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Desloratadine oral liquid preparation and preparation method thereof

A technology for desloratadine and liquid preparations, which is applied in the field of pharmacy, and can solve the problems of degraded impurities, poor stability of desloratadine, and unsatisfactory effects, and achieve the effect of improving stability and not producing degraded impurities

Active Publication Date: 2012-10-03
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of desloratadine in liquid preparations is poor. Researchers have tried to add some stabilizers to enhance the stability of desloratadine, but the effect is not ideal, and there are still degradation impurities

Method used

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  • Desloratadine oral liquid preparation and preparation method thereof
  • Desloratadine oral liquid preparation and preparation method thereof
  • Desloratadine oral liquid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation method of the oral liquid preparation of desloratadine in this example is as follows (wherein the molar ratio of desloratadine to cyclodextrin is 1:4):

[0048] (1) Dissolve 960mg of HP-β-CD (hydroxypropyl-β-cyclodextrin), 25mg of EDTA-2NaCa, 100mg of sodium benzoate (preservative), and 150mg of citric acid (organic acid) in 60ml of water , To obtain a cyclodextrin solution;

[0049] (2) Dissolve 50 mg of desloratadine in 10 ml of propylene glycol to obtain a desloratadine solution;

[0050] (3) Dissolve the desloratadine solution obtained in step (2) in the cyclodextrin solution obtained in step (1), adjust the pH to 5.5, add water to the volume to 100ml, mix well, and sterilize with moist heat at 115°C for 30 minutes The oral liquid preparation of desloratadine described in this example was obtained.

[0051] The HPLC chart of desloratadine oral liquid preparation obtained in this example is as follows image 3 As shown, it can be seen from the figure that th...

Embodiment 2

[0053] The preparation method of the oral liquid preparation of desloratadine in this example is as follows (wherein the molar ratio of desloratadine to cyclodextrin is 1:2):

[0054] (1) Dissolve 680 mg of SBE-β-CD (sulfobutyl-β-cyclodextrin) in 60 ml of water to obtain a cyclodextrin solution;

[0055] (2) Dissolve 50 mg of desloratadine in 10 ml of propylene glycol to obtain a desloratadine solution;

[0056] (3) Dissolve the desloratadine solution obtained in step (2) in the cyclodextrin solution obtained in step (1), add water to make the volume to 100ml, mix well, and sterilize with moist heat at 115°C for 30 minutes to obtain this example The oral liquid preparation of desloratadine.

[0057] The HPLC chart of desloratadine oral liquid preparation obtained in this example is as follows Figure 4 As shown, it can be seen from the figure that there is only a desloratadine peak at 8.740 minutes, no impurity peaks, and no degraded impurities exist.

Embodiment 3

[0059] The preparation method of the oral liquid preparation of desloratadine in this example is as follows (the molar ratio of desloratadine to cyclodextrin is 1:1):

[0060] (1) Dissolve 240mg of HP-β-CD (hydroxypropyl-β-cyclodextrin), 100mg of sodium benzoate (preservative), and 150mg of citric acid (organic acid) in 60ml of water to obtain a cyclodextrin solution ;

[0061] (2) Add 50 mg of desloratadine to the cyclodextrin solution obtained in step (1), dissolve ultrasonically for 15 minutes to obtain a transparent solution, adjust the pH to 6.0, add water to the volume to 100ml, mix and filter to obtain The oral liquid formulation of desloratadine described in this embodiment.

[0062] The HPLC chart of desloratadine oral liquid preparation obtained in this example is as follows Figure 5 As shown, it can be seen from the figure that there is only a desloratadine peak at 8.707 minutes, no impurity peaks, and no degraded impurities exist.

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Abstract

The invention discloses a desloratadine oral liquid preparation which comprises desloratadine, cyclodextrin, EDTA and water, wherein the mole ratio of desloratadine to cyclodextrin is 1:1-1:10, the concentration of desloratadine in the oral liquid preparation is 0.1mg / ml-1mg / ml, and the cyclodextrin is hydroxypropyl-beta-cyclodextrin or sulfobutyl-beta-cyclodextrin. According to the invention, cyclodextrin is added to the desloratadine oral liquid preparation prescription, the stability of the oral liquid preparation is greatly increased, and no degradation impurity is produced.

Description

Technical field [0001] The invention belongs to the field of pharmacy, and particularly relates to a desloratadine oral liquid preparation and a preparation method thereof. Background technique [0002] The chemical name of desloratadine is 8-chloro-6,11-dihydro-11-(4-azahexylidene)-5H-benzene-[5,6]cyclohepta[1,2-b]pyridine , The molecular formula is C 19 H 19 ClN 2 , The structural formula is as follows: [0003] [0004] Deloratadine is a non-sedating long-acting histamine antagonist, which has a potent and selective antagonistic effect on peripheral H1 receptors. Deloratadine has been proven to have anti-allergic, antihistamine and anti-inflammatory effects. After oral administration, desloratadine is effectively rejected from the central nervous system (CNS), so it can selectively block peripheral histamine H1 receptors. A large number of in vitro (mainly human tissue cells) and in vivo studies have shown that in addition to antihistamine effects, desloratadine also shows an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/4545A61K47/40A61P29/00A61P37/08
Inventor 吴传斌章正赞聂金媛王雪峰
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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