Transdermal therapeutic system

• US 20040101550A1
• Filed: 07/07/2003
• Published: 05/27/2004
• Est. Priority Date: 08/24/2000
• Status: Abandoned Application

• Current Assignee: Axxonis Pharma AG
• Original Assignee: Axxonis Pharma AG
• Inventors: Tack, Johannes, Horowski, Reinhard, Windt-Hanke, Fred, Gunther, Clemens
• Application Number:
  US10/362,248
• Publication Number:
  US 20040101550A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 31/48 Ergoline derivatives, e.g. lysergic acid, ergotamine
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/14 for lactation disorders, e.g. galactorrhoea
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/08 for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

Use of a transdermal therapeutic system (TTS) comprising a pharmaceutical layer containing at least one matrix having an active ingredient and/or an active ingredient reservoir; a diffusion barrier that is permeable to said active ingredient and arranged on the skin side of the active ingredient reservoir; and an ergoline derivative or salt thereof as an active ingredient for producing an agent for obtaining and maintaining the circadian rhythm under dopamine therapy.

Claims

1. ) Use of a transdermal therapeutic system (TTS) comprising a pharmaceutical layer containing at least one matrix having an active ingredient, and/or an active ingredient reservoir;

a diffusion barrier which is permeable to active ingredients and which is arranged on the skin side of the active ingredient reservoir; and

an ergoline derivative according to formula I or physiologically compatible salt thereof with an acid,

2. ) The use according to claim 1 wherein the matrix and/or diffusion barrier are selected so that the transdermal flux F through human skin is in the range from 0.1 to 5.0 μ

g/cm²/h.

3. ) The use according to claims 1 or 2 wherein the ergoline derivative is lisuride or a physiologically compatible salt thereof.

4. ) The use according to any one of claims 1 through 3 wherein a covering layer is provided on the side of the matrix and/or active ingredient reservoir that faces away from the skin.

5. ) The use according to any one of claims 1 through 4 wherein the matrix and/or diffusion barrier comprise as their main matrix component a substance selected from the group consisting of “

polyacrylate, polyurethane, cellulose ether, silicone, polyvinyl compounds, silicate and mixtures of these substances as well as copolymers of these polymeric compounds,”

preferably hydrophilic polyacrylate with basic substituents.

6. ) The use according to any one of claims 1 through 5 wherein the diffusion barrier comprises as its main barrier component a synthetic polymer selected from the group consisting of “

cellulose ester, cellulose ether, silicone, polyolefin and mixtures as well as copolymers of these substances.”

7. ) The use according to any one of claims 1 through 6 wherein the matrix and/or the active ingredient reservoir and/or the diffusion barrier contain a penetration-enhancing agent that is preferably selected from the group consisting of “

C1-C8 aliphatic, cycloaliphatic and aromatic alcohols, saturated and unsaturated C8-18 fatty alcohols, saturated and unsaturated C8-18 fatty acids, hydrocarbons and hydrocarbon mixtures, fatty acid esters from C3-19 fatty acids and C1-6-alkyl monools, dicarboxylic acid diesters from C4-8-dicarboxylic acids and C1-6 alkyl monools, and mixtures of these substances.

8. The use according to any one of claims 1 through 7 wherein the matrix and/or the active ingredient reservoir and/or the diffusion barrier contain a crystallization inhibitor that is selected from the group consisting of “

highly dispersed silicon dioxide or macromolecular substances such as polyvinyl pyrrolidone, polyvinyl alcohols, dextrines, dextranes, sterines, bile acids and, in particular, vinyl pyrrolidone vinylacetate copolymers.”

9. The use according to any one of claims 1 through 8 wherein the matrix and/or active ingredient reservoir and/or diffusion barrier contain an antioxidant that is selected from the group consisting of “

sulfur-containing amino acids such as cysteine, methyl donors such as methionine, or antioxidants such as glutathione or sodium hydrogensulfite.”

10. ) Use of a TTS according to any one of claims 1 through 9 to produce an agent for the treatment or prevention of premenstrual syndrome wherein the preferred F value is in the range from 0.1 to 0.5 μ

g/cm²/h.

11. ) Use of a TTS according to any one of claims 1 through 9 to produce an agent for lactation inhibition wherein the preferred F value is in the range from 0.1 to 0.5 μ

g/cm²/h.

12. ) A TTS set for the treatment of circadian disturbances under dopamine therapy wherein the set contains a multitude of TTS elements and wherein said elements are configured for releasing different doses.

13. ) A TTS set according to claim 12 wherein the TTS elements are separated and wherein each TTS element is configured for a continuously ascending sequence of F ranging from 0.1 to 5 μ

g/cm²/h.

14. ) The TTS set according to claims 12 or 13 wherein the TTS elements are equipped with different active surfaces in a continuous sequence.