Rotigotine percutaneous absorption patch, and preparation and application thereof
An absorption enhancer and patch technology, applied in the field of medicine, can solve the problems of poor compatibility between drugs and pressure-sensitive adhesives, poor compatibility between drugs and substrates, inaccurate doses, etc., so as to improve transdermal penetration. ability, preventing the risk of crystallization, and improving the effect of drug loading
Active Publication Date: 2020-01-03
SHENYANG PHARMA UNIVERSITY
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- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Poor compatibility between drug and matrix can lead to crystallization of drug molecules and inaccurate dosing
The main reason for the crystallization of the drug in the patch is the poor compatibility of the drug with the pressure-sensit...
Method used
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Effect test
Embodiment 1
[0039] Dissolve 0.1 mol of rotigotine free base in 40 ml of acetone, add 0.1 mol of benzoic acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain rotigotine benzoate ionic liquid.
Embodiment 2
[0041] Dissolve 0.1 mol of rotigotine free base in 40 ml of acetone, add 0.1 mol of oleic acid under stirring, continue to stir for 2 hours, and spin evaporate to dry the solvent to obtain rotigotine oleic acid ionic liquid.
Embodiment 3
[0043] Dissolve 0.1 mol of rotigotine free base in 40 ml of acetone, add 0.1 mol of lactic acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain rotigotine lactate ionic liquid.
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The invention belongs to the technical field of medicine, and relates to a rotigotine percutaneous absorption patch, and preparation and application thereof. The patch can obviously relieve a crystalseparation phenomenon of a rotigotine patch and provides good skin penetration delivery performance. The rotigotine percutaneous absorption patch consists of a back lining layer, a medicine loaded pressure-sensitive adhesive layer and an anti-bonding layer, wherein the medicine loaded pressure-sensitive adhesive layer comprises rotigotine free alkali or rotigotine organic acid ionic liquid, pressure-sensitive adhesives and a percutaneous absorption enhancing agent, wherein the weight of the rotigotine free alkali or rotigotine organic acid ionic liquid accounts for 2.0 to 20 weight percent ofthe total weight of the medicine loaded pressure-sensitive adhesive layer; the weight of the pressure-sensitive adhesives accounts for 77 to 90 weight percent of the total weight of the pressure-sensitive adhesive layer; and the consumption of the percutaneous absorption enhancing agent accounts for 0 to 10 weight percent of the total weight of the pressure-sensitive adhesive layer. In the rotigotine organic acid ionic liquid, a mol ratio of the rotigotine free alkali to different organic acids is 0.5:1-2:1. The rotigotine percutaneous absorption patch has the advantages that the accumulated penetration amount of rotigotine in 24h can reach 0.5mg/cm<2>. The preparation technology of the patch is simple; the stability of the patch is high; and the use is convenient.
Description
Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a rotigotine percutaneous absorption patch and its preparation and application. The patch can significantly improve the crystallization phenomenon of the rotigotine patch and provide good skin penetration performance. Background technique: [0002] Parkinson's disease, also known as Parkinson's paralysis, is one of the most common central nervous system degenerative diseases in middle-aged and elderly people. It is a chronic central nervous system neurodegenerative disease caused by extrapyramidal system dysfunction. Typical symptoms include motor symptoms such as resting tremor, muscle stiffness, slowness of movement, abnormal posture and gait, and non-motor symptoms such as anxiety and depression, smell disturbance, sleep disturbance, numbness and pain. According to statistics, there are more than 10 million Parkinson's disease patients in the world, and nearly 3 million of th...
Claims
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Patent Timeline
Login to view more IPC IPC(8): A61K9/70A61K47/32A61K31/381A61P25/16
CPCA61K9/7053A61K31/381A61P25/16
Inventor 方亮刘超权鹏曲鑫
Owner SHENYANG PHARMA UNIVERSITY
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