Pharmaceutical formulation for producing rapidly disintegrating tablets
A pharmaceutical formulation in the form of agglomerates comprising a) 60-97% by weight of sugar or sugar alcohols, b) 1-25% by weight of crosslinked polyvinylpyrrolidone, c) 1-15% by weight of water-insoluble, film-forming polymers, d) 0-15% by weight of water-soluble polymers and e) 0-15% by weight of further pharmaceutically customary excipients, the sum of the components a) to e) being 100% by weight.
1. A pharmaceutical formulation comprising agglomerates of:
a) 60% to 97% by weight of sugar or sugar alcohols;
b) 1% to 25% by weight of crosslinked polyvinylpyrrolidone;
c) 1% to 15% by weight of water-insoluble, film-forming polymers;
d) 0% to 15% by weight of water-soluble polymers; and
e) 0% to 15% by weight of further pharmaceutically acceptable excipients, wherein the sum of a), b), c), d), and e) equals 100% by weight, and the mean particle size of said agglomerates is in the range of from 100 μm to 600 μm.
2. The formulation of claim 1 , wherein said sugar alcohol is mannitol, erythritol, or mixtures thereof.
3. The formulation of claim 1 , wherein said crosslinked polyvinylpyrrolidone comprises particles having a mean size of less than 50 μm.
4. The formulation of claim 1 , wherein the hydration capacity of said crosslinked polyvinylpyrrolidone is greater than 6.5 g/g.
5. The formulation of claim 1 , wherein said water-insoluble film-forming polymer is polyvinyl acetate.
6. The formulation of claim 1 , wherein said water-insoluble film-forming polymer is polyvinyl acetate in the form of an aqueous dispersion.
7. The formulation of claim 1 , wherein said water-soluble polymer is polyvinylpyrrolidone.
8. The formulation of claim 1 , wherein said further pharmaceutically acceptable excipients are acidifying agents, sweeteners, flavors, flavor enhancers, colorants, thickeners, surfactants, and/or finely divided pigments.
9. The formulation of claim 1 , comprising agglomerates of
a) 70% to 95% by weight of sugar or sugar alcohols;
b) 2% to 15% by weight of crosslinked polyvinylpyrrolidone;
c) 1% to 10% by weight of water-insoluble, film-forming polymers;
d) 0% to 2% by weight of water-soluble polyvinylpyrrolidone; and
e) 0% to 15% by weight of further pharmaceutically acceptable excipients.
10. The formulation of claim 1 , comprising agglomerates of
a) 75% to 95% by weight of mannitol or erythritol or a mixture thereof;
b) 3% to 10% by weight of crosslinked polyvinylpyrrolidone;
c) 1% to 10% by weight of polyvinyl acetate;
d) 0% to 2% by weight of water-soluble polyvinylpyrrolidone; and
e) 0% to 15% by weight of further pharmaceutically acceptable excipients.
11. A tablet comprising the formulation of claim 1 , said tablet having a disintegration time of less than 30 seconds in an aqueous medium.
12. The tablet of claim 11 , wherein said tablet has a hardness greater than 50 N.
13. The tablet of claim 11 , wherein said tablet comprises from 20% to 99% by weight, based on the total tablet weight, of the formulation of claim 1 .
14. The tablet of claim 11 , wherein said tablet comprises further excipients.
15. A process for preparing the formulation of claim 1 comprising agglomerating said sugar or sugar alcohol and said crosslinked polyvinylpyrrolidone with an aqueous dispersion of said water-insoluble, film-forming polymers, wherein said sugar or sugar alcohol comprises finely divided particles.
16. The process of claim 15 , wherein said aqueous dispersion of the water-insoluble, film-forming polymers further comprises suspended crosslinked polyvinylpyrrolidone.
17. The process of claim 15 , wherein said agglomeration is effected in a fluidized-bed granulator, a mixer, or a spray tower.