CN114867455B - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- CN114867455B CN114867455B CN202080090372.1A CN202080090372A CN114867455B CN 114867455 B CN114867455 B CN 114867455B CN 202080090372 A CN202080090372 A CN 202080090372A CN 114867455 B CN114867455 B CN 114867455B
- Authority
- CN
- China
- Prior art keywords
- discoloration
- component
- oral composition
- composition
- polyacrylate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000203 mixture Substances 0.000 title claims abstract description 69
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 claims abstract description 36
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 claims abstract description 18
- 229960000458 allantoin Drugs 0.000 claims abstract description 18
- 229920000058 polyacrylate Polymers 0.000 claims abstract description 17
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 claims abstract description 17
- 229960000401 tranexamic acid Drugs 0.000 claims abstract description 17
- YGWKXXYGDYYFJU-SSDOTTSWSA-N (+)-menthofuran Chemical compound C1[C@H](C)CCC2=C1OC=C2C YGWKXXYGDYYFJU-SSDOTTSWSA-N 0.000 claims abstract description 15
- 239000001745 (6R)-3,6-dimethyl-4,5,6,7-tetrahydro-1-benzofuran Substances 0.000 claims abstract description 15
- YGWKXXYGDYYFJU-UHFFFAOYSA-N Menthofuran Natural products C1C(C)CCC2=C1OC=C2C YGWKXXYGDYYFJU-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000000551 dentifrice Substances 0.000 claims description 19
- MBDOYVRWFFCFHM-SNAWJCMRSA-N (2E)-hexenal Chemical compound CCC\C=C\C=O MBDOYVRWFFCFHM-SNAWJCMRSA-N 0.000 claims description 12
- DTUQWGWMVIHBKE-UHFFFAOYSA-N phenylacetaldehyde Chemical compound O=CCC1=CC=CC=C1 DTUQWGWMVIHBKE-UHFFFAOYSA-N 0.000 claims description 12
- 229940100595 phenylacetaldehyde Drugs 0.000 claims description 6
- MBDOYVRWFFCFHM-UHFFFAOYSA-N trans-2-hexenal Natural products CCCC=CC=O MBDOYVRWFFCFHM-UHFFFAOYSA-N 0.000 claims description 6
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- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
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- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 2
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- KZRXPHCVIMWWDS-AWEZNQCLSA-N (4S)-4-amino-5-dodecanoyloxy-5-oxopentanoic acid Chemical compound CCCCCCCCCCCC(=O)OC(=O)[C@@H](N)CCC(O)=O KZRXPHCVIMWWDS-AWEZNQCLSA-N 0.000 description 1
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 description 1
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- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 238000000569 multi-angle light scattering Methods 0.000 description 1
- 229940070800 myristoyl glutamate Drugs 0.000 description 1
- TWNQGVIAIRXVLR-UHFFFAOYSA-N oxo(oxoalumanyloxy)alumane Chemical compound O=[Al]O[Al]=O TWNQGVIAIRXVLR-UHFFFAOYSA-N 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
- 235000019477 peppermint oil Nutrition 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 229940051841 polyoxyethylene ether Drugs 0.000 description 1
- 229920000056 polyoxyethylene ether Polymers 0.000 description 1
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 229940085605 saccharin sodium Drugs 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- 229960000414 sodium fluoride Drugs 0.000 description 1
- SUKJFIGYRHOWBL-UHFFFAOYSA-N sodium hypochlorite Chemical compound [Na+].Cl[O-] SUKJFIGYRHOWBL-UHFFFAOYSA-N 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 229960004711 sodium monofluorophosphate Drugs 0.000 description 1
- URLJMZWTXZTZRR-UHFFFAOYSA-N sodium myristyl sulfate Chemical compound CCCCCCCCCCCCCCOS(O)(=O)=O URLJMZWTXZTZRR-UHFFFAOYSA-N 0.000 description 1
- 229950005425 sodium myristyl sulfate Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 description 1
- 229960002799 stannous fluoride Drugs 0.000 description 1
- 229910001631 strontium chloride Inorganic materials 0.000 description 1
