WO2017209088A1 - 口腔用組成物 - Google Patents
口腔用組成物 Download PDFInfo
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- WO2017209088A1 WO2017209088A1 PCT/JP2017/019996 JP2017019996W WO2017209088A1 WO 2017209088 A1 WO2017209088 A1 WO 2017209088A1 JP 2017019996 W JP2017019996 W JP 2017019996W WO 2017209088 A1 WO2017209088 A1 WO 2017209088A1
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- WIPO (PCT)
- Prior art keywords
- composition
- component
- oral cavity
- tocopherol
- mass
- Prior art date
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Classifications
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- 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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/25—Silicon; Compounds thereof
-
- 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
- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
-
- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
-
- 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
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
-
- 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
- A61K8/67—Vitamins
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
Definitions
- the present invention relates to a composition for oral cavity in which tocopherol or a derivative thereof has excellent retention in the oral cavity.
- Tocopherol or its derivative (vitamin E) is an ingredient effective for the prevention and treatment of gingivitis and periodontitis, and its excellent retention in the oral cavity is thought to be useful in terms of expression of the effect,
- vitamin E is an ingredient effective for the prevention and treatment of gingivitis and periodontitis, and its excellent retention in the oral cavity is thought to be useful in terms of expression of the effect.
- Patent Document 1 Japanese Patent Publication No.
- Patent Document 3 Patent No. 4396429 discloses a dentifrice composition in which vitamin E or a derivative thereof and an anionic surfactant are blended, and contains vitamin E or a derivative thereof in a container. Stability is maintained by a specific nonionic surfactant mixture
- Patent Document 4 Japanese Patent Application Laid-Open No. 2015-110664 further discloses storage of vitamin E or its derivatives together with ascorbic acid phosphate or a salt thereof.
- the present invention has been made in view of the above circumstances.
- An oral composition having excellent retention in the oral cavity of tocopherol or a derivative thereof, excellent extrudability of a preparation from a container, and good usability (spinning property).
- the purpose is to provide.
- the present inventors have identified both xanthan gum and carrageenan and a specific anionic surfactant in an oral composition containing tocopherol or a derivative thereof. It has been found that mixing in an amount improves the retention in the oral cavity of tocopherol or a derivative thereof, and the extrudability of the preparation from the container is excellent and the usability is also good. That is, according to the present invention, one or more anionic surfactants selected from (A) tocopherol or derivatives thereof, (B) xanthan gum and carrageenan, (C) acylamino acid, acyltaurine and salts thereof.
- component content is 1.2 to 3 mass%
- component content is 0.1 to 3 mass%. Excellent retention, excellent extrudability that gives moderate hardness that allows the formulation to be smoothly extruded from the container, and good usability of kneading (spinning) when placed on a toothbrush As a result, the present invention has been made.
- the combined retention of the (B) and (C) components makes the retention in the oral cavity of the (A) component. It is markedly improved and gives a special effect that cannot be achieved by addition of an inappropriate binder or an inappropriate anionic surfactant.
- the use of xanthan gum or carrageenan alone does not satisfactorily improve the retention in the oral cavity of component (A), and in the case of xanthan gum alone, the kneading (spinning property) when placed on a toothbrush is poor.
- the present invention (A) Tocopherol or a derivative thereof, (B) xanthan gum and carrageenan, (C) contains one or more anionic surfactants selected from acylamino acids, acyltaurines and salts thereof, and the content of component (B) is 1.2 to 3% by mass, (C) Provided is an oral composition characterized in that the content of the component is 0.1 to 3% by mass.
- an oral composition having excellent retention in the oral cavity of tocopherol or a derivative thereof, excellent extrudability of a preparation from a container, and good usability such as spinnability. Furthermore, even in the oral cavity where saliva is always secreted, the component (A) can be satisfactorily retained, and prevention of gingivitis and periodontitis can be expected. It is suitable as.
- composition for oral cavity of the present invention contains an anionic surfactant selected from (A) tocopherol or a derivative thereof, (B) xanthan gum and carrageenan, (C) acylamino acid, acyltaurine and salts thereof as an essential component. .
- Tocopherol or a derivative thereof has a blood circulation promoting action and is a component for preventing or suppressing gingivitis and periodontitis.
