Paraxanthine-based bioactive compositions and methods of using the same

Abstract

To provide a dietary supplement for human consumption, including enhancement of at least one of endurance, mood, vitality, lipolysis, energy expenditure, task performance and / or appetite reduction. Further provided are methods of enhancing physical performance or energy in a subject.SOLUTION: A dietary supplement is provided comprising a first active ingredient comprising paraxanthine, whether natural or synthetic, from about 2mg to about 800mg.SELECTED DRAWING: Figure 1

Description

[Technical Field]

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS

[0001] This application relates to the "Biological Activity of Paraxanthine-Based Compounds" filed on January 23, 2020. This application claims priority to U.S. Patent Application No. 62 / 964,976, entitled "Suitable Compositions and Methods of Using the Same," which is incorporated herein by reference in its entirety.

[0002]

[0002] The disclosed technology generally relates to paracetamol for use in providing physiological benefits. The present disclosure relates to compositions, methods, and systems utilizing paraxanthine alone and in combination. More particularly, the present disclosure relates to paraxanthine and other compounds, whether synthetically produced or derived from natural sources, and the use of these chemical compounds to provide physiological benefits, which can be varied by the concentration of paraxanthine and the presence of synergists and antagonists. [Background technology]

[0003] Paraxanthine is 1,7-dimethylxanthine or 1,7-dimethyl-3H Also known as 1,7-purine-2,6-dione, it is a dimethyl derivative of xanthine. It is structurally related to caffeine and its metabolites and accounts for 80% of total caffeine excretion in humans. In humans and other animals, caffeine is first broken down into either paraxanthine (1,7-dimethylxanthine), theobromine, or theophylline. Paraxanthine is naturally observed as a caffeine metabolite in animals and humans. Paraxanthine has also been found naturally occurring in various plant species, such as Citrus paradisi (grapefruit), Theobroma cacao (cocoa), and Camilia sinensis (tea).

[0004] Caffeine is a bitter-tasting white crystalline purine and methylxanthine alkaloid. It is a base that is chemically related to the adenine and guanine bases of deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). Caffeine is found in the seeds, fruits, or leaves of several plants native to Africa, East Asia, and South America, where it helps protect these areas from predatory insects and prevent nearby seeds from germinating. The best-known source of caffeine is coffee beans, which are the incorrectly named seeds of plants in the genus Coffea.

[0005] Caffeine is by far the most common vitamin D compound found in coffee and tea products. It is the most commonly studied and used stimulant. Paraxanthine appears to have effects greater than those of caffeine, despite being very similar in chemical structure to caffeine. Recent experiments have shown that paraxanthine exhibits a range of activities, some of which appear inconsistent.

[0006]

[0006] Past epidemiological studies have raised the potential for coffee and caffeine consumption Concerns about health risks appear to be exacerbated by the association of heavy coffee consumption with unhealthy behaviors, such as smoking and physical inactivity. More recently, coffee consumption has been associated with a reduced risk of several chronic diseases.

[0007]

[0007] The caffeine concentration in coffee beverages can vary considerably. A standard cup of coffee is often said to contain 100 mg of caffeine, but A recent analysis of 14 different specialty coffees purchased from a coffee shop found that the amount of caffeine in an 8-ounce serving of brewed coffee ranged from 72 to 130 mg (McCusker, RR, Goldberger, BA, and Cone, EJ, 2003, Caffeine content of specialty coffees. J. Anal. Toxicol., 27:520-522). Caffeine in espresso coffee ranged from 58 to 76 mg per single shot. Interestingly, the caffeine content of the same type of coffee purchased from the same store on six separate days varied from 130 mg to 282 mg per 8-ounce serving. Summary of the Invention [Problem to be solved by the invention]

[0008]

[0008] Therefore, the art is replete with alternative chemical compounds and methods that may offer benefits. It is also desirable to provide chemical compounds and mixtures thereof that can be used to provide different benefits in varying concentrations, thereby requiring less raw material production. [Means for solving the problem]

[0009]

[0009] The present disclosure relates to paraxanthine, whether naturally produced or synthetically produced. The present invention relates to the use of a chemical composition containing paraxanthine and optionally other chemicals, such as paraxanthine homologs or analogs, to provide multiple desired effects. Paraxanthine analogs include, but are not limited to, caffeine, methylcaffeine, theobromine, theophylline, liberine, and methylliberine, and variants thereof. Other suitable active substances may include one or more ergogenic or nootropic compounds, such as St. John's wort, sulbutiamine, etc.

[0010]

[0010] Paraxanthine exhibits a wide variety of effects depending on the dosage. Its effects can also be modulated by increasing the amount of paraxanthine. Paraxanthine can be used to enhance endurance, mood, calmness and concentration, vitality, lipolysis, energy expenditure, exercise performance, and / or appetite reduction. Paraxanthine can also function as an antioxidant and anti-inflammatory agent.

[0011] In one embodiment, paraxanthine is used to regulate stimuli, thereby preventing insufficiency. It can be used to provide increased energy without increased relaxation or tension. As noted herein, inter-individual variability is possible.

[0012] In another embodiment, paraxanthine is a mild mood enhancer. It can be used as a relaxant or sedative.

[0013] In a further embodiment, paraxanthine is effective in reducing appetite. It can be used to promote weight loss and as an antioxidant and anti-inflammatory agent. Paraxanthine can be used transdermally to enhance one or more of these effects.

[0013]

[0014] In one embodiment, paraxanthine, whether natural or synthetic, is used via fermentation. A dietary supplement containing about 2 mg to about 800 mg of niacin is provided.

[0015] In another embodiment, the treatment for enhancing physical performance or energy in an individual The method includes providing an individual with a composition containing about 2 mg to about 800 mg of paraxanthine, whether natural or synthetic, wherein, upon administration of the composition, the individual experiences improved endurance, mood, calmness and focus, increased energy, and a decreased fat content. The subject experiences at least one of increased lipolysis, energy expenditure, task performance, and / or decreased appetite. In another embodiment, a second compound, such as caffeine, can also be used in the composition.

[0014]

[0016] Therefore, the purpose of this disclosure is to develop a parametric system that can provide multiple positive effects. The present invention provides a composition comprising sanchin.

[0017] Another object of the present disclosure is to provide paraxanthine homologs, derivatives and iterants. The objective of the present invention is to provide a synthetic chemical equivalent of paraxanthine, as well as a synthetic chemical equivalent of paraxanthine.

