Preparation of ebastine dispersible tablets by hot-melt dispersion
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摘要: 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15 min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30 min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。Abstract: 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.
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Key words:
- ebastine /
- dissolution /
- hypromellose
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