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Polymorphism of desloratadine disodium hydrogen citrate complex salt

A technology of disodium hydrogen citrate and delotadine, which is applied in the field of medicinal chemistry, can solve the problems of inability to fully exert the medicinal effect, low solubility of delotadine, poor solubility, etc. The effect of non-toxic dosage and low production cost

Active Publication Date: 2015-04-22
HEFEI AMVITE PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, the solubility of desloratadine in water is low, and the solubility in water at 25°C is only 0.0723 mg / ml, which may directly affect its absorption in the body and cannot fully exert its drug effect
Chinese patent CN02128998.0 has reported that desloratadine disodium hydrogen citrate double salt can well solve the defect of poor solubility

Method used

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  • Polymorphism of desloratadine disodium hydrogen citrate complex salt
  • Polymorphism of desloratadine disodium hydrogen citrate complex salt
  • Polymorphism of desloratadine disodium hydrogen citrate complex salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Preparation of Form A:

[0027] Add 3g of desloratadine disodium hydrogen citrate double salt into a 50ml eggplant-shaped bottle, add 30ml of acetone and 5ml of water (volume ratio 6:1), stir electromagnetically, heat to 65°C to completely dissolve, and cool to about 20 minutes. Room temperature, and placed at 5-10°C for 3 hours, the precipitated solid was suction-filtered, and dried at 80°C for 6 hours to obtain about 2.6 g of white powder, which was identified as Compound I crystal form A.

[0028] X-ray powder diffraction pattern see figure 1 , see the DSC analysis chart figure 2 , see the thermogravimetric analysis spectrum image 3 , see the infrared absorption spectrum Figure 4 .

Embodiment 2

[0030] Preparation of Amorphous Solid:

[0031] In this method, a Labconco lyophilizer was used under the following conditions: pre-freezing at -40°C for 2 hours; drying at -40°C for 3 hours, -30°C for 6 hours, and -15°C for 6 hours under reduced pressure. hours, dry at -5°C for 8 hours, and dry at 18°C ​​for 10 hours.

[0032] Dissolve 2 g of desloratadine disodium hydrogen citrate double salt in 6 ml of water at room temperature, then freeze-dry according to the above conditions to obtain 1.6 g of white powder, which is identified as desloratadine disodium hydrogen citrate double salt Amorphous solid.

[0033] X-ray powder diffraction pattern see Figure 5 , see the DSC analysis chart Figure 6 , see the thermogravimetric analysis spectrum Figure 7 , see the infrared absorption spectrum Figure 8 .

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Abstract

The invention belongs to the field of medicinal chemistry and specifically relates to a polymorphic and amorphous state of a desloratadine disodium hydrogen citrate complex salt and a preparation method thereof. The polymorphic and amorphous state is characterized in that an X-ray powder diffraction pattern of polymorphism has characteristic peaks in the vicinity of 2 theta angles of 11.45 degrees, 16.36 degrees, 17.74 degrees, 18.55 degrees, 19.13 degrees, 24.23 degrees, 27.54 degrees, 30.99 degrees, 32.82 degrees and 37.39 degrees. The preparation method of the polymorphic and amorphous state of the desloratadine disodium hydrogen citrate complex salt, disclosed by the invention, has the benefits of simplicity in operation, small using quantity of solvents, no toxicity and low production cost, and further has obvious advantages in the aspect of industrialization.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to the polymorph and amorphous form of desloratadine disodium hydrogen citrate double salt and a preparation method thereof. Background technique [0002] Desloratadine is an active metabolite of the non-sedating antihistamine Loratadine, which selectively inhibits H1 receptors. According to U.S. Patent No. 5,595,997 (authorized on January 21, 1997), the antihistamine effect of desloratadine is safe and effective and has no sedative effect, which can avoid the effects caused by common antihistamines and non-sedating antihistamines (especially such as loratadine). Common serious side effects associated with the administration of hepatidine, terfestatin, and astemizole). More importantly, the inhibitory activity of desloratadine on histamine receptors is at least 20 times higher than that of loratadine. Therefore, compared with loratadine, desloratadine has stronger ef...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04C07C51/43C07C59/265
Inventor 徐云根周海平何广卫陆静
Owner HEFEI AMVITE PHARM CO LTD
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