- AHBGXTDRMVNFER-UHFFFAOYSA-L strontium dichloride Chemical compound [Cl-].[Cl-].[Sr+2] AHBGXTDRMVNFER-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 229920003002 synthetic resin Polymers 0.000 description 1
- 239000000057 synthetic resin Substances 0.000 description 1
- UJMBCXLDXJUMFB-GLCFPVLVSA-K tartrazine Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1\N=N\C1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-GLCFPVLVSA-K 0.000 description 1
- 239000004149 tartrazine Substances 0.000 description 1
- 229960000943 tartrazine Drugs 0.000 description 1
- 235000012756 tartrazine Nutrition 0.000 description 1
- GBNXLQPMFAUCOI-UHFFFAOYSA-H tetracalcium;oxygen(2-);diphosphate Chemical compound [O-2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GBNXLQPMFAUCOI-UHFFFAOYSA-H 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- VXYADVIJALMOEQ-UHFFFAOYSA-K tris(lactato)aluminium Chemical compound CC(O)C(=O)O[Al](OC(=O)C(C)O)OC(=O)C(C)O VXYADVIJALMOEQ-UHFFFAOYSA-K 0.000 description 1
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 238000004383 yellowing Methods 0.000 description 1
- 239000010457 zeolite Substances 0.000 description 1
- 239000011746 zinc citrate Substances 0.000 description 1
- 235000006076 zinc citrate Nutrition 0.000 description 1
- 229940068475 zinc citrate Drugs 0.000 description 1
- 239000011670 zinc gluconate Substances 0.000 description 1
- 235000011478 zinc gluconate Nutrition 0.000 description 1
- 229960000306 zinc gluconate Drugs 0.000 description 1
- GFQYVLUOOAAOGM-UHFFFAOYSA-N zirconium(iv) silicate Chemical compound [Zr+4].[O-][Si]([O-])([O-])[O-] GFQYVLUOOAAOGM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K8/40—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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
-
- 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
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
-
- 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
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)
- Birds (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
Abstract
The present invention provides an allantoin and/or tranexamic acid-containing oral composition as follows: even if stored at high temperature for a long period of time, the coloring and discoloration of the preparation can be suppressed, the appearance stability is excellent, the odor is suppressed, and the taste is also excellent. The oral composition comprises: (A) at least 1 selected from allantoin and tranexamic acid, (B) at least 1 selected from a compound having an aldehyde group and menthofuran, and (C) a polyacrylate having a weight average molecular weight of 1000 to 20000, wherein the mass ratio of (C)/(A) is 0.1 to 21.
Description
Technical Field
The present invention relates to an oral composition which contains allantoin and/or tranexamic acid, suppresses coloring and discoloration even after storage, and has excellent appearance stability and good taste.
Background
For preventing periodontal diseases, it is known that the alleviation of inflammation is effective, and an anti-inflammatory agent is formulated in an oral composition with an active ingredient having an amino group such as tranexamic acid or allantoin.
On the other hand, in the case of an oral composition, a flavor is necessary for preparing a preparation having a high preference, and among them, a compound having an aldehyde group and menthofuran are important components, and are essential flavor components for preparing an oral composition having a high preference.
However, when a flavor is blended with an active ingredient having an amino group in an oral composition, depending on the type of flavor ingredient, it may be difficult to maintain the appearance of the preparation, and when a compound having an aldehyde group is blended, the active ingredient having an amino group reacts with the compound having an aldehyde group, and problems such as coloration and discoloration of the oral composition occur, and the problem of ensuring the stability of the appearance is a problem.
