WO2006057893A2 - Composition, delivery system and method for promoting healthy sexual function - Google Patents
Composition, delivery system and method for promoting healthy sexual function Download PDFInfo
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- WO2006057893A2 WO2006057893A2 PCT/US2005/041765 US2005041765W WO2006057893A2 WO 2006057893 A2 WO2006057893 A2 WO 2006057893A2 US 2005041765 W US2005041765 W US 2005041765W WO 2006057893 A2 WO2006057893 A2 WO 2006057893A2
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G1/00—Cocoa; Cocoa products, e.g. chocolate; Substitutes therefor
- A23G1/30—Cocoa products, e.g. chocolate; Substitutes therefor
- A23G1/32—Cocoa products, e.g. chocolate; Substitutes therefor characterised by the composition containing organic or inorganic compounds
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
- A23L27/60—Salad dressings; Mayonnaise; Ketchup
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/17—Amino acids, peptides or proteins
- A23L33/175—Amino acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
- A61K36/489—Sophora, e.g. necklacepod or mamani
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/85—Verbenaceae (Verbena family)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Definitions
- This invention relates in general to compositions for supporting and promoting healthy sexual function, preventing sexual dysfunction, and treatment of sexual dysfunction, and also to a more effective delivery system for such compositions.
- Erectile dysfunction is a common disorder affecting about 30 million men in the U.S. alone. ED has been defined as the inability to achieve or maintain an erection sufficient for intercourse. The predominant etiology for this condition is vascular insufficiency. Studies have shown that during sexual arousal, nitric oxide molecules are released into the surrounding tissue from nerve endings and endothelial cells in the genitals. These nitric oxide molecules then cause the enzyme guanylate cyclase to produce cyclic guanosine monophosphate (cGMP) which lowers the level of intracellular calcium in the surrounding tissue and allows for the relaxation of vascular smooth muscle cells. In the penis, relaxation of the corpus cavernosa!
- cGMP cyclic guanosine monophosphate
- vascular smooth muscle cells permits increased blood flow into the cavernosal spaces. This expands the sinusoidal tissues in the corpora cavernosa. This expansion then restricts venous outflow. The combination of increased arterial inflow and diminished venous outflow leads to enhanced intra- cavernosal pressure thereby producing penile rigidity.
- cGMP cyclic nucleotide phosphodiesterases
- sildenafil citrate Viagra: Pfizer Inc, New York, NY
- PDE5 inhibitors designed to elevate cGMP in the corpus cavemosum and thus produce an improvement in ED.
- These drugs include vardenafii, tadalafil, sildenafil and other agents which inhibit cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
- Apomorphine hydrochloride and its variations, conventionally all referred to in the art as apomorphine, which is planned to be sold by Abbot Laboratories under the trademarks Uprima or Ixense, is a pharmaceutical that enhances sexual function by affecting the brain.
- Apomorphine is a dopaminergic agonist that, once absorbed and transported into the brain, initiates a chain of reactions that result in increased blood flow to the male genital organs and an erection.
- the invention solves the above and other problems by recognizing that sexual health and sexual dysfunction are complex conditions, and that good, consistent sexual response, particularly in females, not only requires appropriate physiological conditions, but also requires appropriate psychological environments. For example, a single inappropriate word or gesture can ruin a sexual experience for many individuals, particularly women.
- the invention overcomes the above and other problems by providing a method and apparatus for delivery of a sexual health or sexual dysfunction composition that is more appropriate to the sexual experience.
- the invention provides a sexual health composition delivery vehicle and method that does not interfere with the psychological aspects of sexual activity, and preferably enhances the psychological aspects of sexual activity.
- the delivery vehicle comprises an edible film, a breath-care strip, mint or lozenge, or a food, beverage, spice, condiment or salad dressing or other functional food.
- nutraceuticals are compositions that promote health in humans and other animals, which contain ingredients that occur naturally and/or ingredients that are extracted from naturally-occurring substances. Since they are naturally occurring compounds from plants and animals that have evolved together with human beings, nutraceuticals are more likely to have fewer and less serious adverse side effects than synthetic pharmaceuticals to which humans have never been exposed.
- the invention also solves the above problem by providing a sexual health composition that nurtures and/or sustains multiple metabolic pathways that contribute to sexual health, and for modulating (i.e., altering or normalizing) metabolic pathways that inhibit sexual health and lead to sexual dysfunction.
- metabolic pathways that affect sexual function: the metabolic pathways associated with the production of nitric oxide by the nerve endings and endothelial cells in the genitals; the pathways associated with the break down of nitric oxide before it can stimulate guanylate cyclase; the metabolic pathways associated with production of cyclic guanosine monophosphate (cGMP) by the enzyme guanylate cyclase; the pathways that cause breakdown of cGMP, and the pathways by which a dopaminergic agonist can enhance sexual health via the brain.
- the compositions according to the invention address one or more of these metabolic pathways, and preferably a plurality of these pathways.
- the nutraceutical formulation is comprised of an agent, or a combination of agents, capable of enhancing cGMP in the genitalia of one in need of the therapy.
- the formulation is preferably admixed with a pharmaceutically acceptable carrier, diluent, or excipient.
- the present invention relates to a method of treating an individual with sexual dysfunction; the method comprising delivering a nutraceutical formulation that is capable of enhancing cGMP in the genitalia, and the formulation is preferably mixed with a pharmaceutically acceptable carrier, diluent or excipient.
- the nutraceutical is combined with pharmaceutical sexual function or performance ingredients to improve the efficacy of the pharmaceutical.
- the invention provides a composition for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the composition comprising an ingredient including a portion of or a constituent of the plant Sophora flavescens or an extract of the plant Sophora flavescens in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- ingredient comprises sophoflavescenol.
- the ingredient comprises a portion of the root of the plant.
- the ingredient comprises an extract of the plant.
- the ingredient comprises an extract of the root of the plant.
