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US 2004O120895A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0120895 A1 Dugger, III (43) Pub. Date: Jun. 24, 2004

(54) BUCCAL POLAR AND NON-POLAR SPRAY tion No. 09/537,118, filed on Mar. 29, 2000, which is OR CAPSULE CONTAINING DRUGS FOR a continuation-in-part of application No. PCT/US97/ TREATING DSORDERS OF THE CENTRAL 17899, filed on Oct. 1, 1997. NERVOUS SYSTEM Publication Classification (75) Inventor: Harry A. Dugger III, Flemington, NJ (US) (51) Int. Cl...... A61L 9/04 (52) U.S. Cl...... 424/44 Correspondence Address: JONES DAY (57) ABSTRACT 51 Louisiana Aveue, N.W WASHINGTON, DC 20001-2113 (US) Buccal aeroSol Sprays or capsules using polar and non-polar solvent have now been developed which provide biologi (73) Assignee: Novadel Pharma, Inc., Flemington, NJ cally active compounds for rapid absorption through the oral (21) Appl. No.: 10/726,585 mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: acque (22) Filed: Dec. 4, 2003 ous polar Solvent, active compound, and optional flavoring agent; formulation II: acqueous polar Solvent, active com Related U.S. Application Data pound, optionally flavoring agent, and propellant; formula tion m: non-polar Solvent, active compound, and optional (60) Division of application No. 10/230,060, filed on Aug. flavoring agent; and formulation IV: non-polar Solvent, 29, 2002, which is a continuation-in-part of applica active compound, optional flavoring agent, and propellant. Patent Application Publication Jun. 24, 2004 US 2004/O120895 A1

TRANSMUCOSA FORMULATION ORAL FORMULATION

STO MACH ORAL FORMULATION DISSOLUTION

STOMACH SOLUTION OF DRUG FECES

COLON PORTAL BLOOD ENEROHEPATC BILE RECIRCULATION

BLE isis LIVER 1ST PASS ETABOTE

ENEROHEPATIC COLON RECIRCULATION

FECES SYSTEMIC CIRCULATION URINE

RECEPTOR

THERAPEUTIC EFFECT US 2004/O120895 A1 Jun. 24, 2004

BUCCAL POLAR AND NON-POLAR SPRAY OR 0005 The buccal polar aerosol spray compositions of the CAPSULE CONTAINING DRUGS FOR TREATING present invention, for transmucosal administration of a DSORDERS OF THE CENTRAL NERVOUS pharmacologically active compound Soluble in a pharmaco SYSTEM logically acceptable polar Solvent are also administrable in aeroSol form driven by a propellant. In this case, the com CROSS REFERENCE TO RELATED position comprises in weight % of total composition: aque APPLICATIONS ous polar solvent 10-97%, active compound 0.1-25%, Suit 0001. This application is a continuation-in-part of appli ably additionally comprising, by weight of total composition cation Ser. No. 09/537,118, filed Mar. 29, 2000 which is a a flavoring agent 0.05-10% and propellant: 2-10%. Prefer continuation-in-part of the U.S. national phase designation ably the composition comprises: polar solvent 20-97%, active compound 0.1-15%, flavoring agent 0.1-5% and of PCT/US97/17899 filed Oct. 1, 1997, the disclosures of propellant 2–5%; most suitably polar solvent 25-97%, active which are incorporated by reference herein in their entirety. compound 0.2-25%, flavoring agent 0.1-2.5% and propel BACKGROUND OF THE INVENTION lant 2-4%. 0002. It is known that certain biologically active com 0006 The buccal pump spray composition of the present pounds are better absorbed through the oral mucosa than invention, i.e., the propellant free composition, for transmu through other routes of administration, Such as through the cosal administration of a pharmacologically active com stomach or intestine. However, formulations Suitable for pound wherein Said active compound is Soluble in a phar Such administration by these latter routes present their own macologically acceptable non-polar Solvent comprises in problems. For example, the biologically active compound weight % of total composition: non-polar Solvent must be compatible with the other components of the 30-99.69%, active compound 0.005-55%, and suitably addi composition Such as propellants, Solvents, etc. Many Such tionally, flavoring agent 0.1-10%. formulations have been proposed. For example, U.S. Pat. 0007. The buccal polar pump spray compositions of the No. 4,689,233, Dvorsky et al., describes a soft gelatin present invention, i.e., the propellant free composition, for capsule for the administration of the anti-coronary drug transmucosal administration of a pharmacologically active nifedipine dissolved in a mixture of polyether . U.S. compound Soluble in a pharmacologically acceptable polar Pat. No. 4,755,389, Jones et al., describes a hard gelatin Solvent comprises in weight% of total composition: aqueous chewable capsule containing nifedipine. A chewable gelatin polar solvent 30-99.69%, active compound 0.001-60%, Suit capsule containing a Solution or dispersion of a drug is ably additionally comprising, by weight of total composition described in U.S. Pat. No. 4,935,243, Borkan et al. U.S. Pat. No. 4,919,919, Aouda et al, and U.S. Pat. No. 5,370,862, a flavoring agent 0.1-10%. Preferably the composition com Klokkers-Bethke, describe a nitroglycerin Spray for admin prises: polar solvent 37-98.58%, active compound 0.005-55 istration to the oral mucosa comprising nitroglycerin, etha %, flavoring agent 0.5-8%; most suitably polar solvent nol, and other components. An orally administered pump 60.9-97.06%, active compound 0.01-40%, flavoring agent spray is described by Cholcha in U.S. Pat. No. 5,186,925. O.75-7.5%. AeroSol compositions containing a hydrocarbon propellant 0008. The soft bite gelatin capsules of the present inven and a drug for administration to a mucosal Surface are tion for transmucosal administration of a pharmacologically described in U.K. 2,082,457, Su, U.S. Pat. No. 3,155,574, active compound, at least partially Soluble in a pharmaco Silson et al., U.S. Pat. No. 5,011,678, Wang et al., and by logically acceptable non-polar Solvent, having charged Parnell in U.S. Pat. No. 5,128,132. It should be noted that thereto a fill composition comprise in weight % of total these references discuss of solutions by inha composition: non-polar solvent 4-99.99%, emulsifier 0-20 lation rather than through the membranes to which they are %, active compound 0.01-80%, provided that said fill com administered. position contains less than 10% of water, Suitably addition ally comprising, by weight of the composition: flavoring SUMMARY OF THE INVENTION agent 0.01-10%. Preferably, the soft bite gelatin capsule 0003) A buccal aerosol spray or soft bite gelatin capsule comprises: non-polar solvent 21.5-99.975%, emulsifier using a polar or non-polar Solvent has now been developed 0-15%, active compound 0.025-70%, flavoring agent 1-8%; which provides biologically active compounds for rapid most suitably: nonpolar solvent 28.5-97.9%, emulsifier absorption through the oral mucosa, resulting in fast onset of 0-10%, active compound 0.1-65.0%, flavoring agent 2-6%. effect. 0009. The soft bite polar gelatin capsules of the present 0004. The buccal aerosol spray compositions of the invention for transmucosal administration of a pharmaco present invention, for transmucosal administration of a logically active compound, at least partially Soluble in a pharmacologically active compound Soluble in a pharmaco pharmacologically acceptable polar Solvent, having charged logically acceptable non-polar Solvent comprise in weight% thereto a composition comprising in weight % of total of total composition: pharmaceutically acceptable propellant composition: polar solvent 25-99.89%, emulsifier 0-20%, 5-80%, nonpolar solvent 19-85%, active compound 0.05 active compound 0.01-65%, provided that said composition 50%, suitably additionally comprising, by weight of total contains less than 10% of water, suitably additionally com composition a flavoring agent 0.01-10%. Preferably the prising, by weight of the composition: flavoring agent composition comprises: propellant 10-70%, non-polar Sol 01-10%. Preferably, the soft bite gelatin capsule comprises: vent 25-89.9%, active compound 0.01-40%, flavoring agent polar solvent 37-99.95%, emulsifier 0-15%, active com 1-8%; most suitably propellant 20-70%, non-polar solvent pound 0.025-55%, flavoring agent 1-8%; most suitably: 25-74.75%, active compound 0.25-35%, flavoring agent polar solvent 44-96.925%, emulsifier 0-10%, active com 2-7.5%. pound 0.075-50%, flavoring agent 2-6%. US 2004/O120895 A1 Jun. 24, 2004

