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WO2014089646A1 - Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur - Google Patents

Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur Download PDF

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Publication number
WO2014089646A1
WO2014089646A1 PCT/BR2012/000514 BR2012000514W WO2014089646A1 WO 2014089646 A1 WO2014089646 A1 WO 2014089646A1 BR 2012000514 W BR2012000514 W BR 2012000514W WO 2014089646 A1 WO2014089646 A1 WO 2014089646A1
Authority
WO
WIPO (PCT)
Prior art keywords
paullinia cupana
product
treatment
prevention
hot flushes
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/BR2012/000514
Other languages
English (en)
Portuguese (pt)
Inventor
Auro Del GIGLIO
Luiz Francisco Pianowski
João Batista CALIXTO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to BR112015010750-8A priority Critical patent/BR112015010750B1/pt
Priority to PCT/BR2012/000514 priority patent/WO2014089646A1/fr
Publication of WO2014089646A1 publication Critical patent/WO2014089646A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/77—Sapindaceae (Soapberry family), e.g. lychee or soapberry
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to the use of Paullinia cupana products in the preparation of medicaments for the prevention or treatment of hot flushes, particularly related to cancers and menopause. Also subject to the present invention are medicines containing the same and method for treating hot flushes.
  • Hot flashes are defined as transient periods of intense heat in the upper body, arms and face, often accompanied by flushing, vasodilation, sweating, anxiety, irritability, insomnia, depression, change in concentration and increased frequency. heart
  • Hot flushes are common in breast cancer patients, affecting about two thirds of them, and may contribute to the aggravation of other unwanted occurrences such as fatigue, depression, anxiety, sleep and quality of life. It also affects a high percentage (over 50%) of women in the transition period to menopause.
  • Intensity, duration and persistence vary among patients and seem to be influenced by emotional changes such as anxiety or stress, systemic diseases, neurological disorders, food and drink intake, especially alcohol and drugs, among others.
  • thermoregulatory center and hormone levels have already been pointed out.
  • Predisposing factors were studied in addition to hormonal levels, race, body mass index, smoking, tubal ligation and surgical menopause.
  • Figure 1 shows the measurement of hot flushes per day after a study with 15 patients who took guarana powder.
  • Figure 2 shows the severity score per week throughout the study for the same group of patients.
  • the present invention relates to the use of Paullinia cupana (guarana) product products in the prevention or treatment, as well as the preparation of medicaments for the prevention or treatment of hot flushes, particularly related to cancer and menopause.
  • “Paullinia cupana products” include, without limitation, derivatives obtained directly or indirectly from any part of the plant, including leaves, fruits or roots.
  • the present invention contemplates as a product of Paullinia cupana, guarana powder, obtained by methods known to the man of the art, which employ the milling of Paullinia cupana seed, which has been previously roasted and peeled, as mentioned in Publication by Oliveira J ⁇ nior et al: Regional Potentials Project, Economic Feasibility Study, Guarana, ISAE Higher Institute of Administration and Economics / Get ⁇ lio Vargas Foundation (FGV), 2003, incorporated herein by reference.
  • the present invention also contemplates as a product of Paullinia cupana active fractions derived from Paullinia cupana or Paullinia cupana seed powder.
  • the present invention contemplates an active fraction of Paullinia cupana containing an average theobromine content ranging from about 0.05 to about 1 wt%, particularly about 0.1 wt%, and particularly about 10 to about 20% by weight of caffeine as described in International Patent Application WO2012129629, incorporated herein by reference.
  • hot flushes are transient episodes of intense heat.
  • treatment efficacy is meant that the number of these episodes should decrease by at least 50% with a given treatment, as well as their intensity.
  • Paullinia cupana product may be supplied directly to the patient or may be delivered in appropriate pharmaceutical
  • the present invention also relates to pharmaceutical compositions containing the active moiety according to the present invention or medicaments containing the same.
  • compositions according to the present invention may be liquid, semi-solid or solid and may be adapted for any enteral or parenteral administration route, with immediate or modified release.
  • said pharmaceutical composition is adapted for oral administration, particularly in the form of tablets or capsules.
  • Suitable pharmaceutically acceptable excipients according to the present invention are, for example and without limitation, those cited in Remington's Pharmaceutical Sciences, Mack Publishing, American or European Pharmacopoeia or Brazilian Pharmacopoeia.
  • the present invention further relates to a method for the prevention or treatment of hot flushes, particularly cancer or menopause, which is to provide a Paullinia cupana product according to the present invention to a patient in need.
  • An amount of the active fraction according to the present invention was prepared using 2 kg of guarana powder.
  • the guarana powder was extracted on a mechanical stirrer with 4 liters of a mixture of ethanol and 70:30 water for 1 hour at full speed.
  • the obtained product was filtered through a Buckner funnel, obtaining the first intermediate fraction.
  • the filter residue was then extracted with 2 liters of 70:30 ethanol and water for 1 hour at full speed.
  • the obtained product was filtered, also in a Buckner funnel, obtaining the second intermediate fraction.
  • the two intermediate fractions were mixed and dried on a rotary evaporator, yielding about 500 grams of the active fraction according to the present invention.
  • the 500 grams of the active fraction according to the present invention was subjected to HPLC analysis (High Performance Liquid Chromatography) to determine the theobromine and caffeine contents.
  • the analytical curve was prepared by weighing about 10 mg of the theobromine and caffeine analytical standards in 25 mL volumetric flasks and bulging with the mobile phase. From these stock solutions, successive dilutions were made to construct the analytical curve for the standards, filtered through 0.45 ⁇ membrane and injected into a chromatograph.
  • the samples were prepared by analytically weighing about 50mg of the sample in a 25mL volumetric flask and completing the volume with the mobile phase, filtering through 0.45 ⁇ membrane and injecting into the chromatograph.
  • LC-DAD Waters Alliance LC-DAD system consisting of 2695 pump, column heater, 2996 diode array detector and Empower ® software (Empower Software Solutions, Inc, US).
  • the average content of theobromine in the active fraction sample according to the present invention was 0.096% and the average caffeine content was 16.16%.

