L-amlodipine maleate compound, and preparation method and medicinal preparation thereof

A technology for levamlodipine and pharmaceutical preparations, applied in the field of medicine, can solve problems such as research on the form of solid existence, inability to form hydrates, etc., and achieve the effects of being conducive to production and storage, stable quality and better quality

Active Publication Date: 2015-02-04
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN01140027.7 discloses the hydrate forms of levamlodipine besylate, aspartate, acetate, sulfate, hydrobromide and tartrate (R, R) salt, and specifically discloses The preparation method of lodipine besylate dihydrate, but according to the composition and properties of the amlodipine salt hydrate part of the patent specification, whether it is the maleate of levamlodipine or the maleate of racemic amlodipine Tomate, none of which can form hydrates
CN200410104297.2 discloses a preparation method and refining method of levamlodipine maleate. The preparation method is to carry out a salt-forming reaction between levamlodipine and maleic acid to obtain a crude product of levamlodipine maleate. The reaction system is acetic acid Ethyl ester or acetone; refined using ethanol as solvent, but not studied as a solid

Method used

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  • L-amlodipine maleate compound, and preparation method and medicinal preparation thereof
  • L-amlodipine maleate compound, and preparation method and medicinal preparation thereof
  • L-amlodipine maleate compound, and preparation method and medicinal preparation thereof

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Effect test

Embodiment 1

[0032] Embodiment 1: Preparation of levamlodipine maleate compound of the present invention

[0033] a. Dissolve 10 g of crude levamlodipine maleate in 200 ml of acetone, and heat to 60° C. to dissolve to obtain solution 1;

[0034] b. Under the action of an ultrasonic field (power 0.4KW), slowly add 50ml of purified water dropwise to solution 1, and turn off the ultrasonic field after adding, to obtain solution 2;

[0035] c. Lower the temperature of solution 2 to 20°C and maintain it, keep it warm and stir (40 rpm) for 2 hours, then lower the temperature to 10°C and maintain it, keep it warm for 5 hours to grow the crystal, and obtain solution 3;

[0036] d. The solution 3 was filtered, and the filter cake was dried at 50° C. for 5 hours to obtain 9.36 g of levamlodipine maleate compound of the present invention, with a yield of 92.0%.

Embodiment 2

[0037] Embodiment 2: Preparation of levamlodipine maleate compound of the present invention

[0038] a. Dissolve 10 g of crude levamlodipine maleate in 100 ml of acetone, and heat to 65° C. to dissolve to obtain solution 1;

[0039] b. Under the action of an ultrasonic field (power 0.3KW), slowly add 20ml of purified water dropwise to solution 1, and turn off the ultrasonic field after adding, to obtain solution 2;

[0040] c. Lower the temperature of solution 2 to 15°C and maintain it, keep stirring (60 rpm) for 0.5 hours, then lower the temperature to 5°C and maintain it, keep the crystal for 3 hours to obtain solution 3;

[0041] d. The solution 3 was filtered, and the filter cake was dried at 60° C. for 1 hour to obtain 9.28 g of the levoamlodipine maleate compound of the present invention, with a yield of 91.2%.

Embodiment 3

[0042] Embodiment 3: Preparation of levamlodipine maleate compound of the present invention

[0043] a. Dissolve 10 g of crude levamlodipine maleate in 300 ml of acetone, and heat to 50° C. to dissolve to obtain solution 1;

[0044] b. Under the action of an ultrasonic field (power 0.5KW), slowly add 80ml of purified water dropwise to solution 1, and turn off the ultrasonic field after adding, to obtain solution 2;

[0045] c. Lower the temperature of the solution 2 to 18°C ​​and maintain it, keep stirring (50 rpm) for 1 hour, then lower the temperature to 7°C and maintain it, and keep the crystal for 6 hours to obtain solution 3;

[0046] d. The solution 3 was filtered, and the filter cake was dried at 45° C. for 3 hours to obtain 9.16 g of the levoamlodipine maleate compound of the present invention, with a yield of 90.1%.

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Abstract

The invention relates to an L-amlodipine maleate compound, and a preparation method and a medicinal preparation thereof, and belongs to the technical field of medicines. Element analysis, water analysis and thermogravimetric analysis (TGA) detection of the L-amlodipine maleate compound prepared in the invention determines that the molecular formula of the L-amlodipine maleate compound is C20H25ClN2O5.C4H4O4.0.5H2O. Compared with products in the market, the compound has better stability to light, temperature and humidity, is more suitable for preparing various forms of medicinal preparations, such as an L-amlodipine maleate tablet and an L-amlodipine maleate dispersible tablet, as a raw medicine.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a compound, a preparation method and a pharmaceutical preparation containing the same, in particular to a levoamlodipine maleate compound, a preparation method and a pharmaceutical preparation containing the same. Background technique [0002] Amlodipine is a long-acting dihydropyridine calcium ion antagonist developed by Pfizer of the United States. It was first listed in the UK in 1990 and entered the Chinese market under the trade name "Norvasc" in 1994. It is used for the treatment of various Types of hypertension and angina. Amlodipine binds to receptors, dissociates slowly, lowers blood pressure gently, and has obvious effects. It has no effect on myocardial conduction and contractility, does not cause sympathetic nerve excitation, and is safe for patients with heart failure. It has become the drug of choice for the treatment of hypertension. . Amlodipine is a racemic comp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61K31/4422A61P9/12A61P9/10
CPCC07D211/90
Inventor 高志峰张文静马园园胡瑞娟王小英
Owner CSPC OUYI PHARM CO LTD
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