0010. It is an object of the invention to coat the mucosal 0019 Soft gelatin capsules are well known in the art. See, membranes either with extremely fine droplets of Spray for example, U.S. Pat. No. 4,935,243, Borkan et al., for its containing the active compounds or a Solution or paste teaching of Such capsules. The capsules of the present thereof from bite capsules. invention are intended to be bitten into to release the low Viscosity Solution or paste therein, which will then coat the 0011. It is also an object of the invention to administer to buccal mucosa with the active compounds. Typical capsules, the oral mucosa of a mammalian in need of Same, preferably which are Swallowed whole or bitten and then Swallowed, man, by Spray or bite capsule, a predetermined amount of a deliver the active compounds to the Stomach, which results biologically active compound by this method or from a Soft in Significant lag time before maximum blood levels can be gelatin capsule. achieved or Subject the compound to a large first pass effect. 0012. A further object is a sealed aerosol spray container Because of the enhanced absorption of the compounds containing a composition of the non polar or polar aeroSol through the oral mucosa and no chance of a first pass effect, Spray formulation, and a metered valve Suitable for releasing use of the bite capsules of the invention will eliminate much from Said container a predetermined amount of Said com of the lag time, resulting in hastened onset of biological position. effect. The shell of a soft gelatin capsule of the invention may comprise, for example: gelatin: 50-75%, glycerin 0013 As the propellant evaporates after activation of the 20-30%, colorants 0.5-1.5%, water 5-10%, and Sorbitol aerosol valve, a mist of fine droplets is formed which 2-10%. contains Solvent and active compound. 0.014. The propellant is a non-Freon material, preferably 0020. The active compound may include, biologically a Cs hydrocarbon of a linear or branched configuration. active peptides, central nervous System active amines, Sul The propellant should be Substantially non-aqueous. The fonyl ureas, antibiotics, antifungals, antivirals, Sleep induc propellant produces a pressure in the aerosol container Such ers, antiasthmatics, bronchial dilators, antiemetics, hista that under expected normal usage it will produce Sufficient mine H-2 antagonists, , prostaglandins preSSure to expel the Solvent from the container when the and neutraceuticals. Valve is activated but not excessive pressure Such as to 0021. The active compounds may also include antihista damage the container or valve Seals. mines, alkaloids, hormones, and narcotic 0.015 The non-polar solvent is a non-polar hydrocarbon, analgesics. While not limited thereto, these active com preferably a C7 is hydrocarbon of a linear or branched pounds are particularly Suitable for non-polar pump Spray configuration, esters, and triglycerides, Such as formulation and application. miglyol. The Solvent must dissolve the active compound and 0022. The active compounds may also include p-FOX be miscible with the propellant, i.e., Solvent and propellant (fatty acid oxidation) inhibitors, acetylcholinesterase inhibi must form a single phase at a temperature of 0-40 C. a tors, nerve impulse inhibitors, anti-cholinergics, anti-con preSSure range of between 1-3 atm. Vulsants, anti-psychotics, agents, 0016. The polar and non-polar aerosol spray composi inhibitors, agents to treat post Sequelae, tions of the invention are intended to be administered from neuroprotectants, agents to treat Alzheimer's disease, neu a Sealed, pressurized container. Unlike a pump Spray, which rotransmitters, neurotransmitter , , agents allows the entry of air into the container after every activa for treating attention deficit disorder, agents for treating tion, the aeroSol container of the invention is Sealed at the narcolepsy, central adregenic antagonists, anti-depression time of manufacture. The contents of the container are agents, agents for treating Parkinson's disease, benzodiaz released by activation of a metered valve, which does not epine antagonists, Stimulants, neurotransmitter antagonists, allow entry of atmospheric gasses with each activation. Such tranquilizers, or a mixture thereof. containers are commercially available. BRIEF DESCRIPTION OF THE DRAWING 0.017. A further object is a pump spray container contain ing a composition of the pump Spray formulation, and a 0023 FIG. 1. is a schematic diagram showing routes of metered valve Suitable for releasing from Said container a absorption and processing of pharmacologically active Sub predetermined amount of Said composition. stances in a mammalian System. 0.018. A further object is a soft gelatin bite capsule DESCRIPTION OF THE PREFERRED containing a composition of as Set forth above. The formu EMBODIMENTS lation may be in the form of a Viscous Solution or paste containing the active compounds. Although Solutions are 0024. The preferred active compounds of the present preferred, paste fills may also be used where the active invention are in an ionized, Salt form or as the free base of compound is not Soluble or only partially Soluble in the the pharmaceutically acceptable Salts thereof (provided, for solvent of choice. Where water is used to form part of the the aerosol or pump Spray compositions, they are Soluble in paste composition, it should not exceed 10% thereof. (All the spray Solvent). These compounds are Soluble in the percentages herein are by weight unless otherwise indi non-polar Solvents of the invention at useful concentrations cated.) The polar or non-polar Solvent is chosen Such that it or can be prepared as pastes at useful concentrations. These is compatible with the gelatin Shell and the active com concentrations may be less than the Standard accepted dose pound. The solvent preferably dissolves the active com for these compounds Since there is enhanced absorption of pound. However, other components wherein the active com the compounds through the oral mucosa. This aspect of the pound is not Soluble or only slightly Soluble may be used and invention is especially important when there is a large will form a paste fill. (40-99.99%) first pass effect. US 2004/O120895 A1 Jun. 24, 2004