In patent document 1 (japanese patent No. 5842565), discoloration after 3 months of storage at room temperature is suppressed by adding sodium lauryl sulfate to a mouthwash composition containing tranexamic acid and cinnamaldehyde, which are active ingredients having an amino group. In addition, in patent document 2 (japanese patent publication No. 62-16926), coloring and discoloration after two days of storage at 50 ℃ are suppressed by adding a specific suitable aldehyde-based flavor as an aldehyde-based flavor to a toothpaste containing tranexamic acid.
However, in the conventional art, it is difficult to suppress coloring and discoloration of an oral composition even when stored at high temperature for a long period of time due to the reaction of an active ingredient having an amino group with a flavor ingredient such as a compound having an aldehyde group, and a technique for further suppressing coloring and discoloration with time has been desired.
Prior art literature
Patent literature
Patent document 1: japanese patent No. 5842565
Patent document 2: japanese patent publication No. 62-16926
Patent document 3: japanese patent laid-open publication No. 2019-99483
Disclosure of Invention
Problems to be solved by the invention
The present invention has been made in view of the above circumstances, and an object thereof is to provide an allantoin and/or tranexamic acid-containing oral composition as follows: even if stored at high temperature for a long period of time, the coloring and discoloration of the preparation can be suppressed, and the preparation is excellent in appearance stability and taste.
Technical scheme for solving problems
The present inventors have made intensive studies to achieve the above object, and as a result, have found that when a low molecular weight polyacrylate is blended in a specific ratio into an oral composition containing allantoin or tranexamic acid having an amino group and a compound having an aldehyde group or menthofuran as a flavor component, the discoloration and discoloration of the composition can be suppressed even if the composition is stored at a high temperature for a long period of time, the stability of the appearance can be improved, and further, the odor can be suppressed, the taste can be kept good, high preference can be ensured, and excellent stability of the appearance can be provided.
That is, the following findings are obtained, and according to the present invention, an oral composition comprises: the present invention has been completed by the fact that (A) at least 1 selected from allantoin and tranexamic acid, (B) at least 1 selected from compounds having an aldehyde group and menthofuran, and (C) a polyacrylate having a weight average molecular weight of 1000 to 20000, wherein the mass ratio of (C)/(A) is 0.1 to 21, and the oral composition can suppress coloration and discoloration of the preparation even after long-term storage at high temperature, and is excellent in appearance stability and taste.
In an oral composition containing allantoin or tranexamic acid as an anti-inflammatory agent, there is a problem that the preparation is colored or discolored with time and the stability of the appearance is lowered, not only when a compound having an aldehyde group is added as a flavor component, but also when menthofuran is added as a flavor component. However, in the present invention, in the oral composition, particularly in the dentifrice composition, by combining the component (a) and the component (B) and the component (C), coloring and discoloration of the preparation with time due to the reaction of the component (a) and the component (B) are suppressed by the component (C), and the external stability is excellent. In this case, when the mass ratio of (C)/(a) is within the specific range, the component (C) unexpectedly exerts an excellent effect on the system in which the components (a) and (B) are combined as a discoloration inhibitor, whereby the discoloration (coloring, discoloration) of the preparation can be suppressed even after long-term storage at high temperature, and as shown in examples described later, discoloration of the preparation can be suppressed after 1 month storage at 60 ℃ and an excellent discoloration suppressing effect can be imparted without occurrence of a unique odor of the component (C) itself and ensuring a good taste.
As the binder for the oral composition, polyacrylic acid or a salt thereof having a weight average molecular weight of 10 ten thousand or more, usually about 30 ten thousand is generally used. In contrast, in the present invention, the above-described particularly remarkable effect can be imparted by (C) a specific polyacrylate having a low molecular weight.
The effect of the present invention is that the composition (A), (B) and (C) are combined so that the mass ratio of (C)/(A) falls within a specific range, and as shown in comparative examples described later, the discoloration inhibition effect is poor even when sodium polyacrylate having a weight average molecular weight of 30 ten thousand is blended (comparative examples 1 and 2), and the discoloration inhibition effect or taste (unobvious degree of odor) is poor even when the mass ratio of (C)/(A) is improper (comparative examples 3 and 4).
