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Monosialotetrahexosyl ganglioside sodium liposome injection

A technology of sodium ganglioside and monosialic acid, applied in the field of medicine

Inactive Publication Date: 2012-03-07
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0020] The purpose of the present invention is that the problem to be solved by the present invention is to overcome the defects of the prior art, provide a monosialotetrahexosylganglioside sodium liposome injection and its preparation method, the purpose is to solve the existing monosialic acid Tetrahexosyl ganglioside sodium preparation stability problem, liposomes play a protective role on the active ingredient, improve its bioavailability, and further effectively promote the blood-brain barrier of monosialotetrahexosyl ganglioside sodium permeability

Method used

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  • Monosialotetrahexosyl ganglioside sodium liposome injection
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  • Monosialotetrahexosyl ganglioside sodium liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 Preparation of Monosialotetrahexosylganglioside Sodium Liposome Injection

[0080] Prescription (1000 sticks)

[0081]

[0082] Preparation Process:

[0083] (1) 140g hydrogenated egg yolk lecithin, 60g soybean sterol, 50g poloxamer 188 and 36g sodium deoxycholate are dissolved in 2000ml volume ratio of isopropanol and ethanol mixed solvent of 1:3 to obtain lipid solution;

[0084] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 65° C. to form a uniform lipid film;

[0085](3) Dissolve 20g sodium monosialotetrahexosylganglioside, 0.6g sodium bisulfite and 18g sodium chloride in 600ml water, add it into a pear-shaped bottle and shake gently to elute the lipid film and disperse it in The hydration medium is dissolved to obtain the liposome suspension;

[0086] (4) Place the above-mentioned suspension in an ultrasonic instrument and sonicate to...

Embodiment 2

[0088] Example 2 Preparation of Monosialotetrahexosylganglioside Sodium Liposome Injection

[0089] Prescription (1000 sticks)

[0090]

[0091] Preparation Process:

[0092] (1) 400g hydrogenated egg yolk lecithin, 200g soybean sterol, 200g poloxamer 188 and 120g sodium deoxycholate are dissolved in 6000ml volume ratio of isopropanol and ethanol mixed solvent of 1:3 to obtain lipid solution;

[0093] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 55° C. to form a uniform lipid film;

[0094] (3) Dissolve 40g sodium monosialotetrahexosylganglioside, 1.6g sodium bisulfite and 18g sodium chloride in 600ml water, add it into a pear-shaped bottle and shake gently to elute the lipid film and disperse it in The hydration medium is dissolved to obtain the liposome suspension;

[0095] (4) Place the above-mentioned suspension in an ultrasonic instrument and sonicat...

Embodiment 3

[0097] Example 3 Preparation of Monosialotetrahexosylganglioside Sodium Liposome Injection

[0098] Prescription (1000 sticks)

[0099]

[0100] Preparation Process:

[0101] (1) 800g of hydrogenated egg yolk lecithin, 360g of soybean sterol, 450g of poloxamer 188 and 190g of sodium deoxycholate are dissolved in 15000ml of isopropanol and ethanol mixed solvent with a volume ratio of 1:3 to obtain a lipid solution;

[0102] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 60° C. to form a uniform lipid film;

[0103] (3) Dissolve 100g of sodium monosialotetrahexosylganglioside, 2g of sodium bisulfite and 45g of sodium chloride in 800ml of water, add it into a pear-shaped bottle and shake gently to elute the lipid film and disperse to hydrated The medium is dissolved to obtain a liposome suspension;

[0104] (4) Place the above-mentioned suspension in an ultras...

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Abstract

The invention discloses a monosialotetrahexosyl ganglioside sodium liposome injection and its preparation method. The liposome injection is made from monosialotetrahexosyl ganglioside sodium, hydrogenated egg yolk lecithin, soybean derived sterol, sodium deoxycholate, poloxamer 188, sodium bisulfite and other auxiliary materials. The liposome injection provided by the invention has good stability; the liposome will not break due to fusion and ice crystals during the freezing process and will also maintain good entrapment rate after stored for a long time. According to the invention, the quality of the preparation product is improved, toxic and side effects are minimized, retention time of the medicament in systematic circulation is increased, bioavailability and blood-brain barrier permeability of the medicament are raised and the curative effect is obviously enhanced. In addition, the preparation method is simple and is suitable for industrial production.

Description

technical field [0001] The invention relates to a monosialotetrahexosyl ganglioside sodium liposome, an injection thereof and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Monosialotetrahexosyl ganglioside sodium is a substance that is extracted from pig brain and has an effect on nerve cell function damage, and can promote the functional recovery of central nervous system damage caused by various reasons. The mechanism of action is to promote "neuroplasticity" (including the survival of nerve cells, axon growth and synapse growth). Monosialotetrahexosyl ganglioside is protective against neurodegeneration secondary to injury. Monosialotetrahexosyl gangliosides have positive effects on cerebral hemodynamic parameters and cerebral edema after injury. Monosialotetrahexosyl ganglioside reduces nerve cell edema by improving the activity of cell membrane enzymes. Animal experiments have shown that monosialotetrahexosyl...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7032A61K47/34A61K47/24A61P25/28A61P25/16
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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