- the composition further comprises Vitex agnus-castus extract in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition further comprises an ingredient that enhances the amount, or activity, of guanylate cyclase, an ingredient that enhances the production of nitric oxide, or an ingredient that inhibits the breakdown of nitric oxide; the ingredients included in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the ingredient that enhances the amount, or activity, of guanylate cyclase comprises biotin
- the ingredient that enhances the production of nitric oxide comprises a compound selected from the group consisting of L-arginine and policosanol
- the ingredient that inhibits the breakdown of nitric oxide comprises an anti-oxidant selected from the group consisting of idebenone, co ⁇ enzyme Q10, vitamin E, ALA (Alpha Lipoic Acid), vitamin C, camosine, tocotrienols, flavonoids, ALC, vinpocetine, selenium, lycopene, creatine, arginine, taurine, cysteine, NADH, resveratrol, ginkgo biloba, oligomeric proanthocyanidins, and phenolic antioxidants and folic acid, folate, folinic acid and tetrahydrofolate.
- the composition is contained in a vehicle selected from the group consisting of: nutritional supplements, edible films
- the invention provides a method for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the method comprising orally, sublingually, transdermal ⁇ , subcutaneously or parenterally administering to the human, for an effective period, a composition comprising an ingredient comprising a portion of the plant Sophora flavescens or an extract of the plant Sophora flavescens in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the administering comprises delivering the composition in a vehicle selected from the group consisting of: nutritional supplements, edible films, breath-care strips, mints or lozenges, mouth sprays, dietary supplements, foods, and beverages.
- the invention provides a composition for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the composition comprising Vitex agnus-castus extract in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition further comprises an ingredient that enhances the amount, or activity, of guanylate cyclase, an ingredient that enhances the production of nitric oxide, or an ingredient that inhibits the breakdown of nitric oxide; the ingredients included in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition is contained in a vehicle selected from the group consisting of: edible films, breath-care strips or lozenges, foods, and beverages.
- the invention provides a composition for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the composition comprising: a cGMP-specific PDE5 inhibitor ingredient; and Vitex agnus-castus extract ingredient; the ingredients included in the composition in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the cGMP-specific PDE5 inhibitor ingredient comprises an ingredient selected from the group consisting of sophoflavescenol, vardenafil, tadalafil, and sildenafil.
- the composition further comprises an ingredient that enhances the amount, or activity, of guanylate cyclase, an ingredient that enhances the production of nitric oxide, or an ingredient that inhibits the breakdown of nitric oxide; the ingredients included in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition is contained in a vehicle selected from the group consisting of: nutritional supplements, edible films, breath-care strips or lozenges, foods, and beverages.
- the invention provides a method for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the method comprising orally or parenterally administering to the human, for an effective period, a composition comprising: a cGMP-specific PDE5 inhibitor ingredient; and a Vitex agnus-castus extract ingredient; the method including providing the ingredients in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the cGMP-specific PDE5 inhibitor ingredient comprises an ingredient selected from the group consisting of sophoflavescenol, vardenafil, tadalafil, and sildenafil.
- the administering comprises delivering the composition in a vehicle selected from the group consisting of: edible films, breath-care strips or lozenges, foods, and beverages.
- the invention also provides a product for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the product comprising: a delivery vehicle selected from the group consisting of edible films, breath-care strips, mints, and breath-care lozenges; and a sexual health or sexual dysfunction prevention composition carried by the vehicle in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the sexual health or sexual dysfunction prevention composition can comprise any of the above compositions.
- the sexual health or sexual dysfunction prevention composition comprises an ingredient selected from the group consisting of: a portion of the plant Sophora flavescens, an extract of the plant Sophora flavescens such as sophoflavescenol, and a Vitex agnus-castus extract, the ingredient provided in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition further comprises an ingredient that enhances the amount, or activity, of guanylate cyclase, an ingredient that enhances the production of nitric oxide, or an ingredient that inhibits the breakdown of nitric oxide; the ingredients included in effective amounts for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the ingredient that enhances the amount, or activity, of guanylate cyclase comprises biotin
- the ingredient that enhances the production of nitric oxide comprises a compound selected from the group consisting of L-arginine and policosanol
- the ingredient that inhibits the breakdown of nitric oxide comprises an anti-oxidant selected from the group consisting of idebenone, co ⁇ enzyme Q10, vitamin E, ALA, vitamin C, camosine, tocotrienols, flavonoids, ALC, vinpocetine, selenium, lycopene, creatine, arginine, taurine, cysteine, NADH, resveratrol, ginkgo biloba, oligomeric proanthocyanidins, and phenolic antioxidants and folic acid, folate, folinic acid and tetrahydrofolate.
- the sexual health or sexual dysfunction prevention composition comprises a cGMP-specific PDE5 inhibitor.
- the cGMP-specific PDE5 inhibitor is selected from the group consisting of vardenafil, tadalafil, and sildenafil.
- the sexual health or sexual dysfunction prevention composition comprises a dopaminergic agonist, Preferably the dopaminergic agonist is apomorphine.
- the edible film comprises pullulan.
- the invention also provides a food or beverage product for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the product comprising: a food or beverage base; and a sexual health or sexual dysfunction composition in an effective amount for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction.
- the composition selected from the group consisting of: a portion of the plant Sophora flavescens, an extract of the plant Sophora flavescens, sophoflavescenol, vardenafil, tadalafil, sildenafil, apomorphine , and Vitex agnus-castus extract.
- the base is a beverage base and the beverage is selected from the group consisting of: soft drinks, tea, coffee, milk, fruit juices, and sports drinks.
- the base is a beverage base and the beverage comprises an alcoholic beverage.
- the base is a food base and the food is selected from the group consisting of: fruit, chocolate, candy, trail mix, nutritional bars, ice cream, yogurt, cheese, steak sauce, salsa and salad dressing.
- the invention further provides a method of administering a composition for supporting and promoting healthy sexual function, for preventing human sexual dysfunction, for preventing human sexual dysfunction, or for treatment of human sexual dysfunction, the method comprising: incorporating the composition in an edible film, breath-care strip, mint, or breath-care lozenge; and placing the edible film, breath-care strip, mint, or breath-care lozenge in the mouth of a human being.
- the invention not only provides a nutraceutical-based sexual health composition and method of delivering it that has fewer adverse reactions than pharmaceutical-based sexual health compounds, but one that is more broadly effective, more potent than prior art pharmaceutical sexual health compounds, and more psychologically appropriate.
- FIG. 1 is a block diagram illustrating the food or beverage product according to the invention and the method of making it.
- the invention relates to certain compositions that promote healthy sexual function and/or sexual well being in humans and other animals and which contain ingredients that occur naturally and/or ingredients that are extracted from naturally occurring substances.
