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共非晶化过程中的前沿方法。

Cutting-Edge Approaches in the Co-Amorphization Process.

作者信息

Mahmoud Azza A K, Regdon Géza, Kristó Katalin

机构信息

Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary.

出版信息

Pharmaceutics. 2025 Jun 29;17(7):850. doi: 10.3390/pharmaceutics17070850.

DOI:10.3390/pharmaceutics17070850
PMID:40733059
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12297907/
Abstract

Recently, the co-amorphization method has been widely used to refine the bioavailability characteristics of poorly soluble drugs in addition to overcoming the drawbacks of other traditional amorphization techniques. The main aim of this systematic review is to present an extensive outline of different co-former classes, co-former selection, and evaluation of produced co-amorphous systems. Methods: The systematic research was carried out based on three different databases, including PubMed, Scopus, and Web of Science time using co-amorphous, co-former, and drug as keywords. The selected papers were written in the English language and published between 2016 and 2024, and they focused on the co-amorphous systems, while articles discussing other amorphization techniques and crystallization processes were excluded. 127 peer-reviewed articles were selected and summarized. This paper revealed that amino acid is the most commonly used co-former, specifically arginine with acidic drugs and tryptophan with acidic and basic drugs, and it reported other co-formers that were used and different co-amorphous systems with their dissolution behaviour and stabilities, and different computational tools that were applied in the selection of co-former and process result evaluation.

摘要

最近,共无定形化方法除了克服其他传统无定形化技术的缺点外,还被广泛用于改善难溶性药物的生物利用度特性。本系统综述的主要目的是对不同种类的共形成剂、共形成剂的选择以及所制备的共无定形体系的评估进行全面概述。方法:基于三个不同的数据库进行系统研究,包括PubMed、Scopus和Web of Science,使用“共无定形”“共形成剂”和“药物”作为关键词,检索时间范围为2016年至2024年。所选论文为英文撰写且聚焦于共无定形体系,同时排除了讨论其他无定形化技术和结晶过程的文章。共筛选并总结了127篇同行评议文章。本文表明氨基酸是最常用的共形成剂,特别是精氨酸与酸性药物、色氨酸与酸性和碱性药物搭配使用的情况,并报道了其他使用的共形成剂以及不同共无定形体系的溶解行为和稳定性,还介绍了在共形成剂选择和工艺结果评估中应用的不同计算工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9919/12297907/5c52c8a7241a/pharmaceutics-17-00850-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9919/12297907/75d74f519296/pharmaceutics-17-00850-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9919/12297907/5c52c8a7241a/pharmaceutics-17-00850-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9919/12297907/75d74f519296/pharmaceutics-17-00850-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9919/12297907/5c52c8a7241a/pharmaceutics-17-00850-g002.jpg

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本文引用的文献

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Nucleotides as new co-formers in co-amorphous systems: Enhanced dissolution rate, water solubility and physical stability.核苷酸作为共无定形系统中的新共晶形成剂:提高溶解速率、水溶性和物理稳定性。
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Multicomponent Amorphous Solid Forms of Telmisartan: Insights into Mechanochemical Activation and Physicochemical Attributes.替米沙坦的多组分无定形固体形式:机械化学活化与物理化学性质的深入研究。
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Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying.
喷雾干燥制备辛伐他汀钙三水合物共无定形物改善其溶出度。
Chem Pharm Bull (Tokyo). 2024;72(2):190-199. doi: 10.1248/cpb.c23-00673.
4
Preparation and Characterization of a Rifampicin Coamorphous Material with Tromethamine Coformer: An Experimental-Theoretical Study.制备并表征利福平共无定形物与三羟甲基氨基甲烷共晶形成剂:实验-理论研究。
Mol Pharm. 2024 Mar 4;21(3):1272-1284. doi: 10.1021/acs.molpharmaceut.3c00947. Epub 2024 Feb 15.
5
Insight into Formation, Synchronized Release and Stability of Co-Amorphous Curcumin-Piperine by Integrating Experimental-Modeling Techniques.通过整合实验-建模技术深入了解姜黄素-胡椒碱共无定形物的形成、同步释放和稳定性。
J Pharm Sci. 2024 Jul;113(7):1874-1884. doi: 10.1016/j.xphs.2024.02.009. Epub 2024 Feb 12.
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Monophasic coamorphous sulpiride: a leap in physicochemical attributes and dual inhibition of GlyT1 and P-glycoprotein, supported by experimental and computational insights.单相共无定形舒必利:物理化学特性的飞跃以及对甘氨酸转运体1和P-糖蛋白的双重抑制作用,得到实验和计算分析的支持。
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7
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