IP Library › Patent Application 11225741
Patent Application
App. No. 11/225,741

Controlled release metformin compositions

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Patent No.
US None
App. No.
11/225,741
Abstract

A composition for treating patients having non-insulin-dependent diabetes mellitus (NIDM) 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 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.

Claims (35)

1 - 42 . (canceled)

43 . A controlled release oral dosage form for the reduction of serum glucose levels in human patients with NIDDM, comprising metformin or a pharmaceutically acceptable salt thereof and a controlled-release carrier, said dosage form (i) providing an in-vitro dissolution of metformin or salt thereof of from 0-30% at 2 hours when tested in a USP type II apparatus at 75 rpm in 900 mL of pH 7.5 phosphate buffer and at 37 degrees C; and (ii) being suitable for providing once-a-day oral administration of the metformin or pharmaceutically acceptable salt thereof and providing a mean maximum plasma concentration (C 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 to human patients.

44 . The controlled release oral dosage form of claim 43 , which provides a mean maximum plasma concentration (C max ) of metformin from about 750 ng/ml to about 1500 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

45 . The controlled release oral dosage form of claim 43 , which provides a mean maximum plasma concentration (C max ) of metformin from about 1125 ng/ml to about 2250 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

46 . The controlled release oral dosage form of claim 43 , which provides a mean maximum plasma concentration (C max ) of metformin from about 1875 ng/ml to about 3750 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

47 . A controlled release oral dosage form for the reduction of serum glucose levels in human patients with NIDDM, comprising metformin or a pharmaceutically acceptable salt thereof and a controlled-release carrier, said dosage form (i) providing an in-vitro dissolution of metformin or salt thereof of from 0-30% at 2 hours when tested in a USP type II apparatus at 75 rpm in 900 mL of pH 7.5 phosphate buffer and at 37 degrees C.; and (ii) being suitable for providing once-a-day oral administration of the metformin or pharmaceutically acceptable salt thereof and providing a mean maximum plasma concentration (C max ) of metformin from about 1582 ng/ml to about 3646 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin to human patients.

48 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin from about 791 ng/ml to about 1823 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

49 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin from about 1187 ng/ml to about 2735 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

50 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin from about 1978 ng/ml to about 4558 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

51 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2127 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

52 . The controlled release oral dosage form of claim 51 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1064 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

53 . The controlled release oral dosage form of claim 51 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1596 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

54 . The controlled release oral dosage form of claim 51 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2659 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

55 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2053 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

56 . The controlled release oral dosage form of claim 55 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1027 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

57 . The controlled release oral dosage form of claim 55 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1540 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

58 . The controlled release oral dosage form of claim 55 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2566 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

59 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2435 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

60 . The controlled release oral dosage form of claim 59 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1218 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

61 . The controlled release oral dosage form of claim 59 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1827 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

62 . The controlled release oral dosage form of claim 59 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 3044 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

63 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2288 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

64 . The controlled release oral dosage form of claim 63 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1144 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

65 . The controlled release oral dosage form of claim 63 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1716 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

66 . The controlled release oral dosage form of claim 63 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2860 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

67 . The controlled release oral dosage form of claim 47 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2849 ng/ml, based on administration of a 2000 mg once-a-day dose of metformin.

68 . The controlled release oral dosage form of claim 67 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 1425 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

69 . The controlled release oral dosage form of claim 67 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 2138 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

70 . The controlled release oral dosage form of claim 67 , which provides a mean maximum plasma concentration (C max ) of metformin therapeutically equivalent to 3561 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

71 . The controlled release oral dosage form of claim 43 , which provides a mean AUC 0-24 hr of metformin 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.

72 . The controlled release oral dosage form of claim 71 , which provides a mean AUC 0-24 hr of metformin from about 8600 ng/ml to about 16950 ng/ml upon administration of a 1000 mg once-a-day dose of metformin.

73 . The controlled release oral dosage form of claim 71 , which provides a mean AUC 0-24 hr of metformin from about 12900 ng/ml to about 25425 ng/ml upon administration of a 1500 mg once-a-day dose of metformin.

74 . The controlled release oral dosage form of claim 71 , which provides a mean AUC 0-24 hr of metformin from about 21500 ng/ml to about 42375 ng/ml upon administration of a 2500 mg once-a-day dose of metformin.

75 . The controlled release oral dosage form of claim 43 , wherein said dosage form comprising said metformin or pharmaceutically acceptable salt thereof is contained in two formulations.

76 . The controlled release oral dosage form of claim 43 , wherein said core is a tablet core and said membrane comprise a hydrophobic material.