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Skin paste capable of improving dementia, delusion and myasthenia due to cholinergic

A technology for skin patch and muscle weakness, applied in the field of medicine, can solve problems such as unreasonableness and fluctuation of blood drug concentration, and achieve the effect of reducing burden and improving quality of life

Inactive Publication Date: 2009-06-17
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Traditionally marketed galantamine dosage forms include oral preparations and injection preparations. Injection administration requires special technology. For symptoms that require long-term medication, such as dementia caused by AD, it is very unreasonable to use injection administration
The oral dosage form is convenient for administration, but the blood concentration fluctuation caused by the traditional oral dosage form can cause gastrointestinal side effects such as nausea and vomiting

Method used

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  • Skin paste capable of improving dementia, delusion and myasthenia due to cholinergic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1. take emulsion type acrylate pressure-sensitive adhesive as the skin patch of matrix

[0018] Formula and ratio:

[0019] Galantamine Hydrobromide 0.3g

[0020] Acrylate Emulsion Pressure Sensitive Adhesive 36.9g

[0021] Thickener 1.2g

[0022] Concentrated ammonia water 1.5ml

[0023] Purified water 6.25ml

[0024] The preparation method is:

[0025] Dissolve galantamine hydrobromide in pure water, add it to the acrylate emulsion pressure-sensitive adhesive, stir evenly while adding, add thickener, concentrated ammonia water, stir evenly, and spread on 1000cm 2 On anti-sticking paper, bake at 80°C for 30 minutes, cover the backing layer, leave at room temperature overnight, cut into 5×7cm 2 ,sealed package.

Embodiment 2

[0026] Embodiment 2. take solvent-type acrylate pressure-sensitive adhesive as the skin patch of matrix

[0027] Formula and ratio:

[0028] Galantamine Hydrobromide 0.3g

[0029] Alkaline absolute ethanol 2.0mL

[0030] Solvent Acrylic Pressure Sensitive Adhesive (38%) 46.0g

[0031] The preparation method is:

[0032] Dissolve galantamine hydrobromide in alkaline absolute ethanol (adjust absolute ethanol to pH 10 with 5mol / L NaOH solution), and add it to solvent-based acrylate pressure-sensitive adhesive (DURO-TAK 87-2677, American National Starch Company), stir evenly while adding, spread on 1000cm 2 On anti-sticking paper, bake at 80°C for 30 minutes, cover the backing layer, leave at room temperature overnight, cut into 5×7cm 2 ,sealed package.

Embodiment 3

[0033] Embodiment 3. take polyisobutylene pressure-sensitive adhesive as the skin patch of matrix

[0034] Formula and ratio:

[0035] Galantamine 3.1g

[0036] High Molecular Weight Polyisobutylene 5.3g

[0037] Low molecular weight polyisobutylene 2.8g

[0038] Liquid paraffin 5.4g

[0039] Carbopentyl resin 7.0g

[0040] 2,6-di-tert-butyl-p-cresol 14mg

[0041] Azone 1.8g

[0042] Medical gasoline 100mL

[0043] Steps:

[0044] Add the non-polar polymer high molecular weight polyisobutylene and low molecular weight polyisobutylene, plasticizer liquid paraffin and thickener carbopentyl resin to the medical gasoline according to the above ratio to completely swell, then add the drug galantamine and the transdermal accelerator Azone and antioxidant 2,6-di-tert-butyl-p-cresol, stir evenly, ultrasonically remove air bubbles, and then apply it on the anti-adhesive layer on a coating machine as usual, with a coating area of ​​1000cm 2, drying while coating, drying at 60°C...

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Abstract

A skin patch which improves symptoms of ashronesia, delusion and myasthenia caused by cholinergic deficit is composed of an antiseizing layer, a medicine storing layer and a back lining layer, wherein the medicine storing layer comprises medicine, dissolvent and pressure-sensitive adhesive. The invention is characterized in that the medicine is galantamin or hydrobromate thereof. The galantamin or hydrobromate thereof is 0.007mg-10mg / cm<2>, and the medication area is 2.5-70cm<2>. The pressure-sensitive adhesive is selected from polyisobutene pressure-sensitive adhesive, emulsion and dissolvent type acrylate. When the pressure-sensitive adhesive is polyisobutene, the medicine storing layer is composed of medicine, dissolvent, pressure-sensitive adhesive, thickening agent, anti-oxidant and transdermal promoter. When the pressure-sensitive adhesive is emulsion type acrylate, the medicine storing layer is composed of medicine, dissolvent, pressure-sensitive adhesive, thickening agent and concentrated ammonia liquor. When the pressure-sensitive adhesive is dissolvent type acrylate, the medicine storing layer is composed of medicine, dissolvent, and pressure-sensitive adhesive. The skin patch of the invention can effectively treat the symptoms of ashronesia, delusion and myasthenia caused by cholinergic deficit, increase the life quality of patient and alleviate the burden of kin and society.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a galantamine skin patch for treating dementia, delusion, muscle weakness and other symptoms caused by cholinergic deficiency. Background technique [0002] Galanthamine is a phenanthridine alkaloid extracted and isolated from Amaryllidaceae. It is a reversible, selective and competitive cholinesterase inhibitor, and can allosterically activate tobacco Alkaline acetylcholine receptors reduce the degradation of acetylcholine through these two pathways, activate cholinergic receptors, and improve symptoms such as dementia, delusions, and muscle weakness caused by choline deficiency. [0003] Alzheimer's disease (Alzheimer disease, AD) is a common chronic progressive neurodegenerative disease in the elderly, with dementia as the main symptom, a large number of patients, and a wide range of effects. Among the elderly over 65 years old, about 10% have AD. Because most AD patients hav...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/55A61P25/28
Inventor 胡晋红刘艳霞朱全刚陆松伟孙创斌
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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