Asarone injection and preparation method thereof

A Xinnao injection and asarone technology are applied in medical formulas, medical preparations of non-active ingredients, and the digestive system. It can solve the problems of toxic and side effects of lysophospholipids, complex dispersion systems, and high production costs. It achieves high solubilization ability, Good reconstitution effect and increased solubility

Active Publication Date: 2010-02-17
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, phospholipids are very easy to oxidize, and nitrogen protection is required during production, resulting in high production costs; the produced lysophospholipids have strong toxic and side effects, and are impurities that must be strictly controlled in injections
When the formulation does not contain phospholipids, a variety of surfactants are used in combination. Since different surfactants exist in different phases, the dispersion system is too complicated, resulting in potential safety hazards, that is, most of the surfactants can form micelles. , the particle size is small, but some surfactants can also form vesicles, and the particle size is large, so the loaded drug will gather in some parts due to the particle size, and the local high concentration will cause toxicity
In addition, the preparations prepared by this method are all prepared by dissolving drugs and auxiliary materials in ethanol, making concentrated solutions for storage, adding 10 times the amount of normal saline or 5% glucose solution to dilute before use, and the solution contains 10% ethanol, which has certain side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh 50mg of α-asarone and 500mg of HS15, add 7ml of water for injection, stir in a 50°C water bath until completely dissolved, add 500mg of glucose, 5mg of sodium bisulfite and 1mg of calcium sodium edetate, stir to dissolve, add 0.2 Stir with activated carbon for 20 minutes, filter to remove carbon, filter through a 0.22 μm microporous membrane, add water for injection to 10 ml, subpackage, and autoclave at 115° C. for 30 minutes to obtain α-asarone injection.

Embodiment 2

[0046] Weigh 50mg of β-asarone and 350mg of HS15, add 7ml of water for injection, stir in a 60°C water bath until completely dissolved, then add 90mg of sodium chloride, 5mg of sodium bisulfite and 1mg of calcium sodium edetate, stir to dissolve, Add 0.2% activated carbon and stir for 20 minutes, filter to remove carbon, filter through a 0.22 μm microporous membrane, add water for injection to 10 ml, subpackage, and autoclave at 121 ° C for 12 minutes to obtain β-asarone injection.

Embodiment 3

[0048] Weigh 50mg of α-asarone and 400mg of HS15, add 7ml of water for injection, stir in a 70°C water bath until completely dissolved, add 500mg of glucose, stir to dissolve, add 0.3% activated carbon and stir for 20 minutes, filter to remove carbon, 0.22μm micro Filter through a pore filter, add water for injection to 10ml, subpackage, and sterilize by autoclaving at 121°C for 15 minutes to obtain α-asarone injection.

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PUM

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Abstract

The invention provides an alpha-asarone injection. In the preparation of the alpha-asarone injection, alpha-asarone (with the chemical name of 2,4,5-trimethoxy-1-propenylbenzene) is used as an activecomponent and carbowax-12-hydroxy stearate is adopted as a solubilizing agent to prepare an injection, thereby effectively solving the problem that the asarone is not dissolved in water, and greatly enhancing the medicament carrying quantity of the injection. The injection prepared by the preparation method has the advantages of good stability and simple preparation technology.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an injection of asarone and a preparation method thereof. technical background [0002] The chemical name of α-asarone is 2,4,5-trimethoxy-1-propenylbenzene, which is one of the main active ingredients of the traditional Chinese medicine Shichangpu. Cough-relieving, blood-fat-lowering, choleretic, anti-cancer and other pharmacological effects; at the same time, it has different degrees of inhibitory effects on the growth of pneumococcus, staphylococcus aureus and Escherichia coli. Clinically, asarone has been widely used in the treatment of diseases such as upper respiratory tract infection, bronchitis, bronchial asthma, acute and chronic cholecystitis, cholelithiasis, and grand mal seizures, especially for pneumonia, bronchial asthma and chronic obstructive pulmonary disease ( For example, the treatment of acute exacerbations of chronic obstructive pulmonary disease a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/09A61K47/34A61P11/00A61P11/06A61P1/16A61P25/12A61K47/14
Inventor 许玉琼龚涛张志荣梁臻
Owner SICHUAN UNIV
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