WO2002002124A1 - Compositions renfermant des esters d'acide ascorbique-acide phosphorique - Google Patents

Compositions renfermant des esters d'acide ascorbique-acide phosphorique Download PDF

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Publication number
WO2002002124A1
WO2002002124A1 PCT/JP2001/002466 JP0102466W WO0202124A1 WO 2002002124 A1 WO2002002124 A1 WO 2002002124A1 JP 0102466 W JP0102466 W JP 0102466W WO 0202124 A1 WO0202124 A1 WO 0202124A1
Authority
WO
WIPO (PCT)
Prior art keywords
ascorbic acid
salt
composition
phosphate
sodium
Prior art date
Application number
PCT/JP2001/002466
Other languages
English (en)
Japanese (ja)
Inventor
Mizuya Yamamoto
Susumu Hiratsuka
Original Assignee
Lion Corporation
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 Lion Corporation filed Critical Lion Corporation
Priority to AU2001242807A priority Critical patent/AU2001242807A1/en
Publication of WO2002002124A1 publication Critical patent/WO2002002124A1/fr

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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
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • 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
    • A61K8/60—Sugars; 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
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0063—Periodont
    • 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 a composition for oral cavity and dermis containing ascorbic acid phosphates.
  • Ascorbic acid phosphate and salts thereof play an important role in the expression of various enzyme activities in living organisms, and are known to have various physiological activities. In particular, it acts as a coenzyme for prolyl and lysyl hydroxylase and is said to be essential for collagen synthesis. In recent years, it has also attracted attention as an antioxidant bimin which eliminates excess active oxygen produced in the body and protects biological tissues from oxygen damage, and is known to have various physiological activities. .
  • compositions containing ascorbic acid phosphate and its salts include cosmetics (JP-A-62-298508 and JP-A-3-63208), and whitening cosmetics (JP-A-63-243014).
  • Gazettes JP-A-1-305509, JP-A-3-133914), oral agents (JP-A-62-96408), bath agents (JP-A-62-96410), oral compositions ( JP-A-2-292210, JP-A-2-292211, JP-A-173173727), skin external preparations (JP-A-3-34908, JP-A-7-206632, JP-A-133951), etc. Stuff has been proposed.
  • An object of the present invention is to provide a composition containing ascorbic acid phosphate and a salt thereof in a stable and active state.
  • the present inventors have found that, in a composition containing ascorbic acid phosphate or a salt thereof, an anionic surfactant, a monosaccharide alcohol having 4 or more carbon atoms, an oligosaccharide, Selected from alcohol and reduced syrup
  • the stability over time of the composition containing the ascorbic acid phosphate or a salt thereof is improved, and the ascorbic acid phosphate is maintained even after long-term storage.
  • many of the compositions containing the ascorbic acid phosphate or a salt thereof have an initial pH of 8.0 or more, particularly 8.5 to 9.5, even if adjusted to around room temperature after production. Even after storage, pH may change significantly within one month, and pH may be lower than 8.0.
  • composition of the present invention comprises (A) ascorbic acid phosphate or a salt thereof, (B) anionic surfactant, (C) a monosaccharide alcohol having 4 or more carbon atoms, an oligosaccharide alcohol, and reduced starch syrup.
  • A ascorbic acid phosphate or a salt thereof
  • B anionic surfactant
  • C a monosaccharide alcohol having 4 or more carbon atoms
  • an oligosaccharide alcohol an oligosaccharide alcohol
  • reduced starch syrup reduced starch syrup.
  • One or more selected sugar alcohols are contained, the content of calcium and aluminum ion sources is less than 10% by mass of the whole composition, and after storage at 25 ° C for one month, pH is 8.0 or more.
  • ascorbic acid phosphoric acid ester is one in which one or more of the hydroxyl groups at any of the 2, 3, 5, and 6 positions of ascorbic acid has become an ester of a compound such as phosphoric acid or polyphosphoric acid.
  • examples thereof include ascorbic acid-2-phosphate, ascorbic acid-3-phosphate, ascorbic acid-6-phosphate, and ascorbic acid-12-polyphosphate.
  • the salts include alkali metal salts such as sodium salt, potassium salt, calcium salt, and magnesium salt, and alkaline earth metal salts.
