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Preparation method of fat emulsion of cerebral protection therapeutic drug

A fat emulsion and emulsifier technology, applied in the field of preparation, can solve the problems of increased hemolysis percentage, non-advocated use, toxic and side effects, and achieve the effects of reducing toxic and side effects, saving time and cost, and improving solubility

Active Publication Date: 2012-09-19
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poloxamers can replace sphingomyelin and gangliosides in the red blood cell membrane, resulting in an increase in the percentage of hemolysis. In addition, it has been reported in the literature that it can cause toxic side effects on the human kidney and cause azotemia, so it should not be used in the preparation of emulsions. Advocate the use of
In the Chinese patent CN101536979A formula, a high-concentration emulsifier is adopted, so the hemolysis percentage of the preparation is greatly improved, and the ethanol in the formula can produce certain arachidonic acid and thrombophlebitis (thrombophlebitis) by intravenous injection, which is This preparation is obviously inappropriate and unsafe for edaravone, a vascular drug preparation.

Method used

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  • Preparation method of fat emulsion of cerebral protection therapeutic drug
  • Preparation method of fat emulsion of cerebral protection therapeutic drug
  • Preparation method of fat emulsion of cerebral protection therapeutic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 Edaravone fat emulsion injection (0.15%):

[0047]

[0048] Preparation Process:

[0049] (1) Dissolve 12g of egg yolk lecithin with 100g of soybean oil for injection in a water bath at 70°C under nitrogen protection, add 1.5g of edaravone and 10g of vitamin E, heat and stir to dissolve, and obtain an oil phase;

[0050] (2) 22.5g glycerol and 5g EDTA were dissolved in 500ml water to obtain the water phase;

[0051] (3) Slowly add the oil phase to the water phase dropwise, at the same time under the protection of nitrogen, shear (shear speed: 10000r / min) for 20min, add water for injection to 1000ml to obtain colostrum, and use sodium hydroxide or hydrochloric acid if necessary Adjust the pH value to around 7.0;

[0052] (4) Under the pressure of 800-900 bar, the colostrum was homogenized 5-8 times by a high-pressure homogenizer, filtered through a microporous membrane, filled with nitrogen, potted, and sterilized under high pressure at 115° C. to obtai...

Embodiment 2

[0053] Embodiment 2 Edaravone fat emulsion injection (0.1%):

[0054]

[0055] Preparation Process:

[0056] (1) Dissolve 12g of egg yolk lecithin with 100g of soybean oil for injection in a water bath at 70°C under nitrogen protection, add 1g of edaravone and 10g of vitamin E, heat and stir to dissolve, and obtain an oil phase;

[0057] (2) 22.5g glycerol and 5g EDTA were dissolved in 500ml water to obtain the water phase;

[0058] (3) Slowly drop the oil phase into the water phase, and at the same time, shear for 20 minutes under the protection of nitrogen, replenish water for injection to 1000 ml, obtain colostrum, and adjust the pH value to about 7.0 with sodium hydroxide or hydrochloric acid;

[0059] (4) Under the pressure of 800-900 bar, the colostrum was homogenized by a high-pressure homogenizer for 5-8 times, filtered through a microporous membrane, filled with nitrogen, potted, and sterilized under high pressure at 115° C. to obtain a fat emulsion injection.

Embodiment 3

[0060] Long-chain Edaravone fat emulsion injection (0.5%) in Example 3:

[0061]

[0062] Preparation process: with embodiment 1.

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Abstract

The invention relates to an Edaravone fat emulsion injection and a preparation method thereof. The method comprises the following steps of: preparing Edaravone into a fat emulsion injection; and preparing a fat emulsion injection capable of being used for intravenous injection through homogenizing under high pressure by utilizing injection oil as a solvent and high-purity yolk lecithin with good biocompatibility as an emulsifier. Compared with the preparations clinically applied at present, the preparation is prepared without using organic solvents such as alcohol, propylene glycol, and the like and adding cosolvents such as poloxamer, and the like, thereby improving the medication safety, meanwhile, proved by animal experiments, the preparation has stronger antioxidative cerebral protection effect, and shown as relevant safety test results, the new preparation does not have the phenomena of hemolysis and blood vessel stimulation.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a medicinal injection preparation and a preparation method thereof, in particular to a fat emulsion injection with edaravone as an active ingredient and a preparation method thereof. Background technique [0002] Edaravone is a new type of free radical scavenger, the first oxygen free radical scavenger for the treatment of cerebral infarction developed by Japan's Mitsubishi Pharmaceutical Company and first listed in the world in 2001. Edaravone can scavenge free radicals and inhibit lipid peroxidation, thereby inhibiting the oxidative damage of brain cells, vascular endothelial cells, and nerve cells. [0003] At present, there is only one Edaravone preparation on the market at home and abroad, which is an ordinary water injection, but Edaravone is easily oxidized in a solution state, has poor stability, and has a short shelf life. In order to effectively solve this problem, in the preparat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4152A61K47/44A61P9/10A61P39/06
Inventor 王汝涛陈涛安龙王惟娇张阳
Owner XIAN LIBANG PHARMA
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