WO2022220045A1 - Composition pour cavité buccale - Google Patents

Composition pour cavité buccale Download PDF

Info

Publication number
WO2022220045A1
WO2022220045A1 PCT/JP2022/013661 JP2022013661W WO2022220045A1 WO 2022220045 A1 WO2022220045 A1 WO 2022220045A1 JP 2022013661 W JP2022013661 W JP 2022013661W WO 2022220045 A1 WO2022220045 A1 WO 2022220045A1
Authority
WO
WIPO (PCT)
Prior art keywords
monoterpene
weight
oral composition
composition
oral
Prior art date
Application number
PCT/JP2022/013661
Other languages
English (en)
Japanese (ja)
Inventor
忠杜 渋谷
Original Assignee
小林製薬株式会社
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 小林製薬株式会社 filed Critical 小林製薬株式会社
Publication of WO2022220045A1 publication Critical patent/WO2022220045A1/fr

Links

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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • the present invention relates to an oral composition containing a phenolic compound and having reduced irritation perceived when applied to the oral cavity.
  • Thymol (2-isopropyl-5-methylphenol) is known to permeate biofilms and exhibit bactericidal action, and is widely used in oral compositions such as dentifrices and mouthwashes.
  • Paraoxybenzoic acid esters are also widely used in oral compositions as preservatives.
  • Various reports have hitherto been made on formulation techniques for oral compositions containing phenolic compounds such as thymol and paraoxybenzoic acid esters.
  • Patent Document 1 a phenolic fungicide such as thymol or paraoxybenzoic acid ester, an anionic surfactant, and a nonionic surfactant are contained, and a nonionic interface to the anionic surfactant
  • An oral composition having a weight ratio of the active agent of 0.1 to 3 and a water content of 40% by weight or less prevents the phenolic disinfectant from adsorbing to the container, and prevents the phenolic disinfectant from It is described that the aging stability of is improved.
  • oral compositions containing phenolic compounds such as thymol and paraoxybenzoic acid esters have the drawback of causing irritation when applied to the oral cavity and reducing the feeling of use.
  • a method for reducing the irritation of oral compositions containing phenolic compounds a method of blending a sweetener such as saccharin sodium, stevia extract, erythritol, etc. as a taste masking agent is known.
  • a sweetener such as saccharin sodium, stevia extract, erythritol, etc.
  • an oral composition containing such a taste masking agent exhibits a sweet taste, and does not always give a satisfactory feeling during use.
  • An object of the present invention is to provide an oral composition that contains a phenolic compound and that suppresses irritation perceived when applied to the oral cavity.
  • the present inventors have made extensive studies to solve the above problems, and found that by including a monoterpene together with a phenolic compound in an oral composition, irritation caused by the phenolic compound can be suppressed.
  • the present invention has been completed through further studies based on such findings.
  • Section 1 An oral composition comprising a phenolic compound and a monoterpene.
  • Section 2. Item 2. The oral composition according to Item 1, wherein the phenol compound is thymol and/or paraoxybenzoic acid ester.
  • Item 3. Item 3.
  • Section 4. Item 4. The oral composition according to any one of items 1 to 3, wherein the monoterpene is contained in an amount of 0.01 to 100 parts by weight per 1 part by weight of the total amount of the phenolic compound.
  • Item 5. Item 5.
  • Item 5. The oral composition according to any one of Items 1 to 4, wherein the content of the monoterpene compound is 0.001 to 5% by weight.
  • Item 7. A method for suppressing irritation of an oral composition containing a phenolic compound, comprising: A method for suppressing irritation, comprising adding a phenolic compound and a monoterpene to an oral composition.
  • the present invention by including a monoterpene together with a phenol compound in the oral cavity composition, it is possible to suppress the stimulation of the phenol compound when applied to the oral cavity, and to provide an excellent feeling of use.
  • composition of the present invention is characterized by containing a phenolic compound and a monoterpene.
  • the composition for oral cavity of the present invention is described in detail below.
  • the oral composition of the present invention contains a phenolic compound.
  • a phenol compound is a general term for compounds having a phenol skeleton.
