TWI295929B - Oral rinse composition - Google Patents

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a mouthwash composition for oral health care. The prior art U.S. Patent Publication No. US 2002/0173485 A1 discloses a pharmaceutical composition which can alleviate the pain caused by ulcers of mucous membranes (e.g., oral cavity, stomach, etc.) and to treat or prevent inflammation of the mucosa, including 1 to 0.05% by weight. Hyaluronic acid, 0.04 to 15% by weight of polyvinylpyrrolidone, and between 86 and 98% by weight of water, the composition has a viscosity of 50 to 500 centipoise (CPS). However, hyaluronic acid is a raw material that is expensive and must be stored at a low temperature, so the use of hyaluronic acid is not conducive to manufacturing costs. The content of this patent is incorporated herein by reference. Chitin and chitosan are natural non-toxic polymers and are biodegradable. Their structure is similar to cellulose, from 1000-3000 N-acetylglucosamine (N- ACETYL-2 AMINO-2 DEOXY-d-D_GLUCOSE or n-ACETYL-d-GLUCOSAMINE) A linear polymer saccharide composed of cold-1,4 bonds (the structural formulas are as follows). In nature, chitin is the most abundant amine-based polysaccharide on earth, second only to cellulose. It is mainly found in the shells of invertebrates such as insects and aquatic crustaceans, as well as the cell wall of fungi. Its role in the organism is mainly used as a body skeleton and protection. Chitosan is a chitin-deacetylated product, usually a chitin to a degree of more than 70%, which turns into an acid-soluble chitin 1295929 glycan product.

Chitosan is insoluble in water and organic solvents, but is soluble in some organic acids. Chitosan acidic solution can be used as a bacteriostatic agent due to the amino group of chitosan

(-nh2) is positively charged (_nh3+) in an acidic solution, and the cell wall of the microorganism is negatively charged, so that it can bind to the cell wall and destroy cell formation, thereby achieving an antibacterial effect. The salt after protonation (or neutralization) of chitosan can be directly dissolved in water, for example, Kytamer PCA, which is neutralized by pyrr〇lidone carboxylic acid. Chitin produced from Amerchol Corporation, which is neutralized with glutainic acid, is commercially available from Protasan Corporation. The solids of chitosan vinegar are currently used as an oral agent for adsorbing fats and lowering cholesterol, in addition to being used as an adsorbent for adsorbing heavy metals and odor molecules. In addition, an aqueous solution of a neutralized chitosan and an aqueous solution of polyvinylpyrrolidone are mixed 1295929 to prepare a film for use as a wound dressing, for example, US Pat. No. 5,420,197 and 6,379,702, the contents of each of which are incorporated by reference. Into the case.

Taiwan Patent Publication No. 520283 discloses a chitosan brewing oral liquid which is prepared by dissolving chitosan in an aqueous acid solution and preparing an aqueous solution of chitosan, wherein the chitosan has a degree of deacetylation. It is 5 〇 _99%, the molecular weight is 1000-400000, and the aqueous solution of chitosan is attached to the inner wall of the oral cavity by a mouthwash to form a film to prevent the oral mucosa from being invaded by the bacteria. The previous invention claims that its oral protective fluid can form a layer of chitosan film on the inner wall of the mouth through the mouth, protecting the oral mucosa and gums and the gums to reduce damage and pathology. Although the film formation of the chitosan solution can be used to achieve the above objectives, the bitterness of the chitosan solution is a problem, and the consumer is excluded from using the oral protective liquid of the previous case, so the oral protective liquid of the previous case is still extremely large. Improved space. The contents of this Taiwan patent are incorporated into the case by reference.

