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Stable Levosimendan pharmaceutical composition and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve unsolved substantive problems, increase the number of final preparation steps, inconvenient storage and transportation, etc., and achieve the effects of not easy to degrade, reduce toxic and side effects, and convenient transportation

Active Publication Date: 2010-12-22
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent document CN1373665 (application number 00812645.3) discloses an injection containing polyvinylpyrrolidone and absolute ethanol. At present, levosimendan is also such an injection clinically, but this injection requires cryogenic refrigeration (2-8°C) And keep away from light, which brings inconvenience to storage and transportation
Although Chinese patent document CN1839842 (application number 200610000963.7) has Solutor HS 15, which belongs to the polyethylene glycol solubilizer, has no substantial difference from the above patent and does not solve the substantive problem
[0006] Chinese patent documents CN1611219 (application number 200310102271.X), CN1611220 (application number 200310102272.4) and CN1626085 (application number 200310118504.5) all disclose the freeze-dried formulations of levosimendan of different auxiliary materials, although the problem of transportation and storage has been solved, but The regimens disclosed in these three patent documents all incorporate povidone or other surfactants, all of which are clinically proven to be hemolytic, posing treatment risks to patients
The schemes disclosed in these two patent documents have more steps to prepare the final preparation and take a long time

Method used

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  • Stable Levosimendan pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Accurately weigh 12.5g of levosimendan sterile powder (calculated as 1000 tubes), pack into 7ml vials, each 12.5mg; weigh 250g of hydroxypropyl beta cyclodextrin, add to 4500ml under stirring In absolute ethanol, continue to stir until the solution is clear, and set the volume to 5000ml; add 0.05% activated carbon for adsorption for 15min, decarbonize and filter, sterilize and filter with a 0.22um microporous membrane, and then pack into vials, 5ml each. The vials of the above-mentioned sterile powder and solvent for injection are covered with rubber stoppers, pressed with aluminum caps, and packaged to obtain the product.

Embodiment 2

[0044] Accurately weigh 6.25g of levosimendan sterile powder (calculated according to 1000 tubes), and pack it into 7ml vials, 6.25mg per tube; weigh 150g of hydroxypropyl beta cyclodextrin, add it to 2000ml under stirring In absolute ethanol, continue to stir until the solution is clear, and set the volume to 2500ml; add 0.05% activated carbon to absorb for 15min, decarbonize and filter, sterilize and filter with a 0.22um microporous membrane filter, and then pack into vials, 2.5ml each . The vials of the above-mentioned sterile powder and solvent for injection are covered with rubber stoppers, pressed with aluminum caps, and packaged to obtain the product.

Embodiment 3

[0046] Accurately weigh 25g of levosimendan sterile powder (calculated according to 1000 pieces), pack into 15ml vials, each 25g; weigh 650g of hydroxypropyl beta-cyclodextrin, add it to 11000ml anhydrous In ethanol, continue to stir until the solution is clear, and set the volume to 12000ml; add 0.05% activated carbon to absorb for 15min, decarbonize and filter, sterilize and filter with a 0.22um microporous membrane, and then pack into vials, each 12ml. The vials of the above-mentioned sterile powder and solvent for injection are covered with rubber stoppers, pressed with aluminum caps, and packaged to obtain the product.

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PUM

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Abstract

The invention relates to a stable levosimendan medicine composition. The medicine composition consists of two chambers, wherein a medicine chamber is filled with the levosimendan or a pharmaceutically acceptable salt thereof; and a solvent chamber is filled with a pharmaceutically usable solvent. The solvent contains a pharmaceutically acceptable organic solvent and solubilizing agent, and also can be added with a pharmaceutically acceptable acid. The composition can be used for intravenous injection, or taken orally. The invention also relates to a method for preparing the composition.

Description

technical field [0001] The invention relates to a stable levosimendan pharmaceutical composition and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Levosimendan, the chemical name is (-)-[[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]hydrazono ] malononitrile, the structural formula is as follows: [0003] [0004] Levosimendan is a calcium sensitizer anti-acute heart failure drug researched and developed by Orion Company of Finland. It is widely used clinically. [0005] Levosimendan is poorly soluble in water and easily degradable, with a Pka of 6.26 and a solubility in water of pH6 and pH2 of 0.03mg / ml and 0.02mg / ml, respectively. Chinese patent document CN1373665 (application number 00812645.3) discloses an injection containing polyvinylpyrrolidone and absolute ethanol. At present, levosimendan is also such an injection clinically, but this injection requires cryogenic refrigeration (2-8°C) An...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/50A61K9/00A61P9/04
Inventor 赵娥杨清敏张明会王晶翼
Owner QILU PHARMA CO LTD
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