Magnesium plus interactive agent delivery

• US 6,887,492 B2
• Filed: 12/14/2001
• Issued: 05/03/2005
• Est. Priority Date: 12/14/2000
• Status: Expired due to Term

• Current Assignee: NBTY Aquisition LLC (Nestle SA)
• Original Assignee: Leiner Health Services Corp. (Nestle SA)
• Inventors: Kay, Robert A., Thomas, Larry K.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Sheikh, Humera N.
• Application Number:
  US10/017,478
• Publication Number:
  US 20030129228A1
• Time in Patent Office: 1,236 Days
• Field of Search: 424/474, 424/464, 424/468, 424/463, 424/451, 424/457, 424/472, 424/469, 424/489
• US Class Current: 424/474
• CPC Class Codes: A61K 33/06 Aluminium, calcium or magnesium; Compounds thereof , e.g. clay
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/5084 Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077

Abstract

The present invention is an orally administered pharmaceutical composition that provides for the controlled release of magnesium. The composition has an interactive agent component and a magnesium component which has an enteric coating that controls the release of the magnesium until the composition is in the small intestine or colon. The other component is released in the stomach and is substantially absorbed prior to the release of the magnesium component. Normally, the interactive agent component decreases the absorption of magnesium when the two components are released simultaneously in the gastrointestinal tract.

Claims

1. A unit dosage form tablet or capsule composition for oral administration comprising

a) an enteric coated magnesium component having an active ingredient consisting essentially of one or more magnesium compounds, wherein said enteric coating is a polymeric release-controlling agent which substantially prevents release of said one or more magnesium compounds until passage out of the stomach and into the intestine of the host, and wherein said release-controlling agent has a pH dissolution point of from about 5 to about 8;

and

b) an uncoated calcium component having an active ingredient consisting essentially of one or more calcium compounds;

wherein substantially all of said calcium component is released before passage into said intestine of said host, and wherein the ratio of said calcium component to said magnesium component is from 1;

5 to 5;

1.

2. A unit dosage form tablet or capsule composition according to claim 1, wherein said release-controlling agent has a pH dissolution point of from about 6.5 to about 7.2.

3. A unit dosage form tablet or capsule composition according to claim 1, wherein the ratio of said calcium component to said magnesium component is from 2:

1 to 3;

1.

4. A unit dosage form tablet or capsule composition according to claim 1, wherein said enteric coating is applied by contacting said magnesium component with an aqueous suspension or an organic solvent.

5. A unit dosage form tablet or capsule composition according to claim 1, wherein said enteric coating is selected from the group consisting of hydroxypropyl methylcellulose phthalate (“

HPMCP”

) and a methacrylic acid copolymer.

6. A unit dosage form tablet or capsule composition according to claim 4, wherein said aqueous suspension is polyvinylacetate phthalate or cellulose acetate phthalate or a mixture thereof in combination with a plasticizing agent.

7. A unit dosage form tablet or capsule composition according to claim 1, wherein said magnesium component of said composition is one of a core, a layer or granules.

8. A unit dosage form tablet or capsule composition according to claim 7, wherein said one or more magnesium compounds is selected from the group consisting of magnesium citrate, magnesium gluconate, magnesium oxide, magnesium carbonate, magnesium hydroxide, magnesium sulfate, magnesium phosphate, magnesium aspartate and combinations thereof.

9. A unit dosage form tablet or capsule composition according to claim 1, wherein said composition is selected from the group consisting of a direct compression tablet, a hard shell capsule, a layered tablet or a dry coated tablet.

10. A unit dosage form tablet or capsule composition according to claim 1, wherein said one or more calcium compounds is calcium carbonate, calcium citrate, calcium propionate, calcium gluconate, calcium sulfate, calcium ascorbate or combinations thereof.

11. A unit dosage form tablet or capsule composition for oral administration comprising:

a) an enteric coated magnesium component having an active ingredient consisting essentially of one or more magnesium compounds selected from the group consisting of magnesium citrate, magnesium gluconate, magnesium oxide, magnesium carbonate, magnesium hydroxide, magnesium sulfate, magnesium phosphate, magnesium aspartate and combinations thereof, wherein said magnesium component has a pH sensitive enteric polymer coating having a pH dissolution point of from about 5 to about 8; and

b) an uncoated calcium component having an active ingredient consisting essentially of one or more calcium compounds selected from the group consisting of calcium carbonate, calcium citrate, calcium propionate, calcium gluconate, calcium sulfate, calcium ascorbate and combinations thereof,

wherein the ratio of said calcium component to said magnesium component is from 1;

5 to 5;

1.

12. A method for delivering to a host magnesium and calcium, said method comprising:

ingesting a unit dosage form tablet or capsule composition comprising;

a) an enteric coated magnesium component having an active ingredient consisting essentially of one or more magnesium compounds selected from the group consisting of magnesium citrate, magnesium gluconate, magnesium oxide, magnesium carbonate, magnesium hydroxide, magnesium sulfate, magnesium phosphate, magnesium aspartate and combinations thereof, wherein said enteric coating is a pH sensitive enteric polymer coating having a pH dissolution point of from about 5 to about 8; and

b) an uncoated calcium component having an active ingredient consisting essentially of one or more calcium compounds;

wherein substantially all of said calcium component is released before passage into said intestine of said host and substantially all of said magnesium component is released after passage out of the stomach and into the intestine of the host, and wherein the ratio of said calcium component to said magnesium component is from 1;

5 to 5;

1.

13. A method for delivering to a host magnesium and calcium according to claim 12, wherein the ratio of said calcium component to said magnesium component is from 2:

1 to 3;

1.

14. A method for delivering to a host magnesium and calcium according to claim 12, wherein said one or more calcium compounds is calcium carbonate, calcium citrate, calcium propionate, calcium gluconate, calcium sulfate, calcium ascorbate or combinations thereof.