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Levosimendan sodium crystal form and preparation method thereof

A technology for sodium and sodium crystals of levosimendan, which is applied in the field of levosimendan sodium crystal form and its preparation, can solve the problems of insolubility and irritation of levosimendan, achieve simple production process and operation, save energy, Effects of avoiding irritation and hemolysis

Active Publication Date: 2020-08-18
CHENGDU XINJIE HIGH TECH DEV CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Based on the above problems, on the one hand, the present invention provides a kind of levosimendan sodium, the levosimendan sodium has good solubility in water, solves the problem of levosimendan insoluble in water, can avoid levosimendan Irritation and hemolysis caused by using ethanol as a solvent in Mengdan injection

Method used

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  • Levosimendan sodium crystal form and preparation method thereof
  • Levosimendan sodium crystal form and preparation method thereof
  • Levosimendan sodium crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0058] Embodiment 1: Preparation of levosimendan sodium crystal form A

[0059] Add 2.9g of sodium hydroxide and 120ml of purified water into a 250ml flask, stir and dissolve at room temperature. Add 20 g of levosimendan and stir to dissolve levosimendan. Stir and crystallize at 5-10°C for 2 hours. Filter and wash the filter cake with 30ml of absolute ethanol. Dry under reduced pressure at 60°C to obtain 17.8 g of crystalline form A levosimendan sodium, with a weight yield of 89.0%.

[0060] After testing, its X-ray powder diffraction pattern is consistent with figure 1 Basically the same, HPLC purity and figure 2 Basically the same.

[0061] figure 1 Among them, crystalline form A levosimendan sodium has characteristic peaks at 2θ of 12.101°, 15.139°, 18.338°, 19.403°, 22.956°, 24.301°, 27.451°, 29.397°, 32.342°, 33.899°.

Embodiment 2

[0062] Embodiment 2: Preparation of levosimendan sodium crystal form A

[0063] Add 2.8g of sodium hydroxide and 200ml of absolute ethanol into a 500ml flask, and heat to about 40°C to dissolve the sodium hydroxide. Add 20g of levosimendan, stir into salt. Stir and crystallize at 10-15°C for 4 hours. Filter and wash the filter cake with 30ml of absolute ethanol. Dry under reduced pressure at 40°C to obtain 16.7 g of crystalline form A levosimendan sodium. The weight yield is 83.5%.

[0064] After testing, its X-ray powder diffraction pattern is consistent with figure 1 Basically the same, HPLC purity and figure 2 Basically the same.

Embodiment 3

[0065] Embodiment 3: Preparation of levosimendan sodium crystal form A

[0066] Add 3.9 g of sodium ethoxide and 150 ml of methanol into a 500 ml flask, and heat to about 40° C. to dissolve the sodium ethoxide. Add 20g of levosimendan, stir into salt. Stir and crystallize at 5-10°C for 5 hours. Filter and wash the filter cake with 20ml of methanol. Dry under reduced pressure at 40°C to obtain 15.0 g of crystalline form A levosimendan sodium, with a weight yield of 75.0%.

[0067] After testing, its X-ray powder diffraction pattern is consistent with figure 1 Basically the same, HPLC purity and figure 2 Basically the same.

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Abstract

The invention discloses levosimendan sodium represented by a formula I and a crystal form of the levosimendan sodium, and the levosimendan sodium and the levosimendan sodium crystal form A has good solubility in water and is beneficial to production of a preparation.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a crystal form of levosimendan sodium and a preparation method thereof. Background technique [0002] Levosimendan is the first listed variety among the new generation of cardiotonic drugs-calcium sensitizers, and it is mainly used clinically to treat various acute heart failure diseases. The drug was developed by the Finnish company Orion and was first listed in Sweden in October 2000. At present, Zuosimendan has been listed and used in dozens of countries including Europe and the United States. But there is no public report that levosimendan and its pharmaceutically acceptable salt compounds are in use, especially levosimendan sodium and its thermally stable crystal form of levosimendan sodium are reported in open literature, and are used for the treatment of congestive Heart failure or symptoms of acute decompensated heart failure (ADHF). [0003] Levosimendan is insolubl...

Claims

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Application Information

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IPC IPC(8): C07D237/04
CPCC07B2200/07C07B2200/13C07D237/04
Inventor 刘力超黄汉伟蒲洪伍伟王刚强
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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