摘要
目的以硝苯地平为模型药制备固体分散体,考察共聚维酮(PVP/VA),乙酸羟丙甲纤维素琥珀酸酯(HPMCAS)和羟丙甲纤维素(HPMC)对固体分散体中药物分散状态和溶出度的影响。方法采用热熔挤出技术(HME)制备了不同载体的硝苯地平固体分散体,以差示扫描量热法(DSC)测定了药物在其中的分散状态,并测定体外溶出度。结果药物与载体材料在1∶2至1∶4时,硝苯地平均以无定型态存在于热熔挤出物中。载体材料为乙酸羟丙甲纤维素琥珀酸酯时,各固体分散体在30min的溶出度即可达到100%。共聚维酮为载体材料时,30 min的溶出度最高只有约75%,加入5%的羟丙甲纤维素E5后可将溶出度提高至90%以上。结论乙酸羟丙甲纤维素琥珀酸酯单一聚合物或共聚维酮与羟丙甲纤维素E5的聚合物组合都是制备硝苯地平固体分散体的良好载体材料。
OBJECTIVE To investigate the effect of copovidone（ PVP / VA）,hydroxypropylmethylcellulose acetate succinate（ HPMCAS） and hydroxypropylmethylcellulose（ HPMC） on drug dispersion and in vitro dissolution of solid dispersion by using nifedipine as model drug. METHODS Nifedipine solid dispersion was prepared by hotmelt extrusion（ HME） technology,and the drug dispersion was evaluated by differential scanning calorimetry（ DSC） and dissolution test. RESULTS DSC analysis results showed that nifedipine was amorphous in all HME extruders. Drug release from solid dispersion prepared with HPMCAS reached 100% in 30 min,but was only 75% for PVP / VA solid dispersion. Adding 5% HPMC E5 to PVP / VA extruders before dissolution test could raise the drug release from 75% to 90%. CONCLUSION HPMCAS or combination of PVP / VA and HPMC E5 are desirable polymers for nifedipine solid dispersion.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2016年第8期635-638,共4页
Chinese Pharmaceutical Journal
关键词
硝苯地平
固体分散体
溶出度
热熔挤出
nifedipine
solid dispersion
dissolution
hot melt extrusion
