Rivastigmine long-acting percutaneous absorption patch and preparation method thereof
An absorption enhancer, long-acting technology, applied in the field of medicine, can solve problems such as complex patch structure, achieve low cost, easy to use, and increase the effect of high release
Pending Publication Date: 2022-04-12
SHENYANG PHARMA UNIVERSITY
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- Claims
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AI Technical Summary
Problems solved by technology
The patch of this patent still needs to use a controlled-release film to control the release of rivastigmine, the patch structure is relatively complex, and the anti-oxidant DL-α-tocopherol needs to be added to the drug-containing pressure-sensitive adhesive layer
Method used
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Experimental program
Comparison scheme
Effect test
Embodiment 1
[0044] Dissolve 0.1 mol of rivastigmine free base in 100 ml of acetone, add 0.1 mol of n-butyric acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain rivastigmine n-butyrate ionic liquid.
Embodiment 2
[0046] Dissolve 0.1 mol of rivastigmine free base in 100 ml of acetone, add 0.1 mol of n-octanoic acid under stirring, continue to stir for 2 hours, and rotatively evaporate to dry the solvent to obtain n-octanoic acid rivastigmine ionic liquid.
Embodiment 3
[0048] Dissolve 0.1 mol of rivastigmine free base in 100 ml of acetone, add 0.1 mol of lauric acid under stirring, continue stirring for 2 hours, and dry the solvent by rotary evaporation to obtain rivastigmine lauric acid ionic liquid.
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The invention relates to a rivastigmine long-acting percutaneous absorption patch, and belongs to the technical field of medicines. The percutaneous absorption patch is suitable for being applied for at least three days, and the patch is composed of a backing layer, a medicine-carrying pressure-sensitive adhesive layer and an anti-sticking layer. The drug-loading pressure-sensitive adhesive layer comprises rivastigmine free alkali or organic acid ionic liquid thereof, a pressure-sensitive adhesive and a percutaneous absorption enhancer. Wherein the weight of the rivastigmine free alkali or the organic acid ionic liquid of the rivastigmine free alkali accounts for 5-45wt% of the total weight of the drug-loaded pressure-sensitive adhesive layer, the weight of the pressure-sensitive adhesive accounts for 50-90wt% of the total weight of the pressure-sensitive adhesive layer, and the dosage of the percutaneous absorption enhancer accounts for 1-20wt% of the total weight of the pressure-sensitive adhesive layer. Wherein in the rivastigmine organic acid ionic liquid, the molar ratio of rivastigmine free alkali to different organic acids is (0.5: 1)-(2: 1). In the patch provided by the invention, the cumulative permeation amount of rivastigmine within 72 hours can reach 2.8 mg / cm < 2 >. The patch is simple in preparation technology, low in cost, capable of releasing medicine at constant speed, safe, effective, good in stability and convenient to use.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a rivastigmine long-acting percutaneous absorption patch, a preparation method thereof and an application thereof. Background technique [0002] Alzheimer's disease is a progressive, irreversible neurodegenerative disease and the most common cause of progressive mental decline in people over the age of 65. Alzheimer's disease is characterized by three main groups of symptoms: cognitive dysfunction, psychiatric symptoms and behavioral disturbances, and deterioration of activities of daily living and behavior. These deficits develop over time and are often accompanied by behavioral disturbances such as aggression, depression, confusion, and wandering. In 2018, the global prevalence of Alzheimer's disease was 50 million, and the global economic loss was close to US$1 trillion. The Population Division of the United Nations predicts that by 2050, the population over the...
Claims
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Patent Timeline
Login to View More IPC IPC(8): A61K9/70A61K31/27A61K47/32A61P25/28
Inventor 方亮权鹏刘超才煜
Owner SHENYANG PHARMA UNIVERSITY
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