DESC:Priority Claim:

[0001] This application claims priority from the provisional application numbered 202041044342 filed with Indian Patent Office, Chennai on 12th October 2020 entitled “A formulation of phytochemicals to boost male sexual health”, the entirety of which is expressly incorporated herein by reference.
Preamble to the Description

[0002] The following specification describes the invention and the manner in which it is to be performed:
DESCRIPTION OF THE INVENTION
Technical field of the invention
[0003] The present invention relates to a phytochemical formulation to boost male sexual health. More particularly, the invention discloses a specific combination of natural ingredients such as Kaempferia parviflora (black ginger), Trigonella foenum-graecum (fenugreek) and Tribulus terrestris (Tribulus), aqueous extract of turmeric (Curcuma longa) whose synergistic action makes the formulation effective to boost male sexual health.
Background of the invention
[0004] One of the aspects of male sexual health is male libido, commonly called as sex drive and today, due to lifestyle changes, low male libido, arising from low testosterone levels seems to be a major health issue. The causes of low libido are many, including, workplace stress, no or over exercise, alcohol or drug abuse, psychological conditions, such as, depression, poor eating habits or continued medication. About 4 out of 10 men over age of 45 years or 15% to 16% of men, have been found to have low testosterone levels.
[0005] Even though low libido affects women more generally, it scares men more than women as their masculinity is so linked to their sexuality that it is very threatening, leading to lack of confidence, anxiety and depression.
[0006] The male libido is regulated by the cerebral cortex and the limbic system of the brain and these parts of the brain are considered to be vital for a man’s libido and performance. The cerebral cortex is the gray matter of the brain that is responsible for thinking about sex, whereas the limbic system includes, mainly, the hippocampus, hypothalamus and amygdala and these parts are involved with emotion, motivation and sex drive.
[0007] Testosterone, produced mainly in the testicles, is the hormone which is closely associated with male sex drive. This hormone performs various biological functions such as, development of male sex organs, body hair, sperm production etc.
[0008] There are various treatments available to cure low testosterone levels, including, exercises, counselling behavioral or relationship related issues, supplements, testosterone therapy and other drugs. A large number of drugs are available in the market today, however, due to side effects of most of the drugs available in the market today, everyone wants to switch over to holistic approach to cure and heal body naturally. Moreover, low libido is not a disease to be cured, but it has more to do with managing and maintaining testosterone levels by making lifestyle changes or switching over to natural formulations.
[0009] Plant extracts and their derivatives have received considerable attention as therapeutic agents for preventing and treating majority of complex health problems. Among them, to provide tangible overall benefit for men's health, various phytotherapeutic approaches have been widely proposed. However, having a relative paucity of controlled clinical studies on the formulations containing vegetal derivatives, an optimal therapeutic approach remains an elusive challenge.
[0010] Among the natural aphrodisiac plants, black ginger is well-recognized in traditional Thai medicine in the form of tablets, capsules, pills, and medicinal liquor or tonic to cure impotence and infertility. Black ginger mainly comprises 5-hydroxy-3,7,3’,4’ tetramethoxyflavone, 3,5,7-trimethoxyflavone, 5-hydroxy-3,7,4’-trimethoxyflavone, 5- hydroxy-7,4’-dimethoxyflavone, 5-hydroxy-3,7-dimethoxyflavone, 5-hydroxy-7-4 methoxyflavone, 5,7,3’,4’-tetramethoxyflavone, 3,5,7,4’-tetramethoxyflavone,5,7,4’-trimethoxyflavone (TMF), 5,7-dimethoxyflavone (DMF), 3,5,7,3’4’pentamethoxyflavone (PMF) that are biologically active.
[0011] Fenugreek, which is native to India, North Africa and Mediterranean region possess multifunctional, restorative, nutritive, antihyperglycemic properties and has the potential of accelerating T production and male libido. Fenugreek comprises Diosgenin Trigonelline (Alkaloid), 4-Hydroxyisoleucine and Galactomannan as major components of which Diosgenin work against sexual dysfunction.
[0012] Tribulus terrestris native to warm temperate and tropical regions such as Africa, Sourthern Asia, Northern Australia and Southern Europe mainly comprises steroidal saponins and is effective for sperm motility and male infertility.
[0013] The Patent Application No. WO2017019107A1 entitled “Herbal dietary supplement for increasing testosterone and improving sexual performance” discloses an herbal dietary supplement for increasing the testosterone level, libido, and sexual performance of a human. The herbal dietary supplement also increases the energy level of a human. The herbal dietary supplement may be prepared and provided in the forms of a liquid beverage or food bar for oral consumption. In such forms, the herbal dietary supplement comprises Ashwagandha and Mucuna Pruriens. Other ingredients may be included to further increase a human's testosterone level, libido, and/or energy level or to customize and/or enhance the effects of the other ingredients in the herbal dietary supplement. Such other ingredients may include, without limitation, Maca, Tinospora Cordiofolia, Asparagus Racemosus, Orchis Latifolia, Tribulus Terrestris, Anacylus Pyrethrum, L-dopa, Epimedium, King Oyster mushrooms, Vitamin-B6, Ginseng, and D-aspartic acid.