[0015]

[0018] Another object of the present disclosure is to provide agglomerated paraxanthine, paraxanthine salts, mica, and the like. The present invention provides encapsulated, liposomal or esterified paraxanthine.

[0016]

[0019] Another object of the present disclosure is to provide a method for the preparation of glycerides, propylene glycol, polyethylene glycol, The present invention provides paraxanthine combined with PEG, lauroyl macrogol, lauroyl macrogol derivatives, and co-crystallized products of paraxanthine.

[0017]

[0020] While multiple embodiments are disclosed, still other embodiments of the present disclosure include the combination of the present disclosure. It will become apparent to those skilled in the art from the following detailed description, which shows and describes exemplary embodiments of the compositions, systems, and methods. It will be understood that the compositions, systems, and methods of the present disclosure are capable of modification in various obvious aspects, all without departing from the spirit and scope of the present disclosure. Accordingly, the drawings and detailed description are to be regarded as illustrative in nature and not as restrictive. [Brief explanation of the drawings]

[0018] [Figure 1]

[0021] 1 is a graph showing the number of correct responses in the BCST test. [Figure 2]

[0022] 1 is a graph showing the number of incorrect answers in a BSCT test. [Figure 3]

[0023] 1 is a graph showing the number of perseverative errors (PEBL) in the BSCT test. [Figure 4]

[0024] 1 is a graph showing the number of perseverative errors (PAR) in the BSCT test. [Figure 5]

[0025] 1 is a graph showing the mean accuracy of correct responses in a Go / No-Go test. [Figure 6]

[0026] 10 is a graph showing the average response time under condition P in the first round of the Go / No-Go test. [Figure 7]

[0027] 1 is a graph showing the average response time under condition R in the first round of the Go / No-Go test. [Figure 8]

[0028] 10 is a graph showing the average response time under condition P in the second round of the Go / No-Go test. [Figure 9]

[0029] 10 is a graph showing the average response time in the second round of the Go / No-Go test under condition R. [Figure 10]

[0030] 1 is a graph showing the average response time of a Go / No-Go test. [Figure 11]

[0031] 10 is a graph showing reaction times for trial number 2 in the vigilance test. [Figure 12]

[0032] 10 is a graph showing reaction times for trial number 10 in the vigilance test. [Figure 13]

[0033] 10 is a graph showing reaction times for trial number 20 in the vigilance test. [Figure 14]

[0034] 1 is a graph showing the average reaction time of a vigilance test. [Figure 15]

[0035] 1 is a graph showing absent reaction times for letter length 2 in the Sternberg test. [Figure 16]

[0036] 10 is a graph showing reaction times for the non-presence task of letter length 4 in the Sternberg test. [Figure 17]

[0037] 10 is a graph showing reaction times for the absence task of letter length 6 in the Sternberg test. [Figure 18]

[0038] 10 is a graph showing reaction times for the character length 2 presence task in the Sternberg test. [Figure 19]

[0039] 10 is a graph showing reaction times for the character length 4 presence task in the Sternberg test. [Figure 20]

[0040] 10 is a graph showing reaction times for the presence task of character length 6 in the Sternberg test. [Figure 21]

[0041] FIG. 1 shows a bitterness scale. [Figure 22]

[0042] 1 is a table showing solutions, abbreviations and concentrations. [Figure 23]

[0043] 1 is a table showing the results of a tasting survey on bitterness. [Figure 24]

[0044] FIG. 1 shows the results of a tasting survey on bitterness on a bitterness scale. [Figure 25]

[0045] 1 is a table showing comments from tasters who participated in a bitterness study. DETAILED DESCRIPTION OF THE INVENTION

[0019]

[0046] Before describing one or more embodiments of the present invention in detail, it is important to note that the present invention is not limited to the above embodiments. It is to be understood that the present invention is not limited to the details of construction and the arrangement of components set forth in the following description or illustrated in the drawings. The invention is capable of other embodiments and of being practiced and carried out in various ways. Also, it is to be understood that the phraseology and terminology used herein is for the purpose of description and should not be regarded as limiting.

[0020]

[0047] As used herein, ranges are expressed from "about" one particular value and / or to "about" another particular value. Ranges may be expressed in terms such as "up to a particular value." When such a range is expressed, a further aspect includes from the one particular value stated and / or to the other particular value stated. Similarly, when values ​​are expressed as approximations, by use of the antecedent "about," it is understood that the particular value stated forms a further aspect. It is further understood that the endpoints of each of the ranges are significant both in relation to the other endpoint, and independently of the other endpoint. It is also understood that there are a number of values ​​disclosed herein, and that each value is herein disclosed "about" that particular value as well as the particular value itself. For example, if the value "10" is disclosed, then "about 10" is also disclosed. It is also understood that each intervening unit value is disclosed. For example, if 10 and 15 are disclosed, then 11, 12, 13, and 14 are also disclosed.

[0021]

[0048] As used herein, the term "subject" refers to the target of administration, e.g., an animal. Thus, the subject of the methods disclosed herein may be a human, non-human primate, horse, pig, rabbit, dog, sheep, goat, cow, cat, guinea pig, or rodent. The term does not denote a particular age or sex. Thus, it is intended to encompass adult and newborn / baby subjects, as well as fetuses / babies, regardless of sex. In one embodiment, the subject is a mammal. A patient refers to a subject suffering from a disease or disorder.

[0022]

[0049] As used herein, the term "treatment" means the cure of a disease, pathological condition, or disorder. "Medical management" refers to the medical management of a patient with the goal of improving, ameliorating, stabilizing, or preventing a disease, pathological condition, or disorder. The term encompasses active treatment, i.e., treatment specifically aimed at reversing the disease, pathological condition, or disorder, and also encompasses causal treatment, i.e., treatment aimed at eliminating the cause of the associated disease, pathological condition, or disorder. In addition, the term encompasses palliative treatment, i.e., treatment designed to relieve symptoms rather than cure the disease, pathological condition, or disorder; preventative treatment, i.e., treatment aimed at minimizing or partially or completely inhibiting the onset of the associated disease, pathological condition, or disorder; and supportive treatment, i.e., treatment used to supplement another specific therapy aimed at reversing the associated disease, pathological condition, or disorder. In various embodiments, the term encompasses all treatments of subjects, including mammals (e.g., humans), and includes (i) preventing the onset of the disease in subjects who may be predisposed to the disease but have not yet been diagnosed as having the disease, (ii) inhibiting the disease, i.e., preventing its development, or (iii) alleviating the disease, i.e., causing regression of the disease. In one embodiment, the subject is a mammal, e.g., a primate, and in a further embodiment, the subject is a human. The term "subject" also encompasses domestic animals (e.g., cats, dogs, etc.), livestock (e.g., cattle, horses, pigs, sheep, goats, etc.), and laboratory animals (e.g., mice, rabbits, rats, guinea pigs, fruit flies, etc.).

