New sunitinib malate crystal form and preparation method therefor

Abstract

The present invention relates to a new sunitinib malate crystal form and a preparation method therefor. The sunitinib malate is detected by Cu-Ka radiation to form an X-ray powder diffraction pattern, wherein characteristic peaks of Form VIII are at approximately 3.15 degree, 9.43 degree, 10.07 degree, 12.63 degree, 14.85 degree, 15.74 degree, 17.65 degree, 18.96 degree and 20.53 degree(2 theta). Characteristic peaks of Form IX are at approximately 3.09 degree, 7.63 degree, 9.15 degree, 9.63 degree, 12.16 degree, 12.84 degree, 15.21 degree, 16.13 degree, 18.36 degree, 18.93 degree, 22.47 degree and 27.39 degree(2 theta). The present invention further provides a method for preparing the Form VIII and the Form IX of the sunitinib malate. The sunitinib malate crystal form prepared by the preparation method is good in solubility, high in stability, and is suitable for industrial production.

Description

technical field

[0001] The invention relates to a new pharmaceutically acceptable crystal form of sunitinib malate and a preparation method thereof. technical background

[0002] Sunitinib is represented by formula (I), and its chemical name is N-[2-(diethylamino)ethyl]-5-[-(5-fluoro-1,2-dihydro-2-oxo- 3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide is a novel multi-targeted tyrosine kinase inhibitor (TKI).

[0003]

[0004] Polymorphism is defined as the ability of a substance to exist in two or more different crystal structures. Crystal form can affect different aspects of the solid-state properties of a drug, such as its solubility, stability, dissolution rate, crystallinity, bioavailability, and affect the preparation of pharmaceutical formulations and their properties.

[0005] Therefore, in order to pursue better solubility, bioavailability or stability, a lot of screening work has been carried out for different crystal forms of sunitinib malate....

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