Argatroban composition and preparation method thereof

A technology of argatroban and its composition, applied in the field of chemical pharmacy, can solve the problems of slow cooling, large volume of liquid medicine, and inconvenient adjustment of pH value, etc., and achieve the effect of reducing cycle time, shortening working hours, and reducing steam consumption

Active Publication Date: 2016-08-03
北京先通源医药科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If it is allowed to cool down naturally, the volume of the medicinal liquid will be large and the temperature

Method used

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  • Argatroban composition and preparation method thereof
  • Argatroban composition and preparation method thereof
  • Argatroban composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086]

[0087] 【Preparation】

[0088] A. Add sorbitol to 80% of the total amount of water for injection, stir to dissolve, add 0.1% (w / v) activated carbon for needles, stir for 10 minutes, filter to obtain solution A, and the pore size of the filter material is 0.8 μm.

[0089] B. Add an appropriate amount of ethanol to solution A to make a solution containing 75% (w / w) ethanol, add argatroban and stir to dissolve, add the remaining solution A, add water for injection to 95% of the total amount, Use 0.1mol / L hydrochloric acid solution or 0.1mol / L sodium hydroxide solution to adjust the pH value to 4.5-6.5, add water for injection to the total amount, stir and mix.

[0090] C. Take samples according to the law, measure the pH value and content of the medicinal liquid, and filter the medicinal liquid after the result is qualified. The filter material has a pore size of 0.22 μm, fills it with nitrogen gas and seals it. The inner packaging material is a 20ml brown ampoule, and...

Embodiment 2

[0092]

[0093] 【Preparation】

[0094] A. Add sorbitol to 70% of the total amount of water for injection, stir to dissolve, add 0.1% (w / v) activated carbon for needles, stir for 15 minutes, filter to obtain solution A, and the pore size of the filter material is 0.45 μm.

[0095] B. Add an appropriate amount of ethanol to solution A to make a solution containing 50% (w / w) ethanol, add argatroban and stir to dissolve, add the remaining solution A, add water for injection to 95% of the total, Use 0.1mol / L lactic acid solution or 0.1mol / L sodium hydroxide solution to adjust the pH value to 4.5-6.5, add water for injection to the total amount, and stir to mix.

[0096] C. Take samples according to the law, measure the pH value and content of the medicinal liquid, and filter the medicinal liquid after the result is qualified. The filter material has a pore size of 0.22 μm, fills it with nitrogen gas and seals it. The inner packaging material is a 20ml brown ampoule, and steriliz...

Embodiment 3

[0098]

[0099] 【Preparation】

[0100] A. Add sorbitol to 60% total amount of water for injection, stir to dissolve, add 0.1% (w / v) activated carbon for needles, stir for 20 minutes, filter to obtain solution A, and the filter material pore size is 0.22 μm.

[0101] B. Add an appropriate amount of ethanol to solution A to make a solution containing 50% (w / w) ethanol, add argatroban and stir to dissolve, add the remaining solution A, add water for injection to 95% of the total, Use 0.1mol / L hydrochloric acid solution or 0.1mol / L sodium hydroxide solution to adjust the pH value to 4.5-6.5, add water for injection to the total amount, stir and mix.

[0102] C. Take samples according to the law, measure the pH value and content of the medicinal liquid, and filter the medicinal liquid after the result is qualified. The filter material has a pore size of 0.22 μm, fills it with nitrogen gas and seals it. The inner packaging material is a 20ml brown ampoule, and sterilized by autoc...

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Abstract

The invention belongs to the field of pharmaceutical chemistry, and particularly relates to an argatroban composition and a preparation method thereof. The argatroban composition provided by the invention comprises 0.5 mg/ml-1.0 mg/ml of argatroban, 2.4%-10% (w/v) of sorbitol, 0.75%-1.25% (w/v) of ethanol, a pH adjusting agent and the balance of water for injection, wherein the argatroban composition has a pH value of 4.5-6.5. The composition is precipitate-free; an acceleration test (38 DEG C to 42 DEG C; RH 70% to 80%) proves that the composition is stable.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy in the field of medicine, and in particular relates to an argatroban composition and a preparation method thereof. Background technique [0002] Argatroban, English name Argatroban, chemical name: (2R,4R)-4-methyl-1-{(2S)-2-[(3RS)-3-methyl-1,2,3,4- Tetrahydro-8-quinolinesulfonylamino]-5-guanidinopentanoyl}piperidine-2-carboxylic acid monohydrate. [0003] Chemical Structure: [0004] [0005] Molecular formula: C 23 h 36 N 6 o 5 S·H 2 o [0006] Molecular weight: 526.65 [0007] Argatroban is white or off-white crystalline powder, odorless and hygroscopic. Argatroban is easily soluble in glacial acetic acid, slightly soluble in methanol, slightly soluble in ethanol, and very slightly soluble in water. [0008] Argatroban is a small molecular compound derived from L-arginine. Its structural formula includes a tripod structure of arginine, piperidine, and quinoline. It can bind three-di...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/10A61K38/05A61P7/02
CPCA61K9/0019A61K9/08A61K38/05A61K47/10
Inventor 齐慧
Owner 北京先通源医药科技股份有限公司
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