摘要
双嘧达莫溶解度具有较强的pH依赖性,在胃肠道内吸收不规则、生物利用度低且个体差异性大,采用固体分散技术改善双嘧达莫的体外溶解性。以L-型肠溶丙烯酸树脂(Eudragit L)、EC和PEG6000作为载体混合物。将药物与载体混和物的有机溶液喷洒于微晶纤维素(MCC)上制备成缓释微丸。利用X射线衍射,扫描电镜等方法研究固体分散物中双嘧达莫的晶体性质,考察不同pH条件下缓释微丸的释放特性。表明缓释微丸中药物的晶型消失,药物体外释放呈pH非依赖型释放特征,符合一级动力学方程。双嘧达莫经固体分散技术处理及载体混合物的调节,制成pH非依赖型缓释制剂。
The solubility of dipyridamole is pH-dependent, which produce irregular intestinal absorbance, low bioavailability and great inter individual variation. This study is to improve the in vitro dissolving ability of dipyridamole using solid dispersion method. Eudragit L ,PEG6000 and EC were used as drug carrier mixture. Sustained- release pellet was prepared by spraying organic solution of drug and carrier mixture onto micro crystal cellulose (MCC) pellets. By using X-ray diffraction and Scan Electronic Microscopy, the crystal characteristics of dipyri- damole in solid dispersion were investigated. The dissolution rates of the sustained-release pellet were determined under a series of pH values. The crystal form of DIP disappeared in the solid dispersion system. The release of DIP from sustained release pellets was pH-independent and the dissolution profiles followed the first grade model kinetics. Dipyridamole was made into pH-independent sustained release preparations after solid dispersion treatment and carrier mixture regulatory effect.
出处
《科学技术与工程》
2008年第9期2340-2343,共4页
Science Technology and Engineering
关键词
双嘧达莫
肠溶固体分散物
缓释微丸
dipyridamole enteric solid dispersion sustained release pellets