏水缔合性质。应用IR、XRD、DSC测试技术研究了各组分的相互作用。结果表明，所制备的P（DMDAAC-NVP—IOA）同时具有聚电解质和疏水缔合特性。随P（DMDAAC-NVP-IOA）量增加，IR分析中萘普生羧基的羰基伸缩振动峰1684cm^-1处峰变宽、强度明显减弱：XRD分析中的12°～29°间衍射峰逐渐变宽、变小直至消失；DSC分析中只有1个转变曲线，P（DMDAAC-NVP—IOA）与萘普生之间存在分子级相互作用。在pH=7．4磷酸盐缓冲液中，疏水缔合水溶性聚合物具有药物缓释特性，可用扩散－溶解模型进行最佳拟合。Poly （DMDAAC-NVP-IOA） was prepared from dimethyldiallylammonium chloride （ DMDAAC ）, N-vinyl pyrrolidone （NVP） and isooctyl acrylate （IOA） via radical micellar polymerization in water. The polyelectrolyte and hydrophobic association properties of the polymer were studied. The interactions of P（DMDAAC-NVP-IOA） with naproxen were investigated by IR, XRD and DSC. As the amount of P（DMDAAC-NVP-IOA） increased, the peak at 1 684 cm^-1 assigned to the carbonyl of naproxen became broader and the peak intensity decreased. The diffraction peaks between 12° and 29° in the XRD pattern also became wider and even disappeared. There was only one transition observed by DSC with the increase of the amount of the polymer. All these results suggest the presence of interactions at molecular level between P（DMDAAC-NVP-IOA） and naproxen. Sustained-release tablets by naproxen were prepared from the copolymer and naproxen, and the drug release results suggest that the sustained-release tablets in the presence of P（DMDAAC-NVP-IOA） exhibit excellent properties in phosphate buffer, and the kinetics can be fit to a diffusion-erosion model.

关 键 词：疏水缔合 水溶性聚合物 萘普生 缓释 

分 类 号：O633[理学—高分子化学] TB39[理学—化学]