- Examples of tocopherol or derivatives thereof include d- ⁇ -tocopherol, dl- ⁇ -tocopherol, ⁇ -tocopherol, ⁇ -tocopherol, ⁇ -tocopherol, and organic acids such as acetic acid, nicotinic acid, succinic acid, and linolenic acid. And their salts.
- tocopherol derivatives include d- ⁇ -tocopherol acetate, dl- ⁇ -tocopherol acetate, d- ⁇ -tocopherol nicotinate, dl- ⁇ -tocopherol nicotinate, d- ⁇ -tocopherol succinate, succinate
- examples thereof include dl- ⁇ -tocopherol acid, d- ⁇ -tocopherol linolenate, dl- ⁇ -tocopherol linolenate, and calcium tocopherol succinate. These may be used alone or in combination of two or more.
- dl- ⁇ -tocopherol, dl- ⁇ -tocopherol acetate, dl- ⁇ -tocopherol nicotinate, particularly dl- ⁇ -tocopherol acetate, Is preferable in that it is good.
- tocopherol or its derivative a product conforming to the former cosmetic raw material standard (Mandarin base) or quasi-drug raw material standard 2006 can be used, manufactured by DSM Nutrition Japan, manufactured by Eisai Food Chemical, manufactured by BASF Japan, etc. Commercial products can be used.
- Component (A) is blended in an amount of 0.1% (mass%, the same shall apply hereinafter) or more, preferably 0.1-2%, more preferably 0.2-2%, even more preferably 0% of the total composition. .3 to 1.5%, particularly preferably 0.5 to 1.5%. The greater the compounding amount, the more effectively the medicinal effect is exhibited.
- (B) component is a mixture of xanthan gum and carrageenan, and using both together improves the retention in the oral cavity of (A) component. In the single use of xanthan gum or carrageenan, the retention in the oral cavity is poor.
- any xanthan gum may be used as long as it is usually used in a dentifrice composition, but the viscosity of xanthan gum is 600 to 2,000 mPa ⁇ s in a 1% xanthan gum aqueous solution containing 1% potassium chloride. In particular, those of 1,000 to 2,000 mPa ⁇ s are preferred.
- the above-mentioned viscosity is a Brookfield type rotational viscometer, rotor No. 3, 60 rpm, 25 ° C., measurement time 30 seconds.
- xanthan gum commercially available products such as Novazan manufactured by ADM Far East Co., Ltd., Monato Gum DA manufactured by CP Kelco, Kelzan T, Keldent, Echo Gum manufactured by Dainippon Pharmaceutical Co., Ltd. and the like can be used.
- Carrageenan includes ⁇ (kappa) -carrageenan, ⁇ (iota) -carrageenan, and ⁇ (lambda) -carrageenan, and one or more can be used, but ⁇ (iota) -carrageenan is preferably used. Can do.
- Examples of ⁇ -carrageenan include GENUVISCO manufactured by CP Kerco.
- the blending amount of the xanthan gum and carrageenan as component (B) is 1.2% or more, particularly preferably 1.2 to 3%, more preferably 1.4 to 2.5% of the total composition.
- the greater the blending amount the higher the retention of the component (A) in the oral cavity. If the amount is less than 1.2%, the oral retention is inferior. As the blending amount increases, the retention in the oral cavity increases, but it is preferably 3% or less in order to maintain the extrudability of the preparation well.
- the blending amount of xanthan gum is preferably 0.6 to 2.8% of the total composition, more preferably 0.9 to 2.1%, and the blending amount of carrageenan is The content is preferably 0.2 to 2.4%, more preferably 0.4 to 1.6% of the total composition.
- xanthan gum / carrageenan which indicates the blending ratio of xanthan gum and carrageenan, is preferably 0.5 to 5, more preferably 1 to 3, as a mass ratio.
- the retention in the oral cavity of the component (A) is more excellent, and the spinnability is further improved. If it is less than 0.5, the retention in the oral cavity may not be sufficiently improved, and if it exceeds 5, the spinnability may be increased.
- the anionic surfactant of the component is one or more selected from acylamino acids, acyltaurines and salts thereof.
- acyl amino acid an acyl group having 8 to 20 carbon atoms, particularly 12 to 16 carbon atoms is preferable, and as the amino acid residue, glutamic acid, aspartic acid, glycine, sarcosine, alanine, methionine, phenylalanine, leucine. And isoleucine.
- the salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts, and organic amine salts.
