The structural diversity of ibuprofen sustained-release pellets on the same goal of bioequivalence consistency

Zeying Cao; Ningyun Sun; Hongyu Sun; Jun Liu; Jing Li; Dezhong Bi; Caifen Wang; Li Wu; Xianzhen Yin; Tiqiao Xiao; Rui Yang; Mingdi Xu; Wei Wu; Jiwen Zhang

Materials & Design (May 2022)

The structural diversity of ibuprofen sustained-release pellets on the same goal of bioequivalence consistency

Zeying Cao,
Ningyun Sun,
Hongyu Sun,
Jun Liu,
Jing Li,
Dezhong Bi,
Caifen Wang,
Li Wu,
Xianzhen Yin,
Tiqiao Xiao,
Rui Yang,
Mingdi Xu,
Wei Wu,
Jiwen Zhang

Affiliations

Zeying Cao: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China
Ningyun Sun: Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China; SPH Sine Pharmaceutical Laboratories Co., Ltd., Shanghai 201206, China
Hongyu Sun: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Jun Liu: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Jing Li: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China
Dezhong Bi: SPH Sine Pharmaceutical Laboratories Co., Ltd., Shanghai 201206, China
Caifen Wang: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Li Wu: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Xianzhen Yin: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Lingang Laboratory, Shanghai 201602, China
Tiqiao Xiao: Shanghai Synchrotron Radiation Facility/Zhangjiang Lab, Shanghai Advanced Research Institute, Chinese Academy of Sciences, Shanghai 201204, China
Rui Yang: NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients, National Institutes for Food and Drug Control, Beijing 100050, China
Mingdi Xu: NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs, National Institutes for Food and Drug Control, Beijing 100050, China; Corresponding authors at: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China (J. Zhang).
Wei Wu: Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China; Corresponding authors at: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China (J. Zhang).
Jiwen Zhang: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China; NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients, National Institutes for Food and Drug Control, Beijing 100050, China; Corresponding authors at: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China (J. Zhang).

Journal volume & issue: Vol. 217
p. 110583

Abstract

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The consistency evaluation, which is largely unexplored is crucial in regulating the quality and efficacy of generic drugs. In this report, after generic ibuprofen (IBU) sustained-release pellets were developed and validated as bioequivalent to the reference list drug (RLD) in 48 healthy human volunteers (p < 0.001***), three-dimensional (3D) structures of generic IBU pellets from bioequivalence tests, along with RLD were investigated and compared for architecture using Micro-computed tomography (Micro-CT). The surface and internal architectures of the pellets, sphericity, pellet volume, core volume and gray value have been evaluated in both static and dynamic conditions. The material distribution and composition of IBU pellets were characterized using synchrotron radiation-FTIR mapping. Although the structures of RLD and the generic products were not similar dynamically, identical release profiles and bioequivalence were obtained. Overall, micro-CT could be very useful for characterization of internal structure, material design and development of new dosage form.

Published in Materials & Design

ISSN: 0264-1275 (Print); 1873-4197 (Online)
Publisher: Elsevier
Country of publisher: United Kingdom
LCC subjects: Technology: Electrical engineering. Electronics. Nuclear engineering: Materials of engineering and construction. Mechanics of materials
Website: https://www.journals.elsevier.com/materials-and-design

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