In patent document 3 (japanese patent application laid-open No. 2019-99483), menthol and a specific aldehyde-based perfume are combined with a specific low-molecular-weight polyacrylate to suppress irritation and impart a fresh feeling in use. In contrast, the present invention is realized by the inhibition of discoloration and the inhibition of odor of a system in which the component (A) and the component (B) are used in combination.
Accordingly, the present invention provides the following oral compositions.
[ 1] an oral composition comprising:
(A) More than 1 kinds of allantoin and tranexamic acid,
(B) More than 1 selected from aldehyde group-containing compounds and menthofuran, and
(C) A polyacrylate having a weight average molecular weight of 1000 to 20000,
wherein the mass ratio of (C)/(A) is 0.1-21.
The composition for oral cavity according to [ 2], wherein,
(B) The component is selected from trans-2-hexenal, phenylacetaldehyde, citral and menthofuran.
The composition for oral cavity according to [ 1] or [ 2], wherein,
the oral composition contains 0.005-1% by mass of component (A), 0.0001-0.5% by mass of component (B), and 0.01-1% by mass of component (C).
The composition for oral cavity according to any one of [ 1] to [ 3], wherein,
the oral composition is a dentifrice composition.
Effects of the invention
According to the present invention, there can be provided an allantoin or tranexamic acid-containing oral composition as follows: even if stored at high temperature for a long period of time, the preparation can be inhibited from coloring and discoloring, and is excellent in appearance stability, and further, is inhibited from odor, good in taste and high in preference. The oral composition has antiinflammatory effect based on allantoin or tranexamic acid, and is effective for preventing or inhibiting periodontal diseases such as gingivitis.
Detailed Description
The oral composition of the present invention is characterized by comprising: (A) at least 1 selected from allantoin and tranexamic acid, (B) at least 1 selected from a compound having an aldehyde group and menthofuran, and (C) a polyacrylate having a weight average molecular weight of 1000 to 20000, wherein the mass ratio of (C)/(A) is 0.1 to 21.
(A) The components are allantoin and tranexamic acid, either of which may be used alone or in combination. They are anti-inflammatory agents having amino groups as a common structure.
As the allantoin, for example, commercial products such as Merck & co, trade name RonaCare Allantoin manufactured by inc. And products manufactured by Permachem Asia Ltd. Can be used, and products manufactured by Kyowa Pharma Chemical co, ltd, and the like can be used.
(A) The blending amount of the components is preferably 0.005 to 1% by mass (hereinafter, the same applies) of the entire composition, more preferably 0.01 to 0.5%. The more the amount is, the more the anti-inflammatory effect is obtained, but from the viewpoint of the discoloration inhibition effect, it is preferably 1% or less. When it exceeds 1%, the formulation may undergo a yellow to brown discoloration with time.
(B) The component (A) is a compound with aldehyde group and menthofuran. They are perfume ingredients, or both may be used. (B) The component (C) has an effect of suppressing the occurrence of the odor itself generated by the blending of the component (C). In addition, the composition also has an effect of suppressing the generation of an odor due to the blending components other than the component (C).
The component (B) is, for example, trans-2-hexenal, phenylacetaldehyde, propionaldehyde, citral, ethylvanillin, cinnamaldehyde, menthofuran or the like, particularly from the viewpoint of suppression of discoloration of the preparation, and among them, trans-2-hexenal, phenylacetaldehyde, citral, menthofuran or the like is preferable.
(B) The components may be used singly in an amount of 1 kind, or in terms of the effect, 2 or more kinds may be used in combination.
(B) The components may be blended with components separated from the essential oil or synthesized components, or may be blended in a state of being contained in the essential oil without being separated from the essential oil, for example, peppermint oil containing menthofuran may be blended.
