Liquid pharmaceutical composition

• US 9,827,231 B2
• Filed: 07/20/2016
• Issued: 11/28/2017
• Est. Priority Date: 03/19/2014
• Status: Active Grant

• Current Assignee: Ferring International Center SA (Ferring Holding SA)
• Original Assignee: Ferring International Center SA (Ferring Holding SA)
• Inventors: Nam, Bong Gil
• Primary Examiner(s): Heyer, Dennis
• Application Number:
  US15/214,768
• Publication Number:
  US 20160324837A1
• Time in Patent Office: 496 Days
• Field of Search: None
• 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 31/194 having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• CPC Class Codes: A61K 31/4402 only substituted in position 2, e.g. pheniramine, bisacodyl
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 33/08 Oxides; Hydroxides
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• 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: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 1/10 Laxatives

Abstract

The present invention provides a physically and chemically stable pharmaceutical liquid composition including sodium picosulfate, magnesium oxide, citric acid and malic acid and methods of making and using such a composition.

Claims

1. A pharmaceutical liquid composition comprising sodium picosulfate, magnesium oxide, citric acid and malic acid.

2. The pharmaceutical liquid composition of claim 1, wherein from 50 mL to 500 mL of the composition provides a single effective dose.

3. The pharmaceutical liquid composition of claim 1, wherein from 150 mL to 200 mL of the composition provides a single effective dose.

4. The pharmaceutical liquid composition of claim 1, wherein the pharmaceutical liquid composition is aqueous.

5. The pharmaceutical liquid composition of claim 1, wherein pH of the pharmaceutical liquid composition ranges from 4.1 to 5.4.

6. The pharmaceutical liquid composition of claim 1, wherein the pharmaceutical liquid composition further comprises an excipient and purified water.

7. The pharmaceutical liquid composition of claim 6, wherein the excipient is at least one excipient selected from the group consisting of a pH adjuster, a stabilizer, a preservative, a sweetener and a fragrance ingredient.

8. The pharmaceutical liquid composition of claim 7, comprising a pH adjuster.

9. The pharmaceutical liquid composition of claim 8, wherein the pH adjuster is an alkalizing agent.

10. The pharmaceutical liquid composition of claim 9, wherein the alkalizing agent is at least one alkalizing agent selected from the group consisting of sodium hydroxide, potassium hydroxide, sodium bicarbonate, ammonia solution, potassium citrate, triethanolamine and sodium citrate.

11. The pharmaceutical liquid composition of claim 1, wherein the sodium picosulfate, magnesium oxide, citric acid and malic acid have a weight ratio of 0.003 to 0.009:

1 to 3;

3.5 to 10.5;

0.01 to 13 (sodium picosulfate;

magnesium oxide;

citric acid;

malic acid).

12. The pharmaceutical liquid composition of claim 1, comprising about 0.005 parts by weight of sodium picosulfate, about 1.75 parts by weight of magnesium oxide, about 6 parts by weight of citric acid, about 4.19 parts by weight of malic acid, and about 75 parts by weight of water.

13. The pharmaceutical liquid composition of claim 1, wherein the composition has a pH in the range from about 4.1 to about 5.4, and wherein, when the composition is left for 24 months at room temperature, Substance A related to sodium picosulfate is generated in an amount of about 2.0 wt. % or less, and precipitation either does not occur or occurs at about 5.0 vol. % or less.

14. A method of treatment for cleansing the large intestine of a subject in need of such treatment, comprising administering to the subject an effective amount of the pharmaceutical liquid composition according to claim 1.

15. The method of claim 14, wherein the cleansing is performed to prepare the subject prior to surgery, colonoscopy or colon X-ray inspection.

16. A pharmaceutical composition comprising sodium picosulfate, magnesium oxide, citric acid and malic acid.

17. A method of preparing a pharmaceutical liquid composition comprising dissolving ingredients comprising sodium picosulfate, magnesium oxide, citric acid and malic acid.

18. The method of claim 17, comprising dissolving the pharmaceutical composition in water.

19. A pharmaceutical liquid composition prepared by the method of claim 17.

20. A pharmaceutical liquid composition prepared by the method of claim 18.