0.025 AS propellants for the non polar sprays, propane, agent for treating Parkinson's disease, N-, iso-butane, N-pentane, iso-pentane, and neo-pen antagonist, Stimulant, neurotransmitter antagonist, tranquil tane, and mixtures thereof may be used. N-butane and izer, or a mixture thereof. iso-butane, as Single gases, are the preferred propellants. It is permissible for the propellant to have a water content of 0033. In one embodiment the active compound is a no more than 0.2%, typically 0.1-0.2%. All percentages p-FOX inhibitor. A suitable p-FOX inhibitor for use in the herein are by weight unless otherwise indicated. It is also buccal Sprays of the invention includes, but is not limited to, preferable that the propellant be Synthetically produced to ranolazine. minimize the presence of contaminants which are harmful to 0034. In one embodiment the active compound is an the active compounds. These contaminants include oxidiz acetylcholinesterase inhibitor. Suitable acetylcholinesterase ing agents, reducing agents, Lewis acids or bases, and Water. inhibitors for use in the buccal sprays of the invention The concentration of each of these should be less than 0.1%, include, but are not limited to, galantamine, neostigmine, except that water may be as high as 0.2%. phySOStigmine, and edrophonium. 0.026 Suitable non-polar solvents for the capsules and the 0035) In one embodiment the active compound is a nerve non-polar sprays include (C-C) fatty acid (C-C) esters, impulse inhibitor. Suitable nerve impulse inhibitors for use C7-Cs hydrocarbon, C-C alkanoyl esters, and the triglyc in the buccal sprays of the invention include, but are not erides of the corresponding acids. When the capsule fill is a limited to, levobupivacaine, lidocaine, prilocaine, mepiv paste, other liquid components may be used instead of the acaine, propofol, rapacuronium , ropivacaine, tub above low molecular weight Solvents. These include Soya ocurarine, atracurium, doxaurium, mivacurium, pancuro oil, corn oil, other vegetable oils. nium, Vercuronium, pipecuronium, and rocuronium. 0.027 AS solvents for the polar capsules or sprays there 0036). In one embodiment the active compound is an may be used low molecular weight polyethyleneglycols anti-cholinergic. Suitable anti-cholinergicS for use in the (PEG) of 400-1000 Mw (preferably 400-600), low molecu buccal Sprays of the invention include, but are not limited to, lar weight (C-C) mono and polyols and alcohols of C7-Cs , ipratropium, OXitropium, and dicycloverine. linear or branch chain hydrocarbons, glycerin may also be present and water may also be used in the SprayS, but only 0037. In one embodiment the active compound is an in limited amount in the capsules. anti-convulsant. Suitable anti-convulsants for use in the buccal Sprays of the invention include, but are not limited to, 0028. It is expected that Some glycerin and water used to , , , , make the gelatin shell will migrate from the shell to the fill divalproex (Valproic acid), , lamotrignine acid, during the curing of the shell. Likewise, there may be Some levetriacetam, , , , migration of components from the fill to the shell during , , , , topira curing and even throughout the Shelf-life of the capsule. mate, , and . 0029. Therefore, the values given herein are for the 0038. In one embodiment the active compound is an compositions as prepared, it being within the Scope of the anti-psychotic. Suitable anti-psychotics for use in the buccal invention that minor variations will occur. Sprays of the invention include, but are not limited to, 0030 The preferred flavoring agents are synthetic or , , bromperidol, clozap natural oil of peppermint, oil of Spearmint, citrus oil, fruit ine, , , illoperidone loperidone, flavors, Sweeteners (Sugars, aspartame, Saccharin, etc.), and , , fluiphenazine, fumarate, , combinations thereof. thiothixene, , Sulpride, and , 0031. The active substances include the active com 0039. In one embodiment the active compound is an pounds Selected from the group consisting of cycloSporine, anxiolytic agent. Suitable anxiolytic agents for use in the Sermorelin, octreotide acetate, calcitonin-Salmon, insulin buccal Sprays of the invention include, but are not limited to, lispro, Succinate, clozepine, , amitryptiline, atracurium, , chlorZOXaZone, clo hydrochloride, glyburide, Zidovudine, raZepate, cisatracurium, cyclobenzaprine, eperisone, esopi erythromycin, ciprofloxacin, hydrochloride, clone, hydroxy Zine, , mivacurium, pagoclone, dimenhydrinate, cimetidine hydrochloride, famotidine, Sulperide, Zaleplon, and Zopiclone. phenytoin Sodium, phenytoin, carboprost thromethamine, 0040. In one embodiment the active compound is a carboprost, hydrochloride, isoproterenol dopamine metabolism inhibitor. Suitable dopamine metabo hydrochloride, terbutaline Sulfate, terbutaline, theophylline, lism inhibitors for use in the buccal sprays of the invention albuterol Sulfate and neutraceuticals, that is to Say nutrients include, but are not limited to, entacapone, lazebemide, with pharmacological action Such as but not limited to Selegiline, and tolcapone. camitine, , echinacea, and the like. 0032. In another embodiment, the active compound is a 0041. In one embodiment the active compound is an p-FOX (fatty acid oxidation) inhibitor, acetylcholinesterase agent to treat post Stroke Sequelae. Suitable agents to treat inhibitor, nerve impulse inhibitor, anti-cholinergic, anti post Stroke Sequelae for use in the buccal sprays of the convulsant, anti-psychotic, anxiolytic agent, dopamine invention include, but are not limited to, glatiramer, inter metabolism inhibitor, agent to treat post Stroke Sequelae, feron beta 1A, interferon beta 1B, estradiol, and progester neuroprotectant, agent to treat Alzheimer's disease, neu OC. rotransmitter, neurotransmitter , , agent for 0042. In one embodiment the active compound is a treating attention deficit disorder, agent for treating narco neuroprotectant. Suitable neuroprotectants for use in the lepsy, central adregenic antagonist, anti-depression agent, buccal Sprays of the invention include, but are not limited to, US 2004/O120895 A1 Jun. 24, 2004 donepezil, memanine, nimodipine, , rivastigmine, 0052. In one embodiment the active compound is a tacrine, TAK147, and . benzodiazepine antagonist. A Suitable benzodiazepine 0043. In one embodiment the active compound is an antagonist for use in the buccal Sprays of the invention agent to treat Alzheimer's disease. Suitable agents to treat includes, but is not limited to, flumazenil. Alzheimer's disease for use in the buccal sprays of the 0053. In one embodiment the active compound is a invention include, but are not limited to, carbidopa, neurotransmitter antagonist. A Suitable neurotransmitter levodopa, tacrine, doneZepil, rivastigmine, and galantamine. antagonist for use in the buccal Sprays of the invention includes, but is not limited, to . 0044) In one embodiment the active compound is a neurotransmitter. Suitable neurotransmitters for use in the 0054. In one embodiment the active compound is a buccal Sprays of the invention include, but are not limited to, Stimulant. Suitable Stimulants for use in the buccal Sprays of acetylcholine, , 5-hydroxytryptamine (5-HT), the invention include, but are not limited to, , GABA, glutamate, aspartate, , histamine, epineph dextroamphetamine, dinoprostone, methylphenidate, meth rine, norpinephrine, dopamine, adenosine, ATP, and nitric ylphenidate, modafinil, and pemoline. oxide. 0055. In one embodiment the active compound is a 0.045. In one embodiment the active compound is a tranquilizer. A Suitable tranquilizer for use in the buccal neurotransmitter agonist. Suitable neurotransmitter agonists Sprays of the invention includes, but is not limited to, for use in the buccal Sprays of the invention include, but are . not limited to, , aniracetam, , benSer 0056. The formulations of the present invention comprise azide, , , , citalopram, an active compound or a pharmaceutically acceptable Salt , , diazepam, , thereof. The term “pharmaceutically acceptable salts' refers dulloxetine, , , fluvoxamine, to Salts prepared from pharmaceutically acceptable non , , moclobemide, , nefaz toxic acids or bases including organic and inorganic acids or odone, acamproSate, , nortryptiline, bases. paroxetine, , pramipexole, , ropinirole, 0057 When an active compound of the present invention Sertraline, Sibutramine, Sumatriptan, , , is acidic, Salts may be prepared from pharmaceutically Venlafaxine, and . acceptable non-toxic bases. Salts derived from all stable 0046. In one embodiment the active compound is a forms of inorganic bases include aluminum, ammonium, Sedative. Suitable Sedatives for use in the buccal sprays of calcium, copper, iron, lithium, , manganese, the invention include, but are not limited to, deXmedetomi potassium, Sodium, , etc. Particularly preferred are the dine, eSZopiclone, indiplon, Zolpidem, and Zaleplon. ammonium, calcium, magnesium, potassium, and Sodium Salts. Salts derived from pharmaceutically acceptable 0047. In one embodiment the active compound is an organic non-toxic bases include Salts of primary, Secondary, agent for treating attention deficit disorder. Suitable agents and tertiary amines, Substituted amines including naturally for treating attention deficit disorder for use in the buccal occurring Substituted amines, cyclic amines and basic ion Sprays of the invention include, but are not limited to, eXchange resins Such as arginine, betaine, caffeine, choline, amphetamine, dextroamphetamine, methylphenidate, and N.N dibenzylethylenediamine, diethylamine, 2-diethylami pemoline. noethanol, 2-dimethyl-aminoethanol, ethanolamine, ethyl enediamine, N-ethylmorpholine, N-ethylpiperidine, glu 0.048. In one embodiment the active compound is an camine, glucosamine, histidine, isopropylamine, , agent for treating narcolepsy. Suitable agents for treating methyl-glucosamine, morpholine, , piperidine, narcolepsy for use in the buccal Sprays of the invention polyamine resins, procaine, purine, theobromine, triethy include, but are not limited to, modafinil and mazindol. lamine, trimethylamine, tripropylamine, etc. 0049. In one embodiment the active compound is a 0058 When an active compound of the present invention central adregenic antagonists. A Suitable central adregenic is basic, Salts may be prepared from pharmaceutically antagonists for use in the buccal Sprays of the invention acceptable non-toxic acids. Such acids include acetic, ben includes, but is not limited to, meSoridazine. ZeneSulfonic, benzoic, camphorSulfonic, citric, ethane-Sul 0050. In one embodiment the active compound is an fonic, fumaric, gluconic, glutamic, hydrobromic, hydrochlo anti-depression agent. Suitable anti-depression agents for ric, isethionic, lactic, maleic, mandelic, methaneSulfonic, use in the buccal Sprays of the invention include, but are not mucic, nitric, pamoic, pantothenic, phosphoric, Succinic, limited to, , , bupropion, clomi Sulfuric, tartaric, p-toluenesulfonic, etc. Particularly pre pramine, clomipramine, clorgyline, desipramine, doxepin, ferred are citric, hydrobromic, maleic, phosphoric, Sulfuric, , imipramine, isocarboxazid, , mirtaza and tartaric acids. pine, , , paroxetine, , pro 0059. In the discussion of methods of treatment herein, triptyline, Sertraline, tranylcypromine, traZodone, and ven reference to the active compounds is meant to also include lafaxine. the pharmaceutically acceptable Salts thereof. While certain 0051. In one embodiment the active compound is an formulations are Set forth herein, the actual amounts to be agent for treating Parkinson's disease. Suitable agents for administered to the mammal or man in need of Same are to treating Parkinson's disease for use in the buccal Sprays of be determined by the treating physician. the invention include, but are not limited to, amantadine, 0060. The invention is further defined by reference to the bromocriptine, carvidopa, levodopa, pergolide, and Sel following examples, which are intended to be illustrative egiline. and not limiting. US 2004/O120895 A1 Jun. 24, 2004

0061 The following are examples of certain classes. All 0.066) values unless otherwise Specified are in weight percent.

EXAMPLES E. Sermorelin (as the acetate) lingual spray Example 1 preferred Amounts amount most preferred 0.062 Biologically Active Peptides Including Peptide sermorelin (as the acetate) .01-5 .1-3 .2-1.0 Hormones mannitol 1-25 5-20 10-15 monobasic sodium phosphate, 0.1-5 1-31 .5-2.5 dibasic sodium phosphate water 0.01-5 .05-3 0.1-0.5 ethanol 5-30 7.5-25 9.5-15 polyethylene glycol 20-60 30-45 35-40 A. Cyclosporine lingual spray propylene glycol 5-25 10-20 12-17 flavors 0.1-5 1-4 2-3 most Amounts preferred amount preferred amount cyclosporine 5-50 10-35 15-25 0067 water 5-20 7.5-50 9.5-12 ethanol 5-60 7.5-50 10-2O polyethylene glycol 20-60 30-45 35-40 flavors 0.1-5 1-4 2-3 F. Octreotide acetate (Sandostatin) lingual Spray

most Amounts preferred amount preferred amount 0063) octreotide acetate 0.001-0.5 O.OOS-O.2SO O.O1-0.10 acetic acid 1-10 2-8 4-6 sodium acetate 1-10 2-8 4-6 sodium chloride 3-30 5-25 15-20 B. Cyclosporine Non-Polar lingual spray flavors 0.1-5 0.5-4 2-3 ethanol 5-30 7.5-2O 9.5-15 preferred most water 15-95 35-90 65-85 Amounts amount preferred amount flavors 0.1-5 1-4 2-3 cyclosporine 1-50 3-40 5-30 Migylol 2O 25 30-40 Polyoxyethylated castor oil 2O 25 30-40 0068) Butane 25-80 30-70 33-50 flavors 0.1-5 1-4 2-3

G. Calcitonin-Salmon lingual spray

0.064 most Amounts preferred amount preferred amount calcitonin-salmon 0.001-5 0.005-2 O1-1.5 C. Cyclosporine non-polar bite caosule ethanol 2-15 3-10 7-9.5 water 30-95 SO-90 60-80 Amounts preferred amount most preferred amount polyethylene glycol 2-15 3-10 7-9.5 sodium chloride 2.5-20 5-15 10-12.5 cyclosporine 1-35 5-25 10-2O flavors 0.1-5 1-4 2-3 olive oil 25-60 35-55 30-45 polyoxyethylated 25-60 35-55 30-45 oleic glycerides flavors 0.1-5 1-4 2-3 0069

0065 H. Insulin lispro, lingual Spray most preferred Amounts preferred amount amount D. CycloSporine bite capsule insulin 20-60 4-55 5-50 most glycerin 0.1-10 O.25-5 0.1-1.5 Amounts preferred amount preferred amount dibasic sodium 1-15 2.5-10 4-8 phosphate cyclosporine 5-50 10-35 15-25 m-cresol, 1-25 5-25 7.5-12.5 polyethylene glycol 20-60 30-45 35-40 Zinc oxide 0.01-0.25 .05-0.15 O.O75-0.10 glycerin 5-30 7.5-25 10-2O m-cresol 0.1-1 0.2-0.8 0.4-0.6 propylene glycol 5-30 7.5-25 10-2O phenol trace amounts trace amounts trace amounts flavors 0.1-10 1-8 3-6 ethanol 5-20 7.5-15 9-12 water 30-90 40-80 50-75 US 2004/O120895 A1 Jun. 24, 2004

