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A gastrodin compound and its preparation method, preparation and application

A technology of gastrodin and its compounds, which is applied in the field of gastrodin compounds and their preparation, can solve problems such as the stable existence of gastrodin, the instability of the pH value of gastrodin compounds, and the increase in the safety risk of gastrodin use, so as to achieve drug efficacy and Improved safety, simplified preparation and post-treatment process, and improved bioavailability

Active Publication Date: 2020-04-10
KPC PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of gastrodin in this application requires microwave and magnetic field control, and the process is extremely complicated, and we found in the test that the pH value of the gastrodin compound prepared in this application is unstable, and the related substances are also unstable, which increases rapidly, increasing the gastrodin compound. Use of security risks
It can be seen from this that the prior art does not completely solve the problem of the stable existence of gastrodin, which limits the clinical use of gastrodin

Method used

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  • A gastrodin compound and its preparation method, preparation and application
  • A gastrodin compound and its preparation method, preparation and application
  • A gastrodin compound and its preparation method, preparation and application

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preparation example Construction

[0030] The preparation method of the gastrodin compound of the present invention is prepared by reacting gastrodin and urea in an organic solvent system, and the organic solvent is one of alcohols, ketones, alkyl nitriles and cyclic ethers or more.

[0031] The mass ratio of gastrodin and urea is 4~5:1.

[0032] The alcohols are ethanol; the ketones are acetone.

[0033] The gastrodin compound preparation of the present invention is prepared by adding pharmaceutically acceptable auxiliary materials to the gastrodin compound to prepare powder, granule, tablet, capsule and pill.

[0034] The application of the gastrodin compound in the present invention is the application of the gastrodin compound in the preparation of drugs for the prevention / treatment of cardiovascular and cerebrovascular diseases.

[0035] The present invention will be further described below with specific implementation case:

[0036] In the following examples, the test methods are usually implemented acc...

Embodiment 1

[0056] Preparation of gastrodin and urea cocrystal compound:

[0057]Dissolve 2.86g gastrodin in 20mL ethanol, add 0.6g urea, heat to 60°C, stir at 60°C for 60min, then cool down to 5°C, filter after the reaction, wash the obtained solid with ethanol, dry, Collect solids. After testing, the solid obtained in this example is a eutectic compound of gastrodin and urea, and its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , its TGA diagram is shown in Figure 2, and its 1H NMR diagram is shown in Figure 3.

Embodiment 2

[0059] Preparation of gastrodin and urea cocrystal compound:

[0060] Dissolve 2.86g of gastrodin in 20mL of ethanol, add 0.6g of urea, heat to 60°C, stir at 60°C for 60min, then cool down to 5°C, after the reaction, the ethanol solvent is naturally volatilized, and the obtained solid is washed with ethanol Wash and dry. After testing, the solid obtained in this example is consistent with the crystal form obtained in Example 1.

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Abstract

The invention discloses a gastrodin compound and a preparation method, preparation and application thereof. The gastrodin compound is co-crystal of a compound as shown in the formula (I ) and urea, and the structural formula of the compound of the formula (I) is as shown in the specification. According to the preparation method, gastrodin and the urea react with each other in an organic solvent system to prepare the gastrodin compound, and the organic solvent is one or more of alcohols, ketones, alkyl nitrile and cyclic ethers. The preparation is powder, granules, tablets, capsules and pills which are prepared by adding pharmaceutically acceptable adjuvant materials in the gastrodin compound. The application is application of the gastrodin compound in preparation of drugs for preparing drugs for preventing and treating cardiovascular and cerebrovascular diseases. The solubility of the co-crystal of the gastrodin and the urea is high, the medicine absorbing efficiency is improved, the bioavailability of the medicine is improved, and therefore, the gastrodin compound plays an important role in improvement of curative effect of the medicine and the safety.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a gastrodin compound and its preparation method, preparation and application. Background technique [0002] Gastrodin: English name is Gastrodin, CAS: 62499-27-8, molecular formula: C 13 h 18 o 7 , molecular weight: 286.28, English chemical name: 4-(hydroxymethyl)phenyl-β-D-Glucopyranoside, Chinese chemical name: 4-hydroxymethylphenyl-β-D-glucopyranoside. [0003] Gastrodin is extracted from the dried root of the orchid plant Gastrodia elata, and the origin of the raw material is Yunnan. Gastrodin has good sedative and hypnotic effects, and can relieve neurasthenia, insomnia, and headache symptoms. The traditional Chinese medicine Gastrodia elata can treat headache, dizziness, limb numbness, convulsions and convulsions. Clinical application: treatment of vertebral-basilar artery insufficiency; treatment of vestibular neuronitis; treatment of vertigo. [0004] C...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/203C07H1/06C07C273/16A61K31/7034A61P9/00
CPCC07B2200/13C07C273/16C07H1/06C07H15/203
Inventor 宋立明普俊学董知旭杨兆祥
Owner KPC PHARM INC
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