Sun, Hongyu; He, Siyu; Wu, Li; Cao, Zeying; Sun, Xian; Xu, Mingwei; Lu, Shan; Xu, Mingdi; Ning, Baoming; Sun, Huimin; Xiao, Tiqiao; York, Peter; Xu, Xu; Yin, Xianzhen; Zhang, Jiwen

ACTA PHARMACEUTICA SINICA B

2022, 12, 2211-3835

Sun, Hongyu; He, Siyu; Wu, Li; Cao, Zeying; Sun, Xian; Xu, Mingwei; Lu, Shan; Xu, Mingdi; Ning, Baoming; Sun, Huimin; Xiao, Tiqiao; York, Peter; Xu, Xu; Yin, Xianzhen; Zhang, Jiwen

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.