SUMMARY OF THE INVENTION A primary object of the present invention is to provide a mouthwash composition which has the bactericidal effect itself and which is advantageous in forming a protective film on the inner wall of the oral cavity. The mouthwash composition of the present invention comprises water and the following active ingredients dissolved in water: polyvinylpyrrolidone having a K value of from 30 to 100; and protonated chitosan; wherein the protonated chitosan pair Preferably, the weight ratio of polyvinylpyrrolidone is between i: 1295929 100 and 100: 100 Torr, and the mass ratio of protonated chitosan to polyvinylpyrrolidone of the mouthwash composition of the present invention is between 25: 100 to 3: 1〇〇. Preferably, the mouthwash composition of the present invention has a chitosan of 〇 丨 丨 % by weight. Preferably, the mouthwash composition of the present invention has a viscosity of from ϋ 〇 厘 centipoise, more preferably from 0.5 to 50 centipoise at room temperature. • Embodiment 1 A method suitable for preparing the mouthwash composition of the present invention comprises the steps of: a) mixing chitosan, water and acid to form an acidic aqueous solution in which chitosan is dissolved; b) comparing polyethylene 11 Lotenone' and optionally water are added to the chitosan acidic aqueous solution of step a) and stirred to form a mouthwash composition having the desired viscosity. Another suitable method for preparing the mouthwash compositions of the present invention comprises dissolving the neutralized chitosan in water, adding the polyvinylpyrrolidone to the aqueous solution, and agitating to form a mouthwash composition having the desired viscosity. It is apparent that the polyvinylpyrrolidone can also be added to the aqueous solution in which chitosan is dissolved in the form of an aqueous solution. Chitosan suitable for use in the present invention has a deacetylation degree of 60-99% and a molecular weight of 1 〇, 〇〇〇 to 1, 〇〇〇, 〇〇〇. Suitable for use in the present invention, the chitosan is suitable for use in the foregoing

1295929 The polybutyral polyacetate of the invention is subjected to a neutralized salt, such as pyrrolidone hydroxy acid salt and glutamate as described in the aforementioned prior art section. Polyvinylpyrrole, which is suitable for use in the present invention, is a polyvinylpyrrolidone having a K value of from 3 Torr to 1 Torr. The K value represents a function of the molecular weight of the polyvinylpyrrolidone. The K value is calculated from the viscosity measurement and is calculated according to the Eikentscher's formula described by Kiine, G. M., "Polyvinylpyrrolidone", Modern Plastics, ρ. 157 (Nov. 1945).

The ratio of the chitosan to the polyvinylpyrrolone in the hydrophobic composition of the present invention is in a weight ratio of from 1 to 100:100. The acid used in the step a) of the aforementioned method for preparing the mouthwash composition of the present invention is preferably selected from, but not limited to, formic acid, acetic acid, lactic acid, citric acid (citric acid). Acid), tartaric acid, succinie acid, malic acid, oxalic acid, giyC〇iic acid, diehloroacetic acid, tri-acetic acid (trifluoroacetic acid), tannic acid (tannic acid) group. The mouthwash compositions of the present invention may include, but are not limited to, a Viscosity-increasing agent, a Surfactant, a Stabilizing Agent/

Preservatives) 'flavors, fragrances, sweeteners, bioadehesives and co-solubilizers. For example, cellulose derivatives, (meth)acrylic polymers and copolymers, ethylene glycol or propylene glycol, polyethoxylated hydrogenated castor oil, EDTA, benzoic acid

1295929 P0tassiuin sorbate, dextrin, various fruit flavors, mint flavors, sodiuin saccharin, aspartame, and other ingredients that can be used in mouthwash formulations. The clear water composition of the present invention may further comprise a pharmaceutically active ingredient such as a bactericide, a disinfectant, an antifungal agent, an antiallergic agent, an anti-inflammatory agent and the like. Suitable antimicrobial agents include, but are not limited to, a fourth recorded salt such as benzalkonium chloride. When the clear water composition of the present invention contains the above components other than polybutanose and polyethylene, the components may be directly added to an aqueous solution in which polybutanose and polyvinylpyrrolidone are dissolved, or as an aqueous solution. The organic solution or dispersion is mixed with the aqueous solution in which the polybutanol and the polyethylene 11 are compared to the fluorenone. The invention is further described by the following examples, which are intended to be illustrative only and not to limit the scope of the invention. Example 1 0. 150 g of chitosan (97% deacetylation degree and a molecular weight of 10,000 to 330,000, Kaidesheng Technology Co., Ltd., Taiwan) was suspended in 30 g of pure water, and Add 〇〇75 kg of lactic acid solution (concentration > 8%) and stir until clear and clear. 68.775 grams of water was added and polyvinylpyrrolidone (a total of 1 gram) (K value of 90, Huimin Pharmaceutical Co., Ltd., Taiwan) was added in portions and continuously stirred into a clear mouthwash composition (0.1 weight). Chitosan). The mouthwash composition was measured by a viscosity meter (DV-II + Viscometer, Brookfield ENG LABS, INC. USA) to have a viscosity of 8.64 centipoise at 25 ° C; 1295929 and a pH of 6.8. Comparative Example 1

