CN115400039A - Oral acid-base balance preparation and application thereof - Google Patents

Oral acid-base balance preparation and application thereof Download PDF

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Publication number
CN115400039A
CN115400039A CN202211264870.0A CN202211264870A CN115400039A CN 115400039 A CN115400039 A CN 115400039A CN 202211264870 A CN202211264870 A CN 202211264870A CN 115400039 A CN115400039 A CN 115400039A
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oral
acid
histidine
cysteine
base
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陈新宇
郑伟
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Yongzhi Shanghai Biotechnology Co ltd
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Yongzhi Shanghai Biotechnology Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A61K8/447Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof containing sulfur
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cosmetics (AREA)

Abstract

The invention belongs to the technical field of oral care, and particularly relates to an oral acid-base balance preparation and application thereof. The preparation is a mixed aqueous solution of histidine and cysteine, the concentration of histidine and cysteine in the mixed aqueous solution is the same and is between 0.1 and 0.3mol/L, and the buffering pH range of the oral acid-base equilibrium preparation is between 5.5 and 7.5; the oral acid-base balance preparation is used in mouthwash or oral spray, not only can clean the oral cavity and leave a comfortable and refreshing feeling in the oral cavity, but also can keep the acid-base balance of the oral cavity and reduce the incidence rate of dental erosion.