- Acyl amino acids and salts thereof include acyl glutamates having the above-mentioned carbon number, acyl aspartates, acyl glycine salts, particularly acyl glutamates, particularly sodium lauroyl glutamate, which is different from those having other amino acid residues. (Bitterness) is weak and suitable.
- the acyl amino acid salt include acyl glutamates such as sodium N-lauroyl-L-glutamate, sodium N-myristoyl-L-glutamate, N-coconut oil fatty acid acyl-L-glutamate potassium, and N-lauroyl-L-aspartic acid.
- Examples include acyl aspartates such as sodium, acyl glycine salts such as N-coconut oil fatty acid acyl glycine potassium, and the like.
- acylamino acids and salts thereof include aminosurfact ALMS-P1 (N-lauroyl-L-glutamate sodium, Asahi Kasei Chemicals Corporation), Amisoft LS-11 (N-lauroyl-L-glutamate sodium, Ajinomoto Healthy Supply Corporation), Amino Surfact AMMS-P1 (N-myristoyl-L-glutamate sodium, Asahi Kasei Chemicals Corporation), Amisoft MS-11 (N-myristoyl-L-glutamate sodium, Ajinomoto Healthy Supply Corporation), Amino Four Mer FLDS-L (N-lauroyl-L-sodium aspartate, Asahi Kasei Chemicals Corporation), Amlite GCK-12K (N-coconut oil fatty acid acylglycine potassium, Ajinomoto Healthy Supply Co., Ltd.), etc. Those that are commercialized under the trade name can be used.
- acyl taurine those having an acyl group having 8 to 20 carbon atoms, particularly 12 to 16 carbon atoms are preferred, and the taurine residue is taurine, methyl taurine or the like.
- the salt include alkali metal salts such as sodium salt and potassium salt.
- Specific examples of acyl taurine salts include cocoyl methyl taurine sodium, cocoyl methyl taurine potassium, lauroyl methyl taurine sodium, stearoyl methyl taurine sodium, myristoyl methyl taurine sodium, oleoyl methyl taurine sodium, palmitoyl methyl taurine sodium and cocoyl taurine sodium. It is done. Of these, acylmethyl taurine salts, particularly lauroylmethyl taurine sodium, are preferred.
- component (C) one kind selected from acylamino acids, acyltaurines and salts thereof may be used alone, or two or more kinds may be used in combination. Is preferred.
- the amount of component (C) is 0.1 to 3%, preferably 0.3 to 1.5% of the entire composition. If the blending amount is less than 0.1%, the retention in the oral cavity of the component (A) is not sufficiently improved, and the formulation is difficult to extrude from the container after storage, and the extrudability is poor. The greater the blending amount, the better the retention in the oral cavity and the extrudability, but when it exceeds 3%, bitterness and irritation occur, and the stability of the component (A) decreases.
- (B) / (C) indicating the blending ratio of the component (B) and the component (C) is preferably 0.5 to 10, more preferably 1 to 8, particularly preferably 1.2 as the mass ratio. ⁇ 6. Within this range, the retention in the oral cavity is more excellent, and the pushability and stringiness are further improved.
- anionic surfactants other than the component (C) can be blended as long as the effects of the present invention are not hindered, the total amount of anionic surfactant is 50% or less, preferably 20% or less. .
- the composition for oral cavity of the present invention can be prepared in the form of a toothpaste such as a toothpaste, a liquid toothpaste, a liquid toothpaste, a toothpaste, a mouthwash, etc. in the form of a liquid, liquid, gel or paste.
- a dentifrice is particularly suitable.
- other known components can be blended as necessary and prepared by a conventional method.
- abrasives, binders, thickeners, surfactants, sweeteners, colorants, preservatives, pH adjusters, fragrances, active ingredients and the like can be mentioned.
- silica-based abrasives such as precipitated silica, aluminosilicate and zirconosilicate, dicalcium phosphate dihydrate and hydrates, calcium phosphate compounds such as primary calcium phosphate and tertiary calcium phosphate, calcium carbonate , Calcium hydroxide, aluminum hydroxide and the like.
- the blending amount of the abrasive is usually 2 to 40%, preferably 10% or less, more preferably 5% or less, and may be unblended (0%).
- water-insoluble powder particularly silica-based polishing is preferred. It is preferable that the amount of the abrasive such as an agent is small.
