Synchrotron-based X-ray in-situ imaging techniques for advancing the understanding of pharmaceutical granulation

• Published in: International journal of pharmaceutics Vol. 572; p. 118797
• Main Authors: Li, Chen, Zhu, Ning, Emady, Heather N., Zhang, Lifeng
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 15.12.2019
• Subjects: Acetaminophen - chemistry; Carboxymethylcellulose Sodium - chemistry; Cellulose - chemistry; Drug Compounding; Excipients - chemistry; Granulation; Humans; Hydrophobic and Hydrophilic Interactions; Ibuprofen - chemistry; Lactose - chemistry; Molecular Imaging; Nucleation; Particle Size; Pharmaceutical powders; Powders; Synchrotron; Synchrotrons; Technology, Pharmaceutical - methods; X-ray imaging; X-Rays; APAP; CCS; Nucleation; Granulation; LMH; VAR; HAR; Pharmaceutical powders; Synchrotron; MCC; IBU; X-ray imaging
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2019.118797

[Display omitted] Wet granulation of powders is a key unit operation in the pharmaceutical industry. Due to the complexity of the granulation process taking place in a short time, observing and measuring the granulation process is challenging with conventional experimental methods. In this study, synchrotron-based X-ray imaging techniques were, for the first time, employed to capture the dynamic granulation process with a single drop impacting method in pharmaceutical powder beds. Five common pharmaceutical excipients, two active pharmaceutical ingredients (APIs) and their mixtures were used as the powder beds. The dynamic interaction between the liquid binder and solid powders were observed from high resolution X-ray images captured. Results show that pharmaceutical powder properties, including particle size, hydrophilicity, and morphology, have significant influence on the dynamic granulation process and the final granular product.