Gastrodine compound and pharmaceutical composition thereof

A technology of gastrodin and its compounds, which is applied in the field of gastrodin compounds and their pharmaceutical compositions, can solve problems related to unstable substances, complex processes, unstable pH value of gastrodin compounds, etc., and achieve improved safety and effectiveness, stable Enhanced performance and simple prescription process

Active Publication Date: 2013-07-31
湖北美林药业有限公司
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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, and the increase is relatively fast, which increases the gastrodin compound. Use of security risks
As can be seen from this, the prior art does not fully solve the existing problems of gastrodin, which limits the clinical use of gastrodin

Method used

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  • Gastrodine compound and pharmaceutical composition thereof
  • Gastrodine compound and pharmaceutical composition thereof
  • Gastrodine compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] 20 ℃, under the stirring speed of 150 rpm, gastrodin (commercially available gastrodin raw material, Jiangsu Hanstone Pharmaceutical Co., Ltd.) was dissolved in ethanol and methanol with a volume ratio of 1:8 at a volume ratio of 2:1. In the mixed solution; maintain 20°C, add gastrodin weight 1.0% activated carbon, stir at 150 rpm for 25 minutes, filter to remove carbon, filter the filtrate through a 0.22μm filter membrane; 25°C, at a stirring speed of 100 rpm , while stirring, slowly and uniformly add dropwise at a speed of 40ml / min a mixed solution of chloroform and ether whose volume ratio is 7 times that of ethanol and methanol mixture and whose volume ratio is 4:1; at the same time, the temperature is lowered to 8°C at a speed of 0.4°C / min, and the stirring is stopped. , cooling down to 2°C at a speed of 0.1°C / min and standing for crystal growth for 10 hours, then filtering; washing the filter cake obtained by filtering twice with a mixed solution of chloroform and ...

Embodiment 2

[0053] 25 ℃, under the stirring speed of 200 rev / mins, gastrodin (commercially available gastrodin raw material, Jiangsu Hanstone Pharmaceutical Co., Ltd.) was dissolved in ethanol and methanol with a volume ratio of 1:10 in a volume ratio of 2:1 In the mixed solution; maintain 25°C, add 1.0% gastrodin weight activated carbon, stir at 200 rpm for 25 minutes, filter to remove carbon, and filter the filtrate through a 0.22μm filter membrane; 30°C, at a stirring speed of 150 rpm , while stirring, slowly and uniformly add dropwise at a speed of 50ml / min a mixed solution of chloroform and ether whose volume ratio is 9 times that of ethanol and methanol mixture and whose volume ratio is 4:1; at the same time, the temperature is lowered to 10°C at a speed of 0.6°C / min, and the stirring is stopped , lower the temperature to 4°C at a rate of 0.2°C / min and let the crystal grow for 10 hours, filter; wash the filter cake obtained by filtering in 4 twice with a mixed solution of chloroform ...

Embodiment 3

[0055] prescription:

[0056] The gastrodin compound 100g that embodiment 1 makes

[0057] Mannitol 60g

[0058] Water for injection 2000ml

[0059] Make 1000 pieces

[0060] Process:

[0061] 1. Add the prescribed amount of gastrodin into 70% of the amount of water for injection, stir to dissolve at 30°C, add water for injection to 80%, then add mannitol according to the prescribed amount, stir to dissolve, add water for injection to the full amount, and stir evenly.

[0062] 2. Add 0.15% activated carbon to 1, stir for 20 minutes, decarbonize by filtration, and sterilize by filtration with a 0.22 μm filter membrane to detect intermediates.

[0063] 3. Freeze-drying:

[0064] ① Pre-freezing: Put the filtrate in 2 into a half-packed and stoppered container and place it in a pre-cooled freezer at -25°C, keep it for 1 hour, then cool it down to -35°C at a speed of 0.2°C / min, and keep it warm for 2 hours;

[0065] ②Sublimation: Turn on the vacuum device, control the vacuum ...

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Abstract

The invention relates to a gastrodine compound and a pharmaceutical composition thereof. The gastrodine compound is a crystal. The X-ray powder diffraction determines that the characteristic peaks are displayed when 2theta+/-0.2 degree is 4.5 degrees, 5.7 degrees, 7.9 degrees, 10.3 degrees, 11.2 degrees, 13.0 degrees, 16.4 degrees, 19.6 degrees, 21.2 degrees, 22.7 degrees, 24.8 degrees, 26.7 degrees, 29.6 degrees, 34.1 degrees and 35.3 degrees. The gastrodine compound has very high stability, thereby greatly enhancing the medicine safety. The invention also relates to a pharmaceutical composition preparation containing the gastrodine compound. The composition preparation can be a freeze-dried powder injection, injection, tablet or capsule. The gastrodine freeze-dried powder injection, injection, tablet or capsule preparation provided by the invention has the advantages of simple prescription technique, obviously higher stability, and enhances the medicine safety and effectiveness.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a gastrodin compound and a pharmaceutical composition thereof. Background technique [0002] Gastrodin, the chemical name is 4-hydroxymethylbenzene-β-D-glucopyranoside hemihydrate. 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. [0003] The commonly used dosage forms of using gastrodin clinically are: injection, powder injection, tablet, capsule etc., because gastrodin stability is relatively poor, in order to solve this problem prior art, generally adopt a large amount of auxiliary materials, as: stabilizer, complexing agent, buffer salt to solve this problem, the addition of a large nu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/06A61K31/7034A61P25/20A61P25/00
Inventor 李美林马虹
Owner 湖北美林药业有限公司
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