摘要
目的研究塞来昔布胶囊自研制剂与参比制剂体外溶出的相似性,分析并建立其体内外相关性。方法考察自研制剂与参比制剂在不同溶出介质、不同表面活性剂用量下塞来昔布胶囊的溶出曲线,采用相似因子(f_(2))法评价溶出曲线的相似性。同时通过体内生物等效性研究结合体外溶出试验结果分析体外溶出和体内吸收的相关性。结果自研制剂在5种溶出介质中的溶出曲线与参比制剂f_(2)均大于50。采用0.4%SLS水作为溶出介质时,体外溶出曲线与体内药动学参数及药时曲线变化趋势一致,提示该介质中溶出曲线具有一定的体内外相关性。结论本研究为塞来昔布胶囊初步建立了具有一定体内外相关性的溶出方法,为仿制药的溶出曲线一致性评价提供了依据。
Objective To research the in vitro dissolution similarity between self-prepared drug and reference drug of celecoxib capsules,and to establish the in vitro and in vivo correlation.Methods The dissolution curves of celecoxib capsules in various dissolution media with different concentrations of surfactant were determined,Similarity factor(f_(2))was used to evaluate the similarity of dissolution curves between the self-prepared drug and reference drug.The bioequivalence study was used to analyze correlation between in vitro drug dissolution and in vivo drug absorption combined with dissolution test.Results The similarity factors(f_(2))were all more than 50 between the self-prepared drug and reference drug in five dissolution media.When water(0.4%SLS)was used as dissolution medium,the dissolution curves were consistent with pharmacokinetic parameters and plasma concentration-time curves,the result indicated that the dissolution curves in water(0.4%SLS)had good in vitro and in vivo correlation.Conclusion The study helps establish a dissolution method for celecoxib capsules with in vivo-in vitro correlation,and provides the basis for the consistency evaluation of the dissolution curves of generic drugs.
作者
丁强
金波
管志美
王彬
周莎莎
殷美园
刘雁鸣
刘翔
DING Qiang;JIN Bo;GUAN Zhi-mei;WANG Bin;ZHOU Sha-sha;YIN Mei-yuan;LIU Yan-ming;LIU Xiang(Hinye Pharmaceutical Co.,Ltd.,Changsha 410331;Hunan Engineering and Technology Research Center for Bone&Joint Disease Drugs,Changsha 410331;Hunan Center for Drug Inspection,Changsha 410013;NMPA Key Laboratory of Pharmaceutical Excipients Engineering Technology Research,Changsha 410001;Hunan Engineering&Technology Research Center for Quality Evaluation of Pharmaceutical,Changsha 410001)
出处
《中南药学》
CAS
2022年第8期1810-1815,共6页
Central South Pharmacy
基金
湖南省自然科学基金项目(No.2020JJ9052)。
关键词
塞来昔布胶囊
溶出曲线
生物等效性
体内外相关性
celecoxib capsule
dissolution curve
bioequivalence study
in vivo and in vitro correlation
