Escitalopram percutaneous patch and preparation method thereof
A patch and organic solvent technology, applied in the field of medicine, can solve problems such as difficulties, complicated production process, burst release, etc., and achieve the effects of long-lasting and stable curative effect, good adhesion, and convenient use
Active Publication Date: 2015-08-19
SHENYANG PHARMA UNIVERSITY
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Problems solved by technology
However, if the content of escitalopram is increased in the traditional transdermal drug delivery system, the initial release rate of the drug will be large, and the penetration rate will be very small due to dose failure after a long time
In addition, in order to control the release rate of escitalopram by adding polymers or using controlled-release membranes, the production process becomes complicated and difficult, the cost is higher, and there will be burst release in transdermal preparations. Phenomenon
Method used
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Embodiment 1
[0027] The preparation of embodiment 1 escitalopram free base
[0028] 2 g of escitalopram oxalate was dissolved in 20 ml of distilled water, and 4% (W / V) aqueous sodium hydroxide solution was added dropwise until no oily liquid was produced. Use 240ml of ethyl acetate to extract three times, combine the extracts, add an appropriate amount of anhydrous sodium sulfate for dehydration, and then dry by rotary evaporation to obtain escitalopram free base.
Embodiment 2
[0030] Dissolve 0.1 mol of escitalopram free base in 40 ml of acetone, add 0.1 mol of maleic acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain escitalopram benzoate ion-pair complex.
Embodiment 3
[0032] Dissolve 0.1 mol of escitalopram free base in 40 ml of acetone, add 0.1 mol of fumaric acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain escitalopram benzoate ion-pair complex.
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Abstract
The invention belongs to the technical field of medicine and relates to an escitalopram percutaneous patch and a preparation method thereof. The escitalopram percutaneous patch is composed of a backing layer, a medicine-carrying pressure-sensitive adhesive layer and an anti-sticking layer, the medicine-carrying pressure-sensitive adhesive layer comprises escitalopram free alkali or organic acid ion pair compound thereof, pressure-sensitive adhesive and percutaneous absorption promoter, the escitalopram free alkali or organic acid ion pair compound thereof accounts for 2.0-20wt% of total weight of the medicine-carrying pressure-sensitive adhesive layer, pressure-sensitive adhesive accounts for 77-97wt% of the total weight, the percutaneous absorption promoter accounts for 0-6.8wt% of the total weight, and in the escitalopram organic acid ion pair compound, a ratio of escitalopram free alkali and different organic acids is 0.5:1-2:1. Compared with an escitalopram organic acid ion pair compound percutaneous absorption patch and an escitalopram free alkali percutaneous absorption patch, the escitalopram percutaneous patch has the advantages that medicine release up to seven days and similar to constant rate can be provided, so that medication compliance of a patient is improved greatly.
Description
Technical field: [0001] The invention belongs to the technical field of medicine, and relates to an escitalopram transdermal patch and a preparation method thereof. Background technique: [0002] As the pace of life continues to accelerate, people's mental stress is also gradually increasing. Depression has become a common disease in modern society with a high incidence. Second largest disease. Depression is a syndrome with affective mental disorder as the main manifestation type and marked and persistent depression as the main feature. [0003] Currently antidepressant drugs are mainly divided into the following categories: monoamine oxidase inhibitors, tricyclic antidepressants, 5-HT reuptake inhibitors and norepinephrine reuptake inhibitors. Among them, the use of the first two has been limited due to their large side effects, while 5-HT reuptake inhibitors are the most widely used in clinical practice. There are five commonly used 5-HT reuptake inhibitors: fluoxetine,...
Claims
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IPC IPC(8): A61K47/48A61K9/70A61K31/343A61P25/24
Inventor 方亮宋田权鹏寸冬梅
Owner SHENYANG PHARMA UNIVERSITY
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