- these compositions may be label: functional foods, dietary supplements, nutritional supplements, herbal supplements, botanical drugs, medical foods, and sometimes even drugs. In the future, other terms may be applied to these compounds, if, for example, Congress creates new categories of FDA-regulated products.
- the invention is intended to cover the compositions disclosed herein, no matter what they are called. Nutraceuticals do not include pharmaceuticals, which are defined herein to be man-made, synthetic medical compounds that do not occur in nature.
- the present invention provides a method and composition for maintaining sexual health, for preventing sexual dysfunction, and for treatment of sexual dysfunction in humans or other animals, such as horses.
- the composition is preferably a nutraceutical or a combination of nutraceuticals, although in one aspect it could includes one or more pharmaceuticals. In the most preferred embodiments, it includes a combination of ingredients that address a plurality of metabolic pathways, and thus is more broadly effective than prior art sexual function compositions.
- the cellular concentration of cGMP is determined by the balance between its synthesis by guanylyl cyclase, and its breakdown to 5'- GMP by cyclic nucleotide phosphodiesterases (PDE5).
- the synthesis is stimulated by nitric oxide molecules that are released into the surrounding tissue from nerve endings and endothelial cells in the genitals.
- the enhanced production of cGMP may be achieved by enhancement of the amount, or activity, of guanylate cyclase, the enhancement of the production of nitric oxide, the inhibition of the breakdown of nitric oxide, and the inhibition of the breakdown of cGMP.
- the compositions according to the invention address one or more of these metabolic pathways, and preferably a plurality of these pathways. They also address the impact of brain pathways, such as the dopaminergic agonist pathway, upon sexual function.
- the inhibition of the breakdown of cGMP is achieved either by sophoflavescenol or other extract from the plant Sophora flavescens, or other selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
- the PDE5 inhibitor is an extract from Sophora flavescens, more preferably an extract from the root of Sophora flavescens, and most preferably, sophoflavescenol.
- Sophoflavescenol is a selective cGMP PDE5 inhibitor that is not structurally related to the pharmaceutical cGMP PDE5 inhibitors that have been synthesized by modification of the sildenafil structure.
- sophoflavescenol may be considered as a unique agent with a different, more desirable pharmacological PDE5 profile.
- sophoflavescenol a C-8 prenylated flavonol
- the methanol extract of S. flavescens is suspended in water and then partitioned consecutively with dichloromethane, ethyl acetate, and butanol.
- sophoflavescenol is the most potent.
- the IC50 ratio PDE4/PDE5 is 196.2 showing high selectivity in the inhibition of these PDE isoforms.
- sophoflavescenol The structure of sophoflavescenol is shown below:
- sophoflavescenol may be used directly and alone, or may serve as the lead ingredient for the formulation of compositions effective for sexual function and performance. Since it is a naturally-occurring compound from the root of a plant that has grown wild for centuries and has been cultivated for generations, it is likely to have more desirable pharmacological profiles than pharmaceuticals to which humans have never been exposed. As will be discussed in detail below, it is preferably combined with other synergistically acting agents for enhanced function.
- Sophoflavescenol elevates cGMP in genital tissue by inhibiting cGMP breakdown. It may be used alone, or in combination with other biologically active compounds that directly, or indirectly, increase the production of cGMP and/or inhibit its breakdown, and thus act synergistically to enhance sexual function. Without being exhaustive, the enhanced production of cGMP may be achieved by augmentation of the amount, or activity, of guanylate cyclase, the augmentation of the production of nitric oxide, the inhibition of the breakdown of nitric oxide or the providing of a dopaminergic agonist.
- nitric oxide may be achieved by increased supply of metabolic substrate of the enzyme Nitric Oxide Synthase (NOS), and by provision of agents that augment the activity or amount of NOS.
- NOS Nitric Oxide Synthase
- Nitric oxide readily combines with the superoxide radical to form peroxynitrate. This and other related reactions consume nitric oxide.
- Inactivation of nitric oxide may be diminished by the use of anti-oxidants, such as idebenone, co-enzyme Q10, vitamin E, ALA, vitamin C, carnosine, tocotrienols, flavonoids, ALC, vinpocetine, selenium, lycopene, creatine, certain amino acids (e.g., taurine and cysteine), resveratrol, ginkgo biioba, oligomeric proanthocyanidins, and phenolic antioxidants, and related compounds such as folic acid, folate, folinic acid and methyltetrahydrofolate.
- anti-oxidants such as idebenone, co-enzyme Q10, vitamin E, ALA, vitamin C, carnosine, tocotrienols, flavonoids, ALC, vinpocetine, selenium, lycopene, creatine, certain amino acids (e.g., taurine and cysteine), resveratrol, g
- vascular health and vascular function are key mediators in the control of blood flow to the genitalia.
- the vascular abnormality that is most commonly associated with sexual dysfunction relates to a diminished ability to accumulate cGMP via the nitric oxide synthesis pathway. It involves the endothelium, the cells that form the inner lining of all blood vessels. This is referred to as endothelial dysfunction.
- nitric oxide may not be produced, or it may be broken down into compounds that actually damage blood vessels further contributing to vascular disease and endothelial dysfunction.
- Superoxide overproduction is a prominent mediator of endothelial dysfunction acting in a number of ways to inhibit effective endothelial nitric oxide activity.
- the ability of superoxide to quench nitric oxide is well known, but oxidants derived from superoxide also appear to inhibit dimethylarginine dimethylaminohydrolase (DDAH) and to oxidize tetrahydrobiopterin (THBP).
- DDAH dimethylarginine dimethylaminohydrolase
- THBP oxidize tetrahydrobiopterin
- DDAH deficiency boosts the level of methylated arginines that act as potent competitive inhibitors of NOS, whereas the latter effect decreases the ability of the enzyme to generate nitric oxide, while converting it to a form that readily generates further superoxide.
- the adverse impact of DDAH deficiency on nitric oxide production may be offset with supplemental arginine.
- a practical way to optimize NOS activity in the context of THBP-depleted endothelial cells is the administration of high dose folic acid independent of modulation of homocysteine levels.
- the administration of either arginine or folate alone, or preferably simultaneously, is effective in preventing or ameliorating vascular pathology that contributes to sexual dysfunction.