  • the type of phenol compound used in the present invention is not particularly limited as long as it is applicable to the oral cavity, but examples include thymol, paraoxybenzoic acid ester, and the like.
  • paraoxybenzoic acid esters include methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, isopropyl parahydroxybenzoate, and butyl parahydroxybenzoate.
  • phenol compounds may be used singly or in combination of two or more.
  • phenol compounds thymol, methyl parahydroxybenzoate, and ethyl parahydroxybenzoate are preferred.
  • the content of the phenolic compounds in the oral composition of the present invention may be appropriately set according to the type of phenolic compounds used, the form of the oral composition, etc.
  • the total amount of phenolic compounds is 0.001. ⁇ 5% by weight.
  • the total amount of phenolic compounds in the oral cavity composition of the present invention is preferably 0.005 to 2% by weight, more preferably 0.01 to 1% by weight, More preferably 0.05 to 0.3% by weight is mentioned.
  • the oral compositions of the present invention contain monoterpenes in addition to phenolic compounds.
  • the coexistence of a phenol compound and a monoterpene makes it possible to suppress the stimulation of the phenol compound.
  • a monoterpene is a known component that has a structure containing two isoprene units in its molecule and has a cooling effect.
  • the type of monoterpene used in the present invention is not particularly limited as long as it can be applied in the oral cavity.
  • Aldehyde monoterpenes such as citral, citronellal, perillaldehyde and safranal; ketone monoterpenes such as camphor, menthone, carbomentone and ionone; These monoterpenes may be d-, l-, or dl-forms when optical isomers are present. These monoterpenes may be used singly or in combination of two or more.
  • the monoterpene may be used in the form of an essential oil containing monoterpene.
  • the essential oil containing monoterpene can be appropriately selected from known ones and used.
  • Examples of essential oils containing menthol include peppermint oil, peppermint oil, and spearmint oil.
  • the description about the content and ratio of monoterpene in this specification is the value converted into the amount of monoterpene contained in the said essential oil, when using the essential oil containing a monoterpene.
  • These monoterpenes may be used singly or in combination of two or more.
  • ketone-based monoterpenes ketone-based monoterpenes, alcohol-based monoterpenes, and still more preferably camphor and menthol are preferred from the viewpoint of more effectively suppressing the irritation of phenolic compounds.
  • the ratio of monoterpene to phenolic compound may be appropriately set according to the type of phenolic compound and monoterpene used.
  • the total amount of monoterpene is 0.01 to 100 parts by weight.
  • the total amount of monoterpene per 1 part by weight of the total amount of phenolic compounds is preferably 0.1 to 30 parts by weight, more preferably 0.5 to 20 parts by weight. parts, more preferably 1 to 10 parts by weight.
  • the content of monoterpene in the oral composition of the present invention is, for example, 0.001 to 5% by weight. From the viewpoint of more effectively suppressing the stimulation of phenolic compounds, the content of monoterpene in the oral cavity composition of the present invention is preferably 0.01 to 3% by weight, more preferably 0.05 to 2% by weight. %, more preferably 0.1 to 1% by weight.
  • the oral composition of the present invention may further contain a monohydric lower alcohol.
  • the monohydric lower alcohol is not particularly limited as long as it can be applied in the oral cavity. mentioned. Among these monohydric lower alcohols, ethanol is preferred. These monohydric lower alcohols may be used singly or in combination of two or more.
  • the oral composition of the present invention contains a monohydric lower alcohol
  • the content is not particularly limited, but is, for example, 0.01 to 5% by weight, preferably 0.1 to 4% by weight, and more preferably. is 0.5 to 3% by weight.
  • the oral composition of the present invention may further contain a polyhydric alcohol.
  • Polyhydric alcohols are not particularly limited as long as they are applicable in the oral cavity, but examples include ethylene glycol, 1,3-butylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polypropylene glycol, glycerin and the like. Among these polyhydric alcohols, glycerin is preferred. These polyhydric alcohols may be used singly or in combination of two or more.
