SPORTS HEALTH PERFORMANCE COMPOSITION BACKGROUND

Abstract

A topical composition that includes L-arginine that is used as a sports health composition. The composition can further include forskolin. Disclosed is a method of using the topical composition.

Claims

1. A topical composition comprising an effective amount of L-arginine with a base or carrier component and skin penetration enhancer, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.

2. The topical composition of claim 1, wherein the L-arginine comprises about 5 wt % to 60 wt %, about 15 wt % to 50 wt %, or about 20 wt % to 40 wt % of the total weigh of the topical composition.

3. The topical composition of claim 1, wherein the L-arginine is L-arginine ethyl ester, L-arginine hydrochloride or a free base of L-arginine.

4. The topical composition of claim 1, further comprising forskolin.

5. The topical composition of claim 4, wherein the forskolin comprises about 0.01 to about 1 wt %, about 0.1 to about 0.5 wt %, or about 0.1 wt % based on the weight of the topical composition.

6. The topical composition of claim 1, wherein the base components comprises from about 30 wt % to 80 wt %, about 40 wt % to 70 wt %, or about 50 wt % to 60 wt. based on the total weight of the topical composition.

7. The topical composition of claim 1, wherein the base is selected from oil in water emulsion or water in oil emulsion, anhydrous silicone base, lipophilic foam base, transdermal cream base, or transdermal gel base.

8. The topical composition of claim 1, wherein the skin penetration enhancers comprise essential oils, fatty acids, or polysaccharides.

9. The topical composition of claim 1, wherein the skin penetration enhancers are selected from methyl salicylate, menthol, arnica, capsaicin and hyaluronic acid.

10. The topical composition of claim 1, wherein the skin penetration enhancers comprise about 1 wt % to 50 wt %, about 5 wt % to 40 wt %, or about 10 wt % to 35 wt % based on the weight of the topical composition.

12. The topical composition of claim 1, wherein the skin penetration enhancers comprise methyl salicylate in a range of about 1 wt % to 30 wt %, about 5 wt % to 25 wt %, or about 10 wt % to 20 wt % based on the total weight of the topical composition.

13. The topical composition of claim 1, wherein the skin penetration enhancers comprise menthol in a range of about 1 wt % to 16 wt %, about 4 wt % to 12 wt %, or about 6 wt % to 10 wt % based on the total weight of the topical.

14. The topical composition of claim 1, wherein the topical composition is in the form of a gel, cream, ointment, foam, spray or patch.

15. The topical composition of claim 1, wherein in topical composition further comprises a pain reliever and/or a muscle relaxant.

16. A method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise comprising delivering a topical composition to an area of the skin where desired, the topical composition comprising an effective amount of L-arginine with a base or carrier component and skin penetration enhancer.

17. The method of claim 16, wherein the L-arginine is L-arginine ethyl ester, L-arginine hydrochloride or a free base of L-arginine.

18. The method of claim 16, wherein the base components comprises about 30 wt % to 80 wt %, about 40 wt % to 70 wt %, or about 50 wt % to 60 wt % based on the total weight of the topical composition.

19. The method of claim 16, wherein the base is selected from oil in water emulsion or water in oil emulsion, anhydrous silicone base, lipophilic foam base, transdermal cream base.

20. A method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise comprising topically administering an effective amount of a topical composition consisting essentially of L-arginine to a subject in combination with use of a transdermal electrically polarized conductive pad attached to an electro-stimulation power controlled device, wherein the effective amount of L-arginine in combination with an electric field (or current) enhancing skin penetration allows lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.

Description

DETAILED DESCRIPTION

[0027] The present disclosure is generally directed to a product of a nitrous oxide (NO) donor that may be used to enhance both women's and/or men's sports health performance and active rest recovery. An exemplary nitrous oxide donor can include L-arginine, which acts by keeping blood vessels dilated. The dilated blood vessels allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise. L-arginine also has several roles in the body such as assisting in wound healing, ensuring that cells divide properly, helping to remove ammonium from the body, facilitating immune function, and promoting the secretion of several hormones including glucagon, insulin, and growth hormone (The Natural Pharmacy, 1998.