  • magnesium ascorbate phosphate sodium salt is preferably used from the viewpoint of the effect of preventing and improving periodontal disease.
  • the compounding amount is preferably 0.01 to 10%, particularly preferably 0.01 to 5% of the whole composition. If the amount is too small, the effect may not be sufficiently exhibited, and if the amount is too large, the usability may be reduced.
  • an anionic surfactant is blended for the purpose of imparting an appropriate foaming power or imparting dispersibility. In this case, it has been said that the anionic surfactant reduces the stability of the ascorbic acid phosphate or a salt thereof due to its combination.
  • the composition is stored at 25 ° C for one month. By adjusting the pH to 8.0 or more, stabilization of ascorbic acid phosphate or a salt thereof was successfully achieved even when an anionic surfactant was added.
  • anionic surfactant various kinds of conventionally known anionic surfactants, for example, alkyl sulfate, polyoxyethylene alkyl sulfate, ⁇ -sulfo fatty acid ester, ⁇ olefin sulfonate, alkyl Or hydroxyalkyl ether carboxylate, ⁇ -acylated taurine, ⁇ -acylated glycine, ⁇ -asinoleated aspartate, ⁇ -acylated sarcosine, ⁇ -acylated glutamate, monoalkyl phosphate ester salt , Alkyl amide ether sulfate, alkyl (poly) glyceryl ether sulfonate, alkyl (poly) dali seryl ether carboxylate, secondary amide-type amino acid salt, alkyl tartrate, alkyl amide malate , Quinic acid alkylamide, alkyl ( Li) glyceryl sulf
  • the compounding amount of the anionic surfactant is appropriately selected, but is preferably 0.1 to 10%, particularly preferably 0.5 to 3% of the whole composition.
  • the composition of the present invention further contains one or more of monosaccharide alcohols having 4 or more carbon atoms, oligosaccharide alcohols, and reduced starch syrups.
  • monosaccharide alcohol having 4 or more carbon atoms include erythritol, xylitol, mannitol, sorbitol, galactitol, and iditol.
  • Oligosaccharide alcohols include, for example, mulch!
  • One example is Examples of the reduced syrup include reduced saccharified reduced syrup, highly saccharified reduced syrup, and reduced maltose syrup. These may be used alone or in combination of two or more.
  • the content of these sugar alcohols can be 1 to 80%, particularly 5 to 60% of the whole composition, but is 0.5 as a weight ratio to the amount of water contained in the composition. As described above, it is more preferable that the compound is blended at a ratio of 0.5 to 2.0, and more preferably 0.75 to 1.5, whereby the effect of ascorbic acid phosphate ester or a salt thereof is reduced. It can be more effectively exerted.
  • Glycerin a monosaccharide alcohol having 3 carbon atoms, has no such effect.
  • the content of a calcium ion source, an aluminum ion source, for example, a calcium-containing compound such as calcium hydrogen phosphate, tertiary calcium phosphate, or calcium pyrophosphate, or an aluminum-containing compound such as aluminum hydroxide is adjusted to the entire composition. Is less than 10%, preferably 1% or less, more preferably 0.1% or less, and it is particularly preferable not to mix these calcium-containing compounds and aluminum-containing compounds.
  • the ascorbic acid phosphate or a salt thereof reacts with calcium to form an insoluble calcium salt.
  • the decomposition of a salt thereof is promoted, but these disadvantages can be prevented by limiting the content of the calcium-containing compound and the aluminum-containing compound to less than 10% of the whole composition.
  • composition of the present invention can be used for various uses, such as for the oral cavity and for the outer skin, and its dosage form is variously selected. However, it may be prepared into a dosage form such as a paste, liquid, or cream. Is preferred.
  • compositions for the oral cavity are prepared as dentifrices such as toothpastes and liquid dentifrices, gingival massage creams, topical coatings and mouthwashes.
  • dentifrices such as toothpastes and liquid dentifrices, gingival massage creams, topical coatings and mouthwashes.
  • abrasives, binders and sweeteners are used.
  • Agents, perfumes, various active ingredients, and the like can be added at ordinary doses.
  • the polishing agent is preferably a silica-based polishing agent such as silica gel, precipitated silica, aluminosilicate, zirconosilicate (titanium-binding silica), and other components such as magnesium carbonate, bentonite, and polymethyl methacrylate.
