TRANSDERMAL THERAPEUTIC SYSTEM CONTAINING ASENAPINE Russian patent published in 2023 - IPC A61K9/70 A61K31/407 A61K47/14 A61K47/22 A61K47/58 A61P25/18 

FIELD: medicine.

SUBSTANCE: group of inventions refers to a transdermal therapeutic system for transdermal administration of asenapine which includes a self-adhesive layer structure containing a therapeutically effective amount of asenapine, while the said self-adhesive layer structure contains the following: A) substrate; B) an asenapine-containing matrix layer, consisting of a matrix layer composition that contains the following: 1) asenapine included in free base form; 2) a polymer selected from acrylic polymers, wherein the polymer is a copolymer based on vinyl acetate, 2-ethylhexyl acrylate, 2-hydroxyethyl acrylate and glycidyl methacrylate or a copolymer based on vinyl acetate, 2-ethylhexyl acrylate and 2-hydroxyethyl acrylate; 3) an additional polymer selected from polyvinylpyrrolidones; and 4)α-tocopherol in an amount of 0.01 to 2 wt.% of the composition of the matrix layer and ascorbyl palmitate in an amount of at least 0.01 wt.% of the composition of the matrix layer, as stabilizers, also refers to a method of treating one or more of the following conditions: schizophrenia, bipolar disorder, post-traumatic stress disorder, major depressive disorder, dementia-related psychosis, anxiety and manic disorder, including the use of a transdermal therapeutic system on the skin of a patient and also relates to a method for producing a matrix layer for use in a transdermal therapeutic system, comprising the following steps: 1) combining in a solvent at least such components as asenapine included in the form of a free base, a copolymer based on vinyl acetate, 2-ethylhexyl acrylate, 2-hydroxyethyl acrylate and glycidyl methacrylate or a copolymer based on vinyl acetate, 2-ethylhexyl acrylate and 2-hydroxyethyl acrylate, an additional polymer, selected from polyvinylpyrrolidones, α-tocopherol and ascorbyl palmitate to form a coating composition; 2) applying the coating composition to a substrate or release substrate or any intermediate substrate; and 3) drying the applied coating composition to form a matrix layer.

EFFECT: group of inventions provides a transdermal therapeutic system of asenapine with improved stability and at the same time provides a penetration rate sufficient to achieve a therapeutically effective dose.

20 cl, 80 tbl, 44 dwg