戊酸雌二醇阴道泡腾片的制备及体外质量评价

Preparation and in vitro Quality Evaluation of Estradiol Valerate Vaginal Effervescent Tablets

目的:研制戊酸雌二醇(EV)阴道泡腾片,对其体外质量进行评价。方法:采用酸碱分开制粒法制备EV阴道泡腾片。以p H、发泡量及崩解时间综合评分为指标,正交试验优选处方中酒石酸、酒石酸氢钾、碳酸氢钠及硼酸的用量。考察EV泡腾片的p H、发泡量、崩解时限、含量均匀度、稳定性、体外溶出度等体外质量。结果:优选处方中,酒石酸、酒石酸氢钾、碳酸氢钠及硼酸的用量分别为8,5,12,6 g。EV泡腾片水溶液呈弱酸性,发泡量、崩解时限、含量均匀度均符合中国药典的相关要求,且本品稳定性良好。体外药物溶出较快,10 min内基本溶出完全。结论:EV阴道泡腾片制备简单,体外质量良好,值得进一步研发。

Objective:To prepare estradiol valerate(EV)vaginal effervescent tablets and study the quality in vitro.Methods:EV vaginal effervescent tablets were prepared by an acid-base separating granulation method.Using the comprehensive score of p H value,foaming volume and disintegration time as the evaluation index,the amounts of tartaric acid,potassium bitartrate,sodium bitartrate and boric acid in the formulation were optimized by orthogonal design.The main in vitro quality indices including p H value,foaming volume,disintegrtation time,content uniformity,stability and dissolution were investigated.Results:The amount of tartaric acid,potassium bitartrate,sodium bitartrate and boric acid in the formulation was 8 g,5 g,12 g and 6 g,respectively.The water solution of the tablets was weak acid,and the foaming volume,disintegrating time and content uniformity met the requirements described in Chinese Pharmacopoeia(2015 edition).The stability of the tablets under the conditions of stability test was promising.EV could be released completely from the tablets in 10 min in vitro,suggesting the quick release property.Conclusion:EV vaginal effervescent tablets show simple preparation and good in vitro quality,which are valuable to be studied further.