Druggability enhancement by modification of physicochemical properties of drugs via crystal engineering
10.16438/j.0513-4870.2020-0813
- VernacularTitle:晶体工程学技术改善药物理化性质以提高成药性
- Author:
Xing-ye WENG
1
;
Zun-ting PANG
2
;
Shuai QIAN
2
;
Yuan-feng WEI
2
;
Yuan GAO
2
;
Jian-jun ZHANG
1
Author Information
1. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
2. School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China
- Publication Type:Research Article
- Keywords:
polymorphism;
amorphous;
coamorphous;
cocrystal;
physicochemical property;
ruggability
- From:
Acta Pharmaceutica Sinica
2020;55(12):2883-2891
- CountryChina
- Language:Chinese
-
Abstract:
The solubility/dissolution, hygroscopicity and mechanical properties of drug candidates have a profound effect on oral bioavailability, processability and stability. The physicochemical properties of crystalline drug are closely related to inner crystal structure. Crystal engineering technologies, as strategies of altering the crystal structure and tailoring physicochemical properties at molecular level, possess the potential of enhancing the pharmaceutical performance of product. The current article reviewed the modification of drug solubility/dissolution, hygroscopicity and mechanical properties by crystal engineering technologies through polymorphic selection, amorphization/co-amorphization, as well as co-crystallization, which provided a reference for the applications of pharmaceutical crystallography in improving physicochemical properties and druggability.
