High dose orally dissolvable/disintegrable lyophilized dosage form

1 . An orally dissolvable/disintegrable lyophilized dosage form comprising:

a protected granulate comprising at least one first active ingredient and at least one protective granulation binder; and

a matrix, said dosage form being a lyophilized, orally dissolvable/disintegrable dosage form adapted for direct oral dosing in the mouth of a patient.

2 . The dosage form of claim 1 , wherein said active ingredient is a sulfur containing compound.

3 . The dosage form of claim 1 , wherein said active ingredient is modafinil, famotidine or fentanyl and/or salts thereof.

4 . The dosage form of claim 1 , wherein said protective granulation binder will dissolve at basic pH.

5 . The dosage form of claim 1 , wherein said protective granulation binder will dissolve at neutral pH.

6 . The dosage form of claim 1 , wherein said protective granulation binder will dissolve at acidic pH.

7 . The dosage form of claim 1 , wherein said protective granulation binder will dissolve at a pH of about 7 or less.

8 . The dosage form of claim 1 , wherein said matrix comprises at least one of a binder, lyophilization binder, filler, sugar, artificial sweetener, polymer, flavoring agent, taste masking material, active ingredient, coloring agent, lubricant, effervescent disintegrant, non-effervescent disintegrant, viscosity modifier, surfactant, and buffer.

9 . The dosage form of claim 1 , further comprising at least one flavor selected to be complimentary with the active ingredient such as to provide a pleasant organoleptic sensation to the mouth.

10 . The dosage form of claim 9 , wherein said flavor is selected from the group consisting of fruit punch, orange, banana, cherry, mint, bubble gum, grape, paradise punch, peach, mango, and combinations thereof.

11 . The dosage form of claim 1 , wherein said active ingredient is present in an amount of about 0.01 mg to about 2 g by weight of the dosage form.

12 . The dosage form of claim 1 , wherein said active ingredient is present in an amount of about 0.05 mg to about 1 g by weight of the dosage form.

13 . The dosage form of claim 1 , wherein said active ingredient is present in an amount of about 1 mg to about 800 mg by weight of the dosage form.

14 . The dosage form of claim 1 , wherein said active ingredient is present in an amount of about 85 mg to about 425 mg.

15 . The dosage form of claim 1 , wherein said active ingredient is present in an amount of about 50 mg or greater.

16 . The dosage form of claim 1 , wherein said protected granulate is provided in an amount of about 0.1% to about 90% by weight of the dosage form.

17 . The dosage form of claim 1 , wherein said protected granulate is provided in an amount of about 1% to about 80% by weight of the dosage form.

18 . The dosage form of claim 1 , wherein said protected granulate further comprises at least one excipient.

19 . The dosage form of claim 18 , wherein said excipient is a binder, pH adjusting substance, filler, disintegrant, solid support or buffer.

20 . The dosage form of claim 1 , wherein said protective granulation binder is provided in an amount of about 0.1% to about 50%, based on the weight gain of said protected granulate.

21 . The dosage form of claim 1 , wherein said protective granulation binder is provided in an amount of about 2% to about 25%, based on the weight gain of said granulate.

22 . The dosage form of claim 1 , wherein said protective granulation binder is provided in an amount of about 5% to about 15% based on the weight gain of said granulate.

23 . The dosage form of claim 1 , wherein said protective granulate has an average particle size of about 1 to about 1000 microns.

24 . The dosage form of claim 1 , wherein said protective granulate has an average particle size of about 10 to about 800 microns.

25 . The dosage form of claim 1 , wherein said protective granulate has an average particle size of about 20 to about 600 microns.

26 . The dosage form of claim 1 , wherein said protective granulate has a particle size distribution wherein no more than about 10% are less than 45 microns and no more than about 10% are larger than 600 microns.

27 . The dosage form of claim 1 , wherein said protective granulate has a particle size distribution wherein no more than about 10% are less than 75 microns and no more than about 10% are larger than 425 microns.

28 . The dosage form of claim 1 , wherein said active ingredient is generally water insoluble.

29 . A method of making an orally dissolvable/disintegrable lyophilized dosage for direct oral dosing form comprising the steps of:

granulating at least one active ingredient and at least one protective granulation binder to produce a protected granulate;

mixing said protected granulate with a matrix and a lyophilization solvent to form a blend; and

lyophilizing said blend to form a dosage form.

30 . The method of claim 29 , further comprising the step of placing said blend into a portion of a container prior to lyophilization and sealing said dosage form into said container after lyophilization.

31 . The method of claim 29 , further comprising the step of adding an organoleptically complimentary pleasant flavor during mixing said protected granulate with a matrix to form a mixture.

32 . The method of claim 31 , wherein said flavor is selected from the group consisting of fruit punch, orange, banana, cherry, mint, bubble gum, grape, paradise punch, peach, mango, and combinations thereof.

33 . A method of treating a patient comprising the steps of:

placing an orally dissolvable/disintegrable lyophilized dosage form of claim 1 into the mouth of a patient in need of treatment;

allowing said dosage form to disintegrate/dissolve sufficiently in the mouth of a patient to form a solution, suspension or slurry; and

swallowing said solution suspension or slurry.