Bridging the structure gap between pellets in artificial dissolution media and in gastro-intestinal tract in rats
| Autor: | Tiqiao Xiao, Li Wu, Xu Xu, Mingwei Xu, Siyu He, Xianzhen Yin, Zeying Cao, Hongyu Sun, Shan Lu, Peter York, Huimin Sun, Mingdi Xu, Jiwen Zhang, Baoming Ning, Xian Sun |
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| Rok vydání: | 2022 |
| Předmět: |
Pellets
RM1-950 Dosage form Synchrotron radiation X-ray micro computed tomography 03 medical and health sciences 0302 clinical medicine Pepsin Pellet Internal 3D structure Omeprazole magnesium 3D reconstruction General Pharmacology Toxicology and Pharmaceutics Dissolution 030304 developmental biology Esomeprazole magnesium 0303 health sciences Esomeprazole Magnesium biology Chemistry Structural parameter Omeprazole Magnesium Glass microsphere 030220 oncology & carcinogenesis In vivo and in vitro structure correlation biology.protein Original Article Therapeutics. Pharmacology Enteric coated pellets Nuclear chemistry |
| Zdroj: | Acta Pharmaceutica Sinica B, Vol 12, Iss 1, Pp 326-338 (2022) Acta Pharmaceutica Sinica. B |
| ISSN: | 2211-3835 |
| DOI: | 10.1016/j.apsb.2021.05.010 |
| Popis: | 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 × 108 μm3, 0.44 × 108 μm3 and 27.6%, respectively. After adding pepsin and glass microspheres, the above parameters in vitro reached to 0.44, 1.64 × 108 μm3, 0.38 × 108 μm3 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. Graphical abstract The differences in dynamic structure of enteric pellets during dissolution in vitro and in vivo were first observed. By introducing pepsin and glass microspheres into pharmacopoeia medium, the structures of pellets were bridged.Image 1 |
| Databáze: | OpenAIRE |
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