Transdermal patch and topical compositions comprising propylnorapomorphine

• US 6,592,893 B1
• Filed: 01/12/2001
• Issued: 07/15/2003
• Est. Priority Date: 07/17/1998
• Status: Expired due to Fees

• Current Assignee: Unihart Corporation
• Original Assignee: Unihart Corporation
• Inventors: Gessa, Gian Luigi
• Primary Examiner(s): Kishore, Gollamudi S.
• Assistant Examiner(s): GHALI, ISIS A D
• Application Number:
  US09/743,576
• Time in Patent Office: 914 Days
• Field of Search: 424/449, 424/448, 424/443
• US Class Current: 424/449
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs

Abstract

A pharmaceutical composition is characterized by: an active principle selected from one or more components of the group consisting of R(−)-propylnorapomorphine hydrochloride, S(+)-propylnorapomorphine hydrochloride, derivatives of R(−)-propylnorapomorphine hydrochloride and derivatives of S(+)-propylnorapomorphine hydrochloride, in pharmaceutically acceptable and effective doses, and further comprising components selected from the group consisting of stabilizers, solubilizers and permeation activators to facilitate the passage of the active principle through the skin. A transdermal patch that includes the pharmaceutical composition is also disclosed as well as a method of treatment for Parkinson'"'"'s disease, hemicrania, sexual impotence, and psychotic disorders using the pharmaceutical composition or a transdermal patch that includes the pharmaceutical composition are described.

Claims

1. A transdermal patch comprising:

at least one support film;

an intermediate matrix comprising a pharmaceutical composition; and

a protective release strip, wherein the pharmaceutical composition comprises an active principle selected from one or more components of the group consisting of R(−

)-propylnorapomorphine hydrochloride, S(+)-propylnorapomorphine hydrochloride, derivatives of R(−

)-propylnorapomorphine hydrochloride and derivatives of S(+)-propylnorapomorphine hydrochloride, in pharmaceutically acceptable and effective doses, and further comprising components selected from the group consisting of stabilizers, solubilizers and permeation activators to facilitate the passage of the active principle through skin.

2. A transdermal patch according to claim 1, wherein said derivatives of R(−

)-propylnorapomorphine hydrochloride and derivatives of S(+)-propylnorapomorphine hydrochloride are salts or organic derivatives.

3. A transdermal patch according to claim 1, wherein said stabilizers are antioxidant substances.

4. A transdermal patch according to claim 1, wherein said solubilizer is a glycol.

5. A transdermal patch according to claim 1, wherein said permeation activators are fatty acids or alcohols.

6. A transdermal patch according to claim 3, said antioxidant substance comprises sodium metabisulphite and EDTA.

7. A transdermal patch according to claim 1, wherein the pharmaceutical composition additionally comprises a surfactant.

8. A transdermal patch according to claim 1, wherein the pharmaceutical composition additionally comprises an acrylic resin to improve the cohesive strength, cellulose derivatives to improve the cohesive strength, and a mixture of pressure contact adhesives.

9. A transdermnal patch according to claim 1, wherein said matrix comprises a lower side layer comprising a permeable membrane that does not include adhesives.

10. A transdermal patch according to claim 9, wherein said permeable membrane modifies the release of the active principle and is an adhesive layer for fixing on the skin.

11. A transdermal patch according to claim 9, wherein said permeable membrane is not adhesive and has an adhesive layer underneath for fixing on the skin.

12. A transdermal patch according to claim 1, wherein an adhesive layer is applied on sides of the matrix not containing adhesives.

13. A transdermal patch according to claim 1, comprising an adhesive matrix containing an acrylic resin, cellulose derivatives to improve the cohesive strength, and a mixture of pressure contact adhesives.

14. A method of treatment of a disorder selected from the group consisting of Parkison'"'"'s disease, hemicrania, sexual impotence and psychotic disorders, comprising the step of administering the transdermal patch of claim 1 to obtain slow release of the active component through the skin.

15. A transdermal patch according to claim 7, wherein said surfactant is sodium dodecyl sulfate.