WO2014209099A1 - Composition pour améliorer l'endurance et la performance athlétiques - Google Patents

Composition pour améliorer l'endurance et la performance athlétiques Download PDF

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Publication number
WO2014209099A1
WO2014209099A1 PCT/MY2014/000089 MY2014000089W WO2014209099A1 WO 2014209099 A1 WO2014209099 A1 WO 2014209099A1 MY 2014000089 W MY2014000089 W MY 2014000089W WO 2014209099 A1 WO2014209099 A1 WO 2014209099A1
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WO
WIPO (PCT)
Prior art keywords
composition
leaves
extract
endurance
labiatae
Prior art date
Application number
PCT/MY2014/000089
Other languages
English (en)
Inventor
Mohamed Suhaila
Mohamad Shalan NOR AIJRATUL ASIKIN
Wan Osman WAN NURFARAHIN
Original Assignee
Universiti Putra Malaysia
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Universiti Putra Malaysia filed Critical Universiti Putra Malaysia
Publication of WO2014209099A1 publication Critical patent/WO2014209099A1/fr

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Classifications

    • 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)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • 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)
    • A61K36/74Rubiaceae (Madder family)
    • A61K36/746Morinda
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to an endurance or performance enhancing composition. More particularly, the present invention relates to a composition comprising herbal extract of a plant from the family Rubiaceae and/or Labiatae that prevents fatigue and improves athletic endurance or performance.
  • compositions and formulations containing plant extracts and/or metabolites for improving endurance and performance of a mammal.
  • Polynesians consume Morinda citrifolia noni fruit to combat fatigue and help restore vigor to the body (Thaman, 1990, 1992).
  • Two clinical studies demonstrated on athletes and post-menopausal women have revealed the ability of noni juice to improve endurance.
  • Forty highly-trained athletes consuming 100 mL of Tahitian Noni fruit Juice (TNJ) twice daily had increased endurance (time-to-fatigue) by 21 %, and improved antioxidant status as measured by a 25% decrease in blood chemiluminescence.
  • TNJ Tahitian Noni fruit Juice
  • JP2006282576 discloses an endurance-enhancing composition having good flavor, easily formulated with various kinds of food and drink, and capable of preventing the reduction of exercise performance and convulsions of muscles caused after carrying out endurance exercise; and to provide a food and drink containing the composition.
  • the endurance-enhancing composition discloses herein contains a cacao nib and/or a processed product thereof as an active ingredient.
  • the cacao nib and/or the processed product thereof is preferably at least one kind selected from cacao mass, cocoa powder and a cacao extract, and the cacao extract is preferably a theobromine.
  • the endurance-enhancing composition preferably contains at least one kind selected from an organic acid, a branched amino acid and a saccharide with low response to insulin as the other components.
  • athletic performance may be improved by administering a composition comprising galanthamine as an active ingredient to an athlete before and during sports activities.
  • a herbal sports performance composition comprising whole plant extract of Leucojum aestivum.
  • U.S. 7,820,222 discloses an organic, ergogenic, isotonic soft drink composition that causes energy enhancing internally soothing effect.
  • the composition comprises a brewed extract from leaves of Cymbopogon Citratus, and of ginger, and of peppermint, sugar or other sweeteners and optionally, other flavors and purified water and a method of producing the soft drink composition; which drink imbibed produces in the imbiber an energy, internally soothing effect which includes stimulation of mitochondrial efficiency in the digestive organs, and enhancement of a more efficient intake of oxygen into the user's body.
  • United States patent publication number 20070224292 discloses a therapeutic extended effect ergogenic drink whose composition includes: caffeine, chromium in the form of chromium, polynicotinate, niacin and the electrolytes calcium, potassium, magnesium, sodium, and the nutrient Vitamin C.
  • This publication also discloses a method to use the composition, with the following effects: increased mental alertness, decreased fatigue, improved aerobic capacity, elevated mood, and increased overall circulation along with the associated benefits such as improved sensations of warmth in the extremities.
  • the synergistic relationships of the caffeine, electrolytes, niacin, and chromium polynicotinate in this formulation result in an enhanced and prolonged ergogenic effect without the requirement of additional calories from carbohydrates.
  • the present invention provides novel compositions, use and methods pharmaceutical or nutraceutical use in a mammal, preferably in a human.
  • the present invention provides a composition comprising a plant extract from the family Rubiaceae and/or Labiatae.
  • the plant from the family Rubiaceae and/or Labiatae is derived from the leaves of any one or combination of the plant species of Morinda spp and Orthosiphon spp.
  • the plant species of Morinda spp is preferably Morinda citrifolia.
  • composition of the present invention may further include one or more excipients, organic caffein, catechins, flavanoids and antioxidants derived from a food sources.
  • the plant extract from the family Rubiaceae and/or Labiatae is about 0.1 % -100% w/w of the total weight of the composition.
  • the present invention provides use of a composition comprising a plant extract from the family Rubiaceae and/or Labiatae in the manufacture of a preparation that prevents fatigue and improves athletic endurance or performance.
  • the composition of the present invention can be formulated and can stand alone as a complete product preparation for enhancing endurance, performance, stamina and other physical performance, or it may be included as a compound ingredient in other products.
  • Non-limiting examples of other products include food, medicine, sport beverages, meal replacement drinks, powders, ointments, dietary supplement capsules, tablets, or a simple water additive.
  • the formulation can be prepared in a variety of forms.
  • Non-limiting examples of such forms include capsules, tablets, pills, dispersions, suspensions, solutions, powders, teas, syrup concentrates, bars and chews. It can be further packed packages in bottles or other packaging for sale.
