Patch preparation containing an acid scavenger

• US 10,016,502 B2
• Filed: 09/28/2016
• Issued: 07/10/2018
• 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:
  US15/279,272
• Publication Number:
  US 20170056503A1
• Time in Patent Office: 650 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 oxycodone, a fatty acid-based ionic liquid, and potassium salts and/or potassium ions; and

a molar ratio of the fatty acid-based ionic liquid to the oxycodone is between about 0.4 to about 5.

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 oxycodone 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.

5. The patch preparation according to claim 1, wherein the fatty acid-based ionic liquid is selected from the group consisting of oleic acid-diisopropanolamine, levulinic acid-diisopropanolamine, sorbic acid-diisopropanolamine, and a combination thereof.

6. A composition for a patch preparation comprising:

An acid addition salt of a oxycodone;

a fatty acid-based ionic liquid;

a potassium ion generating compound; and

wherein a molar ratio of the fatty acid-based ionic liquid to the oxycodone is between about 0.4 to about 5.

7. The composition of claim 6, wherein the fatty acid-based ionic liquid is selected from the group consisting of oleic acid-diisopropanolamine, levulinic acid-diisopropanolamine, sorbic acid-diisopropanolamine, and a combination thereof.

8. The composition of claim 6, 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.

9. A method for forming a patch, comprising:

providing an acid addition salt of a oxycodone;

providing a fatty acid and an organic amine compound for forming a fatty acid-based ionic liquid;

providing a potassium ion generating compound;

forming an adhesive composition by mixing the acid addition salt of oxycodone, the fatty acid, the organic amine, and the potassium ion generating compound in a polymer solution for forming an adhesive layer, wherein a molar ratio of the fatty acid-based ionic liquid to the oxycodone is between about 0.4 to about 5.

10. The method of claim 9, wherein the fatty acid and the organic amine compound are mixed to form the fatty acid-based ionic liquid prior to mixing with the acid addition salt of oxycodone and the potassium ion generating compound.

11. The method of claim 9, further comprising forming a potassium salt and the oxycodone in the adhesive composition by reacting the potassium generating compound with the acid addition salt of oxycodone.

12. The method of claim 9, wherein the fatty acid is a C_5-20 saturated or unsaturated fatty acid.

13. The method of claim 9, wherein the organic amine compound is a C_4-9 alkanolamine.

14. The method of claim 9, 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.