摘要
目的:采用溶剂-冷冻干燥法制备硝苯地平(nifedipine,NF)速释固体分散体(SD)来提高其体外溶出度,并通过添加碱性调节剂来调节溶出微环境的pH值,进一步提高SD中药物的溶出速率。方法:以原料药在各辅料水溶液的溶解度及固体分散体的体外溶出度为指标,从聚乙烯吡咯烷酮K30(PVPK30)、羟丙甲基纤维素(HPMC)、泊洛沙姆407(Poloxamer 407)中筛选最优载体及其比例,并添加适量的碳酸钠(Na_2CO_3)来进一步调节溶出速率。结果:当以PVPK30为载体,Na_2CO_3为碱性调节剂,且NF:PVPK30:Na_2CO_3=30mg:150mg:9mg时,制备的SD中药物的溶出速率显著提高,在2h内累积溶出度百分率可达84%。
OBJECTIVE: Prepare the solid dispersions( SD) of nifedipine( NF) by the solvent-freeze drying method to improve the dissolution rate of the drug. The dissolution rate has been further improved by the alkalizer to modifier the PH.METHODS: The solid dispersions of NF have been prepared with polyvinyl pyrrolidone( PVPk30),hydroxypropyl methyl cellulose( HPMC),poloxamer407 and sodium carbonate( Na_2CO_3),respectively. The optimal carrier were chose from the solubility and dissolution test, then the dissolution rate of the drug has been further improved by the Na_2CO_3.CONCLUSION: The dissolution rate improved to the 84% during 2hours,when used PVPk30 as the carrier,Na_2CO_3 as the alkalizer and the ratio of NF: PVPk30: Na_2CO_3 was 30mg: 150mg: 9mg in this solid dispersion system.
出处
《山东化工》
CAS
2015年第22期109-111,共3页
Shandong Chemical Industry