Landscapes

  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Mycology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne l'utilisation de produits de Paullinia cupana dans la préparation de médicaments pour la prévention ou le traitement des bouffées de chaleur associées notamment aux cancers et à la ménopause. La présente invention concerne également des médicaments contenant un tel produit, ainsi qu'une méthode pour traiter les bouffées de chaleur.
PCT/BR2012/000514 2012-12-13 2012-12-13 Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur Ceased WO2014089646A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
BR112015010750-8A BR112015010750B1 (pt) 2012-12-13 2012-12-13 Uso de produto de paullinia cupana
PCT/BR2012/000514 WO2014089646A1 (fr) 2012-12-13 2012-12-13 Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/BR2012/000514 WO2014089646A1 (fr) 2012-12-13 2012-12-13 Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur

Publications (1)

Publication Number Publication Date
WO2014089646A1 true WO2014089646A1 (fr) 2014-06-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/BR2012/000514 Ceased WO2014089646A1 (fr) 2012-12-13 2012-12-13 Utilisation de produits de paullinia cupana dans la prévention ou le traitement des bouffées de chaleur

Country Status (2)

Country Link
BR (1) BR112015010750B1 (fr)
WO (1) WO2014089646A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020115475A1 (fr) * 2018-12-04 2020-06-11 Phytoquest Limited Produits phytochimiques bioactifs dans zizyphus et guarana

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012129629A1 (fr) * 2011-03-31 2012-10-04 Luiz Francisco Pianowski Fraction active de paullinia cupana à activité améliorée contre la fatigue, procédé de production d'une fraction active, utilisation, composition pharmaceutique, médicament et méthode de traitement de la fatigue

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012129629A1 (fr) * 2011-03-31 2012-10-04 Luiz Francisco Pianowski Fraction active de paullinia cupana à activité améliorée contre la fatigue, procédé de production d'une fraction active, utilisation, composition pharmaceutique, médicament et méthode de traitement de la fatigue

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BLAES, AH ET AL.: "Nonpharmacologic complementary therapies in symptom management for breast cancer survivors.", SEMINARS IN. ONCOLOGY, vol. 38, no. 3, 2011, pages 394 - 402 *
CAMPOS, MPO ET AL.: "Effect of guarana (Paullinia cupana) on fatigue in breast cancer patients undergoing systemic chemotherapy.", JOURNAL OF CLINICAL ONCOLOGY, vol. 28, no. 15, 2010 *
SUCHSHINSKAYA, OY.: "The effect of body mass index, physical activity and caffeine consumption on hot flashes in hispanic women.", DISSERTAÇÃO DE MESTRADO EM DIETÉTICA. BALL STATE UNIVERSITY, 2012, Retrieved from the Internet <URL:http://cardinalscholar,bsu.edu/bitstream/123456789/195952/SuchshinskayaO_2012-2_BODY.pdf> *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020115475A1 (fr) * 2018-12-04 2020-06-11 Phytoquest Limited Produits phytochimiques bioactifs dans zizyphus et guarana

Also Published As

Publication number Publication date
BR112015010750B1 (pt) 2021-06-01
BR112015010750A2 (pt) 2017-07-11

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