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Gastrodin drugs and their compositions and uses

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of acetylgastrodin and crystalline hydrate, which is applied in the field of medicine, can solve problems such as unpublished literature reports, and achieve the effects of improving hygroscopicity, improving operability, and facilitating storage and transportation

Active Publication Date: 2018-09-04
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 preventing and treating vascular dementia and Alzheimer's disease, CN201010127264.5; acetyl gastrodin dripping pills and its preparation method CN03143336.7, etc., but so far, there are no public reports at home and abroad Acetyl gastrodin crystal hydrate of the present invention [C 21 h 26 o 11 · n H 2 O, wherein n=0.5] and compositions thereof, as well as their preparation methods and uses

Method used

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  • Gastrodin drugs and their compositions and uses
  • Gastrodin drugs and their compositions and uses
  • Gastrodin drugs and their compositions and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1 (attached figure 2 ), 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, 23.00, 243.6 , 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 diffraction method, within the measurement range of diffraction angle 2θ (3-60°), the acetylgastrodin 0.5 hydrate of the present invention can have corresponding characteristic values ​​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.

Embodiment 2

[0072] Example 2 Preparation of Acetyl Gastrodin 0.5 Hydrate In a three-necked flask, add 230ml of distilled THF, 20ml of methanol, 4-formylphenyl-2',3',4',6'-tetraacetyl-β -D-Glucopyranoside 10g, stir to dissolve, add 0.5g of sodium borohydride, 1g of potassium borohydride, stir, control the temperature between about 5-40°C, stir, monitor the reaction process with thin layer chromatography (TLC) After the reaction is completed, mix the reactant with an appropriate amount of ice water, control the pH of the solution to about 6.5-7.0, continue to stir for about 30 minutes, extract with chloroform, concentrate the chloroform extract to dryness, and add an appropriate amount of methanol to heat the obtained solid to dissolve it. 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 muddy, let it cool, and fully separate out the solid crystals, filter, and recrystallize the o...

Embodiment 3

[0073] Example 3 Preparation of acetylgastrodin 0.5 hydrate In a three-necked flask, add isopropanol 1000ml, methanol 30ml, 4-formylphenyl-2',3',4',6'-tetraacetyl-β- D-Glucopyranoside 10g, stir to dissolve, add 3g of sodium borohydride, stir, control the temperature at about 0-30°C, stir, monitor the reaction progress with thin layer chromatography (TLC), after the reaction is completed, the reactant Mix with an appropriate amount of ice water, control the solution pH=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 appropriate amount of activated carbon, stir for about 30 minutes, filter , Concentrate the obtained filtrate to dryness, add an appropriate amount of methanol to heat to dissolve, add an appropriate amount of water, cool, leave to precipitate the solid crystallization completely, filter, and recrystallize the obtained solid twice with an appropriate amount of ...

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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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Patent Type & Authority Patents(China)
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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