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Cabazitaxel amorphous crystal and preparation method thereof

A cabazitaxel, amorphous technology, applied in the field of the crystal form of cabazitaxel and its preparation

Active Publication Date: 2013-04-17
重庆兴泰濠制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the amorphous crystal of cabazitaxel has not been reported

Method used

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  • Cabazitaxel amorphous crystal and preparation method thereof
  • Cabazitaxel amorphous crystal and preparation method thereof
  • Cabazitaxel amorphous crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0157] Embodiment 1 Preparation of Cabazitaxel Amorphous Crystal

[0158] Add 5 g of cabazitaxel anhydrous crystals into 75 mL of ethanol, stir and dissolve, concentrate to dryness at 50°C to obtain cabazitaxel powder, and dry the cabazitaxel powder at 60°C under reduced pressure for 12 hours to obtain 4.9 g of cabazitaxel Race amorphous crystal. The purity detected by HPLC is ≥99.87%, the residue of ethanol detected by GC is 1608ppm, and the moisture is 0.9%.

Embodiment 2

[0159] Embodiment 2 Preparation of Cabazitaxel Amorphous Crystal

[0160] Dissolve 10 g of cabazitaxel hydrate crystals in 100 mL of dichloromethane and concentrate to dryness at 30°C to obtain cabazitaxel powder. Dry the cabazitaxel powder under vacuum at a temperature of 50-60°C to obtain 9.9g Cabazitaxel amorphous crystal. The purity detected by HPLC is ≥99.84%, the residual dichloromethane detected by GC is 13080ppm, and the water content is 0.5%.

Embodiment 3

[0161] Example 3 Preparation of Cabazitaxel Amorphous Crystal

[0162] Dissolve 10 g of cabazitaxel solvate crystals in 250 mL of acetone, then concentrate to dryness at 40°C to obtain cabazitaxel powder, and vacuum-dry the cabazitaxel powder at a temperature of 50-60°C to obtain 9.9 g of cabazitaxel He is an amorphous crystal. The purity detected by HPLC is ≥99.84%, the residual acetone detected by GC is 8562ppm, and the water content is 0.6%.

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Abstract

The invention relates to the field of cabazitaxel crystal forms and preparation methods thereof, in particular to a cabazitaxel amorphous crystal and a preparation method thereof. A DSC (differential scanning calorimetry) map of the cabazitaxel amorphous crystal has an exothermic peak at 210-260 DEG C. The cabazitaxel amorphous crystal is a novel crystal form of cabazitaxel, and has good stability. The preparation method simplifies operation steps, does not require special equipment, is low in production cost, and is suitable for industrial production.

Description

technical field [0001] The present invention relates to the field of crystal forms of cabazitaxel and preparation methods thereof, in particular to an amorphous form of cabazitaxel and a preparation method thereof. Background technique [0002] Prostate cancer is a disease with high incidence in elderly men. In Western countries, prostate cancer is the second most malignant tumor in men, second only to lung cancer. According to statistics, in 2001, 198,100 cases of prostate cancer were newly discovered in the world, and 31,500 cases died. In recent years, the incidence rate in our country has also been increasing year by year, and it has been listed as the third place among urinary system tumors, and the age of onset is also getting younger. [0003] Cabazitaxel is a second-line drug for the treatment of prostate cancer developed by Sanofi-Aventis in France. It was approved for marketing in the United States in June 2010. It is a semi-synthetic taxane-like small molecule co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14A61K31/337A61P35/00
Inventor 李靖姚全兴
Owner 重庆兴泰濠制药有限公司
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