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Gastrodin compound and preparation thereof

A technology for gastrodin and compound, applied in the field of gastrodin compounds and preparations thereof, can solve the problems of poor storage stability of gastrodin, loss of active ingredients, and reduced curative effect, etc., achieve good comprehensive physical and chemical properties, improve drug safety, and storage stability Good results

Active Publication Date: 2014-05-14
ANHUI YOUCARE KAIYUE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Gastrodin is a volatile oil, and the characteristic of volatile oil is that it is easy to volatilize when exposed to high temperature. Therefore, no matter whether Gastrodia elata is fried together or separately, the active ingredients will be lost due to high temperature, and the longer the frying time, the more active ingredients will be lost. , thereby reducing the curative effect, although gastrodin is extracted from Gastrodia elata in the pharmaceutical field and made into various dosage forms for patients to use, but in the prior art, gastrodin has disadvantages such as poor storage stability and easy moisture absorption.

Method used

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  • Gastrodin compound and preparation thereof
  • Gastrodin compound and preparation thereof
  • Gastrodin compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of Gastrodin Compounds

[0038] Take 50g of gastrodin crude product, add acetone to make a saturated solution at 40°C, stir for 40min, adjust the pH to 7, then add dimethyl sulfoxide whose volume is 1 / 5 of the volume of acetone, continue to heat up to 55°C and keep stirring for 0.5h, add For activated carbon decolorization, the amount of activated carbon added is 0.3% g / ml of the total volume of the liquid medicine, stirred and adsorbed for 30 minutes, decarbonized and sterilized by filtration; chloroform at 45°C is slowly added at a stirring rate of 30 rpm, and the volume of chloroform used is 1 / 2 of the volume of acetone. 4 times, after the addition, continue to stir at a rate of 20rmp and cool down to room temperature naturally, wash with acetone for 3 times, and dry under reduced pressure for 2h to obtain the final product. Yield 64.8%, HPLC content 99.90%.

[0039] The X-ray powder diffraction spectrum obtained by Cu-Kα ray measurement is figure 1 dis...

Embodiment 2

[0041] Preparation of Gastrodin Compounds

[0042]Take 50g of crude gastrodin, add acetone to make a saturated solution at 30°C, stir for 20min, adjust the pH to 6, then add dimethyl sulfoxide whose volume is 1 / 7 of the volume of acetone, continue to heat up to 45°C and keep stirring for 3h, add active For carbon decolorization, the amount of activated carbon added is 0.3% g / ml of the total volume of the liquid medicine, stirred and adsorbed for 30 minutes, decarbonized and sterilized by filtration; 55°C chloroform is slowly added at a stirring rate of 20 rpm, and the volume of chloroform used is 8% of the volume of acetone. After the addition, continue to stir at a rate of 10rmp and cool down to room temperature naturally, wash with acetone for 3 times, and dry under reduced pressure for 2h to obtain the product. The yield is 66.9%, and the HPLC content is 99.92%.

[0043] The X-ray powder diffraction pattern obtained by Cu-Kα ray measurement is consistent with the result of...

Embodiment 3

[0045] Preparation of Gastrodin Injection

[0046]

[0047] The ampoules are cleaned as usual for injections, first the initial washing and then the fine washing (the water for injection in the fine washing needs to be filtered through a 0.45 μm microporous membrane), then dried and sterilized for later use. Weigh gastrodin according to the prescribed amount, put it in an appropriate sterile container, add an appropriate amount of water for injection, stir to dissolve it, add water for injection until the prescribed amount is constant, and mix well. Add 0.05% (g / ml) activated carbon for needles, stir and adsorb at room temperature for 20 minutes, and filter to decarbonize. Filter with a 0.22 μm microporous membrane. Sampling, intermediate inspection (pH value, content, clarity), subpackage into 1ml ampoules after passing the test, make 1000 bottles, and melt seal. Autoclave at 115°C for 30 minutes. Light inspection, packaging, inspection, storage.

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Abstract

The invention relates to the technical field of medicines, and particularly relates to a gastrodin compound, a preparation method and a preparation thereof. An X-ray powder diffraction spectrum of the gastrodin compound, measured by using a Cu-K alpha ray, is shown as a figure 1. The preparation is of a tablet, a capsule, an injection and a powder injection. The gastrodin compound provided by the invention is good in stability, difficult in absorbing moisture, and better in comprehensive physical and chemical properties; and the gastrodin preparation, especially gastrodin injection, is good in storage stability, difficult in absorbing moisture, and high in bioavailability; and the medication safety of a patient is greatly improved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a gastrodin compound and its preparation. Background technique [0002] Gastrodin: English name is Gastrodin, CAS: 62499-27-8, molecular formula: C13H18O7, molecular weight: 286.28, English chemical name: 4-(hydroxymethyl)phenyl-β-D-Glucopyranoside, Chinese chemical name 4-hydroxymethylbenzene base-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 dizziness, numbness, and convulsions. Clinical application: treatment of vertebral-basilar artery insufficiency; treatment of vestibular neuronitis; treatment of vertigo. [0004] The patent application with the publication number CN101704855A discloses a preparation m...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/06A61K31/7034A61P25/20
Inventor 李琦杨磊
Owner ANHUI YOUCARE KAIYUE PHARMA
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