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Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin

机译:通过与β-环糊精及其衍生物羟丙基-β-环糊精的包合作用增强诺氟沙星的溶解性

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Abstract The objectives of the study were to investigate the effects of β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) on the solubility and dissolution rate of norfloxacin prepared using three different methods, at drug to cyclodextrin weight ratios of 1:1, 1:2, 1:4 and 1:8. All the methods increased the solubility and dissolution rate of norfloxacin via inclusion complexation with βCD and HPβCD. Norfloxacin was converted from crystalline to amorphous form through inclusion complexation. Solvent evaporation method was the most effective method in terms of norfloxacin solubilisation, while inclusion complex of HPβCD has higher solubility than βCD complex when prepared using the same procedure.
机译:摘要研究的目的是研究药物-环糊精重量比为1时,三种方法制备的β-环糊精(βCD)和羟丙基-β-环糊精(HPβCD)对诺氟沙星的溶解度和溶出度的影响。 1、1:2、1:4和1:8。所有方法均通过与βCD和HPβCD的包合作用提高了诺氟沙星的溶解度和溶出度。诺氟沙星通过包合络合从结晶形式转变为无定形形式。就诺氟沙星的溶解而言,溶剂蒸发法是最有效的方法,而当使用相同的方法制备时,HPβCD的包合物与βCD相比具有更高的溶解度。

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