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目的:制备达比加群酯自微乳分散片并评价其质量。方法:筛选可在45 min内完全释药的固体吸附材料,以粉末直接压片法制备自微乳分散片,通过单因素实验优化处方,考察所得自微乳分散片的质量。结果:以MCC KG 802作为固体吸附材料,能有效吸附达比加群酯自微乳液并形成固体吸附混合物(Mix)。分散片处方组成为:25%Mix,25%崩解剂PVPP,适量由4%微粉硅胶与0.5%硬脂酸镁组成的润滑剂,其余为填充剂MCC 102。制得分散片的硬度、脆碎度、分散均匀性及崩解时间均符合要求。在纯化水中分散后形成的微乳粒径为200~230 nm,与达比加群酯液体自微乳液的粒径相当。结论:自微乳分散片能较好的保持液体自微乳系统的特性,有望提高达比加群酯生物利用度,扩展了自微乳系统的应用范围。
Objective: To prepare dabigatran-based self-microemulsive dispersible tablets and evaluate their quality. Methods: The solid adsorbent which can be completely released within 45 min was screened. The self-microemulsifying dispersible tablets were prepared by powder direct compression. The quality of the microemulsion dispersible tablets was investigated by single-factor experiment. Results: MCC KG 802 was used as a solid adsorbent to adsorb dabigatran etexilate microemulsion efficiently and form a solid adsorption mixture. Dispersible tablets prescription composition: 25% Mix, 25% disintegrating agent PVPP, appropriate amount of 4% silica fume and 0.5% magnesium stearate composition of the lubricant, the rest filler MCC 102. The hardness, friability, dispersion uniformity and disintegration time of the prepared dispersible tablets all meet the requirements. The diameter of the microemulsions formed after dispersion in purified water was 200-230 nm, which corresponded to the particle size of dabigatran etexilate self-microemulsions. CONCLUSION: Self-microemulsions dispersible tablets can better maintain the properties of liquid self-microemulsifying system and improve the bioavailability of dabigatran etexilate and expand the application range of self-microemulsifying system.