Preparation of tenofovir amibufenamide fumarate spherical particles to improve tableting performance and sticking propensity by designing a spherical crystallization process.

Autor: Liu Y; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China., Wang X; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Jiangsu Hansoh Pharmaceutical Group Co., Ltd, Jiangsu 222047, China., Zhao C; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China., Wang S; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China., Lian X; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Jiangsu Hansoh Pharmaceutical Group Co., Ltd, Jiangsu 222047, China., Chen W; Jiangsu Hansoh Pharmaceutical Group Co., Ltd, Jiangsu 222047, China., He L; Jiangsu Hansoh Pharmaceutical Group Co., Ltd, Jiangsu 222047, China., Chen M; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China. Electronic address: chenmingyang@tju.edu.cn., Wu S; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China. Electronic address: wusonggu@tju.edu.cn., Gong J; State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China; Haihe Laboratory of Sustainable Chemical Transformations, Tianjin 300192, China.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2024 Nov 15; Vol. 665, pp. 124709. Date of Electronic Publication: 2024 Sep 19.
DOI: 10.1016/j.ijpharm.2024.124709
Abstrakt: Tenofovir amibufenamide fumarate (TMF) is the first oral drug developed in Asia for the treatment of adult patients with chronic viral hepatitis B, however, further applications are limited by poor tableting performance and high sticking propensity. In this work, the spherulitic growth process of TMF has been designed and explored with the help of molecular dynamics simulation and process analysis technologies (ATR-FTIR, FBRM and EasyViewer). The spherical particles with high bulk density, good flowability and uniform particle size distribution are prepared by a simple quenching process. More importantly, experimental results show that spherical particles have higher average tensile strength (100.8% increase), higher plastic deformability and lower amount of punch sticking (87.4% decrease in 30 tablets) compared to the commercial powder products. These contributions not only shed light on the design principle of drug spherulitic growth processes, but also provide guidance for the manufacture of high-quality tablet products.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024. Published by Elsevier B.V.)
Databáze: MEDLINE
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