Inclusion preparation of levosimendan and beta cyclodextrin

A technology of β-cyclodextrin and inclusion compound, which is applied in the field of anti-heart failure drug-β-cyclodextrin inclusion preparation, can solve the problems of poor effect and achieve the effect of strong solubility, good stability and simple operation

Inactive Publication Date: 2008-02-13
王思清
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The levosimendan preparation that has been on the market is levosimendan-KollidonPF12 injection. However, the Chinese Pharmacopoeia 2000 edition does not include KollidonPF12 as a non-vascular excipient. It is reported that KollidonPF12 is not effective as a solubilizing and stabilizing agent

Method used

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  • Inclusion preparation of levosimendan and beta cyclodextrin
  • Inclusion preparation of levosimendan and beta cyclodextrin

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Levosimendan 2.5 mg / ml, hydroxypropyl β-cyclodextrin 50 mg / ml, and ethanol for injection 5 ml were dissolved to obtain a solution for injection.

Embodiment 2

[0033] Levosimendan 2.5mg / ml, hydroxypropyl beta cyclodextrin 50mg / ml, citrate 2mg / ml, and ethanol for injection 5ml are dissolved to obtain a solution for injection.

Embodiment 3

[0035] Levosimendan 2.5 mg / ml, hydroxypropyl β-cyclodextrin 50 mg / ml, dissolved in 5 ml of ethanol for injection, filtered, and vacuum-dried to obtain levosimendan-hydroxypropyl β-cyclodextrin inclusion compound dry powder.

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PUM

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Abstract

The present invention relates to one kind of heart failure resisting medicine, cyclodextrin or its derivative included preparation of levosimendan. The preparation has calcium-sensitive positive muscle medicine levosimendan as main component, and beta-cyclodextrin or its derivative, such as hydroxypropyl beta-cyclodextrin as including matter.

Description

Technical field: [0001] The invention relates to an anti-heart failure drug-beta-cyclodextrin inclusion preparation, in particular to a calcium-sensitive positive inotropic drug levosimendan as the main molecule and hydroxypropyl beta-cyclodextrin as the guest molecule. preparation. technical background: [0002] Levosimendan, chemical name [(4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl)hydrazono]malononitrile, Its structural formula is as follows: [0003] [0004] Levosimendan is a calcium-sensitizing myocardial inotrope mainly used in the treatment of congestive heart failure. Its preparation method is found in EP56556B1, WO97 / 35841, WO01 / 19334, WO98 / 01111, CN1470238A. [0005] Levosimendan is yellow powder crystal, slightly soluble in water, pKa is 6.26, solubility in phosphate buffer (pH7.4) is 0.4mg / ml, solubility in water at pH6 and pH2 is 0.03mg / ml and 0.02 respectively mg / ml; insoluble and easily degradable in water. The levosimendan preparation...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/50A61K9/08A61K47/40A61P9/04
Inventor 王思清毛白杨
Owner 王思清
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