Bridging the structure gap between pellets in artificial dissolution media and in gastro-intestinal tract in rats.
10.1016/j.apsb.2021.05.010
- Author:
Hongyu SUN
1
;
Siyu HE
2
;
Li WU
2
;
Zeying CAO
2
;
Xian SUN
2
;
Mingwei XU
3
;
Shan LU
2
;
Mingdi XU
4
;
Baoming NING
4
;
Huimin SUN
5
;
Tiqiao XIAO
3
;
Peter YORK
2
;
Xu XU
1
;
Xianzhen YIN
2
;
Jiwen ZHANG
1
Author Information
1. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, China.
2. Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201210, China.
3. Shanghai Synchrotron Radiation Facility/Zhangjiang Lab, Shanghai Advanced Research Institute, Chinese Academy of Sciences, Shanghai 201204, China.
4. National Institutes for Food and Drug Control, Beijing 100050, China.
5. NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients, National Institutes for Food and Drug Control, Beijing 100050, China.
- Publication Type:Journal Article
- Keywords:
3D reconstruction;
Enteric coated pellets;
Esomeprazole magnesium;
Internal 3D structure;
In vivo and in vitro structure correlation;
Omeprazole magnesium;
Structural parameter;
Synchrotron radiation X-ray micro computed tomography
- From:
Acta Pharmaceutica Sinica B
2022;12(1):326-338
- CountryChina
- Language:English
-
Abstract:
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.