A lactic acid solution (concentration > 80%) of 〇·75 gram was added and mixed with 999.25 g of water. Take 100 grams of the 0.075% lactic acid aqueous solution prepared above and add the chitosan in batches (the degree of deacetylation is 97% and the molecular weight is between 10,000 and 330,000, Kaidesheng Technology Co., Ltd., Taiwan) And adding the mixture 'continuously adding chitosan until a precipitate is produced, filtering and centrifuging the mixture' to obtain a chitosan saturated 0.075% aqueous lactic acid solution. The viscosity at 25 ° C was determined to be 8.79 cps by a viscosity meter (DV-II + Viscometer, Brookfield ENG LABS, INC. USA); and its pH was 5.9. Adhesion test: Since the viscosity of the solution is positively correlated with the adhesion of the solution, the change in viscosity is used as the adhesion property of the composition. a·Test method: It is known that the mouthwash composition of Example 1 and Comparative Example 1 has a similar viscosity, and the concentration of chitosan in Example 1 is kept constant but the concentration of polyethylene is changed compared with the concentration of anthrone. Viscometer (DV-II +

Viscometer ‘ Brookfield ENG LABS, INC· USA) measured its viscosity change at 25 °C. b. Results: The viscosity change of the mouthwash composition prepared with the same chitosan concentration but different polyvinylpyrrolidone is shown in Fig. 1. It can be seen from the viscosity change of Fig. 1 that the composition of the present invention can be concentrated by different polyvinylpyrrolidone at the same concentration of chitosan solution. 1295929

Table 1 Bitter sensation \\^ article code 11 person control example 1 Example 1 Comparative Example 1 Example 1 5 1 5 1 5 3 5 3 5 3 5 1 5 3 5 3 5 4 5 1 5 2 5 2 5 4 4 2 5 3 5 1 5 4 5 1 5 1 5 1 4 3 4 1 After statistical analysis of the above data (α =0·05, 95% confidence), Comparative Example 1 and Example 1 were obtained. There was a significant difference between the sense of sensation and the sensation of sensation. The mouthfeel of Comparative Example 1 was more wet than the bitter temperature of the chitosan solution in the same viscosity as the chitosan solution of the carbamazepine. It can be known from the above test that the present invention has better adhesion and oral protection effect than the general mouthwash of chitosan at the same concentration of chitosan, and has the same viscosity, that is, adhesion. Better mouthfeel. 13 1295929 BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 shows the relationship between viscosity (CP) and polyvinylpyrrolidone (PVP) concentration (% by weight) of the mouthwash composition of the present invention having the same chitosan concentration.

Claims (1)

1205929 Japanese repair (more) original notice (revised in July 2007) Patent application scope: 1 · A mouthwash composition, basically consisting of water and water soluble in addition to preservatives, flavoring agents, flavorings and sweeteners The following active ingredients are composed of: polyvinylpyrrolidone having a K value of 30-100; and protonated chitosan, wherein the protonated chitosan has a deacetylation degree of 60-99% and a molecular weight between 1 〇, 〇〇〇 to 1, 〇〇〇, 〇〇〇; Wherein the weight ratio of protonated chitosan to polyethylene u pyrrolidone is between 1 and 100 to 100:100, and the mouthwash composition has a viscosity of 0 to 100 centipoise at room temperature. 2. A mouthwash composition as claimed in claim 1, wherein the weight ratio is between 2.5:100 and 30:100. 3. The mouthwash composition of claim 1, which has 0.01 to 1% by weight of chitosan. 4. The mouthwash composition of any one of claims 1 to 3 wherein the mouthwash composition has a viscosity of _ 5_5 () centipoise at room temperature. 15