WO2016120844A1 - Energizing mixture, particulary on sexual level - Google Patents

Energizing mixture, particulary on sexual level Download PDF

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Publication number
WO2016120844A1
WO2016120844A1 PCT/IB2016/050468 IB2016050468W WO2016120844A1 WO 2016120844 A1 WO2016120844 A1 WO 2016120844A1 IB 2016050468 W IB2016050468 W IB 2016050468W WO 2016120844 A1 WO2016120844 A1 WO 2016120844A1
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Prior art keywords
plant extract
mixture
weight
evaluated
total weight
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PCT/IB2016/050468
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French (fr)
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Giovanni Ferrari
Francesco Palladini
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Giovanni Ferrari
Francesco Palladini
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Publication of WO2016120844A1 publication Critical patent/WO2016120844A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/889Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/29Berberidaceae (Barberry family), e.g. barberry, cohosh or mayapple
    • A61K36/296Epimedium
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/31Brassicaceae or Cruciferae (Mustard family), e.g. broccoli, cabbage or kohlrabi
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/77Sapindaceae (Soapberry family), e.g. lychee or soapberry
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence

Definitions

  • the present invention relates to an energizing mixture, particularly on sexual level.
  • erectile dysfunction understood as the inability of a man to attain and/or maintain an erection adequate to conduct satisfactory sexual intercourse, is a disorder that affects millions of men worldwide.
  • Erection in fact, is a physiological process involving different psychological, neurological, vascular and hormonal aspects and many, therefore, are the factors that may affect the normal erectile function.
  • Some therapies act on the causes of the dysfunction of a psychological, behavioral or relational nature, and may provide for a simple dialectic confrontation, activities of recovery of bodily sensory perceptions, activities of recovery of couple communication, or even the targeted intervention of a specialized psychologist.
  • erectile supporting drugs include the oral intake of erectile supporting drugs, among the most known and used being sildenafil (Viagra®) and yohimbine (Yohimbine®, Yocon® and others).
  • the main aim of the present invention is to provide an energizing mixture, particularly on sexual level which allows to overcome the drawbacks and contraindications of use normally present in traditional treatments.
  • Another object of the present invention is to provide an energizing mixture, particularly on sexual level, which is usable in the presence of energy deficits, as revitalizing product and with a protective effect on the vascular and nervous level.
  • a further object of the present invention is to provide an energizing mixture, particularly on sexual level, that is usable by men of all ages without any limitation of use, even by elderly people.
  • Another object of the present invention is to provide an energizing mixture, particularly on sexual level, which allows to overcome the mentioned drawbacks of the prior art within the ambit of a simple, rational, easy and effective to use as well as affordable solution.
  • an energizing mixture particularly on sexual level, usable e.g. by a person who has energy deficiencies, as a revitalizing product with protective functions at vascular and nervous level and which allows both achieving a normal physiological penis erection process, and maintaining this physiological process for a time interval long enough to conduct satisfactory sexual intercourse.
  • the mixture comprises a first plant extract obtained from Epimedium sagittatum, a second plant extract obtained from Tribulus terrestris and at least a policosanol.
  • the first plant extract contains flavonoids, polysaccharides with organic activity and Vitamin C.
  • the flavonoids comprise Icariin (C33H 4 oOi5) which is the primary active component of Epimedium sagittatum extracts.
  • Icariin due to its chemical structure shown hereunder, has an antioxidant, neuroprotective, osteoprotective and cardio-protective action, protecting the cells of the different tissues from damage induced by reactive oxygen species (ROS).
  • ROS reactive oxygen species
  • the antioxidant activity of Icariin results in an improvement of the peripheral blood flow, thanks to the protective action of endothelium against reactive oxygen species with positive effects in the treatment of erectile dysfunction. This activity is attributed to two different mechanisms.
  • the first is a nervous type mechanism whereby the Icariin can lead to an improvement in the peripheral nerve conduction properties, structurally invigorating the nerves and protecting them from the harmful and oxidizing action of various chemical species.
