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为提高联苯双酯的体外溶出度,采用超临界CO_2流体技术制备固体分散体。采用单因素法考察了载体种类、药物与载体质量比、CO_2的超临界条件(压强和温度)、反应时间对固体分散体中药物溶出行为的影响,优化制备工艺。结果表明,以气相二氧化硅为载体、药载比为1∶15,在45℃、25 MPa条件下反应2 h得到的优化产品中药物溶出速度和程度显著高于原料药,在pH 6.85介质中90 min溶出率约80%。差示扫描量热法和粉末X射线衍射法分析表明,在药载比为1∶15的固体分散体中,联苯双酯以无定形状态存在于载体中。
In order to improve the in vitro dissolution of bifendate, a solid dispersion was prepared by supercritical CO 2 fluid technology. The single factor method was used to investigate the influence of the kind of carrier, mass ratio of drug to carrier, supercritical conditions of CO_2 (pressure and temperature) and reaction time on the dissolution behavior of the solid dispersion, and optimize the preparation process. The results showed that the drug dissolution rate and extent of the optimized product obtained with fumed silica as the carrier and the drug-loading ratio of 1:15 at 45 ℃ and 25 MPa for 2 h were significantly higher than that of the drug substance at pH 6.85 90 min dissolution rate of about 80%. Differential scanning calorimetry and powder X-ray diffraction analysis showed that in the solid dispersion with a drug-loading ratio of 1:15, the bifendate was present in the carrier in an amorphous state.