0073) -continued

H. Insulin lispro, lingual spray D. Clozepine non-polar lingual spray with propellant Amounts preferred amount most preferred amount most preferred Amounts preferred amount amount clozepine 0.5-30 1-20 10-15 Migylol 20-85 25-70 30-40 Butanol 5-80 30-75 60-70 propylene glycol 5-20 7.5-15 9-12 flavors 0.1-5 1-4 2-3 flavors 0.1-5 0.5-3 O.75-2 0074) adjust pH to 7.0–7.8 with HCI or NaOH

Example 2 E. Clozepine non-polar lingual Spray without propellant 0070 CNS active amines and their salts: including but Amounts preferred amount most preferred amount not limited to tricyclic amines, GABA analogues, thiazides, clozepine 0.5-30 1-20 10-15 derivatives, Serotonin antagonists and Seroto Migylol 70-99.5 80-99 85-90 nin reuptake inhibitors flavors 0.1-5 1-4 2-3

0075) A. Sumatriplan succinate lingual spray

most Amounts preferred amount preferred amount F. Cyclobenzaprine non-polar lingual spray Sumatriptan succinate 0.5-30 1-20 10-15 most ethanol 5-60 7.5-50 10-2O Amounts preferred amount preferred amount propylene glycol 5-30 7.5-2O 10-15 cyclobenzaprine (base) 0.5-30 1-20 10-15 polyethylene glycol O-60 30-45 35-40 Migylol 20-85 25-70 30-40 water 5-30 7.5-2O 10-15 Iso-butane 15-80 30-75 60-70 flavors 0.1-5 1-4 2-3 flavors 0.1-5 1-4 2-3

0.071) 0076)

B. Sumatriptan Succinate bite capsule G. Dexfenfluramine hydrochloride lingual spray most most Amounts preferred amount preferred amount Amounts preferred amount preferred amount dexfenfluramine Hc 5-30 7.5-2O 10-15 Sumatriptan succinate 0.01-5 O.O5-3.5 O.O75-1.75 ethanol 5-60 7.5-50 10-2O polyethylene glycol 25-70 30-60 35-50 propylene glycol 5-30 7.5-2O 10-15 glycerin 25-70 30-60 35-50 polyethylene glycol O-60 30-45 35-40 flavors 0.1-10 1-8 3-6 water 5-30 7.5-2O 10-15 flavors 0.1-5 1-4 2-3 0072) Example 3

C. Clozepine lingual spra 0.077 Sulfonylureas

most Amounts preferred amount preferred amount A. Glyburide lingual Spray clozepine 0.5-30 1-20 10-15 ethanol 5-60 7.5-50 10-2O most propylene glycol 5-30 7.5-2O 10-15 Amounts preferred amount preferred amount polyethylene glycol O-60 30-45 35-40 water 5-30 7.5-2O 10-15 glyburide O.25-25 0.5-20 O.75-15 flavors 0.1-5 1-4 2-3 ethanol 5-60 -7.5-50 10-2O propylene glycol 5-30 7.5-2O 10-15 US 2004/O120895 A1 Jun. 24, 2004

-continued -continued A. Glyburide lingual spray C. Ciprofloxacin hydrochloride bite capsule

most preferred most preferred Amounts preferred amount preferred amount Amounts amount amount polyethylene glycol O-60 30-45 35-40 polyethylene glycol 120-75 30-65 40-60 water 2.5-30 5-20 6-15 flavors 1-10 2-8 3-6 flavors 0.1-5 1-4 2-3 0082) 0078 D. zidovudine formerly called azidothymidine (AZT) (Retrovir) lingual Spray B. Glyburide non-polar bite capsule most preferred most Amounts preferred amount amount Amounts preferred amount preferred amount Zidovudine 10-50 15-40 25-35 glyburide 0.01-10 O.O25-7.5 0.1-4 water 30-80 40-75 45-70 olive oil 30-60 35-55 30-50 ethanol 5-20 7.5-15 9.5-12.5 polyoxyethylated oleic 30-60 35-55 30-50 polyethylene glycol 5-20 7.5-15 9.5-12.5 glycerides flavors 0.1-5 1-4 2-3 flavors 0.1-5 1-4 2-3 Example 5 Example 4 0083) Anti-emetics 0079 Antibiotics Anti-fungals and Anti-virals A. Ondansetron hydrochloride lingual spray A. Zidovudine formerly called azidothymidine preferred most preferred AZT) (Retrovir) non-polar lingual spray Amounts amount amount ondansetron hydrochloride 1-25 2-20 2.5-15 Amounts preferred amount most preferred amount citric acid monohydrate 1-10 2-8 2.5-5 sodium citrate dihydrate O.5-5 1-4 1.25-2.5 Zidovudine 10-50 15-40 25-35 water 1-90 5-85 10-75 Soya oil 20-85 25-70 30-40 ethanol 5-30 7.5-2O 9.5-15 Butane 15-80 30-75 60-70 propylene glycol 5-30 7.5-2O 9.5-15 flavors 0.1-5 1-4 2-3 polyethylene glycol 5-30 7.5-2O 9.5-15 flavors 1-10 3-8 5-7.5

0080) 0084)

B. Erythromycin bite capsule bite capsule B. Dimenhydrinate bite capsule most preferred Amounts preferred amount amount most preferred Amounts preferred amount amount erythromycin 25-65 30-50 35-45 polyoxyethylene glycol S-70 30-60 45-55 dimenhydrinate 0.5-30 2-25 3-15 glycerin 5-20 7.5-15 10-12.5 glycerin 5-20 7.5-15 10-12.5 flavors 1-10 2-8 3-6 polyethylene glycol 45-95 SO-90 55-85 flavors 1-10 2-8 3-6

0081) 0085

C. Ciprofloxacin hydrochloride bite capsule C. Dimenhydrinate polar lingual spray preferred most preferred most preferred Amounts amount amount Amounts preferred amount amount ciprofloxacin hydrochloride 25-65 35-55 40-50 dimenhydrinate 3-50 4-40 5-35 glycerin 5-20 7.5-15 10-12.5 water 5-90 10-80 15-75 US 2004/O120895 A1 Jun. 24, 2004

Example 7 -continued 0089 Barbiturates C. Dimenhydrinate polar lingual spray

most preferred A. Phenytoin sodium lingual spray Amounts preferred amount amount most preferred Amounts preferred amount amount ethanol 1-80 3-50 5-10 phenytoin sodium 10-60 15-55 20-40 polyethylene glycol 1-80 3-50 5-15 water 2.5-25 3-2O 5-10 sorbitol 0.1-5 0.2-40 0.4-1.0 ethanol 5-30 7.5-2O 9.5-15 aspartame 0.01-0.5 0.02-0.4 0.04-0.1 propylene glycol 5-30 7.5-2O 9.5-15 flavors 0.1-5 1-4 2-3 polyethylene glycol 5-30 7.5-2O 9.5-15 flavors 1-10 3-8 5-7.5

Example 6 0090) 0.086 HistamineH-2 recepor antagonists B. Phenytoin non-polar lingual spray most preferred A. Cimetidine hydrochloride bite capsule Amounts preferred amount amount phenytoin 5-45 10-40 15-35 most preferred migylol 10-50 15-40 15-20 Amounts preferred amount amount Butane 15-80 30-75 60-70 polyoxyethylated 10-50 15-40 15-20 oleic glycerides cimetidine HCI 10-60 15-55 25-50 flavors 0.1-10 1-8 5-7.5 glycerin 5-20 7.5-15 10-12.5 polyethylene glycol 20-90 25-85 30-75 flavors 1-10 2-8 3-6 Example 8 0091 Prostaglandins 0087

A. Carboprost thromethamine lingual Spray B. Famotidine lingual spray preferred most preferred most preferred Amounts amount amount Amounts preferred amount amount carboprost thromethamine 0.05-5 0.1-3 0.25-2.5 famotidine 1-35 5-30 7-2O water 50-95 60-80 65-75 water 2.5-25 3-2O 5-10 ethanol 5-20 7.5-15 9.5-12.5 L- 0.1-20 1-15 5-10 polyethylene glycol 5-20 7.5-15 9.5-12.5 polyethylene glycol 20-97 30-95 SO-85 sodium chloride 1-20 3-15 4-8 flavors 0.1-10 1-7.5 2-5 flavors 0.1-5 1-4 2-3

0088) 0092 pH is adjusted with sodium hydroxide and/or hydrochloric acid

C. Famotidine non-polar lingual spray B. Carboprost non-polar lingual Spray most preferred Amounts preferred amount amount Amounts preferred amount most preferred amount famotidine 1-35 5-30 7-2O carboprost O.O5-5 0.1-3 0.25-2.5 Soya oil 10-50 15-40 15-20 migylol 25-50 30-45 35-40 Butanel 5-80 30-75 45-70 Butane 5-60 10-50 20-35 polyoxyethylated 10-50 15-40 15-20 polyoxyethylated 25-50 30-45 35-40 oleic glycerides oleic glycerides flavors 0.1-5 1-4 2-3 flavors 0.1-10 1-8 5-7.5 US 2004/O120895 A1 Jun. 24, 2004

Example 9 Example 10 0093 Neutraceuticals 0097 Sleep Inducers (Also CNS Active Amine)

A. Diphenhydramine hydrochloride lingual spray A. Carnitine as bite capsule (contents are a paste) Amounts preferred amount most preferred amount Amounts preferred amount most preferred amount diphenhydramine 3-50. 4-40 5-35 HCl water 5-90 10-80 50-75 ethanol 1-80 3-50 5-10 carnitine 6-8O 30-70 45-65 polyethylene 1-80 3-50 5-15 fumarate glycol soya oil 7.5-50 10-40 125-35 Sorbitol 0.1-5 0.2-4 0.4-1.0 soya lecithin OOO1-10 O.OOS-O.S .01-0.1 aspartame 0.01-0.5 0.02-0.4 0.04-0.1 flavors 0.1-5 1-4 2-3 Soya fats 7.5-50 10-40 125-35 flavors 1-10 2-8 3-6 Example 11 0094) 0098 Anti-Asthmatics-Bronchodilators

