Perazopanib-quercetin eutectic crystal as well as preparation method and application thereof

A technology for pazopanib and quercetin, applied in the field of pazopanib-quercetin co-crystal and its preparation, can solve the problem of pazopanib co-crystal is less, achieve obvious curative effect and good stability , Significant effect of medical application value

Active Publication Date: 2022-07-15
SHENZHEN NYCRIST TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few reports on the pazopanib co-crystal in the prior art

Method used

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  • Perazopanib-quercetin eutectic crystal as well as preparation method and application thereof
  • Perazopanib-quercetin eutectic crystal as well as preparation method and application thereof
  • Perazopanib-quercetin eutectic crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Preparation of pazopanib-quercetin co-crystals:

[0027] The co-crystal was prepared according to the molar ratio of pazopanib and quercetin as 1:1, 21.88 mg of pazopanib and 15.11 mg of quercetin were weighed, and 5 mL of acetonitrile was added. At room temperature (25°C), the slurry was magnetically stirred for 3 days, filtered, and the filter cake was dried at 60°C for 2 hours to obtain a yellow solid, which was the pazopanib-quercetin co-crystal. The product was characterized using powder X-ray diffractometer (PXRD) and the results were as follows figure 1 shown. The PXRD pattern of the co-crystal was compared with pazopanib and quercetin, such as figure 2 shown. from figure 2 It can be seen that the PXRD pattern of the co-crystal is significantly different from that of pazopanib and quercetin. The characteristic peaks of the three are further compared, as shown in Table 1. It can be seen from Table 1 that the co-crystal has characteristic diffraction peaks ...

Embodiment 2

[0031] Preparation of pazopanib-quercetin co-crystals:

[0032] Prepare a co-crystal according to the molar ratio of pazopanib and quercetin as 1:2, weigh 21.88 mg of pazopanib and 30.22 mg of quercetin, add 5 mL of acetonitrile, and stir magnetically at room temperature (25°C). Beat for 3 days, filter, and place the filter cake to dry at 60°C for 2h. A yellow solid was obtained and characterized using a powder X-ray diffractometer (PXRD), and the results were as follows image 3 shown. from image 3 It can be seen that the characteristic diffraction peaks of this product are basically consistent with those of the product obtained in Example 1, that is, the pazopanib-quercetin co-crystal.

Embodiment 3

[0034] Stability of pazopanib-quercetin co-crystal:

[0035] The pazopanib-quercetin co-crystal obtained in Example 1 was placed in an artificial climate chamber under accelerated conditions (40°C, 75% RH), and samples were taken on the 5th and 10th days and X-rays were used It was characterized by powder diffractometer (PXRD), and the results were as follows Figure 4 shown. It can be seen from the figure that the pazopanib-quercetin co-crystal does not undergo crystal transformation under accelerated conditions for at least 10 days.

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PUM

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Abstract

The invention discloses a pezopanib-quercetin eutectic crystal as well as a preparation method and application of the pezopanib-quercetin eutectic crystal. The eutectic crystal is formed by pezopanib and quercetin, and in an X-ray powder diffraction pattern obtained through Cu-K alpha radiation measurement, the eutectic crystal has characteristic diffraction peaks when the diffraction angles 2 theta are 5.3 degrees +/-0.2 degrees, 7.6 degrees +/-0.2 degrees, 12.6 degrees +/-0.2 degrees, 15.3 degrees +/-0.2 degrees, 17.7 degrees +/-0.2 degrees and 20.0 degrees +/-0.2 degrees. The pezopanib-quercetin eutectic crystal is good in stability, and does not generate crystal form transformation in at least 10 days under an accelerated condition (40 DEG C, 75% RH). The preparation method is simple, and industrial production can be amplified. Quercetin is introduced, so that the solubility of the pezopanib-quercetin eutectic crystal is obviously higher than that of a pezopanib monomer.

Description

technical field [0001] The invention belongs to the field of medicine, and particularly relates to a pazopanib-quercetin co-crystal and a preparation method and application thereof. Background technique [0002] Renal cell carcinoma (renal cell carcinoma for short) is a highly malignant tumor in the urinary system and the second largest tumor in the genitourinary system in my country. Pazopanib is a first-line drug developed by GlaxoSmithKline for the treatment of advanced renal cell carcinoma. For vascular endothelial growth factor receptor (VEGFR), it works by inhibiting the formation of new blood vessels that supply blood to tumors. It has been reported that pazopanib is often discontinued due to adverse reactions, and hepatotoxicity is one of the common adverse reactions. For severe-grade hepatotoxicity caused by the use of pazopanib in the treatment of tumors, it is necessary to reduce the dose or take hepatoprotective drugs to prevent it. In addition, pazopanib is a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07D311/30C07D311/40A61P13/12A61P35/00A61K31/352A61K31/506
CPCC07D403/12C07D311/30C07D311/40A61P13/12A61P35/00A61K31/352A61K31/506C07B2200/13A61K2300/00
Inventor 田芳高明杨海武
Owner SHENZHEN NYCRIST TECH CO LTD
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