Controlled release metformin formulations

• US 7,919,116 B2
• Filed: 03/02/2007
• Issued: 04/05/2011
• Est. Priority Date: 03/20/1998
• Status: Expired due to Fees

• Current Assignee: Andrx Labs LLC (Abbvie Incorporated)
• Original Assignee: Andrx Labs LLC (Abbvie Incorporated)
• Inventors: Chou, Joseph, Jan, Steve, Cheng, Xiu Xiu, Chen, Chih-Ming
• Primary Examiner(s): Fubara; Blessing M
• Application Number:
  US11/713,143
• Publication Number:
  US 20070154548A1
• Time in Patent Office: 1,495 Days
• Field of Search: 424/468, 514/635
• US Class Current: 424/468
• CPC Class Codes: A61K 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics

Abstract

Sustained release pharmaceutical formulations comprising an antihyperglycemic drug or a pharmaceutically acceptable salt thereof are disclosed. The formulations provide therapeutic plasma levels of the antihyperglycemic drug to a human patient over a 24 hour period after administration.

Claims

1. A method of treating a human diabetic patient with an oral solid sustained release tablet of metformin hydrochloride, comprising:

administering the sustained release tablet to the human diabetic patient once a day under fed conditions, wherein the sustained release tablet comprises (i) metformin hydrochloride and (ii) a sustained release material, wherein the tablet does not employ an expanding polymer, the sustained release tablet provides therapeutic plasma levels of said metformin to the human patient over a 12 to 24 hour period after administration; and

the sustained release tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37°

C.;

0-25% of the metformin is released after 2 hours;

10-45% of the metformin is released after 4 hours;

30-90% of the metformin is released after 8 hours;

not less than 50% of the metformin is released after 12 hours;

not less than 60% of the metformin is released after 16 hours and not less than 70% of the metformin is released after 20 hours.

2. The method as defined in claim 1 wherein the tablet exhibits the following in vitro dissolution profile when tested in a USP Type 2 apparatus at 75 rpms in 900 ml of a pH 7.5 phosphate buffer and 37°

C.;

0-15% of the metformin is released after 2 hours;

20-40% of the metformin is released after 4 hours;

45-90% of the metformin is released after 8 hours;

not less than 60% of the metformin is released after 12 hours;

not less than 70% of the metformin is released after 16 hours and

not less than 80% of the metformin is released after 20 hours.

3. The method of claim 1 wherein the tablet is administered with or after a meal.

4. The method of claim 1 wherein the tablet is administered with or after evening meal.

5. The method of claim 1 wherein the tablet is an osmotic tablet with a homogeneous osmotic core.