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Preparation method of solid pharmaceutical composition containing desloratadine

A technology of desloratadine and its composition, which is applied in the field of preparation of solid pharmaceutical compositions, can solve the problems of insufficient product stability, cumbersome process, and increased quantity, and achieve low density, uniform particle size distribution, and low strength Effect

Active Publication Date: 2010-10-06
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent discloses a pharmaceutical composition containing an alkaline salt, which improves the stability of the desloratadine preparation product to a certain extent, but its disclosed examples show that its preparation product is at 40°C and 75% relative humidity. After 6 months of storage under conditions, the amount of impurity N-formyldesloratadine increased to 0.8% (bottle) and 1.2% (aluminum-plastic blister pack)
The daily dose of desloratadine is 5 mg. According to the guidelines of the National Drug Evaluation Center, the quality control limit of impurities is 0.5%. Obviously, the patented scheme is not enough to guarantee the stability of the product
Moreover, the preparation method disclosed in this patent needs to heat the starch / water dispersion to 95°C to prepare starch slurry as a binder. This method is cumbersome and consumes a lot of energy. It has been gradually replaced by other processes.

Method used

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  • Preparation method of solid pharmaceutical composition containing desloratadine
  • Preparation method of solid pharmaceutical composition containing desloratadine
  • Preparation method of solid pharmaceutical composition containing desloratadine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0070] See Table 3 for the prescription:

[0071] table 3

[0072]

[0073]

[0074] Wherein, the desloratadine particle size d (0.9) that embodiment 1 uses is 150 μ m; The desloratadine particle size d (0.9) that embodiment 2 uses is 330 μ m; The desloratadine that embodiment 3 uses The particle size d(0.9) was 350 μm.

[0075] Preparation Process:

[0076] 1. Disperse 5g of desloratadine into 100g of water to form a dispersion;

[0077] 2. Pour calcium hydrogen phosphate dihydrate, microcrystalline cellulose, and cornstarch into the fluidized bed, and spray the desloratadine aqueous dispersion in a heated fluidized state;

[0078] 3. Heat and dry the material in the fluidized bed so that the drying weight loss of the material is less than 3.0%;

[0079] 4. Sieve the dried material, add talcum powder and magnesium stearate to form a mixture;

[0080] 5. Compress the mixture into tablets with a 7 mm round punch to obtain tablets with a table...

Embodiment 4-6

[0087] See Table 5 for the prescription:

[0088] table 5

[0089]

[0090] Preparation Process:

[0091] 1. Disperse 5g of desloratadine into 100g of water to form a dispersion;

[0092] 2. Pour calcium hydrogen phosphate dihydrate, optimized microcrystalline cellulose, and cornstarch into the fluidized bed, and spray desloratadine water dispersion in a heated fluidized state;

[0093] 3. Heat and dry the material in the fluidized bed so that the drying weight loss of the material is less than 3.0%;

[0094] 4. Sieve the dried material, add talcum powder and magnesium stearate to form a mixture;

[0095] 5. Compress the mixture into tablets with a 7 mm round punch to obtain tablets with a tablet weight of about 100 mg.

[0096] 6. Use a high-efficiency coating pan to coat the tablets.

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Abstract

The invention relates to a pharmaceutical preparation containing valsartan, which at least comprises active ingredient valsartan or a pharmaceutically acceptable salt thereof and at least two disintegrants in a ratio between 1: 2 and 2;1. The invention also relates to a preparation method of the valsartan preparation, which comprises the following steps of: firstly, pelletizing the valsartan or the pharmaceutically acceptable salt thereof by a rolling method; mixing with at least two disintegrants and other pharmaceutic accessories; and tabletting or filling capsules. Compared with a product prepared by the prior art, the valsartan preparation of the invention has better stability. The method of the invention has simple production process and high production efficiency and is suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation method of a solid pharmaceutical composition, in particular to a preparation method of a solid pharmaceutical composition containing desloratadine. Background technique [0002] Desloratadine is a non-sedating long-acting tricyclic antihistamine used in the treatment of allergic rhinitis and chronic idiopathic urticaria. [0003] Its chemical name is: 8-chloro-6,11-dihydro-11(4-piperidinylene)-5H-benzo-[5,6]heptane[1,2-b]pyridine. [0004] English name: Desloratadine. [0005] Simple structure: [0006] [0007] US 4659716 first described desloratadine in detail: it is an active metabolite of loratadine, which can inhibit the release of various allergic inflammatory chemical mediators by selectively blocking peripheral H1 receptors, Such as inhibition of mast cells and basophils to release histamine, prostaglandins, interleukins and so on. [0008] US 5595997 proposes that desloratadine can provide effectiv...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4545A61K47/02A61P37/08A61P11/02A61P17/00
Inventor 彭俊清李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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