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Levosimendan emulsion for intravenous injection and preparation thereof

A technology of oil for injection and water for injection, which is applied in the field of medicine, can solve the problems of levosimendan difficulty, obstruction of blood circulation, patient irritation and side effects, and achieve the effects of reducing irritation, improving compliance and increasing safety.

Inactive Publication Date: 2008-12-17
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Levosimendan is poorly soluble in water, and it is easy to precipitate in aqueous solution, and it is easy to chemically degrade in solution. Precipitation in intravenous solution is very dangerous, because the precipitated particulate matter can easily hinder the circulation of blood
[0007] The patent ZL00812645.3 of Finland Orion Company provides a kind of pharmaceutical aqueous solution containing levosimendan or its pharmaceutically acceptable salt as an active ingredient and a solubilizer, but the solubilizer used in it is polyvinylpyrrolidone or other surface Active agents have clinically proven coagulation side effects, presenting treatment risks to patients
[0008] Also have the solution that adopts organic solvents such as ethanol in the prior art in addition, but use organic solvent to be easy to produce irritation and side effect to patient, especially just be difficult to use to the patient of alcohol allergy, and use a large amount of volatile organic solvents also make the preparation process more difficult

Method used

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  • Levosimendan emulsion for intravenous injection and preparation thereof
  • Levosimendan emulsion for intravenous injection and preparation thereof
  • Levosimendan emulsion for intravenous injection and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Under the protection of nitrogen, weigh 0.25g of levosimendan, 5g of lecithin, 15g of soybean oil, and 0.5g of oleic acid, heat and mix evenly to obtain an oil phase; take 2g of glycerin, 10g of sucrose and add 80ml of water for injection to dissolve, add the water phase to In the oil phase, stir at high speed, then add water for injection to 100ml, adjust the pH to 3-4.5, and continue stirring to prepare colostrum. Repeated homogenization by a high-pressure homogenizer, and checking the size of the obtained emulsion particles, the average particle size is 104.8nm. The emulsion is sterile filtered, filled, sealed, and ready after passing the inspection.

Embodiment 2

[0049] Under nitrogen protection, weigh 0.5g of levosimendan, 20g of medium-chain triglyceride, 5g of polyoxyethylene castor oil, and 0.5g of oleic acid, and mix them uniformly to obtain an oil phase; weigh PEG4005g, glucose 8g, EDTA-2Na0. 0.05 g was dissolved in 80 ml of water for injection, the water phase was added to the oil phase, stirred at high speed, then water for injection was added to 100 ml, the pH was adjusted to 3-4.5, and the colostrum was prepared by continuing to stir. Repeated homogenization by a high-pressure homogenizer, and checking the size of the obtained emulsion particles, the average particle size is 191.2nm. The emulsion is sterile filtered, filled, sealed, and ready after passing the inspection.

Embodiment 3

[0051] Under the protection of nitrogen, weigh 25g of cottonseed oil for injection and heat it to 60°C. Under high-speed stirring, add 5g of soybean lecithin, 0.5g of Tween-800.5g, and 0.7g of levosimendan, and stir evenly as the oil phase; Add 80ml of water for injection to 15g to dissolve, add the water phase to the oil phase, stir at high speed, then add water for injection to 100ml, adjust the pH to 3-4.5, and continue to stir to prepare colostrum. Repeated homogenization by a high-pressure homogenizer, and checking the size of the obtained emulsion particles, the average particle size is 204.3nm. The emulsion is sterile filtered, filled, sealed, and ready after passing the inspection.

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Abstract

The invention relates to a levosimendan emulsion or a levosimendan salt emulsion for intravenous injection and a preparation method thereof. The invention is a stable levosimendan oil-in-water emulsion which comprises the active components such as levosimendan or levosimenda salt, oil for injection, emulsifier and water for injection. The emulsion alleviates the irritation to blood vessels while ethanol is taken as solvent, reduces the adverse reaction, improves stability of the emulsion, ensures the safety in the clinical application of the emulsion, and enhances the compliance of patients with the emulsion.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a levosimendan emulsion for intravenous injection and a preparation method thereof. Background technique [0002] Levosimendan, chemical name (R)-(-)-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazine)phenyl]hydrazine Base] malononitrile, clinically used for the treatment of congestive heart failure. [0003] The structural formula of levosimendan is as follows: [0004] [0005] Levosimendan was researched and developed by Orion Company of Finland, and was first listed in Sweden in 2000. Levosimendan is available in the form of freeze-dried powder injection and water injection, with two specifications of 12.5mg / 5ml and 25mg / 10ml. As a positive inotropic drug, levosimendan enhances myocardial contractility by increasing the sensitivity of cardiomyocytes to calcium ions without increasing the concentration of cardiomyocytes. WO93 / 21921 describes the use of this compound in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/50A61K9/107A61K47/44A61P9/04A61K47/14
Inventor 李青坡阮建山杜斯文何佳奇
Owner HANGZHOU MINSHENG PHARM CO LTD
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