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Levosimendan-containing injection medicine preparation and preparation method thereof

A technology of levosimendan and injection, applied in the field of pharmaceutical preparations, can solve the problems of carcinogenicity, toxicity and side effects, and achieve the effects of reducing toxicity and side effects, less hemolysis and good safety

Inactive Publication Date: 2018-07-10
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chinese patents CN100367964C, CN100428937C and CN1470238 disclose pharmaceutical preparations prepared by levosimendan and hydroxypropyl beta cyclodextrin, but some data show that hydroxypropyl beta cyclodextrin has certain nephrotoxicity and hemolytic properties, and also has Carcinogenicity, and there may be unknown and more serious toxic side effects, especially when it is used as an intravenous administration preparation, it should be carefully selected

Method used

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  • Levosimendan-containing injection medicine preparation and preparation method thereof
  • Levosimendan-containing injection medicine preparation and preparation method thereof
  • Levosimendan-containing injection medicine preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Add to 50ml

[0038] Take 8.0 g of sulfobutylbeta cyclodextrin, dissolve it in 40 ml of water for injection, add 125 mg of levosimendan, stir until the drug is completely dissolved, add water for injection to 50 ml, and obtain 2.5 mg / ml of levosimendan The quibeta cyclodextrin solution was sterilized by filtration through a 0.22 μm filter membrane, filled with 5ml / bottle, stoppered, and capped to obtain the injection A;

[0039] Or take 8.0g of sulfobutylbeta cyclodextrin, dissolve it in 40ml of water for injection, add 125mg of levosimendan, stir until the drug is completely dissolved, add water for injection to 50ml, and get 2.5mg / ml of levosimendan The butyl beta-cyclodextrin solution is sterilized by filtration through a 0.22 μm filter membrane, filled and semi-stoppered according to 5ml / bottle, freeze-dried, plugged, and capped. The yellow levosimendan freeze-dried powder A was obtained.

Embodiment 2

Add to 50ml

[0042] Take 2.5g of mannitol, 100mg of anhydrous citric acid, and 5.0g of sulfobutylbeta cyclodextrin, dissolve them in 40ml of water for injection, add 125mg of levosimendan, ultrasonicate until the drug is completely dissolved, add water for injection to 50ml, Obtain 2.5 mg / ml levosimendan sulfobutyl beta-cyclodextrin solution, filter and sterilize through a 0.22 μm filter membrane, fill with 5 ml / bottle, stopper, press the cap, and then sterilize at 121°C for 15 minutes, Get injection B;

[0043]Or take 2.5g of mannitol, 100mg of anhydrous citric acid, and 5.0g of sulfobutylbeta-cyclodextrin, dissolve in 40ml of water for injection, add 125mg of levosimendan, ultrasonically until the drug is completely dissolved, add water for injection to 50ml , to obtain 2.5 mg / ml levosimendan-sulphur-butyl-beta-cyclodextrin solution, which was sterilized by filtration through a 0.22 μm filter membrane, filled and semi-stoppered according to 5ml / bottle, freeze-dried, p...

Embodiment 3

Add to 50ml

[0046] Take 2.5g of mannitol, 100mg of anhydrous citric acid, and 12.5g of sulfobutylbeta cyclodextrin, dissolve in 40ml of water for injection, add 125mg of levosimendan, stir until the drug is completely dissolved, add water for injection to 50ml, Obtain 2.5 mg / ml levosimendan sulfobutyl beta-cyclodextrin solution, filter and sterilize through a 0.22 μm filter membrane, fill with 5 ml / bottle, stopper, press the cap, and then sterilize at 121°C for 15 minutes, Obtain injection C;

[0047] Or take 2.5g of mannitol, 100mg of anhydrous citric acid, and 12.5g of sulfobutylbeta cyclodextrin, dissolve in 40ml of water for injection, add 125mg of levosimendan, stir until the drug is completely dissolved, add water for injection to 50ml , to obtain 2.5 mg / ml levosimendan-sulphur-butyl-beta-cyclodextrin solution, which was sterilized by filtration through a 0.22 μm filter membrane, filled and semi-stoppered according to 5ml / bottle, freeze-dried, plugged, and capped...

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Abstract

The invention provides a levosimendan-containing injection medicine preparation and a preparation method thereof, and belongs to the field of medicine preparations. The preparation can be injection solution or freeze-dried powder and is mainly used for administrating medicines by injection. The injection solution comprises levosimendan serving as an active component or medicinal derivative of thelevosimendan and sulfobutyl beta cyclodextrin serving as a solubilizing stabilizer or medicinal salt of the sulfobutyl beta cyclodextrin, the weight ratio of the active component to the solubilizing stabilizer is 1:10-300, preferably, the weight ratio is 1:40-100, and most preferably, the weight ratio is 1:64-100. According to the preparation, the accessory sulfobutyl beta cyclodextrin has betterwater solubility, less hemolytic action and low renal toxicity as compared with hydroxypropyl beta cyclodextrin and is firstly used as a clathration material of the levosimendan or the medicinal derivative of the levosimendan. Compared with marketed similar injection solution, the injection solution takes water as a solvent, does not contain ethyl alcohol and is better in safety, and a freeze-dried preparation is more stable and easily stored at the room temperature.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a pharmaceutical preparation containing levosimendan or its pharmaceutically acceptable derivatives and sulfobutylbeta cyclodextrin or its pharmaceutically acceptable salts. The preparation of the invention can be an injection Or freeze-dried powder, mainly used for administration by injection route. The present invention also relates to a preparation method of the above-mentioned pharmaceutical preparation. Background technique [0002] Levosimendan, the chemical name is (R)-[[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]-hydrazine Base]-malononitrile, the structural formula is as follows: [0003] [0004] Levosimendan is a calcium sensitizer anti-acute heart failure drug developed by Orion Company in Finland. It was first launched in Sweden in 2000 under the trade name "Simdax". Marketed in the region, the specifications are 12.5mg / 5ml a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/08A61K31/50A61K47/40A61P9/04
CPCA61K47/40A61K9/0019A61K9/08A61K9/19A61K31/50
Inventor 李留法刘宝明杨清敏张明会
Owner QILU PHARMA CO LTD
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