[0023]

[0050] As used herein, the terms "effective amount" and "amount effective" refer to a dose that is effective to achieve a desired result. The term "therapeutically effective amount" refers to an amount sufficient to achieve a desired therapeutic result or to affect an undesired condition. For example, a "therapeutically effective amount" refers to an amount sufficient to achieve a desired therapeutic result or to affect an undesired symptom, but generally insufficient to cause unacceptable adverse side effects. The specific therapeutically effective dose level for any particular patient will depend on various factors. Such factors include the disorder being treated and the severity of the disorder; the specific composition used; the patient's age, weight, general health, sex, and diet; the time of administration; the route of administration; the excretion rate of the specific compound used; the duration of treatment; and drugs used in combination with or in combination with the specific compound used, all of which are well known in the medical field. For example, it is well within the skill of the art to start a dose of a compound at a level lower than that required to achieve the desired therapeutic effect and gradually increase the dose until the desired effect is achieved. If desired, an effective daily dose may be divided into doses for multiple administration. Consequently, a single dose of a composition can contain the amount that is the daily dose, or submultiples thereof that together make up the daily dose. Dosage and administration can be adjusted by individual physicians if there are any contraindications.Dosage and administration can be varied, and can be administered once or multiple times a day for one or several days.Guidance can be found in the literature for the appropriate dosage and administration of a given class of pharmaceutical product.In further various embodiments, the preparation can be administered in a "prophylactically effective amount", that is, in an amount effective for preventing a disease or condition.

[0024]

[0051] Compositions containing paraxanthine and related uses thereof are disclosed. Paraxanthine is also known as 1,7-dimethylxanthine or 1,7-dimethyl-3H-purine-2,6-dione. Paraxanthine may be produced synthetically or isolated from natural sources or via fermentation. Paraxanthine isolated from such sources may be purified to greater than 95% purity. Optionally, lower purification may be used, such that paraxanthine constitutes 50% or even less of the raw material. In some embodiments, it may be preferable to utilize paraxanthine isolated from natural sources, which may include other paraxanthine congeners typically found in paraxanthine sources.

[0025]

[0052] In certain embodiments, paraxanthine has multiple positive effects in a subject. Paraxanthine may be combined with one or more other chemical compounds (e.g., other active ingredients) to improve the efficacy of paraxanthine. By varying the dosage of paraxanthine and / or the chemical compounds combined with paraxanthine, various targeted physiological effects can be selected. The composition may primarily provide a single benefit, or may simultaneously provide multiple benefits.

[0026]

[0053] In certain embodiments, paraxanthine is a soluble form of gallic acid, (+)-catechin (C ), (-)-epicatechin (EC), (+)-gallocatechin (GC), (-)-epigallocatechin (EGC), (-)-catechin gallate (CG), (-)-gallocatechin gallate (GCG), (-)-epicatechin gallate (ECG) and (-)-epigallocatechin gallate (EGCG), glycerides, propylene glycol, lauroyl macrogol, lauroyl macrogol derivatives, bio Co-crystallized products of bioperine, piperine, black pepper, bergamottin, dihydroxybergamottin (CYP3A4), flavonoids (naringin, hesperidin, nobiletin, tangeretin, quercetin), pterostilbene, fisetin, phytosome, salicin, fish oil (ω-3 fatty acids and specialized small lipid resolution epoxide derivatives) Lipid pro-resolving epoxide derivative), oxylipins, tart cherry, krill oil, astaxanthin, proteolytic enzymes, glucosamine sulfate, chondroitin sulfate, MSM (methylsulfonylmethane), SAMe (S-adenosylmethionine), ASU (avocado-soybean unsapponizable fraction), cetyl myristoleate, Dolichos falcate, triterpenoids, acacia catechu, Andrographis paniculata, Scutalleria baicalensis, agmatine sulfate, nettle, sea buckthorn, curcumin, Cissus quadrilangularis, Boswellia serrata, Wasabia japonica (wasabi extract used in tea tree oil), emu oil, arnica, Mangifera indica L.(Anacardiaceae), Lagenaria breviflora, Zingiber officinale (ginger and gingerol / shogaol), Hoodia gordonii, Caffeine, Yohimbine, Methylsynephrine, Synephrine, Theobromine, Flavenoids, Tocopherol, Theophylline, Alpha-Yohimbine, Conjugated Linoleic Acid (CLA), Octopamine, Evodiamine, Passionflower, Red Pepper, Cayenne, Raspberry Ketone, Guggul, Green Tea, Guarana, Kola Nut, Beta-Phenethylamine, Acacia rigidula, Forskolin (Coleus forskohlli), Theophylline, Synephrine, Yohimbine, Rhodiola, Ashwagandha, Ginseng, Ginkgo Biloba, Siberian ginseng), Astragalus ginseng, licorice root, green tea, reishi mushroom, dehydroepiandrosterone (DHEA), pregnenolone, tyrosine, N-acetyltyrosine, glucuronolactone, taurine, acetyl-L-carnitine, 5-hydroxytryptophan, tryptophan, phenethylamine, Sceletium tortuosum (and mesembrine alkaloids), Dendrobium species, Acacia rigidula, PQQ (pyrroloquinoline quinone), ubiquinone (01), nicotinamide riboside, picamilon, huperzine A (Huperzia serrata), L-dopa, Mucuna pruriens, and forskolin (Coleus forskohlii), 2-(dimethylamino)ethanol (DMAE), DMAE bittertrate, and combinations thereof.

[0027]

[0054] In another embodiment, paraxanthine is administered at lower dosage levels and / or Alternatively, it may be used in conjunction with a compound that regulates or antagonizes its activity. Such compositions may induce enhanced endurance performance, mood, energy, lipolysis, energy expenditure, task performance and / or appetite reduction.

[0028]

[0055] The advantage of using the present invention is that the person using the chemical composition according to the principles of the present invention is The main drawback is that they may be less likely to develop resistance to the effects induced in a person, i.e., they may not reduce the person's sensitivity to the effects induced in them.

