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WO2017020138A1 - Formulation topique cosmétique à base d'extraits naturels pour le traitement du fibro- oedème géloïde muqueux sous-cutané - Google Patents

Formulation topique cosmétique à base d'extraits naturels pour le traitement du fibro- oedème géloïde muqueux sous-cutané Download PDF

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Publication number
WO2017020138A1
WO2017020138A1 PCT/CL2015/000038 CL2015000038W WO2017020138A1 WO 2017020138 A1 WO2017020138 A1 WO 2017020138A1 CL 2015000038 W CL2015000038 W CL 2015000038W WO 2017020138 A1 WO2017020138 A1 WO 2017020138A1
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WO
WIPO (PCT)
Prior art keywords
treatment
cellulite
topical formulation
extract
topical
Prior art date
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Ceased
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PCT/CL2015/000038
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English (en)
Spanish (es)
Inventor
Jorge Iván SANHUEZA SEPÚLVEDA
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Individual
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Individual
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Priority to PCT/CL2015/000038 priority Critical patent/WO2017020138A1/fr
Publication of WO2017020138A1 publication Critical patent/WO2017020138A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis

Definitions

  • Subcutaneous geloid fibroedema is the medical term with which cellulite is called, although it should be noted that other terms also accepted in the medical area are used such as: degenerative edematous panniculitis, liposclerosis, panniculosis.
  • Subcutaneous geloid fibroedema is a type of lipodystrophy widely considered an aesthetic disorder of the skin (dermisepidermis and hypodermis), whose alteration is based on a morphological disorder of fat tissue cells. It is mainly characterized by an alteration in the circulation of blood and lymphatic system, causing structural changes in subcutaneous adipose tissue, collagen, proteoglycans and adjacent tissues.
  • cellulite is 85-98% in women of all races.
  • Cellulite is a problem that affects young or middle-aged, thin or overweight women. It manifests itself after puberty, hormonal, nutritional and emotional factors directly influence its appearance.
  • the alteration is a constitutional morphological disposition, without significant changes both histopathological and biological, of only aesthetic implication, the patient leads a normal life and does not present general symptomatology.
  • triggers and / or aggravating factors are added to the first condition, evolving towards stages with more serious alterations, whether clinical or histopathological, taking the patient to varying degrees of disability.
  • the data that support their participation in the pathogenesis of cellulite are: a) it is a pathology of the female sex, b) arises after puberty where it is intimately related to a critical production of fat mass that has as a triggering mechanism the bleeding menstrual, c) the direct or indirect relationship of female hormones during episodes of sexual life (menstruation, pregnancy, abortions, puerperium, lactation, pre-menopause and estrogen therapy) with progressive evolution to cellulite and d) by the interrelation of estrogens with other hormones that are also part of this series of factors.
  • Adjuvant factors Endogenous and exogenous, are those factors that directly or indirectly participate in the process both to provoke and aggravate it. They are classified as: endogenous those of biological origin and in exogenous environmental or aggregates, such as sedentary lifestyle, smoking, among others. There is currently enough evidence to ensure that the anatomy of the female adipose tissue contributes greatly to the appearance of cellulite, it is known that the fibrous tissue surrounding the adipocytes has a high percentage of septa in the perpendicular direction in the "problem" areas "of women with cellulite, unlike men, all this is corroborated by studies with magnetic resonance imaging.
  • the main problem of the genesis of cellulite is the microcirculatory alteration, with five stages in cellulite formation.
  • First stage It is not clinically evidenced. It is characterized by a slowing of the venous and lymphatic microcirculation. The vessels dilate and the blood stays in them longer than usual.
  • Second stage Due to the persistence of blood stasis and vasodilation, the wall of small venous and lymphatic vessels becomes more permeable by letting liquid out. It is what is called edematization of connective tissue.
  • Third stage Due to this blood stasis there is a transformation of the serous fluid into a denser geloid substance that hinders the exchange of nutrients between the vessels and the fat cells. These cells unable to shed their metabolites into the microcirculatory torrent, they hypertrophically increasing considerably in size, breaking up by spilling their fatty and toxic content abroad.
  • ⁇ Drainage It is focused on increasing capillary resistance, reducing its permeability and activating circulation, favoring the elimination of toxic substances and excess water by retention.
  • Collagen stiffness causes the appearance of cellulite like orange peel. If it is possible to reduce the intake of sugars or its fixation to the collagen is blocked, the stiffness decreases. Another way is to stimulate the synthesis of collagen responsible for skin elasticity using preparations of plant origin.
  • Fat reduction lipolysis: Here they recommend mineral salts and trace elements help to drain adipose tissue.
  • medical advice that are also recommended, such as food that aims to maintain a balanced diet in calories, protein, fruits, vegetables and vegetables that ensure a supply of vitamins and Enough minerals for the metabolism of our body. Physical exercise, which should be moderate and continuous focused to tone and not lose weight.
  • Centella asiatica extract is proposed, it is a plant of the Umbelliferae family native to India and Indonesia whose main property is to be anti-edematous, since it favors the tissue repair process by releasing the trapped fat cells. It is also used in the treatment of ulcers of vascular origin. Research results indicate that it can be used in the treatment of skin photoaging, cellulite and stretch marks. It has also been reported that Ruscus, a sharp-leaved shrub found in the Mediterranean regions, has vasoconstrictive effects, prevents capillary fragility, anti-edematous, anti-inflammatory activity and is used as an adjuvant in anti-cellulite treatment.
  • TEA-hydroiodide triethanolamine hydroiodide
  • US patent US4795638 refers to a cosmetic composition that can reduce or eliminate cellulite fat accumulation in the human body.
  • the composition includes at least one rubefacient, at least one soluble plant extract oil and at least volatile polysiloxane.
  • the ingredients are contained in an oily base which can be of animal or vegetable origin and mineral oil or synthetic oils or mixtures thereof.