(B) The component (c) may be commercially available products such as those manufactured by the well-known fragrance manufacturing method (incorporated herein by reference), those manufactured by Feng Yu fragrance (incorporated herein by reference), and those manufactured by Changchun fragrance (incorporated herein by reference).
(B) The blending amount of the component (A) is preferably 0.0001 to 0.5%, more preferably 0.0005 to 0.1% of the whole composition. The taste is much better and the odor can be suppressed, but from the viewpoint of the discoloration suppressing effect, it is preferably 0.5% or less.
(C) The components are polyacrylate with weight average molecular weight of 1000-20000. (C) The component (A) is a discoloration inhibitor, and exhibits a discoloration inhibition effect that can inhibit discoloration and discoloration of the preparation caused by the combination of the components (A) and (B) even with time.
The weight average molecular weight (Mw) of the polyacrylate is 1000 to 20000, preferably 1000 to 10000. When the weight average molecular weight is 1000 or more, a sufficient discoloration inhibition effect can be obtained. When the content is 20000 or less, the discoloration-inhibiting effect can be sufficiently ensured. When the content exceeds 20000, the discoloration inhibition effect may be reduced, and yellowing to brown discoloration may occur in the preparation with time.
The weight average molecular weight is measured by GPC (gel permeation chromatography) under the method and measurement conditions described in japanese patent No. 5740859 (the same applies hereinafter). The following is shown in detail.
The method for measuring the weight average molecular weight comprises the following steps:
the weight average molecular weight is a value measured using a gel permeation chromatograph/multi-angle laser light scattering detector (GPC-MALLS), under the following conditions.
Mobile phase: 0.3M NaClO 4
NaN 3 Column of aqueous solution: TSKgel alpha-M2 root
Pre-column: TSKguardcolumnα
Standard substance: polyethylene glycol
From the viewpoint of the discoloration inhibition effect, the polyacrylate as the component (C) is preferably a linear polyacrylate. The salt is preferably a monovalent salt, more preferably an alkali metal salt or an ammonium salt, further preferably an alkali metal salt such as a sodium salt or a potassium salt, and particularly preferably a sodium salt.
As such polyacrylate, commercially available products sold by Polysciences Inc. and Toyama Synthesis (Inc.) can be used. Specifically, as a commercial product, it is possible to use: sodium polyacrylate (Mw: 1000), manufactured by Polysciences inc; sodium polyacrylate (Mw: 6000), straight chain, manufactured by Toyama Synthesis (Co., ltd.); jurymer AC-10NP; AC-10NPD; aron T-50; sodium polyacrylate (Mw: 9000), manufactured by Polysciences inc; sodium polyacrylate (Mw: 20000), straight chain, manufactured by Toyama Synthesis (Co., ltd.); aron A-20UN, etc.
The polyacrylate component (C) has a lower weight average molecular weight than the crosslinked polyacrylate of a binder usually used in a dentifrice, and is different from the polyacrylate known as a binder. When a polyacrylate other than the component (C) is used instead of the component (C) or when a polyacrylic acid other than a salt is used, discoloration of the preparation cannot be suppressed and the discoloration suppressing effect is poor.
(C) The blending amount of the components is preferably 0.01 to 1%, more preferably 0.05 to 0.5% of the entire composition. When the blending amount is 0.01% or more, the discoloration inhibiting effect can be sufficiently obtained. When the content is 1% or less, the peculiar smell due to the component (C) itself can be sufficiently suppressed, and a favorable taste can be maintained.
In the oral composition of the present invention, the mass ratio of (C)/(a), which is the ratio of the amounts of the component (a) and the component (C), is 0.1 to 21, preferably 0.5 to 15. (C) The mass ratio/(a) is within the above range, whereby the off-flavor can be suppressed and an excellent discoloration suppressing effect can be obtained. When the content is less than 0.1, the discoloration inhibition effect is poor, and the preparation undergoes a yellow-brown discoloration with time, and when the content exceeds 21, the odor of the component (C) itself cannot be inhibited, the taste becomes poor, and the preference is lowered.
