湿法研磨技术提高硝苯地平溶出度的研究  

Improved dissolution of nifedipine by wet milling

作　　者：于红霞[1] 张宁[1] 唐星[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药剂学杂志（网络版）》2014年第4期25-32,共8页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的采用湿法研磨技术,对硝苯地平做速释化处理。方法比较了聚乙二醇(polyethylene glycol,PEG),泊洛沙姆(poloxamer,F68),羟丙基甲基纤维素(hydroxypropyl methylcellulose,HPMC),聚维酮(povidone,PVP)4种常用水溶性辅料与硝苯地平共研磨物的溶出度,粒径分布,并运用差式扫描量热法(differential scanning calorimetry,DSC)及X射线衍射法(X-ray diffraction,XRD)对研磨后的药物物理性质做了鉴别。此外,对HPMC研磨液的室温稳定性做了测定。结果经湿法共研磨后,硝苯地平的粒径显著减小,溶出加快,但是药物晶型经研磨后并未发生变化。HPMC研磨液室温放置两个月溶出未发生变化。结论湿法共研磨技术能显著增加难溶性药物硝苯地平的溶出度,进而有望解决其生物利用度低的问题。Objective To improve dissolution of nifedipine, wet milling method was applied. Methods nifedipine was coground with four common hydrophilic excipients, polyethylene glycol(PEG), poloxamer(F68), hydroxypropyl methylcellulose(HPMC) and povidone(PVP), respectively. Next, the dissolution, size distribution of these cogrounds were compared.Moreover, the physical properties of cogrounds were determined using differential scanning calorimetry(DSC) and powder X-ray diffraction(XRD). Followed, the stability of coground with HPMC at room temperature was investigated. Results The particle size of drug decreased and dissolution rate was enhanced after wet milling. However, the crystalline morphology of cogrounds was unaltered after grinding. Also, after two months storage at room termperature, the coground with HPMC was unchanged in dissolution. Conclusion Wet grinding process offers an alternative approach to improve the dissolution of poorly water soluble nifedipine, thereby, enhances the bioavailability of the drug potentially.

关 键 词：药剂学 湿法研磨物 溶出对比 硝苯地平 粒度分布 DSC XRD 

分 类 号：R[医药卫生]