  • the second is a haemodynamic type mechanism which attributes to this active ingredient the ability to increase local production of nitric oxide, increasing local vascular flow.
  • the first plant extract is present in the mixture in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • the first plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • the first plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and
  • the second vegetable extract contained in the mixture has a revitalizing and energizing action thanks to a steroidal saponin, as shown hereunder, known by the name of protodioscin (C5i3 ⁇ 4 4 O22).
  • Steroidal saponins have tonic-energizing and anabolic properties which stimulate sexual and spermatogenisis activity.
  • LH luteinizing hormone
  • the second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • the second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • the second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
  • Policosanols are linear aliphatic long chain alcohol blends, mainly of natural origin and traditionally in use thanks to their energizing effects.
  • Policosanols comprise octacosanol, hexacosanol, tetracosanol etc., which differ from each other as regards the length of their aliphatic chain.
  • the mixture according to the invention comprises octacosanol
  • octacosanol reduces triglycerides, increases the concentration and, therefore, the peripheral availability of free fatty acids and also, by stimulating the peripheral lipoprotein lipase, increases the input of lipids in the skeletal muscles.
  • Octacosanol is present in the mixture in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • octacosanol is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
  • the mixture comprises a third plant extract obtained from Ptycopetalum olacoides.
  • Such third plant extract has tonic-energizing properties thanks to the presence of muira puamina, a bitter substance.
  • the third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • the third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • the third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 7% and 20%.
  • the mixture also comprises a fourth plant extract obtained from Paullinia cupana, also known as Guarana.
  • the fourth plant extract contains an equivalent of caffeine, a substance known as guaranine, which gives it its tonic-energizing properties.
  • Guaranine acts primarily on the central nervous and cardiovascular system. In the brain it causes the stimulation of the cerebral cortex cells, increasing attention, memory and mental performance and also reduces the feeling of fatigue. [4]
  • the fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
  • the fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • the fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 7% and 20%.
  • the mixture comprises a fifth plant extract obtained from Lepidium Meyenii, also known as Maca.
  • the fifth plant extract exerts tonic-energizing properties thanks to the presence of zinc, iodine, amino acids such as, in particular, arginine, vitamins C and E, substances of an alkaloid nature, phytosterols and other molecules such as macaridine, macamide, octadecadienamide and octadecadienoic acid.
  • the different components of the fifth extract act in synergy with each other, producing a stimulating effect on the hypothalamic-pituitary axis and also causing an energizing effect on the gonads.
  • the fifth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
  • the fifth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 10%.
  • the mixture also comprises a sixth plant extract obtained from Euterpe oleracea, also known as Acai.
  • the sixth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
  • the sixth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 3% and 10%.
  • the mixture comprises at least one precursor of nitric oxide.
  • Nitric oxide performs relaxing functions on the blood vessels and, for this reason, improves blood circulation throughout the body, including that of the cavernous body of the penis.
  • nitric oxide precursors are ornithine and L-arginine, semi-essential amino acid in which the ornithine is decomposed during the metabolic processes of the organism.
  • the ornithine and L-arginine cause increased nitric oxide, thereby improving the elasticity of the arteries.
  • This effect can reduce blood pressure and improve erectile capacity.
  • the mixture comprises L-arginine present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • L-arginine is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • L-arginine is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
  • the mixture can comprise, alternatively, or in addition, ornithine cannot be ruled out.
  • the mixture comprises a seventh plant extract obtained from Turnera diffusa.
  • the seventh plant extract commonly known as Damiana, carries out its tonic - revitalizing action thanks to the presence of tannins, flavonoids, rubbers and resins.
  • the seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
  • the seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
  • the seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
  • the mixture comprises an eighth plant extract obtained from Rye.
  • the eight plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
  • the eight plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 4% and 9%.
  • the mixture comprises excipients such as hydroxypropyl cellulose and magnesium stearate, present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 10%.
  • the hydroxypropylcellulose is present in concentration by weight, evaluated with respect to the total weight of the mixture, equal to 3%.
