Lu Gao, Xia-Lin Dai*, Shun-Yu Li, Nikita A. Vasilev, German L. Perlovich, Tong-Bu Lu and Jia-Mei Chen*,
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引用次数: 0
Abstract
Olaparib (OLA) is an insoluble targeting antitumor drug for the treatment of ovarian cancer. Herein, polyamorphism of OLA was systematically studied aiming to improve its solubility and dissolution properties. Three amorphous forms of OLA were prepared by ball milling (form I), rotary evaporation (form II), and melting (form III) methods, and the effects of polyamorphism on the morphology, thermodynamic properties, dissolution and gelation phenomenon, and the stability of OLA were studied for the first time. The results indicate that morphology has an impact on the gelation process of amorphous forms and thereby affects the dissolution of the drug. Among them, form II shows the best solubility and dissolution rate due to its slightest gelation, as well as relatively good stability and tabletability, which exhibits good application prospects in the amorphous solid formulation development of OLA.
期刊介绍:
The aim of Crystal Growth & Design is to stimulate crossfertilization of knowledge among scientists and engineers working in the fields of crystal growth, crystal engineering, and the industrial application of crystalline materials.
Crystal Growth & Design publishes theoretical and experimental studies of the physical, chemical, and biological phenomena and processes related to the design, growth, and application of crystalline materials. Synergistic approaches originating from different disciplines and technologies and integrating the fields of crystal growth, crystal engineering, intermolecular interactions, and industrial application are encouraged.