Gastrodin medicine, and composition and use thereof

A technology of gastrodin and acetylgastrodin, which is applied in the field of medicine, can solve problems such as unpublished literature reports, and achieve the effects of improving hygroscopicity, facilitating storage and transportation, and preventing adhesion

Active Publication Date: 2015-05-20
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently published literature only reports on acetylgastrodin [C 21 h 26 o 11 , molecular weight: 454.15, CAS: 64291-41-4], preparation, pharmacology and clinical, etc., such as literature: Acetyl gastrodin orally disintegrating tablet for sedation, hypnosis and nervous headache and its preparation method, CN200410039846.2; The application of gastrodin in the preparation of drugs for pre

Method used

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  • Gastrodin medicine, and composition and use thereof
  • Gastrodin medicine, and composition and use thereof
  • Gastrodin medicine, and composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0069] Example 1 (attached figure 2 ), at the positions of the following 2θ values ​​about 6.29, 8.24, 9.75, 10.93, 12.65, 13.79, 14.17, 14.72, 15.58, 16.55, 16.94, 17.97, 19.60, 19.93, 20.32, 21.55, 21.92, 22.55, 24.00, 23.64 , 24.82, 25.33, 26.40, 27.42, 28.81, 29.64, 31.66, 34.01, etc. have characteristic peaks.

[0070] In another embodiment (implementation 2) (attached Figure 4 ), measured by powder X-ray diffractometry, within the measurement range of the diffraction angle 2θ (3-60°), the acetyl gastrodin 0.5 hydrate of the present invention can have corresponding eigenvalues ​​at positions including the following 2θ values, about 6.30, 8.33,9.80,11.00,12.59,13.84,14.21,14.78,15.61,16.64,17.08,18.04,19.65,20.02,20.36,21.61,21.96,22.60,23.70,24.30,25.27,26.53,27.66,28.58,29.65,31.75, There are characteristic peaks such as 34.43.

Example Embodiment

[0072] Example 2 Preparation of acetyl gastrodin 0.5 hydrate In a three-necked flask, add 230 ml of distilled tetrahydrofuran, 20 ml of methanol, 4-formylphenyl-2', 3', 4', 6'-tetraacetyl-β -D-glucopyranoside 10g, stir to dissolve, add sodium borohydride 0.5g, potassium borohydride 1g, stir, control the temperature between about 5-40 ℃, stir, monitor the reaction progress with thin layer chromatography (TLC) After the reaction is completed, the reactant is mixed with an appropriate amount of ice water, the pH of the solution is controlled to be about 6.5-7.0, and the stirring is continued for about 30 minutes, extracted with chloroform, and the chloroform extract is concentrated to dryness. Add an appropriate amount of activated carbon, stir for about 30 minutes, filter, add an appropriate amount of water to the filtrate until the solution is nearly cloudy, let cool, make the solid crystals fully separate out, filter, and the obtained solid is recrystallized three times with an...

Example Embodiment

[0073] Example 3 Preparation of acetyl gastrodin 0.5 hydrate In a three-necked flask, add 1000 ml of isopropanol, 30 ml of methanol, 4-formylphenyl-2', 3', 4', 6'-tetraacetyl-β- D-glucopyranoside 10g, stir to dissolve, add sodium borohydride 3g, stir, control the temperature at about 0-30 ℃, stir, monitor the reaction progress by thin layer chromatography (TLC), after the reaction is completed, the reactant Mix with an appropriate amount of ice water, control the pH of the solution to be about 6.5-7.0, continue stirring for about 30 minutes, extract with chloroform, concentrate the chloroform extract to dryness, add ethyl acetate to dissolve, add an appropriate amount of activated carbon, stir for about 30 minutes, filter , the obtained filtrate was concentrated to dryness, an appropriate amount of methanol was added for heating to dissolve, an appropriate amount of water was added, cooled, and the precipitated solid crystallized completely, filtered, and the obtained solid was...

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Abstract

The invention relates to a gastrodin medicine, and a composition and a use thereof, and also relates to a gastrodin derivative, and a preparation method and a use thereof. The gastrodin derivative has good storage stability, and is suitable for preparing medicines for increasing the cerebral blood flow, alleviating the cerebral vasospasm, calming, sleeping, easing pains, and treating or preventing Alzheimer's syndrome.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides gastrodin derivatives and compositions thereof, which have the effects of increasing cerebral blood flow and relieving cerebral vasospasm, sedation, hypnosis and analgesia, as well as their preparation and application. Background technique [0002] Acetyl gastrodin has the effects of increasing cerebral blood flow and relieving cerebral vasospasm, sedation, hypnosis and analgesia. Currently published literature only reports on acetylgastrodin [C 21 h 26 o 11 , molecular weight: 454.15, CAS: 64291-41-4], preparation, pharmacology and clinical, etc., such as literature: Acetyl gastrodin orally disintegrating tablet for sedation, hypnosis and nervous headache and its preparation method, CN200410039846.2; The application of gastrodin in the preparation of drugs for preventing and treating vascular dementia and Alzheimer's disease, CN201010127264.5; acetyl gastrodin dripp...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/06A61K31/7034A61P9/00A61P9/08A61P25/20A61P25/04A61P25/28
CPCC07B2200/13C07H1/06C07H15/203
Inventor 刘力
Owner 刘力
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