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Claims for Patent: 6,770,295

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Claims for Patent: 6,770,295

Title: Therapeutic formulation for administering tolterodine with controlled release
Abstract:The present invention is drawn to a method of treating an unstable or overactive urinary bladder by treating the patient with tolterodine or a tolterodine-related compound, or pharmaceutically acceptable salt thereof, with a controlled release formulation that maintains a substantially constant serum level of the active moiety or moieties for at least 24 hours. The present invention is further drawn to a formulation for the method.
Inventor(s): Kreilg.ang.rd; Bo (Hillerod, DK), Orup Jacobsen; Lene (Gentofte, DK), Hoeck; Ulla (Hillerod, DK), Kristensen; Helle (Slangerup, DK), Gren; Torkel (Uppsala, SE), Nilvebrant; Lisbeth (Bromma, SE), Ringberg; Anders (Stockholm, SE), Wikberg; Martin (Kullavik, SE), Hallen; Bengt (Sollentuna, SE), Olsson; Birgitta (Stenhamra, SE), Strombom; Jan (Vattholma, SE)
Assignee: Pharmacia AB (Stockholm, SE)
Application Number:09/582,498
Patent Claims: 1. A method of treating unstable or overactive urinary bladder, wherein the method comprises administering to a patient in need of such treatment tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, in a pharmaceutically effective amount thereof through a controlled release formulation capable of maintaining a substantially constant serum level of the active moiety or moieties for at least 24 hours, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from 5 to about 150 nM*h.

2. The method according to claim 1, wherein the controlled release formulation provides a mean fluctuation index of said serum level of active moiety or moieties that is not higher than about 2.0, said fluctuation index, FI, being defined as FI=(Cmax-Cmin)/AUC.tau./.tau., wherein Cmax and Cmin are the maximum and minimum concentrations, respectively, of active moiety or moieties, AUC.tau. is the area under the serum concentration profile, and .tau. is the length of the dosage interval.

3. A method of treating unstable or overactive urinary bladder, wherein the method comprise administering to a patient in need of such treatment tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, in a pharmaceutically effective amount thereof through controlled release formulation capable of maintaining a substantially constant serum level of the active moiety or moieties for at least 24 hours with reduced undesirable side effects and with no reduction in the efficacy of the tolterodine compound, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from 5 to about 150 nM*h.

4. The method according to claim 1, wherein tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine is administered, and the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.2 to about 6.3 nM.

5. The method according to claim 1 wherein the controlled release formulation is a capsule or tablet for oral administration once daily.

6. The method according to claim 1, wherein the controlled release formulation is a transdermal preparation.

7. The method according to claim 1 wherein tolterodine is administered.

8. The method according to claim 1 wherein urinary incontinence is treated.

9. A pharmaceutical formulation containing tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, which formulation when administered to a patient provides controlled release of tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or salt thereof, such that a substantially constant serum level of the active moiety or moieties is maintained for at least 24 hours, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from 5 to about 150 nM*h.

10. The formulation of claim 9, which provides a mean fluctuation index of said serum level of active moiety or moieties that is not higher than about 2.0, said fluctuation index, FI, being defined as FI=(Cmax-Cmin)/AUC.tau./.tau., wherein Cmax and Cmin are the maximum and minimum concentrations, respectively, of active moiety or moieties, AUC.tau. is the area under the serum concentration profile, and .tau. is the length of the dosage interval.

11. A pharmaceutical formulation containing tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a pharmaceutically acceptable salt thereof, which formulation when administered to a patient provides controlled release of said tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or pharmaceutically acceptable salt thereof, such that a substantially constant serum level of the active moiety or moieties is maintained for at least 24 hours for efficacious therapy with reduced undesirable side effects, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from 5 to about 150 nM*h.

12. The formulation according to claim 9, wherein tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine is administered, and the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.2 to about 6.3 nM.

13. The formulation according to claim 9, which is a capsule or tablet for oral administration once daily.

14. The formulation according to claim 1, which is a transdermal preparation.

15. The formulation according to claim 9, which provides controlled release of tolterodine.

16. The method of claim 3, wherein the controlled release formulation is administered orally.

17. The formulation of claim 11, which is in a form for oral administration.

18. The method according to claim 2, wherein the controlled release formulation provides a mean fluctuation index of said serum level of active moiety or moieties that is not higher than about 1.0.

19. The method according to claim 3, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from about 10 nM*h to about 120 nM*h.

20. The method according to claim 4, wherein the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.4 to about 5.0 nM.

21. The method according to claim 6, wherein the transdermal preparation is a transdermal patch.

22. The formulation of claim 10, wherein the mean fluctuation index of said serum level of active moiety or moieties that is not higher than about 1.0.

23. The formulation according to claim 11, wherein the 24-hour serum profile, expressed as the AUC of unbound tolterodine and 5-hydroxymethyl metabolite, is from about 10 nM*h to about 120 nM*h.

24. The formulation according to claim 12, wherein the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.4 to about 5.0 nM.

25. The transdermal preparation of claim 14, which is a transdermal patch.

26. The method of claim 3, wherein increased efficacy of the tolterodine compound is obtained with minimal undesirable side effects.

27. The formulation of claim 11, wherein increased efficacy of the tolterodine compound is obtained with minimal undesirable side effects.
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