Controlled release levetiracetam formulations and methods for producing the same
View Patent ↗Pharmaceutical compositions in the form of tablets are disclosed including water-soluble active ingredients such as levetiracetam and a polymer component which primarily includes water-insoluble polymers comprising between 60% and 100% of the polymer component in the tablet core, preferably the entire polymer component in the tablet core. The pharmaceutical compositions can also include an extended-release coating including both water-soluble and water-insoluble polymers.
1. A pharmaceutical composition in the form of a tablet comprising a compressed tablet core comprising a water-soluble active ingredient comprising levetiracetam and a polymer component consisting essentially of a water-insoluble polymer comprising from between about 1 and 50 wt. % of said compressed tablet core, and comprising substantially the only polymer in said compressed tablet core, such that said compressed tablet core is free of any water-soluble polymer.
2. The pharmaceutical composition of claim 1 wherein said water-insoluble polymer comprises from between about 4 and 20 wt. % of said compressed tablet core.
3. The pharmaceutical composition of claim 2 wherein said water-insoluble polymer comprises about 12 wt. % of said compressed tablet core.
4. The pharmaceutical composition of claim 1 including an extended release coating surrounding said compressed tablet core.
5. The pharmaceutical composition of claim 4 wherein said extended release coating comprises from about 1 to 20 wt. % of said pharmaceutical composition.
6. The pharmaceutical composition of claim 5 wherein said extended release coating comprises from about 2 to 10 wt. % of said pharmaceutical composition.
7. The pharmaceutical composition of claim 6 wherein said extended release coating comprises about 6 wt. % of said pharmaceutical composition.
8. The pharmaceutical composition of claim 4 wherein said extended release coating includes a water-insoluble polymer selected from the group consisting of ethylcellulose, butylcellulose, cellulose acetate, cellulose acetate butyrate, ethylene vinyl acetate copolymer, polyvidone acetate, polyvinyl acetate, polyvinyl butyrate, polymethacrylate, ammonia methacrylate copolymer, and mixtures thereof.
9. The pharmaceutical composition of claim 8 wherein said water-insoluble polymer in said extended release coating comprises ethylcellulose.
10. The pharmaceutical composition of claim 4 wherein said extended release coating includes a water-soluble polymer selected from the group consisting of methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl pyrrolidone, polyvinyl alcohol, polyethylene glycol, and mixtures thereof.
11. The pharmaceutical composition of claim 10 wherein said water-soluble polymer in said extended release coating comprises hydroxypropylmethylcellulose.
12. The pharmaceutical composition of claim 4 wherein said extended release coating includes a water-soluble polymer and a water-insoluble polymer, and wherein the ratio of said water-soluble polymer to said water-insoluble polymer in said extended release coating ranges from 10:90 to 90:10.
13. The pharmaceutical composition of claim 12 wherein the ratio of said water-soluble polymer to said water-insoluble polymer in said extended release coating is from 30:70 to 70:30.
14. The pharmaceutical composition of claim 1 wherein said water-insoluble polymer is selected from the group consisting of ethyl cellulose, butyl cellulose, cellulose acetate, cellulose acetate butyrate, ethylene vinyl acetate copolymer, polyvidone acetate, polyvinyl acetate, polyvinyl butyrate, polymethacrylate, ammonia methacrylate copolymer, and mixtures thereof.
15. The pharmaceutical composition of claim 14 wherein said water-insoluble polymer is selected from the group consisting of ethylcellulose, polymethacrylates, ammonia methacrylate copolymer, and mixtures thereof.
16. The pharmaceutical composition of claim 15 wherein said water-insoluble polymer comprises ethylcellulose.
17. The pharmaceutical composition of claim 16 wherein said levetiracetam is present in an amount of about 83.3 wt. % of said compressed tablet core.
18. The pharmaceutical formulation of claim 16 wherein said compressed tablet core includes an inert diluent.
19. The pharmaceutical composition of claim 18 wherein said inert diluent comprises lactose.
20. The pharmaceutical composition of claim 19 wherein said lactose is present in an amount of between about 2 wt. % and 20wt. % of said core.
21. The pharmaceutical composition of claim 16 wherein said compressed tablet core includes a lubricant.
22. The pharmaceutical composition of claim 21 wherein said lubricant comprises magnesium stearate.
23. The pharmaceutical composition of claim 22 wherein said magnesium stearate is present in an amount of between about 0.5 wt. % and 2 wt. % of said compressed tablet core.
24. The pharmaceutical composition of claim 16 wherein said compressed tablet core includes a glidant.
25. The pharmaceutical composition of claim 24 wherein said glidant comprises colloidal silicon dioxide.
26. The pharmaceutical composition of claim 16 wherein said ethylcellulose comprises from between about 4 wt. % and 20 wt. % of the compressed tablet core.
27. The pharmaceutical composition of claim 26 wherein said ethylcellulose comprises about 12 wt. % of said compressed tablet core.
28. The pharmaceutical composition of claim 27 wherein said compressed tablet core includes an inert diluent comprising lactose, in an amount of between about 2 wt. % and 20 wt. % of said core.
29. The pharmaceutical composition of claim 28 wherein said compressed tablet core includes a lubricant comprising magnesium stearate in an amount between about 0.5 wt. % and 2 wt. % of said compressed tablet core.
30. The pharmaceutical composition of claim 29 wherein said compressed tablet core includes a glidant comprising colloidal silicon dioxide.