  • the oral composition of the present invention contains a polyhydric alcohol
  • the content is not particularly limited, but is, for example, 0.1 to 50% by weight, preferably 1 to 40% by weight, more preferably 10 to 50% by weight. 35% by weight.
  • the oral composition of the present invention preferably contains water as a base.
  • the content of water in the composition for oral use of the present invention may be the remainder excluding the components to be added, and is appropriately set according to the form of the composition for oral use, for example, 10 to 99.9. % by weight, preferably 15 to 99% by weight, more preferably 35 to 98% by weight, and even more preferably 40 to 88% by weight.
  • the oral composition of the present invention may contain components commonly used in the art according to the form of the oral composition within a range that does not impair the effects of the present invention. good.
  • Such components include, for example, antiseptics, disinfectants, antibacterial agents, antiphlogistic agents, abrasives, glucosyltransferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, anticalculus agents, dentin strengthening/regenerating agents. Calcifying agents, local anesthetics, blood circulation promoters, thickeners, humectants, sweeteners, pigments, deodorants, pH adjusters and the like.
  • the dosage form of the oral composition of the present invention is not particularly limited as long as it can be applied to the oral cavity, and examples thereof include liquid or semi-solid forms (gel, paste).
  • the form of the oral composition of the present invention is not particularly limited as long as it can be applied to the oral cavity and stay in the oral cavity for a certain period of time.
  • Dentifrices and mouthwashes are generally referred to as mouthrinses, mouthwashes, dental rinses, etc.), mouth fresheners (mouthsprays, etc.), and oral hygiene agents such as oral ointments.
  • mouthrinses mouthwashes
  • dental rinses, etc. mouth fresheners
  • oral hygiene agents such as oral ointments.
  • liquid dentifrices, toothpastes, and mouthwashes are preferred.
  • the present invention further provides a method for suppressing irritation of an oral composition containing a phenolic compound, comprising blending a phenolic compound and a monoterpene into the oral composition.
  • the type and amount of the phenol compound, the type and amount of the monoterpene, other components that can be blended and their amount, pH, oral dosage form, form, etc. are as described in "1. Composition” column.
  • Liquid formulations having the compositions shown in Tables 1 and 2 were prepared according to a conventional method. 500 ⁇ l of the resulting liquid preparation was placed in the mouth of an evaluator who had been trained in taste testing, and irritation was evaluated according to the following criteria. ⁇ Irritation Criteria> 6: No tingling sensation is felt on the tongue. 5: Almost no tingling sensation is felt on the tongue. 4: A slight tingling sensation is felt on the tongue after about 10 seconds have passed since putting it in the mouth. 3: A tingling sensation is felt on the tongue when about 5 seconds have passed since putting it in the mouth. 2: A tingling sensation is felt on the tongue about 2 to 3 seconds after putting it in the mouth. 1: A tingling sensation is felt on the tongue immediately after putting it in the mouth.
  • Production Example A toothpaste having the composition shown in Table 3 and a mouthwash having the composition shown in Table 4 were prepared.
  • the obtained toothpaste and mouthwash were used to confirm the irritation, and both of them showed reduced irritation caused by the phenolic compound.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Birds (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention a pour objet de fournir une composition pour cavité buccale qui contient un composé phénol, et qui est telle que parallèlement l'irritation perçue lors de sont application à l'intérieur de la cavité buccale est inhibée. Selon l'invention, un monoterpène est incorporé avec le composé phénol dans la composition pour cavité buccale, et l'irritation provoquée par le composé phénol, peut ainsi être inhibée.
PCT/JP2022/013661 2021-04-13 2022-03-23 Composition pour cavité buccale WO2022220045A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2021067881A JP2022162849A (ja) 2021-04-13 2021-04-13 口腔用組成物
JP2021-067881 2021-04-13

