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Asarin compound and freeze-dried powder injection thereof

A technology of freeze-dried powder injection and asarone, applied in freeze-dried delivery, drug combination, organic chemistry, etc., to achieve ideal stability, ideal curative effect, simple and feasible preparation process

Active Publication Date: 2015-02-18
SHANXI PUDE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the above-mentioned technical methods cannot really meet the high requirements of the asarone raw material in the freeze-dried preparation itself and in the clinical application process. Therefore, it is still necessary to find an ideal asarone compound to further obtain stability, curative effect, etc. Significantly better than the prior art asarum freeze-dried powder injection

Method used

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  • Asarin compound and freeze-dried powder injection thereof
  • Asarin compound and freeze-dried powder injection thereof
  • Asarin compound and freeze-dried powder injection thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of embodiment 1 asarone compound

[0048] (1) Weigh 100g of asarone crude product, dissolve 96g of it in an organic solvent whose volume is equivalent to 6 times the weight of asarone crude product, and the organic solvent is acetonitrile / In ether / ethanol, stir evenly at a stirring speed of 15rmp to obtain solution A;

[0049] (2) Fully dissolve the remaining 4g of Asarone crude product in 0.05mol / L ethanol aqueous solution at 42°C with a stirring speed of 25rmp to form solution B;

[0050] (3) Within 2.5 hours, add solution B dropwise to solution A at a constant speed, while controlling the temperature of solution A at 22°C, stirring at a low speed of 8rmp during the feeding process;

[0051] (4) After the feeding is completed, the temperature of the solution is lowered to 2°C, placed in an ultrasonic field with a power of 0.2KW to grow crystals for 8 hours, filtered, the filter cake is washed with water, and dried at a low temperature below 40°C to o...

Embodiment 2

[0053] The preparation of embodiment 2 Asarone compounds

[0054] (1) Weigh 100g of asarone crude product, dissolve 95g of it in an organic solvent whose volume is equivalent to 5 times the weight of asarone crude product, and the organic solvent is acetonitrile / In ether / ethanol, stir evenly, the stirring speed is 5rmp, obtain solution A;

[0055] (2) Fully dissolve the remaining 5g of Asarone crude product in 0.075mol / L ethanol aqueous solution at 40°C with a stirring speed of 30rmp to form solution B;

[0056] (3) Within 2 hours, add solution B dropwise to solution A at a constant speed, while controlling the temperature of solution A at 20°C, stirring at a low speed of 5rmp during feeding;

[0057] (4) After the feeding is completed, the temperature of the solution is lowered to 0°C, placed in an ultrasonic field with a power of 0.1KW to grow crystals for 10 hours, filtered, the filter cake is washed with water, and dried at a low temperature below 40°C to obtain the asar...

Embodiment 3

[0059] The preparation of embodiment 3 asarone compounds

[0060] (1) Weigh 100g of asarone crude product, dissolve 98g of it in an organic solvent whose volume is equivalent to 8 times the weight of asarone crude product, and the organic solvent is acetonitrile / In ether / ethanol, stir evenly, the stirring speed is 25rmp, obtain solution A;

[0061] (2) Fully dissolve the remaining 2g of Asarone crude product in 0.025mol / L ethanol aqueous solution at 45°C with a stirring speed of 20rmp to form solution B;

[0062] (3) Within 2-3 hours, add solution B to solution A dropwise at a constant speed, while controlling the temperature of solution A at 25°C, stirring at a low speed of 10rmp during the feeding process;

[0063] (4) After the feeding is completed, the temperature of the solution is lowered to 5°C, placed in an ultrasonic field with a power of 0.3KW to grow crystals for 6 hours, filtered, the filter cake is washed with water, and dried at a low temperature below 40°C to ...

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Abstract

The invention discloses an asarin compound with a brand new activity. Both the asarin compound and a preparation thereof are remarkably superior to conventional asarin compounds in a stability test and the like. As the stability of the preparation can be remarkably improved by the asarin compound, the medication safety of patients can be guaranteed. Besides, the invention further discloses a preparation method of the asarin compound and a freeze-dried powder injection containing the asarin compound.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to asarone for injection and freeze-dried powder injection thereof. Background technique [0002] Asarone (2,4,5-trimethoxy-1-propenylbenzene), also known as asarone (Alpha-Asaronum), mainly exists in the volatile oil of plants such as Acorus granulues Soland , In 1982, my country's Liuzhou Pharmaceutical Factory succeeded in artificially synthesizing it for the first time in China. Since the 1960s, extensive research on asarone has been carried out at home and abroad, and it has been confirmed that it has strong pharmacological activity, and has cough-relieving, expectorant, asthma-relieving, sedative, antispasmodic and anticonvulsant effects. It also has different degrees of inhibitory effect on the growth of pneumococcus, staphylococcus aureus and Escherichia coli, and has received good results in clinical applications such as pneumonia, asthma, and grand ma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C43/205C07C41/40A61K31/09A61K9/19A61P11/14A61P11/10A61P11/06A61P25/20A61P25/08
Inventor 李立忠王勇解晓荣李润宝苏志强姚荷云闫洁胡成伟
Owner SHANXI PUDE PHARMA CO LTD
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