Abstract: A method for suppressing a plasma concentration of an asenapine metabolite includes applying to a subject a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer includes asenapine and/or a pharmaceutically acceptable salt thereof, and an adhesive base agent.

Abstract: A method for producing a patch including a support layer, and an adhesive agent layer formed on the support layer and including sodium diacetate, a pressure-sensitive adhesive base agent, and asenapine and/or a pharmaceutically acceptable salt thereof. The sodium diacetate is generated from sodium acetate in the presence of the asenapine and/or salt thereof, a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is in range of 3.0 to 20 mg, and when a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is 6.4 mg and the patch is in contact with skin for 24 hours, Cmax of free asenapine is in range of 0.5 to 6.0 ng/mL and tmax of free asenapine is in range of 8 to 28 hr.

Abstract: A patch for administering asenapine includes a support layer, and an adhesive agent layer formed on the support layer and including an adhesive base agent and asenapine and/or a pharmaceutically acceptable salt thereof. The adhesive base agent has a content in a range of 10 to 90% by mass in the adhesive agent layer and includes a natural rubber, polyisobutylene, an alkyl vinyl ether(co)polymer, polyisoprene, polybutadiene, a styrene-butadiene copolymer, a styrene-isoprene copolymer, a styrene-isoprene-styrene block copolymer, or a combination thereof. When a content of the asenapine and/or pharmaceutically acceptable salt thereof in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC2-120 for a period starting from the time when the patch is brought into contact with a skin for 24 hours is 27,000 pg·hr/mL or more, and an AUC2-120 of an asenapine metabolite is 20% or less of the AUC2-120 of the free asenapine.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.

Abstract: A method for suppressing a plasma concentration of an asenapine metabolite includes applying to a subject a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer includes asenapine and/or a pharmaceutically acceptable salt thereof, and an adhesive base agent.

Abstract: A method for producing a patch including a support layer, and an adhesive agent layer formed on the support layer and including sodium diacetate, a pressure-sensitive adhesive base agent, and asenapine and/or a pharmaceutically acceptable salt thereof. The sodium diacetate is generated from sodium acetate in the presence of the asenapine and/or salt thereof, a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is in range of 3.0 to 20 mg, and when a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is 6.4 mg and the patch is in contact with skin for 24 hours, Cmax of free asenapine is in range of 0.5 to 6.0 ng/mL and tmax of free asenapine is in range of 8 to 28 hr.

Abstract: In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises asenapine and/or a pharmaceutically acceptable salt thereof, isopropyl palmitate, and an adhesive base agent.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.

Abstract: In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises asenapine and/or a pharmaceutically acceptable salt thereof, isopropyl palmitate, and an adhesive base agent.

Abstract: A patch for administering asenapine includes a support layer, and an adhesive agent layer formed on the support layer and including an adhesive base agent and asenapine and/or a pharmaceutically acceptable salt thereof. The adhesive base agent has a content in a range of 10 to 90% by mass in the adhesive agent layer and includes a natural rubber, polyisobutylene, an alkyl vinyl ether(co)polymer, polyisoprene, polybutadiene, a styrene-butadiene copolymer, a styrene-isoprene copolymer, a styrene-isoprene-styrene block copolymer, or a combination thereof. When a content of the asenapine and/or pharmaceutically acceptable salt thereof in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC2-120 for a period starting from the time when the patch is brought into contact with a skin for 24 hours is 27,000 pg·hr/mL or more, and an AUC2-120 of an asenapine metabolite is 20% or less of the AUC2-120 of the free asenapine.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.

Abstract: In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises asenapine and/or a pharmaceutically acceptable salt thereof, isopropyl palmitate, and an adhesive base agent.

Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 ?m, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 ?m or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.