  • the rubefacient substance that is used includes Capsicum extract, salts, esters and nicotinic acid alcohols.
  • the soluble oil can be from the extract of: Hedera helix, ginseng, hiperycum, seaweed in any combination.
  • the Romanian patent R0121583 describes a gel for the care of the anti-cellulite, revulsive, anti-inflammatory body, with vasodilator effect, in addition to the preparation process.
  • the gel comprises: Herald helix extract, chestnut extract, paprica tincture (Capsicum), peppermint essential oil, lavender essential oil, rose essential oil and sage oil, embedded and stabilized in a gel base.
  • the claimed process consists in the sequence of stages of the natural mixing of the compounds by stirring.
  • the technology presented in this invention patent differs from the technology proposed in the formulation and process, despite the fact that its elaboration includes the use of chili pepper extract. The differences are obvious.
  • the patent application US2012219621 of the North American Patent Office, describes a composition with an improved thermogenic activity and the use of said composition in the prevention and treatment of obesity.
  • the pharmaceutical composition that is used for the treatment and prevention of overweight, obesity and metabolic syndrome comprises: menthol or peppermint essential oil in association with one or more components having thermogenic activity selected from capasaicin or capsinoids derived from Capsicum extract, active substance containing sulphides derived from Allium extract and active catechins derived from Camellia extract.
  • the technology presented in this patent application differs from the technology proposed in this document, basically in the formulation, they are totally different despite the fact that it includes the use of chili pepper extract. The differences are obvious.
  • the Chinese patent CN102743547 provides a weight reduction composition with obesity preventive effect and a weight reduction solution.
  • the composition comprises yellow pepper extract, green tea extract, lotus leaf extract.
  • the invention has the following beneficial effects: it promotes intestinal peristalsis, cardiac and gastrointestinal tract protection.
  • the technology presented in this Chinese patent differs from our technology in the formulation via administration and final objective, although its elaboration includes garlic extract. The differences are obvious.
  • the Korean patent application KR2011127454 refers to an anti-obesity composition containing a species of corn and edible fungi Lentinus edodes, which provides a suppressor of the increase in glucose and the increase in adiposity.
  • the composition includes among its ingredients Capsicum annum extract. A method for preparing said formulation is also protected. The purpose of the technology proposed in this patent is totally different from what you want to protect.
  • Figure N ° 1 Patient record 6 at time 0 day (A), at 5 days (B), at 10 days (C) and at 15 days of treatment (D) in the area of the left thigh.
  • the present invention describes a topical formulation comprising a mixture, comprising at least terpenes, phenolic compounds and alkaloids of extracts from Ugni molinae (murta) and Capsicum spp. (chili), respectively, preferably capsaicinoids, capsinoids and saponins, for the treatment of subcutaneous geloid fibroedema, better known as orange peel and / or cellulite.
  • chili pepper, Capsicum spp. It corresponds to an introduced species, an easily cultivated shrub, does not require special substrates, is not affected by pests, and depending on the species can be biannual.
  • the murtilla, Ugni molinae is a native species, an evergreen shrub, of spontaneous growth and resistant to pathogens. Both species are widely distributed in our country, without ecological restrictions. Given this background, a formulation was developed, effective based on extracts of chili fruits and murtilla leaves for the treatment of subcutaneous mucous geloid fibroedema (orange peel).
  • This formulation was carried out by characterizing, separately, hydroalcoholic extracts and also extracted with mixtures of water-propanediol, water-propanediol-ethanol in different proportions from murtilla and chili pepper, and subsequently, the mixture was made and incorporated into a base gel as a vehicle for topical administration of the formulation. It should be considered that it can be used as an administration vehicle in addition to the gel, a cream, a lotion, etc.
  • Example No. 1 Obtaining the raw material
  • Branches of Murta "Ugni molinae” were collected in the Tenth Region, near the sector called Ensenada and in the Ninth Region, in the area comprised of Gorbea, Lastarr ⁇ a costs in Chile. In both cases, they were species that grew wild in forest renewals and inside the native forest of the area. The collection was made at different times of the year, corresponding to flowering, fruit and dormancy states; in adult plants in full development and reproduction with strong development of secondary metabolites.
  • the dried and pulverized leaves of "Ugni molinae" murta were extracted in a mixture of 40:60 ethanohagua; 20:80 ethanol: water; 60:40 ethanol: water; 50:50 ethanol: water; 60:40 etanohagua; 80:20 ethanol: water; in a ratio between 1: 6; 1: 10; biomass: solvent, at temperatures between 10 ° C and 30 ° C, for a period of 5 to 15 days until material depletion.
  • the biomass was separated from the extract by filtration with housings between 200 and 0.2 microns and centrifuged between 400 and 1600 rpm and 200 to 0.2 microns.
  • Formulas were developed using a base gel, to test in the volunteers, with different concentrations of active compounds, in ranges of at least 0.20% to 5%, maintaining the base.
  • the formulation with lower concentration of assets was tested, since in this way it could be known first that a formulation with a higher concentration of agents should have a better result; This also ensured the test with adequate concentrations to avoid " potential irritation problems " or any unwanted conditions in the volunteers.
  • the gel base formula is summarized in the following table:
  • a base gel is manufactured as a vehicle with the following concentration range of the extracts:
  • the M3 extract is a hydroalcoholic extract of Capsicum spp standardized in capsaicin, in a range between 14% to 20%, preferably 17.3%; where he active ingredient comprises at least the capsaicinoid active, in a concentration range between 0.05% to 2%, preferably 0.15%.
  • Extract M is a hydroalcoholic extract of Ugni molinae standardized in equivalents of quercetin, in a range between 14% to 20%, preferably 16.4%; where the active ingredient comprises at least pentacyclic triterpenic saponins in a concentration range between 0.01% to 2%, preferably 0.05%.
  • the product was applied to previously exfoliated skin, in the affected area with circular movements for 3 minutes, twice a day for a period of 15 days.
  • the following dermatological parameters were studied:

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Botany (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medical Informatics (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne une formulation topique cosmétique qui comprend des composés actifs, des capsaïcinoïdes et saponines, provenant respectivement d'extraits de fruits de Capsicum spp. et de feuilles de Ugni molinae; pour le traitement du fibro- oedème géloïde muqueux sous-cutané (cellulite). La synergie des deux extraits assure une efficacité qui n'avait jamais été observée auparavant, en raison du mécanisme d'action que possèdent les composés actifs, présents dans l'extrait du fruit de Capsicum spp. et les feuilles de Ugni molinae, qui sont utiles dans cette affection; ce qui constitue une solution de remplacement topique efficace.
PCT/CL2015/000038 2015-08-03 2015-08-03 Formulation topique cosmétique à base d'extraits naturels pour le traitement du fibro- oedème géloïde muqueux sous-cutané Ceased WO2017020138A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/CL2015/000038 WO2017020138A1 (fr) 2015-08-03 2015-08-03 Formulation topique cosmétique à base d'extraits naturels pour le traitement du fibro- oedème géloïde muqueux sous-cutané

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CL2015/000038 WO2017020138A1 (fr) 2015-08-03 2015-08-03 Formulation topique cosmétique à base d'extraits naturels pour le traitement du fibro- oedème géloïde muqueux sous-cutané

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4795638A (en) * 1984-11-16 1989-01-03 L'oreal Thermo slimming cosmetic composition
WO2006086764A2 (fr) * 2005-02-11 2006-08-17 The Board Of Supervisor Of Louisiana State University Agricultural And Mechanical College Procedes et composes pour le traitement de l'obesite et des troubles lies a l'obesite
KR101105542B1 (ko) * 2010-12-10 2012-01-13 이경록 슬리밍 화장료 조성물

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4795638A (en) * 1984-11-16 1989-01-03 L'oreal Thermo slimming cosmetic composition
WO2006086764A2 (fr) * 2005-02-11 2006-08-17 The Board Of Supervisor Of Louisiana State University Agricultural And Mechanical College Procedes et composes pour le traitement de l'obesite et des troubles lies a l'obesite
KR101105542B1 (ko) * 2010-12-10 2012-01-13 이경록 슬리밍 화장료 조성물

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"MURTA CELULITIKA.", 25 June 2015 (2015-06-25), Retrieved from the Internet <URL:http://www.yapo.cl/region_metropolitana/salud-belleza /termogel_reductivo_y_anticelulitis murta_20082824.htm> *
CARO ET AL.: "Determinaciôn de la efectividad de una formulaciôn cosmética en base a un extracto de las hojas de Ugní Molinae Turc z. (Murtilla) en el tratamiento de la lipodistrofia (celulitis)''.", TESIS DE QUÍMICO FARMACÉUTICO. UNIVERSIDAD DE CHILE, FACULTAD DE CIENCIAS QUÍMICAS Y FARMACÉUTICAS, 2009, Retrieved from the Internet <URL:http://catalogo.uchile.cl/uhtbin/cgisir i/x/O/0/57/5/3?searchdata1 =671330{CKEY} amp; searchfield1 =GENERALASUBJECTAGENERA AA&user_id=WEBSERVER> *
OESTERHELD, P. ET AL.: "Desarrollo de una formulaciôn en base a extracto de Capsicum spp. para el tratamiento del síndrome de piel de naranja.", REV. FARMACOL. CHILE, vol. 5, no. 3, 2012, Villarrica, Chile, pages 64 *

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