非布司他自微乳胶囊的研制

Development of febuxostat self-emulsion capsules

目的制备非布司他固体自微乳制剂,提高非布司他溶解度与溶出速度。方法通过溶解度测定,选择对非布司他溶解度较大的油相,乳化剂及助乳化剂中,并通过绘制伪三元相图,确定成乳区域,采用Design Expert 8.0.5,以自乳化时间、平均粒径、Zeta电位为评价指标优化处方。结果制备出最佳处方油酸乙酯39.60%,Tween-80 45.54%,TRANSCUTOL HP 14.85%,所制得的微乳外观均一透明,蒸馏水稀释100倍后,其平均粒径为35.3 nm, Zeta电位为24.8 mV,自乳化时间为48.7 s,体外溶出10 min内达80%以上。结论非布司他固体自微乳制备工艺简单,质量稳定,自微乳化效率较高,可提高难溶性药物的溶解度、溶出速度,并能提高制剂的稳定性。

Objective solid self-microemulsion formulation of febuxostat is prepared to increase the solubility and dissolution rate of febuxostat.Methods Through the determination of solubility, selected the oil phase, emulsifier and co-emulsifier with higher solubility for febuxostat, and draw a pseudo-ternary phase diagram to determine the region of milk formation.Design Expert 8.0.5 was used to determine the average particle diameter and Zeta potential were optimized prescriptions for evaluation indicators.Results The best prescription of ethyl oleate was 39.60%, Tween-80 45.54%, and TRANSCUTOL HP 14.85%.The micro-emulsion obtained had a uniform and transparent appearance.After being diluted 100 times with distilled water, its average particle size was 35.3 nm and the zeta potential was 24.8 mv, self-emulsifying time was 48.7 s, and the dissolution rate reached over 80% within 10 minutes.Conclusion The preparation process of febuxostat solid self-microemulsion is simple, the quality is stable, and the self-microemulsifying efficiency is high.It can improve the solubility and dissolution rate of poorly soluble drugs and improve the stability of the preparation.