Correlation Engine 2.0
Clear Search sequence regions


Sizes of these terms reflect their relevance to your search.

Punch sticking during tablet manufacturing is a prevalent issue for many active pharmaceutical ingredients (APIs) encountered by the pharmaceutical industry. Tenofovir amibufenamide fumarate (TMF), a heavyweight drug for the treatment of hepatitis B, was selected as a model drug due to its tendency to punch sticking during tablet compression. In this study, the cause of sticking was explored by investigating crystal habits, excipients and structure characteristics. The difference in sticking of three crystal habits can be visually represented through direct compression experiments on powdered samples and analysis of crystal surfaces. The excipients play a direct role in decreasing the probability of sticking, and the extent of sticking can be assessed by measuring the tensile strength of the tablet. Additionally, the plasticity index was utilized to theoretically analyze the potential enhancements of four excipients. These experimental results indicate that the block-shaped crystals have superior ability of anti-sticking and that suitable excipients can significantly improve the sticking situation of TMF. Ultimately, the phenomenon of punch sticking was additionally examined through computational calculations, focusing on the mechanical characteristics of TMF molecules and intermolecular interactions. The strategy of combining experiments and simulation calculations has broader significance for the study of drug production. Copyright © 2024 Elsevier B.V. All rights reserved.

Citation

Chenyang Zhao, Xiaolei Wang, Yanbo Liu, Xueyou Qin, Weiqi Chen, Jin Zhang, Songgu Wu, Junbo Gong. Uncovering the mechanism of Tenofovir amibufenamide fumarate punch sticking by combining direct compression experiment and computational simulation. International journal of pharmaceutics. 2024 Mar 25;653:123813

Expand section icon Mesh Tags

Expand section icon Substances


PMID: 38272192

View Full Text