Buccal, polar and non-polar spray or capsule
Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: aqueous polar solvent 30-99.89%, active compound 0.001-60%, optionally containing flavoring agent 0.1-10%. Propellant 2-10% The non polar composition of the invention comprises formulation II: non-polar solvent 20-85%, active compound 0.005-50%, and optionally flavoring agent 0.1-10% and propellant 50-80%.
1 - 25 . (canceled)
26 . A method for administering an effective amount of a pharmacologically active compound to a mammal to provide transmucosal absorption of a pharmacologically effective amount of the active compound through the oral mucosa of the mammal to the systemic circulatory system of the mammal, comprising:
spraying the oral mucosa of the mammal with a buccal spray composition, containing a pharmacologically active compound dissolved in a pharmacologically acceptable solvent, comprising in weight percent of the composition:
an active compound in an amount between 0.05 and 50 percent selected from the group consisting of a biologically active peptide, central nervous system active amine, sulfonyl urea, antibiotic, antifungal, sleep inducer, antiasthmatic, antiemetic, antiviral, histamine H-2 receptor antagonist, barbiturate, prostaglandin, or bronchial dilator;
a non-polar solvent in an amount between 20 and 85 percent; and
a propellant in an amount between 5 and 70 percent, wherein said propellant is a C 3 to C 8 hydrocarbon of linear or branched configuration.
27 . The method of claim 26 , wherein the spray composition further comprises a flavoring agent in an amount of between 0.1 and 10 percent by weight of the total composition.
28 . The method of claim 26 , wherein the active compound is selected from the group consisting of cyclosporine, clozapine, zidevedine, erythromycin, ondansetron, cimetidine, phenytoin, carbprost thromethamine, valerian, or a pharmaceutically acceptable salt thereof
29 . The method of claim 27 , wherein the flavoring agent comprises a synthetic or natural oil of peppermint, oil of spearmint, citrus oil, fruit flavor, sweetener or a mixture thereof.
30 . The method of claim 26 , wherein the propellant is present in an amount between 5 and 70 percent by weight of the total composition, the non-polar solvent is present in an amount between 25 and 85 percent by weight of the total composition, the active compound is present in an amount from between 0.1 and 40 percent by weight of the total composition, and a flavoring agent is present in an amount between 1 and 8 percent by weight of the total composition.
31 . The method of claim 26 , wherein the propellant is present in an amount between 20 and 70 percent by weight of the total composition, the non-polar solvent is present in an amount between 30 and 75 percent by weight of the total composition, the active compound is present in an amount from between 0.25 and 35 percent by weight of the total composition, and a flavoring agent is present in an amount between 2 and 7.5 percent by weight of the total composition.
32 . The method of claim 26 , wherein the propellant comprises propane, n-butane, iso-butane, n-pentane, iso-pantane, neo-pentane or a mixture thereof.
33 . The method of claim 32 , wherein the propellant is n-butane or iso-butane and has a water content of not more than 0.2 percent and a concentration of oxidizing agents, reducing agents, Lewis acids, and Lewis bases of less than 0.1 percent.
34 . The method of claim 26 , wherein the solvent comprises a (C 2 -C 24 ) fatty acid (C 2 -C 6 ) ester, C 7 -C 18 hydrocarbon of linear or branched configuration, C 2 -C 6 alkanoyl ester or a triglyceride of C 2 -C 6 carboxylic acids.
35 . The method of claim 26 , wherein the solvent comprises one or more fatty acid esters.
36 . The method of claim 26 , wherein the propellant is present in an amount between 15 and 70 percent by weight of the total composition, the non-polar solvent is present in an amount between 20 and 85 percent by weight of the total composition, the active compound is clozapine in an amount between 0.5 and 30 percent by weight of the total composition, and a flavoring agent is present in an amount between 1 and 5 percent by weight of the total composition.
37 . The method of claim 26 , wherein the propellant is present in an amount between 15 and 70 percent by weight of the total composition, the non-polar solvent is present in an amount between 20 and 85 percent by weight of the total composition, the active compound is zidovudine in an amount between 25 and 35 percent by weight of the total composition, and a flavoring agent is present in an amount between 1 and 5 percent by weight of the total composition.
38 . The method of claim 26 , wherein the propellant is present in an amount between 5 and 60 percent by weight of the total composition, the non-polar solvent is present in an amount between 20 and 85 percent by weight of the total composition, the active compound is carboprost in an amount between 0.5 and 5 percent by weight of the total composition, and a flavoring agent is present in an amount between 0.1 and 10 percent by weight of the total composition.
39 . The method of claim 26 , wherein the propellant is present in an amount between 5 and 60 percent by weight of the total composition, the non-polar solvent is present in an amount between 50 and 85 percent by weight of the total composition, the active compound is terbutaline in an amount between 0.5 and 6 percent by weight of the total composition, and a flavoring agent is present in an amount between 0.01 and 10 percent by weight of the total composition.