- the composition of the present invention is more preferably a dentifrice having no abrasive (abrasive amount 0%), a gel composition, particularly an aqueous gel composition.
- a binder other than xanthan gum and carrageenan can be blended within a range that does not hinder the effects of the present invention.
- thickening silica such as gelling silica as the inorganic binder
- cellulose derivatives such as sodium carboxymethylcellulose, methylcellulose and hydroxymethylcellulose as organic binder
- alginic acid derivatives such as sodium alginate, sodium polyacrylate, etc.
- inorganic binders such as thickening silica are preferred in terms of retention feeling, appearance (moldability), and extrudability.
- the amount of these binders is preferably 0.5-10%, particularly 1-8%.
- the organic binder other than the component (B) has a blending amount of 0.2% or less, particularly 0.1% or less, in terms of retention in the oral cavity of the component (A) and extrudability of the preparation. Is preferable, and it is also preferable not to add (0%).
- the thickening agent examples include sugar alcohols such as sorbit and xylit, and polyhydric alcohols such as glycerin and propylene glycol.
- the blending amount is usually 5 to 50%, particularly 20 to 45%.
- nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters.
- sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters.
- Polyoxyethylene fatty acid esters such as polyoxyethylene sorbitan fatty acid esters and polyoxyethylene hydrogenated castor oil, polyoxyethylene higher alcohol ethers such as polyoxyethylene lauryl ether, and the like can be blended.
- cationic surfactants such as alkylammonium type such as distearylmethylammonium chloride, amphoteric surfactants such as betaine type, betaine acetate type, and imidazoline type can also be blended.
- the amount of these surfactants is usually from 0.01 to 10%, particularly from 0.1 to 5%.
- sweetening agent examples include saccharin sodium.
- colorant examples include blue No. 1, yellow No. 4, titanium dioxide and the like.
- preservative examples include paraoxybenzoic acid esters such as methyl paraoxybenzoate, benzoic acid such as sodium benzoate, and salts thereof.
- a pH adjuster may be added, and examples thereof include alkali metal hydroxides such as sodium hydroxide, hydrogen carbonates, carbonates and sulfates.
- Perfumes include peppermint oil, spearmint oil, anise oil, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, Lime oil, lavender oil, rosemary oil, laurel oil, camomil oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie Natural fragrances such as oil, bran oil, Iris concrete, absolute peppermint, absolute rose, orange flower, and processing of these natural fragrances (front reservoir cut, rear reservoir cut, fractional distillation, liquid-liquid extraction, essence, powder Perfumed, menthol, moss Bonn, Anethole, Cineol, Methyl salicylate, Synamic aldehyde, Eugenol, 3-l-Mentoxyprop
- the blending amount is not particularly limited, but the above fragrance material is preferably used in the composition in an amount of 0.000001 to 1%. Further, as a flavoring fragrance using the above fragrance material, it is preferable to use 0.1 to 2% in the composition.
- a nonionic fungicide such as isopropylmethylphenol, a cation such as cetylpyridinium chloride, benzalkonium chloride, and benzethonium chloride
- Antibacterial agents anti-inflammatory agents, enzymes such as dextranase, fluorides such as sodium fluoride and sodium monofluorophosphate, vitamins, calculus inhibitors, dental plaque inhibitors and the like.
- the said active ingredient can be mix
- Dentifrice compositions having the compositions shown in Tables 1 to 3 were prepared by the following methods and evaluated by the following methods. The results are shown in the table. Production method: After blending water-soluble components in purified water, add (B) component dispersed in propylene glycol, mix, then add fragrance, (A) component, (C) component sequentially, defoaming and mixing Produced.
- the xanthan gum used had a viscosity of 1% aqueous solution of xanthan gum containing 1% potassium chloride (Brookfield type rotational viscometer, rotor No. 3, 60 rpm, 25 ° C., measurement time 30 seconds) at about 1,500 mPa ⁇ s. Yes, carrageenan is ⁇ -carrageenan.
- Measurement conditions were as follows: a stainless steel tube having an inner diameter of 4.6 mm and a length of 15 cm was filled with a 5 ⁇ m octadecylsilylated silica gel for liquid chromatography, methanol was used as the mobile phase, the column temperature was 25 ° C., and 1.0 mL / min. was measured by an absolute calibration curve method with an ultraviolet absorptiometry (measurement wavelength: 284 nm).
