碱性调节剂对缬沙坦固体分散体体外溶出度的影响  

Effect on the Dissolution Rate of the Solid Dispersion of Valsartan by the Alkalizer

作　　者：王洁[1] 孙杨 金刚[1] 于世华[1] 刘治刚[3] 

机构地区：[1]吉林化工学院化学与制药工程学院,吉林吉林132022 [2]吉林大地地球物理科学研究院,吉林长春130012 [3]吉林化工学院分析测试中心,吉林吉林132022

出　　处：《吉林化工学院学报》2015年第11期30-33,共4页Journal of Jilin Institute of Chemical Technology

摘　　要：目的:采用溶剂-冷冻干燥法制备缬沙坦(VAL)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药物溶出时周围微环境的p H值,使药物在特定的pH环境下溶解释放,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,从聚乙二醇6000(PEG6000)、羟丙甲基纤维素(HPMC)、聚乙烯吡咯烷酮K30(PVPK30)中筛选最优载体,确定其最佳比例,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HPMC为载体,Na_2CO_3为碱性调节剂,且VAL HPMC Na_2CO_3=80 mg 80 mg 16 mg时,相对于原料药而言溶出速率显著提高,在2 h内累计溶出度百分率可达97%.OBJECTIVE： Prepare the solid dispersions（ SD） of valsartan 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 p H,because the drug dissolved in a certain p H environments. METHODS： The solid dispersions of valsartan have been prepared with polyethylene glycol 6000（ PEG6000）,hydroxypropyl methyl cellulose（ HPMC）,polyvinyl pyrrolidone（ PVPk30） and sodium carbonate（ Na2CO3）,respectively. The optimal carrier was chose by the solubility and dissolution test.,then the dissolution rate of the drug has been further improved by the Na2CO3. CONCLUSION： The dissolution rate improved to the 97% during 2hours,when used HPMC as the carrier,Na2CO3 as the alkalizer and the ratio of VAL HPMC Na2CO3 was 1 1 10% in this solid dispersion system.

关 键 词：碱性调节剂 固体分散体 缬沙坦 体外溶出度 

分 类 号：R94[医药卫生—药剂学]