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Argatroban liposome injection

A technology of argatroban fat and argatroban, which is applied in the field of medicine, can solve the problems of pH reduction, poor stability, instability, etc., and achieves the improvement of preparation product quality, good preparation stability, and good bioavailability. Effect

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

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
[0006] At present, argatroban injection has been sold in China, but the clarity of the injection after long-term storage is unqualified, the pH value decreases, the stability is poor, and the content of argatroban decreases.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Argatroban liposome injection

[0039] Prescription (1000 sticks)

[0040]

[0041] Preparation Process:

[0042] (1) Weigh 10g argatroban, 150g sphingomyelin, 150g octadecylamine, and 75g Tween 80 respectively and place them in a pear-shaped bottle, add 1000ml n-butanol, heat and stir to disperse evenly, and put them on a rotary evaporator for 50 Remove n-butanol under reduced pressure at ℃ to obtain a phospholipid film;

[0043] (2) Hydrate the above drug-containing phospholipid film with 1000ml pH of 5.6 phosphate buffer solution, and place it in a tissue masher at 1000rpm to mash, then add pH 5.6 phosphate buffer solution to dilute to 20L, mix well ;

[0044] (3) Filter the above-mentioned liposome solution through a 0.45 μm microporous membrane, pack in ampoules, each 20 ml, and sterilize with flowing steam for 30 minutes to obtain argatroban liposome injection.

Embodiment 2

[0045] Example 2 Argatroban liposome injection

[0046] Prescription (1000 sticks)

[0047]

[0048] Preparation Process:

[0049] (1) Weigh 10g argatroban, 200g sphingomyelin, 50g octadecylamine, and 25g Tween 80 respectively and place them in a pear-shaped bottle, add 1000ml n-butanol, heat and stir to disperse evenly, place on a rotary evaporator for 50 Remove n-butanol under reduced pressure at ℃ to obtain a phospholipid film;

[0050] (2) Hydrate the above drug-containing phospholipid film with 1000ml of pH 5.6 phosphate buffer solution, and place it in a tissue grinder at 10000rpm to mash, then add pH 5.6 phosphate buffer solution to dilute to 20L, and mix well;

[0051] (3) The above-mentioned liposome solution was filtered through a 0.45 μm microporous membrane, dispensed into ampoules, each 20 ml, and sterilized by circulating steam for 30 minutes to obtain argatroban liposome injection.

Embodiment 3

[0052] Example 3 Argatroban liposome injection

[0053] Prescription (1000 sticks)

[0054]

[0055] Preparation Process:

[0056] (1) Weigh 10g argatroban, 200g sphingomyelin, 80g octadecylamine, and 30g Tween 80 respectively and place them in a pear-shaped bottle, add 1000ml n-butanol, heat and stir to disperse evenly, and put them on a rotary evaporator for 50 Remove n-butanol under reduced pressure at ℃ to obtain a phospholipid film;

[0057] (2) Hydrate the above drug-containing phospholipid film with 1000ml of pH 5.6 phosphate buffer solution, and place it in a tissue grinder at 10000rpm to mash, then add pH 5.6 phosphate buffer solution to dilute to 20L, and mix well;

[0058] (3) The above-mentioned liposome solution was filtered through a 0.45 μm microporous membrane, dispensed into ampoules, each 20 ml, and sterilized by circulating steam for 30 minutes to obtain argatroban liposome injection.

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Abstract

The invention discloses an Argatroban liposome injection and a preparation method thereof. The Argatroban liposome injection with excellent quality is prepared by selecting Argatroban, sphingomyelin, octadecylamine, and tween 80 according to specific proportion. Compared with preparations in the prior art, the injection disclosed herein has improved stability and bioavailability, improved qualityof the preparation products, reduced toxic and side effect, stable drug release, and remarkable curative effect.

Description

technical field [0001] The invention relates to a new dosage form of argatroban, in particular to a liposome injection of argatroban and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Argatroban (Argatroban) is an antithrombotic drug developed and synthesized by Mitsubishi Chemical Research Institute in Japan. Its chemical name is (2R, 4R)-4-methyl-1-[N-((R, S)-3- Methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid, molecular formula C 23 h 36 N 6 o 5 S, molecular weight 508.63, structural formula: [0003] [0004] Argatroban is a thrombin inhibitor that reversibly binds to the active site of thrombin, and the antithrombotic effect of argatroban does not require the cofactor antithrombin III. Argatroban exerts its anticoagulant effect by inhibiting thrombin-catalyzed or induced reactions, including fibrin formation, activation of coagulation factors V, VIII, and XIII, activa...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K38/05A61K47/26A61K47/24A61P7/02A61P9/00A61P9/10
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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