A new crystal form of metoprolol succinate and its preparation method

A technology of metoprolol succinate and crystal form, applied in the field of new crystal form of metoprolol succinate and its preparation, can solve the problems of small particle size, poor fluidity, unfavorable preparation processing, etc.

Inactive Publication Date: 2017-06-20
ZHEJIANG SCI-TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, as far as the obtained crystalline form or amorphous form is concerned, the particle size is often small and the fluidity is poor, which is not conducive to the processing of preparations

Method used

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  • A new crystal form of metoprolol succinate and its preparation method
  • A new crystal form of metoprolol succinate and its preparation method
  • A new crystal form of metoprolol succinate and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Weigh 0.4g of metoprolol succinate raw material in a flask, add 10ml of methanol dropwise to the flask while stirring, dissolve at room temperature, place in a blast oven with temperature set at 80°C, and evaporate for 3h to obtain White blocky crystals, the target product is obtained after proper grinding, it is crystal form II by powder diffractometer, the diffraction pattern is shown in figure 1 , the measured particle size is 250±20μm. The calculated yield after weighing the product is about 93%.

[0030] The raw material of metoprolol succinate in the present invention refers to metoprolol succinate salt with a purity of more than 99.9%, which is available from many domestic pharmaceutical companies.

Embodiment 2

[0032] Weigh 1g of metoprolol succinate raw material in a flask, add 23ml of methanol dropwise to the flask while stirring, dissolve at room temperature, place in a blast oven with temperature set at 100°C, and evaporate for 2 hours to obtain white Blocky crystals, the target product can be obtained after proper grinding, the X-ray diffractometer test is the crystal form II, the thermal analysis detects and calculates its melting point to be 125.2°C, see the thermal analysis spectrum figure 2 , the measured particle size is 220±30μm. The product is weighed and the calculated yield is about 92%.

Embodiment 3

[0034] Weigh 0.8g of metoprolol succinate raw material in a flask, add 20ml of methanol dropwise to the flask while stirring, dissolve at room temperature, place in a blast oven with temperature set at 50°C, and evaporate for 24h to obtain White blocky crystals, the target product is obtained after proper grinding, the X-ray diffractometer test is the crystal form II, the infrared spectrum test results are shown in image 3 , the measured particle size is 180±30μm. The calculated yield after weighing the product is about 95%.

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Abstract

The invention provides a new crystal form of metroprolol succinate. The new crystal form of metroprolol succinate is a white powder crystal; molecular formula is C34H56N2O10; chemical name is 1-isopropylamino-3-[p-(2-methoxyethyl)phenoxyl]-2- propanol succinate; and corresponding 2 theta positions of X-ray's characteristic diffraction peaks are 3.8, 7.7, 10.7, 12.0, 14.3, 15.9, 18.1, 19.4, 20.3 and 23.4+ / -0.2 degree. The invention also provides a preparation method of the above new crystal form of metroprolol succinate, comprising the following steps: (1) a methanol solution or aqueous solution or methanol and water mixed solution of metroprolol succinate is prepared at room temperature, and the above solution is stirred to make the solution to be completely dissolved; (2) the above solution is evaporated slowly for a period of time under the high-temperature or room-temperature vacuum condition; and (3) a white product obtained is dried and crushed properly so as to obtain a large-granule target product.

Description

technical field [0001] The invention belongs to the field of development and preparation of new crystal forms of medicines, in particular to a new crystal form of metoprolol succinate and a preparation method thereof. Background technique [0002] Metoprolol is a selective β1-receptor blocker, which belongs to the aminopropanol class of drugs, and its effect on cardiac β1 receptors requires a lower dose than its effect on peripheral blood vessels and bronchial β2 receptors required dose. The selectivity of metoprolol succinate is dose-dependent, because the peak blood concentration of sustained-release tablets is significantly lower than that of ordinary plain tablets of the same dose, so that this dosage form has relatively higher β1 receptor selectivity. Metoprolol has no β-receptor agonism and almost no membrane activation. Beta-blockers have negative inotropic and chronotropic effects. [0003] Treatment with metoprolol attenuates the effects of catecholamines associa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C217/32C07C213/10C07C55/10C07C51/43
Inventor 张国庆敖桔刘松
Owner ZHEJIANG SCI-TECH UNIV
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