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Sustained-release transdermal patch containing ketotifen and application thereof

A technology of slow-release transdermal and ketotifen, which is applied in the field of sustained-release transdermal preparations for external use and sustained-release transdermal preparations containing ketotifen, which can solve the problems of inability to maintain stability, low skin permeability, and irritation To achieve the effect of balanced blood drug concentration, high transdermal rate and gentle onset

Inactive Publication Date: 2017-11-24
徐静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The patch of the present invention can solve the problem that the skin permeability of the patch occurs in the acid addition salt (such as ketotifen fumarate) form of ketotifen; Or the acid addition salt form of ketotifen can be selected to add the base containing metal ions to react to generate the patch of ketotifen free base form, but the strong alkalinity containing metal ions produces obvious skin irritation problems

Method used

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  • Sustained-release transdermal patch containing ketotifen and application thereof
  • Sustained-release transdermal patch containing ketotifen and application thereof
  • Sustained-release transdermal patch containing ketotifen and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: prepare the sustained release transdermal patch containing ketotifen, formula is as follows:

[0065]

[0066]

[0067] Prepare according to the following preparation process:

[0068] ①Dissolve ketotifen, azone, tocopherol or its esters, squalane in acetone, add fat-soluble acrylate pressure-sensitive adhesive and mix well; ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, and then covered with a protective layer; ③ cut according to the required size, packaged, and then made into a sustained-release transdermal patch containing ketotifen.

Embodiment 2

[0069] Embodiment 2: prepare the sustained-release transdermal patch containing ketotifen, the formula is as follows:

[0070]

[0071] Prepare according to the following preparation process:

[0072] ①Dissolve ketotifen, azone, tocopherol or its esters, squalane in acetone, add fat-soluble acrylate pressure-sensitive adhesive and mix well; ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, and then covered with a protective layer; ③ cut according to the required size, packaged, and then made into a sustained-release transdermal patch containing ketotifen.

Embodiment 3

[0073] Embodiment 3: prepare the sustained-release transdermal patch containing ketotifen, the formula is as follows:

[0074]

[0075] Prepare according to the following preparation process:

[0076] ①Dissolve ketotifen, azone, tocopherol or its esters, squalane in acetone, add fat-soluble acrylate pressure-sensitive adhesive and mix well; ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, and then covered with a protective layer; ③ cut according to the required size, packaged, and then made into a sustained-release transdermal patch containing ketotifen.

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Abstract

The invention relates to a sustained-release transdermal patch containing ketotifen and application thereof. The sustained-release transdermal patch comprises a backing layer, a medicine-containing reservoir layer and an anti-sticking protective layer, wherein the medicine-containing reservoir layer contains a transdermal accelerant selected from azone, oleic acid and isopropyl myristate, contains antioxidant tocopherol or ester thereof for improving the stability of ketotifen free alkali, and contains squalene to reduce skin irritation of a ketotifen sustained-release transdermal patch.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a slow-release transdermal preparation for external use of medicine, in particular to a sustained-release transdermal preparation containing ketotifen and its application. Background technique [0002] Ketotifen is an oral potent allergenic transmitter release agent. The drug can not only inhibit the antigen-induced release of histamine and allergic slow-response substance (SRS-A) from mast cells in the lung and bronchial tissue, but also inhibit the induction of eosinophils or neutrophils by antigens, serum or calcium ion transmitters. Slow-reacting substances that release histamine and allergies. The drug has a strong H1 receptor antagonistic effect and can antagonize 5-hydroxytryptamine and allergic slow-response substances. Studies have found that the drug can inhibit non-specific airway hyperresponsiveness in patients with bronchial asthma, ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/22A61K47/06A61K31/4535A61P11/02A61P37/08A61P11/06
CPCA61K9/7023A61K31/4535A61K47/06A61K47/22
Inventor 徐静
Owner 徐静
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