Uncoated pharmaceutical reaction tablet

• US 5,064,656 A
• Filed: 08/28/1990
• Issued: 11/12/1991
• Est. Priority Date: 11/14/1989
• Status: Expired due to Term

• Current Assignee: Dr. Gergely & Co.
• Original Assignee: Dr. Gergely & Co.
• Inventors: Gergely, Thomas, Gergely, Irmgard, Gergely, Gerhard
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): BROUILLETTE, D GABRIELLE
• Application Number:
  US07/574,585
• Time in Patent Office: 441 Days
• Field of Search: 424/466, 424/464, 424/465, 424/463
• US Class Current: 424/463
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence

Abstract

An uncoated compressed tablet which is used for the preparation of an orally applicable aqueous suspension or solution of a pharmaceutically active substance contains a mixture of the pharmaceutically active substance, a swelling disintegrant and an effervescent system. The weight ratio of the disintegrant to the effervescent system is from 0.1:1 to 4:1.

Claims

1. Uncoated, compressed tablet for the preparation of an orally applicable aqueous suspension or solution of a pharmaceutically active substance, comprising in a mixture with one another at least one pharmaceutically active substance, a disintegrant effective amount of at least one water insoluble, water swellable disintegrant which is starch or crosslinked polyvinylpolypyrrolidone and an effervescent effective amount of an effervescent system which generates a gas upon contact with water comprising a first constituent selected from the group consisting of L-tartaric acid, fumaric acid, citric acid, malic acid, monosodium citrate and adipic acid and a second constituent which is an alkali metal or alkaline earth metal carbonate or bicarbonate, wherein the weight ratio of disintegrant to said system is from 0.1:

1 to 4;

1.

2. Tablet according to claim 1, wherein the weight ratio of disintegrant to reactants is from 0.3 :

1 to 1 ;

1.

3. Tablet according to claim 1, wherein at least one constituent dissolves more slowly in water than any one of the disintegrants absorbs water.

4. Tablet according to claim 1, wherein the disintegrants and constituents together account for 25 to 75 percent by weight of the tablet.

5. Tablet according to claim 4, wherein the disintegrants and constituents account for 33 to 60 percent by weight of the tablet.

6. Tablet according to claim 1, wherein one of the constituents is selected from the group of alkali and alkaline earth metal carbonates and bicarbonates, and wherein at least 50% of said constituent have a particle size of more than 0.05 mm.

7. Tablet according to claim 6, wherein at least 50% of said reactant have a particle size of more than 0.1 mm.

8. Tablet according to claim 1, wherein one of the constituents is L-tartaric acid of which at least 50% have a particle size of between 0.2 and 0.5 mm.

9. Tablet according to claim 1, wherein one of the reactants is fumaric acid of which at least 50% have a particle size of less than 0.1 mm.

10. Tablet according to claim 1, wherein one of the reactants is citric acid of which at least 50% have a particle size of more than 0.3 mm.

11. Tablet according to claim 1, wherein one of the constituents is selected from the group of monosodium citrate and adipic acid and wherein at least 50% of said constituent have a particle size of 0.05 to 0.2 mm.

12. Tablet according to claim 1, wherein the particles of at least one constituent are coated with a slowly soluble, physiologically acceptable substance.

13. Tablet according to claim 12, wherein said slowly soluble substance is selected from long-chain polyvinylpyrrolidone and polyethylene glycol.

14. Tablet according to claim 1, wherein said disintegrant is selected from the group of crosslinked polyvinylpolypyrrolidone and starch.

15. Tablet according to claim 14, wherein crosslinked polyvinylpolypyrrolidone and starch are both present in a ratio of from 1 :

0.25 to 1 ;

3.0.

16. Tablet according to claim 1, wherein said disintegrant is coated with 1 to 20 percent by weight of a physiologically acceptable compound being soluble in a solvent which does not swell the disintegrant.

17. Tablet according to claim 16, wherein said disintegrant is coated with 3 to 10 percent by weight of said physiologically acceptable compound.

18. Tablet according to claim 16, wherein said compound is selected from the group of edible organic acids and long chain non-crosslinked polyvinylpyrrolidone.

19. Tablet according to claim 1, wherein said disintegrant is anchored to the surface of the particles of at least one of the constituents.

20. Tablet according to claim 17, wherein said compound is selected from the group of edible organic acids and long-chain non-crosslinked polyvinylpyrrolidone.

21. Tablet according to claim 16, wherein said disintegrant is anchored to the surface of the particles of at least one of the reactants.

22. Tablet according to claim 1 wherein the constituents of the effervescent system and the disintegrants are such that the reaction of the effervescent system constituents to generate a gas upon contact with water occurs more slowly than the rate of water absorption by the disintegrant.