Real-time in-line prediction of drug loading and release rate in the coating process of diclofenac sodium spheres based on near infrared spectroscopy

Zhongyu Sun; Kefan Zhang; Boran Lin; Ruiqi Huang; Xiangchun Yang; Shuangshuang Li; Mengying Liang; Lei Nie; Wenping Yin; Hui Wang; Hui Zhang; Lian Li; Aoli Wu; Hengchang Zang

doi:10.1016/j.saa.2023.122952

Real-time in-line prediction of drug loading and release rate in the coating process of diclofenac sodium spheres based on near infrared spectroscopy

Spectrochim Acta A Mol Biomol Spectrosc. 2023 Nov 15:301:122952. doi: 10.1016/j.saa.2023.122952. Epub 2023 Jun 1.

Authors

Zhongyu Sun¹, Kefan Zhang¹, Boran Lin¹, Ruiqi Huang¹, Xiangchun Yang¹, Shuangshuang Li¹, Mengying Liang¹, Lei Nie¹, Wenping Yin², Hui Wang², Hui Zhang¹, Lian Li³, Aoli Wu¹, Hengchang Zang⁴

Affiliations

¹ NMPA Key Laboratory for Technology Research and Evaluation of Drug Products, Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, 250012, Shandong, China.
² Shandong SMA Pharmatech Co., Ltd, Zibo, 255000, Shandong, China.
³ NMPA Key Laboratory for Technology Research and Evaluation of Drug Products, Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, 250012, Shandong, China; Key Laboratory of Chemical Biology (Ministry of Education), Shandong University, Jinan, 250012, Shandong, China.
⁴ NMPA Key Laboratory for Technology Research and Evaluation of Drug Products, Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, 250012, Shandong, China; Key Laboratory of Chemical Biology (Ministry of Education), Shandong University, Jinan, 250012, Shandong, China; National Glycoengineering Research Center, Shandong University, Jinan, 250012, Shandong, China. Electronic address: [email protected].

PMID: 37270976
DOI: 10.1016/j.saa.2023.122952

Abstract

The preparation of diclofenac sodium spheres by fluidized bed is a common production mode for the pharmaceutical preparations at present, but the critical material attributes in the production process is mostly analyzed off-line, which is time-consuming and laborious, and the analysis results lag behind. In this paper, the real-time in-line prediction of drug loading of diclofenac sodium and the release rate during the coating process was realized by using near infrared spectroscopy. For the best near infrared spectroscopy (NIRS) model of drug loading, R²_cv, R²_p, RMSECV, RMSEP were 0.9874, 0.9973, 0.002549 mg/g, 0.001515 mg/g respectively. For the best NIRS model of three release time points, the R²_cv, R²_p, RMSECV and RMSEP were 0.9755, 0.9823, 3.233%, 4.500%; 0.9358, 0.9965, 2.598%, 0.7939% and 0.9867, 0.9927, 0.4085%, 0.4726% respectively. And the analytical ability of these model was verified. The organic combination of these two parts of work constituted an important basis for ensuring the safety and effectiveness of diclofenac sodium spheres from the perspective of production process.

Keywords: Coating process; Drug loading; Near infrared spectroscopy; Real-time in-line prediction; Release rate.

MeSH terms

Diclofenac* / chemistry
Least-Squares Analysis
Spectroscopy, Near-Infrared* / methods

Substances

Diclofenac