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 not being suitable for large-scale production in workshops and complicated preparation methods, and achieve the effects of increased drug use risk, good stability, and low drug risk

Active Publication Date: 2013-05-01
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the pharmaceutical compositions described in these two inventions do not contain organic solvents such as ethanol and glycerin, amino ac

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation of embodiment 1 argatroban injection

[0028] Weigh 80g of D-sorbitol, add 5000mL of water for injection, stir to dissolve, add 0.1% activated carbon for needles (5.0g) according to the mass volume ratio, stir for 15 minutes, filter the liquid through a 1um titanium rod to decarbonize.

[0029] Add 1 part of argatroban to the above filtrate, stir to suspend the argatroban in the liquid medicine, heat the liquid medicine to 60°C, and stir until the argatroban is completely dissolved. Add water for injection to the above medicinal solution to 10000 parts, circulate and filter to mix evenly, and adjust the pH of the medicinal solution to 4.2 with 0.1mol / L hydrochloric acid solution. The medicinal solution is sterilized and filtered through a 0.22um microporous membrane, filled in brown glass ampoules, and filled with nitrogen gas before filling. Melt seal, check for leaks, and steam sterilize at 121°C for 20 minutes.

Embodiment 2

[0030] The preparation of embodiment 2 argatroban injection

[0031] Weigh 100g of D-sorbitol, add 1000mL of water for injection, stir to dissolve, add 0.1% activated carbon for needles (1.0g) according to the mass volume ratio, stir for 15 minutes, filter the liquid through a 1um titanium rod for decarbonization.

[0032] Add 1 part of argatroban to the above filtrate, stir to suspend the argatroban in the liquid medicine, heat the liquid medicine to 80°C, and stir until the argatroban is completely dissolved. Add water for injection to the above medicinal solution to 2000 parts, circulate and filter to mix evenly, and adjust the pH of the medicinal solution to 5.5 with 1mol / L sodium bicarbonate solution. The medicinal solution is sterilized and filtered through a 0.22um microporous membrane, filled in brown glass ampoules, and filled with nitrogen gas before filling. Melt seal, check for leaks, and steam sterilize at 121°C for 20 minutes.

Embodiment 3

[0033] The preparation of embodiment 3 argatroban injection

[0034] Weigh 150g of D-sorbitol, add 500mL of water for injection, stir to dissolve, add 0.1% activated carbon for needles (0.5g) according to the mass volume ratio, stir for 15 minutes, filter the liquid through a 1um titanium rod for decarbonization.

[0035] Add 1 part of argatroban to the above filtrate, stir to suspend the argatroban in the liquid medicine, heat the liquid medicine to 80°C, and stir until the argatroban is completely dissolved. Add water for injection to the above medicinal solution to 1000 parts, circulate and filter to mix evenly, and adjust the pH of the medicinal solution to 6.0 with 1mol / L sodium carbonate solution. The medicinal solution is sterilized and filtered through a 0.22um microporous membrane, filled in brown glass ampoules, and filled with nitrogen gas before filling. Melt seal, check for leaks, and steam sterilize at 121°C for 20 minutes.

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Abstract

The invention relates to an argatroban injection and a preparation method thereof. The injection is composed of 1 part of argatroban, 80-150 parts of a solubilizer, a proper amount of a pH regulation agent, and injection water. The addition amount of the pH regulation agent satisfies that the pH value of a full amount of the solution is regulated to 4.2-7.0. During medicine solution preparation, the medicine solution with argatroban added is not subjected to an active carbon absorption treatment. The argatroban injection provided by the invention has the advantages of no organic solvent, simple components, stable quality, and convenient application.

Description

technical field [0001] The invention relates to an argatroban injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Argatroban (Argatroban), chemical name (2R,4R)-4-methyl-1-[N-(R,S)-3-methyl-1,2,3,4-tetrahydro-8 -Quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid, the molecular weight is 508.63. [0003] 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. Since argatroban can greatly reduce the level of thrombin-antithrombin complex in plasma and effectively improve the hypercoagulable state of patients, ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K38/02A61K47/10A61P7/02
Inventor 赵志全赵震震石其德
Owner SHANDONG NEWTIME PHARMA
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