Publications (1)

Publication Number Publication Date
WO2022220045A1 true WO2022220045A1 (fr) 2022-10-20

Family

ID=83640575

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2022/013661 WO2022220045A1 (fr) 2021-04-13 2022-03-23 Composition pour cavité buccale

Country Status (3)

Country Link
JP (1) JP2022162849A (fr)
TW (1) TW202302067A (fr)
WO (1) WO2022220045A1 (fr)

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523355A (ja) * 1998-08-24 2002-07-30 ザ、プロクター、エンド、ギャンブル、カンパニー 口腔用液体粘膜粘着性組成物
JP2004238375A (ja) * 2003-02-10 2004-08-26 Earth Chem Corp Ltd 殺菌性口腔用組成物
JP2007031394A (ja) * 2005-07-29 2007-02-08 Lion Corp 液体口腔用組成物及びｌ−メントールの析出防止方法
JP2008143825A (ja) * 2006-12-08 2008-06-26 Lion Corp 歯磨組成物
JP2018002719A (ja) * 2016-06-27 2018-01-11 サンスター株式会社 口腔用組成物
JP2018095574A (ja) * 2016-12-09 2018-06-21 ライオン株式会社 口腔用組成物
JP2018100245A (ja) * 2016-12-21 2018-06-28 サンスター株式会社 口腔用及び／又は咽喉用組成物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523355A (ja) * 1998-08-24 2002-07-30 ザ、プロクター、エンド、ギャンブル、カンパニー 口腔用液体粘膜粘着性組成物
JP2004238375A (ja) * 2003-02-10 2004-08-26 Earth Chem Corp Ltd 殺菌性口腔用組成物
JP2007031394A (ja) * 2005-07-29 2007-02-08 Lion Corp 液体口腔用組成物及びｌ−メントールの析出防止方法
JP2008143825A (ja) * 2006-12-08 2008-06-26 Lion Corp 歯磨組成物
JP2018002719A (ja) * 2016-06-27 2018-01-11 サンスター株式会社 口腔用組成物
JP2018095574A (ja) * 2016-12-09 2018-06-21 ライオン株式会社 口腔用組成物
JP2018100245A (ja) * 2016-12-21 2018-06-28 サンスター株式会社 口腔用及び／又は咽喉用組成物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
1 October 1998 (1998-10-01), WARNER-LAMBERT. USA.: " Tartar Control Mouthwash ID# 10073000. ", XP009540258 *
DATABASE GNPD [online] MINTEL; MISTINE: "Peppermint Flavoured Herbal Extract Mouthwash", XP002760753, Database accession no. 2760425 *
DATABASE Mintel BIOCLIN. ITALY : " Cream Toothpaste", XP055977027, retrieved from GNPD *

Also Published As

Publication number Publication date
JP2022162849A (ja) 2022-10-25
TW202302067A (zh) 2023-01-16

Similar Documents

Publication Publication Date Title
JP5251350B2 (ja) 歯磨組成物
JP5597970B2 (ja) 歯磨剤組成物
WO2013094504A1 (fr) Composition orale
WO2011055707A1 (fr) Composition de dentifrice
JP2008514573A (ja) 口臭に対する作用物質としての芳香物質混合物の使用
WO2016093279A1 (fr) Composition destinée à être utilisés dans la cavité buccale
JP5493731B2 (ja) 歯磨剤組成物
JP6740901B2 (ja) 口腔用組成物及び口腔用組成物におけるカチオン性殺菌剤の異味抑制方法
JP5842565B2 (ja) 洗口剤組成物及び洗口剤組成物における変色抑制方法
WO2005072691A1 (fr) Composition servant a empecher la mauvaise haleine
WO2018066341A1 (fr) Composition pour cavité buccale, et procédé d'inhibition de variation de couleur de préparation et de séparation de liquide associés
JP2019167297A (ja) 歯磨剤組成物
WO2022220045A1 (fr) Composition pour cavité buccale
JP6409618B2 (ja) 歯磨組成物
JP4158036B2 (ja) 歯磨剤組成物及びその製造方法
JP2009137897A (ja) 歯磨組成物
JP5825088B2 (ja) 液体口腔用組成物
KR101773227B1 (ko) 치마제 조성물
WO2019107340A1 (fr) Composition pour utilisation par voie orale
JP6173735B2 (ja) 歯磨剤組成物
AU783747B2 (en) Dentifrice compositions having reduced abrasivity
JP5471318B2 (ja) 歯磨剤組成物
JP7172392B2 (ja) 口腔用組成物
WO2016136719A1 (fr) Composition de dentifrice
JPWO2018151076A1 (ja) ジェル状歯磨剤組成物及びそのべたつき抑制剤

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 22787970

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 22787970

Country of ref document: EP

Kind code of ref document: A1