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A kind of rotigotine percutaneous absorption patch and its preparation and application

An absorption enhancer and patch technology, applied in the field of medicine, can solve problems such as inaccurate dosage, poor compatibility of drugs and pressure-sensitive adhesives, crystallization of drug molecules, etc.

Active Publication Date: 2022-04-19
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • 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-sensitive adhesive.
[0007] Therefore, need to seek a kind of preparation method, thereby overcome the problem of crystallization of rotigotine percutaneous absorption patch, make rotigotine percutaneous absorption patch be better applied to clinical

Method used

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  • A kind of rotigotine percutaneous absorption patch and its preparation and application
  • A kind of rotigotine percutaneous absorption patch and its preparation and application
  • A kind of rotigotine percutaneous absorption patch and its preparation and application

Examples

Experimental program
Comparison scheme
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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PUM

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Abstract

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. The rotigotine percutaneous absorption patch of the present invention is composed of a backing layer, a drug-loaded pressure-sensitive adhesive layer and a release layer; the drug-loaded pressure-sensitive adhesive layer includes rotigotine free base or its organic acid ionic liquid , Pressure sensitive adhesive, transdermal absorption enhancer. Wherein the weight of rotigotine free base or its organic acid ionic liquid accounts for 2.0-20wt% of the total weight of the drug-loaded pressure-sensitive adhesive layer, and the pressure-sensitive adhesive accounts for 77-90wt% of the total weight of the pressure-sensitive adhesive layer, and the percutaneous absorption is promoted The dosage of the agent accounts for 0-10wt% of the total weight of the pressure-sensitive adhesive layer. Wherein in the rotigotine organic acid ionic liquid, the molar ratio of rotigotine free base to different organic acids is 0.5:1-2:1. In the patch of the present invention, the cumulative permeation amount of rotigotine in 24 hours can reach 0.5 mg / cm 2 . The preparation technology of the patch is simple, the stability of the patch is good, 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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Application Information

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Patent Type & Authority Patents(China)
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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