  • the magnesium stearate is present in concentration by weight evaluated with respect to the total weight of the mixture, equal to 1%.
  • this mixture thanks to the additive action of the various components, has tonic -revitalizing, rejuvenating and antioxidant actions, and, furthermore, has a protective action with respect to the vascular and nervous tissue.
  • the mixture is in the form of tablets.
  • the mixture can be presented in the form of granular powder, in gel form, or in liquid form.
  • the mixture is orally administered.
  • said mixture is obtained by a dry granulation process.
  • the mixture is obtained joining the first plant extract, the second plant extract, octacosanol, the third plant extract, the fourth plant extract, the fifth plant extract, the sixth plant extract, L-arginine, hydroxypropyl cellulose and magnesium stearate in the following concentrations by weight evaluated compared to the total weight of the mixture:
  • the mixture is obtained joining the first plant extract, the second plant extract, octacosanol, the third plant extract, the fourth plant extract, the fifth plant extract, the sixth plant extract, L-arginine, hydroxypropyl cellulose, magnesium stearate, the seventh plant extract and the eight plant extract in the following concentrations by weight evaluated compared to the total weight of the mixture:
  • the fifth plant extract is present in the form of a blend comprising a first component obtained from the extract of the roots of Lepidium Meyenii and a second component commercially known as Maca 4: 1.
  • the extract of the roots of Lepidium Meyenii is present in concentration by weight evaluated with respect to the total weight of the mixture substantially equal to 10.87%
  • Maca 4: 1 is present in concentration by weight, evaluated with respect to the total weight of the mixture, substantially equal to 5%.
  • Epimedium extract promotes peripheral nerve regeneration in rats, Kou Y, Wang Z, Wu Z, Zhang P, Zhang Y, Yin X, Wong X, Qiu G, Jiang B, Evid Based Compleme;
  • icariin a purified extract of horny goat weed (Epimedium spp.) in vitro and in vivo;
  • Nadkarni's K.M. Indian Materia Medica, vol. I, Popular Prakashan, Bombay, 1993;
  • Nadkarni's K.M. Indian Materia Medica, vol. I, Popular Prakashan, Bombay, 1993;

Abstract

The energizing mixture, particularly on sexual level, comprises at least a first plant extract obtained from Epimedium sagittatum, at least a second plant extract obtained from Tribulus terrestris and at least a policosanol.

Description

ENERGIZING MIXTURE, PARTICULARLY ON SEXUAL LEVEL
Technical Field
The present invention relates to an energizing mixture, particularly on sexual level.
Background Art
It is well known that the problems of modern man whose current lifestyle is often characterized by poor organic stimuli, physical inactivity and stress, often lead to energy deficiencies that also affect the emotional and sexual life of a person, leading to a decline in sexual performance and, sometimes, even to erectile dysfunctions.
It is well known that erectile dysfunction, understood as the inability of a man to attain and/or maintain an erection adequate to conduct satisfactory sexual intercourse, is a disorder that affects millions of men worldwide.
In recent years, in fact, extensive clinical studies have shown that an increasing number of people suffer from this disorder, the causes of which are various and not necessarily a direct result of aging.
Erection, in fact, is a physiological process involving different psychological, neurological, vascular and hormonal aspects and many, therefore, are the factors that may affect the normal erectile function.
It cannot be ruled out, furthermore, that a major cause is to be found in environmental pollution.
In fact, there are many chemical substances foreign to the body and present in air, water and food, substances that if taken daily can significantly compromise the homeostasis of a man.
Following the spread of this disorder, therapeutic treatments of various kinds have been developed in relation to the various possible responsible causes.
Some therapies act on the causes of the dysfunction of a psychological, behavioral or relational nature, and may provide for a simple dialectic confrontation, activities of recovery of bodily sensory perceptions, activities of recovery of couple communication, or even the targeted intervention of a specialized psychologist.