[0028] Forskolin is a naturally occurring alkaloid derived from the Indian herb Coleus forskohlii that has been shown to induce smooth muscle relaxation and increase blood flow. Forskolin binds directly and stimulates adenylate cyclase increasing cAMP concentrations, and can directly reduce intracellular calcium concentrations in smooth muscle causing relaxation in a NO-independent pathway. Forskolin can optionally be used in compositions with L-arginine to enhance dissipation of lactic, thereby increasing sport performance via a NO independent pathway.

[0029] L-arginine may be provided as a free base, as L-arginine hydrochloride or as L-arginine alkyl (ethyl, methyl propyl, isopropyl butyl, isobutyl,) esters of L-arginine and salts thereof. Pharmaceutically acceptable salts include hydrochloride, glutamate, butyrate and glycolate.

[0030] Administration of L-arginine by intravenous infusion (IV) or orally at doses (6 to 30 gm) induced peripheral vasodilation in humans and improved endothelium-dependent vasodilation, resulting in improved muscle blood flow. [0031] L-arginine oral (12 capsules of 0.5 gm of L-arginine HCL) was administered Bioavailability was 50 to 87% with a time to Cmax of 40 to 60 min [0032] Mean Cmax: 6223 and 822 umol/L for 30 and 6 gm IV, and 310+/−152 umol/L for 6 gm oral [0033] Half life 60 (IV) to 90 (PO) min [0034] No significant changes in hemodynamics at 6 gm doses; blood pressure and total peripheral resistance were significantly decreased after 30 gm IV [0035] Increased urinary cGMP and nitrate excretion (correlate with plasma concentrations) with 6 gm and 30 gm IV causing significant increases.

[0036] Numerous over the counter products (gels and creams) are available with or without other agents such as ginseng, niacin and L-citrulline (concentrations up to 5%). Since an oral dose of 10 gm of L-arginine produces a peak arginine plasma concentration of 200 to 300 uM and the Km of NOS activity for endothelial cells is approximately 30 to 40 uM, a 10 gm oral dose produces plasma concentrations that are 10-fold above the Km. Therefore, topical administration of L-arginine needs to be delivered at concentrations greater than about 30 to 40 uM to achieve the desired physiological effects. Suitable topical formulations should deliver at least about 50 to 70 mg/L (50 to 70 ug/ml) to the endothelial cell membrane to achieve desired effective amounts of arginine free base. One skilled in the art would readily determine suitable amounts to be delivered in formulations comprising L-arginine hydrochloride or L-arginine alkyl (ethyl, methyl propyl, isopropyl butyl, isobutyl,) esters of L-arginine and salts thereof. In some embodiments, the L-arginine includes about 5 wt % to 60 wt %, about 15 wt % to 50 wt %, or about 20 wt % to 40 wt % of the total weigh of the topical composition.

[0037] In some embodiments, the composition can further include forskolin from about 0.01 to about 1 wt %, about 0.1 to about 0.5 wt %, or about 0.1 wt % based on the weight of the topical composition.

Base Components

[0038] The L-arginine is included with base or carrier components. The base components include glycols (e.g. propylene glycol USP, polyethylene glycol), oil-in water emulsions, water-in oil emulsions, lipophilic foams, water, anhydrous silicone base, lipophilic foam base, transdermal cream base and mineral oils. In some embodiments, the base component is from about 30 wt % to 80 wt %, about 40 wt % to 70 wt %, or about 50 wt % to 60 wt % based on the total weight of the topical composition. In some embodiments, the base components include base selected from oil in water emulsion, water in oil emulsion, anhydrous silicone base, lipophilic foam base, transdermal cream base, or transdermal gel base.

[0039] Those skilled in the art would readily understand how to prepare suitable topical compositions that are formulated with a transdermal cream base. A typical cream base may include commercially available components such as, for example, purified water, humectants, oil in water emulsifiers, lubricants, silicones, rheology enhancers, preservatives, vitamin E and liposomes.

