依托考昔片自研制剂处方优选及体外溶出度评价  

Prescription Optimization and in Vitro Dissolution Evaluation of Self-Made Etoricoxib Tablets

作　　者：尹朋朋 刘茜英 肖慧 许俊博 YIN Pengpeng;LIU Qianying;XIAO Hui;XU Junbo(China Resources Double-Crane Pharmaceutical Co.,Ltd.,Beijing,China 100102)

机构地区：[1]华润双鹤药业股份有限公司,北京100102

出　　处：《中国药业》2024年第6期65-69,共5页China Pharmaceuticals

摘　　要：目的优选依托考昔片自研制剂处方,并评价其体外溶出度。方法以依托考昔片参比制剂(商品名Arcoxia,规格为每片120 mg)为开发目标,采用高效液相色谱法测定制剂中依托考昔含量,计算溶出度,并绘制溶出曲线。以在4种不同介质(pH 1.0盐酸溶液、pH 4.5醋酸盐溶液、pH 6.8磷酸盐溶液、水)中的溶出曲线相似因子(f2)值为评价标准,优选处方中原料药粒径及微晶纤维素SH-101、无水磷酸氢钙、硬脂酸镁(外加)的用量。结果优选pH 4.5醋酸盐溶液为溶出介质。依托考昔片最佳处方为原料药粒径>10~<50μm,微晶纤维素SH-101、无水磷酸氢钙、硬脂酸镁(外加)用量分别为每片125 mg、140 mg、3 mg。最终拟订处方自研制剂以pH4.5醋酸盐溶液、pH 6.8磷酸盐溶液和水为溶出介质的f2值分别为79,68,78,在pH 1.0盐酸溶液中参比制剂和自研制剂15 min的溶出度≥85%。结论确定的依托考昔片自研制剂处方与参比制剂的体外溶出曲线基本一致,可为其生物等效性研究提供参考。Objective To optimize the prescription of self-made Etoricoxib Tablets,and to evaluate their in vitro dissolution.Methods With the Etoricoxib Tablets reference(trade name:Arcoxia,specification:120 mg per tablet)as the development goal,the content of etoricoxib in the prescription was determined by the high-performance liquid chromatography method,the dissolution was calculated,and the dissolution profile was plotted.The particle size of active pharmaceutical ingredients(APIs)and dosages of microcrystalline cellulose SH-101,anhydrous calcium hydrogen phosphate,magnesium stearate added in the prescription were optimized with the similarity factor(f2)of the dissolution profile in four different media(pH 1.0 hydrochloric acid solution,pH 4.5 acetate solution,pH 6.8 phosphate solution and water)as the evaluation standard.Results The pH 4.5 acetate solution was selected as the dissolution medium.The optimal preparation of Etoricoxib Tablets was as follows:the particle size of APIs was greater than 10μm but smaller than 50μm,the dosages of microcrystalline cellulose SH-101,anhydrous calcium hydrogen phosphate and magnesium stearate added were 125 mg,140 mg,3 mg per tablet respectively.With pH 4.5 acetate solution,pH 6.8 phosphate solution and water as the dissolution media,the f2 of the final self-made preparation was 79,68,78 respectively,and the dissolution of the reference and self-made preparations with pH 1.0 hydrochloric acid solution as the dissolution medium was no lower than 85%in 15 min.Conclusion The in vitro dissolution profile of determined self-made Etoricoxib Tablets is basically consistent with that of the reference preparation,which can provide a reference for the study of its bioequivalence.

关 键 词：依托考昔 自研制剂 参比制剂 处方优选 溶出曲线 

分 类 号：R943[医药卫生—药剂学]