达格列净片的制备及体内外评价  

Preparation,in Vitro and in Vivo Evaluation of Dapagliflozin Tablets

作　　者：郭昊 牟聪[1,2] 杨迎迎 路珊珊 吴青青[1,2] 吕慧敏 GUO Hao;MU Cong;YANG Yingying;LU Shanshan;WU Qingqing;LYU Huimin(Yangtze River Pharmaceutical Group,Taizhou,Jiangsu,China 225321;National Key Laboratory of Complex Drug Formulations for Overcoming Delivery Barriers,Taizhou,Jiangsu,China 225321)

机构地区：[1]扬子江药业集团有限公司,江苏泰州225321 [2]克服递药屏障高端制剂全国重点实验室,江苏泰州225321

出　　处：《中国药业》2024年第21期19-22,共4页China Pharmaceuticals

摘　　要：目的为达格列净仿制药的研发提供参考。方法制备达格列净片自制制剂,考察自制制剂的崩解时限、溶出曲线。分别选择30名健康受试者开展空腹及餐后生物等效性试验,比较自制制剂与参比制剂的体内药代动力学参数[最大血药浓度(Cmax)、血药浓度-时间曲线下面积(AUC0-t和AUC0-∞)],计算上述参数的几何均数比(T/R)的90%置信区间(90%CI),判定2种制剂在人体内是否生物等效。结果自制制剂与参比制剂在4种溶出介质中的溶出量相当,15 min内溶出量均大于85%。空腹和餐后状态下,自制制剂与参比制剂的Cmax,AUC0-t,AUC0-∞的T/R(90%CI)相似,且均在80.00%~125.00%等效区间内。结论达格列净片自制制剂与参比制剂的体内外溶出行为一致,具有生物等效性,可用于大规模生产。Objective To provide a reference for the research and development of reference preparation of Dapagliflozin Tablets.Methods The self-made preparation of Dapagliflozin Tablets was prepared,and the disintegration time and dissolution curve of the self-made preparation were investigated.Thirty healthy subjects were selected to conduct fasting and postprandial bioequivalence tests,the in vivo pharmacokinetic parameters[maximum blood concentration(Cmax),area under the blood concentration-time curve(AUC0-t and AUC0-∞)]of the self-made preparation and the reference preparation were compared.The 90%confidence interval(CI)of the geometric mean ratio(T/R)of the above parameters was calculated to determine whether the two preparation are bioequivalence in the human body.Results The dissolution rates of the self-made preparation and the reference preparation in the four dissolution media were comparable,with dissolution rates exceeding 85%within 15 min.Under the fasting and postprandial conditions,the T/R of Cmax,AUC0-t,AUC0-∞of the self-made preparation and the reference preparation were similar,and they were within the equivalent range of 80.00%-125.00%.Conclusion The in vitro and in vivo dissolution behavior of the self-made preparation of Dapagliflozin Tablets is consistent with that of the reference preparation with bioequivalence and suitability,which can be used for large-scale production.

关 键 词：达格列净 溶出曲线 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R977.12[医药卫生—药学]