  • the present invention provides a method of preventing fatigue and improving endurance or performance in a mammal, comprising administering to the mammal in need thereof an effective amount of the composition described herein.
  • the mammal may be a human or an animal, but preferably a human.
  • composition disclosed herein to a mammal is via an oral route.
  • the composition is administered to a mammal at a dose of about 0.1 to 5000 mg/kg of body weight of a mammal per day. More preferably, the usual dose or therapeutically effective amount of the composition is in the range from about 5 to 500 mg/kg of body weight of a mammal administered in equal portions twice a day or thrice a day.
  • Figure 1 is a graph showing the swimming time to exhaustion throughout the experiment period
  • Figure 2 is a graph showing endurance of Balb/C mice were tested with forced swim test for 6 weeks after treatment of Morinda citrifolia leaves solvent with low dose (MCLD) and high dose (MCHD); and
  • Figure 3 is a graph showing comparative effects of the selected herbs of Morinda and Orthosiphon for improving endurance, performance, and stamina in swimming tests.
  • therapeutically effective amount used herein throughout the specification refers to the amount of the active ingredient, the extract, to be administered orally to the subject to trigger the desired effect without or causing minimal toxic adverse effect against the subject.
  • therapeutically effective amount can vary from one individual to another due to the external factors and age, sex, diseased state, races, body weight, formulation of the extract, availability of other active ingredients in the formulation and so on.
  • the present invention provides novel compositions for nutraceutical or pharmaceutical use in a mammal, preferably in a human.
  • the composition comprises a plant extract from the family Rubiaceae and/or Labiatae at about 0.1 % to 100% w/w based on the total weight of the composition. Any combination of proportions of the extracts of Rubiaceae and/or Labiatae is envisioned to be encompassed by the compositions disclosed herein. The percentage provided herein refers to the w/w ratio based on the total weight of the extract portion of the composition and does not include any excipient and extra ingredients added to a formulation.
  • the plant from the family Rubiaceae and/or Labiatae is any one or combination of the leaves of Morinda spp and Orthosiphon spp.
  • the Morinda spp is Morinda citrifolia.
  • compositions of the present invention may be, for example, solid, liquid, suspension, concentrate, powder, ointment or aerosol formulations comprising one or more of the extracts as disclosed herein.
  • compositions of the present invention may also comprise other components, for example, one or more excipients, organic caffein, catechins, flavanoids and antioxidants derived from a food sources.
  • composition of the present invention can be formulated and can stand alone as a complete product preparation for enhancing endurance, performance, stamina and other physical performance, or it may be included as a compound ingredient in other products.
  • Non-limiting examples of other products include food, medicine, sport beverages, meal replacement drinks, powders, dietary supplement capsules, tablets, or a simple water additive.
  • the formulation can be prepared in a variety of forms.
  • Non-limiting examples of such forms include capsules, tablets, pills, dispersions, suspensions, solutions, powders, teas, syrup concentrates, bars and chews. It can be further packed packages in bottles or other packaging for sale.
  • the desired compounds to be extracted from the extract of the invention are mainly constituted of, but not limited to, biophenols, proteins, lipids, saccharides, minerals and small peptides.
  • the present invention provides use of the composition described herein comprising a plant extract from the family Rubiaceae and/or Labiatae in the manufacture of a preparation that prevents fatigue and improves human and animal endurance or performance.
  • the preparation is preferably a pharmaceutical preparation that can be formulated into therapeutic dosage forms and tablets, capsules, liquid orals, sterile injections, aqueous or oily solutions or suspensions and the like.
  • the preparation may be administered as food ingredients or as cosmaceuticals by known techniques, and oral and parenteral administration (including subcutaneous injection, intravenous or intramuscular technique), in dosage unit formulations containing conventional nontoxic pharmaceutically acceptable carriers, diluents or excipient.
  • the extract of the leaves of Rubiaceae and Labiatae family, as it is in the preparation may be a liquid, paste or a solid powder.
  • the term pharmaceutically acceptable carrier means a non-toxic, inert solid, semi-solid or liquid filler, diluent, encapsulating material or formulation auxiliary of any type.
  • materials that can serve as pharmaceutically acceptable carriers are sugars and lactose, glucose, and sucrose; starches and com starch and potato starch; cellulose and its derivatives and sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; powdered tragacanth; malt; gelatin; talc; excipients and cocoa butter and suppository waxes; oils and peanut oil, cotton seed oil, safflower oil, sesame oil, olive oil, com oil, and soybean oil; glycols, and propylene glycol; esters, and ethyl oleate and ethyl laurate; agar; buffering agents and magnesium hydroxide and aluminum hydroxide; alginic acid; pyrogen-free water; isotonic
  • the pharmaceutical and comestible preparation of the present invention may be prepared by mixing the various components of the preparation using conventional methods.
  • the preferred composition of the preparation may be prepared according to the preferred constituent ranges.
  • the usual dose or therapeutically effective amount of the extract varies from about 0.1 to 10 g/kg of body weight of the patient per day. More preferably, the usual dose or therapeutically effective amount of the extract is in the range of from about 5 to 5 g/kg of body weight of the patient administered in equal portions twice a day or thrice a day.
  • the comestibles mentioned herein can be any common daily consumed processed food such as bread, noodles, confections, chocolates, beverages (for example instant tea preparation), and the like.
