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Claims for Patent: 6,630,162

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Claims for Patent: 6,630,162

Title: Pharmaceutical formulation and its use
Abstract:The invention relates to a pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, as active ingredient, in which the formulation exhibits a controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours. The invention also relates to the use of the pharmaceutical formulation for treating overactive bladder and gastrointestinal disorders.
Inventor(s): Nilvebrant; Lisbeth (Bromma, SE), Hallen; Bengt (Sollentuna, SE), Olsson; Birgitta (Stenhamra, SE), Strombom; Jan (Vattholm, SE), Gren; Torkek (Kalamazoo, MI), Ringberg; Anders (Stockholm, SE), Wikberg; Martin (Kullavik, SE)
Assignee: Pharmacia AB (Stockholm, SE)
Application Number:09/708,428
Patent Claims: 1. An oral pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmaceutically acceptable salt thereof, as active ingredient, wherein said formulation exhibits controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours, and 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.

2. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is not less than about 80% after 15 hours.

3. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is not less than about 80% after 12 hours.

4. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is less than about 50% after 1 hour.

5. The formulation according to claim 4, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is less than about 30% after 1 hour.

6. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is from about 30 to about 95% after 3 hours.

7. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is from about 40 to about 85% after 3 hours.

8. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is more than about 50% after 7 hours.

9. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is more than about 80% after 7 hours.

10. The formulation according to claim 1, wherein the fraction of tolterodine, tolterodine-related compound or salt thereof that is released in vitro is not more than about 50% after 1 hour, from about 30 to about 95% after 3 hours, and not less than about 50% after 7 hours.

11. The formulation according to claim 1, wherein the in vitro release is measured by a drug release test which utilizes the United States Pharmacopea (USP) Apparatus 1 (rotating basket) at 100 rpm with 900 ml of deaerated phosphate buffer at pH 6.8 and 37.degree. C., where the phosphate buffer solution is prepared as described on pages 2049-2050 of USP 23, and nominally contains 0.05 M phosphate.

12. The formulation according to claim 1, which comprises tolterodine, its 5-hydroxymethyl metabolite or the racemate corresponding to tolterodine, or a salt thereof.

13. The formulation according to claim 1, which comprises tolterodine, or a salt thereof.

14. The formulation according to claim 1, 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.

15. The formulation according to claim 14, wherein the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.2 to about 6.3 nM.

16. A method of treating an overactive bladder, which comprises administering a therapeutically effective amount of a pharmaceutical formulation according to claim 1.

17. A method of treating urinary incontinence, which comprises administering a therapeutically effective amount of a pharmaceutical formulation according to claim 1.

18. A method of treating nocturia, which comprises administering a therapeutically effective amount of a pharmaceutical formulation according to claim 1.

19. A method of treating gastrointestinal disorders, which comprises administering a therapeutically effective amount of a pharmaceutical formulation according to claim 1.

20. A method for orally administering tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, to a patient to maintain a substantially constant serum level of the active moiety or moieties for 24 hours, which method comprises administering a pharmaceutical formulation containing tolterodine, a tolterodine-related compound or a salt thereof, which formulation exhibits a controlled in vitro release in phosphate buffer at pH 6.8 of tolterodine, tolterodine-related compound or salt thereof of not less than about 80% after 18 hours.

21. The formulation 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 1.0.

22. The formulation according to claim 15, wherein the 24-hour serum profile, is from about 10 nM*h to about 120 nM*h.

23. The formulation according to claim 16, wherein the serum level of unbound tolterodine and 5-hydroxymethyl metabolite is in the range of about 0.4 to about 5.0 nM.
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