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Controlled release metformin compositions

a composition and metformin technology, applied in the field of oral dosage, can solve the problems of no fixed dosage regimen, little research in the field of controlled or sustained release compositions that employ antihyperglycemic drugs, etc., and achieve the effect of effective control of blood glucose levels

Inactive Publication Date: 2006-01-12
ANDRX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012] It is an object of the present invention to provide a controlled or sustained release of an antihyperglycemic drug which provides effective control of blood glucose levels in humans.
[0013] It is a further object of the present invention to provide a method of treating human patients with non-insulin-dependent diabetes mellitus (NTDDM) on a once-a-day basis with an antihyperglycemic drug which provides effective control of blood glucose levels in humans.
[0014] It is a further object of the present invention to provide formulations for treating human patients with non-insulin-dependent diabetes mellitus (NIDDM) which provides advantages over the state-of-the-art, and which may be administered on a once-a-day basis by itself or together with other antidiabetic agents, and methods thereof.
[0015] It is a further object of the present invention to provide a controlled or sustained release formulation of an antihyperglycemic drug wherein the bioavailability of the drug is not decreased by the presence of food.
[0017] It is also a further object of the present invention to provide a controlled or sustained release formulation of an antihyperglycemic drug that can provide continuous and non-pulsating therapeutic levels of the drug to an animal or human in need of such treatment over a twelve hour to twenty-four hour period.
[0037] The dosage form of the present invention can provide therapeutic levels of the antihyperglycemic drug for twelve to twenty-four hour periods and does not exhibit a decrease in bioavailability if taken with food. In fact, a slight increase in the bioavailability of the antihyperglycemic drug is observed when the controlled release dosage form of the present invention is administered with food. In a preferred embodiment, the dosage form can be administered once-a-day, ideally with or after a meal, preferably with or after the evening meal, and provides therapeutic levels of the drug throughout the day with peak plasma levels being obtained between 5.5 to 7.5 hours after administration.

Problems solved by technology

Although vast amounts of research has been performed on controlled or sustained release compositions and in particular on osmotic dosage forms, very little research has been performed in the area of controlled or sustained release compositions that employ antihyperglycemic drugs.
There is no fixed dosage regimen for the management of hyperglycemia in diabetes mellitus with GLUCOPHAGE®.

Method used

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  • Controlled release metformin compositions
  • Controlled release metformin compositions
  • Controlled release metformin compositions

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0117] A controlled release tablet containing 500 mg of metformin HCl and having the following formula is prepared as follows:

I. CoreIngredientsAmount (mg / tab)Metformin HCl500.0Povidone3, USP36.0Sodium Lauryl Sulfate25.8Magnesium Stearate2.8

3approximate molecular weight = 1,000,000; dynamic viscosity (10% w / v solution at 20° C.) = 300-700 m Pa s.

[0118] (a) Granulation

[0119] The metformin HCl and sodium lauryl sulfate are delumped by passing them through a 40 mesh screen and collecting them in a clean, polyethylene-lined container. The povidone, K-90-F is dissolved in purified water. The delumped metformin HCl and sodium lauryl sulfate are then added to a top-spray fluidized bed granulator and granulated by spraying with the binding solution of povidone under the following conditions: inlet air temperature of 50-70° C.; atomization air pressure of 1-3 bars; and spray rate of 10-100 m / min.

[0120] Once the binding solution is depleted, the granules are dried in the granulator until...

example 2

[0128] A controlled release tablet containing 850 mg of metformin HCl and having the following formula is prepared as follows:

I. CoreIngredientsAmount (mg / tab)Metformin HCl850.0Povidone3, USP61.1Sodium Lauryl Sulfate43.9Magnesium Stearate4.8

3approximate molecular weight = 1,000,000; dynamic viscosity (10% w / v solution at 20° C.) = 300-700 m Pa s.

[0129] (a) Granulation

[0130] The metformin HCl and sodium lauryl sulfate are delumped by passing them through a 40 mesh screen and collecting them in a clean, polyethylene-lined container. The povidone, K-90-F is dissolved in purified water. The delumped metformin HCl and sodium lauryl sulfate are then added to a top-spray fluidized bed granulator and granulated by spraying with the binding solution of povidone under the following conditions: inlet air temperature of 50-70° C.; atomization air pressure of 1-3 bars; and spray rate of 10-100 m / min.

[0131] Once the binding solution is depleted, the granules are dried in the granulator until...

example 3

[0139] A controlled release tablet containing 1000 mg of metformin HCl and having the following formula is prepared as follows:

I. CoreIngredientsAmount (mg / tablet)Metformin HCl1000.0Povidone3, USP71.9Sodium Lauryl Sulfate51.7Magnesium Stearate5.6

3approximate molecular weight = 1,000,000; dynamic viscosity (10% w / v solution at 20° C.) = 300-700 m Pa s.

[0140] (a) Granulation

[0141] The metformin HCl and sodium lauryl sulfate are delumped by passing them through a 40 mesh screen and collecting them in a clean, polyethylene-lined container. The povidone, K-90-F is dissolved in purified water. The delumped metformin HCl and sodium lauryl sulfate are then added to a fluidized bed granulator and granulated by spraying with the binding solution of povidone under the following conditions: inlet air temperature of 50-70° C.; atomization air pressure of 1-3 bars; and spray rate of 10-100 ml / min.

[0142] Once the binding solution is depleted, the granules are dried in the granulator until the...

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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 (Tmax) 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.

Description

BACKGROUND OF THE INVENTION [0001] The present invention relates to controlled release unit dose formulations containing an antihyperglycemic drug. More specifically, the present invention relates to an oral dosage form comprising a biguanide such as metformin or buformin or a pharmaceutically acceptable salt thereof such as metformin hydrochloride or the metformin salts described in U.S. Pat. Nos. 3,957,853 and 4,080,472 which are incorporated herein by reference. [0002] In the prior art, many techniques have been used to provide controlled and extended-release pharmaceutical dosage forms in order to maintain therapeutic serum levels of medicaments and to minimize the effects of missed doses of drugs caused by a lack of patient compliance. [0003] In the prior art are extended release tablets which have an osmotically active drug core surrounded by a semipermeable membrane. These tablets function by allowing a fluid such as gastric or intestinal fluid to permeate the coating membran...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/22A61K9/00A61K9/28A61K9/52A61K31/155
CPCA61K9/0004A61K31/155A61K9/2866A61K9/2027
Inventor CHEN, CHIH-MINGCHENG, XIU-XIUJAN, STEVECHOU, JOSEPH
Owner ANDRX
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