Hydrogel composition for transdermal drug delivery

• US 20030170295A1
• Filed: 11/15/2002
• Published: 09/11/2003
• Est. Priority Date: 05/16/2000
• Status: Abandoned Application

• Current Assignee: Samyang Corporation (Samyang Holdings Corporation)
• Original Assignee: Samyang Corporation (Samyang Holdings Corporation)
• Inventors: Kim, Ho-Jin, Yoon, Hye-Jeong
• Application Number:
  US10/276,498
• Publication Number:
  US 20030170295A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to a hydrogel composition for transdermal drug delivery, more specifically to a hydrogel composition for transdermal drug delivery containing acrylate polymers like acrylic acid polymer, methacrylic acid polymer, alkyl acrylate polymer, alkyl methacrylate polymer or copolymers thereof as compatibilizers which enable both hydrophilic and lipophilic permeation enhancers to be applicable in the hydrogel composition in order to effectively control skin penetration of drugs.

Claims

1. A transdermal drug delivery composition comprising a hydrophilic polymer base, a drug, a lipophilic permeation enhancer and a compatibilizer consisting essentially of an acrylate polymer which compatibilizes said lipophilic enhancer with said hydrophilic polymer base and which renders said composition thermodynamically stable.

2. The composition according to claim 1, wherein said acrylate polymer is within the range of 0.1-10 wt. % based on the entire composition.

3. The composition according to claim 2, wherein said acrylate polymer is included in the range of 2-8 wt. % to the entire composition.

4. The composition according to claim 1, wherein said acrylate polymer is a copolymer comprising a 1:

2 ratio of methyl methacrylate and ethyl acrylate expressed by the following Formula (1a),

5. The composition according to claim 1, wherein said acrylate polymer is a copolymer comprising a 1:

1 ratio of methacrylic acid and ethyl acrylate expressed by the following Formula (1b),

6. The composition according to claim 1, wherein said acrylate polymer has average molecular weight in the range of 50 KD to 5000 KD.

7. The composition according to claim 1, wherein said effective drug is one or more compounds selected from the group consisting of beta-adrenaline activators, beta-adrenaline inhibitors, analgesics, antianginas, antiarrhythmic drugs, antidepressants, antiestrogens, antigonadotrophins, hypotensive drugs, anti-inflammatory drugs, anti-tumor drugs, anti-prostatomegaly drugs, antipsychotics, spasmolytics, antianxiety drugs, bronchodilators, calcium regulators, cardiotonics, dopamine receptors, liver enzyme inducers, estrogens, glucocorticoids, mineral corticoids, monoamine oxidase inhibitors, muscle relaxation drugs, narcotic antagonists, progestogens and peripheral vasodilators.

8. The composition according to claim 7, wherein said effective drug is one or more analgesics selected from the group consisting of buprenorphine and fentanyls like fentanyl, norfentanyl, sufentanyl and alfentanyl.

9. The composition according to claim 1, wherein said hydrophilic polymer is one or more compounds selected from the group consisting of polyvinyl alcohol, polyvinyl pyrrolidone, maleic anhydride/vinyl ether copolymer, gelatin, alginate, hydroxyethyl methacrylate, cargeenane, hydroxyethyl cellulose, silicone rubber, agar, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, carboxyvinyl copolymer, polyethylene oxide, polyethylene glycol, polyacryl amide, polyhydroxyethyl methacrylate, polydioxolane, polyacrylic acid, polyacryl acetate, polyacryl amide and polyvinyl chloride.

10. The composition according to claim 9, wherein said hydrophilic polymer is one or more compounds selected from the group consisting of polyvinyl alcohol, polyvinyl pyrrolidone, maleic anhydride/vinyl ether copolymer and hydroxyethyl cellulose.

11. The composition according to claim 10, comprising 2-30 wt. % of polyvinyl alcohol and 2-20 wt. % of polyvinyl pyrrolidone based on said hydrophilic polymer.

12. The composition according to claim 11, wherein said hydrophilic polymer further comprises 0.1-15 wt. % of hydroxyethyl cellulose or 0.1-20 wt. % of maleic anhydride/vinyl ether copolymer.

13. The composition according to claim 1, wherein said permeation enhancer is one or more compounds selected from the group consisting lauryl alcohol, propylene glycol monolaurate, lauroglycol, isopropyl myristate, triacetin, nonanol, oleyl alcohol, linoleyl alcohol, methyl laurate, glycerol monolaurate and glycerol monooleate.

14. The composition according to claim 13, wherein said permeation enhancer is included in the range of 0.1-65 wt. % to the entire composition.

22. A transdermal drug delivery system comprising the transdermal drug delivery composition according to one of the claims 1 to 21.

15. A transdermal drug delivery composition comprising a hydrophilic polymer base comprising 2-30 wt. % of polyvinyl alcohol and 2-20 wt. % of polyvinyl pyrrolidone of said hydrophilic polymer base;

a drug;

a 0.1-65 wt. % of a lipophilic permeation enhancer based on the entire composition; and

0.1-10 wt. % of a compatibilizer based on the entire composition, said compatibilizer consisting essentially of an acrylate polymer which compatibilizes said lipophilic enhancer with said hydroplhilic polymer base and which renders said composition thermodynamically stable.

16. The composition according to claim 15, wherein said acrylate polymer is included in the range of 2-8 wt. % of the entire composition.

17. The composition according to claim 15, wherein said acrylate polymer is a copolymer comprising a 1:

2 ratio of methyl methacrylate and ethyl acrylate expressed by the following Formula (1a),

18. The composition according to claim 15, wherein said acrylate polymer is a copolymer comprising a 1:

1 ratio of methacrylic acid and ethyl acrylate expressed by the following Formula (1b),

19. The composition according to claim 15, wherein said acrylate polymer has average molecular weight in the range of 50 KD to 5000 KD.

20. The composition according to claim 15, wherein said hydrophilic polymer further comprises 0.1-15 wt. % of hydroxyethyl cellulose or 0.1-20 wt. % of maleic anhydride/vinyl ether copolymer.

21. The composition according to claim 15, wherein said permeation enhancer is one or more compounds selected from the group consisting lauryl alcohol, propylene glycol monolaurate, lauroglycol, isopropyl myristate, triacetin, nonanol, oleyl alcohol, linoleyl alcohol, methyl laurate, glycerol monolaurate and glycerol monooleate.