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热熔挤出法已广泛用于制备水难溶性药物无定形固体分散体的研究。很多文献报道,含有可电离基团的肠溶性聚合物具有改善物理稳定性和维持药物过饱和状态的能力,继而增强药物的口服生物利用度。然而,前期研究表明,伊曲康唑(ITZ)肠溶聚合物无定形固体分散体是疏水性的,可润湿性较差;并且,在酸性环境(如胃部)中药物的释放量非常有限,提示吸收窗狭窄。本研究中考察了亲水性添加物对ITZ肠溶聚合物无定形固体分散体体外和体内性能的影响。结果显示,以醋酸羟
Hot-melt extrusion has been widely used to prepare water-insoluble drug amorphous solid dispersion. Many reports have reported that enteric polymers containing ionizable groups have the potential to improve physical stability and maintain the drug’s supersaturation, which in turn enhances the oral bioavailability of the drug. However, previous studies have shown that itraconazole (ITZ) enteric polymer amorphous solid dispersions are hydrophobic and poorly wettable; and that the release of the drug in an acidic environment (such as the stomach) is very poor Limited, suggesting narrow absorption window. In this study, we investigated the effect of hydrophilic additives on in vitro and in vivo properties of ITZ enteric-coated amorphous solid dispersions. The results show that with acetic acid hydroxyl