WO2014191009A1 - Pâte dentifrice comprenant de l'extrait de propolis - Google Patents

Pâte dentifrice comprenant de l'extrait de propolis Download PDF

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Publication number
WO2014191009A1
WO2014191009A1 PCT/EP2013/001565 EP2013001565W WO2014191009A1 WO 2014191009 A1 WO2014191009 A1 WO 2014191009A1 EP 2013001565 W EP2013001565 W EP 2013001565W WO 2014191009 A1 WO2014191009 A1 WO 2014191009A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition according
toothpaste composition
propolis
toothpaste
humectant
Prior art date
Application number
PCT/EP2013/001565
Other languages
English (en)
Inventor
Martha Herminia Pérez VIÑAS
Estela de los Angeles Gispert ABREU
Jorge Daniel García SALMAN
Original Assignee
Vitalgaia Sas
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 Vitalgaia Sas filed Critical Vitalgaia Sas
Priority to PCT/EP2013/001565 priority Critical patent/WO2014191009A1/fr
Publication of WO2014191009A1 publication Critical patent/WO2014191009A1/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • 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
    • A61K8/98Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of animal origin
    • A61K8/987Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of animal origin of species other than mammals or birds
    • A61K8/988Honey; Royal jelly, Propolis

Definitions

  • the present invention relates to a novel toothpaste formulation.
  • the invention relates to a toothpaste formulation comprising a soft extract of propolis.
  • Propolis is a resinous mixture collected by honey bees from tree buds, sap flows, broken bark or other botanical sources. Vegetable resins are collected by bees and carried to the hive by bees where the resins are mixed with wax to become into propolis.
  • the colour of propolis may vary depending upon, inter alia, its botanical source. Its colour can vary from yellow to black, including tones of brown and green.
  • Propolis is sticky at and above room temperature, 20°C (68 F). At lower temperatures, it can become hard and very brittle.
  • propolis is a natural and biologic product and is known to have a number of medical applications, including for example, as an antimicrobial, emollient, immunomodulator, anti- plaque dental agent, antitumor growth agent and a radioprotector. Although all types of propolis have similar properties, its effect may depend upon, inter alia, the source and type, among other factors.
  • the present invention provides a toothpaste composition that possesses antimicrobial, antifungal and/or anti-inflammatory properties. These properties make it useful for oral cleaning, prevention of dental caries, periodontopathies and candidiasis.
  • a toothpaste composition comprising from 0.5% w/w to 2% w/w of soft extract of propolis wherein the soft propolis extract comprises from 85 to 95% w/w of active material.
  • the toothpaste composition comprises from about 0.5% w/w to about 1.5% w/w of soft extract of propolis, i.e. from about 0.5g to about 1.5g of soft extract of propolis per lOOg of toothpaste, or from about 0.7% w/w to about 1.5% w/w of soft extract of propolis, i.e. from about 0.7g to about 1.5g of soft extract of propolis per lOOg of toothpaste, or from about 0.8% w/w to about 1% w/w of soft extract of propolis, i.e. from about 0.8g to about lg of soft extract of propolis per lOOg of toothpaste.
  • R is the weight of residue after extraction of the raw propolis [obtained after alcohol evaporation]
  • PSE is the weight of the soft extract.
  • C% should be from about 85% to about 90% w/w.
  • the toothpaste of the invention generally does not require other conventionally used additives, such as, extracts of natural fruit juices, traditional Chinese components, weed extracts, etc. More specifically, the toothpaste of the invention does not contain other additives such as extract of natural fruit juice, traditional Chinese components, weed extracts with coenzyme Q10, extract of pommel seeds, particles of silver and gold, cane and bamboo salt dust, dust of ganoderma, natural sericite, zeolite", dust of green algae, snakes or pearls, carrageen, aloe, farnesol and xylitol, xanthan gum, lemon (essential) oil, tocopherol, pyranose, perfume and/or fluoride.
  • other additives such as extract of natural fruit juice, traditional Chinese components, weed extracts with coenzyme Q10, extract of pommel seeds, particles of silver and gold, cane and bamboo salt dust, dust of ganoderma, natural sericite, zeolite", dust of green algae, snakes or pearls, carrageen,
  • raw propolis is a complex combination of as many as 180 different compounds created from the materials collected by honeybees. The raw materials are further transformed by the bee's saliva as they are harvested and mixed with beeswax when taken back to the beehive.
  • the toothpaste composition of the invention may include one or more humectants. It will be understood by the person skilled in the art that a humectant is a generally hygroscopic substance used to help a product retain water.
  • a humectant When a humectant is present in the toothpaste composition of the invention it will generally be in an amount of from about 10 to about 30% w/w, or about 15 to about 25% w/w, for example about 20% w/w.
  • a variety of humectants may be used in the toothpaste composition and it will be understand that more than one humectant may be used.
  • the humectant used in accordance with the invention is typically a polyol, in particular a polyol selected from glycerol, sorbitol, propylene glycol, xylitol, lactitol, or mixtures thereof. Sorbitol is especially useful as a humectant since it may also function as a sweetener.