[0029]

[0056] According to certain embodiments, the paraxanthine-containing compositions of the present disclosure are Paraxanthine offers at least the following distinct advantages over the administration of compositions containing paraxanthine: Paraxanthine is substantially less toxic; Paraxanthine is more stable (e.g., it does not lose its potency over time as much as caffeine); Paraxanthine-containing compositions are more potent wake-promoting agents (in certain embodiments, via adenosine receptor antagonism); Paraxanthine-containing compositions enhance striatal dopaminergic tone; Paraxanthine does not produce sleep rebound; Paraxanthine does not produce withdrawal effects as frequently as caffeine upon cessation of use; Paraxanthine does not increase anxiety; Paraxanthine is less bitter than caffeine; and Paraxanthine is more effective in larger populations than caffeine.

[0030]

[0057] In another embodiment, paraxanthine is administered at higher dosage levels and / or Or it can be used together with a synergistic compound. These compositions can increase an individual's basal / resting metabolic rate, increase thermogenesis, reduce appetite, improve cognitive performance, increase alpha wave brain activity, and / or induce a sense of well-being. Without being bound by theory, the inventors believe that at higher dosage levels, paraxanthine can exhibit noradrenergic and dopaminergic properties and can exhibit increased adenosine receptor inhibition.

[0031]

[0058] In another embodiment, paraxanthine is selected from the group consisting of ephedrine, caffeine, salicylic acid, and the like. The combination may be combined with paraxanthine or other benzoates, such as benzocaine, benzoyl alcohol, or benzocaine. This combination may result in a synergistic effect with the stimulating effect of paraxanthine. For example, in certain embodiments, paraxanthine is combined with a much smaller amount of caffeine to modulate the excessive stimulating effect of caffeine, thereby stabilizing heart rate and other metabolic activity. Thus, the combination of paraxanthine and caffeine results in a composition that provides the increased focus and energy induced by caffeine, but does not increase heart rate or blood pressure, due to the modulation of caffeine's effects by paraxanthine. Therefore, this combination can result in increased alertness and calmness without the jitteriness that can be caused by caffeine.

[0032]

[0059] According to a further embodiment, a dietary supplement comprising paraxanthine improves exercise performance. Paraxanthine is used to enhance athletic performance. According to exemplary aspects of these embodiments, dietary supplements containing paraxanthine can reduce fatigue, increase energy, improve mobility, and enhance alertness. In further embodiments, the composition of the present disclosure is administered for cardioprotection. In further embodiments, the composition of the present disclosure enhances muscle contraction and muscle performance. In exemplary aspects of these embodiments, muscle performance is enhanced through increasing potassium (K+) transport into skeletal muscle. In a further aspect, muscle performance is enhanced through increasing intracellular calcium (e.g., by activating ryanodine receptors (RyRs)).

[0033]

[0060] In another embodiment, paraxanthine has skin lightening and firming properties. Paraxanthine may be used as a topical agent for incorporation into body creams or lotions to produce creams or lotions for the purpose of reducing sebum and / or increasing skin elasticity. Paraxanthine topical agents may be used to promote transdermal fat loss in localized areas. Furthermore, paraxanthine may be used in creams or lotions to promote enhanced metabolism and / or enhanced thermogenesis in localized areas.

[0034]

[0061] According to a further embodiment, paraxanthine is an analgesic and / or anti-inflammatory agent. In an exemplary implementation, paraxanthine is combined with one or more of ibuprofen, salicylic acid, anti-inflammatory agents, salicin, fish oil (omega-3 fatty acids and specific small lipid resolution epoxide derivatives), tart cherry, krill oil, astaxanthin, proteolytic enzymes, glucosamine sulfate, chondroitin sulfate, MSM (methylsulfonylmethane), SAMe (S-adenosylmethionine), ASU (avocado-soybean unsaponifiable fractions), cetyl myristoleate, Dolichos falcate, and / or triterpenoids.

[0035]

[0062] The dosage of paraxanthine can range from about 2 mg to about 800 mg. In another embodiment, the dosage range of paraxanthine may be from about 50 mg to about 400 mg.

[0036]

[0063] In another embodiment, paraxanthine is In exemplary embodiments, bioavailability enhancers include, but are not limited to, bioperine, piperine, black pepper, bergamottin, dihydroxybergamottin (a CYP3A4 inhibitor), flavonoids (including hesperidin, naringin, tangeritin, quercetin, and nobiletin, either individually or in combination), pterostilbene, fisetin, nanoencapsulation, microencapsulation, liposomes, and / or phytosomes. The enhancer or enhancers combined with paraxanthine may depend on the properties of paraxanthine desired for a particular use.

[0037]

[0064] In another embodiment, paraxanthine is administered using one or more delivery methods. Paraxanthine may be administered via various topical applications, including transdermal patches and / or creams, ready-to-mix powders, intravenous injections, capsules, tablets, liquids (including liquids that are mixed with other beverages), softgels, shot formats, and / or cosmetic applications such as soaps, lotions, and shampoos. The anti-inflammatory properties of paraxanthine may be desirable for a variety of topical applications. Treatment method

[0065] According to certain embodiments, the compositions disclosed herein may be used in combination with one or more medical In certain implementations, the compositions of the present disclosure are used in treating conditions such as narcolepsy, sleep apnea and shift work sleep disorder, insomnia, epilepsy, attention deficit disorder, attention deficit hyperactivity disorder (ADHD), cognitive deficit disorder, paralysis, uncontrolled anger, migraines, substance abuse and addiction, and the like. The drug is administered to subjects suffering from steroid abuse addiction, eating disorders, depression, anxiety disorders, traumatic head injury (TBI), Parkinson's disease, Alzheimer's disease, and / or dementia.

[0038]

[0066] In certain aspects, the compositions of the present disclosure are neuroprotective agents. In an exemplary aspect of these embodiments, the compositions of the present disclosure are administered to a subject in need thereof for the purpose of neuroprotection. In an exemplary aspect of these embodiments, this neuroprotection takes the form of protection from dopaminergic cell death.

[0039]

[0067] According to further embodiments, the compositions of the present disclosure are useful for treating geriatric depression. In exemplary embodiments, the compositions are effective in treating subjects suffering from geriatric depression, whether of essential, vascular, or traumatic origin, and mental deterioration seen in the elderly.

[0040]

[0068] Administration of the compositions of the present disclosure to a subject includes any method of providing a pharmaceutical preparation to a subject. Such methods are well known to those skilled in the art and include, but are not limited to, oral administration, transdermal administration, administration by inhalation, intranasal administration, topical administration, intravaginal administration, ocular administration, intraaural administration, intracerebral administration, rectal administration, sublingual administration, intradermal administration, buccal administration, and parenteral administration, including injections, e.g., intravenous administration, intraarterial administration, intramuscular administration, and subcutaneous administration. Administration can be continuous or intermittent. In various embodiments, the preparations can be administered therapeutically, i.e., to treat an existing disease or condition. In further various embodiments, the preparations can be administered prophylactically, i.e., to prevent a disease or condition.

