尼美舒利固体分散体的非pH依赖性释放研究pH-independent drug release of nimesulide from solid dispersions
袁园,张莉,陈莉
YUAN Yuan1,2,ZHANG Li1
摘要(Abstract)：
目的以尼美舒利为难溶弱酸性模型药物,研究提高该类药物释放速率的方法。方法以聚乙二醇6000(PEG6000)为载体,采用熔融法制备尼美舒利固体分散体;测定含不同碱化剂(包括NaOH、KOH、Ca(OH)2、Na2CO3、CaCO3)的尼美舒利固体分散体中药物的释放速率。结果加入碱化剂能显著增加尼美舒利在蒸馏水中的释放度,碱化剂不同,药物的释放度不同;碱化剂的碱性越强,分散体的颜色越深,其吸湿性也相对越大。结论在尼美舒利PEG6000固体分散体中加入碱化剂可显著改善该类药物的体外释放特点,并呈现明显的非pH依赖性。
Objective To prepare solid dispersion with alkalizers for a representative poorly water-soluble and weakly acidic drug,nimesulide,and determine its dissolution property.Methods The solid dispersions(SDs)were prepared with drug and polyethylene glycol 6000(PEG6000)without or with alkalizers using the hot melt method.The dissolution rates of drug from SDs containing alkalizers including NaOH,KOH,Na2CO3,CaCO3 and Ca(OH)2 were determined.Results The dissolution rates of drug from SDs containing alkalizers were more pronounced when compared with the physical mixtures and raw powder,especially in distilled water.Conclusions It is evident that the alkalizers in SDs may maximize the dissolution rate of poorly water-soluble weakly acidic drug like nimesulide,thus result in pH-independent drug release.
关键词(KeyWords)：
难溶弱酸性药物;碱化剂;固体分散体;尼美舒利;聚乙二醇;释放速率;pH调节
poorly water-soluble weakly acidic drug;alkalizer;solid dispersion;nimesulide;polyethylene glycol;dissolution rate;pH modulation
基金项目(Foundation):
作者(Author):
袁园,张莉,陈莉
YUAN Yuan1,2,ZHANG Li1
DOI: 10.14066/j.cnki.cn21-1349/r.2012.02.018
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