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Amorphous lercanidipine hydrochloride and preparation method thereof

A lercanidipine hydrochloride, amorphous technology, used in pharmaceutical formulations, medical preparations containing active ingredients, cardiovascular system diseases, etc., can solve the problems of high cost, long cycle, cumbersome operation, etc., and achieve low cost and cycle time. Short, high-purity effects

Active Publication Date: 2012-07-11
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above method has high cost, long cycle and cumbersome operation in the process of commercialization

Method used

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  • Amorphous lercanidipine hydrochloride and preparation method thereof
  • Amorphous lercanidipine hydrochloride and preparation method thereof
  • Amorphous lercanidipine hydrochloride and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Add 10g of high-purity lercanidipine hydrochloride into 100mL of ethylene glycol dimethyl ether, adjust the pH to 7.5-8.0 with saturated aqueous sodium bicarbonate solution at 5°C under stirring, leave to stand and separate the layers, and separate the organic layer. Dry over sodium sulfate, filter, evaporate the filtrate under reduced pressure to remove most of the solvent, and dissolve the light yellow oil in 30ml of isopropanol for later use.

Embodiment 2

[0039] The preparation of embodiment 2 high-purity free state lercanidipine base DMF solution

[0040] Add 10g of high-purity lercanidipine hydrochloride into 100mL of ethylene glycol dimethyl ether, adjust the pH to 7.5-8.0 with saturated aqueous sodium bicarbonate solution at 5°C under stirring, leave to stand and separate the layers, and separate the organic layer. Dry over sodium sulfate, filter, and evaporate the filtrate under reduced pressure to remove most of the solvent. The light yellow oil is dissolved in 20ml of DMF and set aside.

Embodiment 3

[0041] Embodiment 3 Preparation of high-purity free state lercanidipine base acetonitrile solution

[0042] Add 10g of high-purity lercanidipine hydrochloride into 100mL of ethylene glycol dimethyl ether, adjust the pH to 7.5-8.0 with saturated aqueous sodium bicarbonate solution at 5°C under stirring, leave to stand and separate the layers, and separate the organic layer. Dry over sodium sulfate, filter, evaporate the filtrate under reduced pressure to remove most of the solvent, and dissolve the light yellow oil in 20ml of acetonitrile for later use.

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Abstract

The invention provides amorphous lercanidipine hydrochloride and a preparation method thereof. Lercanidipine hydrochloride is a third-generation dihydropyridine calcium antagonist and is mainly used for hypertension and angina in clinic. The invention provides amorphous lercanidipine hydrochloride with the purity being at least 98.5%, particularly at least 99.5% and more particularly at least 99.7%. The invention also provides a preparation method of high-purity amorphous lercanidipine hydrochloride.

Description

Technical field: [0001] The invention relates to a high-purity amorphous lercanidipine hydrochloride and a preparation method thereof. Clinically used for antihypertensive. Background technique: [0002] Lercanidipine Hydrochloride, a third-generation dihydropyridine calcium antagonist developed for the Italian Recordati company, was first listed in the Netherlands in December 1997, with the trade name Zanidip, and was launched in the UK, Italy, and Greece in 1998. It was subsequently launched in other European countries. [0003] Lercanidipine hydrochloride is a third-generation dihydropyridine calcium antagonist, which can reversibly block the Ca2+ inflow of L-type calcium channels in vascular smooth muscle cell membranes, dilate peripheral blood vessels and lower blood pressure. Highly lipophilic dihydropyridine calcium antagonist. Its antihypertensive mechanism is to block the calcium channel of arterial vascular smooth muscle and directly relax the vascular smooth mu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61K31/4422A61P9/12
Inventor 刘意林祁伟杨琰
Owner CHINA RESOURCES SAIKE PHARMA
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