Patch preparation containing an acid scavenger

• US 10,639,374 B2
• Filed: 06/07/2018
• Issued: 05/05/2020
• Est. Priority Date: 08/29/2015
• Status: Active Grant

• Current Assignee: MedRx Co., Ltd.
• Original Assignee: MedRx Co., Ltd.
• Inventors: Hamamoto, Hidetoshi, Tanimoto, Takahiro
• Primary Examiner(s): Packard, Benjamin J
• Application Number:
  US16/002,913
• Publication Number:
  US 20180280513A1
• Time in Patent Office: 698 Days
• CPC Class Codes: A61K 31/433 Thidiazoles
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 9/7038 Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene

Abstract

An object of the present invention is to provide a patch preparation having an excellent skin permeability of medicament using an acid additional salt of basic medicament. Provided is a patch preparation comprising a support and an adhesive layer on one surface of the support, wherein the adhesive layer contains a basic medicament, a fatty acid-based ionic liquid, and potassium salts and/or potassium ions. Said potassium salts and/or potassium ions are generated as a result of reaction of an acid addition salt of the basic medicament with a compound capable of generating potassium ion in the adhesive layer.

Claims

1. A patch preparation comprising:

a support;

an adhesive layer on one surface of the support;

wherein the adhesive layer comprises a basic medicament, a fatty acid-based ionic liquid, and potassium salts and/or potassium ions, the basic medicament comprises tizanidine or an acid addition salt thereof, and the fatty acid-based ionic liquid is a salt of tizanidine and a fatty acid.

2. The patch preparation according to claim 1, wherein said potassium salts and/or potassium ions are generated as a result of reaction of an acid addition salt of the tizanidine with a compound capable of generating potassium ion in the adhesive layer.

3. The patch preparation according to claim 2, wherein the acid addition salt is selected from the group consisting of hydrochloride salt, sulfate salt, and salt of hydrobromic acid.

4. The patch preparation according to claim 1, wherein the potassium salt is potassium hydrochloride.

7. The patch preparation according to claim 1, wherein the basic medicament is tizanidine hydrochloride.

8. The patch preparation according to claim 1, wherein the fatty acid is oleic acid.

9. The patch preparation according to claim 1, wherein the potassium salts and/or potassium ions is potassium sorbate.

10. The patch preparation according to claim 1, wherein the adhesive layer comprises tizanidine hydrochloride, the fatty acid-based ionic liquid, and potassium sorbate, wherein the fatty acid-based ionic liquid is a salt of tizanidine and oleic acid.

5. A composition for a patch preparation comprising:

An acid addition salt of a basic medicament;

a fatty acid-based ionic liquid; and

a potassium ion generating compound, wherein the acid addition salt of the basic medicament is tizanidine hydrochloride and the fatty acid-based ionic liquid is a salt of tizanidine and a fatty acid.

6. The composition of claim 5, wherein the potassium ion generating compound is selected from the group consisting of potassium hydroxide, potassium citrate, potassium acetate, potassium tartrate, potassium lactate, potassium bicarbonate, potassium dihydrogen phosphate, dibasic potassium phosphate, tripotassium phosphate, potassium sorbate, potassium oleate, potassium levulinate, and a combination thereof.

11. The composition of claim 5, wherein the fatty acid is oleic acid.

12. The composition of claim 6, wherein the potassium ion generating compound is potassium sorbate.

13. A method for forming a patch preparation, comprising forming an adhesive composition by mixing an acid addition salt of a basic medicament, a fatty acid, and a potassium ion generating compound in a polymer solution for forming an adhesive layer, wherein the acid addition salt of the basic medicament is tizanidine hydrochloride.

14. The method of claim 13, wherein the fatty acid is a C_5-20 saturated or unsaturated fatty acid.

15. The method of claim 13, wherein the potassium ion generating compound is selected from the group consisting of potassium hydroxide, potassium citrate, potassium acetate, potassium tartrate, potassium lactate, potassium bicarbonate, potassium dihydrogen phosphate, dibasic potassium phosphate, tripotassium phosphate, potassium sorbate, potassium oleate, potassium levulinate, and a combination thereof.

16. The method of claim 13, wherein the fatty acid is oleic acid.

17. The method of claim 13, wherein the potassium ion generating compound is potassium sorbate.