  • the binder include carrageenan, cellulose derivatives such as carboxymethylcellulose sodium, methylcellulose and hydroxyethylcellulose; alginic acid derivatives such as sodium alginate and propylenedaricol alginate; xanthan gum, dielan gum, trangant gum, and karaya gum.
  • gums such as poly (vinyl alcohol), sodium polyacrylate, synthetic binders such as propyloxypiryl polymer, and inorganic binders such as silica gel, veegum, and labonite .
  • the thickener As the thickener, the above sugar alcohol is used, and if necessary, dariserin, propylene glycol, polyethylene glycol, or the like may be added. In addition to the above anionic surfactant, a surfactant such as decayl laurate is used. Nonionic surfactants such as glyceryl and myristic acid diethanolamide, and amphoteric surfactants such as betaine may be blended.
  • the fragrance ingredients include menthol, anethol, carvone, eugenol, n-decyl alcohol, citronellol, ⁇ -terpineol, cineol, linamouth, ethyl linalool, peniline, thymol, peppermint oil, spearmint oil, wintergreen Flavors such as oil, t-shaped oil and eucalyptus oil can be used alone or in combination. Further, sweeteners such as saccharin sodium, perillartin, somatatin and the like may be added.
  • the present invention relates to cationic bactericides such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, decalinium chloride, and the like, such as tricoctane, hinokitiol, and biozol.
  • Enzymes such as phenolic compounds, dextranase, mutanase, lysozyme, amylase, protease, lytic enzyme, and SOD; alkali metal monofluorophosphates such as sodium monofluorophosphate and potassium monofluorophosphate; sodium fluoride; and stannous fluoride.
  • the composition of the present invention has an initial pH adjusted so that the pH after storage at 25 ° C. for one month is 8.0 or more, preferably 8.0 to 9.5, particularly 8.5 to 9.5. I do.
  • the pH after storage for one month was used instead of the initial pH because, for many compositions, the pH greatly changed within one month after production even at around room temperature, and then stabilized. This is because it was found that the pH after storage at 25 C for one month was important.
  • the pH fluctuation differs depending on the ingredients.
  • silica gel when blended, the pH increases after storage at 25 ° C for 1 month compared to the initial pH, and conversely, when precipitated silica is combined. pH drops. Therefore, to adjust the initial pH to the required pH after storage at 25 ° C for one month, set the initial pH to 25 ° C and set the pH after storage for one month according to the formulation of the composition. Adjust to lower or higher. If necessary, a method of examining the relationship between the initial pH and the pH after storage at 25 ° C for one month through preliminary tests may be adopted. For pH adjustment, commonly used pH adjusters can be used, but sodium hydroxide and potassium hydroxide can be suitably used.Also, water-soluble citrate, phosphate, Carbonates, bicarbonates and the like can also be preferably used.
  • the ascorbic acid phosphate-containing composition of the present invention contains ascorbic acid phosphate or a salt thereof in a stable and active state, and effectively exerts its effects even after long-term storage.
  • a dentifrice having the following formulation was prepared.
  • a one-week use test was performed using dentifrice for one to three months after adjustment, and the effect of improving gingivitis was observed. That is, 10 healthy volunteers used the following toothpastes A and B for one week, then stopped oral cleaning for two days, self-evaluated their gingival condition, and filled out a questionnaire. There was at least one week between each dentifrice use. In the questionnaire, the gingiva in the upper and lower jaw of the anterior teeth was observed and scored as shown below with reference to Figures 1 (A) to (C). Table 1 shows the results.
  • X indicates teeth
  • Y indicates gingiva
  • Z indicates gingivitis
  • Dentifrices were prepared by blending the components shown in Table 2 (silica, sorbitol or glycerin) with the common composition below. The pH was measured immediately after preparation of these dentifrices and after storage at 25 ° C for 1 month, 6 months, and 18 months. Also, store in a 60 ° C thermostat for 1 month. After storage for 6 months in a 40 ° C thermostat, and after storage for 18 months at 25 ° C, the residual ratio of magnesium ascorbyl phosphate was measured. It was measured. Table 2 shows the results.
  • Lauroyl sarcosine 0 2 Sodium benzoate 0, 5 Tranexamic acid 0 05 Ascorbic acid phosphate magnesium salt 0 05 Sodium tartrate 0 02 Titanium binding silica 20