- Excessive endothelial superoxide production can be addressed by controlling risk factors that boost activation of endothelial NAD(P)H oxidase such as insulin resistance, diabetes, hypercholesterolemia, and hypertension. Supplemental administration of lipoic acid and other anti-oxidants mentioned above, anti-reductants, and policosanol are helpful in this regard.
- Vitex agnus-castus The brain's function as a sexual enhancer is preferably addressed by Vitex agnus-castus.
- the inventors have found that Vitex agnus-castus appears to be a dopaminergic agonist.
- the function of Vitex agnus-castus is not yet fully understood, and may be more complex than just as a dopaminergic agonist.
- the invention contemplates that, whatever sexual health and performance enhancement function or functions associated with Vitex agnus-castus are eventually determined to be, these sexual health and performance enhancement functions are considered to be part of this invention.
- compositions effective in supporting and promoting healthy sexual function and in addressing sexual dysfunction have been formulated.
- Table 1 lists the preferred ingredients of the compositions, the dosage range, and the preferred dose of each ingredient.
- formulations will preferably include an appropriate amount of sophoflavescenol or other Sophora flavescens extract
- Vitex agnus-castus extract Most formulations will include Vitex agnus-castus extract; 3) Depending upon the clinical circumstances and the insight of the formulator, appropriate amounts of the remaining agents are chosen. None of them, one of them, a combination of some of them, or all may be used.
- Appropriate delivery constituents should be chosen; 5) Mode of delivery and delivery regimen should be specified - this may include oral, sublingual, transdermal, subcutaneous application, or intra-venous administration and may vary from an as-needed basis to taking a preferably lower dosage several times a day.
- the delivery vehicles described in section 3 below should be considered. Exemplary formulations are given below to illustrate the application of the principals of the invention to a variety of situations.
- composition A Sophoflavescenol 100 mg; given orally only when needed.
- Composition B Sophoflavescenol 75 mg combined with Vitex agnus-castus extract 30 mg; given orally as needed.
- composition C Sophoflavescenol 100 mg
- composition D Sophoflavescenol 150 mg
- Composition E Sophoflavescenol 200 mg Lipoic Acid 300 mg L-Arginine 500 mg Folic Acid 800 ⁇ g
- composition G To the above may also be added:
- Composition H Sophoflavescenol 250 mg
- composition I Lipoic Acid 125 mg
- composition J Lipoic Acid 125 mg
- each of the above formulations and methods of administration should be considered only to be the starting point for addressing the indicated condition.
- the formulation should be modified by increasing dosages and/or adding additional ingredients.
- a good rule to follow in altering the formulations above that do not include Vitex agnus-castus extract is that the alternative of adding Vitex agnus-castus extract to the formulation should be considered before increasing dosages.
- the formulation should be modified by dropping ingredients and/or dosages.
- any of the anti-oxidants given above may be substituted for the vitamins C and E or used to augment the vitamins C and E. If formulations given on a daily basis are effective but have side effects, then they may be tried on an as-needed basis.
- Sophoflavescenol A key ingredient in the above and below compositions is sophoflavescenol.
- Sophoflavescenoi is extracted using a methanol extraction from the root (radix) of the plant Sophora flavescens.
- active ingredients in the plant that are not as potent or effective, nor as specific at inhibiting only one specific isoform of the enzyme (cGMP type Phosphodiesterase 5) that produces the desired physiologic response.
- the invention contemplates that any of these ingredients may be substituted or used in combination with sophoflavescenol.
- the root of the plant may be used.
- More preferred forms would include extracts of the plant, and most preferably the following specific ingredients: Kushenol H, Kushenol K, Kuraridine, Kurarinol.
- the lower limit for the root, any extract of the plant, and the forgoing specific ingredients is the same as those indicated for sophoflavescenol, while the upper limit may be increased up to 1000 fold over the dose of sophoflavescenol.
- Vitex agnus-castus extract is a key ingredient of both the nutraceutical formulations and the formulations that include pharmaceutical drugs. It was initially only one of hundreds of possible ingredients considered by the inventors for inclusion in a healthy sexual function formulation. However, initial testing has suggested that this ingredient broadens and increases the effectiveness of almost any formulation. The reason for this is not yet fully understood, but it is believed to be connected to the fact that it addresses metabolic pathways other than the PDE5 pathway.
- compositions each address different metabolic pathways associated with sexual health. If the pathway that needs to be modulated is known, then this should be used as a guide to determine which composition is selected, according to the general guidelines given in the Overview above. If the pathway that needs to be modulated is not known, then it is recommended that the compositions A, B, C, D, E 1 , 1, and J be tried in order before increased dosages be tried.
- compositions described above may also be combined with an erectile dysfunction drug or agent, such as a monohydrochloride salt of vardenafil (mVardenafil HCI), sildenafil citrate, tadalafil, or other selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
- an erectile dysfunction drug or agent such as a monohydrochloride salt of vardenafil (mVardenafil HCI), sildenafil citrate, tadalafil, or other selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
- cGMP cyclic guanosine monophosphate
- MVardenafil HCI is designated chemically as piperazine, 1-[[3-(1 ,4-dihydro-5- methyl-4-oxo-7-propylimidazo [5,1-f] [1 ,2,4] triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4- ethyl-, monohydrochloride and is sold by Bayer Pharmaceuticals under the trademark Levitra.
- Sildenafil citrate is designated chemically as 1-[[3-(6,7-dihydro- 1 methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)4ethoxyphenyl]sulfonyl]- 4-methyl piperazine citrate and is sold by Pfizer, Inc. under the trademark Viagra.
- Tadalafil is sold under the trademark Cialis by Lilly ICOS LLC, and is designated chemically as pyrazino[1 ⁇ ,2 ⁇ :1 ,6]pyrido[3,4-b]indole-1 ,4-dione, 6-(1 ,3-benzodioxol- 5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R,12aR)-. Many variations of such drugs also have been found to be similarly effective.
- vardenafil all variations of mVardenafil HCI that are effective to inhibit PDE5 as vardenafil
- sildenafil citrate as sildenafil
- tadalafil all effective variations of the tadalafil, as tadalafil.
- vardenafil, sildenafil, tadalafil, or any erectile dysfunction drug that addresses the PDE5 pathway may be substituted for sophoflavescenol in any of the above compositions.
