SUBLINGUAL APOMORPHINE
The invention features sublingual formulations of apomorphine and apomorphine prodrugs, and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.
1 .- 2 . (canceled)
3 . A pharmaceutical composition in unit dosage form formulated for sublingual administration, wherein said unit dosage form is a film comprising from 2 mg to 40 mg of an acid addition salt of apomorphine present as a solid solution with a polymer, and wherein said film is impregnated with particles comprising a pH neutralizing agent.
4 . The pharmaceutical composition of claim 3 , wherein said pH neutralizing agent is an inorganic base.
5 . The pharmaceutical composition of claim 4 , wherein said inorganic base is sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, sodium phosphate monobasic, sodium phosphate dibasic, sodium phosphate tribasic, potassium phosphate monobasic, potassium phosphate dibasic, potassium phosphate tribasic, or a mixture thereof.
6 . The pharmaceutical composition of claim 5 , wherein said inorganic base is sodium phosphate monobasic, sodium phosphate dibasic, sodium phosphate tribasic, potassium phosphate monobasic, potassium phosphate dibasic, potassium phosphate tribasic, or a mixture thereof.
7 . The pharmaceutical composition of claim 3 , wherein said film further comprises an antioxidant.
8 . The pharmaceutical composition of claim 7 , wherein said antioxidant is selected from the group consisting of thiols, sulphoximines, metal chelators, sodium metabisulfite, vitamins, phenols, benzoates, uric acid, mannose, propyl gallate, selenium, stilbenes, and combinations thereof.
9 . The pharmaceutical composition of claim 8 , wherein said antioxidant is sodium metabisulfite.
10 . The pharmaceutical composition of claim 8 , wherein said antioxidant is a metal chelator.
11 . The pharmaceutical composition of claim 10 , wherein said metal chelators is EDTA.
12 . The pharmaceutical composition of claim 3 , wherein said film further comprises a plasticizer selected from the group consisting of glycerol, propylene glycol, fatty acid esters, sorbitan esters, citric acid esters, PEG 400, polyvinyl methyl ether, triacetin; mannitol, xylitol, and sorbitol.
13 . The pharmaceutical composition of claim 12 , wherein said plasticizer is glycerol.
14 . The pharmaceutical composition of claim 3 , wherein said film comprises from 2 to 40 mg of said acid addition salt of apomorphine.
15 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 10±3 mg of said acid addition salt of apomorphine.
16 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 15±3 mg of said acid addition salt of apomorphine.
17 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 22±4 mg of said acid addition salt of apomorphine.
18 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 27±4 mg of said acid addition salt of apomorphine.
19 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 30±5 mg of said acid addition salt of apomorphine.
20 . The pharmaceutical composition of claim 14 , wherein said mucoadhesive film comprises 35±5 mg of said acid addition salt of apomorphine.
21 . A method of treating a patient having Parkinson's disease comprising administering to said patient an effective amount of the pharmaceutical composition of claim 3 .
22 . The method of claim 21 , wherein said administering alleviates “off” symptoms of Parkinson's disease.