Ropinirole-containing patch and package thereof

Patent metadata

Field	Value
Publication number	US-9918945-B2
Application number	US-201214123148-A
Country	US
Kind code	B2
Filing date	May 23, 2012
Priority date	May 31, 2011
Publication date	Mar 20, 2018
Grant date	Mar 20, 2018

Abstract

A ropinirole-containing patch comprises an adhesive agent layer and a support layer, the adhesive agent layer containing ropinirole and/or a pharmaceutically acceptable salt thereof, wherein a content of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer satisfies the following two conditions:
5 to 13.2% by mass relative to a total mass of the adhesive agent layer, and 0.12 to 2.7 mg/cm 2 per unit area of the adhesive agent layer.

First claim

The invention claimed is:

1. A ropinirole-containing patch, comprising:
a support layer; and
an adhesive agent layer formed on the support layer and comprising sodium hydroxide and ropinirole and/or a pharmaceutically acceptable salt thereof such that the adhesive agent layer comprises 0.5 to 1.0 mol of the sodium hydroxide per 1 mol of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole,
wherein a content of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer satisfies 8.8 to 13.2% by mass relative to a total mass of the adhesive agent layer, and 0.12 to 2.7 mg/cm 2 per unit area of the adhesive agent layer, the adhesive agent layer has a mass per unit area of 50 to 200 g/m 2 , said adhesive agent layer further comprises a rubber-based adhesive, a tackifier, and a plasticizer, and said adhesive layer has an area of application surface ranging from 3 to 100 cm 2 suitable for treating Parkinson's disease and attains a ropinirole concentration in plasma of 500 to 18000 pg/ml.

2. The ropinirole-containing patch according to claim 1 , wherein the adhesive agent layer has a mass per unit area of 50 to 150 g/m 2 .

3. The ropinirole-containing patch according to claim 1 , wherein the adhesive agent layer further comprises 5 to 50 parts by mass of at least one compound selected from the group consisting of benzyl alcohol, oleyl alcohol, octyldodecanol, and dimethyl isosorbide, per 100 parts by mass of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

4. The ropinirole-containing patch according to claim 1 , wherein the adhesive agent layer further comprises 10 to 150 parts by mass of at least one compound selected from the group consisting of isopropyl myristate, isopropyl palmitate, lauryl alcohol, glycerol monooleate, propylene glycol monolaurate, polyoxyethylene sorbitan monooleate, and lauric acid diethanolamide, per 100 parts by mass of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

5. The ropinirole-containing patch according to claim 1 , wherein the adhesive agent layer comprises 15 to 35% by mass of said rubber-based adhesive relative to the total mass of the adhesive agent layer.

6. The ropinirole-containing patch according to claim 1 , wherein the adhesive agent layer comprises 0.6 to 1.0 mol of the sodium hydroxide per 1 mol of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

7. The ropinirole-containing patch according to claim 1 , wherein the rubber-based adhesive in the adhesive agent layer comprises a synthetic rubber free of a hydroxyl group and a carboxyl group.

8. The ropinirole-containing patch according to claim 1 , wherein the rubber-based adhesive in the adhesive agent layer comprises a styrene-isoprene-styrene block copolymer.

9. A ropinirole-containing patch, comprising:
a support layer; and
an adhesive agent layer formed on the support layer and comprising sodium hydroxide and ropinirole and/or a pharmaceutically acceptable salt thereof such that the adhesive agent layer comprises 0.5 to 1.0 mol of the sodium hydroxide per 1 mol of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole,
wherein a content of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer satisfies 8.8 to 13.2% by mass relative to a total mass of the adhesive agent layer, and 0.12 to 2.7 mg/cm 2 per unit area of the adhesive agent layer, the adhesive agent layer has a mass per unit area of 50 to 200 g/m 2 , said adhesive agent layer further comprises a rubber-based adhesive, a tackifier, and a plasticizer, and said adhesive layer has an area of application surface ranging from 0.5 to 30 cm 2 suitable for treating restless legs syndrome and attains a ropinirole concentration in plasma of 125 to 4500 pg/ml.

10. The ropinirole-containing patch according to claim 9 , wherein the adhesive agent layer has a mass per unit area of 50 to 150 g/m 2 .

11. The ropinirole-containing patch according to claim 9 , wherein the adhesive agent layer further comprises 5 to 50 parts by mass of at least one compound selected from the group consisting of benzyl alcohol, oleyl alcohol, octyldodecanol, and dimethyl isosorbide, per 100 parts by mass of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

12. The ropinirole-containing patch according to claim 9 , wherein the adhesive agent layer further comprises 10 to 150 parts by mass of at least one compound selected from the group consisting of isopropyl myristate, isopropyl palmitate, lauryl alcohol, glycerol monooleate, propylene glycol monolaurate, polyoxyethylene sorbitan monooleate, and lauric acid diethanolamide, per 100 parts by mass of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

13. The ropinirole-containing patch according to claim 9 , wherein the adhesive agent layer comprises 15 to 35% by mass of said rubber-based adhesive relative to the total mass of the adhesive agent layer.

14. The ropinirole-containing patch according to claim 9 , wherein the adhesive agent layer further comprises 0.6 to 1.0 mol of the sodium hydroxide per 1 mol of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole.

15. The ropinirole-containing patch according to claim 9 , wherein the rubber-based adhesive in the adhesive agent layer comprises a synthetic rubber free of a hydroxyl group and a carboxyl group.

16. The ropinirole-containing patch according to claim 9 , wherein the rubber-based adhesive in the adhesive agent layer comprises a styrene-isoprene-styrene block copolymer.

17. A package, comprising the ropinirole-containing patch according to claim 1 and a deoxidizer together sealed in a packaging bag.

18. A package, comprising the ropinirole-containing patch according to claim 9 and a deoxidizes together sealed in a packaging bag.

19. A method for treating Parkinson's disease, comprising:
administering the ropinirole-containing patch of claim 1 to a patient in need thereof, such that a ropinirole concentration in plasma is 500 to 18000 pg/ml.

20. A method for treating restless legs syndrome, comprising:
administering the ropinirole-containing patch of claim 4 to a patient in need thereof, such that a ropinirole concentration in plasma is 125 to 4500 pg/ml.

Assignees

• Uchida Naoyuki
• Takagi Yuka
• Yamaguchi Toshiro
• Hisamitsu Pharmaceutical Co

Inventors

• Uchida Naoyuki
• Takagi Yuka
• Yamaguchi Toshiro

Classifications

• A61K31/4045

  Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin · CPC title

• A61K9/7053 Primary

  obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61K47/14

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