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Amorphous ivabradine hydrochloride

An amorphous technology of ivabradine hydrochloride, applied in the fields of active ingredients of heterocyclic compounds, cardiovascular system diseases, organic chemistry, etc., can solve problems such as high boiling point, non-specific crystal form, and high toxicity

Inactive Publication Date: 2009-12-09
BEIJING SHENLANHAI BIO PHARM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In addition, in the method for preparing the α crystal form provided in the patent CN1683341A, highly toxic solvents-toluene and "1-methyl-2-pyrrolidone" are used, and these solvents are more likely to remain in the product due to their higher boiling points
The method for preparing the βd crystal form provided in the patent CN1827599 is exactly the same as the method for preparing the β crystal form provided in the patent CN1827600, so the crystal form prepared according to this method is not specific, and it is difficult to selectively prepare the desired crystal form during the preparation process. type
Similarly, the method for preparing the γd crystal form provided in CN1827601 is exactly the same as the method for preparing the γ crystal form provided in the patent CN1827602, and the method for preparing the δ crystal form provided in the patent CN1948292 is the same as the method for preparing the δd crystal provided in the patent CN1948293. The method of crystal form is exactly the same, so there is the problem of poor specificity of crystal form preparation method

Method used

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  • Amorphous ivabradine hydrochloride
  • Amorphous ivabradine hydrochloride

Examples

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Effect test

Embodiment 1

[0020] The preparation of embodiment 1 amorphous ivabradine hydrochloride

[0021] 30 grams of ivabradine hydrochloride was dissolved in 500 milliliters of water to prepare ivabradine hydrochloride aqueous solution. Control the external temperature in a water bath to be less than 40°C, and distill to dryness under reduced pressure to obtain a white solid, which is detected by X-ray powder diffraction spectrum and is amorphous ivabradine hydrochloride.

Embodiment 2

[0022] The preparation of embodiment 2 amorphous ivabradine hydrochloride

[0023] 30 grams of ivabradine hydrochloride was dissolved in 300 milliliters of anhydrous methanol to prepare ivabradine hydrochloride methanol solution. Control the external temperature in a water bath to be less than 40°C, and distill to dryness under reduced pressure to obtain a white solid, which is detected by X-ray powder diffraction spectrum and is amorphous ivabradine hydrochloride.

Embodiment 3

[0024] The preparation of embodiment 3 amorphous ivabradine hydrochloride

[0025] Dissolve 10 grams of ivabradine hydrochloride in 100 milliliters of ethanol (95) to prepare ivabradine hydrochloride ethanol solution. Control the external temperature in a water bath to be less than 40°C, and distill to dryness under reduced pressure to obtain a white solid, which is detected by X-ray powder diffraction spectrum and is amorphous ivabradine hydrochloride.

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Abstract

The invention discloses amorphous ivabradine hydrochloride and a preparation method thereof. The amorphous ivabradine hydrochloride is detected by means of powder X-ray diffraction and at least 80 percent of the amorphous ivabradine hydrochloride exists in an amorphous form. The preparation method of the amorphous ivabradine hydrochloride comprises a step of desolvating a solution containing the ivabradine hydrochloride to obtain an amorphous solid. In addition, the invention also relates to a medicament composite containing the amorphous ivabradine hydrochloride.

Description

field of invention [0001] The invention relates to amorphous ivabradine hydrochloride and a preparation method thereof. In addition, the present invention also relates to a pharmaceutical composition containing amorphous ivabradine hydrochloride. Background of the invention [0002] Ivabradine hydrochloride is an If inhibitor for the treatment of chronic stable angina symptoms in patients with normal sinus rhythm who are contraindicated or intolerant to beta-blockers. Ivabradine hydrochloride has the chemical structure shown below: [0003] [0004] European patent EP0534859 describes the preparation method and application of ivabradine hydrochloride, but does not clarify its crystal form. As we all know, crystal form is an important characteristic of pharmaceutical compounds, which involves the stability, solubility, bulk density and fluidity of drugs, and further involves the ease and stability of drug packaging, storage, transportation and preparation preparation. I...

Claims

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Application Information

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IPC IPC(8): C07D223/16A61K31/55A61P9/10
Inventor 雒岗贾炎张金城
Owner BEIJING SHENLANHAI BIO PHARM TECH
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