Argatroban injection liposome and preparation method thereof

A lipid and plastid technology of argatroban, which is applied in the field of argatroban injection liposome and its preparation, can solve problems such as not being suitable for large-scale production, affecting the clinical application of drugs, and complicated preparation methods, and achieving The effect of reducing toxicity, improving encapsulation efficiency, and simple preparation method

Inactive Publication Date: 2021-12-31
陇南市第一人民医院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the argabantri injection prepared by the above method is unstable in the long-term placement process, which affects the clinical application of the drug
[0008] Patent CN102366410 (published on March 07, 2012) discloses a liposome injection of argatroban, the liposome is composed of sphingomyelin, eighteen Amine, Tween 80, the preparation method of this scheme is relatively complicated, not suitable for large-scale production

Method used

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  • Argatroban injection liposome and preparation method thereof
  • Argatroban injection liposome and preparation method thereof
  • Argatroban injection liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: the preparation of argatroban liposome injection, specifically according to the following prescription by weight

[0034]

[0035] Argatroban liposome injection was prepared by the following preparation process:

[0036] 1) Dissolve the prescribed amount of cultured phosphatidylethanolamine, phosphatidylglycerol, cholesterol and Tween 80 in 120ml of sodium chloride solution, stir and sonicate for 15 minutes to obtain blank liposomes;

[0037] 2) steam-sterilize the blank lipid obtained in step 1) and sonicate for 15 minutes;

[0038] 3) Mix and dissolve the prescribed amount of argatroban and sodium hydroxide in 300ml of water for injection, heat the sterilized blank liposomes to 56°C and keep warm, slowly add the aqueous solution of argatroban under stirring, continue Incubate at 56° C. for 10-15 minutes, add 120 ml of a citrate buffer solution with a pH of 6.5, and mix well to obtain argatroban liposome injection.

Embodiment 2

[0039] Embodiment 2: the preparation of argatroban liposome injection, specifically according to the following prescription by weight

[0040]

[0041] Argatroban liposome injection was prepared by the following preparation process:

[0042] 1) Dissolve the prescribed amount of dicetyl phospholipid, phosphatidylglycerol, cholesterol and Tween 80 in 150ml of ethanol solution, heat and stir, spin evaporate to remove ethanol, and ultrasonicate the remaining components for 15 minutes to obtain blank liposomes;

[0043] 2) steam-sterilize the blank lipid obtained in step 1) and sonicate for 15 minutes;

[0044] 3) Mix and dissolve the prescribed amount of argatroban and sodium hydroxide in 300ml of water for injection, heat the sterilized blank liposomes to 56°C and keep warm, slowly add the aqueous solution of argatroban under stirring, continue Incubate at 56° C. for 10-15 minutes, stir and mix to obtain argatroban liposome injection.

Embodiment 3

[0045] Embodiment 3: the preparation of argatroban liposome injection, specifically according to the following prescription by weight

[0046]

[0047]Injection composition and component content are according to above-mentioned (embodiment 3) prescription, osmotic pressure regulator selects mannitol for use, buffer solution selects the acetate buffer solution that pH is 7.5 for use, all the other specific preparation methods are the same as embodiment 1

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Abstract

The invention discloses an argatroban liposome injection which is mainly prepared from the following components in parts by weight: 1 part of argatroban, 0.1-0.3 part of sodium hydroxide, 10-25 parts of phospholipid, 5-8 parts of phosphatidyl glycerol, 5-10 parts of cholesterol and 5-10 parts of Tween 80, wherein the phospholipid is one of soybean lecithin, phosphatidylethanolamine, dicetyl phospholipid and soybean phosphatidylserine, the solubility of argatroban in a solution is remarkably enhanced, and meanwhile, the use of an organic solution is reduced by virtue of the use of specific lipidosome, so that the toxicity of the injection is improved, and the problem of renal toxicity of the traditional argatroban injection is solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an argatroban injection liposome and a preparation method thereof. Background technique [0002] Cerebral infarction, also known as cerebral infarction, also known as cerebral ischemic stroke, refers to the localized ischemic necrosis or softening of brain tissue caused by cerebral blood supply disorder, ischemia and hypoxia. The common clinical types of cerebral infarction include cerebral thrombosis, lacunar infarction, and cerebral embolism. Cerebral infarction accounts for 80% of all strokes. It is one of the three major diseases threatening human health. According to the "China Stroke Prevention Report", stroke is the number one cause of death in China, and its prevalence is on the rise. With the aging of the population and the increase of various risk factors, the proportion of ischemic stroke will increase. Recurrence rates are higher due to disabili...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K38/05A61P9/10
CPCA61K38/05A61K9/0019A61K9/1277A61P9/10
Inventor 吴江赵伟李元森
Owner 陇南市第一人民医院
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