The oral composition of the present invention can be prepared into a dentifrice, a mouthwash, a coating agent, a patch, etc., and is particularly preferably prepared into a dentifrice or a mouthwash, and is particularly preferably prepared into a dentifrice, preferably a dentifrice composition. The dosage form may be in the form of a liquid, paste, or the like, and among dentifrices, toothpastes, liquid dentifrices, wet dentifrices, and the like are preferable, and toothpastes are particularly preferable. In addition to the above components, any other components may be appropriately blended in accordance with the purpose, formulation, etc., within a range that does not hinder the effects of the present invention. Specifically, a surfactant, an abrasive, a thickener, and a binder may be blended with the toothpaste, and if necessary, a sweetener, a preservative, a coloring matter, a known oral flavor other than the component (B), an active ingredient, and the like may be blended.
As the surfactant, an anionic surfactant and a nonionic surfactant may be blended.
Examples of the anionic surfactant include alkyl sulfates having an alkyl group having 12 to 14 carbon atoms, particularly 12 carbon atoms, acyl amino acid salts, acyl taurates, and the like. The acyl groups of the acyl amino acid salt and the acyl taurate are each preferably 12 to 14 carbon atoms, more preferably 12 carbon atoms. Specifically, as the alkyl sulfate, there may be mentioned: lauryl sulfate, myristyl sulfate, and the like. Examples of the acyl amino acid salt include: acyl glutamate such as lauroyl glutamate and myristoyl glutamate, acyl sarcosinate such as lauroyl sarcosinate, and the like. Examples of the acyl taurates include lauroyl methyl taurates and the like. The salt is preferably an alkali metal salt such as sodium salt or potassium salt. These may be used singly or in combination of 1 or more than 2, and particularly preferably alkyl sulfate, acyl sarcosinate, acyl taurate. Among them, an anionic surfactant having a hydrocarbon group (lauryl group) of 12 carbon atoms is preferable, and particularly, an alkyl sulfate (sodium salt) is more preferable in view of excellent feeling in use such as dispersibility of the preparation than other surfactants.
Examples of the nonionic surfactant include: polyoxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene ether of glyceride, sucrose fatty acid ester, alkanolamide, glycerin fatty acid ester, etc. Among them, polyoxyethylene alkyl ether and polyoxyethylene hydrogenated castor oil are preferably used in view of the solubility and stable compounding of the perfume components. The number of carbon atoms of the alkyl chain of the polyoxyethylene alkyl ether is preferably 14 to 20, and the average addition mole number of ethylene oxide is preferably 3 to 30. The average addition mole number of ethylene oxide of the polyoxyethylene hydrogenated castor oil is preferably 10 to 100. In particular, when incorporated in a dentifrice composition, the average molar number of addition of ethylene oxide is preferably 10 to 30.
Examples of the polishing agent include: silica-based abrasives such as crystalline silica, amorphous silica, silica gel, and aluminum silicate, zeolite, anhydrous calcium hydrogen phosphate, dibasic calcium phosphate dihydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, aluminum oxide, magnesium carbonate, tribasic magnesium phosphate, zirconium silicate, and tricalcium phosphate (Ca) 3 (PO 4 ) 2 ) Hydroxyapatite, tetracalcium phosphate (Ca) 4 (PO 4 ) 2 O), a synthetic resin polishing agent. The amount of the abrasive to be blended is usually 5 to 70%, particularly 10 to 50% of the entire composition.
Examples of the thickener include: sugar alcohols such as sorbitol, xylitol and erythritol, and polyhydric alcohols such as propylene glycol, butylene glycol, glycerin and polyethylene glycol. The amount of the thickener blended is usually 0 to 70%, particularly 3 to 50% of the entire composition.
