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Granule containing acrylic acid resin and desloratadine, and preparation method thereof

A desloratadine and acrylic resin technology, applied in the field of medicine, can solve the problems of elevated related substances, unsuitable desloratadine granules, inability to achieve taste masking and the like

Inactive Publication Date: 2015-01-28
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Desloratadine is slightly soluble in water and has an extremely bitter taste. The use of common flavoring agents cannot achieve the effect of masking the taste, and it is easy to react with sugars, such as sucrose, lactose, etc., causing the increase of related substances
In granules, soluble sugars generally need to be added as fillers, so the preparation method of ordinary granules is not suitable for desloratadine granules

Method used

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  • Granule containing acrylic acid resin and desloratadine, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] In this embodiment, the ratio of desloratadine to acrylic resin is 1:1, the ratio of acrylic resin and desloratadine solid to organic solvent is 1:2, and the selected organic solvent is ethanol. The distribution ratio for each group is:

[0013] components percentage(%) Desloratadine 0.5 Acrylic 0.5 Mannitol 20 sucrose 65 microcrystalline cellulose 9.0 Povidone K30 1.5 Magnesium stearate 1.0 sunset yellow 0.5 xanthan gum 1.0 Sweet Orange Flavor 1.0 Total 100

[0014] Preparation process: Add 5g of acrylic resin and 5g of desloratadine into 20g of ethanol and stir for 30 minutes to fully disperse and form a complex. The clathrate solution is dried at 50°C by spray drying method , collect the clathrate granules after drying, then add 200g mannitol, 650g sucrose, 90g microcrystalline cellulose, with 10% povidone K30, adopt wet granulation process granulation as binder, wet granules are again i...

Embodiment 2

[0016] In this embodiment, the ratio of desloratadine to acrylic resin is 1:10, and the ratio of acrylic resin to desloratadine solid to ethanol is 1:10. The distribution ratio for each group is:

[0017] components percentage(%) Desloratadine Hydrochloride 0.5 Acrylic 5 Mannitol 20 sucrose 60 microcrystalline cellulose 9.0 hypromellose 1.5 Magnesium stearate 1.0 lemon yellow 0.5 Sodium carboxymethyl cellulose 1.0 apple flavor 1.0 Total 100

[0018] Preparation process: Add 50g of acrylic resin and 5g of desloratadine into 550g of ethanol and stir for 30 minutes to fully disperse and form a complex. The clathrate solution is dried at 70°C by spray drying , collect the clathrate particles after drying, then add 200g mannitol, 600g sucrose, 90g microcrystalline cellulose, use 10% hypromellose as a binder to granulate by wet granulation process, and then wet the granules in Dry at 50°C, the solid co...

Embodiment 3

[0020] In this embodiment, the ratio of desloratadine to acrylic resin is 1:5, and the ratio of acrylic resin to desloratadine solid to ethanol is 1:5. The distribution ratio for each group is:

[0021] components percentage(%) Desloratadine Hydrochloride 0.5 Acrylic 2.5 Mannitol 20 sucrose 60 microcrystalline cellulose 11.5 Magnesium stearate 1.0 lemon yellow 0.5 Sodium carboxymethyl cellulose 1.0 apple flavor 1.0 Total 100

[0022] Preparation process: Add 25g of acrylic resin and 5g of desloratadine into 150% ethanol and stir for 30 minutes to fully disperse and form a complex. The clathrate solution is dried at 60°C by spray drying , collect the clathrate granules after drying, then add 200g mannitol, 600g sucrose, 10g microcrystalline cellulose, adopt dry granulation process to granulate, finally add 10g magnesium stearate, 5g tartrazine, 10g carboxymethyl cellulose Su sodium, 10g of apple flavor,...

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Abstract

The present invention discloses a method for preparing desloratadine particles by using a solvent drying method, wherein the method is characterized in that the drug and an acrylic acid resin are prepared into a clathrate through a solvent drying method, and then the particle and an appropriate auxiliary material (such as a filler, a flavoring agent, a disintegrating agent, a suspending aid and the like) are completely mixed to granulate. With the process, the taste can be significantly improved, and the drug stability can be increased.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a method for preparing desloratadine granules by a solvent drying method. Background technique [0002] With the development of society, environmental pollution is becoming more and more serious, the pace of life is faster, and the pressure is greater. These factors lead to a high incidence of allergic diseases and seriously affect people's quality of life. disease is particularly pronounced. [0003] Desloratadine (Desloratadine) is a non-sedating long-acting tricyclic antihistamine, which is the active metabolite of loratadine, and can relieve allergic rhinitis or chronic rhinitis by selectively antagonizing peripheral H1 receptors. Symptoms associated with idiopathic urticaria. [0004] Studies have shown that desloratadine does not easily pass through the blood-brain barrier and is suitable for rapid relief of symptoms related to allergic rhinitis, such as sneezing, run...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4545A61K47/32A61P37/08A61P11/02A61P17/00
Inventor 刁媛媛马苏峰郭夏
Owner AVENTIS PHARMA HAINAN
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