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Milrinone compound and pharmaceutical composition containing milrinone compound

The technology of a composition and milrinone is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., and can solve the effects of milrinone on drug efficacy and bioavailability, poor stability and clarity, and high impurity content, etc. problem, to achieve the effect of high safety, avoid side effects, and low impurity content

Active Publication Date: 2014-12-03
朗天药业(湖北)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The applicant's early patent CN102579329A provides a pharmaceutical composition for milrinone lactate injection, adding optimal doses of vitamin C and meglumine to solve the problems of poor stability and clarity when lactic acid is used to aid dissolution
[0011] But the impurity content of the milrinone injection in the prior art is obviously on the high side, which has a certain impact on the efficacy and bioavailability of milrinone; on the other hand, the higher impurity content may produce certain side effects, The present invention is thus proposed

Method used

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  • Milrinone compound and pharmaceutical composition containing milrinone compound
  • Milrinone compound and pharmaceutical composition containing milrinone compound
  • Milrinone compound and pharmaceutical composition containing milrinone compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Milrinone 1g

[0032] Sodium chloride 9g

[0033] Lactic acid amount

[0034] Water for injection 1000ml

[0035] Preparation Process:

[0036] (1) Add lactic acid to 150 ml of water to adjust the pH to about 2.0, raise the temperature to 80°C while stirring, add 1g of milrinone while stirring after heating, and continue stirring for 10-20 minutes. Then add an appropriate amount of activated carbon with a concentration of 0.15%, and continue stirring for 10-15 minutes.

[0037] (2) Add 500ml of water to the above mixture to keep the temperature at 75-80°C, then add 9g of sodium chloride, and at the same time add an appropriate amount of 0.10% activated carbon, and continue stirring at this temperature for 10-15 minutes.

[0038] (3) Add water to the full amount, keep the temperature at 75-80°C, add an appropriate amount of 0.05% activated carbon at the same time, stir for 10-15 minutes, and adjust the pH at 3.0-4.3 with an appropriate amount of lactic ac...

Embodiment 2

[0042] Milrinone 2g

[0043] Sodium chloride 18g

[0044] Appropriate amount of lactic acid

[0045] Water for injection 2000ml

[0046] Preparation Process:

[0047] (1) Add lactic acid to 300ml of water to adjust the pH to about 2.0, raise the temperature to 80°C with stirring, add 1g of milrinone with stirring after heating, and continue stirring for 10-20 minutes. Then add an appropriate amount of activated carbon with a concentration of 0.15%, and continue stirring for 10-15 minutes.

[0048] (2) Add 1000ml of water to the above mixture to keep the temperature at 75-80°C, then add 9g of sodium chloride, and at the same time add an appropriate amount of 0.10% activated carbon, and continue stirring at this temperature for 10-15 minutes.

[0049](3) Add water to the full amount, keep the temperature at 75-80°C, add an appropriate amount of 0.05% activated carbon at the same time, stir for 10-15 minutes, and adjust the pH at 3.0-4.3 with an appropriate amount of lactic a...

experiment example 1

[0066] This experimental example is mainly to test the adsorption of activated carbon to milrinone.

[0067] In the preparation of injections, an appropriate amount of activated carbon with a concentration of 0.01%-0.5% (g / ml) is usually added to improve the clarity of the liquid and the effect of adsorbing pyrogens, and it may also have a certain adsorption effect on the main drug. In the patent CN102579329A, the verification experiment of the influence of different concentrations of activated carbon on the clarity and color of the liquid medicine and the content of milrinone was given, which proved that activated carbon has a certain adsorption on the main drug milrinone, and with the increase of the concentration of activated carbon The adsorption of milrinone is obvious. Therefore, in order to ensure the effect of activated carbon in removing pyrogens, it is generally recommended to use activated carbon with a concentration of 0.05% for 20-30 minutes during the preparation...

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Abstract

The invention discloses a milrinone compound and a pharmaceutical composition containing the milrinone compound. According to the invention, lactic acid is adopted for helping solubilization and regulating the pH value, so that hyperchloremia which is possibly caused by extremely high Cl- concentration brought by pH regulation by adopting hydrochloric acid is avoided. In addition, the milrinone compound and the pharmaceutical composition are reasonable in prescription, high in quality standard, low in impurity content and high in bioavailability, has unique advantages in safety, effectiveness and quality stability, and also has an international level and more outstanding advantages.

Description

technical field [0001] The invention relates to a milrinone compound, a pharmaceutical composition thereof, and a preparation method of the pharmaceutical composition prepared by using the composition. Background technique [0002] Milrinone (also known as cyanopyrone, milrinone) is off-white crystalline powder, odorless, almost insoluble in water or ethanol, slightly soluble in dilute hydrochloric acid, generally 1-(4-pyridyl)- Acetone is the starting material; react with triethyl orthoformate and acetic anhydride at room temperature to obtain 1-ethoxy-2-(4-pyridyl)-vinyl methyl ketone; finally react with ethyl cyanide in alkaline environment Amide cyclization to obtain milrinone; finally recrystallized with a mixed solvent of dimethylformamide and water. [0003] Milrinone, as a non-cardiac glycoside, non-catecholamine new cardiotonic drug, is mainly suitable for acute and chronic intractable diseases caused by various reasons that are ineffective or ineffective in the tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/444A61K9/08A61K47/04A61P9/04
Inventor 蔡翔黎翩
Owner 朗天药业(湖北)有限公司
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