- the initial dosages for the ED drug should be the smaller dosages directed by the manufacturer.
- Apomorphine hydrochloride and its variations, conventionally all referred to in the art as apomorphine, which is planned to be sold by Abbot Laboratories under the trademarks Uprima or Ixense, is a pharmaceutical that enhances sexual function by affecting the central nervous system.
- Apomorphine is a dopamine receptor agonist that acts on the central nervous system. Once absorbed and transported into the brain, it initiates a chain of reactions that result in increased blood flow to the male genital organs and an erection. Apomorphine can also be added to any of the formulations given above.
- compositions presented above are preferably in the form of an orally administered composition, e.g., powder, chewable wafer, tablet, regular or compressed capsule, etc., wherein the amounts listed may be divided into two or more portions which in combination constitute a single "unit dose" of the composition. Each dose is preferably taken with 8 ounces of water.
- the method of this invention involves the steps of administering to a human on a daily basis for a therapeutically effective period of time an effective amount of the composition of this invention.
- the composition is administered orally, sublingually, transdermal! ⁇ subcutaneously or parenterally, preferably orally and ingested.
- the term "effective amount” means an amount sufficient to modulate metabolic pathways in the body so as to enhance sexual health.
- the active-ingredient composition (not including inactive ingredients) of this invention is administered in a daily dosage of at least about 1 gram, more preferably from about 1 gram to about 200 grams, most preferably from about 4 grams to about 20 grams.
- the inactive ingredients of the composition can be present in any conventional amount used in orally or parenterally administered compositions.
- the term "effective period of time” with respect to the administration of the composition in the method of this invention means that period of time sufficient to modulate healthy sexual function and performance in the human. The "effective period" may be a single time prior to sexual activity.
- the nutraceutical compositions of this invention can administered on a daily basis for a period of at least three weeks, more preferably at least six weeks.
- oral administration is accomplished by ingesting the composition, preferably with water.
- the orally administered composition of this invention can be in any conventional form including, e.g., capsules (regular or compressed), tablets, soft gels, chewable wafers, elixirs, liquid extracts, powders, granules, suspensions in water or non-aqueous media, sachets, etc. Powder, tablet, and chewable wafer forms are most preferred.
- the composition can also be administered parenterally.
- the alternative delivery vehicles discussed below should also be considered.
- the inventors have noticed that the manufactures and marketers of prior art sexual performance and sexual dysfunction compositions, particularly the manufacturers and marketers of pharmaceuticals, appear to have a non-realistic and romanticized view of sexual arousal and function .
- Commercials show older, but sexually vibrant women who appear to have abnormally strong and persistent sex drives.
- the manufacturers and marketers of pharmaceuticals appear to think that sexual encounters can be planned - you take your ED pill two to three hours before the planned encounter, and everything goes off just as planned.
- the invention overcomes the above problem by providing a delivery system and method that is not adverse to the sexual experience, and preferably enhances the sexual experience.
- the delivery system comprises a breath-care element.
- the breath-care product can be an actual or simulated breath-care element.
- An actual breath care element is one that contains one or more ingredients designed to enhance or sweeten the breath.
- ingredients include, for example, a pH control agent, such as urea and buffers, a sulfur precipitating agent to reduce bad breath odor, inorganic components for tartar or caries control, such as phosphates and fluorides, a breath freshening agent, such as zinc gluconate, an anti- plaque/anti-gingivitis agent, such as chlorohexidene, CPC, and triclosan, a saliva stimulating agent including, for example, food acids such as citric, lactic, maleic, succinic, ascorbic, adipic, fumaric and tartaric acids, antimicrobially effective amounts of essential oils such as thymol, methyl salicylate, eucalyptol and menthol, or other like breath enhancement ingredients or combinations thereof.
- a simulated breath-care product is one that has an appearance of a breath-care product, but does not actually contain any ingredient to enhance the breath.
- An example of a simulated breath-care product is an edible strip, mint or lozenge without a breath-care ingredient.
- the delivery system and method comprises a water soluble edible film.
- the film comprises pullulan.
- the film may or may not include breath enhancers.
- the invention also contemplates that the breath-care element can also be a lozenge, mint, candy or other breath-care element. This embodiment lends itself particularly to sexual performance and sexual dysfunction compositions that are intended for one-time use just prior to a sexual encounter, though it also can be used to deliver compositions that are regularly administered.
- the delivery system comprises a food, beverage, spice, condiment or salad dressing.
- the preferred delivery systems include sports beverages, energy bars, candy(such as chocolate), shakes, alcoholic beverages and salad dressings.
- This embodiment lends itself particularly to sexual health and sexual dysfunction compositions that are intended to be administered on a regular basis, such as daily. However, they also can be used for one-time compositions, since food and beverages blend well with sexual activity.
- the preferred breath-care element delivery system comprises an edible film.
- the preferred edible film comprises pulullan.
- Edible films are well-known in the art. For example, see: United States Patent No. 6,596,298 B2 issued July 22, 2003 to Leung et al; United States Patent No. 6,656,493 B2 issued December 2, 2003 to Dzija et al., United States Patent No. 5,411 ,945 issued May 2, 1995 to Ozaki et al., particularly example B-2; United States Patent No. 5,518,902 issued May 21 , 1996 to Ozaki et al.; and International Patent Application Publication No. WO 99/17753.
- the film-forming agent used in the films according to the present invention can be selected from the group consisting of pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, carboxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragacanth gum, guar gum, acacia gum, arabic gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan, collagen, gelatin, zein, gluten, soy protein isolate, whey protein isolate, casein and mixtures thereof.
- Pullulan is used in amounts ranging from about 0.01 to about 99 wt %, preferably about 30 to about 80 wt %, more preferably from about 45 to about 70 wt % of the film and even more preferably from about 60 to about 65 wt % of the film.
- Sulfur precipitating agents pH control agents, tartar or caries control agents, breath freshening agents, anti-plaque/anti-gingivitis agents, antimicrobially agents, saliva stimulating agents, cooling agents, plasticizing agents, surfactants, stabilizing agents, emulsifying agents, thickening agents, and binding agents can also be added to the films.
- Sulfur precipitating agents bind with, and inactivate, the volatile sulfur compounds that cause a large percentage of oral malodor.
