New crystal form of ixabepilone and preparation method thereof

A technology of ixabepilone and crystal form, applied in the field of pharmaceuticals, can solve the problem of low susceptibility of tumor drug resistance mechanism

Active Publication Date: 2016-01-13
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, ixabepilone is less susceptible to tumor resistance mechanisms

Method used

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  • New crystal form of ixabepilone and preparation method thereof
  • New crystal form of ixabepilone and preparation method thereof
  • New crystal form of ixabepilone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Dissolve 0.4g of ixabepilone crude product (HPLC purity 99%) in 10ml of tetrahydrofuran, filter, and place the filtrate in a ventilated place away from light, and wait for tetrahydrofuran to volatilize and precipitate asbestos-like solids, filter, and dry in vacuo to obtain ixabepilone Form M.

Embodiment 2

[0048] Ixabepilone crude product 0.4g (HPLC purity 99%) was dissolved in 20ml of tetrahydrofuran, filtered, and the filtrate was placed in a ventilated place to avoid light, and the asbestos-like solid was precipitated after tetrahydrofuran volatilized, filtered, and vacuum-dried to obtain Ixabepilone Form M.

Embodiment 3

[0050] Ixabepilone crude product 0.4g (HPLC purity 99%) was dissolved in 30ml of tetrahydrofuran, filtered, and the filtrate was placed in a ventilated place to avoid light, and the asbestos-like solid was precipitated after tetrahydrofuran volatilized, filtered, and vacuum-dried to obtain Ixabepilone Form M.

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PUM

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Abstract

The invention provides a new crystal form of ixabepilone, which can be characterized by X-ray powder diffraction (XRD) spectrum, differential scanning calorimetry (DSC) spectrum, infrared absorption spectrum and the like. At the same time, the invention also provides a preparation method of the new crystal form of ixabepilone.

Description

technical field [0001] The present invention relates to the field of pharmacy. More specifically, the present invention relates to a new crystal form of ixabepilone and a preparation method of the new crystal form. technical background [0002] Ixabepilone is a new epothilone anti-tumor chemotherapy drug that is similar to paclitaxel in tubulin polymerization and inhibits microtubule depolymerization activity. It is developed and produced by Bristol-Myers Squibb. In October 2007, the FDA approved Ixempra as a single drug or in combination with capecitabine for the treatment of metastatic or locally advanced breast cancer refractory to anthracyclines, taxane derivatives and capecitabine. Ixabepilone is a semi-synthetic epothilone β-lactam analog, which belongs to a new generation of anti-mitotic drugs. Its mechanism of action is similar to that of paclitaxel. The cells undergo apoptosis and are superior to paclitaxel in terms of anti-tumor spectrum, anti-tumor activity, saf...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/044A61K31/427A61P35/00
CPCA61P35/00C07D491/044
Inventor 张亮王新增赵立柴健蔡青峰
Owner ZHEJIANG HISUN PHARMA CO LTD
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