Sublingual or buccal dosage forms comprising antioxidants for treatment of central nervous system disorders
Sublingual or buccal dosage forms comprise at least one antioxidant compound, such as N-acetyl cysteine (NAC), or a pharmaceutically acceptable salt thereof. The sublingual or buccal dosage forms are administered for treating central nervous system (CNS) disorders, such as traumatic brain injury or stroke.
1 . A sublingual or buccal dosage form comprising:
N-acetylcysteine (NAC) or pharmaceutically salt thereof;
one or more water-soluble polymers or plasticizers; and
one or more masking agents effective to alleviate odor or taste of NAC, wherein said one or more masking agents is present in an amount from 0.05% to 5% by weight.
2 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises NAC in an amount from 20 to 2000 mg/mL.
3 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises NAC in an amount up to 120 mg of NAC.
4 . The sublingual or buccal dosage form of claim 1 , wherein the one or more masking agents is present in an amount that alleviates bitter taste and/or an aftertaste of bitterness.
5 . The sublingual or buccal dosage form of claim 1 , wherein the one or more masking agents further comprises menthol.
6 . The sublingual or buccal dosage form of claim 5 , wherein the menthol is present in an amount from 0.01% to 1% by weight.
7 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises at least one water-soluble polymer, and the at least one water-soluble polymer comprises hydroxypropyl methylcellulose (HPMC) E3, HPMC E5, HPMC E15, HPMC K-3, Methyl cellulose A-3, Methyl cellulose A-6, Methyl cellulose A-15, Pullulan, carboxymethylcellulose, polyvinylpyrrolidone (PVP) K-90, pectin, gelatin, sodium, alginate, hydroxypropyl cellulose, polyvinyl alcohol, maltodextrins, or a combination thereof.
8 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises at least one plasticizer, and the at least one plasticizer comprises glycerol, dibutyl phthalate, polyethylene glycol, or a combination thereof.
9 . The sublingual or buccal dosage form of claim 1 , further comprising a sweetening agent.
10 . The sublingual or buccal dosage form of claim 9 , wherein the sweetening agent comprises mannitol, maltitol, sorbitol, sucrose, sucralose, dextrose, saccharin, cyclamate, aspartame, or a combination thereof.
11 . The sublingual or buccal dosage form of claim 1 , further comprising a saliva stimulating agent, or a salt thereof, comprising citric acid, malic acid, lactic acid, ascorbic acid, or a combination thereof.
12 . The sublingual or buccal dosage form of claim 11 , wherein the dosage form comprises sodium ascorbate in an amount from 0.02M to 2M.
13 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form is a dissolving strip, lozenge, lollypop, or chewing gum.
14 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises butylated hydroxytoluene (BHT) in an amount from 0.002% to 0.2% by weight.
15 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises ethylenediaminetetraacetic acid (EDTA) in an amount from 0.01% to 1% by weight.
16 . The sublingual or buccal dosage form of claim 1 , wherein the dosage form comprises 200 mg/mL NAC, 0.2M sodium ascorbate, 0.02% BHT, 0.1% EDTA, 0.5% HPBCD, 1% mannitol, and 0.1% menthol.
17 . A sublingual or buccal dosage form comprising:
N-acetylcysteine (NAC) or pharmaceutically salt thereof;
one or more water-soluble polymers or plasticizers; and
one or more masking agents effective to alleviate odor or taste of NAC, wherein said one or more masking agents comprises (2-hydroxypropyl) beta-cyclodextrin (HPBCD) present in an amount from 0.05% to 5% by weight.
18 . The sublingual or buccal dosage form of claim 17 , wherein the dosage form comprises (2-hydroxypropyl) beta-cyclodextrin (HPBCD) present in an amount from 0.1% to 1% by weight.
19 . The sublingual or buccal dosage form of claim 17 , wherein the dosage form comprises (2-hydroxypropyl) beta-cyclodextrin (HPBCD) present in an amount of about 0.5% by weight.
20 . The sublingual or buccal dosage form of claim 9 , wherein the sweetening agent is selected from the group consisting of mannitol, maltitol, sorbitol, sucrose, sucralose, dextrose, saccharin, cyclamate, aspartame, and combinations thereof.