Therapies of naturopathic or nutritional rebalancing type intervene on incorrect nutritional choices of the person which are often at the bottom of energy deficits and of erectile dysfunction such as, e.g., the consumption of highly processed foods, eating too fast or hard-to-digest foods, lack of foods such as fruits and vegetables.
Other therapies include the oral intake of erectile supporting drugs, among the most known and used being sildenafil (Viagra®) and yohimbine (Yohimbine®, Yocon® and others).
All of these therapies, however, have some drawbacks.
In fact, it is not always easy to determine and use a specific therapy since, often, erectile dysfunction is the consequence of several problems of a different nature, problems which are therefore difficult to solve by applying a single therapy. Furthermore, it should be emphasized that most therapies do not allow obtaining a definitive result and that most of the time they create conditions of distress and anxiety over time which further complicate the emotional conditions of the person.
Neither should we forget that treatments such as oral medication cause side effects, some of them serious, such as cardiovascular and nervous system problems.
For this reason, the above drug therapies are often not usable by elderly people. Furthermore, these drug therapies are often directed to solving only the erectile dysfunction, without guaranteeing a prolonged energizing and revitalizing effect over time.
Description of the Invention
The main aim of the present invention is to provide an energizing mixture, particularly on sexual level which allows to overcome the drawbacks and contraindications of use normally present in traditional treatments.
Another object of the present invention is to provide an energizing mixture, particularly on sexual level, which is usable in the presence of energy deficits, as revitalizing product and with a protective effect on the vascular and nervous level.
A further object of the present invention is to provide an energizing mixture, particularly on sexual level, that is usable by men of all ages without any limitation of use, even by elderly people.
Another object of the present invention is to provide an energizing mixture, particularly on sexual level, which can be used in a quick and practical manner by people involved.
Another object of the present invention is to provide an energizing mixture, particularly on sexual level, which allows to overcome the mentioned drawbacks of the prior art within the ambit of a simple, rational, easy and effective to use as well as affordable solution.
The above mentioned objects are achieved by the present energizing mixture, particularly on sexual level having the characteristics of claim 1.
Embodiments of the Invention
Other characteristics and advantages of the present invention will become better evident from the description of a preferred, but not exclusive, embodiment of an energizing mixture, particularly on sexual level.
In the present description reference is made to an energizing mixture, particularly on sexual level, usable e.g. by a person who has energy deficiencies, as a revitalizing product with protective functions at vascular and nervous level and which allows both achieving a normal physiological penis erection process, and maintaining this physiological process for a time interval long enough to conduct satisfactory sexual intercourse.
The mixture comprises a first plant extract obtained from Epimedium sagittatum, a second plant extract obtained from Tribulus terrestris and at least a policosanol.
The first plant extract contains flavonoids, polysaccharides with organic activity and Vitamin C.
In particular, the flavonoids comprise Icariin (C33H4oOi5) which is the primary active component of Epimedium sagittatum extracts.
Icariin, due to its chemical structure shown hereunder, has an antioxidant, neuroprotective, osteoprotective and cardio-protective action, protecting the cells of the different tissues from damage induced by reactive oxygen species (ROS).
Figure imgf000005_0001
The antioxidant activity of Icariin results in an improvement of the peripheral blood flow, thanks to the protective action of endothelium against reactive oxygen species with positive effects in the treatment of erectile dysfunction. This activity is attributed to two different mechanisms.
The first is a nervous type mechanism whereby the Icariin can lead to an improvement in the peripheral nerve conduction properties, structurally invigorating the nerves and protecting them from the harmful and oxidizing action of various chemical species.
The second is a haemodynamic type mechanism which attributes to this active ingredient the ability to increase local production of nitric oxide, increasing local vascular flow.
Furthermore, Icariin has been experimented in the treatment of erectile dysfunction, and appears promising thanks to the above action mechanisms. [1] The first plant extract is present in the mixture in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%. Advantageously, the first plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%. Preferably, the first plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and
20%.
