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Last Updated: March 29, 2024

Details for Patent: 7,008,637


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Title:Transdermally administered tolterodine as anti-muscarinic agent for the treatment of overactive bladder
Abstract: The present invention is drawn to set of formulations of at least one compound selected from tolterodine, salts thereof, prodrugs thereof and/or metabolites thereof, wherein in the set of formulations contains at least one device for transdermal administration and at least one formulation for oral, sublingual, buccal, nasal, pulmonary, rectal and/or other transmucosal administration, in order to achieve an effect against overactive bladder and/or symptoms associated with this condition. The present invention is further drawn to methods of treating an overactive bladder with the formulations.
Inventor(s): Jacobsen; Lene Orup (Gentofte, DK), Kreilgard; Bo (Hillerod, DK), Hoeck; Ulla (Hillerod, DK), Kristensen; Helle (Slangerup, DK)
Assignee: Pfizer Health AB (SE)
Filing Date:Nov 22, 2002
Application Number:10/301,719
Claims:1. A delivery system comprising: at least one compound selected from the group consisting of R-tolterodine, salts thereof, prodrugs thereof and metabolites thereof; and at least one device for transdermal administration of said at least one compound, said device selected from the group consisting of a reservoir, a matrix, a drug-in-adhesive, a multi-laminate, a polymer-system with no foils, an iontophoretic and combinations thereof, an electroporation, an electroosmosis, an electroincorporation a jet injection device, said device containing said at least one compound, and said device having an hourly flux rate of tolterodine of about 0.1 .mu.g/h/cm.sup.2 to about 100 .mu.g/h/cm.sup.2; and at least one formulation for oral, sublingual, buccal, nasal, pulmonary, rectal and/or other transmucosal administration of said at least one compound, to a human being or an animal in order to achieve an effect against overactive bladder and/or symptoms associated with this condition.

2. The delivery system according to claim 1, wherein tolterodine essentially is in racemic form.

3. The delivery system according to claim 1, wherein said at least one compound is the tolterodine metabolite (R)-N,N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenylphenyl)-3-phenylpro- panamine.

4. The delivery system according to claim 1, wherein said device has a loading of tolterodine from about 0.1 mg/cm.sup.2 to about 5 mg/cm.sup.2.

5. The delivery system according to claim 1, wherein said device has an area of from about 2 cm.sup.2 to about 100 cm.sup.2.

6. The delivery system according to claim 1, wherein said device delivers tolterodine for a predefined period of time.

7. The delivery system according to claim 1, wherein said tolterodine is present in a complex with cyclodextrin.

8. The delivery system according to claim 1, wherein said device has a release profile such that, when applied on the skin at the appropriate time during day or night, tolterodine is administered in such a way that a therapeutically effective systemic level of tolterodine prevails mainly during such periods of time during day and night when an effect against overactive bladder is most desirable.

9. The delivery system according to claim 1, wherein said device further comprises a substance enhancing transdermal penetration.

10. The delivery system according to claim 1, wherein said device further comprises a substance for reducing irritant reactions.

11. The delivery system according to claim 1, wherein said device is occlusive.

12. The delivery system according to claim 1, further comprising at least one pharmaceutically acceptable carrier.

13. The delivery system according to claim 1, wherein said device has an hourly flux rate of tolterodine from about 0.2 .mu.g/h/cm.sup.2 to about 35 .mu.g/h/cm.sup.2.

14. The delivery system according to claim 5, wherein said device has an area of from about 5 cm.sup.2 to about 30 cm.sup.2.

15. The delivery system according to claim 6, wherein said device delivers tolterodine for a predefined period of time of 12, 24 or 48 hours, or up to 7 or 14 days.

16. The delivery system according to claim 7, wherein said tolterodine is present in a complex with .beta.-cyclo-dextrin.

17. The delivery system according to claim 3, wherein said at least one compound further comprises tolterodine.

18. A method for achieving an effect against overactive bladder in a living body in need thereof by administration a therapeutically effective amount of the delivery system of claim 1.

19. The method according to claim 18, wherein tolterodine essentially is in racemic form.

20. The method according to claim 18, wherein the at least one compound of the set of formulations comprises the tolterodine metabolite (R)-N,N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropanami- ne.

21. The method according to claim 18, wherein the treatment is at least partially achieved through systemic effect of the transdermally administered compound.

22. The method according to claim 18, comprising transdermal administration using more than one device for transdermal delivery at a time.

23. A delivery system comprising: at least one compound having a therapeutic effect against an overactive bladder in a living body which is selected from the group consisting of (R)-tolterodine or the racemate thereof, salts thereof, prodrugs thereof, and metabolites thereof; a transdermal administration device selected from the group consisting of a reservoir, a matrix, a drug-in-adhesive, a multi-laminate, a polymer-system with no foils, a iontophoretic device, and combinations thereof, an electroporation, an electroosmosis, an electroincorporation and a jet injection device which contains said compound and which has an hourly flux rate of said at least one compound from about 0.1 .mu.g/h/cm.sup.2 to about 100 .mu.g/h/cm.sup.2; and at least one formulation for oral, sublingual, buccal, nasal, pulmonary, rectal and/or other transmucosal administration.

24. A method for achieving an effect against an overactive bladder in a living body which comprises administering a therapeutically effective amount of the delivery system of claim 23 to a patient in need thereof.

25. The delivery system according to claim 11, wherein the at least one device is a drug-in-adhesive or reservoir device or a combination thereof.

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