Liquid formulation of metformin

• US 6,890,957 B2
• Filed: 03/06/2003
• Issued: 05/10/2005
• Est. Priority Date: 08/07/2000
• Status: Expired due to Term

• Current Assignee: Ranbaxy Signature, LLC (Sun Pharmaceutical Industries Limited)
• Original Assignee: Ranbaxy Laboratories Limited (Sun Pharmaceutical Industries Limited)
• Inventors: Chandran, Ravi, Gogia, Ashish
• Primary Examiner(s): Cook, Rebecca
• Application Number:
  US10/382,442
• Publication Number:
  US 20030149111A1
• Time in Patent Office: 796 Days
• Field of Search: 514/634, 514/635
• US Class Current: 514/634
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• 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 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention is directed to a liquid formulation of metformin or its pharmaceutically acceptable salts thereof. The liquid pharmaceutical composition comprises a therapeutically effective amount of metformin or its pharmaceutically acceptable salt, in a liquid carrier, which may also include a sweetener that does not increase the blood glucose level of a subject after ingestion thereof. In one embodiment, it may also include alkyl hydroxyethylcellulose, and/or a polyhydroxy alcohol. In another embodiment, the carrier may contain a sweetener, mineral acid, and bicarbonate salt maintained at a pH of 4.0 to 9.0. It is useful for treating hyperglycemia and diabetes.

Claims

1. A liquid pharmaceutical composition for oral administration which comprises a therapeutically effective amount of metformin or its pharmaceutically acceptable salt;

a sweetener that does not increase the blood glucose level of a subject after ingestion thereof;

a polyhydroxy alcohol present in an amount of about 15 to about 55% by weight;

a mineral acid and bicarbonate salt both present in sufficient amounts to maintain the pH of the composition in the range of about 4.0 to about 9.0; and

a pharmaceutically acceptable liquid carrier.

2. The liquid pharmaceutical composition according to claim 1, where the pharmaceutically acceptable carrier is water.

3. The pharmaceutical composition of claim 1 wherein the sweetener is present in amounts ranging from about 50% to about 70% by weight.

4. The liquid pharmaceutical composition of claim 3, wherein the sweetener is present in amounts ranging from about 55% to about 65% by weight.

5. The liquid pharmaceutical composition of claim 1, further comprising alkyl hydroxyethylcellulose.

6. The liquid pharmaceutical composition of claim 5, wherein the alkyl hydroxyethylcellulose is present in amounts ranging from 0.08% to about 0.2% by weight.

7. The liquid pharmaceutical composition of claim 1, wherein the polyhydroxy alcohol is present in amounts ranging from about 15% to about 40% by weight.

8. The liquid pharmaceutical composition of claim 5, wherein the alkyl group in alkyl hydroxyethylcellulose contains 2 to 10 carbon atoms.

9. The liquid pharmaceutical composition of claim 1, wherein the sweetener is a sugar alcohol or non-nutritive sweetener.

10. The liquid pharmaceutical composition of claim 1, wherein the polyhydroxy alcohol contains 2 to 6 carbon atoms and contains 2 to 6 hydroxy groups.

11. The liquid pharmaceutical composition of claim 1, wherein the polyhydroxy alcohol is a polymer having a molecular weight ranging from 200 to 2000 daltons and has a repeating unit of 2 to 6 carbon atoms and the repeating unit contains 2 to 6 hydroxy groups.

12. The liquid pharmaceutical composition according to claim 1 wherein the mineral acid is hydrochloric acid, nitric acid, or sulfuric acid.

13. The liquid pharmaceutical composition according to claim 12 herein the mineral acid is hydrochloric acid.

14. The liquid pharmaceutical composition according to claim 1 herein the pH ranges from about 4.2 to about 7.0.

15. The liquid pharmaceutical composition according to claim 1 wherein the bicarbonate salt is potassium bicarbonate.