  • aforesaid extract can be incorporated into the processed comestibles, capsules, tablets or topical medicine during the course of processing. Therefore, any modification thereon shall not depart from the scope of the present invention.
  • the pharmaceutical preparation with activities of enhancing endurance and/or performance, as well as increasing energy generation in mammals, so that the preparation can be effectively used for the prevention and treatment of fatigue for use during sports and sickness comprises water or alcoholic or aqueous extract or their combinations from leaves of Rubiaceae and Labiatae family, or water or alcoholic or aqueous mixture extract of leaves from Rubiaceae and Labiatae family.
  • the plant of Rubiaceae and Labiatae family is any one or combination Morinda spp. and Orthosiphon spp.
  • the Morinda spp. is Morinda citrifolia.
  • the extract to be incorporated into the comestibles and medicine can be acquired from any known method not limited only to the foregoing disclosed method.
  • the extract is prepared in a concentrated form, preferably paste or powdery form which enables the extract to be incorporated in various formulations of the comestibles, capsules, tablets or topical products.
  • the extract shall be the plant metabolites which are susceptible to an extraction solvent.
  • the compounds and small peptides with the endurance and/or performance, as well as increasing energy generation enhancing properties are those metabolites in the water or alcoholic extracts.
  • the water or alcoholic mixture extracts of leaves of Rubiaceae and Labiatae family is preferably derived from the extraction solvent of water, water or alcohol, acetone, chloroform, liquid CO2 and any combination thereof.
  • further embodiment of the present invention includes a method comprising the step of administrating orally or topically to the subject an effective amount of a mixture extract derived from the leaves of Rubiaceae and Labiatae family.
  • Fresh Morinda spp and Orthosiphon spp leaves were chopped into small pieces, extracted with solvents or boiled in distilled water (1 :3, w/v) at 100°C for 2 hours. The extract was filtered and concentrated to give the leaf bioactive extract.
  • the fresh Morinda (Morinda citrifolia) leaves and Orthosiphon spp. leaves were washed, chopped and then dried at 30-40°C for another 24-48 hours.
  • the completely dried leaves were ground into powder, weighed and soaked with 50% ethanol with the ratio (w/v) of 1 :10.
  • the mixture was left in room temperature for 24 hours and the supernatant was then filtered using Whatmann No. 1 filter paper.
  • the filtered extracts were then rotary evaporatored at 40°C to produce a dark brown sticky bioactive extract.
  • Group one received 1 mg/ml of MCF (Morinda citrifolia fruit -positive control), group two received 2 mg/ml of MCF, group three received 1 mg/ml MCL (Morinda citrifolia leaf), group four received 2 mg/ml MCL, group five received 2 mg/ml coffee, group six received 2 mg/ml green tea and group seven was used as a negative control, which received the vehicle only. All animals were subjected to their respective treatments orally for 10 weeks.
  • the swimming endurance capacity was assessed once a week for 10 weeks. Weight (12% of mice body weight) was tied at each mice tail. The function of weight is to force the mice to swim to survive and prevent from submerging in water. Mice were forced to swim in acrylic plastic pool filled with water maintained at 20-22°C. The endurance was defined as the time they kept swimming actively until they submerged in water for 5 seconds, before immediately being rescued. All values were presented as means ⁇ SE. Comparison data was made by one-way ANOVA. Results with values of P ⁇ 0.05 were considered statistically significant.
  • FIG. 1 shows the swimming time to exhaustion throughout the experimental period. After 10 weeks, the swimming time for control mice were 47.6% longer than baseline.
  • Swimming times for mice treated with Morinda citrifolia leaf aqueous extract (MCL) 1mg/ml and 2mg/ml were 30.1 and 62.2% longer, respectively from control.
  • Mice treated with MCL 2mg/ml showed 38.8, 53.0, and 72.8% longer swim times compared to green tea, coffee and MCF 2mg/ml, respectively.
  • mice Female Balb/C mice, weighing between 18 to 25 g (5 to 7 weeks old) were kept at 22-25°C. Mice were fed with standard chow pellets (Gold Coins supplied by A Sapphire Enterprise, Malaysia) and water ad libitum. Green tea powder (15 g) was extracted with 500ml_ boiling water for 10 min. Extract was then filtered using Whatmann No. 1 filter paper. The animals were divided into six groups consisting of six animals per cage. The dosages used for the treatment were of low and high dose; 1 mg/ml and 2 mg/ml respectively (Morinda citrifolia) and 1 mg/ml for green tea group. Each group was treated with one treatment and the sixth group serves as negative control group. Exhaustive swim test
  • the mouse was placed in 20-25°C water in a container (21 cm ⁇ 15 cm). The swimming endurance of the mouse was observed and recorded. Swim time is defined as the length of time from entering the water to submersion for at least 5 seconds. The exhaustive swimming time is recorded for 6 weeks after the start of treatment.
  • Figure 2 shows the endurance effects of Morinda citrifolia leaves solvent extract on Balb/C mice using forced swim test for 6 weeks after treatment with low dose (MCLD) and high dose (MCHD) [ * p ⁇ 0.05 as compared to control group].
  • Green tea extract (GTE) group was given 1 mg/ml of green tea extract.
  • CTRL is a control group which was given distilled water only.
  • a concentrated cordial can be prepared from all these herbs as follows: 1. Leaves of Morinda spp and Orthosiphon spp were mixed in the ratio of 1 :1 to 1 :4
  • the water extract was then mixed with 2 kg of sugar and 500 ml of any fruit juice (e.g. orange) and added with 1.5 g methyl paraben as preservative. 4.
  • the above mixture was brought to boiling point, cooled and kept in an airtight bottle.
  • the above cordial concentrate can be diluted 1 :10 with water to be used as an ergogenic drink.
  • Figure 3 shows the comparative effects of Morinda and Orthosiphon herbs for improving endurance, performance and stamina in swimming tests. As shown in the figure, leaves of Morinda spp and Orthosiphon spp increased endurance swimming time of rats. Other herbs tested did not show this effect.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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Abstract