[0041]

[0069] One general embodiment can contain from about 2 mg to about 800 mg of paraxanthine. Another embodiment of this aspect includes corresponding computer systems, apparatus, and computer programs recorded on one or more computer storage devices, each configured to perform the operations of the methods of the present invention.

[0042]

[0070] Implementations may include one or more of the following features: The nutritional supplement contains gallic acid, (+)-catechin (c), (-)-epicatechin (ec), (+)-gallocatechin (gc), (-)-epigallocatechin (egc), (-)-catechin gallate (cg), (-)-gallocatechin gallate (gcg), (-)-epicatechin gallate (ecg) and (-)-epigallocatechin gallate (egcg), glycerides, propylene glycol, lauroyl macrogol, lauroyl macrogol derivatives, co-crystallized products of BioPerine, piperine, black pepper, bergamottin, dihydroxybergamottin (cyp3a4), flavonoids. Bonoids (naringin, hesperidin, nobiletin, tangeretin, quercetin), pterostilbene, fisetin, phytosome, salicin, fish oil (omega-3 fatty acids and specific small lipids) anti-inflammatory epoxide derivatives, oxylipins, tart cherry, krill oil, astaxanthin, proteolytic enzymes, glucosamine sulfate, chondroitin sulfate, methylsulfonylmethane (MSM), S-adenosylmethionine (SAME), avocado-soybean unsaponifiable matter fragments (ASU), cetyl myristoleate, dolichosfalcate, triterpenoids, acacia catechu, andrographis paniculata, scutalleria baicalensis, agmatine sulfate, nettle, sea buckthorn, curcumin, cissus quadrilangularis, boswellia serrata, wasabia japonica Japonica (wasabi extract used in tea tree oil), emu oil, arnica, mangifera indical (Anacardiaceae), lagenaria breviflora, zingiber officinale (ginger and gingerol / shogaol), hoodia gordonii, caffeine, yohimbine, methylsynephrine, synephrine, theobromine, flavenoids, tocopherol, theophylline, alpha-yohimbine, conjugated linoleic acid (CLA), octopamine, evodiamine, passionflower, red pepper, cayenne, raspberry ketone, guggul, green tea, guarana, kola nut, beta-phenethylamine, acacia rigidula, forskolin (co leus forskohlli), theophylline, synephrine, yohimbine, Rhodiola rosea, ashwagandha, Korean ginseng, ginkgo biloba, Eleuthero, Astragalus senticosus, licorice, green tea, reishi mushroom, dehydroepiandrosterone (DHEA), pregnenolone, tyrosine, n-acetyltyrosine, glucuronolactone, taurine, acetyl-l-carnitine, 5-hydroxytryptophan, tryptophan, phenethylamine, Sceletium tortuosum (and mesembrine alkaloids), Dendrobium species, Acacia rigidula, PQQ (pyrroloquinoline quinone), ubiquinone (O1), nicotinamide riboside, picamilon, huperzine A (Huperzia serrata or Huperzia serrata), l-dopa, mucuna pruriens, and forskolin (Coleus The dietary supplement of the present invention may comprise a second active ingredient selected from the group that may include DMAE, DMAE (Dimethylamino)ethanol (DMAE), DMAE bitartrate, and combinations thereof. The dietary supplement of the present invention may comprise a pharmaceutically acceptable carrier. The supplement is in a solid oral dosage form. The supplement is in a topical dosage form. The dietary supplement of the present invention may comprise a paraxanthine homolog or analog. The paraxanthine homolog or analog is selected from the group that may include caffeine, methylcaffeine, theobromine, theophylline, liberine, methylliberine, and combinations thereof. The paraxanthine homolog or analog is caffeine. The effective dose of caffeine is lower than the effective dose of caffeine in a composition that does not contain paraxanthine.

[0043]

[0071] One general aspect provides a method for enhancing physical performance or energy in a subject. The method further includes providing to the subject a composition that can include about 2 mg to about 800 mg of paraxanthine, whether natural or synthetic.

[0044]

[0072] Implementations may include one or more of the following features. Upon administration of the composition, a subject experiences an increase in at least one of mood, energy, focus, concentration, or sexual desire, or a reduction in at least one of anxiety, fatigue, perception of effort, or pain perception. When administered continuously to a subject, the composition does not induce dependence and / or withdrawal effects in the subject upon discontinuation of continued use. The amount of paraxanthine provided is about 50 mg to about 400 mg. The subject experiences at least about a 6 percent reduction in fatigue. The subject experiences at least about an 8 percent increase in energy. The composition may further comprise at least one ingredient selected from the group that may include caffeine, theobromine, naringin, hesperidin, 2-(dimethylamino)ethanol (DMAE), DMAE bitartrate, and huperzine A.

[0045]

[0073] One general aspect is a method for treating a condition in a subject in need of treatment. The present invention encompasses a method for treating a condition comprising administering a therapeutically effective amount of paraxanthine to a subject. Implementations may include one or more of the following features. In the method, the condition is selected from narcolepsy, epilepsy, attention deficit disorder, attention deficit hyperactivity disorder (ADHD), cognitive deficit disorder, paralysis, uncontrolled anger, migraine, substance abuse / dependence, eating disorders, depression, anxiety disorders, traumatic head injury (TBI), Parkinson's disease, Alzheimer's disease, and dementia. The paraxanthine is present in an amount of from about 2 mg to about 800 mg. The composition is administered in a therapeutically effective amount. The composition is administered in a prophylactically effective amount. The composition may include paraxanthine in an amount of from about 2 mg to about 800 mg. The composition may include paraxanthine in an amount of from about 50 mg to about 400 mg.

[0046]

[0074] One general aspect is a method for enhancing attention in a subject in need thereof. The present invention includes a method, wherein a composition that can include paraxanthine can be administered to the subject.

[0047]

[0075] One general aspect is to enhance working memory in a subject in need thereof. The method includes administering a paraxanthine-containing composition to the subject.

[0048]

[0076] One general aspect is a method of enhancing cognitive performance in a subject, comprising administering paraxane to a subject. The method includes administering to the subject a composition comprising an anti-inflammatory drug.

[0077] One general aspect is a method for aiding in weight loss and / or fat loss in a subject. The present invention encompasses a method that can be achieved by administering to the subject a composition comprising paraxanthine.

