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Ozagrel sodium crystal type compound

A crystalline form of sodium ozagrel and a technology of sodium ozagrel, applied in the field of sodium ozagrel crystal compounds, can solve problems such as uncontrollable drug release, decreased stability, and low dissolution rate

Active Publication Date: 2016-04-13
ZHENGZHOU SIHUAN MEDICINE ARTICLE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The solubility of ozagrel in water is small, therefore, it is usually made into sodium salt (i.e. sodium ozagrel, English name: sodium ozagrel) in the art to improve its water solubility, but when it is made into sodium salt , its stability in aqueous solution decreased (see JP2001316265)
At present, ozagrel is mainly sold in the market as the injection of ozagrel sodium, but due to the stability of the sodium salt and the characteristics of the injection itself, this sodium salt preparation may be partially isomerized during storage and transformed into It is cis-imidazolium methyl cinnamic acid, or ozagrel dimer and other insoluble substances appear, not only the storage time is short, the transportation is very inconvenient, but also may bring other potential problems to clinical medication
Ozagrel hydrochloride ordinary compressed tablets are available in domestic and foreign marketed drugs at present, but this dosage form has the following problems: due to reasons such as preparation technology, all there is dissolution time long, dissolution rate is low after taking the oral preparation of most drugs, Poor absorption, many times of taking medicine, uncontrollable drug release, low bioavailability and other problems, which affect the efficacy of the drug and directly affect the therapeutic effect, so its bioavailability is low

Method used

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  • Ozagrel sodium crystal type compound
  • Ozagrel sodium crystal type compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take 5 grams of sodium ozagrel and add 15ml of DMF to water in a mixed solution with a volume ratio of 1:5, heat to reflux until fully dissolved, and slowly add dropwise a mixed solution of tetrahydrofuran and acetonitrile with a volume ratio of 1:3 under the condition of stirring under reflux, Until the solution is turbid, it is naturally cooled to room temperature, crystals are precipitated, filtered, and dried.

[0024] The X-ray powder diffraction pattern obtained by measuring the obtained ozagrel sodium crystal form compound using Cu-Kα rays, such as figure 1 shown.

[0025] Elemental Analysis Results:

[0026] Measured value (calculated value), C: 62.39 (62.40), H4.42 (4.43), N: 11.18 (11.20), O: 12.78 (12.79)

Embodiment 2

[0028] Take 10 grams of sodium ozagrel and add 30ml of DMF to water in a mixed solution with a volume ratio of 1:5, heat to reflux until fully dissolved, and slowly add dropwise a mixed solution of tetrahydrofuran and acetonitrile with a volume ratio of 1:3 under reflux and stirring conditions, Until the solution is turbid, it is naturally cooled to room temperature, crystals are precipitated, filtered, and dried.

[0029] The X-ray powder diffraction pattern obtained by measuring the obtained ozagrel sodium crystal form compound using Cu-Kα rays, such as figure 1 The results were similar, and the 2θ difference of the spectral data did not exceed ±0.2.

[0030] Elemental Analysis Results:

[0031] Measured value (calculated value), C: 62.37 (62.40), H4.40 (4.43), N: 11.16 (11.20), O: 12.78 (12.79)

Embodiment 3

[0033] Take 10 grams of sodium ozagrel and add 25ml of DMF to water in a mixed solution with a volume ratio of 1:5, heat to reflux until fully dissolved, and slowly add dropwise a mixed solution of tetrahydrofuran and acetonitrile with a volume ratio of 1:3 under the condition of reflux and stirring, Until the solution is turbid, it is naturally cooled to room temperature, crystals are precipitated, filtered, and dried.

[0034] The X-ray powder diffraction pattern obtained by measuring the obtained ozagrel sodium crystal form compound using Cu-Kα rays, such as figure 1 The results were similar, and the 2θ difference of the spectral data did not exceed ±0.2.

[0035] Elemental Analysis Results:

[0036] Measured value (calculated value), C: 62.38 (62.40), H4.43 (4.43), N: 11.19 (11.20), O: 12.76 (12.79)

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to an ozagrel sodium crystal type compound shown in a formula I. An X-ray powder diffraction pattern, obtained through Cu-K alpha ray measurement, of the compound is shown in figure 1. According to the ozagrel sodium crystal type compound, the bioavailability is improved.

Description

technical field [0001] The invention relates to the field of medicines, and relates to a crystal form compound of ozagrel sodium. Background technique [0002] In recent years, a series of thromboembolic diseases such as cerebral thrombosis, myocardial infarction, peripheral arterial thrombosis, deep vein thrombosis, and pulmonary embolism have seriously threatened human health. According to statistics, the death caused by it has reached 51% of the total death toll in the world. Therefore, thrombus, the ghost in blood vessels, is the common opponent of specialist doctors and has become the greatest enemy of human health. The manifestations of thromboembolic disease range from head to toe. Cerebral vascular thrombosis can cause dysfunction of one side of the limbs of the patient, that is, hemiplegia, aphasia, visual and sensory impairment, coma, and can be disabled or fatal. Cardiovascular thrombosis, that is, coronary artery thrombosis, can lead to severe angina pectoris ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/56A61K31/4174A61P9/10A61P7/02A61P25/14A61P9/08
CPCC07B2200/13C07D233/56
Inventor 郭琨
Owner ZHENGZHOU SIHUAN MEDICINE ARTICLE CO LTD
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