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Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione

A technology of dihydrogen and amino, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of reducing efficacy, and achieve the effect of cheap production costs and cheap materials

Pending Publication Date: 2020-08-25
METRIOPHARM AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Another problem with polysorbates such as Tween 80 is that their efficacy is reduced by combining them with widely used preservatives such as parabens (see Blanchard et al., Effect of sorbitol on interaction of phenolic preservatives with polysorbate 80 , 1977, JPharm Sci 66, p.1470-1473)

Method used

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  • Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione
  • Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione
  • Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione

Examples

Experimental program
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Effect test

Embodiment 1

[0234] Example 1: Solubilization of 5-amino-2,3-dihydro-1,4-phthalazinedione - Embodiment 1

[0235] The following indications refer to the weight percent of the mixture. About 100 ml of solubilized material was produced. 5-Amino-2,3-dihydro-1,4-phthalazinedione was provided, and then the solubilizers were mixed one by one with stirring at room temperature (20±5° C.) and atmospheric pressure for 5 minutes.

[0236]

[0237]

[0238] The composition was then carefully heated in temperature increments of about 1°C / minute under continuous stirring. After about 20 minutes (about 40°C), the composition started to turn into a clear solution. This solubilization process lasted over about 16 minutes. Thus, at about 56° C., the solubilized product according to the invention is obtained after about 36 minutes. Heating and stirring were then discontinued, and the resulting solubilized mass was allowed to cool to room temperature. The solubilized material remained clear and st...

Embodiment 2

[0239] Example 2: Solubilization of 5-amino-2,3-dihydro-1,4-phthalazinedione - Embodiment 2

[0240] The following indications refer to the weight percent of the mixture. About 100 ml of solubilized material was produced. 5-Amino-2,3-dihydro-1,4-phthalazinedione was provided, and then the solubilizers were mixed one by one with stirring at room temperature (20±5° C.) and atmospheric pressure for 5 minutes.

[0241]

[0242] The composition was then carefully heated in temperature increments of about 1.5°C / minute with continuous stirring. After about 23 minutes (about 55°C), the composition started to turn into a clear solution. This solubilization process lasted for about 10 minutes or more. Thus, the solubilisate according to the invention is obtained after about 33 minutes at about 70° C. Heating and stirring were then discontinued, and the resulting solubilized mass was allowed to cool to room temperature. The solubilized material remained clear and stable for a m...

Embodiment 3

[0243] Example 3: Solubilization of 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt

[0244] The following indications refer to the weight percent of the mixture. About 100 ml of solubilized material was produced. Provide 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt (in the form of the type I polymorph as described in WO 2011 / 107295 A1), then at room temperature (20±5 °C) and atmospheric pressure for 5 minutes to mix the solubilizers one by one.

[0245]

[0246] The composition was then carefully heated in temperature increments of about 1°C / minute under continuous stirring. After about 32 minutes (about 52°C), the composition started to turn into a clear solution. This solubilization process lasted for about 8 minutes or more. Thus, the solubilisate according to the invention is obtained after about 40 minutes at about 60° C. Heating and stirring were then discontinued, and the resulting solubilized mass was allowed to cool to room temperature. The so...

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Abstract

The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4- phthalazinedione or salts thereof, to the solubilisate produced by this method and respective uses in pharmaceuticaldosage forms. A phosphatidylcholine-based solubilization method is disclosed.

Description

technical field [0001] The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione or a salt thereof, to a solubilized product produced by the method, to its use and to containing said Pharmaceutical compositions of solubilized substances. Background technique [0002] For decades, crime scene investigators have used 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) to detect traces of blood, even when efforts were made to wash or remove the blood (see Barni et al., Talanta 2007, 72, 896-913). The strong luminescence produced by the catalyzed oxidation of iron in hemoglobin makes luminol a sensitive sensor. Apart from its use in forensics, since the first reports on the synthesis of luminol (A.J.Schmitz, das Hydrazid der und der Heidelberg, 1902), has established many other applications ranging from the environment to medicine. For example, luminol is used for heavy metal detection or biosensing in bioanalytical chemistry (se...

Claims

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Application Information

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IPC IPC(8): C07D237/32A61K31/502A61P37/02
CPCC07D237/32A61K31/502A61K9/0019A61K47/22A61P37/00A61K9/0014A61K9/0053
Inventor I·萨尔W·布里施
Owner METRIOPHARM AG
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