[0049]

[0078] Implementations can include one or more of the following features. The method comprises: The method results in weight loss in the subject by increasing metabolism, the weight loss being caused by a decrease in caloric intake in the subject.

[0050]

[0079] One general aspect is a dietary supplement that can include paraxanthine. The present invention encompasses a caffeine replacement composition for use. Implementations may include one or more of the following features: the composition, when administered to a subject, does not increase anxiety compared to a comparable dose of caffeine; the composition, when administered repeatedly, does not induce dependence in a subject and does not induce withdrawal effects in a subject upon cessation of use; the composition, when administered repeatedly, is less bitter compared to a comparable dose of caffeine; the composition, when administered repeatedly, is less toxic compared to a comparable dose of caffeine. [Example]

[0051]

[0080] The following examples are provided to illustrate the compounds, compositions, articles, and devices claimed herein. The present disclosure provides a complete disclosure and description of some examples of how to make and evaluate the methods and / or processes, and is intended to be purely exemplary of the invention and is not intended to limit the scope of what the inventors regard as their invention. However, those of skill in the art should, in light of the present disclosure, appreciate that many changes can be made in the specific embodiments which are disclosed and still obtain a like or similar result without departing from the spirit and scope of the invention.

[0052]

[0081] A double-blind, randomized, crossover, and repeated measures study was conducted in 13 volunteers. (10 men, 3 women, mean age 24±5 years, mean weight 72.91±19.30 kg, mean height 169.96±11.84 cm, mean BMI 24.80±3.71 kg / m 2 ) participated in this study. Participants restricted their intake of caffeine and other stimulants to reasonable amounts for 48 hours, fasted for 8 hours, and reported to the laboratory after completing four different cognitive tests assessing short-term attention and inhibitory control (Go-No Go test), sustained attention (Vigilance task test), working memory (Sternberg task test), and cognitive flexibility (Berg-Washington card sorting test). Immediately upon completion, participants ingested either a placebo or 200 mg of paraxanthine (WGI, TX, USA) with approximately 240 ml (8 oz) of water. At 1, 2, 3, 4, 5, and 6 hours after supplementation, participants repeated the cognitive tests. One week later, participants repeated the experiment, consuming the reversed dose.

[0053]

[0082] Data analysis involves general linear model multivariate and univariate solutions for repeated measures data. Analysis was performed using body weight as a covariate. Data are presented as mean ± standard deviation for each of the placebo group (PLA) and the paraxanthine group (PrX). The Greenhouse-Geisser univariate p-levels are listed for the interaction effects of time (T), body weight × time (W×T), and group × time (G×T). The results of pairwise comparisons are indicated by the following superscript letters : † = p < 0.5, difference from baseline value; * = 0.5 < p < 0.10, difference from baseline; a = p < 0.5, difference between groups; b = 0.5 < p < 0.10, difference between groups. An Eta2 value is judged to have a small effect size if it is between 0.01 and 0.5, medium if it is between 0.6 and 0.13, and large if it is > 0.14. Berg-Washington Card Sorting Task Test

[0083] The Berg-Washington Card Sorting Task Test is a test for basic cognitive flexibility or the ability to switch sets when new / old rules are changed. This test involves inference, learning, executive control, and attention switching abilities. This test is particularly sensitive to a decline in the ability to switch sets. The fewer the incorrect responses, the more likely it is that the subject was able to recognize and "switch" to the new rule with a higher ability. This test involves inference, learning, executive control, and attention switching abilities.

[0054]

[0084] Overall, the paraxanthine group had 5.3% more positive responses (placebo 10 The paraxanthine group had 23.7% fewer errors (23.6 vs. 18.0 for placebo). After adjusting for baseline differences, the paraxanthine group had 150% more correct responses (1.0 for placebo vs. 2.5 for paraxanthine) and 600% fewer errors (0.3 for placebo vs. -1.5 for paraxanthine). Individual results at different time points (0-6 hours) showed that paraxanthine treatment maintained its potentiation even at 6 hours (+1.9 for errors and -1.5 for correct responses for placebo vs. -0.6 for errors and +1.9 for correct responses for paraxanthine), indicating that the benefits of paraxanthine are long-lasting.

[0055]

[0085] Paraxanthine was shown to be effective in the Berg-Washington Card Sorting Test (B Paraxanthine significantly increased the number of correct answers and decreased the number of incorrect answers in the CST. Paraxanthine also increased cognitive flexibility, or the ability to switch sets when switching between new and old rules.

[0056]

[0086] Figures 1-4 show various graphs of the BCST test results. Figure 2 shows that paraxanthine significantly (p<0.5) increased the number of correct responses from baseline at 2 and 4 hours, with a trend between groups at 4 hours (p<0.1); Figure 2 shows that paraxanthine tended to reduce the number of errors compared to baseline at 6 hours (p<0.1); Figure 3 shows that paraxanthine appeared to maintain PEBL to a greater extent, but there were no significant differences in effect over time or between treatment groups; and Figure 4 shows that paraxanthine tended to reduce the difference between groups in the number of errors at 6 hours (p<0.1).

[0057] [Table 1]

[0058] Go-No Go Test

[0087] It is a test of sustained attention and response control (i.e., attention / inhibition). Response time The shorter the time, the greater the ability to pay attention and exercise inhibitory control.

[0059]

[0088] The mean positive response rate was 1.1% higher in the paraxanthine group than in the placebo group (P<0.05). Compared to baseline, the correct response rate decreased by 1.4% in the placebo group and 0.5% in the paraxanthine group. Mean response time remained unchanged in the paraxanthine group (-0.3%) but decreased by 3.5% in the placebo group. A shorter response time indicates a better ability to pay attention and exercise inhibitory control.

[0060]

[0089] When paraxanthine is administered, First round response time - average value for condition R Average response time for the second round under condition P Average response time for R1 and T2 trials The results showed that the drug prevented mental fatigue by maintaining attention and inhibitory control compared to placebo.

[0061]

[0090] Acute paraxanthine supplementation increased the response rate leading to a correct response in the go / no-go test. The results showed faster response times compared to PLA (indicating less mental fatigue). In addition, paraxanthine maintained the percentage of correct responses, while placebo showed a significant decrease in the percentage of correct responses. Paraxanthine increased the ability to sustain attention and control responses.

