Patch and method for producing the same

Patent metadata

Field	Value
Publication number	US-9511051-B2
Application number	US-201314417205-A
Country	US
Kind code	B2
Filing date	Jul 25, 2013
Priority date	Jul 26, 2012
Publication date	Dec 6, 2016
Grant date	Dec 6, 2016

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 D 50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 μm, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D 50 of 10 μm 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.

First claim

The invention claimed is:

1. A method for producing a patch, comprising:
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 in a range of 40 μm to 1000 μm, such that sodium diacetate having a particle diameter D50 of 10 μm or smaller is generated from the sodium acetate, thereby obtaining a mixture comprising the sodium diacetate and the asenapine or pharmaceutically acceptable salt;
obtaining an adhesive agent layer composition by mixing the mixture and a pressure-sensitive adhesive base agent, wherein acetic acid is not added; and
forming an adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt thereof, and the pressure-sensitive adhesive base agent, by applying the adhesive agent layer composition to a support layer,
wherein the adhesive agent layer measured by X-ray diffraction has a peak intensity from the sodium diacetate which is higher than a peak intensity from the sodium acetate.

2. The method for producing a patch according to claim 1 , wherein the mixing comprises mixing the pharmaceutically acceptable salt of asenapine with the sodium acetate, and the pharmaceutically acceptable salt is asenapine maleate.

3. The method for producing a patch according to claim 1 , wherein the adhesive agent layer composition further comprises isopropyl palmitate.

4. The method for producing a patch according to claim 3 , wherein a mass ratio of the asenapine or pharmaceutically acceptable salt to the isopropyl palmitate where a mass of the asenapine or pharmaceutically acceptable salt is in terms of free asenapine is in a range of 1:0.1 to 1:10.

5. A patch obtained by the method of claim 1 .

6. The method for producing a patch according to claim 2 , wherein the adhesive agent layer composition further comprises isopropyl palmitate.

7. A patch obtained by the method of claim 2 .

8. A patch obtained by the method to of claim 3 .

9. A patch obtained by the method of claim 6 .

10. The method for producing a patch according to claim 1 , wherein the mixing comprises grinding mixing the asenapine or pharmaceutically acceptable salt thereof with sodium acetate.

11. The method for producing a patch according to claim 1 , wherein the mixing comprises contact mixing the asenapine or pharmaceutically acceptable salt thereof with the sodium acetate.

12. The method for producing a patch according to claim 11 , wherein the contact mixing comprises mixing the asenapine or pharmaceutically acceptable salt thereof with the sodium acetate with a propeller mixer.

13. The method for producing a patch according to claim 1 , wherein the sodium acetate and the asenapine and/or pharmaceutically acceptable salt have a mixing ratio in a range of 1.5:1 to 6:1 where the mixing ratio is a number of moles of the sodium acetate to a total number of moles of the asenapine and pharmaceutically acceptable salt.

14. The method for producing a patch according to claim 1 , wherein the sodium acetate has a content of 10% or less relative to the adhesive agent layer.

15. The method for producing a patch according to claim 1 , wherein the sodium acetate has a content of 5% or less relative to the adhesive agent layer.

16. The method for producing a patch according to claim 1 , wherein the sodium diacetate has a content in a range of 0.3% to 10% or less relative to the adhesive agent layer.

17. The method for producing a patch according to claim 1 , wherein the sodium diacetate has a content in a range of 0.5% to 6% or less relative to the adhesive agent layer.

18. The method for producing a patch according to claim 13 , wherein the sodium diacetate has a content in a range of 0.3% to 10% or less relative to the adhesive agent layer.

19. The method for producing a patch according to claim 13 , wherein the sodium diacetate has a content in a range of 0.5% to 6% or less relative to the adhesive agent layer.

20. The method for producing a patch according to claim 13 , wherein the sodium diacetate has a content in a range of 0.3% to 10% or less relative to the adhesive agent layer, and the sodium acetate has a content of 10% or less relative to the adhesive agent layer.

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

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K31/55

  having seven-membered rings, e.g. azelastine, pentylenetetrazole · CPC title