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New crystal of apatinib sulfate

A technology of sulfuric acid and crystal form, which is applied in the field of new crystal forms of apatinib sulfate, can solve the problems such as no patent of crystal form of apatinib sulfate, and achieves excellent stability, good solubility, and is conducive to preservation. Effect

Inactive Publication Date: 2016-06-01
华东理工常熟研究院有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there are no relevant patents on the crystal form of apatinib sulfate

Method used

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  • New crystal of apatinib sulfate

Examples

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Effect test

Embodiment 1

[0013] Embodiment 1. Preparation of new crystal form of apatinib sulfate

[0014] Weigh 500mg of apatinib sulfate into a container, add 100ml of acetone, suspend at 35°C for 48 hours, filter and vacuum dry to obtain a white powder, which is detected by XRPD, and the spectrum is as follows: figure 1 , the new crystal form is crystal form A.

Embodiment 2

[0015] Embodiment 2. Preparation of new crystal form of apatinib sulfate

[0016] Dissolve 500mg of apatinib sulfate in 100mL of acetonitrile, shake at 35°C for 48h, filter, dry, and vacuum-dry at room temperature to obtain a white powder, which is detected by XRPD, and the spectrum is as follows: figure 1 , the new crystal form is crystal form A.

[0017] It can be seen from the XRPD pattern that the diffraction peaks are about 3.681, 7.319, 10.96, 14.62, 15.54, 16.8, 17.62, 18.3, 18.699, 19.48, 20.74, 21.1, 21.58, 22.5, 23.159, 24.16, 24.7, 25.39, 26.77 28.079, 28.5, 29.06, 29.979, 31.181, 33.28, 35.42, where the error range of 2θ value is 0.2.

Embodiment 3

[0018] Example 3. Investigation of high-temperature stability of crystal form Apatinib sulfate

[0019] Place A crystal form sulfate Apatinib sample in 60 o C oven, after 5 days, the sample was taken out for XRPD test to investigate the stability of the crystal form of the sample to temperature. The results show that the crystal form A sample is stable under this condition.

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Abstract

The invention discloses a new crystal of apatinib sulfate; the new crystal has an XRPD pattern having diffraction peaks at 2 theta values approximately: 3.681, 7.319, 10.96, 14.62, 15.54, 16.8, 17.62, 18.3, 18.699, 19.48, 20.74, 21.1, 21.58, 22.5, 23.159, 24.16, 24.7, 25.38, 26.779, 28.079, 28.5, 29.06, 29.979, 31.181, 33.28, and 35.42, wherein a 2 theta value error range is 0.2. The new crystal has the advantages that the obtained crystal A of apatinib sulfate has the stability superior to that of an amorphous form, has good solubility, and is conducive to preservation.

Description

technical field [0001] The invention relates to a new crystal form of apatinib sulfate. Background technique [0002] The chemical name of Apatinib is N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide, which is a molecular targeted antitumor Drugs, a class of new drugs independently developed by Jiangsu Hengrui Medicine Co., Ltd., small molecule vascular endothelial growth factor tyrosine kinase inhibitors with independent intellectual property rights. [0003] The results of the study show that the existence state of the substance, that is, the crystal form of the drug, is an important factor affecting the efficacy of the drug. The same drug has different crystal forms, and its bioavailability may also be different. In addition, its stability, fluidity, and compressibility may also be different. These physical and chemical properties have an important impact on the application of the drug. In fact, drugs with different crystal forms can produ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/82
Inventor 任国宾弋东旭陈金瑶齐明辉洪鸣凰刘岩陈景艳黄志君
Owner 华东理工常熟研究院有限公司
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