Asarone injection and preparation method thereof

A Xinnao injection and asarone technology, which is applied in the fields of medical formula, digestive system, respiratory system diseases, etc., can solve the problems of lysophospholipid side effects and high production cost, and achieve high solubilizing ability, convenient clinical use, and stable quality

Inactive Publication Date: 2013-03-20
张蕊
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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

Method used

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  • Asarone injection and preparation method thereof
  • Asarone injection and preparation method thereof
  • Asarone injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 (1 part by weight of α-asarone, 8 parts of HS15, 50 parts of propylene glycol, and 12 parts of ethanol)

[0033] Weigh 4g α-asarone, 40g HS15, 200g propylene glycol, seal for use; measure 60ml of ethanol and seal for use; prepare 0.01mol / L hydrochloric acid solution with concentrated hydrochloric acid, seal for use; measure 500ml of water for injection, 60 Add 32g HS15 in a water bath at ℃, stir to dissolve; add 4g α-asarone in a water bath at 60℃, stir to dissolve, let cool to room temperature; add 200g propylene glycol and 60ml ethanol in turn, stir well; add water for injection to 950ml, Stir and mix evenly; adjust the pH to 6.03 with 0.01mol / L hydrochloric acid solution, add water for injection to 1000ml, mix evenly, first filter through a 0.45μm microporous membrane, then filter through a 0.22μm microporous membrane, and pack in Put it in a 2ml ampoule, melt seal it, and sterilize it at 100°C for 30 minutes to obtain α-asarone injection.

Embodiment 2

[0034] Example 2 (1 part by weight of α-asarone, 10 parts of HS15, 50 parts of propylene glycol, and 12 parts of ethanol)

[0035]Weigh 4g α-asarone, 40g HS15, 200g propylene glycol, seal for use; measure 60ml of ethanol and seal for use; prepare 0.01mol / L hydrochloric acid solution with concentrated hydrochloric acid, seal for use; measure 500ml of water for injection, 60 Add 40g HS15 in a water bath at ℃, stir to dissolve; add 4g α-asarone in a water bath at 60℃, stir to dissolve, let cool to room temperature; add 200g propylene glycol and 60ml ethanol in turn, stir well; add water for injection to 950ml, Stir and mix evenly; adjust the pH to 6.08 with 0.01mol / L hydrochloric acid solution, add water for injection to 1000ml, mix evenly, first filter through a 0.45μm microporous membrane, then filter through a 0.22μm microporous membrane, and pack in Put it in a 2ml ampoule, melt seal it, and sterilize it at 100°C for 30 minutes to obtain α-asarone injection.

Embodiment 3

[0036] Example 3 (1 part of α-asarone based on parts by weight, 12 parts of HS15, 50 parts of propylene glycol, and 12 parts of ethanol)

[0037] Weigh 4g α-asarone, 40g HS15, 200g propylene glycol, seal for use; measure 60ml of ethanol and seal for use; prepare 0.01mol / L hydrochloric acid solution with concentrated hydrochloric acid, seal for use; measure 500ml of water for injection, 60 Add 48g HS15 in a water bath at ℃, stir to dissolve; add 4g α-asarone in a water bath at 60℃, stir to dissolve, let cool to room temperature; add 200g propylene glycol and 60ml ethanol in turn, stir well; add water for injection to 950ml, Stir and mix evenly; adjust the pH to 6.10 with 0.01mol / L hydrochloric acid solution, add water for injection to 1000ml, mix evenly, first filter through a 0.45μm microporous membrane, then filter through a 0.22μm microporous membrane, and pack in Put it in a 2ml ampoule, melt seal it, and sterilize it at 100°C for 30 minutes to obtain α-asarone injection....

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PUM

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Abstract

The invention provides an alpha-asarone injection. The alpha-asarone injection is prepared by taking alpha-asarone (the chemical name is 2, 4, 5-triethoxy 1-propenylbenzene) as an active ingredient, and adopting polyethylene glycol-12-hydroxystearic acid as a solubilizer, adopting propylene glycol and ethanol as cosolvents. According to the alpha-asarone injection, not only the problem that asarone can not be dissolved in water can be effectively solved, but also the safety and the stabilization of the asarone injection are improved greatly. The asarone injection prepared by the invention has good stability and is simple in preparation process.

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. Background technique [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): A61K9/08A61K31/09A61K47/34A61P1/16A61P11/00A61P11/06A61P25/08
Inventor 张蕊
Owner 张蕊
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