B. Valerian as lingual spray A. Isoproterenol Hydrochloride as polar lingual spray Amounts preferred amount most preferred amount Amounts preferred amount most preferred amount valerian extract 0.1-10 O.2-7 O.25-5 isoproterenol 0.1-10 O.2-7.5 0.5-6 water 50-95 60-80 65-75 Hydrochloride ethanol 5-20 7.5-15 9.5-12.5 water 5-90 10-80 50-75 polyethylene 5-20 7.5-15 9.5-12.5 ethanol 1-80 3-50 5-10 glycol polyethylene 1-80 3-50 5-15 flavors 1-10 2-8 3-6 glycol Sorbitol 0.1-5 0.2-4 0.4-1.0 aspartame 0.01-0.5 0.02-0.4 0.04-0.1 flavors 0.1-5 1-4 2-3 0.095 0099) C. Echinacea as bite capsule Amounts preferred amount most preferred amount B. Terbutaline Sulfate as polar lingual spray echinacea 30-85 40-75 45-55 extract Amounts preferred amount most preferred amount soya oil 7.5-50 10-40 125-35 soya lecithin OOO1-10 O.OOS-O.S .01-0.1 terbutaline sulfate 0.1-10 O.2-7.5 0.5-6 Soya fats 7.5-50 10-40 125-35 water 5-90 10-80 50-75 flavors 1-10 2-8 3-6 ethanol 1-10 2-8 2.5-5 Sorbitol 0.1-5 0.2-4 0.4-1.0 aspartame 0.01-0.5 0.02-0.4 0.04-0.1 flavors 0.1-5 1-4 2-3 0096) 01.00 D. Mixtures of ingredients Amounts preferred amount most preferred amount C. Terbutaline as non-polar lingual Spray magnesium oxide 15-40 20-35 25-30 chromium 0.01-1.0 0.02-0.5 O25-0.75 Amounts preferred amount most preferred amount picolinate folic acid .025-3.0 0.05-2.0 O.25-0.5 terbutaline 0.1-10 O.2-7.5 0.5-6 vitamin B-12 0.01-1.0 0.02-0.5 O25-0.75 migylol 25-50 30-45 35-40 vitamin E 15-40 20-35 25-30 isobutane 5-60 10-50 20-35 Soya oil 10-40 125-35 15-20 polyoxyethylated 25-50 30-45 35-40 soya lecithin 0.1-5 0.2-4 0.5-1.5 oleic glycerides soya fat 10-40 15-35 17.5-2O flavors 0.1-10 1-8 5-7.5 US 2004/O120895 A1 Jun. 24, 2004

01.01 01.05

C. (antiemetic, sleep D. Theophylline polar bite capsule inducer, and CNS active amine Preferred Most-Preferred Amounts preferred amount most preferred amount Amount Amount Amount promethazine 1-25% 3-15% 5-12% theophylline 5-50 10-40 15-30 Ethanol 10-90% 20-75% 25-50% polyethylene 20-60 25-50 30-40 Propylene glycol 1-90% 5-80% 10-75% Water O.O1-5% 0.1-4% 0.2-2% glycol Flavors O.O5-10% O. 1-5% 0.1-2.5% glycerin 25-50 35-45 30-40 Propellant 2-10% 3-5% 3-4% propylene glycol 25-50 35-45 30-40 flavors 0.1-5 1-4 2-3 01.06)

0102) D. Meclizine

Preferred Most-Preferred Amount Amount Amount E. Albuterol sulfate as polar lingual spray meclizine 1-25% 3-15% 5-12% Ethanol 1-15% 2-10% 3-6 preferred most preferred Propylene glycol 20-98%, 5-90% 10-85% Amounts amount amount Water O.O1-5% 0.1-4% 0.2-2% Flavors O.O5-10% O. 1-5% 0.1-2.5% albuterol sulfate 0.1-10 O.2-7.5 0.5-6 Propellant 2-10% 3-5% 3-4% water 5-90 10-80 50-75 ethanol 1-10 2-8 2.5-5 Sorbitol 0.1-5 0.2-4 0.4-1.0 aspartame 0.01-0.5 0.02-0.4 0.04-0.1 What is claimed is: flavors 0.1-5 1-4 2-3 1. A propellant free buccal Spray composition for trans mucosal administration of a pharmacologically active com pound comprising: Example 12 an active compound in an amount of between 0.001 and 60 percent by weight of the total composition Selected 0103) Polar Solvent Formulations. Using a Propellant: from the group consisting of acetylcholinesterase inhibitors, nerve impulse inhibitors, anti-cholinergics, anti-convulsants, anti-psychotics, anxiolytic agents, A. Sulfonylurea dopamine metabolism inhibitors, agents to treat post Stroke Sequelae, neuroprotectants, agents to treat Preferred Most-Preferred Alzheimer's disease, neurotransmitters, neurotransmit Amount Amount Amount ter agonists, Sedatives, agents for treating attention glyburide O.1-25% O.5-15% 0.6-10% deficit disorder, agents for treating narcolepsy, central Ethanol 40-99% 60-97% 70-97% adregenic antagonists, anti-depression agents, agents Water O.O1-5% 0.1-4% 0.2-2% Flavors O.O5-10% O. 1-5% 0.1-2.5% for treating Parkinson's disease, benzodiazepine Propellant 2-10% 3-5% 3-4% antagonists, Stimulants, neurotransmitter antagonists, tranquilizers, and mixtures thereof, and a polar solvent in an amount between 30 and 99 percent 01.04] by weight of the total composition. 2. The composition of claim 1, further comprising a flavoring agent in an amount of between 0.1 and 10 percent by weight of the total composition. B. Prostaglandin E (vasodilator 3. The composition of claim 2, wherein the polar solvent Preferred Most-Preferred is present in an amount between 37 and 98 percent by weight Amount Amount Amount of the total composition, the active compound is present in prostaglandin E 0.01-10% O. 1-5% 0.2-3% an amount between 0.005 and 55 percent by weight of the Ethanol 10-90% 20-75% 25-50% total composition, and the flavoring agent is present in an Propylene glycol 1-90% 5-80% 10-75% amount between 0.5 and 8 percent by weight of the total Water O.O1-5% 0.1-4% 0.2-2% Flavors O.O5-10% O. 1-5% 0.1-2.5% composition. Propellant 2-10% 3-5% 3-4% 4. The composition of claim 3, wherein the polar solvent is present in an amount between 60 and 97 percent by weight of the total composition, the active compound is present in US 2004/O120895 A1 Jun. 24, 2004