The second vegetable extract contained in the mixture has a revitalizing and energizing action thanks to a steroidal saponin, as shown hereunder, known by the name of protodioscin (C5i¾4O22).
Figure imgf000006_0001
Steroidal saponins have tonic-energizing and anabolic properties which stimulate sexual and spermatogenisis activity.
Their action is manifested in men by an increased secretion of luteinizing hormone (LH) from the pituitary gland which stimulates spermatogenesis and testosterone secretion in the testicle.
For this reason, the extract obtained from Tribulus terrestris is traditionally used in the treatment of infertility, impotence and hypogonadism, besides as an anabolic and for its tonic and stimulating activities. [2]
The second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
Advantageously, the second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%. Preferably, the second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
Policosanols are linear aliphatic long chain alcohol blends, mainly of natural origin and traditionally in use thanks to their energizing effects.
Policosanols comprise octacosanol, hexacosanol, tetracosanol etc., which differ from each other as regards the length of their aliphatic chain.
Preferably, the mixture according to the invention comprises octacosanol
(C28l½O), as depicted below. This long-chain alcohol has ergogenic properties and increases work capacity because of its energizing properties.
Thanks to a series of combined effects on enzymes involved in lipid metabolism regulation, octacosanol reduces triglycerides, increases the concentration and, therefore, the peripheral availability of free fatty acids and also, by stimulating the peripheral lipoprotein lipase, increases the input of lipids in the skeletal muscles. [3]
Octacosanol is present in the mixture in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
Advantageously, octacosanol is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
The mixture comprises a third plant extract obtained from Ptycopetalum olacoides.
Such third plant extract has tonic-energizing properties thanks to the presence of muira puamina, a bitter substance.
The third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
Advantageously, the third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%. Preferably, the third plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 7% and 20%.
The mixture also comprises a fourth plant extract obtained from Paullinia cupana, also known as Guarana.
The fourth plant extract contains an equivalent of caffeine, a substance known as guaranine, which gives it its tonic-energizing properties.
Guaranine acts primarily on the central nervous and cardiovascular system. In the brain it causes the stimulation of the cerebral cortex cells, increasing attention, memory and mental performance and also reduces the feeling of fatigue. [4]
The fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
Advantageously, the fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%. Preferably, the fourth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 7% and 20%. The mixture comprises a fifth plant extract obtained from Lepidium Meyenii, also known as Maca.
The fifth plant extract exerts tonic-energizing properties thanks to the presence of zinc, iodine, amino acids such as, in particular, arginine, vitamins C and E, substances of an alkaloid nature, phytosterols and other molecules such as macaridine, macamide, octadecadienamide and octadecadienoic acid.
The different components of the fifth extract act in synergy with each other, producing a stimulating effect on the hypothalamic-pituitary axis and also causing an energizing effect on the gonads. [5]
The fifth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
Advantageously, the fifth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 10%. The mixture also comprises a sixth plant extract obtained from Euterpe oleracea, also known as Acai.
The beneficial properties of the latter extract, such as powerful antioxidant and energizing activity, are linked to the presence of polyphenols (anthocyanins), vitamins, minerals, essential fatty acids and fiber. [6]
The sixth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
Advantageously, the sixth plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 3% and 10%. Besides the above mentioned plant extracts, the mixture comprises at least one precursor of nitric oxide.
Nitric oxide performs relaxing functions on the blood vessels and, for this reason, improves blood circulation throughout the body, including that of the cavernous body of the penis.
The nitric oxide precursors are ornithine and L-arginine, semi-essential amino acid in which the ornithine is decomposed during the metabolic processes of the organism.
In particular, the ornithine and L-arginine cause increased nitric oxide, thereby improving the elasticity of the arteries.
This effect can reduce blood pressure and improve erectile capacity.
Furthermore, the oxygen and other nutrients carried by the blood reach the body organs quicker, and this has an overall positive effect on male potency, duration, and on sexual performance. [7]
Advantageously, the mixture comprises L-arginine present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
Advantageously, L-arginine is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%.
