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首页> 外文期刊>Crystal growth & design >Profoundly Improved Plasticity and Tabletability of Griseofulvin by in Situ Solvation and Desolvation during Spherical Crystallization
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Profoundly Improved Plasticity and Tabletability of Griseofulvin by in Situ Solvation and Desolvation during Spherical Crystallization

机译:在球形结晶期间,通过原位溶解和脱溶解来改善Griseofulvin的可塑性和压缩性

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摘要

Griseofulvin (GSF) is a high dose drug exhibiting poor flowability and tabletability, which makes formulating a high drug loading tablet challenging. In using spherical crystallization to improve flowability, the spherical agglomerates (SA) of GSF were found to have profoundly improved tabletability over the as-received GSF. An improved plasticity of GSF SA was observed despite its identical crystal structure and larger particle size when compared to the as-received GSF. Tracking solid forms during the process revealed the formation of a GSF solvate with dichloromethane, the bridging liquid for spherical agglomeration. With subsequent desolvation during drying, nanoporous GSF crystals were obtained, which could be plastically deformed more easily and exhibited much improved tabletability.
机译:Griseofulvin(GSF)是一种高剂量药物,具有较差的流动性和压缩性,这使得配制高药物负载片剂挑战。 在使用球形结晶以提高流动性,发现GSF的球形附聚物(SA)在接受的GSF上具有深刻的改善的阻垢性。 尽管其与接收的GSF相比,尽管其相同的晶体结构和较大的粒度,但观察到GSF SA的改善的可塑性。 在该过程中跟踪固体形式揭示了与二氯甲烷的GSF溶剂化物的形成,用于球形附聚的桥接液。 随后在干燥期间的脱溶解,获得了纳米多孔的GSF晶体,可以更容易地塑性变形并表现出大量改善的缩放性。

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  • 来源
    《Crystal growth & design》 |2019年第4期|共8页
  • 作者单位

    Univ Minnesota Coll Pharm Dept Pharmaceut Pharmaceut Mat Sci &

    Engn Lab Minneapolis MN 55455 USA;

    Univ Minnesota Coll Pharm Dept Pharmaceut Pharmaceut Mat Sci &

    Engn Lab Minneapolis MN 55455 USA;

    Univ Minnesota Coll Pharm Dept Pharmaceut Pharmaceut Mat Sci &

    Engn Lab Minneapolis MN 55455 USA;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
  • 关键词

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