Colchicine compound, preparation method, preparation, applications and pharmaceutical composition thereof

A technology of colchicine and compounds, applied in the direction of drug combination, organic chemical methods, antipyretics, etc., to achieve the effects of improved bioavailability, high product yield and purity, and improved safety performance

Inactive Publication Date: 2020-02-14
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few reports on the research on the amorphous form of colchicine

Method used

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  • Colchicine compound, preparation method, preparation, applications and pharmaceutical composition thereof
  • Colchicine compound, preparation method, preparation, applications and pharmaceutical composition thereof
  • Colchicine compound, preparation method, preparation, applications and pharmaceutical composition thereof

Examples

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preparation example Construction

[0048] The preparation method of colchicine compound of the present invention comprises the following steps:

[0049] A, heating and dissolving colchicine in a solvent, and filtering to obtain filtrate a;

[0050] B. Cool the filtrate a to -40°C~-30°C and pre-freeze for 3~5h, then sublimate and dry to obtain the target colchicine compound.

[0051] The colchicine in the step A is heated and dissolved at a temperature of 60-80° C., and the heating time is 0.5-2 hours.

[0052] The mass ratio of colchicine and solvent in step A is (0.01-50):100.

[0053] Described solvent is water, methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, ethylene glycol, propylene glycol, glycerol, acetone, ethyl acetate, dimethyl sulfoxide, N , One or more of N-dimethylformamide.

[0054] The sublimation drying described in step B is to control the temperature at -25°C~-20°C and the pressure 10~20Pa for 3~5h.

[0055] The analytical drying described in step B is to control the tem...

Embodiment 1

[0082] Example 1 Preparation of Amorphous Colchicine Compound 1# Sample

[0083] Weigh 0.5 g of colchicine, dissolve it in 100 g of water, heat and dissolve at 70-80°C for 1 hour, filter, put the filtrate in a vacuum freeze dryer, cool down to -40~-30°C, and pre-freeze for 3~5 hour, then control temperature -25~-20℃, pressure 10~20Pa, sublimation drying for 3~5 hours, finally control temperature 30~50℃, pressure 1~10Pa, analysis drying for 4~6 hours, that is.

Embodiment 2

[0084] Example 2 Preparation of Amorphous Colchicine Compound 2# Sample

[0085] Weigh 0.5 g of colchicine, dissolve in 10 g of methanol, heat and dissolve at 70-80°C for 1 hour, filter, put the filtrate in a vacuum freeze dryer, cool down to -40~-30°C, and pre-freeze for 3~ 5 hours, then control temperature -25~-20℃, pressure 10~20Pa, sublimation drying for 3~5 hours, finally control temperature 30~50℃, pressure 1~10Pa, analysis and drying for 4~6 hours, that is.

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Abstract

The invention relates to a colchicine compound, a preparation method, a preparation, applications and a pharmaceutical composition thereof, wherein the colchicine compound is amorphous and has a structure represented by a formula I, the X-ray powder diffraction pattern is represented by figure 2, the differential scanning calorimetry analysis curve is represented by figure 3, and the colchicine compound has an exothermic peak at a temperature of about 118.6 DEG C and an has an endothermic peak at a temperature of about 162.4 DEG C. According to the invention, the colchicine has good treatmenteffects on gout, arthritis, tumors, liver fibrosis and pulmonary fibrosis; compared with the products and the technologies in the prior art, the colchicine disclosed by the invention is amorphous, hasadvantages of goof heat resistance, good moisture resistance, stable properties and high bioavailability, and can well meet the requirements of clinical medication; and the preparation method provided by the invention is simple in process, mild in condition, convenient to operate, stable and controllable in quality and suitable for industrial large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a colchicine compound and its preparation method, preparation, application and pharmaceutical composition. Background technique [0002] Colchicine is a tropolone alkaloid firstly extracted from the bulbs and seeds of Liliaceae colchicine, and has a chemical structure as shown in the following formula I: [0003] [0004] In addition to colchicine contained in Liliaceae colchicine, other genus plants of Liliaceae, such as Auguillaria, Gloriosa, Iphigenia and Aracea, also contain colchicine. (Niel E, Scherrmann JM. Colchicine today [J]. Joint Bone Spine, 2006, 73: 672-678). Colchicine is also contained in Yunnan Guangguzi, Lijiang Arrowhead, and day lily (Shen Lihong, Li Ya. Research and application progress of colchicine[J]. China Agricultural Science Bulletin, 2009,25(21):185- 187). [0005] Colchicine has been clinically used as the first-line drug for the tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/24C07C233/32A61K31/165A61P19/06A61P19/02A61P29/00A61P35/00A61P9/00
CPCC07C231/24C07C233/32A61P19/06A61P19/02A61P29/00A61P35/00A61P9/00C07C2603/30C07B2200/07C07B2200/13
Inventor 周荣光赵加强顾静波王金郭泽剑
Owner KPC PHARM INC
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