- Evaluation criteria For the amount of tocopherol or its derivative retained in the oral cavity, the average value of the repeated three times was obtained, and the ratio of the residual amount to the initial amount (the amount of tocopherol or its derivative contained in 40 ⁇ L of the 3-fold diluted solution treated first) Calculated and evaluated according to the following criteria.
- a dentifrice composition was filled in a laminated tube container having a diameter of 8 mm, and after placing about 1 g on the toothbrush from the tube, the kneading (threading property) when the tube and the toothbrush were separated upward was tested.
- the stringiness refers to the property that the dentifrice composition stretches as if it is pulled out from the tube, and its length was measured. Evaluation was made according to the following criteria.
- Toothpaste (A) Tocopherol acetate 1.0% (B) Xanthan gum 1.5 (B) Carrageenan 0.5 (C) Lauroylmethyl taurine sodium 1.0 Abrasive silica 10 Thickening silica 5 70% sorbite solution 40 Saccharin sodium 0.2 Isopropylmethylphenol 0.1 Sodium fluoride 0.21 Polyoxyethylene (20) hydrogenated castor oil 1.2 Polyoxyethylene (5) stearyl ether 1.2 Propylene glycol 3 Sodium hydroxide 0.1 Sodium dihydrogen phosphate 0.1 Fragrance 0.8 Purified water balance Total 100.0% Xanthan gum / carrageenan ratio; 3 (B) / (C); 2
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Abstract
Description
また、口腔用組成物におけるトコフェロール又はその誘導体の安定性改善に関して、特許文献2(特公平7-88292号公報)には、アルキル硫酸エステル塩存在下でトコフェロール又はその誘導体の保存安定性が特定のアミノ酸によって改善すること、特許文献3(特許第4496429号公報)には、ビタミンE又はその誘導体とアニオン性界面活性剤が配合された歯磨剤組成物で、容器内でのビタミンE又はその誘導体の安定性が特定のノニオン性界面活性剤混合物によって維持されること、更に、特許文献4(特開2015-110664号公報)には、アスコルビン酸リン酸エステル又はその塩と共にビタミンE又はその誘導体の保存安定性が、特定のノニオン界面活性剤によって改善することが開示されているが、トコフェロール又はその誘導体の口腔内滞留性については検討されておらず言及もない。
(A)トコフェロール又はその誘導体、
(B)キサンタンガム及びカラギーナン、
(C)アシルアミノ酸、アシルタウリン及びこれらの塩から選ばれる1種又は2種以上のアニオン性界面活性剤
を含有し、(B)成分の含有量が1.2~3質量%、(C)成分の含有量が0.1~3質量%であることを特徴とする口腔用組成物
を提供する。