- Sulfur precipitating agents useful in the present invention include metal salts such as copper salts and zinc salts.
- Preferred salts include copper gluconate, zinc citrate and zinc gluconate.
- the amount of sulfur precipitating agent is from about 0.01 to about 2 wt %, preferably about 0.15 wt % to about 1.5 wt %, even more preferably about 0.25 wt % to about 1.0 wt % of the film.
- PH control agents include urea and buffers.
- Tartar or caries control agents include phosphates and fluorides.
- Breath freshening agents include zinc gluconate, anti-plaque/anti-gingivitis agents include chlorohexidene, CPC, and triclosan.
- Antimicrobially agents include effective amounts of essential oils such as thymol, methyl salicylate, eucalyptol and menthol.
- Saliva stimulating agents are disclosed in U.S. Pat. No. 4,820,506. These include food acids such as citric, lactic, malic, succinic, ascorbic, adipic, fumaric and tartaric acids, preferably, citric, malic and ascorbic acids.
- the amount of saliva stimulating agents in the film is from about 0.01 to about 12 wt %, preferably about 1 wt % to about 10 wt %, even more preferably about 2.5 wt % to about 6 wt %.
- Cooling agents include monomenthyl succinate, preferably in amounts ranging from about 0.001 to about 2.0 wt %, preferably about 0.2 to about 0.4 wt %.
- a monomenthyl succinate containing cooling agent is available from Mane, Inc.
- Other suitable cooling agents include WS3, WS23, Ultracool Il and the like.
- Plasticizing agents include triacetin, preferably in amounts ranging from about 0 to about 20 wt %, preferably about 0 to about 2 wt %.
- Other suitable plasticizing agents include monoacetin and diacetin.
- Preferred surfactants include mono and diglycerides of fatty acids and polyoxyethylene sorbitol esters, such as, Atmos 300 and Polysorbate 80.
- the surfactant can be added in amounts ranging from about 0.5 to about 15 wt %, preferably about 1 to about 5 wt % of the film.
- Other suitable surfactants include pluronic acid, and sodium lauryl sulfate.
- Stabilizing agents include xanthan gum, locust bean gum, carrageenan, and guar gum, preferably in amounts ranging from about 0 to about 10 wt %, preferably about 0.1 to about 2 wt % of the film.
- Emulsifying agents include triethanolamine stearate, quaternary ammonium compounds, acacia, gelatin, lecithin, bentonite, veegum, and the like, preferably in amounts ranging from about 0 to about 5 wt %, preferably about 0.01 to about 0.7 wt % of the film.
- Thickening agents include methylcellulose, carboxyl methylcellulose, and the like, preferably in amounts ranging from about 0 to about 20 wt %, preferably about 0.01 to about 5 wt %.
- Binding agents include starch, preferably in amounts ranging from about 0 to about 10 wt %, preferably about 0.01 to about 2 wt % of the film.
- Suitable sweeteners include: water-soluble sweetening agents such as monosaccharides, disaccharides and polysaccharides such as xylose, ribose, glucose (dextrose), mannose, galactose, fructose (levulose), sucrose (sugar), maltose, invert sugar (a mixture of fructose and glucose derived from sucrose), partially hydrolyzed starch, corn syrup solids, dihydrochalcones, monellin, steviosides, and glycyrrhizin; water- soluble artificial sweeteners such as the soluble saccharin salts, i.e., sodium or calcium saccharin salts, cyclamate salts, the sodium, ammonium or calcium salt of 3,4-dihydro-6-methyl-1,2,3-oxathiazine-4-
- water-soluble sweetening agents such as monosaccharides, disaccharides and polysaccharides such as xylose,
- auxiliary sweetener is utilized to provide the level of sweetness desired for a particular composition, and this amount will vary with the sweetener selected. This amount will normally be 0.01 % to about 10% by weight of the composition when using an easily extractable sweetener.
- the water-soluble sweeteners described above are usually used in amounts of about 0.01 to about 10 wt %, and preferably in amounts of about 2 to about 5 wt %.
- sweeteners e.g., glycyrrhizin
- these sweeteners are generally used in amounts of about 0.01 to about 10 wt %, with about 2 to about 8 wt % being preferred and about 3 to about 6 wt % being most preferred. These amounts may be used to achieve a desired level of sweetness independent from the flavor level achieved from any optional flavor oils used.
- Flavorings may also be added as known in the art. These flavorings may include synthetic flavor oils and flavoring aromatics, and/or oils, oleo resins and extracts derived from plants, leaves, flowers, fruits and so forth, and combinations thereof.
- Representative flavor oils include: spearmint oil, cinnamon oil, peppermint oil, clove oil, bay oil, thyme oil, cedar leaf oil, oil of nutmeg, oil of sage, and oil of bitter almonds.
- artificial, natural or synthetic fruit flavors such as vanilla, chocolate, coffee, cocoa and citrus oil, including lemon! orange, grape, lime and grapefruit and fruit essences including apple, pear, peach, strawberry, raspberry, cherry, plum, pineapple, apricot and so forth.
- flavorings can be used individually or in admixture.
- Commonly used flavors include mints such as peppermint, artificial vanilla, cinnamon derivatives, and various fruit flavors, whether employed individually or in admixture.
- Flavorings such as aldehydes and esters including cinnamyl acetate, cinnamaldehyde, citral, diethylacetal, dihydrocarvyl acetate, eugenyl formate, p-methylanisole, and so forth may also be used.
- any flavoring or food additive such as those described in Chemicals Used in Food Processing, publication 1274 by the National Academy of Sciences, pages 63-258, may be used.
- aldehyde flavorings include, but are not limited to acetaldehyde (apple); benzaldehyde (cherry, almond); cinnamic aldehyde (cinnamon); citral, i.e., alpha citral (lemon, lime); neral, i.e.
- beta citral lemon, lime
- decanal orange, lemon
- ethyl vanillin vanilla, cream
- heliotropine i.e., piperonal (vanilla, cream); vanillin (vanilla, cream); alpha- amyl cinnamaldehyde (spicy fruity flavors); butyraldehyde (butter, cheese); valeraldehyde (butter, cheese); citronellal (modifies, many types); decanal (citrus fruits); aldehyde C-8 (citrus fruits); aldehyde C-9 (citrus fruits); aldehyde C-12 (citrus fruits); 2-ethyl butyraldehyde (berry fruits); hexenal, i.e.
