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Title:  Compositions and methods for an orally administered inhibitor of biting insects
United States Patent: 
October 3, 2006

 Meredith; Sarah (Laguna Niguel, CA)
Appl. No.: 

June 7, 2004




The present disclosure concerns methods and compositions to inhibit insects from biting a subject. In preferred embodiments, the compositions may be administered orally, for example using a spray bottle to deliver to the mouth. In certain embodiments, the compositions and methods are effective to reduce swelling, itching, redness and/or inflammation of the local area of an insect bite. The compositions may include one or more herbs selected from the group consisting of rice bran, peppermint, barley grass, lobelia; chlorella, watercress, alfalfa and parsley and one or more vitamins selected from the group consisting of thiamin (B-1), riboflavin (B-2), niacin (B-3), pantothenic acid (B-5), pyridoxine (B-6), folic acid (B-9), cyanocobalamin (B-12), choline, inositol, d-biotin, para-aminobenzoic acid, and lecithin. Administration of effective amounts of the compositions is sufficient to inhibit insects from biting and/or treat insect affected areas of a subject.


Certain embodiments of the present invention concern compositions and/or methods of producing and using biting insect inhibitors derived from naturally occurring products. In one aspect, an insect inhibitor composition suitable for human oral and/or topical application comprises one or more vitamins combined with one or more herbs. It will be understood that where the present disclosure refer to a composition comprising one or more herbs, the one or more herbs may be present in any form, including but not limited to the native herb, a crushed herb, an extract, a concentrate, a decoction, an infusion, a homogenate, an essence and/or a distillate of an herb.

In various embodiments, the compositions inhibit insects from biting subjects following oral ingestion of the compositions by the subjects. In other embodiments, the compositions reduce inflammation, swelling, redness and/or itching of the localized region of an insect bite. The compositions may be provided in any form known in the art, but in a preferred embodiment come in the form of a water-based solution suitable for administration with a spray bottle, for example by spraying into the mouth of a subject, followed by ingestion.

In another preferred embodiment, a composition suitable for human oral and/or external application comprises one or more vitamins combined with one or more herbs to inhibit mosquitoes from biting subjects.

A composition suitable for oral and/or external application may be provided in a variety of forms, including but not limited to a dilute liquid, a concentrated liquid, a more concentrated cream, a paste or a hydratable dry composition. Other possible forms may be solutions, lotions, creams, gels, aerosol and pump sprays, and impregnated towelettes. The composition may contain a variety of levels of the individual components. For example, a single application amount of the individual components of the composition may be determined. This amount may be administered as a single application or may be divided into multiple smaller applications dependent on the insect exposure and the individual. Where the composition is a liquid for oral application, for example, one squirt of a standard spray applicator may constitute one-fifth of a predetermined amount of the individual components, making five squirts the suitable application for an adult individual prior to insect exposure. Although dosage may vary, in certain embodiments a one fluid ounce spray applicator may contain enough liquid for about 250 sprays, making a 5-spray application about 1/50 of a fluid ounce.

The effective dosage of composition will depend upon a variety of factors known in the art, such as the body mass of the individual to whom the composition is administered, the relative sensitivities of different target insects to the composition and the length of exposure to insects. Where prolonged exposure may result in a decrease in efficacy, a repeated administration may be used.

Certain embodiments concern methods to minimize, inhibit and/or prevent insect bites. Other embodiments concern methods to treat a subject bitten by an insect. Such methods may comprise administering a composition suitable for oral and/or external application that includes at least one herbal compound combined with at least one vitamin compound. The composition may be administered in various forms as mentioned above. The amount of the individual components of the composition may be adjusted to provide an optimum insect inhibiting formulation, including a predetermined beneficial amount, such as several sprays for an adult subject and fewer for a young subject (e.g. an infant or child). The skilled artisan will realize that the disclosed methods include, but are not limited to administration to human subjects. However, subjects of interest may include humans, cats, dogs, horses, cows, goats, pigs, mammals and vertebrates in general. Where oral spray administration is inappropriate for administering to a particular species of mammal, alternative delivery methods may be utilized. For example, a standard dosage may be determined and mixed with a water and/or food supply for a subject animal. The skilled artisan will realize that with such administration the absorption of the composition may be affected by the type and/or amount of liquid or food ingested and dosages may be adjusted appropriately to compensate for reduced absorption.

In various embodiments, methods to treat subjects for insect bites may comprise oral and/or topical administration of a composition comprising at least one vitamin and at least one herb. The administration may be used to reduce, inhibit or eliminate localized swelling, itching, inflammation, redness and other reactions to insect bites.



The following embodiments relate to compositions that, in one aspect, inhibit insects from biting subjects following oral administration to the subjects. The compositions provide prolonged protection of subjects against biting insects. The subjects may be adult subjects, juvenile subjects and/or infant subjects. Because the compositions exhibit little or no toxicity, they may be administered to infant subjects to protect against biting insects, unlike present commercial insect repellants that are not recommended for use with infants.

Plants whose essential oils reportedly have purported insect repellent activity include citronella, cedar, verbena, pennyroyal, geranium, lavender, pine, cajeput, cinnamon, rosemary, basil, thyme, allspice, garlic, and peppermint. Unlike synthetic insect repellents, plant-derived insect repellents have been poorly studied. When tested, most of the essential oils yield short-lasting protection, lasting from a few minutes to as long as 2 hours. The use of plant derived materials as inhibitors of insect biting remains uncharacterized to date.

Embodiments relate to compositions and the use of these compositions as agents for the prevention and/or treatment of insect bites. The compositions may include combinations or sub-combinations of components derived from one or more vitamins such as thiamin (B-1), riboflavin (B-2), niacin (B-3), pantothenic acid (B-5), pyridoxine (B-6), folic acid (B-9), cyanocobalamin (B-12), choline, inositol, d-biotin, para-aminobenzoic acid, lecithin and one or more herbs such as peppermint, barley grass, lobelia, chlorella, watercress, alfalfa, parsley and rice bran. In one embodiment, the composition may comprise a suitable amount of all the herbs and all the vitamins mentioned.

In one embodiment, the composition is administered to an individual in need of treatment to reduce inflammation (e.g. orally administered and/or externally applied to an insect bite). In another embodiment, the composition may be administered to an individual to inhibit biting insects. In still another embodiment, the compositions may be administered to maintain a continuous protection against biting insects for a prolonged period (e.g. approximately 8 hours).

The following information is presented as general background information relevant to various herbs and vitamins. The herbs discussed below have been reported to have effects as naturopathic and/or homeopathic remedies for a variety of conditions. The skilled artisan will realize that such naturopathic and/or homeopathic uses may or may not be relevant to the compositions and methods disclosed herein for inhibition of biting insects and/or inflammation caused by insect bites.


Barley: Hordeum distichon (LINN.), Hordeum vulgare L.; Graminaceae

Action and Uses: Pearl Barley may be used for the preparation of a decoction which is a nutritive and demulcent drink in febrile conditions and in catarrhal affections of the respiratory and urinary organs. Barley water is used to dilute cows' milk for young infants, reportedly to prevent the formation of hard masses of curd in the stomach. Malt is produced from barley by a process of steeping and drying that develop a ferment `diatase` needed for the production of alcoholic malt liquors, but in the form of Malt Extract it is largely used in homeopathic medicine. Vinegar is an acid liquid produced by oxidation of fermented malt wort. Malt vinegar is the only vinegar that has been used medicinally. The parts of the barley plant usually used include grain and germinated seeds (barley sprouts). Reported properties include demulcent, digestant, carminative, nutritive.

Uses: A mucilaginous substance is obtained when hulled barley (pearl barley) is cooked. It is thought to be a good nutritional source for throat or stomach problems. The demulcent properties of cooked barley may be useful in external treatment of sores, fevers, diarrhea, gout, and tumors. Used as a tonic during convalescence. Barley water is a skin freshener, cleanses and softens skin. Drinking barley water is reported to clear and beautify the skin; sweeten with honey and orange juice.

Nutrient Content: Iron, sulfur, phosphorus, magnesium, niacin, protein, vitamin B1. Barley shoots are reportedly used to dry breast milk, treat food stagnation, weak stomach, weak digestion, loss of appetite, and hepatitis.

Warning: Barley should be avoided by nursing mothers.

Lobelia: Lobelia inflata (LINN.) Family: N.O. Lobeliaceae

Action and Uses: Some reported uses are as an expectorant, diaphoretic, and anti-asthmatic. It should not be employed as an emetic. Some reports indicate value as an expectorant in bronchitis or as a counterirritant when combined with other ingredients in ointment form. It is sometimes given in convulsive and inflammatory disorders such as epilepsy, tetanus, diphtheria and tonsilitis. It may also be used for relaxation purposes. It may also be used as an enema.

Externally, an infusion has been found useful in ophthalmia, and an ointment may be used as a local application for sprains, bruises, or skin diseases, alone, or in powder combined with other components. The oil of Lobelia is reportedly of use in treating tetanus. The oil may be useful as an expectorant, nauseant, sedative, and diaphoretic, when given every one or two hours. In excessive doses the effects may include depression, nausea, cold-sweats, and possibly death.

Other Species--L. Dortmanna is indigenous to Great Britain, and is similar in action to L. inflata. A dose of the fresh plant reportedly cures headaches and noises in the ears. L. Erinus. A dose of the plant has reportedly been used in cancer and has produced pain relief. It has also been used as to treat syphilis. LOBELIA, BLUE (L. Syphilitica) and LOBELIA RED (L. Cardinalia). Both of these are used in homeopathy. The first is diaphoretic, emetic and cathartic and has been used in dropsy, diarrhea, syphilis and dysentery, the root being the part used. The Red Lobelia is said to be anthelmintic, nervine and antispasmodic. L. Kalmit. is said to be used by the Indians in the cure of syphilis. L. purpurascens. also has reported homeopathic medicinal uses.

Watercress: Nasturtium officinale. Family: N.O. Cruciferae

Action and Uses: Watercress is reportedly of use for its antiscorbutic qualities and has been used as such from the earliest times. As a salad it supposedly promotes appetite. Watercress has also reportedly been used in tuberculosis. Its active components are said to be at their best when the plant is flowering. Reported properties include diuretic, expectorant, purgative, stimulant, stomach aid, and tonic.

Reportedly good for urinary bladder problems. Promotes kidney function and relieves fluid retention. Relieves indigestion and stops gas formation. Stimulates rate of metabolism and is taken as a spring tonic. Watercress has reportedly been recommended for use against gout, scurvy, mild digestive disturbances, anemia, and catarrh of the upper respiratory tract. Reportedly effective as an expectorant, it is also beneficial for tuberculosis, scurvy, anemia, and eczema. Its high vitamin C content makes it a good general preventative. Used as a post-partum (after childbirth) remedy to prevent infections. Having a slight iodine content, watercress is a dietary remedy for thyroid problems. In addition, the richness of its mineral, iron and iodine content stimulates glandular activity. Limited loss of hair caused by a fungus may be treated by an application of watercress juice. Leaf extracts are used clinically in India to correct vitamin deficiency.

Dosage: As an expressed juice; 1 to 2 fluid ounces.

Nutrient Content: Iodine, niacin, magnesium, manganese, phosphorus, sodium, iron, calcium, vitamins A, B1, B2, C, E and zinc.

Warning: Do not harvest leaves from polluted waters. Poisonings have resulted from eating leaves from plants growing in polluted waters, from which the plant has absorbed heavy metals and toxins. Excessive or prolonged use can lead to stomach upset and kidney problems. It should not be taken daily and no longer than 4 weeks even with interruptions. The juice should not be taken undiluted, because it can produce inflammations in the throat and stomach. Some doctors caution against use during pregnancy.

Parsley: Carum petroselinum (BENTH.) Family: N.O. Umbelliferae

Action and Uses: The leaves are extensively cultivated, not only for use fresh, but also for the purpose of being dried and powdered. In addition to the leaves, the stems are also dried and powdered. The roots of the turnip-rooted variety are used as a vegetable and flavoring. Two-year-old roots and dried leaves are employed for making Parsley Tea. The seeds are used for the extraction of an oil called Apiol. The best kind of seed for homeopathic or naturopathic medicinal purposes is that obtained from the Triple Moss curled variety.

The oleoresin of parsley has been reported to influence nerve centers of the head and spine, and in large doses may produces giddiness and deafness, decreased blood-pressure and slowing of the pulse and possibly paralysis. Parsley is reportedly used chiefly for its diuretic properties, a strong decoction of the root being used to treat the kidneys, (dropsy and jaundice). The dried leaves are also used for the same purpose.

A report in France indicated a popular remedy for scrofulous swellings is green Parsley and snails, pounded in a mortar to an ointment, spread on linen and applied daily. The bruised leaves, applied externally, have been used in a similar manner as Violet leaves (also Celandine, Clover and Comfrey), to treat tumors suspected to be of a pre-cancerous nature. It is also reported that this may be a remedy for the bites and stings of poisonous insects.

Peppermint: Mentha piperita (SM.). Family: N.O. Labiatae. Synonym--Brandy Mint.

Action and Uses: The parts of the herb used include the leaves, oil and flowering tops. Peppermint oil is the most extensively used of all the volatile oils. The anti-spasmodic action of the volatile oil is more marked than in any other oil, and is reported to relieve pains arising in the alimentary canal.

From its stimulating, stomachic and carminative properties, it is used in certain forms of dyspepsia, being mostly used for flatulence and colic. It may also be employed for other sudden pains and for cramp in the abdomen. Wide use has been made of Peppermint in cholera and diarrhea. May be used for chills, colic, fever, nausea, diarrhea, heart trouble, rheumatism, convulsions, spasms, dizziness, vomiting, travel sickness, dysentery, cholera, dysmenorrhea, palpitations of the heart, the grippe, hysteria, insomnia, neuralgia, and also reportedly used for headaches. Used for colds, flu, sore throat, laryngitis, gas and mild digestive disorders. The leaves can be made into a salve or a bath additive for itching skin conditions. Extracts have been used against herpes simplex, Newcastle disease, and other viruses. The oil reportedly stops spasms of smooth muscles. Externally, peppermint helps rheumatism, neuralgia, and headaches (e.g., migraines).

Reportedly, it is generally combined with other medicines when its stomach aiding effects are required, being also employed with purgatives to prevent griping. Oil of Peppermint reportedly alleviates sickness and nausea, and is used to disguise the taste of unpalatable drugs, as it imparts its aromatic characteristics to whatever prescription it enters into. It is also reportedly used as an infants' cordial. The oil itself is often combined with sugar and added to pills, also a spirit made from the oil, but the preparation in most general use is Peppermint Water, which is the oil and water distilled together.

Peppermint is reportedly used to assist in raising internal heat and inducing perspiration, although its strength is soon exhausted. In slight colds or early indications of disease, a free use of Peppermint tea may treat the disease onset. Peppermint tea is used also for palpitation of the heart. In cases of hysteria and nervous disorders, Peppermint was reported to be augmented by the addition of equal quantities of Wood Betony.

A single cup of peppermint tea, drunk in sips and as warm as possible, may be of use to treat for example queasiness, nausea, a feeling of fullness, or severe vomiting. Peppermint tea promotes bile flow, improves bile production in the liver, and also exercises a positive influence on pancreatic function. But, avoid peppermint if internal ulcers are present.

Warning: May interfere with iron absorption. Oil is toxic if taken internally in large doses; may cause dermatitis. Menthol, the major chemical component of peppermint oil, may cause allergic reactions. Avoid prolonged use of the essential oil as an inhalant. Mint should not be given to children for more than a week at a time without a break. It is advised not to give any form of mint directly to young babies. Also, peppermint may reduce milk flow if breast-feeding.

Alfalfa: Medicago sativa L. Leguminosae

Uses: Alfalfa tea is commonly used as a beverage. Nutritious fresh or dried leaf tea is reportedly used to promote appetite, for weight gain, as a diuretic, and reportedly stops bleeding. It is a source of commercial chlorophyll and carotene. It also contains the anti-oxidant tricin. Alfalfa has anti-fungal, and setrogenic activity. Unsubstantiated claims include use for cancer, diabetes, alcoholism, arthritis, etc. It is high in chlorophyll and nutrients. It is reported to alkalinize the body, as well as detoxify the body, especially the liver. It is reportedly used for colon disorders, anemia, hemorrhaging, indigestion, vitamin or mineral deficiency, laxative, cystitis, blood purifier, gas, edema, diabetes, ulcers, and arthritis. It may promote pituitary gland function. Effects include alterative, antipyretic, diuretic, appetite stimulant and hemostatic effects.

Nutrient Content: It contains biotin, calcium, choline, inositol, iron, magnesium, PABA, phosphorus, potassium, protein, sodium, sulfur, tryptophan (amino acid), and vitamins A, B complex, C, D, E, K, P, and U.

Warning: Alfalfa has been reported to aggravate lupus and other auto-immune disorders. Avoid alfalfa if an auto-immune problem exists. Consuming large quantities of Alfalfa saponins may cause breakdown of red blood cells, causing bloating in livestock (thus weight gain). Recent reports suggest that Alfalfa sprouts (or the canavanine, especially in the seeds), may be associated with lupus (systemic lupus erythematosus), causing recurrence in patients in which the disease had become dormant.

Rice Bran

Rice bran is a by-product of the milling of rice. It consists mostly of the bran layer and germ of the rice with some fragments of hull and broken rice. The calcium level in rice bran will vary with the amount of added calcium carbonate. When the amount of added calcium carbonate exceeds 3 percent (total calcium exceeds 1.2 percent), then the percentage of calcium carbonate must be stated in the product name. Rice bran is similar to oats in crude protein, fat, fiber and energy.

Rice Bran is a source of original B-complex in the outer layers of the rice grain. Vitamin B-complex is a source for strong, steady nerves and sustained energy. The B-complex has been reportedly used for cessation from aggravation. Rice Bran, being a very rich source of a balanced B-complex profile of vitamins, can be used to maintain normal blood sugar levels for those suffering from low blood sugar.


A genus of unicellular green algae, potentially a source of high-grade protein and B-complex vitamins. Any alga of the genus Chlorella. The name Chlorella derives from the Latin words meaning `leaf` (green) and `small`, referring to the unusually high content of chlorophyll (the highest of any known plant) that gives Chlorella its characteristic deep emerald-green color. This particular fresh-water, single celled microscopic plant contains a host of nutrients. In addition to chlorophyll it contains vitamins, minerals, dietary fiber, nucleic acids, amino acids, enzymes, CGF (Chlorella Growth Factor) and other substances. Under favorable growth conditions of strong sunlight, pure water and clean air, Chlorella multiplies at an incredible rate, the complete reproduction cycle taking less than 24 hours.

There are over 70,000 species of algae in the world. Chlorella Pyrensoida is one of the most common species found in watersheds. Chlorella contains the full Vitamin B Complex, Vitamins E & C and has a wide range of minerals, including magnesium, potassium, iron and calcium.

Uses. Reportedly of use for treatment of cancer. May increase production of T-cells and macrophages with activity against cancer. Chlorella has reportedly been shown to promote the production of interferon (IFN), which stimulates macrophage production. Chlorella may stimulate the activity of T-cells and macrophages by increasing IFN levels thus enhancing the immune system's ability to combat infection, cancer and other diseases.

Chlorella has the highest amounts of chlorophyll of any plant known. Chlorophyll is structurally similar to hemoglobin (found in red blood cells) except for containing magnesium instead of iron. Magnesium is essential for the heart to function properly. Chlorophyll has reportedly been used in the treatment of cardiac hypertension. Chlorophyll has also been used to treat anemia and reportedly stimulates the production of red blood cells in the body.

When eaten, Chlorella reportedly causes beneficial stomach bacteria (Lactobacillus) to multiply at four times the normal rate. This improves digestion and thus the body's ability to absorb nutrients.

Chlorella includes a fibrous, indigestible outer shell (20%) and inner nutrients (80%). It is the fibrous material that has been reported to bind with heavy metals and other toxins that may accumulate in the bodies. It is reported that a period of 3 6 months consumption of Chlorella may result in elimination of heavy metals and other toxins. Use of up to 15 20 grams of Chlorella per day has been reported.

Chlorella has been used for treatment of Alzheimer's Dementia and Attention Deficit Disorder. Alzheimer's patients have been demonstrated to have high levels of aluminum in their brains. Chlorella may assist in elimination of aluminum and may also improve oxygen transfer capabilities, aiding alertness and mental focus.

Chlorella has the ability to quadruple in quantity every 20 hours, which is an extraordinarily high growth rate. Exactly what CGF (Chorella growth factor) is remains a mystery. CGF has hormone-like qualities and appears to stimulate tissue repair. Chlorella has been used as a topical treatment for damaged tissue.

Poor diet, for example the consumption of excess carbonated soft drinks and processed sugars, may result in blood acidification. Chlorella is alkaline in nature any may help balance this acidity to maintain a neutral blood pH, optimally 7.4. Chlorella has a number of properties which are helpful to organs and tissues that have been injured by a variety of causes. It has been reported to promote liver health. Although some positive effects of taking Chlorella may be felt immediately, such as correcting constipation and bad breath, Chlorella's full nutritive and detoxifying capabilities often take 3 6 months to be fully appreciated. Chlorella belongs to a small group of foods that have been called Nutriceuticals.

Both Watershed Chlorella and Watershed spirulina are particular strains of algae. Watershed Chlorella is a strain of algae known as Chlorella Pyrensoida. From a single pure source, this algae has been reproduced for thousands of generations. Control of the genetic purity of Watershed Chlorella may provide beneficial effects on its nutritional and nutriceutical properties.

It has been reported that mice injected with cancer cells showed a higher resistance to this challenge if they had been fed Chlorella. Other tests reported that Chlorella growth factor improves resistance to abdominal tumors while increasing the number of immune cells in the abdominal cavity. Chlorella promotes cell reproduction, reduces cholesterol and increases hemoglobin levels. Because of its broad nutritional and detoxifying profile, Chlorella promotes the repair of bodily organs and tissues that have been injured or otherwise damaged.

Numerous research projects in the USA and Europe indicate that Chlorella can also aid the body in the breakdown of persistent hydrocarbon and metallic toxins such as DDT, PCB, mercury, cadmium and lead, while strengthening the immune system response. In Japan, interest in Chlorella has focused largely on its detoxifying properties, its ability to neutralize or remove poisonous substances from the body. The fibrous materials in Chlorella also improve digestion and promote the growth of beneficial aerobic bacteria in the stomach.

Analysis shows that Chlorella Pyrensoidosa contains a comparable variety of minerals, vitamins and amino acids to other algae: Sporopollenin, which is only present in Chlorella Pyrensoida, acts in the same detoxifying way. Chlorella's indigestible cell wall needs to be ruptured to allow access to its nutrients and a variety of methods are used, some of which damage the nutrients.

The method used herein by the Chlorella producer (TCMC) ensures the highest quality, which is confirmed by an annual independent analysis by the Japan Food Research Laboratory. Japan is the only country that has strict standards and importation controls over heavy metals and bacterial content in Chlorella. The digestibility of the Chlorella used is confirmed by the Japan Government's Ministry of Health to be between 76% and 79%, the highest on the market. Chlorella was analyzed by Dr L. Lewis, Doctor of Physiology at Duke University in 1992. Using a Scanning Electron Microscope (SEM), two samples of Chlorella were examined, the source used herein and a competitor's brand. Both were deemed to be free of contamination, however, the source of Chlorella used herein was the only one found to have a disrupted cell wall by SEM examination.

Additive: Potassium Sorbate

In certain embodiments, a preservative may be added to a composition of insect inhibitor to prevent growth of microorganisms and/or to maintain freshness. One example of a preservative is potassium sorbate.

Potassium sorbate is a potassium salt of sorbic acid, a polyunsaturated fat used to inhibit mold growth. Sorbic acid was first isolated from the oil of the unripened rowan berry (sorbapple or mountain ash berry) in 1959 by A. W. Hoffmann. Sorbic acid obtained its name from the scientific name for mountain ash (i.e. Sorbus aucuparia, Linne), the parent of the rowan berry. The value of sorbic acid, or its salts, was not immediately recognized. It was only much later that these compounds were appreciated for their ability to interfere with ATP metabolism in microbes, while posing no health risk when consumed by mammals. Sorbic acid is one of the most thoroughly tested food additives in history. It has been found to be non-toxic even when taken in large quantities, and breaks down in the body into water and carbon dioxide in the Kreb Cycle.

Herbal therapies may be considered a form of combination therapy. The collective effect of these agents typically results in reduced toxicity, and appearance of new and novel activities.


In various embodiments, the compositions disclosed herein comprise one or more vitamins. The following discussion provides general background information on vitamins.


Reportedly important in controlling fat and cholesterol buildup in the body; prevents fat from accumulating in the liver; facilitates the movement of fats in the cells; helps regulate the kidneys, liver and gallbladder; important for nerve transmission; helps improve memory.

Deficiency Symptoms: Reportedly a deficiency may result in cirrhosis and fatty degeneration of the liver, hardening of the arteries, heart problems, high blood pressure and hemorrhaging kidneys. Choline reportedly assists in controlling weight as well as cholesterol levels, keeping cell membranes healthy and in preventing gallstones. It is thought to be useful in the maintenance of the nervous system, assisting memory and learning, and may help to fight infections, including hepatitis and AIDS. Choline is reportedly needed for normal membrane structure and function.

Choline is the major precursor of betaine, and it is used by the kidneys to maintain water balance and by the liver as a source of methyl-groups for methionine formation. It is also used to produce the important neurotransmitter acetylcholine. It assists in nerve impulse transmission, gallbladder regulation, liver functions and lecithin production.

A deficiency of choline does not happen easily but if it is deficient it may lead to liver disease, raised cholesterol levels, high blood pressure as well as kidney problems. Choline deficiency may also manifest itself in the inability to digest fats, stunted growth and fatty buildup in the liver. Memory and brain function may also be impaired.

Dosage: The dosage indicated is the Recommended Dietary Allowance (RDA), but is the minimum required per day, to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. The dosage is relative to the amount of fats ingested in the diet, but for a guide: male 550 mg/per day and female 425 mg per day, although mega dose vitamin proponents use far higher dosages. More choline may be required during alcohol consumption, refined sugar consumption or taking large amounts of nicotinic acid.

Toxicity and Symptoms of High Intake: The maximum level of choline has been set for safety at 3.5 g/day. Taking too much choline could result in nausea, depression, and could trigger existing epilepsy. Hypotension, sweating, salivation and diarrhea have also been reported. Choline is recommended in the same dose as inositol and together with the B group vitamins as well as vitamin A and linoleic acid.

Vitamin B-1 (Thiamin)

Vitamin B-1 reportedly plays a role in the body's metabolic cycle for generating energy, aids in the digestion of carbohydrates and is important for the normal functioning of the nervous system, muscles and heart. It also stabilizes the appetite, promotes growth and good muscle tone.

Deficiency Symptoms: May lead to the loss of appetite, weakness and feeling tired, paralysis and nervous irritability, insomnia, loss of weight, aches and pains, mental depression and constipation, heart and gastrointestinal problems.

Vitamin B1 reportedly is used in many different body functions and deficiencies may have far reaching effects on the body. Yet very little of this vitamin is stored in the body, and depletion of this vitamin can happen within 14 days. Thiamin is also an essential nutrient, somebody suffering from beriberi, scarcely able to lift their head from their pillow, will respond quickly from injected thiamin, and will be on their feet within a matter of hours.

Vitamin B1 may enhance circulation, help with blood formation and the metabolism of carbohydrates. It is also needed for the health of the nervous system and is used in the biosynthesis of a number of cell constituents, including the neurotransmitter acetylcholine and gamma-aminobutyric acid (GABA). It is used in the manufacture of hydrochloric acid, and therefore plays a part in digestion.

It is also good for the brain and may help with depression and assist with memory and learning. In children it is required for growth and additionally it has shown some indication to alleviate arthritis, cataracts and aid in infertility.

Dosage: The Recommended Dietary Allowance (RDA) is the minimum required per day to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. For males: 1.4 mg per day and females: 1.0 mg per day, although 50 mg is usually used in supplementation.


Necessary for the formation of lecithin; aids in the breakdown of fats; helps reduce blood cholesterol; helps prevent thinning hair.

Deficiency Symptoms: May result in high blood cholesterol, constipation, eczema, or hair loss. Inositol is needed for health at the cellular level and a fair concentration is found in the lens of the human eye as well as the heart. Inositol plays an important part in the health of cell membranes especially the specialized cells in the brain, bone marrow, eyes and intestines. Inositol is said to promote healthy hair, hair growth, and helps in controlling estrogen levels and may assist in preventing breast lumps. It may also be of benefit in reducing blood cholesterol levels.

Dosage: The RDA is the minimum required to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. Supplementation is usually 100 mg per day

Toxicity and Symptoms of High Intake: No toxic effects known, but diarrhea has been noted with the intake of very high dosage of inositol.

Folic Acid (Vitamin B-9)

Folic acid, also known as Vitamin B9, is also referred to as folacin or folate. This vitamin can be manufactured by the body and stored in the liver. It is needed for DNA and RNA synthesis, essential to the formation of red blood cells by its action on the bone marrow; aids in amino acid metabolism.

Deficiency Symptoms: A deficiency of folic acid in an unborn baby may increase the risk of the baby being born with spina bifida and other serious defects of the nervous system. Deficiency of folic acid may lead to fatigue, acne, a sore tongue, cracking at the corners the mouth (same as deficiency of vitamin B2, vitamin B6 as well as iron). Long term deficiency may result in anemia and later in osteoporosis, as well as cancer of the bowel and cervix.

Folic acid is reportedly needed for DNA synthesis and cell growth and is important for red blood cell formation, energy production as well as the forming of amino acids. Folic acid is essential for creating heme, the iron containing substance in hemoglobin, crucial for oxygen transport. It is important for cell division and replication. It is also required for protein metabolism and in treating folic acid anemia. This nutrient may be effective in treating depression and anxiety. Folic acid is reportedly very important in the development of the nervous system of a developing fetus.

Dosage: The dosage (400 micrograms per day) is the Recommended Dietary Allowance (RDA). In the therapeutic use of this nutrient, the dosage is usually increased considerably.

Pregnant women are sometimes advised to take a small supplement of folic acid to help prevent spina bifida and other congenial nervous disorders, and it may also reduce the risk of toxemia in pregnancy, premature labor and hemorrhaging. It is also thought to enhance the production of milk after delivery. Sufferers of psoriasis may consider taking extra folic acid, people under stress or anyone consuming alcohol. Women on birth control pills or hormone replacement therapy may benefit from folic acid. Light, heat and storage for extended periods can destroy this vitamin. Localized deficiencies may exist for smokers, as low levels have been detected in the lungs of smokers.

Toxicity and Symptoms of High Intake: Those on medication for epilepsy should be careful with large amounts of folic acid, since it can change the functioning of such drugs. Too much folic acid may mask a Vitamin B12 deficiency. Regular high intake of folic acid may cause digestive upset, energy loss and insomnia. Folic acid is more effective when taken with the B group vitamins--especially vitamin B12 and vitamin B6. Vitamin C is also recommended.

Vitamin B5--Pantothenic Acid

Participates in the release of energy from carbohydrates, fats and protein, aids in the utilization of vitamins; improves the body's resistance to stress; helps in cell building and the development of the central nervous system; helps the adrenal glands, fights infections by building antibodies.

Deficiency Symptoms: May lead to skin abnormalities, retarded growth, dizzy spells, digestive disturbances, vomiting, restlessness, stomach stress, muscle cramps. Consequences of low levels include frequent infection, fatigue, abdominal pains, sleep disturbances and neurological disorders including numbness, paresthesia (abnormal sensation such as "burning feet" syndrome), muscle weakness and cramps are also possible indications that this nutrient is in short supply.

Vitamin B5 plays an important role in the secretion of hormones, such as cortisone. Pantothenic acid is also used in the release of energy as well as the metabolism of fat, protein and carbohydrates. It is used in the creation of lipids, neurotransmitters, steroid hormones and hemoglobin.

Dosage: Recommended dosage of 10 100 mg is indicated.

Toxicity and Symptoms of High Intake: Pantothenic acid does not appear to be toxic in high dosage, although diarrhea, digestive disturbances and water retention have been reported on dosage exceeding 10 g a day.

Vitamin B-2 (Riboflavin)

Necessary for carbohydrate, fat and protein metabolism; aids in the formation of antibodies and red blood cells; maintains cell respiration; needed for the maintenance of good vision, skin, nails & hair; alleviates eye fatigue; promotes general health.

Riboflavin is manufactured in the body by the intestinal flora and is easily absorbed, although very small quantities are stored, so there is a constant need for this vitamin. It is required by the body to use oxygen and for the metabolism of amino acids, fatty acids, and carbohydrates. Riboflavin is further needed to activate vitamin B6 (pyridoxine), helps to create niacin and assists the adrenal gland. It may be used for red blood cell formation, antibody production, cell respiration, and growth.

It eases watery eye fatigue and may be helpful in the prevention and treatment of cataracts. Vitamin B2 is required for the health of the mucus membranes in the digestive tract and helps with the absorption of iron and vitamin B6. Although it is needed for periods of rapid growth, it is also needed when protein intake is high.

Deficiency Symptoms: May result in itching and burning eyes; cracks and sores in the mouth and lips; bloodshot eyes; purplish tongue; dermatitis; retarded growth; digestive disturbances; trembling; and sluggishness. A shortage of this vitamin may manifest itself as eye disorders, inflammation of the mouth and tongue, and skin lesions. Dermatitis, dizziness, hair loss, insomnia, light sensitivity, poor digestion, retarded growth, and slow mental responses have also been reported. Burning feet can also be indicative of a shortage of B2.

Dosage: The RDA is the minimum that required per day to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. Male 1.6 mg per day and female 1.2 mg per day although 50 mg is mostly recommended for supplementation. Extra dosage might be needed when consuming alcohol, antibiotics, and birth control pills or doing strenuous exercise, under stress or on a calorie-restricted diet.

Toxicity and Symptoms of High Intake: The limited capacity to absorb orally administered riboflavin precludes its potential for harm. Riboflavin intake of many times the RDA is without demonstrable toxicity. A yellow discoloration of the urine is seen with an increased intake of this vitamin.

Niacinamide (Niacin--Vitamin B-3)

Niacin is derived from two compounds--nicotinic acid and niacinamide. It improves circulation and reduces the cholesterol level in the blood; maintains the nervous system; helps metabolize protein, sugar and fat; reduces high blood pressure; increases energy through proper utilization of food; prevents pellagra; helps maintain a healthy skin, tongue and digestive system.

Vitamin B3 is required for cell respiration, helps in the release of energy and metabolism of carbohydrates, fats, and proteins, proper circulation and healthy skin, functioning of the nervous system, and normal secretion of bile and stomach fluids. It is used in the synthesis of sex hormones, treating schizophrenia and other mental illnesses, and as a memory-enhancer.

Nicotinic acid (but not nicotinamide) given in drug dosage reportedly improves the blood cholesterol profile, and has been used to clear the body of organic poisons, such as certain insecticides. People report more mental alertness when this vitamin is in sufficient supply. Niacin is best taken with the B group vitamins and vitamin C.

Deficiency Symptoms: May result in pellagra, gastrointestinal disturbance, nervousness, headaches, fatigue, mental depression, vague aches and pains, irritability, loss of appetite, insomnia, skin disorders, muscular weakness, indigestion, and canker sores.

Dosage: The RDA is the minimum that required per day to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. Male 18 mg per day and female 13 mg per day although 100 mg is mostly used in supplementation.

Large doses given to lower cholesterol may produce hyperuricemia, and hepatic abnormalities. These effects are reversed if the drug is reduced in amount or discontinued. People with diabetes, glaucoma, any liver disease or peptic ulcers should be careful of niacin supplementation. Your daily cup of coffee also provides about 3 milligrams of niacin

Toxicity and Symptoms of High Intake: Nicotinic acid, but not nicotinamide in doses larger than 200 mg causes flushing by dilating the blood vessels, which can also cause the blood pressure to drop. These flushes are normally harmless. Large dosages can also cause itching, elevated blood glucose, peptic ulcers and liver damage.

Vitamin B-6 (Pyridoxine)

Necessary for the synthesis and breakdown of amino acids; aids in fat and carbohydrate metabolism; aids in the formation of antibodies; maintains the central nervous system; aids in the removal of excess fluid of premenstrual women; promotes healthy skin; reduces muscle spasms, leg cramps, hand numbness, nausea & stiffness of hands; helps maintain a proper balance of sodium & phosphorous in the body.

Pyridoxine is required for the balancing of hormonal changes in women as well as assisting the immune system and the growth of new cells. It is also used in the processing and metabolism of proteins, fats and carbohydrates. Pyridoxine reportedly may also be of benefit for children with learning difficulties, as well as assisting in the prevention of dandruff, eczema and psoriasis.

Pyridoxine should be taken together with the entire B group vitamins, and in supplementation the quantity of B6 should be nearly the same as B2, as the B2 is needed to activate the Pyridoxine. Vitamin C, magnesium, sodium, potassium, zinc, linoleic acid and fatty acids may also be used in combination.

Deficiency Symptoms: May result in nervousness, insomnia, skin eruptions, loss of muscular control, anemia, mouth disorders, muscular weakness, dermatitis, arm and leg cramps, loss of hair, slow learning, and water retention. Irritability, nervousness and insomnia as well as general weakness, skin changes such as dermatitis and acne as well as asthma and allergies might develop when pyridoxine is in short supply. Symptoms may include nails that are ridged, an inflamed tongue as well as changes to bones--which can include osteoporosis and arthritis. Kidney stones may also appear. Women in particular may suffer from premenstrual fluid retention, severe period pains, emotional PMS symptoms, premenstrual acne and nausea in early pregnancy. Mood swings, depression as well as loss of sexual drive is sometimes noted when pyridoxine is in short supply and the person is on hormone replacement therapy or on birth control pills. Symptoms will be very much like those of B2 and B3 deficiency. Vitamin B6 is needed by the body to manufacture its own B3 vitamin.

Dosage: The RDA is the minimum that required per day to ward off serious deficiency of this particular nutrient. In the therapeutic use of this nutrient, the dosage is usually increased considerably, but the toxicity level must be kept in mind. Males 2 mg per day and females 2 mg per day. More may be required if taking antidepressants, contraceptive pills or on hormone replacement therapy. As this vitamin is readily lost in the urine, it must be taken regularly to ensure an adequate amount in the body. A very high protein diet, alcohol use, or allergies to MSG (mono sodium glutamate) and/or tartrazine may also indicate a need for increased vitamin B6 intake.

Toxicity and Symptoms of High Intake: Supplementation should be controlled as extreme dosage, such as in excess of 2,000 mg per day, may cause neurological damage. People on medication for Parkinson's disease should be careful about taking Vitamin B6 as it can inactivate L-dopa. People taking pyridoxine late at night sometimes experience very vivid dreams.


Aids in the utilization of protein, folic acid, Pantothenic acid, and Vitamin B-12. Biotin is used in cell growth, the production of fatty acids, metabolism of fats, and proteins. It plays a role in the Kreb cycle, which is the process in which energy is released from food. Biotin is also indicated for healthy hair and skin, sweat glands, nerve tissue, bone marrow, and assisting with muscle pain. Biotin also helps with the transfer of carbon dioxide. Biotin is useful for maintaining a steady blood sugar level.

Biotin should be taken with the B-group vitamins, but Vitamin C, Vitamin B5 (pantothenic acid), Vitamin B12 and sulfur are good adjuvants. Biotin is sometimes added to the diet of a patient suffering from alopecia, to help with severe hair loss.

Deficiency Symptoms: May lead to extreme exhaustion, drowsiness, muscle pain, loss of appetite, depression, grayish skin color. Although a shortage of Biotin is rare, it can happen and may result in dry scaly skin, fatigue, nausea and vomiting, mental depression as well as tongue inflammation and high cholesterol.

Dosage: Recommended dosage for adults 300 microgram (0.3 mg) per day and pregnant and lactating women 300 microgram (0.3 mg) per day. Bodybuilders and athletes consuming raw eggs should be careful of not running into a biotin shortage, since raw eggs contain avidin, which binds with the biotin, making it impossible absorb by the body. Long-term use of antibiotics may also decrease the availability of biotin.

Biotin is present in cheese, beef liver, cauliflower, eggs, mushrooms, chicken breasts, salmon, spinach, brewer's yeast, nuts and can be manufactured in the body should a small shortfall occur.

Toxicity and Symptoms of High Intake: No toxic levels are known, as excesses are easily lost in the urine and feces. No side effects are known.

Vitamin B-12 (Cyanocobalamin)

Helps in the formation and regeneration of red blood cells, thus helping prevent anemia; necessary for carbohydrate, fat and protein metabolism; maintains a healthy nervous system; promotes growth in children; increases energy; needed for calcium absorption.

This complex structured compound with its cobalt cofactor is needed in the body in very small amounts. Vitamin B12 is reportedly needed in the manufacture and maintenance of red blood cells. It reportedly stimulates appetite, promotes growth and release of energy. It is often used with older people to give an energy boost, assist in preventing mental deterioration and helps with thought processes. It may aid with clearing up infections and providing protection against allergies and cancer. This vitamin is also used in the metabolism of fats, proteins and carbohydrates.

Deficiency Symptoms: May lead to pernicious anemia, poor appetite, growth failure in children, tiredness, brain damage, nervousness, neuritis, degeneration of spinal cord, depression, lack of balance. Some symptoms of a deficiency include a sore tongue, weakness, fatigue, and weight loss, back pain and apathy. It may further result in loss of balance, decreased reflexes, tingling of the fingers, ringing in the ears etc. A deficiency may also result in the raising of the level of homocysteine in the blood which in high doses can be toxic to the brain, which may be involved in Alzheimer disease. Severe deficiency may result in pernicious anemia, also called Addisonian pernicious anemia. Another problem that appears in deficiency is the eroding of the myelin sheath--the fatty sheath of tissue, which insulates the nerve fibers.

Dosage: The RDA for males and females is 3 .mu.g per day. People on strict vegetarian and macrobiotic diets are often deficient on Vitamin B12. Some individuals exhibit a deficiency in absorption of vitamin B12 from the intestinal tract, which can lead to pernicious (destructive) anemia. Alcohol consumption or regular use of laxatives or antacids may also result in low B12 levels. Older people may require higher levels of this vitamin as many people older than sixty have difficulty extracting the vitamin from ingested food.

Vitamin B12 is not manufactured by any plants, and is only found in animal products. Therefore, a deficiency may result from strict all-vegetable diets. Unlike other water-soluble vitamins, B12 needs some 3 hours to be absorbed where other B vitamins are absorbed nearly immediately.

Toxicity and Symptoms of High Intake: Toxicity not established but vitamin B12 injections may result in skin problems if in large excess, but will normalize once the injections are stopped.

PABA (Para Amino Benzoic Acid)

Aids beneficial bacteria in producing folic acid; aids in the formation of red blood cells; contains sun screening properties; aids in the assimilation of Pantothenic acid. Para-aminobenzoic acid is often thought of as only an ingredient used in sunscreens, while it is actually also a nutritional ingredient. Since it is a moiety of PGA, a form of folic acid, some health professionals do not consider it a vitamin, but only a B-complex factor.

PABA is used to improve protein use in the body, it assists in red blood cell formation as well as manufacturing folic acid in the intestines. Para-aminobenzoic acid is used in sunscreen preparations since it can help protect the skin against ultra-violet radiation.

People suffering from vitiligo, over-pigmentation of skin, or without pigment in some spots, have reported an improvement of the skin after more PABA was ingested. PABA also assists with breaking down of protein and maintaining intestinal flora.

Deficiency Symptoms: May cause extreme fatigue, eczema, irritability, nervousness, constipation, headaches, digestive disorders, or hair turning prematurely gray. When PABA is in short supply fatigue, irritability, and depression might manifest. Weeping eczema has also been noted in people with PABA deficiency as well as patchy areas on the skin.

Dosage: No recommended dosage but 50 mg per day is usually used in supplementation. Long term antibiotic use may require more PABA from the body, but PABA may interfere with the effectiveness of sulfa drugs.

Toxicity and Symptoms of High Intake: When higher than factor (SPF) 8 sunscreens are used, the manufacture of vitamin D in the body may be reduced. Nausea, skin rashes and vomiting might be indicative of PABA taken in excess. Excessive levels of PABA are stored in the body and may cause liver damage. A ban was placed on the sale of OTC supplements containing large single doses of PABA.


Lecithin contains Choline and Inositol that are reportedly essential for the breakdown of fats and cholesterol. It may prevent arterial congestion, help distribute bodyweight, increase immunity to virus infections, clean the liver and purify the kidneys.

Lecithin is a phospholipid. It is produced daily within the liver if the diet is adequate. It is needed by every cell in the body and largely makes up cell membranes, where it increases membrane fluidity. This makes it ideal in preventing arteriosclerosis and assisting in protecting against cardiovascular disease.

Lecithin protects cells from oxidation, and helps make up the protective sheaths surrounding the brain. Using lecithin can improve brain function and has also been known to promote energy. Lecithin aids in the absorption of thiamine by the liver and is needed to help repair the damage to the liver caused by alcoholism.

Although it is a fatty substance, it is also a fat emulsifier. Lecithin enables fats, such as cholesterol, to be dispersed in water and removed from the body. Hence, it also supports the circulatory system by preventing fatty buildup in the arteries and vital organs.

Oral Application

In preferred embodiments, the disclosed compositions are delivered by oral administration. Oral spray is approximately five times faster and more efficient than capsules, pills or tablets. Intra-oral sprays are one of the fastest ways to deliver any drug, nutrient or vitamin into the bloodstream. There is no waiting for them to take effect. In pill form the body will only process a small fraction of the pill, perhaps as low as 10%. The digestive tract will reduce as much as 90% of the pills effectiveness before it is finally absorbed into the bloodstream. Using intra-oral sprays the nutrients are delivered into the bloodstream very rapidly. In certain embodiments, the disclosed compositions may be delivered to a subject intra-orally using delivery by a spray bottle.


One problem with using an intra-oral spray may be the taste of the composition. In one embodiment, peppermint may be used in sufficient amount to mask the flavor of other components of the composition. In other embodiments, other flavor additives for example fruit flavorings or other mint flavorings may be used. In another embodiment, the flavor of a composition may be one palatable to a mammal other than a human such as a dog or cat. These embodiments by no means limit the flavor options of any of the compositions. In other embodiments, the flavor component may be eliminated if the composition is intended for topical application.

Other than human subjects, other mammals may benefit from the effects of an orally delivered insect inhibiting composition. For example, diseases carried by mosquitoes may also affect dogs, cats, horses or birds etc. In one embodiment, a composition may be applied to a household pet prior to exposure to insects. In another embodiment, a composition may be applied to a dog prior to exposure to a species of flea, tick and/or flying insect (e.g. mosquitoes). In yet another embodiment, a composition may be applied to the oral cavity of a dog, cat, horse or bird. In still another embodiment, a composition may be applied orally and/or externally to a horse for inhibiting mosquitoes or flies (e.g. bottle or deer flies).

A composition comprising one or more of the herbs and vitamins disclosed herein may take many forms. These forms include, a portion, including the entire portion of the amounts recommended for inhibiting biting insects. Suitable forms include but are not limited to liquids and lotions. In addition, the composition may take the form of a portion of a predetermined amount such a quarter or a fifth. For example, a liquid formula may require 4 squirts of the liquid of a quarter strength formula for one individual or five squirts for another individual depending on the age and size of the individual. Alternatively, the composition may be in the form of powder-like consistency that can be hydrated and then used as an insect inhibitor. It is to be appreciated that in these other forms (e.g., paste, time-release formula, tablet etc.), the composition may constitute the entire portion of a predetermined amount of the components or a smaller portion of such predetermined amount.

Claim 1 of 9 Claims

1. A composition comprising: peppermint; barley grass; lobelia; chlorella; watercress; alfalfa; parsley; rice bran; thiamin (B-1); riboflavin (B-2); niacin (B-3); pantothenic acid (B-5); pyridoxine (B-6); folic acid (B-9); cyanocobalamin (B-12); choline; inositol; d-biotin; para-aminobenzoic acid; and lecithin wherein said composition inhibits insects from biting a subject after oral administration of the composition to the subject.

If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.



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