Description

Oral acid-base balance preparation and application thereof
Technical Field
The invention belongs to the technical field of oral care, and particularly relates to an oral acid-base balance preparation and application thereof.
Background
The normal pH value of the oral saliva is 5.5-7, and if the pH value of the oral saliva is lower than 5.5, demineralization and caries may occur on teeth. When the oral environment is maintained below pH5 for a long time, the oral environment is in an acidic state, which is likely to increase the risk of dental caries and dental erosion. Especially, when the food containing saccharide is eaten, the pH value of the oral cavity is suddenly reduced, and if the oral cavity is in acid-base imbalance for a long time, the tooth is demineralized and the tooth cavity is damaged.
Oral care products such as mouthwashes or oral sprays can leave a pleasant, refreshing sensation in the mouth by cleaning the mouth; a buffer solution system in a mouth wash or oral spray can resist the influence of a certain amount of external acid-base changes and can keep the pH value of the solution basically unchanged, and the buffer solution is a solution formed by buffering pairs of weak acid and conjugate base thereof or weak base and conjugate acid thereof and can slow down the change of the pH when a certain amount of other substances are added. The gargle or oral spray in the current market mainly adopts an inorganic salt buffer solution formula, but inorganic salts such as citrate and phosphate are easy to combine with calcium ions to cause tooth demineralization. And the phosphate is bitter and astringent in taste and bad in mouthfeel.
Disclosure of Invention
In view of the above-mentioned existing disadvantages, the present invention aims to provide an oral acid-base balance preparation and its application. The invention prepares oral care products, such as gargle or oral spray, based on the acid-base equilibrium preparation, not only can leave comfortable and refreshing feeling in the oral cavity by cleaning the oral cavity, but also the amino acid system can reduce the incidence rate of dental erosion besides maintaining the acid-base equilibrium in the oral cavity.
The oral acid-base balance preparation utilizes the characteristics of the molecular structure of amino acid, and combines weakly acidic amino acid and weakly alkaline amino acid to form a buffer system. The amino acid molecule contains both amino and carboxyl groups and exists in the form of dipole ions in aqueous solution. The amino acid, when fully protonated, can be considered a weak polybasic acid and can be used as a buffer solution. Specifically, the invention provides an oral acid-base balance preparation which is a mixed aqueous solution of histidine and cysteine. Histidine, also known as α -amino β -imidazolyl propionic acid, is a basic amino acid. The dissociation constant of the imidazolyl group is 6.0, namely the concentration of dissociated protons is similar to that of water, and the histidine can be used as a proton donor and a proton acceptor. The pH of the 1wt% aqueous histidine solution was approximately 7.5. Cysteine is weakly acidic amino acid, and the pH value of 1% cysteine aqueous solution is close to 6.1.
The technical scheme of the invention is specifically introduced as follows.
The invention provides an oral acid-base equilibrium preparation which is a mixed aqueous solution of histidine water and cysteine.
The concentrations of histidine and cysteine in the mixed aqueous solution are the same, and are respectively between 0.1 and 0.3 mol/L.
The pH of the mixed aqueous solution is in the range of 5.5-7.5.
The invention also provides application of the oral acid-base balance preparation in oral care products. Preferably, the oral care product is a mouthwash or oral spray.
Compared with the prior art, the invention has the beneficial effects that:
(1) The oral acid-base equilibrium preparation of the invention consists of two amino acids with the same equivalent concentration ratio to form a buffer pair, and is used for gargling
The water and the oral spray liquid can maintain the neutral pH balance of the oral cavity, prevent dental plaque from producing acid, prevent dental erosion caused by residual substances such as saccharides or carbonic acid and the like, and easily increase the risk of dental caries due to enamel demineralization.
(2) The oral acid-base balance preparation adopts amino acid, is nontoxic and mild, is used in oral care products, and has good safety and long-acting stability.
(3) Histidine is an important component of amelogenin in tooth enamel (also called enamel, which is the outermost tissue of teeth) in terms of the composition of the oral acid-base balance preparation of the invention; cysteine protein (cystatin) is an important family of biological active substances in saliva and is one of the main components of the tooth surface acquired membrane. It can regulate oral cavity calcium-phosphorus balance, and has strong inhibiting effect on various endogenous and exogenous cysteine-containing proteinase, so that the invented oral acid-base balance preparation can be used for gargle water and oral cavity spray liquor, and possesses the functions of preventing and curing oral cavity diseases, specially for curing periodontal disease, and possesses the function of protecting oral cavity.
Detailed Description
The technical solution of the present invention is described in detail below with reference to specific examples.
Table 1 shows the raw material formulation of 4 examples for preparing a mouthwash or mouth spray.
Figure DEST_PATH_IMAGE001
In the examples, the inventors prepared oral care products based on oral acid-base balance formulations: the gargle or oral spray liquid is prepared by adding edible essence, flavoring agent, ethanol, surfactant, solubilizer, antiseptic, functional additive and distilled water into oral care product. Wherein the edible essence has the function of suppressing oral cavity peculiar smell by pleasant smell; the flavoring agent is used for improving mouth feel of collutory and oral spray; the ethanol has stimulating and refreshing effects, and can enhance perfume effect; the surfactant and the solubilizer are beneficial to fully dissolving the perfume ingredients and also contribute to the cleaning effect and the sterilization effect; the functional additive is mainly responsible for cleaning oral cavity, sterilizing, inhibiting bacteria and the like.
Example 1
1. Prepare 0.3M buffer pair solution: (0.3M histidine preparation: 46.5 g histidine were dissolved in 1000 mm of water
Distilled water is increased; 0.3M cysteine: weighing 36.3 g of cysteine, and dissolving in 1000 ml of distilled water; mixing 800 ml of 0.3M histidine solution with 200 ml of 0.3M cysteine solution to prepare 1000 ml of 0.3M histidine cysteine buffer solution
2. According to the addition amount in the formula, the hydrogenated castor oil, the cinnamon oil and the glycerol are stirred and dissolved in the ethanol;
3. dissolving lysozyme, glycerol, sorbitol and xylitol in histidine cysteine buffer solution, and stirring for dissolving;
4. mixing the above 2, 3 solutions, aging, cooling (5 deg.C), and filtering.
The pH of the rinse was measured to be 6.88. After adding 1 ml of each of the tobrespectively (pH 3.3) to 5 ml of the rinse and the control (adjusted to pH6.88 but without the addition of the histidine and cysteine buffer pairs), the rinse solution was measured to have a pH of 6.60 and the control to 5.43.
Example 2
1. Prepare 0.3M buffer pair solution: ( Preparing 0.3M histidine: weighing 46.5 g of histidine and dissolving in 1000 ml of distilled water; 0.3M cysteine: weighing 36.3 g of cysteine, and dissolving in 1000 ml of distilled water; 500 ml of 0.3M histidine solution is mixed with 500 ml of 0.3M cysteine solution to prepare 1000 ml of 0.3M histidine cysteine pair buffer solution )
2. According to the addition amount in the formula, the hydrogenated castor oil, the cinnamon oil and the glycerol are stirred and dissolved in the ethanol;
3. dissolving lysozyme, glycerol, sorbitol and xylitol in histidine cysteine buffer solution, and stirring for dissolving;
4. mixing the above 2, 3 solutions, aging, cooling (5 deg.C), and filtering.
The pH of the rinse was measured to be 6.45. After adding 1 ml of each of the tobrespectively (pH 3.3) to 5 ml of the rinse and the control (adjusted to pH6.45 but without the addition of the histidine and cysteine buffer pairs), the rinse solution was measured to have a pH of 6.24 and the control to 5.43.
Example 3
1. Prepare 0.2M buffer pair solution: ( Preparing 0.2M histidine: weighing 31 g of histidine and dissolving in 1000 ml of distilled water; 0.2M cysteine: weighing 24.2 g of cysteine, and dissolving in 1000 ml of distilled water; 700 ml of 0.2M histidine solution is mixed with 300 ml of 0.2M cysteine solution to prepare 1000 ml of 0.2M histidine cysteine pair buffer solution )
2. According to the addition amount in the formula, the hydrogenated castor oil, the cinnamon oil and the glycerol are stirred and dissolved in the ethanol;
3. dissolving lysozyme, glycerol, sorbitol and xylitol in histidine cysteine buffer solution, and stirring for dissolving;
4. mixing the above 2, 3 solutions, aging, cooling (5 deg.C), and filtering.
The pH of the rinse was measured to be 6.65. After adding 1 ml of each of the tobrespectively (pH 3.3) to 5 ml of the rinse and the control (adjusted to pH6.65, but without the addition of the histidine and cysteine buffer pairs), the rinse solution was measured to have a pH of 6.31 and the control to 5.43.
Example 4
1. Prepare 0.1M buffer pair solution: ( Preparing 0.1M histidine: weighing 15.5 g of histidine and dissolving in 1000 ml of distilled water; 0.1M cysteine: weighing 12.1 g of cysteine, and dissolving in 1000 ml of distilled water; mixing 800 ml of 0.1M histidine solution with 200 ml of 0.1M cysteine solution to prepare 1000 ml of 0.1M histidine-cysteine buffer solution )
2. According to the addition amount in the formula, the hydrogenated castor oil, the cinnamon oil and the glycerol are stirred and dissolved in the ethanol;
3. dissolving lysozyme, glycerol, sorbitol and xylitol in histidine cysteine buffer solution, and stirring for dissolving;
4. mixing the above 2, 3 solutions, aging, cooling (5 deg.C), and filtering.
The pH of the rinse was measured to be 6.42. After adding 1 ml of each of the Spicel (pH 3.3) to 5 ml of the rinse and to the control rinse (adjusted to pH6.42 but without the histidine and cysteine buffer pairs), the rinse solution was measured to have a pH of 6.11 and the control rinse to 5.43.
According to the above examples, it can be seen that the buffer pair composed of histidine and glycine has a good buffering effect in the acid-base neutral range (pH 5.5-pH 7.5). The combination of the two parts not only greatly expands the buffering range and the buffering capacity, but also has better physiological compatibility and oral health auxiliary function compared with an inorganic buffering system.

