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A kind of crystal form I of curcumin derivative and its preparation method and application

A technology of curcumin derivatives and crystal forms, which is applied in the field of medicine, can solve the problems of unreported crystal forms, etc., and achieve the effects of good stability, good druggability, and excellent fluidity

Active Publication Date: 2021-09-03
WENZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] C66 is currently in the development stage, we have not reported any crystal form

Method used

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  • A kind of crystal form I of curcumin derivative and its preparation method and application
  • A kind of crystal form I of curcumin derivative and its preparation method and application
  • A kind of crystal form I of curcumin derivative and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0032] The preparation of the crystal form I of embodiment 1 curcumin derivative (C66)

[0033]Add 2.4 g of curcumin derivative (C66) into 60 mL of methanol, stir at room temperature for 2 hours, then take 40 mL and filter with a 0.22 μm filter head. The filtrate was placed in a fume hood to allow it to volatilize naturally at room temperature (temperature: 25° C. to 35° C., relative humidity: 35% to 65%. The same below). The precipitated solid was suction filtered and dried in vacuo. The obtained solid was subjected to experiments such as XRPD, DSC, and TGA.

Embodiment 2

[0034] The preparation of the crystal form I of embodiment 2 curcumin derivatives (C66)

[0035] 2.0 g of curcumin derivatives (C66) were added to 50 mL of acetone, stirred at room temperature for 2 hours, and then filtered through a 0.22 μm filter head. The filtrate was placed in a fume hood to allow it to evaporate naturally at room temperature. The precipitated solid was suction filtered and dried in vacuo. The resulting solid was subjected to experiments such as XRPD, DSC, and TGA.

Embodiment 3

[0036] The preparation of the crystal form I of embodiment 3 curcumin derivatives (C66)

[0037] 3.0 g of curcumin derivatives (C66) were added to 30 mL of methanol, stirred at room temperature for 2 hours, and then filtered through a 0.22 μm filter. Take 20mL of the filtrate, add 20mL of ethanol, mix well and place it in a fume hood to allow it to evaporate naturally at room temperature and atmosphere. The precipitated solid was suction filtered and dried in vacuo. The obtained solid was subjected to experiments such as XRPD, DSC, and TGA.

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Abstract

The invention discloses a crystal form I of a curcumin derivative (C66), a preparation method and an application thereof, and belongs to the field of medicine and chemical industry. The crystal form I of the present invention comprises the following characteristic peaks measured in the X-ray powder diffraction spectrum at 2θ reflection angles: 8.4±0.2°, 11.5±0.2°, 13.1±0.1°, 16.6±0.2°, 18.8±0.1° ( relative intensity maximum peak), 21.2±0.1°. At the same time, there are no sharp diffraction peaks at 33.5±0.2° and 38.1±0.2°. Compared with the other four crystal forms, this crystal form is the most thermodynamically stable crystal form. At the same time, the powder of Form I has good fluidity, no or almost no hygroscopicity, and can be kept stable for 2 weeks under high temperature and high humidity conditions. It has good preparation processing performance and has important application significance in the next step of drug development. .

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a crystal form I of a curcumin derivative (C66) and a preparation method and application thereof. Background technique [0002] Diabetes and its chronic complications have seriously affected human health and quality of life. In recent years, the incidence of diabetes has been on the rise. The prevalence of diabetes in all age groups worldwide was 2.8% in 2000 and is projected to be 4.4% in 2030. The number of people with diabetes will increase from 171 million in 2000 to 250 million currently, and is expected to rise to 333 million in 2030. In recent years, the incidence of diabetes in China has been on the rise. According to the epidemiological survey and statistics of the Diabetes Branch of the Chinese Medical Association, the number of diabetic patients in my country has reached 93 million, ranking first in the world, making the prevention and treatment of such diseases a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C45/81C07C49/697A61P3/10A61P13/12A61P9/12A61P31/20A61P37/08
CPCC07C49/697A61P3/10A61P13/12A61P9/12A61P31/20A61P37/08C07B2200/13C07C49/255
Inventor 梁广伍文奇钱建畅吴迪王怡
Owner WENZHOU MEDICAL UNIV
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