an amount between 0.01 and 40 percent by weight of the 17. The composition of claim 1, wherein the active total composition, and the flavoring agent is present in an compound is an agent to treat Alzheimer's disease Selected amount between 0.75 and 7.5 percent by weight of the total from the group consisting of carbidopa, levodopa, tacrine, composition. doneZepil, rivaStigmine, galantamine, and mixtures thereof. 5. The composition of claim 1, wherein the polar solvent 18. The composition of claim 1, wherein the active is Selected from the group consisting of polyethylene glycols compound is a neurotransmitter Selected from the group having a molecular weight between 400 and 1000, C to C. consisting of acetylcholine, Serotonin, 5-hydroxytryptamine mono- and poly-alcohols, and C7 to Calcohols of linear or (5-HT), GABA, glutamate, aspartate, glycine, histamine, branched configuration. epinephrine, norpinephrine, dopamine, adenosine, ATP, 6. The composition of claim 1, wherein the polar solvent , and mixtures thereof. comprises aqueous polyethylene glycol. 19. The composition of claim 1, wherein the active 7. The composition of claim 1, wherein the polar solvent compound is a neurotransmitter agonist Selected from the comprises aqueous ethanol. group consisting of almotriptan, aniracetam, atomoxetine, 8. The composition of claim 1, wherein the active com benserazide, bromocriptine, bupropion, cabergoline, citalo pound is an acetylcholinesterase inhibitorS Selected from the pram, clomipramine, desipramine, diazepam, dihydroer group consisting of galantamine, neostigmine, phySoStig gotamine, doxepin dulloxetine, eletriptan, escitalopram, flu mine, and edrophonium, and mixtures thereof. VOXamine, gabapentin, imipramine, moclobemide, 9. The composition of claim 1, wherein the active com naratriptan, nefazodone, nefiracetam acamproSate, nicer pound is a nerve impulse inhibitor Selected from the group goline, nortryptiline, paroxetine, pergolide, pramipexole, consisting of levobupivacaine, lidocaine, prilocaine, mepi rizatriptan, ropinirole, Sertraline, Sibutramine, Sumatriptan, vacaine, propofol, rapacuronium bromide, ropivacaine, tub tiagabine, traZodone, Venlafaxine, Zolmitriptan, and mix ocurarine, atracurium, doxaurium, mivacurium, pancuro tures thereof. nium, Vercuronium, pipecuronium, rocuronium, and 20. The composition of claim 1, wherein the active mixtures thereof. compound is a Sedative Selected from the group consisting 10. The composition of claim 1, wherein the active of , eSZopiclone, indiplon, Zolpidem, Zale compound is an anti-cholinergic Selected from the group plon, and mixtures thereof. consisting of amantadine, ipratropium, OXitropium, dicyclo 21. The composition of claim 1, wherein the active verine, and mixtures thereof. compound is an agent for treating attention deficit disorder 11. The composition of claim 1, wherein the active Selected from the group consisting of amphetamine, dextro compound is an anti-convulsant Selected from the group amphetamine, methylphenidate, pemoline, and mixtures consisting of acetazolamide, carbamazepine, clonazepam, thereof. diazepam, divalproex, ethoSuximide, lamotrignine acid, 22. The composition of claim 1, wherein the active levetriacetam, Oxcarbazepine, phenobarbital, phenytoin, compound is an agent for treating narcolepsy Selected from pregabalin, primidone, remacemide, trimethadione, topira the group consisting of modafinil, mazindol, and mixtures mate, vigabatrin, Zonisamide, and mixtures thereof. thereof. 12. The composition of claim 1, wherein the active 23. The composition of claim 1, wherein the active compound is an anti-psychotic Selected from the group compound is an anti-depression agent Selected from the consisting of amisulpride, aripiprazole bifemelane, bromp group consisting of arnitriptyline, amoxapine, bupropion, eridol, , chlorpromazine, haloperidol, illoperidone clomipramine, clomipramine, clorgyline, desipramine, loperidone, olanzapine, quetiapine, , fumarate, epin, fluoxetine, imipramine, isocarboxazid, maprotiline, risperidone, thiothixene, thioridazine, Sulpride, Ziprasidone, mirtazapine, nefazodone, nortriptyline, paroxetine, and mixtures thereof. phenelZine, , Sertraline, tranylcypromine, traZ 13. The composition of claim 1, wherein the active odone, Venlafaxine, and mixtures thereof. compound is an anxiolytic agent Selected from the group 24. The composition of claim 1, wherein the active consisting of amitryptiline, atracurium, buSpirone, chlorZOX compound is an agent for treating Parkinson's disease aZone, , cisatracurium, cyclobenzaprine, Selected from the group consisting of amantadine, bro eperisone, esopiclone, hydroxy Zine, mirtazapine, mivacu mocriptine, carvidopa, levodopa, pergolide, Selegiline, and rium, pagoclone, Sulperide, Zaleplon, Zopiclone, and mix mixtures thereof. tures thereof. 25. The composition of claim 1, wherein the active 14. The composition of claim 1, wherein the active compound is the benzodiazepine antagonist flumazenil. compound is a dopamine metabolism inhibitor Selected from 26. The composition of claim 1, wherein the active the group consisting of entacapone, lazebemide, Selegiline, compound is the neurotransmitter antagonist deramciclane. tolcapone, and mixtures thereof. 27. The composition of claim 1, wherein the active 15. The composition of claim 1, wherein the active compound is a Stimulant Selected from the group consisting compound is an agent to treat post Stroke Sequelae Selected of amphetamine, dextroamphetamine, dinoprostone, meth from the group consisting of glatiramer, interferon beta 1A, ylphenidate, methylphenidate, modafinil, pemoline, and interferon beta 1B, estradiol, progesterone, and mixtures mixtures thereof. thereof. 28. The composition of claim 1, wherein the active 16. The composition of claim 1, wherein the active compound is the tranquilizer mesoridazine. compound is a neuroprotectant Selected from the group 29. The composition of claim 2, wherein the flavoring consisting of donepezil, memanine, nimodipine, riluzole, agent is Selected from the group consisting of Synthetic or rivastigmine, tacrine, TAK147, Xaliproden, and mixtures natural oil of peppermint, oil of Spearmint, citrus oil, fruit thereof. flavors, Sweeteners, and mixtures thereof. US 2004/O120895 A1 Jun. 24, 2004

