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Aspirin pharmaceutical eutecticum, preparation method and application thereof

A technology of aspirin and co-crystal, which is applied in the field of aspirin drug co-crystal and its preparation, can solve the problems of gastric mucosa damage, ineffective drug effect, poor solubility, etc., and achieve good stability, prevention or treatment of cardiovascular diseases, The effect of high solubility

Active Publication Date: 2021-09-17
HEBEI AGRICULTURAL UNIV.
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the problems of poor solubility of aspirin in the stomach in the prior art, the drug effect cannot be fully exerted and damage to the gastric mucosa, etc., the present invention provides an aspirin drug co-crystal and its preparation method and application

Method used

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  • Aspirin pharmaceutical eutecticum, preparation method and application thereof
  • Aspirin pharmaceutical eutecticum, preparation method and application thereof
  • Aspirin pharmaceutical eutecticum, preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0043] This embodiment provides a kind of aspirin-tetramethylmethylpyrazine co-crystal, the preparation method comprises the following steps:

[0044]Weigh 720.6 mg of aspirin (molecular weight 180.16) and 544.8 mg of ligustrazine (molecular weight 136.2), add to a test tube, add 1 mL of acetonitrile, stir for 24 h at 25 ° C and 200 r / min, and then filter with filter paper to obtain The solid powder was placed in a fume hood to evaporate the solvent to obtain aspirin-tetramethylpyrazine co-crystal.

Embodiment 2

[0046] This embodiment provides a kind of aspirin-tetramethylmethylpyrazine co-crystal, the preparation method comprises the following steps:

[0047] Weigh 1441.2 mg of aspirin (molecular weight 180.16) and 1089.6 mg of ligustrazine (molecular weight 136.2), add to a test tube, add 2 mL of acetonitrile, and stir for 24 h at 20 ° C and 250 r / min, then filter with filter paper to obtain The solid powder was placed in a fume hood to evaporate the solvent to obtain aspirin-tetramethylpyrazine co-crystal.

Embodiment 3

[0049] This embodiment provides a kind of aspirin-tetramethylmethylpyrazine co-crystal, the preparation method comprises the following steps:

[0050] Weigh 720.6 mg of aspirin (molecular weight 180.16) and 544.8 mg of ligustrazine (molecular weight 136.2), add to a test tube, add 1 mL of acetonitrile, stir for 24 h at 30°C and 300 r / min, then filter with filter paper to obtain The solid powder was placed in a fume hood to evaporate the solvent to obtain aspirin-tetramethylpyrazine co-crystal.

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Abstract

The invention relates to the technical field of pharmaceutical eutecticums, and particularly discloses an aspirin pharmaceutical eutecticum, a preparation method and application thereof, wherein the aspirin pharmaceutical eutecticum comprises aspirin and ligustrazine in a molar ratio of 1:1. The preparation method comprises the following steps: adding aspirin and ligustrazine into acetonitrile, uniformly stirring and mixing, filtering, collecting powder, and drying to obtain the aspirin pharmaceutical eutecticum. According to the invention, aspirin and ligustrazine form the eutecticum, so that the problems that the aspirin is poor in solubility in the stomach and low in dissolution rate and the ligustrazine is prone to sublimation are solved, the problem that the aspirin and the ligustrazine have large stimulation on gastric mucosa is solved, the bioavailability of the aspirin and the ligustrazine is improved, and the eutecticum can be developed into various preparations, is used as a novel medicine for resisting blood coagulation, resisting thrombus and preventing or treating cardiovascular diseases, and has a relatively high application prospect.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to an aspirin drug co-crystal and a preparation method and application thereof. Background technique [0002] Aspirin (ASA), a class of non-steroidal anti-inflammatory drugs, was initially widely used for antipyretic, analgesic, and anti-inflammatory effects. Later, scientists found that aspirin can also inhibit the aggregation of platelets, so it can be used as an antithrombotic drug. Low-dose aspirin plays a crucial role in the prevention of adverse cardiovascular events, especially in patients with cardiovascular disease. However, aspirin is poorly soluble under gastric juice conditions due to the low pH in gastric juice that hinders the dissolution of aspirin, resulting in the accumulation of insoluble particles in the stomach, which can cause damage to the gastric mucosa, leading to gastritis And peptic ulcer and other problems, and lead to decreased bioavailability ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/157C07D241/12C07C67/52A61K31/616A61K31/4965A61P7/02A61P9/00
CPCC07C69/157C07D241/12C07C67/52A61K31/616A61K31/4965A61P7/02A61P9/00C07B2200/13A61K2300/00
Inventor 赵兴华何欣王凯茹
Owner HEBEI AGRICULTURAL UNIV.