As the binder, an organic binder or an inorganic binder can be blended. Specifically, there may be mentioned: among them, inorganic binders, particularly thickening silica, are preferable from the viewpoints of suppression of discoloration and odor of the preparation. The amount of the binder to be blended is usually 0.1 to 10% by mass, particularly 0.1 to 5% by mass of the entire composition.
Examples of the sweetener include saccharin sodium.
Examples of the preservative include: benzoate such as sodium benzoate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate, and the like.
Examples of the coloring matter include brilliant blue, tartrazine, etc. as an edible coloring matter, and titanium oxide pigment.
Examples of any active ingredient (pharmaceutical ingredient) include: antibacterial agents or antimicrobial agents such as chlorhexidine, triclosan, isopropyl methylphenol, cetylpyridinium chloride, benzethonium chloride, zinc gluconate, zinc citrate, dental calculus preventative agents such as ethane hydroxybisphosphonate, antiinflammatory agents such as glycyrrhizic acid and salts thereof, enzyme agents such as epsilon-aminocaproic acid, dextranase, mutanase, lysozyme chloride, vitamins such as ascorbic acid and tocopherol acetate, astringents such as sodium chloride, sensory allergy inhibitors such as aluminum lactate and strontium chloride, and fluorides such as sodium fluoride, sodium monofluorophosphate and stannous fluoride. These ingredients can be used in effective amounts within pharmaceutically acceptable ranges.
Examples
The present invention will be specifically described below by way of examples and comparative examples, but the present invention is not limited to the examples described below. In the examples described below,% represents% by mass unless otherwise specified.
Examples and comparative examples
Dentifrice compositions (toothpastes) having the compositions shown in tables 1 to 9 were prepared by a usual method, and they were used as test dentifrice compositions and evaluated by the following methods. The results are also recorded in the table.
(1) Method for evaluating appearance stability (discoloration inhibition effect) of preparation
A26 mm diameter laminated tube container (LDPE 55/PET12/LDPE 20/white LDPE60/EMAA20/AL10/EMAA30/LDPE20/LLDPE30 (manufactured by Dain printing Co., ltd.) having an innermost layer composed of a linear low density polyethylene) was filled with 50g of the dentifrice composition, and the container was stored in a constant temperature bath at 60℃for 1 month and then returned to room temperature. Regarding the appearance (degree of discoloration) of the formulation when the dentifrice composition was extruded from the laminate tube container, the dentifrice composition of the same composition stored at-5℃for 1 month was used as a control, and the discoloration inhibition effect was evaluated on the basis of the following evaluation. Furthermore, each dentifrice composition immediately after preparation was white.
Evaluation criterion for discoloration inhibition effect
And (3) the following materials: compared with the reference substance, no color change exists
O: almost no color change compared with the control
Delta: has color change (Huanghe color change) compared with control
X: the color change (Huanghe discoloration) was remarkable as compared with the control
(2) Method for evaluating taste (unobvious degree of odor)
10 subjects placed 1g of the dentifrice composition on a toothbrush and brushed their teeth for 3 minutes, the taste (degree of unnoticeable odor) when cleaned in the oral cavity was evaluated on the following scale. The average score of 10 subjects was determined, and the taste (degree of unnoticeable odor) was evaluated on the basis of the following evaluation criteria.
Scoring criteria for taste (degree of unnoticed off-taste)
4, the following steps: no bad smell is felt in the oral cavity
3, the method comprises the following steps: hardly feel bad smell in oral cavity
2, the method comprises the following steps: slightly perceived bad smell in the oral cavity
1, the method comprises the following steps: a strong bad smell is felt in the oral cavity
Evaluation criterion of taste (unobvious degree of odor)
And (3) the following materials: average 3.5 min to 4.0 min
O: average 3.0 min or more and less than 3.5 min
Delta: average score of 2.0 or more and less than 3.0
X: average 1.0 min or more and less than 2.0 min
Details of the use of the raw materials are shown below.
