Fast release paracetamol tablets
View Patent ↗A pharmaceutical composition such as a swallow tablet or capsule formulation is described comprising paracetamol, calcium carbonate, at least one binding agent and at least one disintegrating agent in the form of a granulate, optionally combined with one or more pharmaceutically acceptable extragranular components.
1. A pharmaceutical composition comprising paracetamol, calcium carbonate in a ratio of paracetamol to calcium carbonate of 3.0: 1.0 to 30.0: 1.0, at least one binding agent, and at least one disintegrating agent, as intragranular components in the form of a granulate, and wherein at least 60% of the paracetamol is released from the composition at 180 seconds as determined by a dissolution method that utilizes a USP paddle apparatus rotating at 30 rpm, employing 900 ml of 0.05M HCl, following storage of the composition for ten days in an open Petri dish at 40° C.±2° C., and 75% RH±5% RH.
2. A pharmaceutical composition according to claim 1 wherein the intragranular binding agent comprises a starch, a polymer, a cellulose derivative or a combination of two or more thereof.
3. A pharmaceutical composition according to claim 2 wherein the intragranular binding agent comprises a cellulose derivative which is microcrystalline cellulose.
4. A pharmaceutical composition according to claim 2 wherein the intragranular binding agent comprises a starch wherein the starch is corn (or maize) starch, modified corn starch, wheat starch, modified wheat starch, potato starch or pregelatinized starch, or a combination of two or more thereof with the proviso that if the binding agent comprises a mixture of corn (or maize) starch and pregelatinized starch then the weight ratio of pregelatinized starch to corn starch is greater than from about 3.0 to 1.0.
5. A pharmaceutical composition according to claim 1 wherein the intragranular binding agent comprises pregelatinized starch.
6. A pharmaceutical composition according to claim 2 wherein the starch is present in an amount ranging from about 5.0% to about 20.0% by weight of the composition.
7. A pharmaceutical composition according to claim 2 wherein the intragranular binding agent comprises a polymer selected from povidone (PVP), polyvinyl alcohol (PVA), polyethylene oxide, polaxamer, polymethacrylate, a carbomer, polyethylene glycol (PEG) and calcium polycarbophil, or a combination of two or more thereof, present in an amount ranging from about 1.5% to about 5.0% by weight of the composition.
8. A pharmaceutical composition according to claim 2 wherein the intragranular binding agent comprises a cellulose derivative selected from hydroxypropyl cellulose (HPC), hydroxypropylmethyl cellulose (HPMC), microcrystalline cellulose (MCC), carboxymethylcellulose (MC), and sodium carboxymethylethyl cellulose; or a combination of two or more thereof.
9. A pharmaceutical composition according to claim 1 wherein the intragranular binding agent comprises a first binding agent and a second binding agent.
10. A pharmaceutical composition according to claim 9 wherein the first binding agent is pregelatinized starch in an amount ranging from about 5.0% to about 20.0% by weight of the composition and the second binding agent is PVP in an amount ranging from about 1.5% to about 15.0% by weight of the composition.
11. A pharmaceutical composition according to claim 1 wherein the intragranular disintegrating agent comprises a super disintegrant selected from sodium starch glycolate, the sodium salt of carboxymethyl starch, cross-linked polyvinyl pyrrolidone, croscarmellose and the sodium salt of carboxymethyl cellulose.
12. A pharmaceutical composition according to claim 11 wherein the super disintegrant is cross-linked polyvinyl pyrrolidone.
13. A pharmaceutical composition according to claim 11 wherein the super disintegrant is in an amount ranging from about 0.5 to about 5.0% by weight of the composition.
14. A pharmaceutical composition according to claim 1 wherein the intragranular binding agent and the intragranular disintegrating agent are the same excipient.
15. A pharmaceutical composition according to claim 14 wherein the said same excipient is pregelatinized starch.
16. A pharmaceutical composition according to claim 15 wherein the pregelatinized starch is present in an amount ranging from about 5.0 to about 20.0% by weight of the composition.
17. A pharmaceutical composition according to claim 1 wherein the intragranular paracetamol is present in an amount ranging from about 60.0% to about 80.0% by weight of the composition.
18. A pharmaceutical composition according to claim 1 wherein the intragranular calcium carbonate is present in an amount ranging from about 5.0% to about 20.0% by weight of the composition.
19. A pharmaceutical composition according to claim 1 comprising at least one extragranular component.
20. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises a binding agent in an amount ranging from about 0.1% to about 10.0% by weight of the intragranular binding agent.
21. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises calcium carbonate in an amount ranging from about 0.1% to about 10.0% by weight of the intragranular calcium carbonate.
22. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises paracetamol in an amount ranging from about 0.1% to about 10.0% by weight of the intragranular paracetamol.
23. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises a super disintegrant in an amount ranging from about 0.1% to about 5.0% by weight of the composition.
24. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises a hydrophilic colloid.
25. A pharmaceutical composition according to claim 24 wherein the hydrophilic colloid is selected from alginic acid, carrageenan, gellan, pectin, agar or a combination of two or more thereof.
26. A pharmaceutical composition according to claim 25 wherein the hydrophilic colloid comprises alginic acid.
27. A pharmaceutical composition according to claim 24 wherein the hydrophilic colloid is present in an amount ranging from about 1.0% to about 5.0% by weight of the composition.
28. A pharmaceutical composition according to claim 19 wherein the extragranular component comprises at least one pharmaceutically active agent, pharmaceutically acceptable adjuvant selected from caffeine, colorant, dye, flavorant, sweetener, lubricant, glidant, or a combination of two or more thereof.
29. A pharmaceutical composition according to claim 28 in a unit dosage form.
30. A pharmaceutical composition according to claim 29 in the form of a swallow tablet.
31. A pharmaceutical composition according to claim 7 wherein the intragranular binding agent is PEG 3350.