Patch

Patent metadata

Field	Value
Publication number	US-9687474-B2
Application number	US-201314416964-A
Country	US
Kind code	B2
Filing date	Jul 25, 2013
Priority date	Jul 26, 2012
Publication date	Jun 27, 2017
Grant date	Jun 27, 2017

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.

First claim

The invention claimed is:

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 2-120 for a period starting from the time when the patch is brought into contact with skin for 24 hours is 27,000 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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 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 pg·hr/mL or more, and an AUC 2-120 of an asenapine metabolite is 20% or less of the AUC 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.

Assignees

• Hisamitsu Pharmaceutical Co

Inventors

• Suzuki Masayuki
• Okutsu Hiroaki
• Yasukochi Takashi
• Takada Yasunori

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61M37/00

  Other apparatus for introducing media into the body (for reproduction or fertilisation A61B17/425; apparatus for iontophoresis or cataphoresis A61N1/30); Percutany, i.e. introducing medicines into the body by diffusion through the skin (salt baths A61H33/04) · CPC title

• A61K9/70

  Web, sheet or filament bases {; Films; Fibres of the matrix type containing drug (hollow drug-filled fibres A61K9/0092)} · CPC title