(A) Composition of the components
Allantoin
Trade names; ronaCare Allantoin Merck & Co., inc
Tranexamic acid
Kyowa Pharma Chemical Co., ltd
(B) Composition of the components
Trans-2-hexenal
Manufactured by the well perfume manufacturing
Phenylacetaldehyde
Feng Yu spice (manufactured by Kagaku Co., ltd.)
Citral
Radix Et rhizoma Rhei spice (from Corp.) and its preparation method
Menthofuran
Feng Yu spice (manufactured by Kagaku Co., ltd.)
(C) Composition of the components
Sodium polyacrylate (Mw: 1000)
Linear, polysciences Inc
Sodium polyacrylate (Mw: 6000)
Straight chain, trade name: jurymer AC-10NP, sodium polyacrylate manufactured by Toyama Synthesis (Mw: 9000)
Linear, polysciences Inc
Sodium polyacrylate (Mw: 20000)
Straight chain, trade name: aron A-20UN, sodium polyacrylate (Mw: 300000) manufactured by Tokyo Co., ltd. (comparative product)
Polysciences Inc. preparation
TABLE 1
TABLE 2
TABLE 3
TABLE 4
TABLE 5
TABLE 6
TABLE 7
TABLE 8
TABLE 9
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Claims (5)
1. An oral composition comprising:
(A) More than 1 kinds of allantoin and tranexamic acid,
(B) More than 1 selected from trans-2-hexenal, phenylacetaldehyde, citral and menthofuran, and
(C) A polyacrylate having a weight average molecular weight of 1000 or more and 10000 or less,
wherein the mass ratio of (C)/(A) is 0.1-21.
2. The oral composition of claim 1, wherein,
(B) The component is selected from trans-2-hexenal, phenylacetaldehyde and menthofuran.
3. The oral composition of claim 1, wherein,
the oral composition contains 0.005-1% by mass of component (A), 0.0001-0.5% by mass of component (B), and 0.01-1% by mass of component (C).
4. The oral composition according to claim 2, wherein,
the oral composition contains 0.005-1% by mass of component (A), 0.0001-0.5% by mass of component (B), and 0.01-1% by mass of component (C).
5. The oral composition according to any one of claims 1 to 4, wherein,
the oral composition is a dentifrice composition.
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| JP2019-232279 | 2019-12-24 | ||
| JP2019232279A JP7342688B2 (en) | 2019-12-24 | 2019-12-24 | Oral composition |
| PCT/JP2020/047387 WO2021132067A1 (en) | 2019-12-24 | 2020-12-18 | Composition for oral cavity |
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| JP (1) | JP7342688B2 (en) |
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| WO (1) | WO2021132067A1 (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62277314A (en) * | 1986-02-05 | 1987-12-02 | Lion Corp | Composition for oral cavity |
| WO2019107340A1 (en) * | 2017-11-30 | 2019-06-06 | ライオン株式会社 | Composition for oral use |
| CN110494123A (en) * | 2017-04-21 | 2019-11-22 | 狮王株式会社 | Oral biological film remover and composition for oral cavity |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS51101115A (en) * | 1975-02-26 | 1976-09-07 | Sunstar Inc | Kokozaisoseibutsuno seiho |
| US4272513A (en) * | 1980-01-31 | 1981-06-09 | Colgate-Palmolive Company | Stabilized oral composition |
-
2019
- 2019-12-24 JP JP2019232279A patent/JP7342688B2/en active Active
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2020
- 2020-12-18 CN CN202080090372.1A patent/CN114867455B/en active Active
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62277314A (en) * | 1986-02-05 | 1987-12-02 | Lion Corp | Composition for oral cavity |
| CN110494123A (en) * | 2017-04-21 | 2019-11-22 | 狮王株式会社 | Oral biological film remover and composition for oral cavity |
| WO2019107340A1 (en) * | 2017-11-30 | 2019-06-06 | ライオン株式会社 | Composition for oral use |
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| CN114867455A (en) | 2022-08-05 |
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