La présente invention concerne une composition destinée à prévenir la fatigue et améliorer la performance ou l'endurance athlétique, cette composition comprenant un extrait de plante de la famille des rubiacées et/ou des labiées. L'invention concerne également l'utilisation de cette composition dans la fabrication d'une préparation qui prévient la fatigue et améliore l'endurance ou la performance athlétique.
PCT/MY2014/000089 2013-06-28 2014-04-30 Composition pour améliorer l'endurance et la performance athlétiques WO2014209099A1 (fr)

Applications Claiming Priority (2)

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MYPI2013701127 2013-06-28
MYPI2013701127 2013-06-28

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WO2014209099A1 true WO2014209099A1 (fr) 2014-12-31

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005089384A (ja) * 2003-09-18 2005-04-07 Kao Corp 持久力向上剤
JP2007302571A (ja) * 2006-05-09 2007-11-22 Tokiwa Yakuhin Kogyo Kk 経口用組成物
JP2009209088A (ja) * 2008-03-04 2009-09-17 Kobayashi Pharmaceut Co Ltd アスペルロシドまたはその類縁体を含む筋肉増強剤
JP2012092028A (ja) * 2010-10-26 2012-05-17 Taisho Pharmaceutical Co Ltd 疲労回復剤

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005089384A (ja) * 2003-09-18 2005-04-07 Kao Corp 持久力向上剤
JP2007302571A (ja) * 2006-05-09 2007-11-22 Tokiwa Yakuhin Kogyo Kk 経口用組成物
JP2009209088A (ja) * 2008-03-04 2009-09-17 Kobayashi Pharmaceut Co Ltd アスペルロシドまたはその類縁体を含む筋肉増強剤
JP2012092028A (ja) * 2010-10-26 2012-05-17 Taisho Pharmaceutical Co Ltd 疲労回復剤

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