Composition for patch preparation comprising drug, organic solvent, lipophilic mass base, and powder

Patent metadata

Field	Value
Publication number	US-12016924-B2
Application number	US-201916564587-A
Country	US
Kind code	B2
Filing date	Sep 9, 2019
Priority date	Jun 20, 2012
Publication date	Jun 25, 2024
Grant date	Jun 25, 2024

Abstract

A non-aqueous patch preparation may include a drug solution in which a drug is dissolved in an organic solvent, a lipophilic mass base, and anhydrous silicic acid powders that are insoluble both in the organic solvent and in the lipophilic mass base. The organic solvent is selected from the group consisting of propylene glycol, 1,3-butanediol, polyethylene glycol, and propylene carbonate. The lipophilic mass base comprises an elastomer, a tackifier, and a softening agent wherein the elastomer is styrene-isoprene-styrene copolymer (SIS). The patch preparation has 2% to 10% by weight of the anhydrous silicic acid powders.

First claim

The invention claimed is:

1. A non-aqueous patch preparation comprising
a drug solution in which a drug is dissolved in an organic solvent, wherein the organic solvent further comprises an ionic liquid,
a lipophilic mass base, and
anhydrous silicic acid powders that are insoluble both in the organic solvent and in the lipophilic mass base,
wherein the drug solution is retained in spaces between the powders or in spaces between the powders and the lipophilic mass base,
the organic solvent is selected from the group consisting of propylene glycol, 1,3-butanediol, polyethylene glycol, and propylene carbonate,
the lipophilic mass base comprises styrene-isoprene-styrene (SIS) copolymer, a tackifier, and a softening agent, and
the patch preparation has 2% to 10% by weight of the anhydrous silicic acid powders,
wherein the non-aqueous patch preparation exhibits at least 30% higher skin permeability than a skin permeability exhibited by an identical non-aqueous patch preparation without the anhydrous silicic acid powders.

2. A non-aqueous patch preparation comprising
a drug solution in which a drug is dissolved in an organic solvent, wherein the organic solvent further comprises an ionic liquid,
a lipophilic mass base, wherein the drug or the drug solution is insoluble in the lipophilic mass base, and
anhydrous silicic acid powders that are insoluble both in the organic solvent and in the lipophilic mass base,
wherein the organic solvent is selected from the group consisting of propylene glycol, 1,3-butanediol, polyethylene glycol, and propylene carbonate,
the lipophilic mass base comprises styrene-isoprene-styrene (SIS) copolymer, a tackifier, and a softening agent, and
the patch preparation has 2% to 10% by weight of the anhydrous silicic acid powders,
wherein the non-aqueous patch preparation exhibits at least 30% higher skin permeability than a skin permeability exhibited by an identical non-aqueous patch preparation without the anhydrous silicic acid powders.

3. The patch preparation according to claim 1 , wherein the tackifier is selected from the group consisting of a SIS resin, a polyterpene resin, a polyolefin resin, a polystyrene resin, an aromatic petroleum resin, rosin, and hydrogenated rosin.

4. The patch preparation according to claim 1 , wherein the softening agent is selected from the group consisting of petroleum-based softening agents; fatty oil-based softening agents; purified lanolin; and liquid paraffin.

5. The patch preparation according to claim 2 , wherein the tackifier is selected from the group consisting of a SIS resin, a polyterpene resin, a polyolefin resin, a polystyrene resin, an aromatic petroleum resin, rosin, and hydrogenated rosin.

6. The patch preparation according to claim 2 , wherein the softening agent is selected from the group consisting of petroleum-based softening agents; fatty oil-based softening agents; purified lanolin; and liquid paraffin.

7. The patch preparation according to claim 1 , wherein the organic solvent is selected from the group consisting of 1,3-butanediol, polyethylene glycol, and propylene carbonate.

8. The patch preparation according to claim 2 , wherein the organic solvent is selected from the group consisting of 1,3-butanediol, polyethylene glycol, and propylene carbonate.

9. The patch preparation according to claim 1 , wherein the anhydrous silicic acid powders are in a range from 2% to 6% by weight.

10. The patch preparation according to claim 2 , wherein the anhydrous silicic acid powders are in a range from 2% to 6% by weight.

11. The patch preparation according to claim 1 , wherein the SIS copolymer is in a range from 10% to 45% by weight.

12. The patch preparation according to claim 2 , wherein the SIS copolymer is in a range from 10% to 45% by weight.

13. The patch preparation according to claim 1 , wherein the non-aqueous patch preparation has the SIS copolymer at a concentration of 20% by weight.

14. A non-aqueous patch preparation comprising
a drug solution in which a drug is dissolved in an organic solvent, wherein the organic solvent further comprises an ionic liquid,
a lipophilic mass base, and
anhydrous silicic acid powders that are insoluble both in the organic solvent and in the lipophilic mass base,
wherein the drug solution is retained in spaces between the powders or in spaces between the powders and the lipophilic mass base,
the organic solvent is selected from the group consisting of propylene glycol, 1,3-butanediol, polyethylene glycol, and propylene carbonate,
the lipophilic mass base comprises styrene-isoprene-styrene (SIS) copolymer, a tackifier, and a softening agent, and
the patch preparation has 2% to 10% by weight of the anhydrous silicic acid powders,
wherein the non-aqueous patch preparation exhibits at least 3 times the transdermal absorbability than a transdermal absorbability exhibited by an identical non-aqueous patch preparation without the anhydrous silicic acid powders.

15. The patch preparation according to claim 14 , wherein the softening agent is selected from the group consisting of petroleum-based softening agents; fatty oil-based softening agents; purified lanolin; and liquid paraffin.

16. The patch preparation according to claim 14 , wherein the softening agent is selected from the group consisting of petroleum-based softening agents; fatty oil-based softening agents; purified lanolin; and liquid paraffin.

17. The patch preparation according to claim 14 , wherein the organic solvent is selected from the group consisting of 1,3-butanediol, polyethylene glycol, and propylene carbonate.

18. The patch preparation according to claim 14 , wherein the anhydrous silicic acid powders are in a range from 2% to 6% by weight.

19. The patch preparation according to claim 14 , wherein the drug comprises a basic drug.

20. The non-aqueous patch preparation of claim 1 , wherein the patch preparation comprises an organic carboxylic acid.

21. The non-aqueous patch preparation of claim 2 , wherein the patch preparation comprises an organic carboxylic acid.

22. The non-aqueous patch preparation of claim 14 , wherein the patch preparation comprises an organic carboxylic acid.

Assignees

• Medrx Co Ltd

Inventors

• Hamamoto Hidetoshi
• Yamanaka Katsuhiro
• Tanimoto Takahiro

Classifications

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title

• A61K38/23

  Calcitonins · CPC title

• A61K31/485

  Morphinan derivatives, e.g. morphine, codeine · CPC title

• A61K31/407

  condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine · CPC title