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A kind of aspirin crystal and its crystallization method and application

An aspirin and crystallization technology, applied in the field of aspirin crystals and their crystallization, can solve problems such as a large amount of preliminary data, complicated operation, difficulty in amplification, etc., and achieve the effects of less interference from external factors, strong experimental repeatability, and good fluidity.

Active Publication Date: 2021-09-21
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the method is complicated to operate, requires a large amount of early data, and is difficult to scale up.

Method used

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  • A kind of aspirin crystal and its crystallization method and application
  • A kind of aspirin crystal and its crystallization method and application
  • A kind of aspirin crystal and its crystallization method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] (1) in 500ml jacketed reactor, add the massfraction of 85g aspirin crude drug and 100g water and be the ethanol solution of 30%;

[0055](2) Add 0.05g polyvinylpyrrolidone to the mixed solution described in step (1), stir at 200rpm at a system temperature of 60°C, and add water at a rate of 1.5mL / min after the additive is completely dissolved.

[0056] (3) After 20 minutes, add 1.5g of aspirin crystals (aspirin crystals have been ground beforehand) and stop adding water, change the stirring to 100rpm for the first crystal growth;

[0057] (4) After the first crystal growth was completed for 30 minutes, water was added at a rate of 1.5 mL / min at a stirring rate of 200 rpm, so that the sum of the amount of water added this time and the amount of water added in step (2) was 130 g.

[0058] (5) After adding water, start to lower the temperature at a cooling rate of 0.2°C / min to lower the temperature of the reaction system to 5°C.

[0059] (6) After cooling down, change the...

Embodiment 2

[0062] The preparation steps are the same as in Example 1, except that 75 g of aspirin bulk drug is added in step (1), and the system temperature in step (2) is 50° C.

Embodiment 3

[0064] The preparation steps are the same as in Example 1, except that 103 g of aspirin bulk drug is added in step (1), and the system temperature in step (2) is 70° C.

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Abstract

The invention discloses an aspirin crystal, a crystallization method and application thereof. In the present invention, water-soluble polymer additives are added to the crystallization system, the ideal morphology of aspirin is obtained through molecular simulation, and the molecular arrangement of the (0 1 1) crystal plane is obtained by cutting, and it is found that the (0 1 1) crystal plane is composed of exposed hydroxyl groups, The carbonyl group and the oxygen atom in the ester group are easy to interact with polyvinylpyrrolidone to form hydrogen bonds and form strong adsorption. In addition, polyvinylpyrrolidone and vinylpyrrolidone-vinyl acetate copolymers have relatively large molecular weights and will not intercalate crystals. cells become impurities. The obtained product particles have small aspect ratio, good fluidity, high bulk density, high yield and up to standard impurity content. Strong repeatability, little interference from external factors, especially suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an aspirin crystal, a crystallization method and application thereof. Background technique [0002] Aspirin is a white crystal or crystalline powder, odorless or slightly smelly of acetic acid, slightly soluble in water, easily soluble in ethanol, soluble in ether and chloroform, and its aqueous solution is acidic. Aspirin has been clinically used for nearly a hundred years, and it has been proved that it is effective in relieving mild or moderate pain, such as toothache, headache, neuralgia, muscle pain and dysmenorrhea. Wait. In recent years, it has been found that aspirin has an inhibitory effect on platelet aggregation and can prevent the formation of thrombus. It is clinically used to prevent the formation of transient ischemic attack, myocardial infarction, artificial heart valve and venous fistula or other postoperative thrombus. [0003] A record of aspirin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C67/52C07C67/62C07C69/157A61K47/58A61K9/20A61P29/00A61P7/02
CPCA61K9/20A61K47/58A61P7/02A61P29/00C07B2200/13C07C67/52C07C67/62C07C69/157
Inventor 王学重李闯张扬
Owner SOUTH CHINA UNIV OF TECH
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