Tulobuterol transdermal patch and preparation method thereof

Abstract

The invention relates to a tulobuterol transdermal patch. A binder of the patch is formed by mixing a polyacrylate pressure-sensitive adhesive and a polyacrylic resin. The invention also relates to a preparation method of the tulobuterol patch. The preparation method is characterized by comprising the steps: drying a coated tulobuterol patch containing a supersaturated drug and a volatile solvent at a temperature higher than the melting point of the drug to remove the solvent, so as to obtain the tulobuterol transdermal patch with the active drug existing in a matrix in an amorphous form. The patch can significantly enhance the initial transdermal rate of the tulobuterol drug, and can maintain more than 24 hours of continuous approximate constant-speed transdermal drug delivery.

Description

technical field [0001] The invention relates to tulobuterol transdermal patch. The adhesive of the patch is composed of polyacrylate pressure-sensitive adhesive and polyacrylic resin. The invention also relates to a preparation method of the tulobuterol patch. The patch can significantly enhance the initial transdermal rate of tulobuterol, and can maintain a continuous approximately constant rate of transdermal administration for more than 24 hours. Background technique [0002] Tulobuterol is a selective agonist acting on sympathetic β2 receptors, clinically used to relieve symptoms such as dyspnea caused by bronchial asthma, acute bronchitis, chronic bronchitis, emphysema and other airway obstructive diseases. [0003] The known tulobuterol transdermal patch technology uses synthetic rubber-based adhesives or acrylate adhesives, the drug has a low drug loading in synthetic rubber-based adhesives and acrylate adhesives, and has the Poor skin permeability, unable to mainta...

AI Technical Summary

Problems solved by technology

[0003] The known tulobuterol transdermal patch technology uses synthetic rubber-based adhesives or acrylate adhesives, the drug has a low drug loading in synthetic rubber-based adhesives and acrylate adhesives, and has the Poor skin permeability, unable to maintain 24-hour transdermal administration and other issues

[0004] WO97 / 14411 describes that the synthetic rubber adhesive contains microcrystalline tulobuterol drug, which can achieve continuous administration for 24 hours, but the drug has a slow initial transdermal rate, poor stability of the microcrystalline drug, and easy crystallization. question

WO2005 / 067910 describes the use of a self-crosslinking acrylate adhesive system and a plasticizer of lipophilic oil to increase the loading of tulobuterol drug and enhance the skin permeability of the drug, but the technical process is more complicated, and Oily plasticizers can also cause skin irritation

WO2003 / 097022 patent describes a composition containing cationic polymers, solubilizers and absorption enhancers to enhance the transdermal penetration of drugs, but too much low molecular weight solubilizers and absorption enhancers will destroy the adhesiveness of the patch. Adherence

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