トコフェロール又はその誘導体としては、例えばd-α-トコフェロール、dl-α-トコフェロール、β-トコフェロール、γ-トコフェロール、δ-トコフェロールや、これらの酢酸、ニコチン酸、コハク酸、リノレン酸等の有機酸とのエステル、これらの塩等が挙げられる。このようなトコフェロール誘導体として具体的には、酢酸d-α-トコフェロール、酢酸dl-α-トコフェロール、ニコチン酸d-α-トコフェロール、ニコチン酸dl-α-トコフェロール、コハク酸d-α-トコフェロール、コハク酸dl-α-トコフェロール、リノレン酸d-α-トコフェロール、リノレン酸dl-α-トコフェロール、コハク酸トコフェロールカルシウム等が挙げられる。これらは、1種又は2種以上使用し得るが、中でもdl-α-トコフェロール、酢酸dl-α-トコフェロール、ニコチン酸dl-α-トコフェロール、特に酢酸dl-α-トコフェロールが、製剤外観(色調)が良好である点で好ましい。
なお、上記粘度は、ブルックフィールド型回転粘度計、ローターNo.3、60rpm、25℃、測定時間30秒による値である。
このようなキサンタンガムとしては、市販品、例えばADMファーイースト(株)製のノヴァザン、CPケルコ社製のモナートガムDA、ケルザンT、ケルデント、大日本製薬(株)製のエコーガム等を使用できる。
更に、上記合計配合量の範囲内で、キサンタンガムの配合量は組成物全体の0.6~2.8%が好ましく、より好ましくは0.9~2.1%であり、カラギーナンの配合量は組成物全体の0.2~2.4%が好ましく、より好ましくは0.4~1.6%である。
アシルアミノ酸及びその塩としては、アシル基が上記炭素数のアシルグルタミン酸塩、アシルアスパラギン酸塩、アシルグリシン塩、特にアシルグルタミン酸塩、とりわけラウロイルグルタミン酸ナトリウムが、他のアミノ酸残基を有するものよりも異味(苦味)が弱く、好適である。
アシルアミノ酸塩としては、例えばN-ラウロイル-L-グルタミン酸ナトリウム、N-ミリストイル-L-グルタミン酸ナトリウム、N-ヤシ油脂肪酸アシル-L-グルタミン酸カリウム等のアシルグルタミン酸塩、N-ラウロイル-L-アスパラギン酸ナトリウム等のアシルアスパラギン酸塩、N-ヤシ油脂肪酸アシルグリシンカリウム等のアシルグリシン塩等が挙げられる。
アシルタウリン塩として具体的には、ココイルメチルタウリンナトリウム、ココイルメチルタウリンカリウム、ラウロイルメチルタウリンナトリウム、ステアロイルメチルタウリンナトリウム、ミリストイルメチルタウリンナトリウム、オレオイルメチルタウリンナトリウム、パルミトイルメチルタウリンナトリウム、ココイルタウリンナトリウムが挙げられる。
これらの中で、アシルメチルタウリン塩、特にラウロイルメチルタウリンナトリウムが好適である。
なお、口腔用組成物では、口腔内に薬用成分を滞留させるには使用後の水すすぎ回数を減らすほうが好ましく、本発明においても、すすぎ易さの観点から、水不溶性粉体、特にシリカ系研磨剤等の研磨剤量は少ないほうが好ましい。本発明組成物は、研磨剤を含まない(研磨剤量0%)、ゲル組成、特に水性ゲル組成の歯磨剤であることが更に好ましい。
これら粘結剤の配合量は、0.5~10%、特に1~8%が好ましい。
なお、(B)成分以外の有機粘結剤は、(A)成分の口腔内滞留性や製剤の押し出し性の点で、配合量が0.2%以下、特に0.1%以下であることが好ましく、無配合(0%)とすることも好ましい。
また、塩化ジステアリルメチルアンモニウム等のアルキルアンモニウム型等のカチオン性界面活性剤、ベタイン型、酢酸ベタイン型、イミダゾリン型等の両性界面活性剤を配合することもできる。
これら界面活性剤の配合量は、通常、0.01~10%、特に0.1~5%である。
防腐剤としては、パラオキシ安息香酸メチル等のパラオキシ安息香酸エステル、安息香酸ナトリウム等の安息香酸又はその塩等が挙げられる。
また、pH調整剤を添加してもよく、例えば水酸化ナトリウム等のアルカリ金属の水酸化物、炭酸水素塩、炭酸塩、硫酸塩等が挙げられる。
また、配合量も特に限定されないが、上記の香料素材は、組成物中に0.000001~1%使用するのが好ましい。また、上記香料素材を使用した賦香用香料としては、組成物中に0.1~2%使用するのが好ましい。
表1~3に示す組成の歯磨剤組成物を下記方法によって調製し、下記方法で評価した。結果を表に併記した。
製造方法:精製水に水溶性成分を配合後、プロピレングリコールに分散させた(B)成分を投入し混合、次いで香料、(A)成分、(C)成分を順次投入し、脱泡混合して作製した。
なお、使用したキサンタンガムは、塩化カリウムを1%含むキサンタンガム1%水溶液の粘度(ブルックフィールド型回転粘度計、ローターNo.3、60rpm、25℃、測定時間30秒)が約1,500mPa・sであり、カラギーナンはι-カラギーナンである。
