热熔挤出技术制备泊沙康唑固体分散体及其体外评价

发布时间：2018-03-10 01:22

  本文选题：热熔挤出　切入点：固体分散体　出处：《中国药科大学学报》2015年03期 　论文类型：期刊论文

【摘要】：采用热熔挤出(HME)技术制备难溶性药物泊沙康唑(POS)固体分散体,提高其溶出度。利用溶解度参数、玻璃化转变温度和熔融法,初步筛选载体。进一步运用HME技术制备POS固体分散体,以溶出度为指标考察载体Kollidon VA64、Soluplus、Eudragit L100以及混合载体Kollidon VA64-Eudragit L100对药物的增溶能力。考察影响固体分散体溶出度的处方以及工艺因素、不同载体、挤出温度、增塑剂和载药量对溶出度的影响。采用差示扫描量热法(DSC)进行物相分析,并通过影响因素实验初步分析固体分散体的稳定性。结果显示以Kollindon VA64-Eudragit L100(2∶8)为载体,10%柠檬酸三乙酯为增塑剂,150℃挤出温度下制备的POS固体分散体,显著提高了POS的溶出度,DSC结果显示药物以无定形或分子形式存在于载体中。混合载体的比例、挤出温度、载药量以及增塑剂均能影响药物的溶出。固体分散体对湿度敏感,高温和强光条件下稳定。采用HME技术制备的固体分散体可以显著提高POS的溶出度。
[Abstract]:The insoluble drug posaconazole (POS) solid dispersion was prepared by hot melt extrusion (HME-HME) technique, and its dissolution was improved. The solubility parameters, glass transition temperature and melting method were used. HME technology was used to prepare POS solid dispersion. The solubilization ability of the carrier Kollidon VA64 Soluplusus Eudragit L100 and the mixed carrier Kollidon VA64-Eudragit L100 was investigated. The formulation and technological factors affecting the dissolution of solid dispersions, different carriers and extrusion temperature were investigated. Effect of plasticizer and drug loading on dissolution. Phase analysis was performed by differential scanning calorimetry (DSC). The stability of the solid dispersion was preliminarily analyzed by the experiment of influencing factors. The results showed that the solid dispersion of POS was prepared by extrusion at 150 鈩，

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