30. A method of administering a pharmacologically active group consisting of levobupivacaine, lidocaine, prilocaine, compound to a mammal comprising Spraying the oral mepivacaine, propofol, rapacuronium bromide, ropivacaine, mucosa of the mammal with the composition of claim 1. tubocurarine, atracurium, doxaurium, mivacurium, pancu 31. The method of claim 30, wherein the amount of the ronium, Vercuronium, pipecuronium, rocuronium, and mix Spray is predetermined. tures thereof. 32. A buccal spray composition for transmucosal admin 41. The composition of claim 32, wherein the active istration of a pharmacologically active compound compris compound is an anti-cholinergic Selected from the group Ing: consisting of amantadine, ipratropium, OXitropium, dicyclo an active compound in an amount of between 0.1 and 25 verine, and mixtures thereof. percent by weight of the total composition Selected 42. The composition of claim 32, wherein the active from the group consisting of consisting of acetylcho compound is an anti-convulsant Selected from the group linesterase inhibitors, nerve impulse inhibitors, anti consisting of acetazolamide, carbamazepine, clonazepam, cholinergics, anti-convulsants, anti-psychotics, anxi diazepam, divalproex, ethoSuximide, lamotrignine acid, olytic agents, dopamine metabolism inhibitors, agents levetriacetam, Oxcarbazepine, phenobarbital, phenytoin, to treat post Stroke Sequelae, neuroprotectants, agents to pregabalin, primidone, remacemide, trimethadione, topira treat Alzheimer's disease, neurotransmitters, neu mate, vigabatrin, Zonisamide, and mixtures thereof. rotransmitter agonists, Sedatives, agents for treating 43. The composition of claim 32, wherein the active attention deficit disorder, agents for treating narcolepsy, compound is an anti-psychotic Selected from the group central adregenic antagonists, anti-depression agents, consisting of amisulpride, aripiprazole bifemelane, bromp agents for treating Parkinson's disease, benzodiazepine eridol, clozapine, chlorpromazine, haloperidol, illoperidone antagonists, Stimulants, neurotransmitter antagonists, loperidone, olanzapine, quetiapine, fluphenazine, fumarate, tranquilizers, and mixtures thereof; risperidone, thiothixene, thioridazine, Sulpride, Ziprasidone, and mixtures thereof. a polar solvent in an amount between 10 and 97 percent 44. The composition of claim 32, wherein the active by weight of the total composition; and compound is an anxiolytic agent Selected from the group a propellant in an amount between 2 and 10 percent by consisting of amitryptiline, atracurium, buSpirone, chlorZOX weight of the total composition, wherein Said propel aZone, cloraZepate, cisatracurium, cyclobenzaprine, lant is a C to Cs hydrocarbon of linear or branched eperisone, esopiclone, hydroxy Zine, mirtazapine, mivacu configuration. rium, pagoclone, Sulperide, Zaleplon, Zopiclone, and mix 33. The composition of claim 32, further comprising a tures thereof. flavoring agent in an amount between 0.05 and 10 percent by 45. The composition of claim 32, wherein the active weight of the total composition. compound is a dopamine metabolism inhibitor Selected from 34. The composition of claim 33, wherein the polar the group consisting of entacapone, lazebemide, Selegiline, solvent is present in an amount between 20 and 97 percent tolcapone, and mixtures thereof. by weight of the total composition, the active compound is present in an amount between 0.1 and 15 percent by weight 46. The composition of claim 32, wherein the active of the total composition, the propellant is present in an compound is an agent to treat post Stroke Sequelae Selected amount between 2 and 5 percent by weight of the compo from the group consisting of glatiramer, interferon beta 1A, Sition, and the flavoring agent is present in an amount interferon beta 1B, estradiol, progesterone, and mixtures between 0.1 and 5 percent by weight of the total composi thereof. tion. 47. The composition of claim 32, wherein the active 35. The composition of claim 34, wherein the polar compound is a neuroprotectant Selected from the group solvent is present in an amount between 25 and 97 percent consisting of donepezil, memanine, nimodipine, riluzole, by weight of the total composition, the active compound is rivastigmine, tacrine, TAK147, Xaliproden, and mixtures present in an amount between 0.2 and 25 percent by weight thereof. of the total composition, the propellant is present in an 48. The composition of claim 32, wherein the active amount between 2 and 4 percent by weight of the compo compound is an agent to treat Alzheimer's disease Selected Sition, and flavoring agent is present in an amount between from the group consisting of carbidopa, levodopa, tacrine, 0.1 and 2.5 percent by weight of the total composition. doneZepil, rivaStigmine, galantamine, and mixtures thereof. 36. The composition of claim 32, wherein the polar 49. The composition of claim 32, wherein the active Solvent is Selected from the group consisting of polyethyl compound is a neurotransmitter Selected from the group eneglycols having a molecular weight between 400 and consisting of acetylcholine, Serotonin, 5-hydroxytryptamine 1000, C to C mono- and poly-alcohols, and C7 to Cs (5-HT), GABA, glutamate, aspartate, glycine, histamine, alcohols of linear or branched configuration. epinephrine, norpinephrine, dopamine, adenosine, ATP, 37. The composition of claim 36, wherein the polar nitric oxide, and mixtures thereof. Solvent comprises aqueous polyethylene glycol. 50. The composition of claim 32, wherein the active 38. The composition of claim 36, wherein the polar compound is a neurotransmitter agonist Selected from the Solvent comprises aqueous ethanol. group consisting of almotriptan, aniracetam, atomoxetine, 39. The composition of claim 32, wherein the active benserazide, bromocriptine, bupropion, cabergoline, citalo compound is an acetylcholinesterase inhibitorS Selected pram, clomipramine, desipramine, diazepam, dihydroer from the group consisting of galantamine, neostigmine, gotamine, doxepin dulloxetine, eletriptan, escitalopram, flu phySOStigmine, and edrophonium, and mixtures thereof. VOXamine, gabapentin, imipramine, moclobemide, 40. The composition of claim 32, wherein the active naratriptan, nefazodone, nefiracetam acamproSate, nicer compound is a nerve impulse inhibitor Selected from the goline, nortryptiline, paroxetine, pergolide, pramipexole, US 2004/O120895 A1 Jun. 24, 2004 rizatriptan, ropinirole, Sertraline, Sibutramine, Sumatriptan, ter agonists, Sedatives, agents for treating attention tiagabine, traZodone, Venlafaxine, Zolmitriptan, and mix deficit disorder, agents for treating narcolepsy, central tures thereof. adregenic antagonists, anti-depression agents, agents 51. The composition of claim 32, wherein the active for treating Parkinson's disease, benzodiazepine compound is a Sedative Selected from the group consisting antagonists, Stimulants, neurotransmitter antagonists, of dexmedetomidine, eSZopiclone, indiplon, Zolpidem, Zale tranquilizers, and mixtures thereof, and plon, and mixtures thereof. 52. The composition of claim 32, wherein the active a non-polar solvent in an amount between 30 and 99 compound is an agent for treating attention deficit disorder percent by weight of the total composition. Selected from the group consisting of amphetamine, dextro 65. The composition of claim 64, further comprising a amphetamine, methylphenidate, pemoline, and mixtures flavoring agent in an amount between 0.1 and 10 percent by thereof. weight of the total composition. 53. The composition of claim 32, wherein the active 66. The composition of claim 64, wherein the active compound is an agent for treating narcolepsy Selected from compound is an acetylcholinesterase inhibitorS Selected the group consisting of modafinil, mazindol, and mixtures from the group consisting of galantarnine, neostigmine, thereof. phySOStigmine, and edrophonium, and mixtures thereof. 54. The composition of claim 32, wherein the active 67. The composition of claim 64, wherein the active compound is an anti-depression agent Selected from the compound is a nerve impulse inhibitor Selected from the group consisting of amitriptyline, amoxapine, bupropion, group consisting of levobupivacaine, lidocaine, prilocaine, clomipramine, clomipramine, clorgyline, desipramine, dox mepivacaine, propofol, rapacuronium bromide, ropivacaine, epin, fluoxetine, imipramine, isocarboxazid, maprotiline, tubocurarine, atracurium, doxaurium, mivacurium, pancu mirtazapine, nefazodone, nortriptyline, paroxetine, ronium, Vercuronium, pipecuronium, rocuronium, and mix phenelZine, protriptyline, Sertraline, tranylcypromine, traZ tures thereof. odone, Venlafaxine, and mixtures thereof. 68. The composition of claim 64, wherein the active 55. The composition of claim 32, wherein the active compound is an anti-cholinergic Selected from the group compound is an agent for treating Parkinson's disease consisting of amantadine, ipratropium, OXitropium, dicyclo Selected from the group consisting of amantadine, bro verine, and mixtures thereof. mocriptine, carvidopa, levodopa, pergolide, Selegiline, and 69. The composition of claim 64, wherein the active mixtures thereof. compound is an anti-convulsant Selected from the group 56. The composition of claim 32, wherein the active consisting of acetazolamide, carbamazepine, clonazepam, compound is the benzodiazepine antagonist flumazenil. diazepam, divalproex, ethoSuximide, lamotrignine acid, 57. The composition of claim 32, wherein the active levetriacetam, Oxcarbazepine, phenobarbital, phenytoin, compound is the neurotransmitter antagonist deramciclane. pregabalin, primidone, remacemide, trimethadione, topira 58. The composition of claim 32, wherein the active mate, vigabatrin, Zonisamide, and mixtures thereof. compound is a Stimulant Selected from the group consisting 70. The composition of claim 64, wherein the active of amphetamine, dextroamphetamine, dinoprostone, meth compound is an anti-psychotic Selected from the group ylphenidate, methylphenidate, modafinil, pemoline, and consisting of amisulpride, aripiprazole bifemelane, bromp mixtures thereof. eridol, clozapine, chlorpromazine, haloperidol, illoperidone 59. The composition of claim 32, wherein the active loperidone, olanzapine, quetiapine, fluphenazine, fumarate, compound is the tranquilizer mesoridazine. risperidone, thiothixene, thioridazine, Sulpride, Ziprasidone, 60. The composition of claim 32, wherein the flavoring and mixtures thereof. agent is Selected from the group consisting of Synthetic or 71. The composition of claim 64, wherein the active natural oil of peppermint, oil of Spearmint, citrus oil, fruit compound is an anxiolytic agent Selected from the group flavors, Sweeteners, and mixtures thereof. consisting of amitryptiline, atracurium, buSpirone, chlorZOX 61. The composition of claim 32, wherein the propellant aZone, cloraZepate, cisatracurium, cyclobenzaprine, is Selected from the group consisting of propane, N-butane, eperisone, esopiclone, hydroxy Zine, mirtazapine, mivacu iso-butane, N-pentane, iso-pentane, neo-pentane, and mix rium, pagoclone, Sulperide, Zaleplon, Zopiclone, and mix tures thereof. tures thereof. 62. A method of administering a pharmacologically active 72. The composition of claim 64, wherein the active compound to a mammal comprising Spraying the oral compound is a dopamine metabolism inhibitor Selected from mucosa of the mammal with the composition of claim 32. the group consisting of entacapone, lazebemide, Selegiline, 63. The method of claim 62, wherein the amount of the tolcapone, and mixtures thereof. Spray is predetermined. 73. The composition of claim 64, wherein the active 64. A propellant free buccal Spray composition for trans compound is an agent to treat post Stroke Sequelae Selected mucosal administration of a pharmacologically active com from the group consisting of glatiramer, interferon beta 1A, pound comprising: interferon beta 1B, estradiol, progesterone, and mixtures an active compound in an amount between 0.005 and 55 thereof. percent by weight of the total composition Selected 74. The composition of claim 64, wherein the active from the group consisting of acetylcholinesterase compound is a neuroprotectant Selected from the group inhibitors, nerve impulse inhibitors, anti-cholinergics, consisting of donepezil, memanine, nimodipine, riluzole, anti-convulsants, anti-psychotics, anxiolytic agents, rivastigmine, tacrine, TAK147, Xaliproden, and mixtures dopamine metabolism inhibitors, agents to treat post thereof. Stroke Sequelae, neuroprotectants, agents to treat 75. The composition of claim 64, wherein the active Alzheimer's disease, neurotransmitters, neurotransmit compound is an agent to treat Alzheimer's disease Selected US 2004/O120895 A1 Jun. 24, 2004 from the group consisting of carbidopa, levodopa, tacrine, (C-C) esters, C7-Cs hydrocarbons of linear or branched doneZepil, rivastigmine, galantamine, and mixtures thereof. configuration, C-C alkanoyl esters, and triglycerides of 76. The composition of claim 64, wherein the active C-C carboxylic acids. compound is a neurotransmitter Selected from the group 89. The composition of claim 88, wherein the solvent is consisting of acetylcholine, Serotonin, 5-hydroxytryptamine miglyol. (5-HT), GABA, glutamate, aspartate, glycine, histamine, 90. A method of administering a pharmacologically active epinephrine, norpinephrine, dopamine, adenosine, ATP, compound to a mammal comprising Spraying the oral nitric oxide, and mixtures thereof. mucosa of the mammal with the composition of claim 64. 77. The composition of claim 64, wherein the active 91. The method of claim 90, wherein the amount of the compound is a neurotransmitter agonist Selected from the Spray is predetermined. group consisting of almotriptan, aniracetam, atomoxetine, 92. A buccal Spray composition for transmucosal admin benserazide, bromocriptine, bupropion, cabergoline, citalo istration of a pharmacologically active compound compris pram, clomipramine, desipramine, diazepam, dihydroer Ing: gotamine, doxepin dulloxetine, eletriptan, escitalopram, flu an active compound in an amount between 0.05 and 50 Voxamine, gabapentin, imipramine, moclobemide, percent by weight of the total composition Selected naratriptan, nefazodone, nefiracetam acamproSate, nicer from the group consisting of acetylcholinesterase goline, nortryptiline, paroxetine, pergolide, pramipexole, inhibitors, nerve impulse inhibitors, anti-cholinergics, rizatriptan, ropinirole, Sertraline, Sibutramine, Sumatriptan, anti-convulsants, anti-psychotics, anxiolytic agents, tiagabine, traZodone, Venlafaxine, Zolmitriptan, and mix dopamine metabolism inhibitors, agents to treat post tures thereof. Stroke Sequelae, neuroprotectants, agents to treat 78. The composition of claim 64, wherein the active Alzheimer's disease, neurotransmitters, neurotransmit compound is a Sedative Selected from the group consisting ter agonists, Sedatives, agents for treating attention of dexmedetomidine, eSZopiclone, indiplon, Zolpidem, Zale deficit disorder, agents for treating narcolepsy, central plon, and mixtures thereof. adregenic antagonists, anti-depression agents, agents 79. The composition of claim 64, wherein the active for treating Parkinson's disease, benzodiazepine compound is an agent for treating attention deficit disorder antagonists, Stimulants, neurotransmitter antagonists, Selected from the group consisting of amphetamine, dextro tranquilizers, and mixtures thereof, and amphetamine, methylphenidate, pemoline, and mixtures a non-polar solvent in an amount between 19 and 85 thereof. percent by weight of the total composition; and 80. The composition of claim 64, wherein the active a propellant in an amount between 5 and 80 percent by compound is an agent for treating narcolepsy Selected from weight of the total composition, wherein Said propel the group consisting of modafinil, mazindol, and mixtures lant is a C to Cs hydrocarbon of linear or brancehed thereof. configuration. 81. The composition of claim 64, wherein the active 93. The composition of claim 92, further comprising a compound is an anti-depression agent Selected from the flavoring agent in an amount of between 0.1 and 10 percent group consisting of amitriptyline, amoxapine, bupropion, by weight of the total composition. clomipramine, clomipramine, clorgyline, desipramine, dox 94. The composition of claim 93, wherein the flavoring epin, fluoxetine, imipramine, isocarboxazid, maprotiline, agent is Selected from the group consisting of Synthetic or mirtazapine, nefazodone, nortriptyline, paroxetine, natural oil of peppermint, oil of Spearmint, citrus oil, fruit phenelZine, protriptyline, Sertraline, tranylcypromine, traZ flavors, Sweeteners, and mixtures thereof. odone, Venlafaxine, and mixtures thereof. 95. A buccal Spray composition for transmucosal admin 82. The composition of claim 64, wherein the active istration of a pharmacologically active compound compris compound is an agent for treating Parkinson's disease ing: Selected from the group consisting of amantadine, bro an active compound in an amount between 0.01 and 40 mocriptine, carvidopa, levodopa, pergolide, Selegiline, and percent by weight of the total composition Selected mixtures thereof. from the group consisting of acetylcholinesterase 83. The composition of claim 64, wherein the active inhibitors, nerve impulse inhibitors, anti-cholinergics, compound is the benzodiazepine antagonist flumazenil. anti-convulsants, anti-psychotics, anxiolytic agents, 84. The composition of claim 64, wherein the active dopamine metabolism inhibitors, agents to treat post compound is the neurotransmitter antagonist deramciclane. Stroke Sequelae, neuroprotectants, agents to treat 85. The composition of claim 64, wherein the active Alzheimer's disease, neurotransmitters, neurotransmit compound is a Stimulant Selected from the group consisting ter agonists, Sedatives, agents for treating attention of amphetamine, dextroamphetamine, dinoprostone, meth deficit disorder, agents for treating narcolepsy, central ylphenidate, methylphenidate, modafinil, pemoline, and adregenic antagonists, anti-depression agents, agents mixtures thereof. for treating Parkinson's disease, benzodiazepine 86. The composition of claim 64, wherein the active antagonists, Stimulants, neurotransmitter antagonists, compound is the tranquilizer mesoridazine. tranquilizers, and mixtures thereof, and 87. The composition of claim 65, wherein the flavoring a non-polar solvent in an amount between 25 and 89 agent is Selected from the group consisting of Synthetic or percent by weight of the total composition; natural oil of peppermint, oil of Spearmint, citrus oil, fruit a propellant in an amount between 10 and 70 percent by flavors, Sweeteners, and mixtures thereof. weight of the total composition, wherein Said propel 88. The composition of claim 64, wherein the solvent is lant is a C to Cs hydrocarbon of linear or brancehed Selected from the group consisting of (C-C) fatty acid configuration; and US 2004/O120895 A1 Jun. 24, 2004

