【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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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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。更多还原

【Abstract】 Objective To improve the dissolution of bifendate by preparing its solid dispersions with different hydrophilic carriers.Methods Solubility parameter method was used to screen the hydrophilic carriers and bifendate solid dispersions were prepared by hot-melt extrusion and characterized by differential scanning calorimetry,X-ray powder diffraction and infrared spectra respectively.Accumulated dissolution of bifendate solid dispersions with different carriers and drug loading was measured.Results It showed that although the dissolution of all bifendate solid dispersions with different carriers was improved,the formulation with Solupluswas better than others and its accumulated dissolution was up to 90%.Thereby Solupluswas chosen as the optimal carrier of bifendate solid dispersions.When drug loading was 20%,the maximum accumulated dissolution of bifendate was reached.Conclusions Dissolution of bifendate is significantly improved by formulating it into solid dispersions with Soluplusas carrier.Properties of carriers and the drug loading were the two main factors affecting the dissolution of solid dispersions.更多还原