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Claims for Patent: 6,866,866

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Claims for Patent: 6,866,866

Title: Controlled release metformin compositions
Abstract:A composition for treating patients having non-insulin-dependent diabetes mellitus (NIDDM) by administering a controlled release oral solid dosage form containing preferably a biguanide drug such as metformin, on a once-a-day basis. The dosage form provides a mean time to maximum plasma concentration (T.sub.max) of the drug which occurs at 5.5 to 7.5 hours after oral administration on a once-a-day basis to human patients. Preferably, the dose of drug is administered at dinnertime to a patient in the fed state.
Inventor(s): Chen; Chih-Ming (Davie, FL), Cheng; Xiu-Xiu (Davie, FL), Jan; Steve (Coral Springs, FL), Chou; Joseph (Manassas, VA)
Assignee: Andrx Labs, LLC (Davie, FL)
Application Number:09/705,630
Patent Claims: 1. A controlled release oral dosage form for the reduction of serum glucose levels in human patients with NIDDM, comprising an effective dose of metformin or a pharmaceutically acceptable salt thereof and a controlled-release carrier to control the release of said metformin or pharmaceutically acceptable salt thereof from said dosage form, said dosage form being suitable for providing once-a-day oral administration of the metformin or pharmaceutically acceptable salt thereof, wherein following oral administration of a single dose, the dosage form provides a mean time to maximum plasma concentration (T.sub.max) of the metformin from 5.5 to 7.5 hours after administration following dinner.

2. The controlled release oral dosage form of claim 1, which provides a mean time to maximum plasma concentration (T.sub.max) of metformin at from 6.0 to 7.0 hours after the administration of the dose.

3. The controlled release oral dosage form of claim 1, which provides a mean time to maximum plasma concentration (T.sub.max) of metformin at from 5.5 to 7.0 hours after the administration of the dose.

4. The controlled release oral dosage form of claim 1, which exhibits the following dissolution profiles when tested in a USP type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37 C: 0-30% of the metformin or salt thereof is released after 2 hours; 10-45% of the metformin or salt thereof is released after 4 hours; 30-90% of metformin or salt thereof is released after 8 hours; not less than 50% of the metformin or salt thereof is released after 12 hours; not less than 60% of the metformin or salt thereof is released after 16 hours; and not less than 70% of the metformin or salt thereof is released after 20 hours.

5. The controlled release oral dosage form of claim 1, which exhibits the following dissolution profiles when tested in a USP type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37 C: 0-25% of the metformin or salt thereof is released after 2 hours; 20-40% of the metformin or salt thereof is released after 4 hours; 45-90% of the metformin or salt thereof is released after 8 hours; not less than 60% of the metformin or salt thereof is released after 12 hours; not less than 70% of the metformin or salt thereof is released after 16 hours; and not less than 80% of the metformin or salt thereof is released after 20 hours.

6. The controlled release oral dosage form of claim 1, which provides a width at 50% of the height of a mean plasma concentration/time curve of the metformin from about 4.5 to about 13 hours.

7. The controlled release oral dosage form of claim 1, which provides a width at 50% of the height of a mean plasma concentration/time curve of the metformin from about 5.5 to about 10 hours.

8. The controlled release oral dosage form of claim 1, which provides a mean maximum plasma concentration (C.sub.max) of metformin which is more than about 7 times the mean plasma level of said metformin at about 24 hours after the administration.

9. The controlled release oral dosage form of claim 1, which provides a mean maximum plasma concentration (C.sub.max) of metformin which is from about 7 times to about 14 times the plasma level of said metformin at about 24 hours after administration.

10. The controlled release oral dosage form of claim 1 which provides a mean maximum plasma concentration (C.sub.max) of metformin which is from about 8 times to about 12 times the plasma level of said metformin at about 24 hours after administration.

11. The controlled release oral dosage form of claim 1 which provides a mean maximum plasma concentration (C.sub.max) of metformin from about 1500 ng/ml to about 3000 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

12. The controlled release oral dosage form of claim 1, which provides a mean maximum plasma concentration (C.sub.max) of metformin from about 1700 ng/ml to about 2000 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

13. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24hr of at least 80% of the mean AUC.sub.0-24 provided by administration of an immediate release reference standard twice a day, wherein the daily dose of the reference standard is substantially equal to the once-a-day dose of metformin administered in the controlled release oral dosage form.

14. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24hr of at least 90% of the mean AUC.sub.0-24 provided by administration of an immediate release reference standard twice a day, wherein the daily dose of the reference standard is substantially equal to the once-a-day dose of metformin administered in the controlled release oral dosage form.

15. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24hr from about 17200 ng.hr/ml to about 33900 ng.hr/ml, based on administration of a 2000 mg once-a-day dose of metformin.

16. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24hr from about 17200 ng.hr/ml to about 26500 ng.hr/ml, based on administration of a 2000 mg once-a-day dose of metformin.

17. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24hr from about 19800 ng.hr/ml to about 33900 ng.hr/ml, based on administration of a 2000 mg once-a-day dose of metformin.

18. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-.infin. of 18277.+-.2961 ng.hr/ml and a mean C.sub.max of 1929.+-.333 ng/ml, for administration of a 1700 mg once-a-day dose of metformin after an evening meal.

19. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-.infin. of 20335.+-.4360 ng.hr/ml and a mean C.sub.max of from 2053.+-.447 ng/ml, for administration of a 2000 mg once-a-day dose of metformin after an evening meal.

20. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24 of 26818.+-.7052 ng.hr/ml and a mean C.sub.max of 2849.+-.797 ng/ml, for, administration of a 2000 mg once-a-day dose of metformin after an evening meal.

21. The controlled release oral dosage form of claim 1 which provides a mean AUC.sub.0-24 of 22590.+-.3626 ng.hr/ml and a mean C.sub.max of 2435.+-.630 ng/ml on the first day of administration and a mean AUC.sub.0-24 of 24136.+-.7996 ng.hr/ml and a mean C.sub.max of 2288.+-.736 ng/ml on the 14.sup.th day of administration, for administration of a 2000 mg once-a-day dose of metformin after an evening meal.

22. The controlled release oral dosage form of claim 12 which provides a mean t.sub.1/2 from 2.8 to 4.4.

23. The controlled release oral dosage form of claim 6, which provides a mean time to maximum plasma concentration (T.sub.max) of metformin from 6.0 to 7.0 hours after the administration.

24. The controlled release oral dosage form of claim 6, which provides a mean time to maximum plasma concentration (T.sub.max) of metformin from 5.5 to 7.0 hours after administration.

25. The controlled release dosage form of claim 1, wherein the metformin or pharmaceutically acceptable salt thereof is provided by at least one controlled-release tablet, said tablet comprising: (a) a core comprising: (i) the metformin or a pharmaceutically acceptable salt; (ii) optionally a binding agent; and (iii) optionally an absorption enhancer; (b) a membrane coating surrounding the core; and (c) at least one passageway in the membrane.
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