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Enhanced solubility and dissolution rate of amiodarone by complexation with β-cyclodextrin through different methods

机译:通过不同方法与β-环糊精络合提高胺碘酮的溶解度和溶解速度

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摘要

The aim of this work was to investigate the inclusion complexation between amiodarone (AMD), a practically water insoluble anti arrhythmic agent, and β-cyclodextrin (βCD) in order to improve the solubility and the dissolution rate of the drug, in an attempt to enhance its bioavailability. The complexation was done through different methods: physical mixture (PM), coevaporated (CV), freeze-drying (FD) and spray-drying (SD). The data analysis indicated that the complexes produced by freeze-drying and spray-drying techniques resulted in amorphous samples (data obtained by DSC and XRPD), and showed a possible chemical interaction between OH-βCD group and AMD tertiary amine (visualized by FT-IR). Also, they presented higher thermal stability (demonstrated by TG) and the improvement of the drug dissolution rate.
机译:这项工作的目的是研究实际上不溶于水的抗心律失常药胺碘酮(AMD)和β-环糊精(βCD)之间的包合物,以改善药物的溶解度和溶解速率。提高其生物利用度。络合通过不同的方法完成:物理混合物(PM),共蒸发(CV),冷冻干燥(FD)和喷雾干燥(SD)。数据分析表明,通过冷冻干燥和喷雾干燥技术生产的配合物产生无定形样品(DSC和XRPD获得的数据),并表明OH-βCD基团和AMD叔胺之间可能存在化学相互作用(通过FT- IR)。而且,它们表现出更高的热稳定性(由TG证明)和药物溶解速率的提高。

著录项

  • 来源
    《Materials science & engineering》 |2010年第7期|P.1008-1013|共6页
  • 作者单位

    Laboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Estadual de Ponta Grossa, Ponta Grossa, PR, Brazil;

    rnLaboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis, SC, Brazil;

    rnLaboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis, SC, Brazil;

    rnLaboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis, SC, Brazil;

    rnLaboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis, SC, Brazil;

    rnLaboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Estadual de Ponta Grossa, Ponta Grossa, PR, Brazil Laboratorio de Controle de Qualidade, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis, SC, Brazil;

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

    amiodarone; β-Cyclodextrin; complexation; solubility;

    机译:胺碘酮β-环糊精;复杂化溶解度;

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