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非洛地平固体分散体的制备和体外溶出度考察
  • ISSN号:1006-2858
  • 期刊名称:《沈阳药科大学学报》
  • 时间:0
  • 分类:R94[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:[1]沈阳药科大学药学院,辽宁沈阳110016
  • 相关基金:973国家重大科学研究计划(2009CB930300)
中文摘要:

目的应用固体分散技术,提高非洛地平的体外溶出度。方法以PVPK30、Lutrol F68、Tween 80(与吸附剂,如PVPP)为载体,分别采用溶剂法、熔融法、溶剂蒸发一沉积等技术制备非洛地平固体分散体,考察不同载体对固体分散体溶出度的影响。并着重考察以Tween80为增溶剂,不同种类吸附剂为载体对固体分散体外观、溶出度的影响。应用差示热分析和X射线衍射鉴别药物在载体中的存在状态。结果采用不同载体和方法制备的非洛地平固体分散体均能明显促进药物的溶出,溶出速度依次为Tween80〉Lutrol F68〉PVPk30。其中m(药物):m(Tween80):m(PVPP)=1:4:5时,溶出速度最快,1h累积释放率达90%以上。差示热分析固体分散体中药物吸热峰前移或消失,X射线衍射固体分散体中药物的结晶衍射峰消失,推测药物在载体中以无定形或分子形式存在。结论制备非洛地平固体分散体可以提高其体外溶出度,尤其是含有表面活性剂的固体分散体可进一步提高药物的溶出。

英文摘要:

Objective To improve the solubility and dissolution of felodipine by preparing its solid dispersions. Methods PVPk30, Lutrol F68 and Tween 80 ( with absorbent, such as crospovidone) were used as carders to prepare the solid dispersions of felodipine by the methods of solvent, melt and solvent evaporationdeposition. When Tween80 was applied as solubilizer, the effect of different absorbents on the appearance and dissolution of solid dispersions were the focus of study. The state of felodipine in carriers was identified by DSC. Results The dissolution rate test demonstrated that all the solid dispersions could improve the dissolution rate of felodipine and the sequence was that: Tween 80 〉 Lutrol F68 〉 PVPk30. Among of this, when weight ratio of felodipine,Tween 80 and PVPP was 1:4:5 ,the dissolution rate was the most fast and the accumulative release rate was up to more than 90% in 1 h. The results of differential scanning calorimetry (DSC) indicated that the drug was in the amorphous state. Conclusions Surfactant is useful in preparing felodipine solid dispersion and significantly improves the dissolution rate of felodipine.

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期刊信息
  • 《沈阳药科大学学报》
  • 中国科技核心期刊
  • 主管单位:辽宁省教育厅
  • 主办单位:沈阳药科大学
  • 主编:毕开顺
  • 地址:沈阳市文化路103号
  • 邮编:110016
  • 邮箱:syyd@chinajournal.net.cn
  • 电话:024-23986082 23994540
  • 国际标准刊号:ISSN:1006-2858
  • 国内统一刊号:ISSN:21-1349/R
  • 邮发代号:
  • 获奖情况:
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  • 美国化学文摘(网络版),日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘
  • 被引量:17272