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Bridging the structure gap between pellets in artificial dissolution media and in gastrointestinal tract in rats

文献类型：期刊论文

作者Sun, Hongyu1,2; He, Siyu2,3; Wu, Li2; Cao, Zeying2,3; Sun, Xian2,3,8; Xu, Mingwei7; Lu, Shan2,4; Xu, Mingdi6; Ning, Baoming6; Sun, Huimin5,6
刊名ACTA PHARMACEUTICA SINICA B
出版日期2022
卷号12期号:1页码:326-338
关键词Internal 3D structure 3D reconstruction Structural parameter Enteric coated pellets Synchrotron radiation X-ray micro computed tomography In vivo and in vitro structure correlation Esomeprazole magnesium Omeprazole magnesium
ISSN号2211-3835
DOI10.1016/j.apsb.2021.05.010
通讯作者Xu, Xu(xuxu3426@sina.com) ; Yin, Xianzhen(xzyin@mail.shcnc.ac.cn) ; Zhang, Jiwen(jwzhanggroup@163.com)
英文摘要Changes in structure of oral solid dosage forms (OSDF) elementally determine the drug release and its therapeutic effects. In this research, synchrotron radiation X-ray micro-computed tomography was utilized to visualize the 3D structure of enteric coated pellets recovered from the gastrointestinal tract of rats. The structures of pellets in solid state and in vitro compendium media were measured. Pellets in vivo underwent morphological and structural changes which differed significantly from those in vitro compendium media. Thus, optimizations of the dissolution media were performed to mimic the appropriate in vivo conditions by introducing pepsin and glass microspheres in media. The sphericity, pellet volume, pore volume and porosity of the in vivo esomeprazole magnesium pellets in stomach for 2 h were recorded 0.47, 1.55 x 10(8) mu m(3), 0.44 x 10(8) mu m(3) and 27.6%, respectively. After adding pepsin and glass microspheres, the above parameters in vitro reached to 0.44, 1.64 x 10(8) mu m(3), 0.38 x 10(8) mu m(3) and 23.0%, respectively. Omeprazole magnesium pellets behaved similarly. The structural features of pellets between in vitro media and in vivo condition were bridged successfully in terms of 3D structures to ensure better design, characterization and quality control of advanced OSDF. (C) 2022 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
WOS关键词CONTROLLED-RELEASE ; IN-VIVO ; TABLETS ; SYSTEM ; BRAIN
资助项目National Key R&D Program of China[2020YFE0201700] ; Major New Drugs Innovation and Development,China[2017ZX09101001-005] ; National Natural Science Foundation of China[81803441] ; National Natural Science Foundation of China[81803446] ; National Natural Science Foundation of China[81773645] ; Youth Innovation Pro-motion Association CAS, China[2018323]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000747012200010
出版者INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
源URL[http://119.78.100.183/handle/2S10ELR8/300534]  
专题中国科学院上海药物研究所
通讯作者Xu, Xu; Yin, Xianzhen; Zhang, Jiwen
作者单位1.Shanghai Inst Technol, Sch Chem & Environm Engn, Shanghai 201418, Peoples R China
2.Chinese Acad Sci, Ctr Drug Delivery Syst, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Shanghai Univ, Ctr Supramol Chem & Catalysis, Sch Mat Sci & Engn, Dept Chem, Shanghai 200444, Peoples R China
5.Natl Inst Food & Drug Control, NMPA Key Lab Qual Res & Evaluat Pharmaceut Excipi, Beijing 100050, Peoples R China
6.Natl Inst Food & Drug Control, Beijing 100050, Peoples R China
7.Chinese Acad Sci, Shanghai Adv Res Inst, Shanghai Synchrotron Radiat Facil Zhangjiang Lab, Shanghai 201204, Peoples R China
8.Chinese Acad Sci, Ctr MOST & Image Fus Anal, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China
推荐引用方式
GB/T 7714		 Sun, Hongyu,He, Siyu,Wu, Li,et al. Bridging the structure gap between pellets in artificial dissolution media and in gastrointestinal tract in rats[J]. ACTA PHARMACEUTICA SINICA B,2022,12(1):326-338.
APA Sun, Hongyu.,He, Siyu.,Wu, Li.,Cao, Zeying.,Sun, Xian.,...&Zhang, Jiwen.(2022).Bridging the structure gap between pellets in artificial dissolution media and in gastrointestinal tract in rats.ACTA PHARMACEUTICA SINICA B,12(1),326-338.
MLA Sun, Hongyu,et al."Bridging the structure gap between pellets in artificial dissolution media and in gastrointestinal tract in rats".ACTA PHARMACEUTICA SINICA B 12.1(2022):326-338.

入库方式： OAI收割

来源：上海药物研究所

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