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Argatroban injection and preparation method thereof

A technology of argatroban and injection, which is applied in the field of pharmaceutical preparations, can solve the problems of increased medication risk, production difficulty, difficult product quality control, high production cost, etc., and achieves convenience for large-scale production operations, high stability of liquid medicine, and The effect of reducing loss in the production process

Active Publication Date: 2013-12-25
ZHEJIANG TIANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Both of these two prescriptions increase the solubility of argatroban by adding organic solvents, but the introduction of organic solvents also increases the risk of medication and the difficulty of production, high production costs, and difficult to control product quality

Method used

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  • Argatroban injection and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A kind of argatroban injection, containing argatroban 0.475g, sorbitol 50g in every 1000ml argatroban injection, balance is water for injection, and the pH value of described argatroban injection is 5.0.

[0023] Taking the preparation of the above-mentioned argatroban injection of 1000ml as an example, the preparation method comprises the following steps:

[0024] (1) Weigh 50g of sorbitol, add 800ml of water for injection, stir to dissolve, then add 0.10% activated carbon for needles according to the mass volume ratio, stir and absorb for 20min, decarbonize and filter to obtain the filtrate;

[0025] (2) Heat the filtrate to 80°C, keep it warm for 10 minutes, add 0.475g of argatroban, stir to dissolve, add water for injection to nearly full amount, adjust the pH value to 5.0, take samples for intermediate detection, and add water for injection according to the test results Or raw materials to the required amount, the content is controlled at about 98.0% based on the c...

Embodiment 2

[0028] A kind of argatroban injection, containing argatroban 0.525g, sorbitol 60g in every 1000ml argatroban injection, balance is water for injection, and the pH value of described argatroban injection is 6.0.

[0029] Taking the preparation of the above-mentioned argatroban injection of 1000ml as an example, the preparation method comprises the following steps:

[0030] (1) Weigh 60g of sorbitol, add 800ml of water for injection, stir to dissolve, then add 0.10% activated carbon for needles according to the mass volume ratio, stir and absorb for 30min, decarbonize and filter to obtain the filtrate;

[0031] (2) Heat the filtrate to 90°C, keep it warm for 10 minutes, add 0.525g of argatroban, stir to dissolve, add water for injection to nearly full amount, adjust the pH value to 6.0, take samples for intermediate detection, and add water for injection according to the test results Or raw materials to the required amount, the content is controlled at about 102.0% based on the ...

Embodiment 3

[0034] A kind of argatroban injection, containing argatroban 0.5g, sorbitol 54g in every 1000ml argatroban injection, surplus is water for injection, and the pH value of described argatroban injection is 6.0.

[0035] Taking the preparation of the above-mentioned argatroban injection of 1000ml as an example, the preparation method comprises the following steps:

[0036] (1) Weigh 54g of sorbitol, add 800ml of water for injection, stir to dissolve, then add 0.10% activated carbon for needles according to the mass volume ratio, stir and absorb for 25min, decarbonize and filter to obtain the filtrate;

[0037] (2) Heat the filtrate to not lower than 85°C, keep it warm for 10 minutes, add 0.5g of argatroban, stir to dissolve, add water for injection to nearly full amount, adjust the pH value to 6.0, take samples for intermediate detection, and make up Add water for injection or raw materials to the required amount, and the content is controlled at about 100.0% based on the content...

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Abstract

The invention relates to an argatroban injection and a preparation method thereof, which belong to the technical field of pharmaceutical preparations. Each 1000 ml of argatroban injection contains 0.475-0.525 g of argatroban, 50-60 g of sorbitol and the balance of injection water, and the pH value of the argatroban injection is 5.0-6.0. The argatroban injection provided by the invention has simple components, thereby effectively reducing the risk of heat source increase caused by addition of exogenous components, a heat source can be completely adsorbed by needle active carbon after adding the argatroban, the liquid medicine stability of the injection provided by the invention is high, as shown in an acceleration test result of a pilot test sample, the external properties, pH value, visible foreign matters, related substance and content of the argatroban injection prepared by the preparation method provided by the invention meet the existing provisions under an acceleration condition, and no obvious change occurs in the argatroban content with the growth of time, so that the stability of the injection is good.

Description

technical field [0001] The invention relates to an argatroban injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Argatroban (Argatroban), the chemical name is (2R, 4R)-4-methyl-1-{(2S)-2-[(3RS)-3-methyl-1, 2, 3, 4-tetra Hydrogen-8-quinolinesulfonylamino]-5-guanidinopentanoyl}piperidine-2-carboxylic acid monohydrate with a molecular weight of 526.65. Argatroban is a highly active and highly selective thrombin inhibitor. Its anticoagulant effect does not depend on antithrombin in the body, but directly binds to free thrombin in the blood and inactivates it; In addition, due to the small molecular weight of argatroban, it can directly enter the thrombus, inactivate the thrombin that has been bound to fibrin, and indirectly inhibit the generation of thrombin. platelet aggregation reaction. Because argatroban can greatly reduce the level of thrombin-antithrombin complex in plasma and effect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K9/08A61K47/10A61P7/02
Inventor 崔友李伟陈志勇王恒彩
Owner ZHEJIANG TIANRUI PHARMA
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