[0014] The Patent application No. WO2014031026A1 entitled “Method for restoring male sex drive (libido) using a food supplement for restoring male sex drive (libido)” discloses a method for restoring male sex drive (libido) using a food supplement for restoring male sex drive (libido) relates to medicine, and more specifically to the pharmaceutical industry producing food supplements for restoring male sex drive (libido) and male sexual function which are based on natural ingredients. The method involves the use of nitric oxide (NO) in terms of L-arginine, pollen or beebread in terms of rutin, drone brood in terms of decenoic acids, a substance containing zinc in terms of zinc, a substance containing vitamin B6 in terms of vitamin B6, horny goat weed in terms of icariin, true or false ginseng root in terms of saponins, and leuzea or crowned saw-wort in terms of ecdysteroids, in various combinations.
[0015] The Patent Application No. US9486482B2 entitled “Herbal composition for treating male sexual dysfunction” discloses a synergistic herbal composition comprising extracts of herbal ingredients of Tribulus terrestris, Withania somnifera, Curculigo orchioides, Mucuna pruriens, Asparagus adscendens, Asteracantha longifolia, Asphaltum, and optionally the extracts of Piper longum and Anacyclus pyrethrum for the treatment of disorders associated with Male Sexual Dysfunction.
[0016] The available medications may not be effective in maintaining male sexual health by means of maintaining right testosterone levels. As the available medications are synthetic or semisynthetic and may cause side effects. Hence, there is a need for a formulation, which is effective to maintain good male sexual health.
Summary of the invention
[0017] In order to overcome the drawbacks of the state of art, the present invention provides a phytochemical formulation to boost male sexual health with complete natural matrix. The formulation comprises black ginger, fenugreek and tribulus in combination, which exhibits synergistic action and makes the formulation effective to maintain and improve male sexual health.
[0018] The formulation of the present invention forms a natural complex and comprises Kaempferia parviflora methoxy flavone extract at a concentration in a range between 15% and 20%, Trigonella foenum-graecum saponins extract at a concentration in a range between 20% and 25%, Tribulus terrestris extract at a concentration in a range between 25% and 30% and aqueous extract of turmeric at a concentration in a range between 30% and 35%. The bioactive component of the formulation forms a natural and uniform complex to form a polar-non-polar matrix.
[0019] The effect of supplementation of the formulation is evaluated in healthy male volunteers aged between 21 and 55. The male volunteers are randomized to an oral dose at a concentration of 500 mg capsules/day of the active treatment or placebo for the duration of 12 weeks. The formulation is analyzed for safety and efficacy in humans.
[0020] The broad-spectrum safety parameters comprise blood profile, lipid profile in humans and the efficacy parameters includes the levels of free testosterone and total testosterone, sperm profile, sperm morphology, libido and sexual health, mood and mental alertness, and safety parameters in a double blind randomized placebo controlled study.
[0021] The results indicated that the formulation was safe, effective in improving the free and total testosterone levels, sperm profile including sperm count, sperm motility in humans supplemented with the formulation.
[0022] The formulation is natural, safe and enhances the testosterone and thus improves the male libido and sexual health in human.
Brief description of the drawings
[0023] The foregoing and other features of embodiments will become more apparent from the following detailed description of embodiments, when read in conjunction with the accompanying drawings. In the drawings, like reference numerals refer to like elements.
[0024] FIG 1 tabulates the formulation of combination of Kaempferia parviflora (black ginger), Trigonella foenum-graecum (fenugreek) and Tribulus terrestris (tribulus) and aqueous extract of turmeric( Curcuma longa).
Detailed description of the invention
[0025] In order to more clearly and concisely describe and point out the subject matter of the claimed invention, the following definitions are provided for specific terms, which are used in the following written description.
[0026] The term “Erectile Dysfunction” refers to inability to get or keep an erection firm enough to have sexual intercourse.
[0027] The term “IIEF (International Index of Erectile Dysfunction)” refers to a multidimensional scale that can be used to evaluate Erectile Dysfunction (ED). It addresses the most relevant aspects of male sexual function, such as erectile strength, orgasm, desire, satisfaction with intercourse, and overall satisfaction.
[0028] The term “Male Libido” refers to a person's overall sexual drive or desire for sexual activity.
[0029] The term “Testosterone” refers to the hormone, which is closely associated with male sex drive.
[0030] The term “Sexual health” refer to a state of physical, mental and social well-being in relation to sexuality.
[0031] The term “SF-36” refers to a set of generic, coherent, and easily administered quality-of-life measures.
[0032] The term “Cerebral cortex” refers to the outer layer of the cerebrum composed of folded grey matter and plays an important role in consciousness.
[0033] Th term “Limbic System” refers to complex system of nerves and networks in the brain, involving several areas near the edge of the cortex concerned with instinct and mood.
[0034] The invention discloses a phytochemical formulation to boost male sexual health with complete natural matrix. The formulation comprises black ginger, fenugreek and tribulus in combination, which exhibits synergistic action and makes the formulation effective to maintain and improve male sexual health.
