热熔分散法制备依巴斯汀分散片

Preparation of ebastine dispersible tablets by hot-melt dispersion

目的以羟丙甲纤维素为载体,用热熔分散法制备依巴斯汀分散片。方法将依巴斯汀原料熔融分散于羟丙甲纤维素热水溶液中,以甘露醇吸附药液,制备分散片。用差示扫描量热分析和X-射线粉末衍射分析热熔分散体特征,并比较自制分散片和原研药的溶出曲线。结果 X-射线衍射和差示扫描量热分析表明,热熔分散体中的依巴斯汀仍具有原料晶型的主要特征,体外溶出结果显示,依巴斯汀热熔分散体的15min溶出度可达到95.07%,显著高于微粉化的依巴斯汀原料药,分散片30min的累积溶出度也比原研药高出约30%。结论以羟丙甲纤维素为载体的热熔分散技术,可显著提高依巴斯汀的溶出度。

Objective To prepare ebastine dispersible tablets by hot-melt dispersion method using hypromellose as a carrier.Methods Ebastine was heated to melt and dispersed in hot solution of hypromellose.The mixture was adsorbed by mannitol and then used to prepare dispersible tablets.The characteristics of hot-melt dispersion were analyzed by the methods of differential scanning calorimetry and X-ray powder diffraction.A comparison of dissolution curves between self-made dispersible tablets and original ebastine tablets was performed.Results The analysis of X-ray diffraction and differential scanning calorimetry showed that the ebastine in solid matrix remained the main crystalline characteristics.The dissolution of ebastine hot-melt dispersion was 95.07% in 15 min in vitro, which was significantly higher than that of micronized ebastine raw material.Moreover, the accumulative dissolution of ebastine dispersible tablets in 30 min was about 30% higher than the original drug.Conclusion The method of hot-melt dispersion using hypromellose as a carrier improved the ebastine dissolution significantly.