卡维地洛自乳化分散片的制备及质量评价

Preparation and evaluation of Carvedilol Self-emulsifying Dispersible Tablets

目的制备卡维地洛自乳化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乳化分散片,通过单因素实验优化处方,考察所得分散片的质量。结果以微晶纤维素KG 802(MCC KG 802)作为固体吸附材料,能有效吸附卡维地洛自微乳并形成固体吸附混合物(Mix)。分散片处方(质量分数)为:20%Mix,6%交联聚维酮(PVPP),3.5%微粉硅胶,0.5%硬脂酸镁与70%微晶纤维素102(MCC 102)。制得的分散片的片质量为300 mg,硬度、脆碎度和分散均匀性均符合要求,在去离子水中分散后形成的微乳粒径与液体自微乳相当。结论制得的卡维地洛自乳化分散片的质量符合要求且较好地保持了液体自微乳的特性。

Objective To establish preparation methods of Carvedilol Self-emulsifying Dispersible Tablets and evaluate their qualities in vitro.Methods The Carvedilol Self-emulsifying Dispersible Tablets were prepared by using direct powder compression method.Solid adsorbent materials which can completely release drug within 45 min were screened,and the formulation of dispersible tablets was optimized by single factor experiments.Results Microcrystalline cellulose KG 802(MCC KG 802)was selected as the suitable solid adsorbent which can effectively absorb the carvedilol self-emulsifying formulation and form solid adsorption mixture(Mix).The final formulation was 20%of Mix,6%of crosslinked polyvinylpyrrolidone(PVPP)as disintegrating agent,3.5%of micro-powder silica gel and 0.5%of magnesium stearate as lubricant,and the remaining was 70%of microcrystalline cellulose 102(MCC 102).The mass of the dispersed tablet was 300 mg.The hardness,friability,uniform dispersion and disintegration time of the tablets was qualified.In vitro study showed that the dispersible tablets could disperse in distilled water and form microemulsion with average particle size comparable to liquid carvedilol self-emulsion.Conclusion The Carvedilol Self-emulsifying Dispersible Tablets was successfully prepared and the characteristics of liquid carvedilol self-emulsion was almost kept.