A kind of acetyl gastrodin compound and its preparation method, preparation and application

A technology of acetylgastrodin and compounds, applied in the field of acetylgastrodin compounds and its preparation, can solve the problems of increasing the safety risk of acetylgastrodin, limiting the clinical use of gastrodin, and poor stability of acetylgastrodin

Active Publication Date: 2020-07-07
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the 1980s, Kunming Pharmaceutical Group Co., Ltd. carried out structural transformation of gastrodin, and exclusively developed highly active acetylgastrodin with high fat solubility and positive therapeutic effects on central nervous system, cardiovascular and cerebrovascular system diseases. (Acetagastrodin), because the stability of acetylgastrodin is relatively poor, in order to solve this problem, prior art generally adopts a large amount of auxiliary materials, as: stabilizing agent, complexing agent, buffer salt, the addition of a large amount of auxiliary materials has increased the use of acetylgastrodin Security Risk
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 kind of acetyl gastrodin compound and its preparation method, preparation and application
  • A kind of acetyl gastrodin compound and its preparation method, preparation and application
  • A kind of acetyl gastrodin compound and its preparation method, preparation and application

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preparation example Construction

[0032] The method for preparing the acetyl gastrodin compound of the present invention is prepared by reacting acetyl gastrodin and urea in an organic solvent system. The organic solvent is selected from alcohols, ketones, alkyl nitriles and cyclic ethers. One or more.

[0033] The mass ratio of acetyl gastrodin and urea is 6-10:1.

[0034] The alcohol is ethanol; the ketone is acetone.

[0035] The acetyl gastrodin compound preparation of the present invention is prepared by adding pharmaceutically acceptable auxiliary materials to the acetyl gastrodin compound to obtain powders, granules, tablets, capsules and pills.

[0036] The application of the acetyl gastrodin compound of the present invention is the application of the acetyl gastrodin compound in the preparation of drugs for preventing / treating cardiovascular and cerebrovascular diseases.

[0037] The present invention will be further explained with specific implementation cases below:

[0038] In the following examples, the tes...

Embodiment 1

[0058] Preparation of acetyl gastrodin and urea co-crystal compound:

[0059] Dissolve 4.54g of acetyl gastrodin in 20mL of ethanol, add 0.6g of urea, heat to 60°C, stir at 60°C for 60min, then cool to 5°C, after the reaction is over, filter, the solid obtained is washed with ethanol and dried , Collect solids. After testing, the solid obtained in this example is eutectic crystal form A, and its XRPD pattern is as figure 1 , Its DSC graph is like figure 2 , The TGA diagram is as figure 2 ,its 1 H NMR chart such as image 3 .

Embodiment 2

[0061] Preparation of acetyl gastrodin and urea co-crystal compound:

[0062] Dissolve 4.54 g of acetyl gastrodin in 20 mL of ethanol, add 0.6 g of urea, heat to 60°C, stir at 60°C for 60 minutes, and then cool to 5°C. After the reaction, the ethanol solvent will naturally volatilize to obtain a solid. Wash with ethanol and dry. After testing, the solid obtained in this example is consistent with the crystal form obtained in Example 1, and is eutectic crystal form A.

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Abstract

The invention discloses an acegastrodine compound as well as a preparation method, a preparation and application thereof. The acegastrodine compound is eutectic crystal of a compound in a formula (I) and urea, wherein the structural formula of the compound in the formula (I) is as shown in the specification (I). The preparation method is reaction of acegastrodine and the urea in an organic solvent system, wherein an organic solvent is one or more of alcohols, ketones, alkyl nitrile and cyclic ethers. The preparation is powder, a granule, a tablet, a capsule or a pill prepared by adding pharmaceutically acceptable auxiliary materials to the acegastrodine compound. The application is an application of the acegastrodine compound in preparation of drugs for preventing / treating cardiovascular and cerebrovascular diseases. The eutectic crystal of the acegastrodine and the urea is high in solubility and is beneficial to improvement of the drug absorption efficiency and improvement of the bioavailability of the drugs, and is of great significance in improvement of the curative effects and the security of the drugs.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to an acetyl gastrodin compound and a preparation method, preparation and application thereof. Background technique [0002] Acetyl gastrodin: English name is Acetagastrodin, CAS: 105054-56-6, molecular formula: C21H26O11, molecular weight: 454.42, chemical name: 4-hydroxymethylbenzene-2ˊ, 3ˊ, 4ˊ, 6ˊ-tetra-ο-acetyl-β -D-glucopyranoside. [0003] Gastrodin is extracted from the dried roots of the orchid plant Gastrodia elata. The raw material is produced in Yunnan. It has good sedative and sleeping effects, and can relieve symptoms of neurasthenia, insomnia and headache. The traditional Chinese medicine Tianma can treat headache, dizziness, numbness, convulsions and convulsions. Clinical application: treatment of vertebrobasilar artery insufficiency; treatment of vestibular neuronitis; treatment of vertigo. [0004] In the 1980s, Kunyao Group Co., Ltd. reformed the structure o...

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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