歯磨剤組成物を水で3倍希釈した歯磨希釈液40μLを直径10mmにパンチアウトしたハムスターチークポーチ(日本SLC(株)製、3週齢♂Syrian)に載せた。3分間静置後、水で7回洗浄し、エタノール1mLで抽出し、液体クロマトグラフィーにより下記方法で油溶性成分のトコフェロール又はその誘導体を定量した。
測定条件は、内径4.6mm、長さ15cmのステンレス管に5μmの液体クロマトグラフ用オクタデシルシリル化シリカゲルを充填したカラムを用い、メタノールを移動相に用い、カラム温度25℃、1.0mL/分の流量で、紫外吸光光度(測定波長284nm)での絶対検量線法により測定した。
トコフェロール又はその誘導体の口腔内滞留量について、繰り返し3回の平均値を求め、初期値量(最初に処置した3倍希釈液40μL中に含まれるトコフェロール又はその誘導体の量)に対する残存量の割合を算出し、下記基準に従って評価した。
評価基準
◎:滞留量が30%以上
○:滞留量が20%以上30%未満
△:滞留量が10%以上20%未満
×:滞留量が10%未満
歯磨剤組成物を口径8mmのラミネートチューブ容器に50g充填し、各組成3本を-5℃で1ヶ月間保存した後、歯磨剤組成物を押し出し、下記の4段階で押し出し固さの度合いを評価した。
評価基準
◎:スムーズに歯磨剤組成物が押し出せる
○:やや固いが問題なく歯磨剤組成物が押し出せる
△:固くて歯磨剤組成物がやや押し出しにくい
×:固くて歯磨剤組成物が押し出しにくい
口径8mmのラミネートチューブ容器に歯磨剤組成物を充填し、チューブより歯ブラシ上に約1g載せた後、上方向にチューブと歯ブラシを引き離した際の練り切れ(曳糸性)を試験した。曳糸性とは、チューブから取り出した時、歯磨剤組成物が糸を引くように伸びる性状をいい、その長さを測定した。下記基準で評価した。
評価基準
◎:曳糸性が0.5cm未満であり、練り切れが良い
○:0.5cm以上、1cm未満の曳糸性が認められるが使用上問題ない
△:1cm以上、1.5cm未満の曳糸性が認められ、使用上やや問題がある
×:1.5cm以上の曳糸性が認められ、使用上問題がある
(A)トコフェロール酢酸エステル 1.0%
(B)キサンタンガム 1.5
(B)カラギーナン 0.5
(C)ラウロイルメチルタウリンナトリウム 1.0
研磨性シリカ 10
増粘性シリカ 5
70%ソルビット液 40
サッカリンナトリウム 0.2
イソプロピルメチルフェノール 0.1
フッ化ナトリウム 0.21
ポリオキシエチレン(20)硬化ヒマシ油 1.2
ポリオキシエチレン(5)ステアリルエーテル 1.2
プロピレングリコール 3
水酸化ナトリウム 0.1
リン酸二水素ナトリウム 0.1
香料 0.8
精製水 バランス
合計 100.0%
キサンタンガム/カラギーナン比;3 (B)/(C);2
Claims (10)
- (A)トコフェロール又はその誘導体、
(B)キサンタンガム及びカラギーナン、
(C)アシルアミノ酸、アシルタウリン及びこれらの塩から選ばれる1種又は2種以上のアニオン性界面活性剤
を含有し、(B)成分の含有量が1.2~3質量%、(C)成分の含有量が0.1~3質量%である口腔用組成物。 - キサンタンガム/カラギーナンで表されるキサンタンガムとカラギーナンとの含有質量比が、0.5~5である請求項1記載の口腔用組成物。
- キサンタンガムの含有量が0.6~2.8質量%、カラギーナンの含有量が0.2~2.4質量%である請求項1又は2記載の口腔用組成物。
- (C)成分が、アシル基の炭素数が8~20であるアシルグルタミン酸塩、アシルアスパラギン酸塩及びアシルグリシン塩、並びにアシル基の炭素数が8~20であるアシルタウリン塩及びアシルメチルタウリン塩から選ばれる1種又は2種以上のアニオン性界面活性剤である請求項1~3のいずれか1項記載の口腔用組成物。
- (B)/(C)で表される(B)成分と(C)成分との含有質量比が、0.5~10である請求項1~4のいずれか1項記載の口腔用組成物。
- (A)成分の含有量が0.1~2質量%である請求項1~5のいずれか1項記載の口腔用組成物。
- 更に、研磨剤を10質量%含有する請求項1~6のいずれか1項記載の口腔用組成物。
- 研磨剤を含有しない請求項1~6のいずれか1項記載の口腔用組成物。
- 更に、無機粘結剤を0.5~10質量%含有する請求項1~8のいずれか1項記載の口腔用組成物。
- 歯磨剤である請求項1~9のいずれか1項記載の口腔用組成物。
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CN109152722A (zh) | 2019-01-04 |
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