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J Pharm Sci ; 111(12): 3224-3231, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36202251

RESUMO

Gefitinib (GEF) is an anti-tumor oral solid formulation with a superior advantage for lung tumors. However, it has poor aqueous solubility which limits its utility in vivo. Herein, a novel cocrystal (GEF-RES) assembled by GEF and RES (Resveratrol) has been successfully prepared and comprehensively characterized by differential scanning calorimetry, thermogravimetric analysis, Raman spectroscopy and powder X-ray diffraction. A single-crystal structure of the GEF-RES cocrystal was solved and illustrated in detail. In aqueous hydrochloric acid, the GEF-RES cocrystal showed that the maximum concentration of GEF was slightly higher than that of raw GEF. Furthermore, the thermal and physical stability of the GEF-RES cocrystal were also evaluated in this paper. The enhanced solubility and excellent solid-state stability results may provide new potential to the application of key GEF in clinical.


Assuntos
Solubilidade , Resveratrol , Gefitinibe , Cristalização/métodos , Varredura Diferencial de Calorimetria , Difração de Raios X , Difração de Pó
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