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Preparation method of composition containing lacidipine

A technology of lacidipine and a composition, which is applied in the field of drug synthesis, can solve the problems of difficult dissolution and stability, long reaction route, insoluble in water, etc., and achieves advantages such as industrialization and clinical application, simplification of preparation process, and low The effect of production costs

Inactive Publication Date: 2015-06-10
哈药集团人民同泰医药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has the disadvantages of long reaction route, cumbersome operation and large pollution
At the same time, lacidipine is unstable under light, easy to decompose, and difficult to dissolve in water, so improving dissolution rate and stability has always been a difficult problem in the preparation process

Method used

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  • Preparation method of composition containing lacidipine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Dissolve 28g of tert-butyl triphenylphosphinoacetate in 60mL of absolute ethanol and set aside. Add 10 g of o-phthalaldehyde and 20 mL of absolute ethanol into a three-necked flask equipped with magnetic stirring, brine bath, thermometer, and dropping funnel, stir to dissolve, control the temperature at 10°C, and slowly add triphenylphosphine The tert-butyl acetate / dehydrated ethanol solution was added dropwise in 40 minutes, and the incubation reaction was continued for 30 minutes. Lower the reaction temperature to 5°C, add 28g ethyl aminocrotonate / 76mL absolute ethanol solution into the flask, stir well, then slowly add 20g trichloroacetic acid / 20mL absolute ethanol solution dropwise, control the dropping time at 60 minutes, After the dropwise addition, the temperature was kept and the reaction was continued for 1.5 hours. After the reaction was completed, the reaction liquid was poured into 400 mL of 5% sodium bicarbonate aqueous solution, and a yellow so...

Embodiment 2

[0028] Example 2: Add 10g of pure racidipine and 90g of mannitol to 400mL of absolute ethanol, stir at 50°C to dissolve completely, pour the hot solution into a tray, and vacuum dry at 30°C for 12 hours to obtain a white loose powder containing Composition of lacidipine.

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Abstract

The invention provides a preparation method of a composition containing lacidipine, which is characterized in that lacidipine is synthesized by a one kettle way and a two-step reaction, and the lacidipine is taken as an effective component. The synthesis technology comprises the advantages of shortened steps, simple operation, and green and safety; the dissolution rate of the composition is obviously increased, stability is better under illumination, and the preparation method is benefit for industrialization and clinical application.

Description

technical field [0001] The invention relates to a method for preparing a lacidipine-containing composition of an antihypertensive drug, belonging to the field of drug synthesis. Background technique [0002] Lacidipine (Lacidipine) is a new type of dihydropyridine calcium antagonist, which was first produced by the Italian Glaxo Company and put on the market in 1991. It is clinically listed as one of the first-choice drugs for the treatment of mild and moderate essential hypertension. [0003] The traditional lacidipine synthetic technique is that o-phthalaldehyde and tert-butyl triphenylphosphinoacetate carry out Wittig reaction earlier to obtain 3-(2-formylphenyl) tert-butyl acrylate, and then with 2-amino-2- Ethyl crotonate cyclization affords the product. It has the disadvantages of long reaction route, cumbersome operation and large pollution. At the same time, lacidipine is unstable under light, easily decomposed, and insoluble in water, so improving dissolution rat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61K31/4422A61P9/12
Inventor 范宁秦雅英张晓霞王敬伟
Owner 哈药集团人民同泰医药股份有限公司
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