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Argatroban drug composition and preparation method and application of argatroban drug composition

A technology of argatroban and its composition, which is applied in the field of argatroban pharmaceutical composition and its preparation, can solve the problems of large pH fluctuations before and after sterilization of injections, weak buffering capacity of argatroban, and increased clinical use Risk and other issues, to achieve the effect of increasing clinical safety, short preparation time, and suitable for clinical use

Inactive Publication Date: 2012-11-21
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] CN102119922A and CN102228677A all proposed the intravenous injection of argatroban using acid as a solubilizing agent, and using inorganic acid or organic acid to dissolve the main drug, but argatroban itself has weak buffering capacity, and it also uses acid as a solubilizing agent. It is necessary to use buffer salts to maintain a stable pH value, resulting in complicated ingredients of preparation excipients and increasing the risk of clinical medication
[0017] Most of the above disclosed documents use alcohol or acid as a solubilizing agent, which cannot completely dissolve the main drug, and at the same time, stabilizers are added to varying degrees, and buffer salts are used to stabilize the pH. Due to the interaction of raw and auxiliary materials during high-temperature sterilization, The obtained injection has the defect that the pH fluctuates greatly before and after sterilization
At the same time, the addition of various excipients makes the composition of the final preparation complex, and complex reactions are prone to occur to degrade the main drug or produce impurities, which greatly increases the risk of clinical use

Method used

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  • Argatroban drug composition and preparation method and application of argatroban drug composition
  • Argatroban drug composition and preparation method and application of argatroban drug composition
  • Argatroban drug composition and preparation method and application of argatroban drug composition

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] prescription:

[0067]

[0068] Weigh 30 g of absolute ethanol and 50 g of propylene glycol, stir evenly to form a stable solvent system, add 1 g of the main drug argatroban in the prescribed amount, stir to fully dissolve the main drug, and the solution becomes clear, add water for injection to dilute to 200 ml, Mix evenly to obtain a preparation solution. After the intermediate is qualified, the solution is filtered, filled into packaging containers, and terminally sterilized by moist heat to obtain the final pharmaceutical composition.

[0069] The content of the finished product is 100.3% by HPLC, the total impurities are 0.056%, the maximum simple impurities are 0.014%, the pH value before sterilization is 6.68, and the pH value after sterilization is 6.57. The content and related substances are detected by HPLC.

Embodiment 2

[0071] prescription:

[0072]

[0073] Weigh 20 g of absolute ethanol and 40 g of propylene glycol, stir evenly to form a stable solvent system, add 1 g of the main drug argatroban in the prescribed amount, stir to fully dissolve the main drug, and the solution becomes clear, add water for injection to dilute to 200 ml, Mix evenly to obtain a preparation solution. After the intermediate is qualified, the solution is filtered, filled into packaging containers, and terminally sterilized by moist heat to obtain the final pharmaceutical composition.

[0074] The content of the finished product is 101.3% by HPLC, the total impurity is 0.068%, the maximum simple impurity is 0.014%, the pH value before sterilization is 6.73, and the pH value after sterilization is 6.61.

Embodiment 3

[0076] prescription:

[0077]

[0078] Weigh 50 g of absolute ethanol and 40 g of propylene glycol, stir evenly to form a stable solvent system, add 1 g of the main drug argatroban in the prescribed amount, stir to fully dissolve the main drug, and the solution becomes clear, add water for injection to dilute to 200 ml, Mix evenly to obtain a preparation solution. After the intermediate is qualified, the solution is filtered, filled into packaging containers, and terminally sterilized by moist heat to obtain the final pharmaceutical composition.

[0079] The content of the finished product is 100.8% by HPLC, the total impurity is 0.047%, the maximum simple impurity is 0.021%, the pH value before sterilization is 6.93, and the pH value after sterilization is 6.75.

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Abstract

The invention provides an argatroban drug composition. Argatroban is used as a main drug, and auxiliary solution consisting of anhydrous ethanol, propylene glycol and water is used as dissolving liquid, so that the argatroban drug composition is prepared. The weight ratio of the argatroban, the anhydrous ethanol and the propylene glycol is 1:(20-50):(40-80). The pH (potential of hydrogen) values of the obtained composition before and after sterilization are stable and tend to be neutral, the content of related substances and clinical irritation are low, and the argatroban drug composition is safe in use.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to the field of preparation of argatroban, more specifically to the pharmaceutical composition of argatroban and a preparation method thereof. Background technique [0002] Argatroban, English name Argatroban, is a chemically synthesized drug derived from arginine, molecular weight: chemical common name: (2R, 4R)-4-methyl-1-[N2-((R, S)-3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid hydrate, molecular formula: C 23 h 36 N 6 o 5 S·H 2 The molecular weight of O is 526.65, and the specific structural formula is as follows: [0003] [0004] Argatroban is a white, odorless crystalline powder, easily soluble in glacial acetic acid, slightly soluble in ethanol, insoluble in acetone and ethyl acetate, and will gradually decompose when exposed to light. This product is a new type of thrombin inhibitor, which reversibly binds to the active site of thro...

Claims

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Application Information

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IPC IPC(8): A61K38/05A61K47/10A61K9/08A61K9/14A61P7/02
Inventor 陈庆财李晓昕贾元超陈祥峰
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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