Edaravone lipid microsphere formulation and preparation method

A technology of edaravone fat and microspheres, which is applied in the field of medicine, can solve problems such as poor stability, achieve the effects of improving stability, reducing side effects of drugs, and ensuring product quality

Inactive Publication Date: 2009-09-23
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For the defects that Edaravone injection exists in the prior art, the object of the present invention is to provide a kind of new Edaravone injection, to solve the problem of poor stability of existing Edaravone injection

Method used

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  • Edaravone lipid microsphere formulation and preparation method
  • Edaravone lipid microsphere formulation and preparation method
  • Edaravone lipid microsphere formulation and preparation method

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0031] The preparation of embodiment 1 Edaravone lipid microsphere preparation

[0032] Prescription (1000 bottles): Edaravone 10g

[0033] Soy Lecithin 50g

[0034] Poloxamer 188 20g

[0035] Linoleic acid 8g

[0036] Sodium bisulfite 15g

[0037] Soybean oil for injection 180g

[0038] Water for injection 1500g

[0039] Preparation Process

[0040] (1) 10g of edaravone was dissolved in 30ml of ethanol, and added in 180g of soybean oil to obtain an oil phase;

[0041] (2) Dissolve 50 g of soybean lecithin, 20 g of poloxamer 188, 8 g of linoleic acid, and 15 g of sodium bisulfite in water to obtain an aqueous phase;

[0042] (3) Mix the oil phase and the water phase, transfer to a tissue grinder, rotate at 10,000r / min, stir at high speed for 10 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to obtain the product.

Embodiment 2

[0043] The preparation of embodiment 2 Edaravone lipid microsphere preparation

[0044] Prescription (1000 bottles): Edaravone 15g

[0045] Soy Lecithin 120g

[0046] Poloxamer 188 50g

[0047] Palmitic acid 20g

[0048] Ascorbyl Palmitate 60g

[0049]Soybean oil for injection 400g

[0050] Water for injection 2500g

[0051] Preparation Process

[0052] (1) 15g of edaravone and 60g of ascorbyl palmitate are dissolved in 100ml of ethanol, and added in 400g of soybean oil to obtain an oil phase;

[0053] (2) 120g of soybean lecithin, 50g of poloxamer 188, and 20g of palmitic acid were dissolved in water to obtain an aqueous phase;

[0054] (3) Mix the oil phase and the water phase, transfer to a tissue grinder, rotate at 12000r / min, stir at high speed for 30 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to obtain the product.

Embodiment 3

[0055] The preparation of embodiment 3 Edaravone lipid microsphere preparation

[0056] Prescription (1000 bottles): Edaravone 30g

[0057] Soy Lecithin 100g

[0058] Poloxamer 188 60g

[0059] Oleic acid 35g

[0060] Sodium formaldehyde bisulfite 40g

[0061] Soybean oil for injection 600g

[0062] Water for injection 5000g

[0063] Preparation Process

[0064] (1) 30g of edaravone was dissolved in 100ml of ethanol, and added in 600g of soybean oil to obtain an oil phase;

[0065] (2) 100g of soybean lecithin, 60g of poloxamer 188, 35g of oleic acid, and 40g of sodium formaldehyde bisulfite were dissolved in water to obtain an aqueous phase;

[0066] (3) Mix the oil phase and the water phase, transfer to a tissue grinder, rotate at 8000r / min, stir at high speed for 20 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to obtain the produc...

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Abstract

The invention relates to an edaravone lipid microsphere formulation and a preparation method thereof. The edaravone lipid microsphere formulation is prepared by taking the mixed emulsifier of granulesten and poloxamer188 with specific rate as an emulsifier and injection soybean oil as oil phase solvent, and also contains pharmaceutically regular antioxidant. Not only does the prepared edaravone lipid microsphere injection have simple process, low cost and easy industrial production, but also obviously improved stability compared with the existing edaravone injection.

Description

technical field [0001] The invention relates to a lipid microsphere preparation, in particular to an edaravone lipid microsphere preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Edaravone is a pyrazolone compound synthesized from phenylhydrazine and butanoneamide, which has a powerful free radical scavenging effect and can effectively relieve neurological symptoms and dysfunction caused by brain tissue damage after cerebral infarction. Listed in Japan, clinically by inhibiting the occurrence and progression of ischemic cerebrovascular disorders such as cerebral edema, cerebral infarction, neurological symptoms, and delayed neuronal cell death, it exerts its protective effect on the brain. It is mainly used for the treatment of acute cerebral infarction. It can reduce neurological damage, reduce the disability rate, and promote rehabilitation. It has the characteristics of high curative effect and small ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4152A61K47/44A61K47/34A61K47/24A61P25/00A61P39/06A61K47/10
Inventor 邓菊娟
Owner HAINAN MEILAN SMITH KLINE PHARMA
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