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Ozagrel sodium liposome injection

A technology of ozagrel sodium lipid and gray sodium lipid, applied in the field of medicine, can solve problems such as poor stability, and achieve the effect of improving stability, low cost, and avoiding freeze-drying process

Inactive Publication Date: 2011-02-02
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the problem that the current sodium ozagrel solution is prone to crystallization and has poor stability when placed for a long time, the object of the present invention is to provide a liposome injection of sodium ozagrel, which obtains high-quality raw materials by combining ozagrel and sodium hydroxide Ozagrel sodium, and provide better quality Ozagrel sodium liposome injection by pH gradient method, thus solving the above-mentioned problems

Method used

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  • Ozagrel sodium liposome injection
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  • Ozagrel sodium liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Preparation of Ozagrel Sodium Liposomes

[0057] Prescription (1000 bottles): Ozagrel 20g

[0058] Sodium hydroxide 3.5g

[0059] Egg Yolk Lecithin 140g

[0060] Cholesterol 72g

[0061] Sodium deoxycholate 40g

[0062] Preparation Process

[0063] (1) Dissolve 140g of egg yolk lecithin, 72g of cholesterol and 40g of sodium deoxycholate in 1500ml of ethanol, slowly inject 1500ml of 0.02mol / L ammonium sulfate solution under stirring, heat and stir to evaporate ethanol, put it in an ice bath and sonicate for 10min to obtain blank liposome;

[0064] (2) Blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in the solution 1000ml of 0.9% sodium chloride and dialyzes 18 hours, removes the ammonium sulfate in the liposome external phase;

[0065] (3) Mix and dissolve 20g of ozagrel and 3.5g of sodium hydroxide in 300ml of water, heat the dialyzed blank liposome at 60°C, sl...

Embodiment 2

[0072] Example 2 Preparation of Ozagrel Sodium Liposomes

[0073] Prescription (1000 bottles): Ozagrel 40g

[0074] Sodium hydroxide 7g

[0075] Soy Lecithin 160g

[0076] Cholesterol 70g

[0077] Sodium deoxycholate 40g

[0078] Preparation Process

[0079] (1) Dissolve 160g of soybean lecithin, 70g of cholesterol and 40g of sodium deoxycholate in 2500ml of isopropanol, slowly inject 2500ml of 0.2mol / L ammonium sulfate solution under stirring, heat and stir to evaporate the isopropanol, and put it in an ice bath Ultrasound for 20 minutes to obtain blank liposomes;

[0080] (2) Blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in the solution 3000ml of 5% glucose and dialyzed for 22 hours, removes the ammonium sulfate in the liposome external phase;

[0081] (3) Mix and dissolve 40g ozagrel and 7g sodium hydroxide in 1000ml water, keep the dialyzed blank liposome at 60°C, slowly...

Embodiment 3

[0089] Example 3 Preparation of Ozagrel Sodium Liposomes

[0090] Prescription (1000 bottles): Ozagrel 80g

[0091] Sodium hydroxide 14g

[0092] Soy Phosphatidylserine 560g

[0093] Cholesterol 288g

[0094] Sodium deoxycholate 160g

[0095] Preparation Process

[0096] (1) Dissolve 560g of soybean phosphatidylserine, 288g of cholesterol and 160g of sodium deoxycholate in 6000ml of ethanol, slowly inject 6000ml of 0.08mol / L ammonium sulfate solution under stirring, heat and stir to remove chloroform, put it in an ice bath and sonicate for 10min, Obtain blank liposome;

[0097] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in the solution 4000ml of 800g sorbitol and dialyzes 24 hours, removes the ammonium sulfate in liposome external phase;

[0098] (3) Mix and dissolve 80g ozagrel and 14g sodium hydroxide in 2000ml water, keep the dialyzed blank liposome at 60°C, slowly add the...

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Abstract

The invention discloses an ozagrel sodium liposome injection which comprises ozagrel, sodium hydroxide, phospholipid, cholesterol, sodium deoxycholate and any pharmaceutically acceptable carrier. The invention also discloses a preferable ozagrel sodium liposome preparation which comprises the following components in parts by weight: 1 part of ozagrel, 0.175 part of sodium hydroxide, 3-20 parts ofphospholipid, 0.5-15 parts of cholesterol and 0.2-13 parts of sodium deoxycholate. The invention also discloses a method for preparing the ozagrel sodium liposome preparation, preferably an ammonium sulfate pH gradient method. The ozagrel sodium liposome preparation with high stability has high entrapment rate, low leaking rate in the process of long-term storage and devitrification-free ozagrel sodium, is suitable for industrialized production and prevents a freezing and drying process generally needed by liposome.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to an ozagrel sodium liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Ozagrel (English name: ozagrel), its chemical name is: trans-3-[4-(1H-imidazolyl-1-methyl)phenyl]-2-acrylic acid, molecular formula: C 13 h 12 N 2 o 2 , molecular weight: 228.25, structural formula: [0003] [0004] It is a highly effective and selective inhibitor of thromboxane synthase, which inhibits the synthesis of thromboxane A2 (TXA2) and promotes the production of prostacyclin (PGI2), thereby anti-platelet aggregation, reducing blood viscosity, and promoting thrombus decomposition and expansion Vascular effects etc. Therefore, it is especially suitable for inhibiting cerebral vasospasm, increasing cerebral blood flow, improving microcirculation disorders and abnormal energy metabolism in the brain, and improving cerebral ische...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4174A61P9/10A61P7/02A61K9/10A61K9/127
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST