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Title: Sleep inducing
toothpaste made with natural herbs and a natural hormone
United States Patent: 6,998,112
Issued: February 14, 2006
Inventors: Zuckerman; Arthur (614 Second
Ave., Suite D, New York, NY 10016)
Appl. No.: 391004
Filed: March 18, 2003
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Covidien Pharmaceuticals Outsourcing
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Abstract
A toothpaste composition for inducing
sleep while simultaneously promoting intraoral cleanliness, which includes
toothpaste base ingredients and at least one sleep-inducing natural herb
or hormone. The sleep-inducing natural herbs and hormone are selected from
the group consisting of Chamomile, Lemon Balm, Passion Flower, and
Valerian, and the hormone Melatonin. The sleep-inducing natural herbs are
in a range of 0.25% to 18% by weight of the composition.
Description of the Invention
FIELD OF THE
INVENTION
The following natural herbs and natural
hormone in combination with toothpaste is used at night to improve sleep.
The expected dose of toothpaste is calculated at 2 grams. The ingredients
have been assessed for range of daily dose for best effects, toxicity in
normal range, recommended proportion of each, and water solubility of key
constituents.
BACKGROUND OF THE
INVENTION
It is an object of the present invention
to provide a sleep-inducing toothpaste or mouth spray which includes
sleep-inducing natural herbs and a natural hormone.
It is a further object of the present invention to provide a
sleep-inducing toothpaste which includes toothpaste base ingredients and
natural herbs being Chamomile, Lemon Balm, Passion Flower, Valerian and
the natural hormone Melatonin.
SUMMARY OF THE
INVENTION
A toothpaste composition is provided for
inducing sleep while simultaneously promoting intraoral cleanliness, which
includes toothpaste base ingredients and at least one sleep-inducing
natural herb or hormone. The sleep-inducing natural herbs and hormone are
selected from the group consisting of the natural herbs Chamomile, Lemon
Balm, Passion Flower, and Valerian, and the natural hormone Melatonin. The
sleep-inducing natural herbs are in a range of 0.25% to 18% by weight of
the composition, which may be in the form of a dental cream or mouth
spray.
DESCRIPTION OF THE
PREFERRED EMBODIMENTS
The toothpaste composition has base
ingredients which comprise a combination of known amounts of: Vegetable
Glycerin; Sorbitol; Hydrated Silica; Purified Water; Xylitol; Carrageenan;
Sodium Lauryl Sulfate; Titanium Dioxide; Propylparaben; Methylparaben;
Sodium Benzoate; and a flavoring agent.
The sleep-inducing natural herbs include the following:
A) Name: Chamomile, Camomile
Scientific Name: Matricaria recutita, Matricaria chamomilla
(German), Anthemis nobilis (Roman)
Chamomile comprises substantially ½ to 3% by weight of the toothpaste
composition and preferably comprises substantially 1% by weight of the
composition.
Chamomile, a member of the daisy family, is native to Europe and western
Asia. German chamomile is the most commonly used. German Chamomile is a
Southern European annual plant found wild along roadsides, in fields, and
cultivated in gardens. It is chiefly grown for commerce in Egypt.
Roman chamomile is a low European perennial found in dry fields and around
gardens and cultivated grounds, cultivated in Eastern Europe.
Parts Used: Flowers. Roman flowers are hollow while Matricaria
flowers are solid.
In the proposed toothpaste chamomile has potential for the treatment of:
Canker sores (mouth ulcers)
Gingivitis (periodontal disease)
Daily Dose Range for Prime Efficacy:
2-4 grams of the ground, dried herb in capsules or tablets, 1-3 times a
day.
1:5 tincture: 5-15 ml, 1-3 times per day, best between or before meals or
at bedtime.
1:2 tincture: 3-6 ml, prn, h.s.
1% of a 1:2 extract. Its presence is important but the desired effect
(sleep) will depend on substantial concentrations of two other strong
sedatives, Valerian and Passionflower, synergistically supported by
adequate amounts of the rest.
Safety and Toxicity in Recommended Dosage Range:
Though extremely rare, allergic reactions to chamomile have been reported.
These reactions have included bronchial constriction with internal use and
allergic skin reactions with topical use.
FDA lists chamomile as generally regarded as safe. There is no restriction
on long term use. It is given in material doses and as a homeopathic
preparation to teething babies.
Active Compounds:
The flowers of chamomile provide 0.5-1.5% volatile oils containing (-)
alpha-bisabolol, alpha-bisabolol oxides A & B, and matricine (usually
converted to chamazulene by water and heat, i.e. steam distillation or
make a tea).
Other active constituents include the bioflavonoids apigenin, luteolin,
and quercitin (0.5-3%). Apigenin is one of several constituents
hypothesized to create mild sedative effects observed in animal
experiments (Mills and Bone p322).
The European Pharmacopoeia recommends 4 ml/kg or more of blue essential
oil. These active ingredients contribute to chamomile's anti-inflammatory,
antispasmodic, and smooth muscle-relaxing effects, particularly in the
gastrointestinal tract.
History:
Chamomile has been used for centuries as a medicinal plant, mostly for
gastrointestinal complaints though it has therapeutic value in a wide
variety of conditions. It is used in various parts of the world as a
beverage tea. Chamomile is used in many nervous diseases, and is a gentle
hypnotic (aids in falling asleep). As a mild sedative and emmenagogue it
is used to regulate painful periods.
B) Name: Lemon Balm
Scientific Name: Melissa officinalis
Family: Lamiacease, the Mint Family
Parts used: Herb, leaves, volatile oil and polyphenols.
Lemon Balm comprises substantially ½ to 3% by weight of the toothpaste
composition and preferably comprises substantially 1% by weight of the
composition.
In the proposed toothpaste lemon balm has potential for the treatment of:
insomnia
headaches
restlessness
toothache
viral sores
minor digestive spasm
Daily Dose Range for Prime Efficacy:
2-3 grams of the ground, dried herb in capsules or tablets, 1-3 times a
day.
1:5 tincture: 2-6 ml, 1-3 times per day, best between or before means or
one daily dose at bedtime.
1:2 tincture: 1-3 ml, as needed, or one daily dose at bedtime.
Tea: 1 ounce of leaves, stems, flowers to a pint of water. Boil water,
pour over herb, steep 5 to 10 minutes, drink 1-2 cups or more per day.
Recommended Percent in Toothpaste Formula: 1% due to Lemon Balm's potent
flavor and its mild sedative properties. When bruised, the aerial parts
smell like lemon and mint. Fresh plant material may be used if it meets
pharmacopoeia standards when a sample is dried.
Safety and Toxicity in Recommended Dosage Range:
No restrictions for ingestion or topical use are found.
US: Generally recognized as safe
UK: General sales list
Canada: approved as an over-the-counter drug
France: Traditional Medicine
Germany: Commission E approved as an over the counter drug.
Active Compounds:
Essential oil 0.06-0.375% with monoterpene aldehydes geranial & neral (Citral
a & b), citronellal
Flavonoids apigenin, luteolin, kaempferol, quercetin
Glycosides
Up to 4% rosmarinic acid, anti-inflammatory and antioxidant
Ursolic, oleanolic acids
Sedative effects long appreciated in folk medicine have been confirmed
only in animal experiments using water/alcohol extracts given by
injection.
C) Name: Passion Flower
Scientific Name: Passiflora incarnata
Family: Passifloraceae
Parts Used: The leaves, stems, and flower before the vine fruits.
In the proposed toothpaste Passionflower has potential for the treatment
of:
Insomnia
Muscle spasm
Pain
Emotional upset
Viral sores
Passion Flower comprises substantially 1 to 4% by weight of the toothpaste
composition and preferably comprises substantially 2% by weight of the
composition.
Passion flower has a depressant effect on the Central Nervous System. The
herb is used for its sedative properties, to lower blood pressure, and
prevent tachycarduia. The alkaloid and flavonoids have both been reported
to have sedative activity in animals.
Many of the flavonoids, such as apigenin, are well-known for
pharmacological activity, particularly anti-spasmodic and
anti-inflammatory activities. It is the herb of choice for treating
intransigent insomnia.
Daily Dose Range for Prime Efficacy:
2-4 grams of the ground, dried herb in capsules or tablets, 1-3 times a
day.
1:5 tincture: 6-12 ml, 1-3 times per day, or one daily dose all at
bedtime.
1:2 tincture: 2-4 ml, as needed, or one daily dose all at bedtime.
Recommended Percent in Toothpaste Formula: 2%
Safety and Toxicity in Recommended Dosage Range:
Passion flower is generally safe and has not been found to negatively
interact with other sedative drugs. The American Botanical Safety Handbook
lists Passion Flower as category 1-no restrictions.
Active Compounds:
Alkaloids: harmine, harman, harmol, harmaline, harmalol, and passaflorine.
No less than 8% flavonoids: apigenin and various glycosides, homo-orientin,
isovitexin, kaempferol, luteolin, orientin, quercitin, rutin, saponaretin,
saponarin and vitexin. The flavonoids in passion flower are the primary
constituents responsible for its relaxing and anti-anxiety effects.
D) Name: Valerian
Scientific Name: Valeriana officinalis
Family: Valerianaceae
Parts Used: Root and rhizome.
In the proposed toothpaste Valerian has potential for the treatment of:
Insomnia
Pain
Blood Pressure
Valerian comprises substantially 3 to 6% by weight of the toothpaste
composition and preferably comprises substantially 4% by weight of the
composition.
Daily Dose Range for Prime Efficacy:
A wide range experimentally and in clinical trials exists, from a minimum
of 60-120 mg per dose up to 300-500 mg of the ground, dried herb in
capsules or tablets, 1-3 times a day or one daily dose 1 hour before
bedtime.
Recommended Percent in Toothpaste Formula: 4% This amount reflects this
herb's primacy in an oral, water-extracted, herbal formula designed for
helping sleep.
Safety and Toxicity in Recommended Dosage Range:
No adverse effects are expected when taken within recommended dosage
ranges. The FDA lists valerian as generally safe.
Valerian has a long history of exceptional safety, which has been
confirmed by clinical studies.
Active Compounds:
0.35-1% essential oils (not less than 5 ml/kg) including monoterpenes (borneol),
sesquiterpenes (beta-bisabolene, valerenal in fresh root), esters of
valerianic, isovalerianic acid Iridoids, 0.5%-2%, a.k.a. valepotriates and
decomposition products including valtrate, isovlatrate, dihidrovaltrate,
acevaltrate
Valerenic acid, its derivatives
Aminos, lignans
The essential oil (aroma and flavor) contribute perhaps ⅓ to the sedating
properties of the herb. Many constituents are thought to synergize for its
sedative effects. Central nervous system sedation is regulated by
receptors in the brain known as GABA-A receptors. Valerian weakly binds to
these receptors for a sedating effect.
Clinical studies have shown that people taking valerian had shown
significantly improved sleep quality without morning grogginess. Some
researchers have compared valerian to benzodiazepines such as Valium (to
which it bears no relation, either etymologically or as a source for drug
development). However, valerian is a much milder and safer sedative.
Unlike Valium, valerian is not addictive or does not promote dependency.
Valerian's sedative effect is not significantly exaggerated by alcohol and
barbiturates, unlike Valium. Valerian extract at a dose of 50 to 100 mg
taken two or three times daily has been shown to relieve performance
anxiety and the stress of driving in heavy traffic. Larger doses of
valerian extract may be necessary for patients who have been using
benzodiazepine prescriptions for anxiety.
E) Name: Melatonin
The chemical symbol for the natural hormone Melatonin is: ##STR1##
In the proposed toothpaste has potential for the treatment of:
Sleep disorders
Daily Dose Range for Prime Efficacy:
1 to 20 mg; thirty minutes before retiring. For sleeplessness due to low
melatonin, the dosage range is 2-10 mg. The lower dose may be taken for at
least three days, then gradually increased by 1-2 mg every three nights up
to 15 mg if results are not what expected. Higher doses, 20 mg up to 50
mg, have been used for patients on chemotherapy.
Recommended Percent in Toothpaste Formula:
Melatonin comprises substantially 0.25% to 2% by weight of the toothpaste
composition and preferably comprises substantially 0.50% by weight of the
composition.
Percent depends on milligrams one dose of toothpaste can provide. The more
there is the better the change that some will be absorbed orally. In a 2
gram dose of toothpaste 10 mg of melatonin may be the upper limit that can
be accommodated. Though this may be effective as much as possible, up to
20 mg, is recommended since toothpaste isn't swallowed.
Safety and Toxicity in Recommended Dosage Range:
No toxicity is expected though studies of melatonin's safety are limited,
with isolated reports of exacerbation of depression and fatigue.
History:
Melatonin has been called the body's own natural sleeping pill. It plays a
key role in the sleep cycle by helping one fall asleep. Low melatonin
levels can cause sleep-onset insomnia. The body changes serotonin into
melatonin, a hormone stored in the pineal gland. The pineal releases
melatonin only when the level of light is low. For most people melatonin
is secreted only at night, during sleep unless lights are left on. The
presence of light is a sign to the brain to shut down melatonin
production.
A latitude of modification, change, and substitution is intended in the
foregoing disclosure, and in some instances, some features of the
invention will be employed without a corresponding use of other features.
Accordingly, it is appropriate that the appended claims be construed
broadly and in a manner consistent with the spirit and scope of the
invention herein.
Claim 1 of 4 Claims
1. A toothpaste for inducing
sleep while simultaneously promoting intraoral cleanliness, comprising:
a) a combination of sleep-inducing herbs comprising:
i) ½ to 3 percent by weight chamomile;
ii) ½ to 3 percent by weight lemon balm;
iii) 1 to 4 percent by weight passion flower;
iv) 3 to 6 percent by weight valerian; and
b) 0.25 to 2 percent by weight melatonin;
wherein all percentages are based on the weight of the toothpaste
composition.
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