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Crystal form of metoprolol succinate and preparation method thereof

A technology of torolol crystal form and torolol crystal, which is applied in the field of antihypertensive drugs, can solve problems such as crystal form research, and achieve the effects of good quality stability, high content, and low impurity content

Inactive Publication Date: 2014-01-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chinese patent CN102295569 discloses a preparation method of (S)-metoprolol succinate, which uses ethanol, acetone, and isopropanol to crystallize, but does not study the crystal form

Method used

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  • Crystal form of metoprolol succinate and preparation method thereof
  • Crystal form of metoprolol succinate and preparation method thereof
  • Crystal form of metoprolol succinate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1: Preparation of metoprolol succinate crystal form

[0056] Add 140g of crude metoprolol succinate, add 565ml of absolute ethanol, heat to reflux until the product dissolves, cool to 45°C within 1.5 hours, stir at 150 rpm, keep warm and stir for 1.0 hour, and cool to 0°C within 2.0 hours , Keep standing for 5.0 hours, precipitate crystals, filter with suction, and dry in vacuum to obtain 131.05 g of white solid, weight yield is 93.6%, melting point is 136.6-137.4°C.

Embodiment 2

[0057] Example 2: Preparation of metoprolol succinate crystal form

[0058] Add 140g of crude metoprolol succinate, add 280ml of absolute ethanol, heat to reflux until the product dissolves, cool to 55°C within 0.5 hours, stir at 100 rpm, keep warm and stir for 0.5 hours, and cool to 5°C within 1.5 hours , Keep standing for 5.0 hours, precipitate crystals, filter with suction, and dry in vacuum to obtain 70.14 g of white solid, with a weight yield of 50.1% and a melting point of 136.1-136.7°C.

Embodiment 3

[0059] Example 3: Preparation of metoprolol succinate crystal form

[0060] Add 140g of crude metoprolol succinate, add 420ml of absolute ethanol, heat to reflux until the product dissolves, cool to 47℃ within 1.5 hours, stir at 150 rpm, keep warm and stir for 1.0 hour, and cool to -5 within 2.0 hours Keep it at temperature for 2.0 hours, precipitate crystals, filter by suction, and dry in vacuum to obtain 133.42 g of white solid with a weight yield of 95.3% and a melting point of 136.2-136.8°C.

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Abstract

The invention discloses a crystal form of metoprolol succinate and a preparation method thereof. The X-ray diffraction of the crystal form of metoprolol succinate has peaks when the reflection angle 2theta is 7.4 + / - 0.2, 14.4 + / - 0.2, 20.4 + / - 0.2, 21.5 + / - 0.2 or 24.4 + / - 0.2. The crystal form of metoprolol succinate provided by the invention has high content (or purity), low impurity content and stable quality and provides safety guarantee for clinical application of a metoprolol succinate medicine.

Description

technical field [0001] The invention belongs to the field of antihypertensive drugs, in particular to a crystal form of metoprolol succinate and a preparation method thereof. Background technique [0002] Metoprolol is a β1-selective (cardioselective) adrenoceptor blocker, i.e. cardioselective drug. It is widely used clinically in the treatment of patients with various cardiovascular diseases such as hypertension, ischemic heart disease, chronic stable heart failure, and arrhythmia. . [0003] In 1975, AstraZeneca went on the market in the form of its tartrate under the trade name "Betaloc". Due to the high solubility of metoprolol tartrate (> 700mg / ml), in order to obtain a more slow and sustained release of metoprolol, AstraZeneca has developed a succinic acid with the trade name "Toprol-XL". Metoprolol, whose solubility in water at 37°C (270mg / ml) is significantly lower than that of metoprolol tartrate, and was approved by the US FDA in 1992 for the treatment of hyp...

Claims

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Application Information

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IPC IPC(8): C07C217/32C07C213/10
CPCC07B2200/13C07C213/10C07C217/32
Inventor 张雅然孙丙辉姚军金凯樊琳静李园园齐军彩
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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