- trans-2 (berry fruits); tolyl aldehyde (cherry, almond); veratraldehyde (vanilla); 2,6-dimethyl-5-heptenal, i.e. melonal (melon); 2-6-dimethyloctanal (green fruit); and 2-dodecenal (citrus, mandarin); cherry; grape; mixtures thereof; and the like.
- the amount of flavoring employed is . normally a matter of preference subject to such factors as flavor type, individual flavor, and strength desired. Thus, the amount may be varied in order to obtain the result desired in the final product. Such variations are within the capabilities of those skilled in the art without the need for undue experimentation.
- Coloring agents or colorants also may be used in amounts effective to produce the desired color. These include pigments such as titanium dioxide, which may be incorporated in amounts of up to about 5 wt %, and preferably less than about 1 wt %. Colorants can also include natural food colors and dyes suitable for food, drug and cosmetic applications. These colorants are known as FD&C (Food, Drug and Cosmetic Act) dyes and lakes. The materials acceptable for the foregoing spectrum of use are preferably water-soluble, and include FD&C Blue No.
- Green No. 3 comprises a triphenylmethane dye and is the monosodium salt of 4-[4-N-ethyl-p-sulfobenzy!amino) dipheny!-methylene]-[1-N-ethyl-N-p- sulfonium benzyl)-2,5-cyclo-hexadienimine].
- the edible films can also include one or more of the following agents: a triglyceride, a preservative, a polyethylene oxide compound, and propylene glycol.
- triglycerides include vegetable oils such as corn oil, sunflower oil, peanut oil, olive oil, canola oil, soybean oil and mixtures thereof.
- a preferred triglyceride is olive oil.
- the triglyceride is preferably added to the film in amounts from about 0.1 wt % to about 12 wt %, preferably in a range from about 0.5 wt % to about 9 wt %, of the film.
- Preferred preservatives include sodium benzoate and potassium sorbate, preferably in amounts from about 0.001 wt % to about 5 wt %, preferably from about 0.01 wt % to about 1 wt % of the film.
- a preferred polyethylene oxide compound is N-10 having molecular weight from about 50,000 to about 6,000,000, which compound is available from Union Carbide Corporation.
- the polyethylene oxide compound is preferably added in amounts from about 0.1 wt % to about 5 wt %, preferably from about 0.2 wt % to about 4.0 wt % of the film. If propylene glycol is added, it is generally in amounts from about 1 wt % to about 20 wt %, preferably from about 5 wt % to about 15 wt % of the film.
- the active ingredient used in the film can be coated to mask the taste of the active ingredient or to prevent the active ingredient from numbing the tongue or other surfaces in the oral cavity.
- the coatings that can be used are known to those skilled in the art. These include polymers such, as EudragitTM acrylic polymers, cellulosics, such as ethylcellulose, and the like.
- An additional way to mask the taste of the active ingredient is by using an ion exchange resin such as Amberlite RP-69, available from Rohm and Haas, and Dow XYS-40010.00, available from the Dow Chemcial Co.
- a film forming agent suitable for delivery of one gram of a sexual health or sexual dysfunction composition according to the invention can be formed from the following ingredients: 2.2 g pullulan, 8 mg xanthan gum, 10 mg locust bean gum, 42 mg carrageenan, 10 mg Sodium Benzoate, 70 mg acesulfame potassium, 500 mg lemon flavoring, 190 mg aspartame NF, 50 mg polysorbate 80 NF, 50 mg Atmos 300, 400 mg propylene glycol, 70 mg triglycerides, 35 mg titanium dioxide.
- the preferred sexual health and sexual dysfunction compositions according to the invention lend themselves to delivery in foods, beverages, powders, spices, condiments and salad dressings, particularly those that are intended for administration on a regular basis, such as a daily basis. It is difficult to take any supplement or medication on a daily basis. Many people have cupboards full of vitamins, supplements, and even medications that were purchased with the intent to take on a daily basis, but never were. Particularly since sexual encounters happen randomly and infrequently, the sexual health compositions of the invention may also sit in a cupboard, and when the time comes when they are needed, it may be too late. Thus, it is useful to have a vehicle and method of delivery of these compositions that is more natural and immediate, such as a food, beverage, spice condiment or salad dressing that is used every day.
- FIG. 1 illustrates the food or beverage product 190 according to the invention and the method of making it.
- the food or beverage product includes a food or beverage base 110 and a sexual health or sexual dysfunction composition 120, examples of which composition 120 are given above.
- it may also include other ingredients 150, such as preservatives, color enhancers, thickening agents, vitamins, minerals, or other ingredients which may be added to foods.
- Food or beverage base 110, sexual health or sexual dysfunction composition 120, and any other desirable ingredient 150 are mixed at 160 to create food or beverage product 190.
- the terms "food base " and "beverage base” as used herein are intended to include any and all normal foods and beverages as well as low-fat or light foods and beverages.
- a low-fat or light salad dressing may be derived from the salad dressing base given below by substituting water and a thickening agent, such as xanthan gum, for all or a portion of the oil given in the formulation, or by other substitutions and formulations known in the salad dressing art.
- a thickening agent such as xanthan gum
- all terms that relate to the food or beverage component have the meaning commonly used in the food art
- all terms that relate to the sexual health composition component have the meaning they commonly have in the nutraceutical art.
- Spices, condiments and salad dressings are intended to be included in the term "foods", though we may at times specify these in particular to remind the reader that they are included in foods.
- the amounts of ingredients were given to make an appropriate dosage. In most cases, the amount given was the appropriate amount for a daily dosage. If it is expected that a food, foods, beverage, or beverages or both with the sexual health or sexual dysfunction composition added are expected to be consumed several times a day, the amounts used for a serving portion should be essentially halved - that is, it is assumed that the intake of the foods and/or beverages will be twice a day. It should be evident that if diets call for such foods or beverages more than twice a day, then the amounts of ingredients in a serving portion should be correspondingly reduced. If a food or beverage amount is such that it is intended for multiple servings, then the amount should also be correspondingly increased.
- the food bases do not include chewing gum, inert ingredients by themselves, or other conventional materials for delivering nutraceuticals.
