In this study, the impact of drug and hydroxypropyl methylcellulose acetate succinate (HPMCAS) grades physicochemical properties on extrusion process, dissolution and stability of the hot melt extruded amorphous solid dispersions (ASDs) of nifedipine and efavirenz was investigated. Incorporation of drugs affected the extrusion temperature required for solid dispersion preparation. Differential scanning calorimetry and powder X-ray diffraction studies confirmed the amorphous conversion of the drugs in the prepared formulations. The amorphous nature of ASDs was unchanged after 3 months of stability testing at 40 °C and 75% relative humidity. The dissolution efficiency of the ASDs was dependent on the log P of the drug. The inhibitory effect of HPMCAS on drug precipitation was dependent on the hydrophobic interactions between drug and polymer, polymer grade, and dose of the drug. The dissolution efficiency and dissolution rate of the ASDs were dependent on the log P of the drug and solubility and hydrophilicity of the polymer grade respectively. The inhibitory effect of HPMCAS on drug precipitation was dependent on the hydrophobic interactions between drug and polymer, polymer grade, and the dissolution dose of the drug.

中文翻译：

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通过热熔挤出制备基于乙酸琥珀酸羟丙甲纤维素的无定形固体分散体：药物理化性质的影响。


在本研究中，研究了药物和醋酸琥珀酸羟丙基甲基纤维素（HPMCAS）等级的理化性质对硝苯地平和依非韦伦热熔挤出无定形固体分散体（ASD）的挤出工艺、溶出度和稳定性的影响。药物的掺入影响固体分散体制备所需的挤出温度。差示扫描量热法和粉末X射线衍射研究证实了所制备制剂中药物的无定形转化。在 40 °C 和 75% 相对湿度下进行 3 个月的稳定性测试后，ASD 的无定形性质没有变化。 ASD 的溶出效率取决于药物的 log P。 HPMCAS 对药物沉淀的抑制作用取决于药物与聚合物之间的疏水相互作用、聚合物等级和药物剂量。 ASD 的溶出效率和溶出速率分别取决于药物的 log P 以及聚合物等级的溶解度和亲水性。 HPMCAS对药物沉淀的抑制作用取决于药物与聚合物之间的疏水相互作用、聚合物等级和药物的溶出剂量。