  • Preferred humectants include one or more of propylene glycol and sorbitol. Preferably, a combination of propylene glycol and sorbitol are used.
  • propylene glycol is used as a humectant it is preferably present in an amount of from about 0.5 to about 10% w/w; from about 1 to about 9% w/w; from about 2 to about 8% w/w; from about 3 to about 7% w/w; from about 4 to about 6% w/w; from about 4.5 to about 5.5% w/w; for example 5% w/w.
  • sorbitol When sorbitol is used as a humectant it is preferably present in an amount of from about 1 to about 30% w/w; from about 5 to about 25% w/w; from about 10 to about 20% w/w; from about 11 to about 19% w/w; from about 12 to about 18% w/w; from about 13 to about 17% w/w; from about 14 to about 16% w/w; from about 14.5 to about 15.5% w/w; for example 15% w/w.
  • the toothpaste composition of the invention may include one or more abrasives, e.g.
  • particulate abrasive material such as a silica, alumina, calcium carbonate, dicalcium phosphate, calcium pyrophosphate, hydroxyapatite, trimetaphosphate, insoluble hexametaphosphate, or mixtures thereof.
  • a preferred abrasive material is precipitated calcium carbonate.
  • the amount of abrasive material may be from about 1 to about 60% w/w; from about 5 to about 55% w/w; from about 10 to about 50% w/w; from about 15 to about 45% w/w; from about 20 to about 40% w/w; from about 25 to about 35% w/w; for example 30% w/w.
  • the toothpaste composition of the invention may include one or more thickening agents.
  • thickening agents include, but shall not be limited to carboxylated polysaccharides.
  • Carboxylated polysaccharides include a cellulose derivative, in particular a carboxyalkyl cellulose, and especially carboxymethylcellulose (CMC), typically used as its sodium salt (SCMC).
  • CMC carboxymethylcellulose
  • SCMC sodium salt
  • the amount of thickening agent may be from about 0.5 to about 2 % w/w; be from about 0.5 to about 1.9 % w/w; from about 0.6 to about 1.8 % w/w; from about 0.7 to about 1.7% w/w; from about 0.8 to about 1.6% w/w; from about 0.9 to about 1.5% w/w; from about 1 to about 1.4% w/w; from about 1.1 to about 1.3% w/w; for example 1.2% w/w.
  • the toothpaste of the present invention is advantageous in that, inter alia, it has antibacterial properties.
  • the toothpaste has antibacterial properties against gram positive bacteria.
  • the toothpaste of the invention is effective against one or more of Staphylococcus aureus, Bacillus cereus, Micrococcus luteus, Enterococcus faecalis, Staphylococcus epidermidis and Staphylococcus aureus (MRS A) (see Table 1).
  • the propolis extract used in the toothpaste of the invention will generally comprise othe propolis extract used in the toothpaste of the invention will generally include one or more of the isoflavonoids isoliquiritigenin, liquiritigenin, formononetin, biochanin A, vestitol and pterocarpans (see Table 2).
  • the propolis extract used in the toothpaste of the invention will generally comprise prenylated benzophenones
  • the propolis extract used in the toothpaste of the invention will generally include one or more of the prenylated benzophenones, selected from the group including nemorosone, propolona A and guttiferone (see Table 3).
  • the propolis extract used in the toothpaste of the invention will generally comprise othe propolis extract used in the toothpaste of the invention will generally include one or more of the triterpenes selected from the group including one or more of ⁇ -amyrin, lupeol, j-amyrin, cycloartenol and lupeol acetate (see Table 4).
  • plaque buffers such as urea, calcium lactate, calcium glycerophosphate and strontium polyacrylates
  • desensitising agents such as potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salts; anti-calculus agents, such as alkali-metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates and phosphocitrates;
  • bio-molecules such as bacteriocins, antibodies, and enzymes
  • proteinaceous materials such as collagen
  • sweetening agents such as saccharin and sorbitol (vide supra);
  • bleaching agents such as peroxy compounds (e.g. potassium peroxydiphosphate); buffers and salts to buffer the pH and ionic strength of the composition; and pharmaceutically acceptable carriers, e.g. starch, sucrose, water or water/alcohol systems.
  • Water is a particularly preferred pharmaceutically acceptable carrier and is typically present in compositions of the invention at from 10 to 40%, in particular 15 to 35%, and especially at from 20 to 30% w/w of the total composition.
  • a toothpaste composition comprising from 0.5% w/w to 2% w/w of soft extract propolis, as hereinbefore described, a humectant, an abrasive and a thickening agent.
  • a method of cleaning teeth comprising brushing with a toothpaste composition comprising from 0.5% w/w to 2% w/w of soft extract propolis as hereinbefore described.
  • a method of cleaning teeth comprising brushing with a toothpaste composition comprising from 0.5% w/w to 2% w/w of soft extract propolis, as hereinbefore described, a humectant, an abrasive and a thickening agent.
  • the present invention also provide a method of treatment or prevention of one or more of dental caries, periodontopathies and candidiasis which comprise the use a toothpaste composition as hereinbefore described.
  • the present invention also provides a method of preparing a toothpaste composition as hereinbefore described which comprises mixing from 0.5% w/w to 2% w/w of a soft extract propolis with a humectant, an abrasive and a thickening agent.