- the common definition of food necessarily includes only materials the provide essential body nutrients. That is, the definition of food is intended to be narrow and is not to be broadened to include materials not commonly recognized as food.
- the preferred foods are: energy bars, salad dressings, condiments(such as steak sauce, mustard, catsup and soy sauce), vegetable oils, fruit products such as jellies, jams and syrups, cereals, trail mix, cookies, pasta, flours including wheat, soy, oat, and potato flour, whey, chocolate, yogurt, tofu, bagels, baked goods, vegetables, soups, trail mix, nutritional bars, snacks, crackers, meats, and meat products such as lunch meats, and milk products such as ice cream, cheese and butter.
- Salad dressing provides a few detailed examples of the process and product of the invention.
- any vegetable oil may be used, preferably soybean oil or canola oil.
- tsp means teaspoon
- tbsp means tablespoon
- mg is milligrams.
- VA cup vinegar red wine vinegar may be used
- 1 tsp sugar optional
- Vz tsp pepper Small amounts of spices such as onion powder and/or garlic powder may be added.
- the amounts given for exemplary salad dressings above are the amounts sufficient to fill a small bottle of about twelve to fifteen ounces. It is intended that the amounts of the ingredients given in the various salad dressing bases should be mixed with three to four dosages of the ingredients given in the various weight sexual health and sexual dysfunction compositions. The amounts are designed so that a serving of salad dressing is two ounces. It is assumed that salads are eaten twice a day so that two salads, or four ounces of salad dressing, provide effective daily amounts sexual health or sexual dysfunction ingredients.
- the various amounts given for salad dressing bases may be varied as known in the art of salad dressings, and the various amounts given for the sexual health and sexual dysfunction ingredients may be varied as known by those skilled in the art of sexual health and healthy, normal sexual function.
- the above oil and vinegar salad dressing base, Caesar salad dressing base, and French salad dressing base are merely exemplary salad dressing bases.
- salad dressing bases there are many other variations of salad dressing bases, and particularly many other variations of oil and vinegar salad dressing bases, Caesar salad dressing bases, French salad dressing bases, Ranch salad dressing bases, Bleu Cheese salad dressing bases, Russian salad dressing bases, and Thousand Island salad dressing bases, all of which may be used in the invention. From the above disclosure, and the sexual health and sexual dysfunction compositions given above, those skilled in the art of foods will understand the invention and how to implement it in a wide variety of foods.
- beverage is used in its common meaning which does not include water or medicines.
- the preferred beverages are sports drinks, soft drinks, alcoholic beverages, tea, coffee, milk, and fruit juices.
- a well-known formula for a basic sports drink is: 1 quart (32 oz) or 1 liter water, 1/3 cup sugar, 1/4 teaspoon sodium chloride, flavoring to taste. Potatssium chloride may be substituted for some of the sodium chloride if potassium levels are a concern. Any of the flavorings mentioned in section 3B above may be used.
- Another general purpose sports beverage that is particularly useful for athletic persons that exercise heavily for long periods, can be made using the following ingredients: saccharose 55 g/l, oligosaccharides 20 g/l, citric acid 1.8 g/l, citric aroma 1.0, sodium chloride 1.0 g/l.
- the fpregoing components can be mixed in the dry state and dissolved in 1 liter of water. In the preferred embodiment, the dry ingredients for the beverage are mixed with two doses of the desired sexual health composition and the mixed combination is dissolved in one liter or one quart of water.
- any of the above-mentioned foods or beverages, as well as other foods or beverages, can be used as a base for the preparation of a functional food or functional beverage product according to the invention.
- a sexual health or sexual dysfunction composition as disclosed above is mixed with the food or beverage base in appropriate amounts to provide the approximate dosages given above in a serving, or a plurality of servings if the food or beverage is expected to be ingested more often.
- the method of the invention preferably involves the administration, preferably daily oral administration, of the above-described compositions in conjunction with a specific dietary plan in a synergistic format.
- the dietary plan preferably involves multiple small meals, each reflecting the overall macronutrient composition of the diet. Carbohydrate content is low as is the glycemic index. Protein content is high.
- the glycemic index is preferably less than 60, more preferably less than 45; the carbohydrate content will constitute less than 50%, more preferably 0% - 50%, most preferably about 7% - 40% of the calories consumed on a daily basis; and the protein intake constitutes preferably at least 20%, more preferably about 20% - 40%, most preferably about 25-35% of total daily caloric intake.
- the number of meals is preferably 2, more preferably 4 to 6, per day. Adequate fluid intake is recommended to insure excellent hydration.
- the nutraceutical compositions of this invention are preferably administered on a daily basis.
- the composition can be administered on a non-daily basis, e.g., on alternate days .
- the frequency of administration will depend on the sexual needs of the user. The more frequent the composition is administered, the faster the attainment of healthy sexual function. Thus, daily administration of the composition will result in faster achievement of sexual health than non-daily administration.
- the method of this invention preferably further includes an exercise program.
- the exercise program will be followed at least 2 days a week and more preferably three to five days per week.
- the exercise program should preferably include components of aerobic and resistance training as tolerated by the individual in need thereof.
- the exercise program increases the over-all well being of the user which aids sexual performance, which leads to sexual confidence.
- the invention may further include a stress reduction program designed to diminish glucocorticoid activity. By downgrading glucocorticoid activity, the stress reduction program acts to improve enjoyment of sex with concurrent improvements in sexual function. Utilizing similar mechanisms, pyridoxine augments both these actions.
- the stress reduction program may involve any activity that lowers glucocorticoid levels. Non-limiting examples of such activities include relaxation, getting a massage, acupuncture, psychotherapy, meditation, taking a sedative, and the like.
- any of the sexual performance or sexual dysfunction pharmaceuticals such as vardenafil, tadalafil, sildenafil, and apomorphine, can also be administered by one of the vehicles disclosed in section 3 above.
- any of the sexual performance or sexual dysfunction pharmaceuticals such as vardenafil, tadalafil, sildenafil, and apomorphine, can also be administered by one of the vehicles disclosed in section 3 above.
- only exemplary additives, such a breath-freshening agents have been mentioned, since this disclosure is not about breath-freshening, but compositions and methods for healthy sexual function. To include all possible additives, such as all possible breath-freshening agents, would make the disclosure unwieldy and detract from the essential focus.
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Abstract
Description
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