Preferably, L-arginine is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
However, that the mixture can comprise, alternatively, or in addition, ornithine cannot be ruled out.
Furthermore, the mixture comprises a seventh plant extract obtained from Turnera diffusa.
The seventh plant extract, commonly known as Damiana, carries out its tonic - revitalizing action thanks to the presence of tannins, flavonoids, rubbers and resins.
The seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
Advantageously, the seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 5% and 30%. Preferably, the seventh plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 10% and 20%.
The mixture comprises an eighth plant extract obtained from Rye.
The eight plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
Preferably, the eight plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 4% and 9%. The mixture comprises excipients such as hydroxypropyl cellulose and magnesium stearate, present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 10%.
Advantageously, the hydroxypropylcellulose is present in concentration by weight, evaluated with respect to the total weight of the mixture, equal to 3%. Usefully, the magnesium stearate is present in concentration by weight evaluated with respect to the total weight of the mixture, equal to 1%.
It is underlined that this mixture, thanks to the additive action of the various components, has tonic -revitalizing, rejuvenating and antioxidant actions, and, furthermore, has a protective action with respect to the vascular and nervous tissue.
Thanks to these activities, it is able to promote peripheral blood flow and peripheral nerve conduction.
It is underlined that the particular expedient of providing different plant extracts, combined with other substances with beneficial action allows obtaining a mixture with a function prolonged over time, without the risk of incurring serious side effects.
Advantageously, the mixture is in the form of tablets.
Alternatively, the mixture can be presented in the form of granular powder, in gel form, or in liquid form.
Preferably, the mixture is orally administered.
In particular, said mixture is obtained by a dry granulation process.
Nevertheless, it cannot be ruled out that the mixture be obtainable by a wet granulation process.
EXAMPLE 1
The mixture is obtained joining the first plant extract, the second plant extract, octacosanol, the third plant extract, the fourth plant extract, the fifth plant extract, the sixth plant extract, L-arginine, hydroxypropyl cellulose and magnesium stearate in the following concentrations by weight evaluated compared to the total weight of the mixture:
- first plant extract 15% - second plant extract 15%
- octacosanol 15%
- third plant extract 15%
- fourth plant extract 9%
- fifth plant extract 7%
- sixth plant extract 6%
- L-arginine 14%
- hydroxypropyl cellulose 3%
- magnesium stearate 1%.
EXAMPLE 2
The mixture is obtained joining the first plant extract, the second plant extract, octacosanol, the third plant extract, the fourth plant extract, the fifth plant extract, the sixth plant extract, L-arginine, hydroxypropyl cellulose, magnesium stearate, the seventh plant extract and the eight plant extract in the following concentrations by weight evaluated compared to the total weight of the mixture:
- first plant extract 14.60%
- second plant extract 13%
- octacosanol 3%
- third plant extract 8%
- fourth plant extract 1%
- fifth plant extract 15.9%
- sixth plant extract 5%
- L-arginine 14%
- hydroxypropyl cellulose 3%
- magnesium stearate 1%
- seventh plant extract 15%
- eight plant extract 6.5%.
Furthermore, the fact is underlined that in a preferred embodiment, the fifth plant extract is present in the form of a blend comprising a first component obtained from the extract of the roots of Lepidium Meyenii and a second component commercially known as Maca 4: 1.
In detail, the extract of the roots of Lepidium Meyenii is present in concentration by weight evaluated with respect to the total weight of the mixture substantially equal to 10.87%, and Maca 4: 1 is present in concentration by weight, evaluated with respect to the total weight of the mixture, substantially equal to 5%.
