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Coated tablet containing desloratadine and preparation method thereof

A technology for desloratadine and coated tablets, which is applied in the field of desloratadine coated tablets and its preparation, can solve the problems of substance increase and stability control of desloratadine tablets. solution, oxidative degradation, etc.

Active Publication Date: 2009-10-07
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it was found in the experiment that desloratadine is prone to oxidative degradation during the co-grinding process, resulting in the increase of related substances.
[0008] So far, the stability control problem of desloratadine tablets has not been well resolved

Method used

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  • Coated tablet containing desloratadine and preparation method thereof
  • Coated tablet containing desloratadine and preparation method thereof
  • Coated tablet containing desloratadine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Tablet core prescription

[0029]

[0030] Coating Solution Prescription

[0031]

[0032] Preparation method: Dissolve desloratadine and β-cyclodextrin in an appropriate amount of 50% ethanol by weighing the prescription ratio, stir to make it fully dissolve, and use it as a binder; Mix precrossed starch evenly; add binder to make soft material, pass through 18-mesh sieve to granulate, and then granulate with 20-mesh sieve after drying in a 40-degree oven; add the prescribed amount of talcum powder, mix evenly, and determine the particle content Pressing into tablets; preparing a coating solution according to the prescription ratio, and coating.

Embodiment 2

[0034] Tablet core prescription

[0035]

[0036] Coating Solution Prescription

[0037]

[0038] Preparation method: Dissolve the desloratadine and PEG6000 in the proportion of the prescription in an appropriate amount of 75% ethanol, stir to make it fully dissolve, and use it as a binder; Mix the starch evenly; add the soft material made of binder, granulate through a 18-mesh sieve, and granulate with a 20-mesh sieve after drying in a 40-degree oven; add the prescribed amount of talcum powder, mix evenly, and press the tablet after determining the granule content; Prepare the coating solution according to the prescription ratio, and coat.

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PUM

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Abstract

The invention discloses a coated tablet containing desloratadine and a preparation method thereof. The coated tablet applies a combination of calcium hydrogen phosphate, microcrystalline cellulose and pregelatinized starch of specific proportion, performs inclusion to the desloratadine by applying the solid dispersion technology, ensures the crushability of the particles so as to be improved in the dissolution rate, reduces the degradation of the desloratadine in the oxygen and the moisture and effectively increases the stability.

Description

technical field [0001] The invention relates to a desloratadine coated tablet and a preparation method thereof, in particular to a desloratadine coated tablet containing a specific auxiliary material composition and a solid dispersion, which is used to relieve allergic rhinitis or chronic Symptoms associated with idiopathic urticaria. Background technique [0002] Desloratadine, the active metabolite of loratadine, is a non-sedating long-acting tricyclic antihistamine. US Patent No. 4,659,716 first described desloratadine in detail. Desloratadine can inhibit the release of various allergic inflammatory mediators by selectively blocking peripheral H1 receptors, such as inhibiting the release of histamine, prostaglandins, interleukins, etc. from mast cells and basophils , to relieve allergic rhinitis or chronic idiopathic urticaria. [0003] Desloratadine is a secondary amine compound that is sensitive to acids and carbohydrates, and is prone to Maillard reaction to produce...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/4545A61P37/08A61P11/00
Inventor 孟凡静
Owner AVENTIS PHARMA HAINAN
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