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne des compositions renfermant des esters d'acide ascorbique-acide phosphorique caractérisées en ce qu'elles contiennent : (A) un ester d'acide ascorbique-acide phosphorique ou son sel ; (B) un tensioactif anionique ; et (C) un ou plusieurs alcools de sucre pris parmi des alcools polysaccharides ayant 4 atomes de carbone ou plus, des alcools oligosaccharides et des sirops d'amidon réducteur. Ces compositions renferment moins de 10 % en poids, par rapport à la composition globale, de sources d'ions calcium et magnésium, et présentent un pH de 8,0 ou plus après stockage pendant 1 mois à une température de 25 °C.
PCT/JP2001/002466 2000-06-30 2001-03-27 Compositions renfermant des esters d'acide ascorbique-acide phosphorique WO2002002124A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001242807A AU2001242807A1 (en) 2000-06-30 2001-03-27 Compositions containing ascorbic acid phosphoric acid esters

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2000199213A JP4257479B2 (ja) 2000-06-30 2000-06-30 アスコルビン酸リン酸エステル又はその塩含有歯磨剤組成物の製造方法
JP2000/199213 2000-06-30

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WO2002002124A1 true WO2002002124A1 (fr) 2002-01-10

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CN (1) CN1245985C (fr)
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WO (1) WO2002002124A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002058662A2 (fr) * 2001-01-24 2002-08-01 Oraceutical Llc Compositions topiques d'hygiene buccale

Families Citing this family (8)

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Publication number Priority date Publication date Assignee Title
JP2004035416A (ja) * 2002-06-28 2004-02-05 Sangi Co Ltd 改良３ｄｓホームケア剤及び虫歯除菌システム
JP4589236B2 (ja) * 2004-01-20 2010-12-01 株式会社コーセー 化粧料
CN101247834B (zh) * 2005-06-17 2013-10-30 生命健康科学公司 包含一种或多种二-和/或单-（电子转移剂）磷酸酯衍生物或其络合物的载体
JP5765225B2 (ja) * 2009-06-08 2015-08-19 ライオン株式会社 口腔用組成物
JP5526619B2 (ja) * 2009-06-25 2014-06-18 ライオン株式会社 練歯磨剤組成物
JP5999173B2 (ja) * 2012-03-07 2016-09-28 ライオン株式会社 口腔用組成物
CN105663015B (zh) * 2016-03-24 2018-06-29 广州健朗医用科技有限公司 一种孕产妇专用蜂胶牙膏及其制备方法
CN111759788A (zh) * 2020-07-27 2020-10-13 浙江爱尚日用品有限公司 一种防治口腔溃疡型牙膏

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04173727A (ja) * 1990-11-06 1992-06-22 Lion Corp 口腔用組成物
JP2000351905A (ja) * 1999-04-05 2000-12-19 Showa Denko Kk アスコルビン酸誘導体含有組成物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04173727A (ja) * 1990-11-06 1992-06-22 Lion Corp 口腔用組成物
JP2000351905A (ja) * 1999-04-05 2000-12-19 Showa Denko Kk アスコルビン酸誘導体含有組成物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002058662A2 (fr) * 2001-01-24 2002-08-01 Oraceutical Llc Compositions topiques d'hygiene buccale
WO2002058662A3 (fr) * 2001-01-24 2003-02-20 Oraceutical Llc Compositions topiques d'hygiene buccale

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CN1245985C (zh) 2006-03-22
AU2001242807A1 (en) 2002-01-14
JP2002020292A (ja) 2002-01-23
CN1443072A (zh) 2003-09-17
JP4257479B2 (ja) 2009-04-22

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