Bibliography:
[1]
Epimedium extract promotes peripheral nerve regeneration in rats, Kou Y, Wang Z, Wu Z, Zhang P, Zhang Y, Yin X, Wong X, Qiu G, Jiang B, Evid Based Compleme;
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Effect of Epimedium brevicornum Maxim extract on elicitation of penile erection in the rat, Chen KK, Chiu JH, Urology. 2006 Mar;67 (3):631 -5;
Erectogenic and neurotrophic effects of icariin, a purified extract of horny goat weed (Epimedium spp.) in vitro and in vivo;
- Shindel AW, Xin ZC, Lin G, Fandel TM, Huang YC, Banie L, Breyer BN, Garcia MM, Lin CS, Lue TF, J Sex Med. 2010 Apr;7(4 Pt l): 1518-28. doi: 10.1111/j.1743-6109.2009.01699.X. Epub 2010 Feb 5.
[2]
Nadkarni's K.M.: Indian Materia Medica, vol. I, Popular Prakashan, Bombay, 1993;
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Chopra R.N.: Indigenous Drugs of India, Academic Publishers, Calcutta, 1982;
Nadkarni's K.M.: Indian Materia Medica, vol. I, Popular Prakashan, Bombay, 1993;
- Kirtikar K.R., Basu B.D.: Indian Medicinal Plants Bishen Singh, Mahendrapal Singh, Dehradun, 1985;
Protich M., Tsvetkov D. et al.: "Clinical trial of Tribestan on infertile males", Scientific Technical Report, 1981. [3]
Taylor JC, Rapport L, Lockwood GB. Octacosanol in human health. Nutrition. 2003 Feb; 19(2): 192-5; Kabir Y, Kimura S. Biodistribution and metabolism of orally administered octacosanol in rats. Ann Nutr Metab 1993; 37: 33-8);
Kato S, Karino K,Hasegawa S, Nagasawa J, Nagasaki A, Eguchi M, Ichinose T, Tago K, Okumori H, Hamatani K, et al.Octacosanol affects lipid metabolism in rats fed on a high-fat diet. Br J Nutr 1995; 73: 433-41).
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Laura Johannes, Can a Caffeine-Packed Plant Give a Boost? in The Wall Street Journal, 2 March 2010, p.D3;
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Walker, Morton, DPM: "Medical Journalist Report of Innovative Biologies - Effects of Peruvian Maca on Hormonal Functions", Townsend Letter for Doctors & Patients, November 1998;
Cabieses F.: La maca y la puna, Universidad de San Martin de Porres, Lima , 1997 Reyna J., Gomez-Sanchez I., Gagliuffi A. y Idelfonso C: "Evaluacion Quimico-Nutricional de la Maca", Agroenfoque, 77, 42-44, 1996;
Dini A., Migluolo G., Rastrelli L., Saturnino P. and Schettino O.: "Chemical composition of Lepidium Meyenii", Food Chemistry, 49, 347-349, 1994. [6]
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Del Pozo-Insfran D. et al.: "Phytochemical Composition and Pigment Stability o Acai ( Euterpe oleracea Mart.)", J. Agric. Food Chem.. 52 (6).1539 - 1545.2004;
Dyer A. P.. "Latet energy in Euterpe oleracea". Biomass Energy Envir.. Proc. Bioenergy Con . 9th, 1996; Plotkin M.J. Balick M.J.: "Medicinal uses of South American Palms". J.Ethnopharmacol.. 10 (2): 157-179, 1984;
Schauss A.G. et al.: "Phytochemieal and nutrient composition o freeze - dried amazonian palmberry. Euterpe oleracea Mart. (Ac i), J. Agric. Food Chem.. 54 (22), 8598-8603, 2006;
Schauss A.G. et al.: "Antioxidanyt capacity and other bioactivities of the freeze-dried amazonian palm berry. Euterpe oleracea Mart (Ac i), Biochem.Biophys.Res.Comm. 332: 3922397, 2005. [7]
Wespes, E. (2013) Erectile Dysfunction: The Medical Treatment, European Urology Supplements, Volume 12, Issue 2, (pp. 13-17);
- Jung, H.C., Mun, K.H., Park, T.C., Lee, Y.C., Park, J.M., Huh, K., Seongh, D.H. & Suh, J.K. (1997) Role of nitric oxide in penile erection Yonsei, Medical Journal, Volume 38, issue 5, (pp. 261-269);
Palloshi, A., Fragasso, G., Piatti, P., Monti, L.D., Setola, E., Valsecchi, G., Galuccio, E., Chierchia, S.L. & Margonato, A. (2004) Effect of Oral L-arginine on Blood Pressure and Symptoms and Endothelial Function in Patients With Systemic Hypertension, Positive Exercise Tests, and Normal Coronary Arteries, The American Journal of Cardiology, Volume 93 (pp. 933-935);
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- Zieve, L. (1986) Conditional deficiencies of ornithine or arginine, J Am Coll Nutr, Volume 5, (pp. 167-176).

