联苯双酯固体分散体处方及体外性质评价

发布时间：2018-10-13 14:50

【摘要】：目的应用不同亲水性载体材料制备联苯双酯固体分散体,提高联苯双酯体外溶出。方法应用溶解度参数法初步筛选载体材料,采用热熔挤出法制备联苯双酯固体分散体,采用差示扫描量热法、X射线粉末衍射法和傅立叶变换红外光谱法对所制备的固体分散体进行表征。对固体分散体进行溶出度测定,以体外累积溶出度为主要指标,分别考察不同载体、不同载药量对固体分散体中联苯双酯溶出度的影响。结果应用不同亲水性载体材料制备的固体分散体均可提高联苯双酯溶出度,其中以Soluplus汶对联苯双酯溶出度的提高最为显著,累积溶出度可达到90%左右。优选Soluplus汶为固体分散体载体材料,并且当载药量为20%时,溶出度最高。结论应用载体材料Soluplus汶制备固体分散体可以显著提高联苯双酯溶出度。载体材料的性质及载药量的高低都会影响固体分散体中药物的溶出度。
[Abstract]:Objective to prepare biphenyl diester solid dispersion with different hydrophilic carrier materials and improve the dissolution of biphenyl diester in vitro. Methods the solid dispersion of biphenyl diester was prepared by hot melt extrusion method by preliminary screening of carrier material by solubility parameter method. The solid dispersion was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The dissolution of solid dispersions was determined, and the effects of different carriers and drug loading on the dissolution of biphenyl diesters in solid dispersions were investigated with the cumulant dissolution in vitro as the main index. Results the dissolution of biphenyl diesters was improved by using solid dispersions prepared with different hydrophilic carrier materials. The dissolution of biphenyl diesters was increased most significantly by Soluplus, and the cumulative dissolution rate was about 90%. Soluplus was selected as solid dispersion carrier, and the dissolution was the highest when the drug loading was 20. Conclusion the dissolution of biphenyl diester can be significantly improved by the preparation of solid dispersion with Soluplus-bun as carrier material. The properties of carrier materials and the amount of drug loaded will affect the dissolution of drugs in solid dispersions.
【作者单位】：沈阳药科大学药学院;
【分类号】：R943

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