不同载体材料改善难溶性药物乙烷硒啉溶出性能的实验研究  

Effect of different carriers on the dissolution of the poorly water-soluble ethaselen

作　　者：张晶[1] 刘昕[2] 武凤兰[2] 于少云[1] 

机构地区：[1]北京化工大学生命科学与技术学院,北京100029 [2]北京大学药学院,北京100083

出　　处：《中国新药杂志》2008年第19期1688-1691,共4页Chinese Journal of New Drugs

摘　　要：目的:改善水不溶性药物乙烷硒啉的溶出性能,以提高乙烷硒啉固体制剂的药物溶出度。方法:以聚维酮(polyvinylpyrrolidone,简称PVP)、枸橼酸、酒石酸、羟丙基-β-环糊精(hydroxylpropyl-β-cyclodex-trin,简称HP-β-CD)等辅料为载体材料,以溶剂溶解与分散法制备乙烷硒啉固体颗粒及其物理混合物,并进行体外溶出度试验。利用差示扫描量热法(Differential Scanning Calorimetry,简称DSC)和X-射线衍射法来验证药物的存在状态。结果:以PVP为载体材料所制固体颗粒的体外溶出行为显著优于其他载体材料,且载体材料的比例越大,药物溶出越快。结论:DSC和X-射线衍射图实验证明,PVP载体材料改变了乙烷硒啉的存在状态与亲水性,溶出性能得到显著改善。Objective： To improve the solubility of poorly water-soluble ethaselen and the dissolution of ethaselen preparations. Methods：Ethaselen solid granules and physical mixtures were prepared by a solvent wetting method and a dispersal method using polyvinylpyrrolidone （PVP） , citric acid, tartaric acid, 2-Hydroxypropyl-β-cy- clodextrin （HP-β-CD） as carriers, and dissolution test was carried out. The state of the drug was verified by Differential Scanning Calorimetry（DSC） and X-ray diffraction. Results：The dissolution behavior of ethaselen solid granules prepared by PVP was superior to those by other carriers, and the more ratio of the carriers of PVP, the faster dissolution of ethaselen. Conclusion：The results of DSC and X-ray diffraction indicated that the state and the hy- drophilicit） were changed by the carrier of PVP,and the dissolution performance was improved significantly.

关 键 词：乙烷硒啉 聚维酮 溶出度 差示扫描量热法 X-射线衍射 

分 类 号：R943[医药卫生—药剂学] R979.1[医药卫生—药学]