  • the invention further provides a method of preparing a soft extract of propolis for use in a toothpaste composition or a method as hereinbefore described which comprises the extraction of raw propolis with an alcohol.
  • the soft extract of propolis may be prepared by the extraction of raw propolis with alcohol, such as ethanol.
  • the raw propolis is mascerated, comminuted or otherwise deagglomerised into particles which generally have a diameter of about 1cm or less. It will be understood by the person skilled in the art that the treated raw propolis will have a particle size distribution such that >75% w/w of the propolis particles have diameter of about 1cm or less.
  • the particle size distribution of the comminuted raw propolis may vary and may be such that >76% w/w of the propolis particles have diameter of about 1cm or less; or >77% w/w of the propolis particles have diameter of about 1cm or less; or >78% w/w of the propolis particles have diameter of about lcm or less; or >79% w/w of the propolis particles have diameter of about 1cm or less; or >80% w/w of the propolis particles have diameter of about lcm or less; or >85% w/w of the propolis particles have diameter of about lcm or less; or >90% w/w of the propolis particles have diameter of about lcm or less; or >95% w/w of the propolis particles have diameter of about lcm or less.
  • a method of preparing a soft extract of propolis which comprises comminuting raw propolis into particles such that >75% w/w of the propolis particles have a diameter of about lcm or less.
  • the raw propolis may be frozen, for example to about -20°C, in order to aid the comminution of the raw propolis into the particles as hereinbefore described.
  • the procedure for the manufacture of a soft extract of propolis is described in more detail.
  • a soft extract of propolis is the end product obtained by selective extraction of the active substances from propolis raw material.
  • a 70% v/v ethanol/ water mixture is preferably used as solvent, to obtain a viscous product comprising from about 85 to about 90% w/w of propolis in ethanol/ water.
  • a quality-graded soft extract should be perfectly soluble in 70% ethanol/ water, without solid waste materials.
  • the yield of the process may vary, depending upon, inter alia, the propolis type or source, according its content of wax and residuals.
  • a mean yield of lOOg of soft extract per kg of raw propolis is estimated.
  • the soft extract of propolis may be purified using the Pichansky method. Thus, for example, the gross (or raw) propolis may be macerated in an ethanol/ water solution.
  • Gross (or raw) propolis VS alcohol based on % of weight/volume is used. The final quality of the product is observed through the presence of total solids.
  • the first extraction is gross propolis 50 kg and alcohol at 70% v/v (ethanol/ water mixture), filtered at a low concentration csp 100 litres. In subsequent extractions, residual propolis is used with 70% v/v ethanol.
  • Soft propolis extract is obtained by selective extraction of the active substances of propolis raw material by 70° proof ethanol (i.e. 40% ethanol/water mixture), used as solvent, to obtain a viscous product with a concentration between 85 and 90 % w/w of propolis, the remainder being made ethanol and water.
  • a soft quality summary must be perfectly soluble in 70° proof ethanol, without generating solid residues.
  • Raw propolis (of organic quality) was collected by beekeepers through a method of scraping. Desirably the propolis does not have detectable traces of wax or mechanical impurities and does not show any signs of degradation.
  • the raw propolis can be stored at from 5 to 10°C, protected from light and moisture, for example, in plastic bottles (latex should be avoided).
  • RP weight of raw propolis to be processed Propolis pieces will be reduced to particles of about 1cm in diameter or less, by means of grinding. If necessary, the propolis can be frozen, prior to grinding, to about -20°C.
  • a crusher employed will generally be a double walled bowl.
  • a warm fluid e.g. water
  • a system of rotating mixing is provided inside the crusher.
  • the crushed or fragmented raw propolis (weight of RP) is mixed with ethanol in a proportion of about 1 litre of ethanol per 600g of raw propolis.
  • the mixture is shaken or stirred at about 50 rpm and then cooled to about 15°C. 3.
  • the mixture is then filtered using a tissue filter under vacuum. It is important that the filtering process is conducted at room temperature (e.g. about 20°C) with a cooled solution, ensuring that all wax is precipitated by solidification. If the mixture is too warm, this can give rise to a risk of wax being transferred to the solution of the raw propolis extract.
  • room temperature e.g. about 20°C
  • the filtered extract is concentrated by means of vacuum evaporation, recovering most of the alcohol from the solution.
  • the extract is concentrated in a vacuum evaporator at a temperature below 50°C, ensuring the quality of the end product.
  • the soft extract is weighted.
  • PSE is the weight of the soft extract.
  • the content of active material C% of the produced soft extract will be:
  • This value should be from about 85% to about 90% w/w.
  • Propolis soft extract should be pasty and sticky, like a glue.
  • the extract may be runny or too liquid. If the alcohol content is too low then the extract may tend to solidify and become hard and unsuitable for use in a toothpaste formulation.
  • Concentration factor of raw propolis related to PSE will be:
  • Each lOOg contains:

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Zoology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition de pâte dentifrice comprenant de 0,5 % en masse à 2 % en masse d'extrait de propolis mou, l'extrait de propolis mou comprenant de 85 à 95 % en masse de matière active.
PCT/EP2013/001565 2013-05-28 2013-05-28 Pâte dentifrice comprenant de l'extrait de propolis WO2014191009A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/EP2013/001565 WO2014191009A1 (fr) 2013-05-28 2013-05-28 Pâte dentifrice comprenant de l'extrait de propolis

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2013/001565 WO2014191009A1 (fr) 2013-05-28 2013-05-28 Pâte dentifrice comprenant de l'extrait de propolis

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WO2014191009A1 true WO2014191009A1 (fr) 2014-12-04

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105012182A (zh) * 2015-07-23 2015-11-04 贵阳中医学院 一种抗炎牙膏及其制作方法
CN113274384A (zh) * 2021-06-02 2021-08-20 北京中医药大学 驴食草酚在制备防治溃疡性结肠炎的药物中的应用及其药物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6027716A (en) * 1997-04-02 2000-02-22 Farmo-Nat Ltd. Synergistic herbal extracts
WO2012029015A2 (fr) * 2010-08-31 2012-03-08 Universidad De La Frontera Composition dentifrice anticariogène comprenant de la propolis comme principe actif anticariogène
US20120288454A1 (en) * 2010-11-25 2012-11-15 Wenzhong Zhao Dental protection toothpaste composition

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6027716A (en) * 1997-04-02 2000-02-22 Farmo-Nat Ltd. Synergistic herbal extracts
WO2012029015A2 (fr) * 2010-08-31 2012-03-08 Universidad De La Frontera Composition dentifrice anticariogène comprenant de la propolis comme principe actif anticariogène
US20120288454A1 (en) * 2010-11-25 2012-11-15 Wenzhong Zhao Dental protection toothpaste composition

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE GNPD [online] MINTEL; April 2013 (2013-04-01), "Salt Clinic Toothpaste", XP002720509, Database accession no. 20426887 *
DATABASE GNPD [online] MINTEL; March 2013 (2013-03-01), "Propolis Herbal & Mineral Toothpaste", XP002720508, Database accession no. 2013782 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105012182A (zh) * 2015-07-23 2015-11-04 贵阳中医学院 一种抗炎牙膏及其制作方法
CN113274384A (zh) * 2021-06-02 2021-08-20 北京中医药大学 驴食草酚在制备防治溃疡性结肠炎的药物中的应用及其药物

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