Claims for Patent: 9,687,474

Summary for Patent: 9,687,474

Title:	Patch
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.
Inventor(s):	Suzuki; Masayuki (Tsukuba, JP), Okutsu; Hiroaki (Tsukuba, JP), Yasukochi; Takashi (Tsukuba, JP), Takada; Yasunori (Tsukuba, JP)
Assignee:	HISAMITSU PHARMACEUTICAL CO., INC. (Tosu-shi, JP)
Application Number:	14/416,964
Patent Claims:	1. A patch, comprising: a support layer; and an adhesive agent layer formed on the support layer and comprising isopropyl palmitate, an adhesive base agent, sodium diacetate, and at least one of asenapine and a pharmaceutically acceptable salt thereof, wherein a mass ratio of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine to the isopropyl palmitate in the adhesive agent layer is in a range of 1:0.1 to 1:5. 2. The patch according to claim 1, wherein a mass ratio of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine to the isopropyl palmitate in the adhesive agent layer is in a range of 1:0.41 to 1:5. 3. The patch according to claim 1, wherein a mole ratio of the asenapine and/or pharmaceutically acceptable salt to the sodium diacetate in the adhesive agent layer is in a range of 1:0.5 to 1:4. 4. The patch according to claim 1, wherein the adhesive base agent is at least one selected from the group consisting of a (meth)acrylic ester (co)polymer, a rubber-based adhesive agent, a silicone polymer, and a polyurethane-based adhesive agent. 5. The patch according to claim 1, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 6. The patch according to claim 2, wherein a mole ratio of the asenapine and/or pharmaceutically acceptable salt to the sodium diacetate in the adhesive agent layer is in a range of 1:0.5 to 1:4. 7. The patch according to claim 2, wherein the adhesive base agent is at least one selected from the group consisting of a (meth)acrylic ester (co)polymer, a rubber-based adhesive agent, a silicone polymer, and a polyurethane-based adhesive agent. 8. The patch according to claim 2, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 9. The patch according to claim 3, wherein the adhesive base agent is at least one selected from the group consisting of a (meth)acrylic ester (co)polymer, a rubber-based adhesive agent, a silicone polymer, and a polyurethane-based adhesive agent. 10. The patch according to claim 3, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 11. The patch according to claim 4, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 12. The patch according to claim 7, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 13. The patch according to claim 6, wherein the adhesive base agent is at least one selected from the group consisting of a (meth)acrylic ester (co)polymer, a rubber-based adhesive agent, a silicone polymer, and a polyurethane-based adhesive agent. 14. The patch according to claim 6, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 15. The patch according to claim 13, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 16. The patch according to claim 9, wherein when a content of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC.sub.2-120 of the free asenapine for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pghr/mL or more, and an AUC.sub.2-120 of an asenapine metabolite is 20% or less of the AUC.sub.2-120 of the free asenapine. 17. The patch according to claim 3, wherein a mass ratio of the asenapine and/or pharmaceutically acceptable salt in terms of free asenapine to the isopropyl palmitate in the adhesive agent layer is in a range of 1:0.5 to 1:5.