[0062]

[0091] Figures 5-10 show various graphs of the Go / No-Go test results. Figure 5 shows that the number of correct responses was significantly reduced in the placebo group (3 hours, p<0.5), Figure 6 shows that no significant differences were observed over time or between treatment groups, Figure 7 shows that in the first test run, paraxanthine maintained the mean response time better over time than PLA, Figure 8 shows that in the second test run, paraxanthine maintained the mean response time better over time than PLA, Figure 9 shows that in the second test run, paraxanthine maintained the mean response time better over time than PLA, but the difference was not significant, and Figure 10 shows that the average response time was significantly reduced in the placebo group, while paraxanthine maintained the mean response time (1st round + 2nd round) over time (i.e., indicating less fatigue).

[0063] [Table 2]

[0064] Vigilance

[0092] Psychomotor vigilance tasks test participants' speed in responding to visual stimuli. This is a sustained attention, reaction timed task. The shorter the reaction time, the better the performance, especially in a large number of tasks. The shorter the reaction time maintained throughout this test of questions, the better the ability to sustain attention.

[0065]

[0093] Paraxanthine had no effect on the average reaction time in vigilance task tests. had no effect.

[0094] Rapid paraxanthine supplementation is recommended for individuals who remain vigilant and alert. In a vigilance task test, which measures performance, the drug resulted in sustained attention (maintained reaction time, prevented mental fatigue), whereas the placebo showed a significant deterioration in reaction time (overall at 3 and 6 hours).

[0066]

[0095] 11-14 show various graphs of the vigilance test results. Figure 11 shows that paraxanthine maintained significantly faster reaction times compared to those in the PLA-treated group; Figure 12 shows that no significant differences were observed over time or between treatment groups; Figure 13 shows that reaction times increased over time in the PLA-treated group but were maintained in the paraxanthine-treated group (i.e., less fatigue); and Figure 14 shows that reaction times increased over time in the PLA-treated group (trending against baseline at 3 and 6 hours, p<0.1) but were maintained in the paraxanthine-treated group (i.e., less fatigue).

[0067] [Table 3]

[0068] Sternberg

[0096] This is a test of working memory, or the ability to utilize short-term memory. The faster the participant can access their working memory, the faster the participants can access their working memory. The Sternberg task test measures short-term / working memory (STM / W), which is involved in cognitive control processes. This is a widely used paradigm in research on M.

[0069]

[0097] Overall, paraxanthine significantly reduced mean response times on the Sternberg test. Paraxanthine significantly increased short-term / working memory in one measure of the Sternberg test (reaction time to the presence task of letter length 6, at 4 and 5 hours; see Figure 21). As list length increased, probe judgments (probe judgments) also improved. Judgment becomes less accurate and slower, indicating increased demands on short-term and working memory.

[0070]

[0098] Figures 15-20 show various graphs of the Sternberg test results. Figure 15 shows that the paraxanthine group showed a trend toward improved reaction times at 3, 4, and 5 hours, whereas the placebo group showed improvements at 4 and 5 hours (p<0.1); Figure 16 shows that there were no significant differences over time or between treatment groups; Figure 17 shows that there were no significant differences over time or between treatment groups, but the paraxanthine group showed greater improvements from 3 to 5 hours; Figure 18 shows that reaction times were significantly improved in the paraxanthine and placebo groups; Figure 19 shows that there were no significant differences over time or between treatment groups, but the paraxanthine group showed greater improvements from 3 to 6 hours; and Figure 20 shows that the paraxanthine group showed improvements in present-task reaction times at later time points (4 and 5 hours), whereas the placebo group showed no improvement.

[0071] [Table 4]

[0072] toxicity

[0099] Relative toxicity between paraxanthine, caffeine, and other caffeine metabolites. To assess the potential of 50 The LD of paraxanthine was determined.50 The average daily intake of 1,601 mg of vitamin D per kg of body weight is 1,601 mg. The LD50 for paraxanthine is 192 mg / kg, indicating that caffeine has a significantly higher level of toxicity than paraxanthine alone. Furthermore, the LD50s for the caffeine metabolites theobromine and theophylline are 1,265 mg / kg and 225 mg / kg, respectively. Taken together, these results indicate that paraxanthine has a substantially better safety profile than caffeine or the other major caffeine metabolites. taste

[0100] A series of blind tasting studies were conducted to assess the palatability of paraxanthine in comparison with methylliberine, liberine, and theacrine. Prior to the blind tasting studies, subjects were trained to distinguish between flavors and to use the scale shown in Figure 21. Solutions A and C shown in Figure 22 were given to subjects, and they were informed of their bitterness scores (solution A = 3, solution C = 10). Next, subjects were given solution B and asked to compare the scores.

[0073]

[0101] In the training session, subjects memorized the scale by administering Solutions A and C for memory purposes and then scoring Solution B. Subjects were then given solutions with varying caffeine concentrations to further memorize the scale.

[0074]

[0102] After completing the four training sessions, subjects were given a blind tasting test in which they scored the bitterness of four product solutions, namely Solution L (Liberine), Solution P (Paraxanthine), Solution T (Theacrine), and Solution M (Methylliberine), on a scale established with the caffeine solutions. Each solution was administered at a concentration of 163 mg / 473 ml, as shown in Figure 22.

[0075]

[0103] The subjects were blinded to the contents of solutions L, P, T, and M and randomly administered them, and asked to score each solution on a scale established by the caffeine solutions. Figures 23 and 24 show the scoring results, which show that the tasters rated paraxanthine as being substantially less bitter than the solutions of methylliberine, liberine, and theacrine at the same concentration. Furthermore, the tasters' comments are shown in Figure 25. Paraxanthine Pre-Workout

[0104] Healthy subjects were given paraxanthine and asked to report their impressions. Subjects reported the following:

[0076]

[0105] A 46-year-old male exercises 4-5 times per week and consumes coffee or an energy drink prior to exercise, and sometimes coffee, an energy drink, or a diet soda in the afternoon. The subject reported, "It's my preference...it's so much better than my caffeine go-to. It feels different. The best way to describe it is that it makes me feel more happy, good, and gives me more energy and focus, but it's not 'strong,' 'dizzy,' or 'anxious,' it just feels like I've got a pure, clean energy boost. It really does feel that way."

[0077]

[0106] A 38-year-old male who prefers nootropics such as piracetam, alpha-GPC, and Noopept, and has extensive experience using brain boosters, reported, "I was amazed. It was amazing when I tried it alone. I really liked it, but when I used it with the other nootropics I have, it felt like there was a synergistic effect, which was even better. I'll buy it. Please let me know where I can buy it."