[0035] FIG 1 tabulates the formulation of combination of Kaempferia parviflora (black ginger), Trigonella foenum-graecum (fenugreek) Tribulus terrestris (tribulus) and Curcuma longa ( turmeric). The formulation comprises of an extract of black ginger, fenugreek and tribulus, in specific proportion, as tabulated in Fig 1. The formulation comprises Kaempferia parviflora (black ginger) flavone extract at a concentration in a range between 15% and 20%, Trigonella foenum-graecum saponins extract at a concentration in a range between 20% and 25%, Tribulus terrestris extract at a concentration in a range between 25% and 30% and aqueous extract of turmeric at a concentration in a range between 30% and 35%.
[0036] Kaempferia parviflora (black ginger) extract comprises 50% methoxy flavones, Trigonella foenum-graecum (fenugreek) saponins, further comprises diosgenin, dioscin, gitogenin and trigonelline chloride at a concentration of 30% and Tribulus terrestis extract comprises 40% saponins.
[0037] The following examples are offered to illustrate various aspects of the invention. However, the examples are not intended to limit or define the scope of the invention in any manner.
Example 1: Effect of the formulation on male libido.
[0038] The formulation of the present invention is effective on male libido in humans. The effect of supplementation of the formulation is evaluated in 60 healthy male volunteers aged between 21 and 55. The male volunteers are randomized to an oral dose at a concentration of 500 mg capsules/day of the active treatment or placebo for the duration of 12 weeks. The parameters that are taken into consideration to assess efficacy of the formulation includes the levels of free testosterone and total testosterone, sperm profile, sperm morphology, libido and sexual health, mood and mental alertness, and broad-spectrum safety parameters in a double blind randomized placebo controlled study. The dose of the formulation, administered orally, used for the study is 500 mg capsules/day of the active treatment or placebo for the duration of 12 weeks.
[0039] After the testing for 12 weeks of time the outcome of the study was assessed. The primary outcome measures include the change in the serum testosterone levels and sperm profile, a measure of possible androgen deficiency symptoms, whereas the secondary outcome measures include International Index of Erectile Dysfunction (IIEF) and a quality of life questionnaire, SF-36.
[0040] The results indicated that though secondary variable, such as, IIEF and SF-36 did not differ between the active and placebo groups, the formulation exhibited significant and distinct beneficial effect on primary efficacy measures. Moreover, formulation is a safe and effective treatment for reducing symptoms of possible androgen deficiency and resulted in improved sexual function and increases serum testosterone in healthy middle-aged and older men.
Example 2: Effect of supplementation of the formulation on testosterone levels in human
[0041] The effect of supplementation of the formulation on total testosterone is analyzed in human. The formulation of the present invention is analyzed for its effect on total testosterone levels in human for 12 weeks. The results indicated that the formulation resulted in increase of the total testosterone with 56.41, 58.38 267 and 35.56 units at end of 4, 8 and 12 weeks respectively in humans with supplementation of the formulation whereas the testosterone levels were decreased in placebo group.
Example 3: Effect of supplementation of the formulation on sperm profile in human
[0042] The effect of supplementation of the formulation on sperm profile is analyzed in human. The formulation of the present invention is analyzed for its effect on serum profile such as of serum count, sperm motility, abnormal sperm morphology in human for 4, 8 and 12 weeks. The results indicated that the formulation resulted in increase in sperm count and sperm motility by 7 times for 12 weeks respectively and without affecting the sperm morphology in humans with supplementation of the formulation.
[0043] The supplementation of the formulation was safe and tolerable without inducing any modifications in the levels of blood glucose profile, total blood count, lipid profile, Alanine Transaminase (ALT), Aspartate Transaminase (AST), Alkaline Phosphatase (ALP), Blood Urea Nitrogen (BUN) and serum creatinine. The formulation did not induce any change in the levels of cholesterol, triglycerides, High Density Lipoprotein Cholesterol (HDL-C), Low-Density Lipoprotein Cholesterol (LDL-C) for 4, 8 and 12 weeks of supplementation.
[0044] The formulation of the present invention is prepared using a specific encapsulation technology namely Polar Non-polar Sandwiching Technology (PNS Technology). The encapsulation process includes the encapsulation of the bioactive components without using any excipients and in powder form to ensure high efficacy without inducing severe adverse effects. The polar fraction is constituted by fenugreek and tribulus saponins, the resinous matter constitutes the midpolar and the methoxy flavones in the black ginger is sandwiched between the two layers. This unique encapsulation technology and the arrangement of polar and non-polar molecules enables the bioactive components to be traced in each part of the formulation thereby increasing the efficacy. The encapsulated complex is subjected to spray drying to form a powder form of the formulation.
[0045] The formulation of the present invention is used in powder form, which enhances the efficacy due to high surface area for the formulation. The formulation is safe as it constitutes phytochemicals and effective in improving the levels of free and total testosterone, sperm profile, sperm morphology, libido and sexual health in human.