Claims (6)

1. An oral acid-base equilibrium preparation is characterized in that the oral acid-base equilibrium preparation is a mixed aqueous solution of histidine and cysteine.
2. The oral acid-base balanced formulation of claim 1, wherein histidine and the moiety are mixed in an aqueous solution
The concentrations of cystine are the same and are respectively between 0.1 and 0.3 mol/L.
3. The oral acid-base balanced formulation of claim 1, wherein the aqueous mixed solution has a buffered pH range
Between 5.5 and 7.5.
4. Use of the oral acid-base balance formulation of claim 1 in an oral care product.
5. The use according to claim 4, wherein the oral care product is a mouthwash or an oral spray.
6. The use of claim 4, wherein the oral care product comprises an oral acid base balancing agent
Besides the agent, the agent also comprises edible essence, flavoring agent, ethanol, surfactant, solubilizer, preservative, functional additive and distilled water.
CN202211264870.0A 2022-10-17 2022-10-17 Oral acid-base balance preparation and application thereof Pending CN115400039A (en)

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62221630A (en) * 1986-03-24 1987-09-29 Lion Corp Artificial saliva composition
CN101938982A (en) * 2008-02-08 2011-01-05 高露洁-棕榄公司 Oral care product and methods of use and manufacture thereof
DE102010003280A1 (en) * 2010-03-25 2011-02-03 Henkel Ag & Co. Kgaa Oral-, dental care- and -cleaning products, useful for plaque reduction and/or caries prevention, comprise oligo- or polypeptide of vegetable origin, containing basic amino acids e.g. arginine, and acidic amino acids e.g. aspartic acid
US20210121392A1 (en) * 2019-09-30 2021-04-29 Yunming Shi Oral Care Compositions Comprising Hops Beta Acid And Amino Acid
WO2021203132A1 (en) * 2020-03-30 2021-10-07 Colgate-Palmolive Company Improving, maintaining, protecting and repairing tissue integrity, barrier function and immunity using a composition comprising a source of zinc ions

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62221630A (en) * 1986-03-24 1987-09-29 Lion Corp Artificial saliva composition
CN101938982A (en) * 2008-02-08 2011-01-05 高露洁-棕榄公司 Oral care product and methods of use and manufacture thereof
DE102010003280A1 (en) * 2010-03-25 2011-02-03 Henkel Ag & Co. Kgaa Oral-, dental care- and -cleaning products, useful for plaque reduction and/or caries prevention, comprise oligo- or polypeptide of vegetable origin, containing basic amino acids e.g. arginine, and acidic amino acids e.g. aspartic acid
US20210121392A1 (en) * 2019-09-30 2021-04-29 Yunming Shi Oral Care Compositions Comprising Hops Beta Acid And Amino Acid
WO2021203132A1 (en) * 2020-03-30 2021-10-07 Colgate-Palmolive Company Improving, maintaining, protecting and repairing tissue integrity, barrier function and immunity using a composition comprising a source of zinc ions

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
马飞等: "唾液有机成分与龋易感性", 中国使用口腔科杂志, vol. 1, no. 10, pages 631 - 633 *

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