Claims

1) Energizing mixture, particularly on sexual level, characterized by the fact that it comprises at least a first plant extract obtained from Epimedium sagittatum, at least a second plant extract obtained from Tribulus terrestris and at least a policosanol.
2) Mixture according to claim 1, characterized by the fact that said first plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
3) Mixture according to one or more of the preceding claims, characterized by the fact that said second plant extract is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
4) Mixture according to one or more of the preceding claims, characterized by the fact that said policosanol is octacosanol.
5) Mixture according to one or more of the preceding claims, characterized by the fact that said octacosanol is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
6) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises a third plant extract obtained from Ptycopetalum olacoides and present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
7) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises a fourth plant extract obtained from Paullinia cupana and present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
8) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises a fifth plant extract obtained from Lepidium Meyenii and present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
9) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises a sixth plant extract obtained from Euterpe oleracea and present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%. 10) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises at least one precursor of nitric oxide.
11) Mixture according to one or more of the preceding claims, characterized by the fact that said precursor of nitric oxide is L-arginine and is present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
12) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises at least one of hydroxypropyl cellulose and magnesium stearate as excipients, present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 10%.
13) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises a seventh plant extract obtained from Turnera diffusa present in concentration by weight, evaluated with respect to the total weight of the mixture, between 1% and 40%.
14) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises an eight plant extract obtained from Rye present in concentration by weight, evaluated with respect to the total weight of the mixture, between 2% and 20%.
15) Mixture according to one or more of the preceding claims, characterized by the fact that it comprises said first plant extract, said second plant extract, said octacosanol, said third plant extract, said fourth plant extract, said fifth plant extract, said sixth plant extract, said L-arginine, said hydroxypropyl cellulose and said magnesium stearate in the following concentrations of weight evaluated compared to the total weight of the mixture:
- first plant extract 15%
- second plant extract 15%
- octacosanol 15%
- third plant extract 15%
- fourth plant extract 9%
- fifth plant extract 7%
- sixth plant extract 6%
- L-arginine 14% - hydroxypropyl cellulose 3%
- magnesium stearate 1%.
16) Mixture according to claims 1 to 14, characterized by the fact that it comprises said first plant extract, said second plant extract, said octacosanol, said third plant extract, said fourth plant extract, said fifth plant extract, said sixth plant extract, said L-arginine, said hydroxypropyl cellulose, said magnesium stearate, said seventh plant extract and said eight plant extract in the following concentrations by weight evaluated compared to the total weight of the mixture:
- first plant extract 14.60%
- second plant extract 13%
- octacosanol 3%
- third plant extract 8%
- fourth plant extract 1 %
- fifth plant extract 15.9%
- sixth plant extract 5%
- L-arginine 14%
- hydroxypropyl cellulose 3%
- magnesium stearate 1%
- seventh plant extract 15%
- eight plant extract 6.5%.
PCT/IB2016/050468 2015-01-29 2016-01-29 Energizing mixture, particulary on sexual level WO2016120844A1 (en)

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IT202100031175A1 (en) * 2021-12-13 2023-06-13 Anvest Group S R L COMPOSITION FOR THE TREATMENT OF ERECTILE DYSFUNCTION
EP4193848A1 (en) * 2021-12-13 2023-06-14 Anvest Group S.r.l. Composition for use in the treatment of erectile dysfunction

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