,CLAIMS:Claims:
We Claim,

1. A phytochemical formulation as supplement for improvement of male sexual health, the formulation comprising:
a. methoxy flavone rich extract from Kaempferia parviflora at a concentration in a range between 15% and 20%;
b. saponin rich extract from Trigonella foenum-graecum at a concentration in a range between 20% and 25%;
c. Tribulus terrestris extract at a concentration in a range between 25% and 30%; and
d. turmeric water extract at a concentration in a range between 30% and 35%
and the extracts form a uniform polar and non-polar matrix upon homogenization and spray drying thus forming an encapsulated powdered form of the formulation.

2. The formulation as claimed in claim 1, wherein the saponin rich extract of Trigonella foenum-graecum also comprises diosgenin, dioscin, gitogenin and trigonelline chloride at a concentration of 30%.

3. The formulation as claimed in claim 1, wherein supplementation of the formulation increased the testosterone levels in human.

4. The formulation as claimed in claim 1, wherein supplementation of the formulation increased the serum count, sperm motility and reduced the abnormal sperm morphology in human.

5. The formulation as claimed in claim 1, wherein polar and non-polar matrix of the formulation constitutes Trigonella foenum-graecum saponin fraction and Tribulus terrestris extract as polar fraction, the resinous matter constitutes the midpolar and the methoxy flavone extract of Kaempferia parviflora is sandwiched between the two layers.

6. The formulation as claimed in claim 1, wherein the formulation in encapsulated form withholds the components firmly and arrangement of polar and non-polar molecules enables the bioactive components to be traced in each part of the formulation thereby increasing the efficacy.