[0078]

[0107] A 44-year-old female nurse who plays beach volleyball twice a week reported, "I really liked it. It felt a little different from my usual caffeine source. "I had lean energy, but I didn't feel stressed or stimulated. Plus, I slept soundly. With caffeine, it definitely disrupts the quality of my sleep and sometimes wakes me up several times during the night."

[0079]

[0108] A 19-year-old female college student and active volleyball player reported, "It clicked. I love it. I want it. The reason is simple: it works. I don't like to take a lot of caffeine, it just makes me feel awful. This is great."

[0080]

[0109] Although the present disclosure has been described with reference to preferred embodiments, those skilled in the art will recognize that changes may be made in form and detail without departing from the spirit and scope of the devices, systems and methods of the present disclosure.

[0081]

[0110] Although the present disclosure has been described with reference to preferred embodiments, those skilled in the art will recognize that changes may be made in form and detail without departing from the spirit and scope of the devices, systems and methods of the present disclosure.

Claims

1. A dietary supplement comprising a first active ingredient comprising from about 2 mg to about 800 mg of paraxanthine, whether natural or synthetic.

2. Gallic acid, (+)-catechin (C), (-)-epicatechin (EC), (+)-gallocatechin (GC), (-)-epigallocatechin (EGC), (-)-catechin gallate (CG), (-)-gallocatechin gallate (GCG), (-)-epicatechin gallate (ECG) and (-)-epigallocatechin gallate (EGCG), glycerides, propylene glycol, lauroyl macrogol, lauroyl macrogol derivatives, co-crystallized product of BioPerine, piperine, black pepper, bergamottin, dihydroxybergamottin (CY P3A4), flavonoids (naringin, hesperidin, nobiletin, tangeretin, quercetin), pterostilbene, fisetin, phytosome, salicin, fish oil (ω-3 fatty acids and specific small lipid-resolving epoxide derivatives, oxylipins, tart cherry, krill oil, astaxanthin, proteolytic enzymes, glucosamine sulfate, chondroitin sulfate, MSM (methylsulfonylmethane), SAMe (S-adenosylmethionine), ASU (avocado-soybean unsaponifiable fraction), cetyl myristoleate, Dolichos falcate, triterpenoids, acacia catechu, Andrographis paniculata, Scutalleria baicalensis, agmatine sulfate, nettle, sea buckthorn, curcumin, Cissus quadrilangularis, Boswellia serrata, Wasabi japonica (wasabi extract used in tea tree oil), emu oil, arnica, Mangifera indica L. (Anacardiaceae), Lagenaria breviflora, Zingiber officinale (ginger and gingerol / shogaol), hoodia gordonii, caffeine, yohimbine, methylsynephrine, synephrine, theobromine, flavenoids, tocopherols, theophylline, alpha-yohimbine, conjugated linoleic acid (CLA), octopamine, evodiamine, passion flower, red pepper, cayenne, raspberry ketone, guggul, green tea, guarana, kola nut, beta-phenethylamine, Acacia rigidula, forskolin (Coleusforskohlli), theophylline, synephrine, yohimbine, Rhodiola rosea, ashwagandha, ginseng, ginkgo biloba, Eleuthero, Astragalus senticosus, licorice, green tea, reishi mushroom, dehydroepiandrosterone (DHEA), pregnenolone, tyrosine, N-acetyltyrosine, glucuronolactone, taurine, acetyl-L-carnitine, 5-hydroxytryptophan, tryptophan, phenethylamine, Sceletium tortuosum (and mesembrine alkaloids), Dendrobium species, Acacia rigidula, PQQ (pyrroloquinoline quinone), ubiquinone (01), nicotinamide riboside, picamilon, huperzine A (from shiitake mushroom or Huperzia serrata, L-dopa, Mucuna pruriens, and a second active ingredient selected from the group consisting of forskolin (Coleus forskohlii), 2-(dimethylamino)ethanol (DMAE), DMAE bitartrate, and combinations thereof.

3. 10. The dietary supplement of claim 1, further comprising a pharmaceutically acceptable carrier.

4. 10. The dietary supplement of claim 1 in solid oral dosage form.

5. 10. The dietary supplement of claim 1 in a topical dosage form.

6. 10. The dietary supplement of claim 1, further comprising a paraxanthine congener or analogue.

7. 7. The dietary supplement of claim 6, wherein the paraxanthine congener or analog is selected from the group consisting of caffeine, methylcaffeine, theobromine, theophylline, liberine, methylliberine, and combinations thereof.

8. 8. The dietary supplement of claim 7, wherein the paraxanthine congener or analog is caffeine.

9. 9. The dietary supplement of claim 8, wherein the effective dose of caffeine is lower than the effective dose of caffeine in a composition that does not contain paraxanthine.

10. A method of enhancing physical performance or energy in a subject, comprising providing to said subject a composition comprising from about 2 mg to about 800 mg of paraxanthine, whether natural or synthetic.

11. 11. The method of claim 10, wherein upon administration of the composition, the subject experiences an increase in at least one of mood, energy, focus, concentration, or sexual desire, or a reduction in at least one of anxiety, fatigue, perception of effort, or perception of pain.

12. 12. The method of claim 11, wherein the composition, when administered continuously to the subject, does not produce dependence in the subject and / or withdrawal effects in the subject when continued use is discontinued.

13. 11. The method of claim 10, wherein the amount of paraxanthine provided is from about 50 mg to about 400 mg.

14. 11. The method of claim 10, wherein the subject experiences at least about a 6 percent reduction in fatigue.

15. 11. The method of claim 10, wherein the subject experiences at least about an 8 percent increase in energy.

16. 11. The method of claim 10, wherein the composition further comprises at least one ingredient selected from the group consisting of caffeine, theobromine, naringin, hesperidin, 2-(dimethylamino)ethanol (DMAE), DMAE bitartrate, and huperzine A.

17. 1. A method of treating a condition in a subject in need thereof, comprising administering to said subject a composition comprising paraxanthine and a pharmaceutically acceptable carrier thereof.

18. 18. The method of claim 17, wherein the condition is selected from narcolepsy, epilepsy, attention deficit disorder, attention deficit hyperactivity disorder (ADHD), cognitive deficit disorder, paralysis, uncontrolled anger, migraine, substance abuse and addiction, eating disorders, depression, anxiety disorders, traumatic head injury (TBI), Parkinson's disease, Alzheimer's disease, and dementia.

19. 19. The method of claim 18, wherein the paraxanthine is present from about 2 mg to about 800 mg.

20. 20. The method of claim 18, wherein the composition is administered in a therapeutically effective amount.

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