A flavoring agent is present in an amount between 1 and 107. The composition of claim 92, wherein the active 8 percent by weight of the total composition. compound is a dopamine metabolism inhibitor Selected from 96. The composition of claim 95, wherein the propellant the group consisting of entacapone, lazebemide, Selegiline, is present in an amount between 20 and 70 percent by weight tolcapone, and mixtures thereof. of the total composition, the non-polar Solvent is present in 108. The composition of claim 92, wherein the active an amount between 25 and 75 percent by weight of the total compound is an agent to treat post Stroke Sequelae Selected composition, the active compound is present in an amount from the group consisting of glatiramer, interferon beta 1A, from between 0.25 and 35 percent by weight of the total interferon beta 1B, estradiol, progesterone, and mixtures composition, and the flavoring agent is present in an amount thereof. between 2 and 7.5 percent by weight of the total composi 109. The composition of claim 92, wherein the active tion. compound is a neuroprotectant Selected from the group 97. The composition of claim 92, wherein the propellant consisting of donepezil, memanine, nimodipine, riluzole, is Selected from the group consisting of propane, n-butane, rivastigmine, tacrine, TAK147, Xaliproden, and mixtures iso-butane, n-pantane, iso-pentane, neo-pentane, and mix thereof. tures thereof. 110. The composition of claim 92, wherein the active 98. The composition of claim 97, wherein the propellant compound is an agent to treat Alzheimer's disease Selected is n-butane or iso-butane and has a water content of not more from the group consisting of carbidopa, levodopa, tacrine, than 0.2 percent and a concentration of oxidizing agents, doneZepil, rivaStigmine, galantamine, and mixtures thereof. reducing agents, Lewis acids, and Lewis bases of less than 111. The composition of claim 92, wherein the active 0.1 percent. compound is a neurotransmitter Selected from the group 99. The composition of claim 92, wherein the solvent is consisting of acetylcholine, Serotonin, 5-hydroxytryptamine Selected from the group consisting of (C-C) fatty acid (5-HT), GABA, glutamate, aspartate, glycine, histamine, (C-C) esters, C7-Cs hydrocarbons of linear or branched epinephrine, norpinephrine, dopamine, adenosine, ATP, configuration, C-C alkanoyl esters, and triglycerides of nitric oxide, and mixtures thereof. 112. The composition of claim 92, wherein the active C-C carboxylic acids. compound is a neurotransmitter agonist Selected from the 100. The composition of claim 99, wherein the solvent is group consisting of almotriptan, aniracetam, atomoxetine, miglyol. benserazide, bromocriptine, bupropion, cabergoline, citalo 101. The composition of claim 92, wherein the active pram, clomipramine, desipramine, diazepam, dihydroer compound is an acetylcholinesterase inhibitorS Selected gotamine, doxepin dulloxetine, eletriptan, escitalopram, flu from the group consisting of galantamine, neostigmine, VOXamine, gabapentin, imipramine, moclobemide, phySOStigmine, and edrophonium, and mixtures thereof. naratriptan, nefazodone, nefiracetam acamproSate, nicer 102. The composition of claim 92, wherein the active goline, nortryptiline, paroxetine, pergolide, pramipexole, compound is a nerve impulse inhibitor Selected from the rizatriptan, ropinirole, Sertraline, Sibutramine, Sumatriptan, group consisting of levobupivacaine, lidocaine, prilocaine, tiagabine, traZodone, Venlafaxine, Zolmitriptan, and mix mepivacaine, propofol, rapacuronium bromide, ropivacaine, tures thereof. tubocurarine, atracurium, doxaurium, mivacurium, pancu 113. The composition of claim 92, wherein the active ronium, Vercuronium, pipecuronium, rocuronium, and mix compound is a Sedative Selected from the group consisting tures thereof. of deXmedetomidine, eSZopiclone, indiplon, Zolpidem, Zale 103. The composition of claim 92, wherein the active plon, and mixtures thereof. compound is an anti-cholinergic Selected from the group 114. The composition of claim 92, wherein the active consisting of amantadine, ipratropium, OXitropium, dicyclo compound is an agent for treating attention deficit disorder verine, and mixtures thereof. Selected from the group consisting of amphetamine, dextro 104. The composition of claim 92, wherein the active amphetamine, methylphenidate, pemoline, and mixtures compound is an anti-convulsant Selected from the group thereof. consisting of acetazolamide, carbamazepine, clonazepam, 115. The composition of claim 92, wherein the active diazepam, divalproex, ethoSuximide, lamotrignine acid, compound is an agent for treating narcolepsy Selected from levetriacetam, Oxcarbazepine, phenobarbital, phenytoin, the group consisting of modafinil, mazindol, and mixtures pregabalin, primidone, remacemide, trimethadione, topira thereof. mate, vigabatrin, Zonisamide, and mixtures thereof. 116. The composition of claim 92, wherein the active 105. The composition of claim 92, wherein the active compound is an anti-depression agent Selected from the compound is an anti-psychotic Selected from the group group consisting of amitriptyline, amoxapine, bupropion, consisting of amisulpride, aripiprazole bifemelane, bromp clomipramine, clomipramine, clorgyline, desipramine, dox eridol, clozapine, chlorpromazine, haloperidol, illoperidone epin, fluoxetine, imipramine, isocarboxazid, maprotiline, loperidone, olanzapine, quetiapine, fluphenazine, fumarate, mirtazapine, nefazodone, nortriptyline, paroxetine, risperidone, thiothixene, thioridazine, Sulpride, Ziprasidone, phenelZine, protriptyline, Sertraline, tranylcypromine, traZ and mixtures thereof. odone, Venlafaxine, and mixtures thereof. 106. The composition of claim 92, wherein the active 117. The composition of claim 92, wherein the active compound is an anxiolytic agent Selected from the group compound is an agent for treating Parkinson's disease consisting of amitryptiline, atracurium, buSpirone, chlorZOX Selected from the group consisting of amantadine, bro aZone, cloraZepate, cisatracurium, cyclobenzaprine, mocriptine, carvidopa, levodopa, pergolide, Selegiline, and eperisone, esopiclone, hydroxy Zine, mirtazapine, mivacu mixtures thereof. rium, pagoclone, Sulperide, Zaleplon, Zopiclone, and mix 118. The composition of claim 92, wherein the active tures thereof. compound is the benzodiazepine antagonist flumazenil. US 2004/O120895 A1 Jun. 24, 2004

119. The composition of claim 92, wherein the active 121. The composition of claim 92, wherein the active compound is the neurotransmitter antagonist deramciclane. compound is the tranquilizer mesoridazine. 122. A method of administering a pharmacologically 120. The composition of claim 92, wherein the active active compound to a mammal comprising Spraying the oral compound is a Stimulant Selected from the group consisting mucosa of the mammal with the composition of claim 92. of amphetamine, dextroamphetamine, dinoprostone, meth 123. The method of claim 122, wherein the amount of the ylphenidate, methylphenidate, modafinil, pemoline, and Spray is predetermined. mixtures thereof. k k k k k