[0040] Those skilled in the art would also readily understand how to prepare suitable topical compositions that are formulated with a transdermal gel base. A typical gel base may include commercially available components such as, for example, purified water, alcohols (benzyl alcohol, isopropyl alcohol, ethanol), nonionic and amphiphilic surfactants, emulsifiers cellulose ethers and cellulose derivatives, polyacrylate/polyalkenyl polyether derivatives, and pH adjusters (hydrochloric acid, sodium hydroxide).

Skin Penetration Enhancers

[0041] In some embodiments, the disclosed composition is delivered topically to the skin. Unfortunately, dermal and transdermal delivery can be limited by the permeability of the substance or composition. To enhance or improve the absorption or delivery of L-arginine through the skin, skin penetration enhancers may be included. Both chemical and/or physical approaches can be used to enhance the penetration of substances across the skin. A skin penetration enhancer may include compounds that assist in the effective delivery of a desired ingredient (e.g. L-arginine) into the skin. Exemplary skin penetration enhances include volatile oils (e.g. essential oils), fixed oils (e.g. fatty acids) and polysaccharides. Essential oils are volatile, odoriferous substances found in the flowers, fruit, leaves and roots of certain plants. Fatty acids, on the other hand, are composed of aliphatic hydrocarbon chains, which can be either saturated or unsaturated, and include a terminal carboxyl group.

[0042] Essential oils are a complex mixture of many diverse and unique chemical compounds. Essential oils can include compounds classified as: [0043] nitrogen- and sulphur-containing compounds (e.g., allyl isothiocyanate found in mustard oil); [0044] aromatic compounds, which are benzene derivatives (e.g., eugenol which is the main constituent of clove oil); [0045] terpenes (e.g., 1,8-cineole in eucalyptus oil) and terpenoids; and [0046] miscellaneous compounds (includes long-chain unbranched substances).

[0047] Exemplary essential oils include niaouli oil, eucalyptus oil, alpinia oxyphylla oil, turpentine oil, sweet basil and tulsi oil, cardamom oil, peppermint oil, fennel oil, black cumin oil.

[0048] Terpenes, which is a constituent of an essential oil can be isolated from essential oils and are also suitable skin penetration enhancers. Terpenes do not have the aromatic character but contains carbon and hydrogen atoms with or without oxygen. Exemplary terpenes include the following classes along with specific examples in that particular class:

TABLE-US-00001 TABLE 1 Class Exemplary Terpenes Source ACYCLIC Geraniol and nerol Geraniol is an unsaturated primary MONOTERPENES alcohol found in geranium and other (Alcohols) essential oils. It is found as esters and as a glucoside, but mainly occurs in the free form. Nerol is the isomeric alcohol and is found in various essential oils, primarily in neroli and bergamot oils Palmarosa oil contains more geraniol than any other oil and for nerol it is Linalol Linalol is found as (+)- and (−)-forms in the oil of Linaloe (a plant found in Central America), but can also be found free and as esters in numerous other essential oils. Rosewood oil contains more linalol than any other oil. MONOCYCLIC Limonene The optically active limonene is MONOTERPENES widespread in nature and is found in (Hydrocarbons) its (+)- and (−)- forms in various essential oils such as bergamot, caraway, lemon and orange oils. The signature oils for d-limonene and l- limonene is grapefruit and fleabane, MONOCYCLIC α-Terpineol Found in many essential oils such as MONOTERPENES camphor, neroli and petitgrain oil. The (Alcohols) Alcohols signature oil is lemon eucalyptus. related to α-terpineol β-Terpineol Isomeric with α-terpineol, but is not isolated from natural sources. Found in commercial terpineol. γ-Terpineol Second isomer of α-terpineol and is found in at least one essential oil and commercial terpineol. MONOCYCLIC Menthol Menthol is a constituent of numerous MONOTERPENES peppermint oils and is found as its (−)- (Alcohols) Alcohols form. derived from thymol MONOCYCLIC Carveol Carveol is found in caraway oil. MONOTERPENES (Alcohols) Alcohols derived from carvacrol MONOCYCLIC Menthone (−)-form is found in numerous MONOTERPENES peppermint oils, (+)-form also occurs (Ketones) naturally. Ketones related to menthone Pulegone Found in pennyroyal and many other essential oils as its (+)- iso-Pulegone Often an accompaniment of pulegone in essential oils. Piperitone Occurs in numerous eucalyptus oils as (+)- and (−)-forms. MONOCYCLIC Carvomenthone Isomeric with menthone and is a MONOTERPENES saturated ketone. (−)-Form is found in (Ketones) numerous essential oils. Ketones related to carvomenthone Carvone Occurs in its (+)-, (−)- and (±)-forms and Unsaturated is the main constituent of caraway and ketone dill oils. It can also be found in spearmint MONOCYCLIC 1,8-Cineole Widespread in essential oils, particularly MONOTERPENES in eucalyptus and wormseed oil. (Oxides) BICYCLIC α-Thujene Found in numerous essential oils. MONOTERPENES (Hydrocarbons) BICYCLIC Car-3-ene Found in several turpentine oils. MONOTERPENES (Hydrocarbons) BICYCLIC α-Pinene Widespread in nature, found in most MONOTERPENES essential oils of Coniferae. It is the (Hydrocarbons) main constituent of turpentine oil. Secreted by conifers, turpentine oil consists of resinous material dissolved in β-Pinene (Nopinene) Isomeric with α-pinene. Its signature oil is galbanum. BICYCLIC Verbenol, verbenone Verbenol and verbenone has been found MONOTERPENES and verbanone in nature, with the latter being found in (Oxygenated verbena oil. The signature oil for derivatives) verbenone is rosemary verbenone. BICYCLIC Camphor Not widely distributed in nature, is the MONOTERPENES major constituent of camphor oil, (Ketones - camphane obtained from the leaves and wood of group) the camphor tree (Cinnamomum BICYCLIC Fenchone Occurs as the optically active forms in MONOTERPENES fennel, thuja and cedar leaf oils. (Ketones - fenchane group SESQUITERPENES Farnesol Widely distributed in flower oils, in (Alcohol) particular those of the acacia, cyclamen and the rose. Nerolidol Isomeric with farnesol and found in neroli oil. (−)-Guaiol A crystalline alcohol found in guaiacum wood oil. (+)-Cedrol Cedarwood oil. (−)-α-Bisabolol Camomile oil. SESQUITERPENES Bisabolene Widespread in nature, found in bergamot (Hydrocarbon) and myrrh oils. Also in many other essential oils. The Azulenes All hydrocarbons are derived from (Unsaturated azulene (C.sub.10H.sub.8), a parent hydrocarbon. hydrocarbons) Most of those attained from natural origin have the molecular formula C.sub.15H.sub.18. Azulenes is responsible for the blue color of certain essential oils, or when essential oils become blue/violet when undergoing processes which might (+)-Longifolene Tricyclic sesquiterpene found in the essential oil of Pinus longifolia. β-Caryophyllene Main hydrocarbon constituent of clove oil. (+)-Aromadendrene Eucalyptus oil. (+)-β-Cedrene Cedarwood oil. ACYCLIC Phytol Found in rosemary oil. DITERPENES (Alcohol) ACYCLIC Squalene It is found in the unsaponifiable fraction TRITERPENES of shark liver oil and in several plant (Hydrocarbon) sources such as vegetable oils and several fungi. Jasmine is the signature oil.

[0049] In some embodiments, the terpene menthol is used as a skin penetration enhancer in a composition containing L-arginine.

[0050] Exemplary fixed oils or fatty acids include fish oil, fatty acids from algae and phospholipids (e.g. phosphatidylglyceol, phosphatidylethanolamine, phosphatidylcholine, phosphatidylserine, phosphatidic acid, phosphdtylinositol.

[0051] Exemplary polysaccharides (polymer of simple sugars and their derivatives) as skin penetration enhancers include chitosan, aloe vera gel or aloe vera juice.

[0052] Other skin penetration enhancers can include methyl salicylate, capsaicin (trans-8-methyl-N-vinilly-6-nonenamide, which is an alkaloid derived from hot chili peppers, belonging from the genus Capsicum of the Solanaceae family), vitamin E (α-tocopherol and methyl salicylate (oil of wintergreen or wintergreen oil is an organic ester naturally produced by many species of plants, particularly wintergreens).

[0053] Skin penetration enhancers such as terpenes and phospholipids can also be used to prepare vesicles (e.g. liposomes, ivansomes and ethosomes) for transdermal delivery. In other embodiments, essential oils can also be incorporated into patches for transdermal delivery. Exemplary oils can include any of the disclosed essential oils. In some embodiments, the essential oils used in patches include menthol oil patches, lemon grass oil, clove oil, eucalyptus oil or combinations thereof. The transdermal patches used can include matrix, microreservoir, reservoir, adhesive and membrane-matrix hybrid type patches.

[0054] In some embodiments, the topical composition may include L-arginine in any suitable form and includes menthol, methyl salicylate, or capsaicin with a base or carrier. In other embodiments, the topical composition includes L-arginine and menthol in a range of about 1 wt % to 16 wt %, about 4 wt % to 12 wt %, or about 6 wt % to 10 wt % based on the total weight of the topical. In still other embodiments, the topical composition includes L-arginine and methyl salicylate in a range of about 1 wt % to 30 wt %, about 5 wt % to 25 wt %, or about 10 wt % to 20 wt % based on the total weight of the topical, base carrier with about 30 wt % of methyl salicylate.

Electrical Stimulation & Related Devices

[0055] Like L-arginine, electrostimulation may also facilitate blood vessel dilation which allows lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise. Both L-arginine and electrostimulation may allow the delivery of alternative actives, such as pain relief medication into the deeper tissue because of the vasodilation that it produces. In contrast to electrophoresis which requires actives to be in the ionized state for delivery, L-arginine and electrostimulation may allow non-ionized actives to be absorbed to a greater extent than in their absence.

[0056] Electro-stimulation may be done with a conductive pad that is separated into 2 polarity regions. An oscillating pulse voltage ranging from 60 Volts to 1000 Volts is applied to pad electrodes and the signal is then transmitted into the muscle transdermal. This is usually the way it is done.

[0057] An advantage of using L-arginine and/or electro stimulation is that it may assist in reducing the amount of topical pain reliever needed to produce the same therapeutic effect and in some cases may even reduce the chance of chemical burns that some topical pain relievers may produce. In some embodiments, the topical composition is applied in combination with electro stimulation. In other embodiment provide a method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise comprising topically administering an effective amount of a topical composition consisting essentially of L-arginine to a subject in combination with use of a transdermal electrically polarized conductive pad attached to an electro-stimulation power controlled device, wherein the effective amount of L-arginine in combination with an electric field (or current) enhancing skin penetration allows lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.

Pain Relief Medication and Muscle Relaxers

[0058] The disclosed topical compositions may also include pain relief medications. Suitable pain relief medications may include non-narcotic analgesics, NSAIDS, COX-2 inhibitors, narcotic pain medication central analgesics, narcotic analgesics and aspirin, topical analgesics or topical anesthetics as well as combinations of these medications. Exemplary pain relief medications include:

TABLE-US-00002 Non-Narcotic Analgesics Acetaminophen NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) Bromfenac Indomethacin Naproxen Diclofenac Ketoprofen Oxaprozin Diflunisal Ketorolac Phenylbutazone Etodolac Meclofenamate Piroxicam Fenoprofen Mefenamic Acid Sulindac Flurbiprofen Meloxicam Tolmetin Ibuprofen Nabumetone COX-2 Inhibitors Celecoxib Narcotic Pain Medications (Painkillers) Buprenorphine Levorphanol Oxycodone Butorphanol Meperidine Oxymorphone Codeine Methadone Pentazocine Hydrocodone Morphine Propoxyphene Hydromorphone Nalbuphine Tapentadol Central Analgesics Tramadol Tramadol and Acetaminophen Combinations Butalbital, Acetaminophen and Aspirin, Caffeine, and Acetaminophen, Codeine Dihydrocodeine and Caffeine Butalbital, Aspirin, Dihydrocodeine, Aspirin and Codeine and Caffeine Acetaminophen, and Caffeine Butalbital, Hydrocodone and Hydrocodone and Aspirin acetaminophen, Acetaminophen caffeine, and codeine Hydrocodone and Oxycodone and Oxycodone and Aspirin Ibuprofen Acetaminophen Morphine/Naltrexone Pentazocine and Pentazocine and Aspirin Acetaminophen Pentazocine/Naloxone Propoxyphene and Propoxyphene, Aspirin, and Acetaminophen Caffeine Topical Analgesics Capsaicin Topical Anesthetics Benzocaine Dibucaine Lidocaine/Prilocaine Benzocaine/Menthol Lidocaine

[0059] The disclosed topical compositions may also include muscle relaxants; suitable muscle relaxant are described below

Skeletal Muscle Relaxants:

[0060] Suitable muscle relaxants are known to those skilled in the art and may be identified, for example, at internet net sites such as http://www.drugs.com/drug-class/skeletal-muscle-relaxants.html and http://www.md-health.com/Muscle-Relaxers.html

Homeopathic and Herbal Preparations

[0061] Suitable homeopathic and herbal preparations are also known to those skilled in the art and may be identified, for example, at internet net sites such http://www.wisegeek.org/what-are-the-different-types-of-over-the-counter-muscle-relaxant.htm. Homeopathic medications generally are based on the idea that you treat a disorder with the same ingredients that cause it, and this holds true for muscle relaxants. Rather than trying to block nerve signals or change the surface chemistry of damaged tissues, these medications typically look to “treat like with like,” intending to stop tension and pain with diluted forms of the very supplements that can cause these problems. Examples include calcarea phosphorica, which may be helpful for neck and upper back pain and tension; kali carb, which is used to treat lower back pain; and arnica, which may help relax overworked muscles.

[0062] A number of herbs and plant materials can also be used to form what is basically an all-natural over-the-counter muscle relaxant. Herbs like catnip, valerian, bergamot, licorice, basil and caraway are typically believed to have anti-inflammatory properties, which can help reduce joint swelling. Valerian, a flowering perennial plant, has been used since medieval times to treat neck tension. Other herbs, such as kava root, white willow, horsetail and devil's claw, do better at combating pain. Many of these natural alternatives can be found either combined or in isolation in health or wellness stores, and are commonly sold as teas, capsules, or powders.

[0063] Some people also find relief by increasing the vitamin and mineral content of their meals. Proper amounts of calcium and magnesium can often help relieve muscle pain, and magnesium can help repair damaged nerve endings, too. Other important vitamins and minerals that help act as muscle relaxants include silica, potassium, vitamin C and alpha lipoic acid.

OTC Muscle Relaxants for Back Pain

[0064] Acetaminophen is a multi-purpose antipyretic medicine that reduces fever and eases pain. Also referred to as paracetamol; acetaminophen has limited side effects and hence can be used safely. However proper guidance is always required and overdose of the drug is often associated with liver disorders, skin and allergic rash along with abdominal pain. However, the action of acetaminophen in management of muscle pains is fairly limited see, for example, http://www.simple-remedies.com/health-tips-3/ote-muscle-relaxants.html. A non-steroidal anti-inflammatory drug or NSAID is another over-the-counter relaxant for muscles.

Natural Muscle Relaxants as Alternate Pain Relief

[0065] The various limitations are risks associated with the use of OTC have resulted in a need to identify natural muscle relaxants which can provide sustained pain relief. Here are certain natural products that can be beneficial.

[0066] Rosemary oil can alleviate pain from muscle cramps and spasms when mixed in a warm bath. Massaging the affected part with rosemary oil can provide sustained relief. Chamomile Essential Oil is also considered to have similar effect and helps in management of muscle spasms, pain and joint aches.

[0067] Herb Catnip has a tranquilizing effect that can help reduce inflamed or swollen joints.

[0068] Homeopathic remedies are yet another famous pain relievers with treatments like Calcarea phosphorica, Arnica and Kali carb. These remedies need to be taken in low dosage and should be repeated over several times in a day.

[0069] Milk containing turmeric and honey. Turmeric has strong anti-inflammatory properties while honey helps in reducing inflammatory response. Milk is considered to be a mood food and helps reduce anxiety and irritability associated with the muscular pain. Magnesium and calcium supplements play a pivotal role in reducing muscular pain and muscle spasms.

Topical Formulations

[0070] The disclosed L-arginine may be formulated as a topical preparation. Topical formulations include creams, ointments, lotions, gels, foams, sprays and patches (transdermal). Typically, the skin surface on which the disclosed topical composition is applied could be on legs, arms, abdomen, or back as may be convenient to the user.

[0071] Suitably, the compositions are administered at least one a day (e.g., one a day, twice a day, three times a day, or the like.) for as long as desired, suitably on the order of days to weeks to months, or longer if desired.

[0072] Those skilled in the art will readily determine suitable dosages of the topical compositions to be applied for a variety of the disclosed applications and formulations.

[0073] The topical compositions disclosed herein may be packaged in any convenient package depending on the particular formulation. Suitable dispensing or packaging may include, for example, squeezable tubes, sachets, pouches, or single or multiple use containers.

[0074] The topical compositions of the present disclosure are suitably used to facilitate blood vessel dilation to allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.

[0075] Also disclosed is a method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise. The method includes applying or delivering the topical composition of L-arginine, base and skin penetration enhancers.

[0076] The topical compositions disclosed herein provide the advantages of increasing blood flow, dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise and for the ability to deliver the composition more selectively to a specific, desired site.

[0077] Some additional non-limiting embodiments are provided below to further exemplify the present disclosure:

1. A topical composition comprising an effective amount of L-arginine with a base or carrier component and skin penetration enhancer, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.
2. A topical composition consisting essentially of an effective amount of L-arginine with a base or carrier component and skin penetration enhancer, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.
3. A topical composition consisting essentially of an effective amount of L-arginine with a base or carrier component and skin penetration enhancer and forskolin, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.
4. A topical composition consisting of an effective amount of L-arginine with a base or carrier component, and skin penetration enhancer, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.
5. A topical composition consisting of an effective amount of L-arginine with a base or carrier component, forskolin, and skin penetration enhancer, the composition capable of dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.
6. The topical composition as in any one of the preceding embodiments, wherein the L-arginine comprises about 5 wt % to 60 wt %, about 15 wt % to 50 wt %, or about 20 wt % to 40 wt % of the total weigh of the topical composition.
7. The topical composition as in any one of the preceding embodiments, wherein the L-arginine is L-arginine ethyl ester, L-arginine hydrochloride or a free base of L-arginine.
8. The topical composition of embodiments 1-5 wherein the effective amount of forskolin comprises about 0.01-1 wt %, preferably about 0.1-0.5 wt %, or more preferably about 0.1 wt % based on the weight of the topical composition.
9. The topical composition as in any one of the preceding embodiments, wherein the base components comprises from about 30 wt % to 80 wt %, about 40 wt % to 70 wt %, or about 50 wt % to 60 wt % based on the total weight of the topical composition.
10. The topical composition as in any one of the preceding embodiments, wherein the base is selected from oil in water emulsion or water in oil emulsion, anhydrous silicone base, lipophilic foam base, transdermal cream base, or transdermal gel base.
11. The topical composition as in any one of the preceding embodiments, wherein the skin penetration enhancers comprise essential oils, fatty acids, or polysaccharides.
12. The topical composition as in any one of the preceding embodiments, wherein the skin penetration enhancers are selected from methyl salicylate, menthol, arnica, capsaicin and hyaluronic acid.
13. The topical composition as in any one of the preceding embodiments, wherein the skin penetration enhancers comprise about 1 wt % to 50 wt %, about 5 wt % to 40 wt %, or about 10 wt % to 35 wt % based on the weight of the topical composition.
14. The topical composition as in any one of the preceding embodiments, wherein the skin penetration enhancers comprise methyl salicylate in a range of about 1 wt % to 30 wt %, about 5 wt % to 25 wt %, or about 10 wt % to 20 wt % based on the total weight of the topical composition.
15. The topical composition as in any one of the preceding embodiments, wherein the skin penetration enhancers comprise menthol in a range of about 1 wt % to 16 wt %, about 4 wt % to 12 wt %, or about 6 wt % to 10 wt % based on the total weight of the topical.
16. The topical composition as in any one of the preceding embodiments, wherein in topical composition is in the form of a gel, cream, ointment, foam, spray or patch.
17. The topical composition as in any one of the preceding embodiments, wherein in topical composition further comprises a pain reliever and/or a muscle relaxant.
18. A method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise comprising delivering a topical composition to an area of the skin where desired, the topical composition comprising an effective amount of L-arginine with a base or carrier component and skin penetration enhancer.
19. The method of claim 18 or any one of the preceding embodiments, wherein the L-arginine is L-arginine ethyl ester, L-arginine hydrochloride or a free base of L-arginine.
20. The method of claim 18 or any one of the preceding embodiments, wherein the base components comprises about 30 wt % to 80 wt %, about 40 wt % to 70 wt %, or about 50 wt % to 60 wt % based on the total weight of the topical composition.
21. The method of claim 18 or any one of the preceding embodiments, wherein the base is selected from oil in water emulsion or water in oil emulsion, anhydrous silicone base, lipophilic foam base, transdermal cream base.
22. The method of claim 18 or any one of the preceding embodiments, wherein the skin penetration enhancers comprise essential oils, fatty acids, or polysaccharides.
23. The method of claim 18 or any one of the preceding embodiments, wherein the skin penetration enhancers are selected from methyl salicylate, menthol, arnica, capsaicin and hyaluronic acid.
24. The method of claim 18 or any one of the preceding embodiments, wherein the skin penetration enhancers comprise about 1 wt % to 50 wt %, about 5 wt % to 40 wt %, or about 10 wt % to 35 wt % based on the weight of the topical composition.
25. The method of claim 18 or any one of the preceding embodiments, wherein the skin penetration enhancers comprise methyl salicylate in a range of about 1 wt % to 30 wt %, about 5 wt % to 25 wt %, or about 10 wt % to 20 wt % based on the total weight of the topical composition.
26. The method of claim 18 or any one of the preceding embodiments, wherein the skin penetration enhancers comprise menthol in a range of about 1 wt % to 16 wt %, about 4 wt % to 12 wt %, or about 6 wt % to 10 wt % based on the total weight of the topical composition.
27. The method of claim 18 or any one of the preceding embodiments, wherein in topical composition is in the form of a gel, cream, ointment, foam, spray or patch.
28. The method of claim 18 or any one of the preceding embodiments, wherein in topical composition further comprises a pain reliever and/or a muscle relaxant.
29. A method for dilating blood vessels to thereby allow lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise comprising topically administering an effective amount of a topical composition consisting essentially of L-arginine to a subject in combination with use of a transdermal electrically polarized conductive pad attached to an electro-stimulation power controlled device, wherein the effective amount of L-arginine in combination with an electric field (or current) enhancing skin penetration allows lactic acid to dissipate from muscular tissue during exercise or during the recovery phase after exercise.

[0078] It will be readily apparent to one of ordinary skill in the relevant arts that other suitable modifications and adaptations to the composition, methods and applications described herein can be made without departing from the scope of any of the embodiments. The following examples are included herewith for purposes of illustration only and are not intended to be limiting.

Examples

[0079] A topical composition as an oil in water emulsion is formulated with L-arginine monohydrochloride 20 wt %, with or without forskolin 0.1% wt %, methyl salicylate 15 wt %, menthol 5 wt %, and oil in water (O/W) emulsion with preservative 60 wt %. This composition is packaged in 5 mL foil package. After exercise, this topical composition is applied to skin to dilate blood vessels allowing lactic acid to dissipate from muscular tissue.