JPH07187975A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity, having excellent retention of triclosan in the oval cavity, exhibiting highly bactericidal effect, having excellent preparation stability, capable of being pharmaceutically manufactured into various preparations and widely used. CONSTITUTION:This composition for oral cavity is obtained by mixing a composition for oral cavity containing triclosan with sodium alginate and xanthan gum.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition having an excellent oral retention of triclosan and having good formulation stability.

[0002]

2. Description of the Related Art Conventionally, the problems to be solved by the invention
Mixing triclosan in an oral composition is disclosed in Japanese Patent Laid-Open Publication No.
No. 0-239409, etc., and pectin, HPC (hydroxypropyl cellulose), cyclodextrin, chitin, chitin derivatives, chitosan, chitosan derivatives, alginic acid, and alginic acid for increasing the retention of triclosan in the oral cavity. It is possible to blend a compound selected from its salts and esters.
It is proposed in Japanese Patent No. 9118.

However, there is still room for studying the retention of triclosan in the oral cavity, and the development of a high-quality oral composition in which the retention of triclosan in the oral cavity is further enhanced is desired.

The present invention has been made in order to meet the above-mentioned demand, and is superior in the retention of triclosan in the oral cavity.
It is an object of the present invention to provide an oral composition having a good formulation stability.

[0005]

Means and Actions for Solving the Problems As a result of intensive studies for achieving the above object, the present inventor has found that an oral composition containing triclosan is used in combination with sodium alginate and xanthan gum. Surprisingly, it was found that the retention of triclosan in the oral cavity was significantly improved and the formulation was stabilized.

In this case, sodium alginate, xanthan gum, HPC, hydroxyethyl cellulose (HEC), carrageenan, carboxymethyl cellulose and the like are usually blended as a binder in the oral composition, but alginic acid is contained in the oral composition containing triclosan. When sodium and xanthan gum are selectively combined and used, as is clear from the results of Experimental Example 1 described later, the adsorption / retention property of triclosan on the teeth is higher than that when the binder is alone added. Is particularly improved, and the retention in the oral cavity is extremely high. Moreover, such a formulation has good shape retention and spinnability and excellent formulation stability without liquid separation. The inventors have found that the obtained oral composition can be obtained, and completed the present invention.

Accordingly, the present invention provides an oral composition comprising a triclosan-containing oral composition in which sodium alginate and xanthan gum are used in combination.

The present invention will be described in more detail below. The oral composition of the present invention can be prepared as toothpaste such as toothpaste, liquid toothpaste, troche, chewing gum and the like, and contains triclosan as an active ingredient. In addition, sodium alginate and xanthan gum are used in combination.

The content of triclosan is 0.01 to 0.5%, especially 0.02 to 0.3% of the total composition.
Is preferred.

Further, it is preferable that sodium alginate and xanthan gum are mixed in a weight ratio of sodium alginate: xanthan gum of 1: 9 to 9: 1, particularly 3: 7 to 7: 3. If the compounding ratio is out of the above range, triclosan may be inferior in oral retention and formulation stability, and especially when the amount of xanthan gum is large and the above ratio is more than 1: 9, the spinnability is lowered and liquid separation occurs. If the amount of sodium alginate is large and the ratio is more than 9: 1, the moldability may be deteriorated. The total content of sodium alginate and xanthan gum is 0.1 to 2% of the total composition, and especially 0.1.
It is preferably set to 2 to 1%.

The oral composition of the present invention may contain other additives as optional components in addition to the above-mentioned essential components depending on the dosage form. In the case of toothpaste, for example, an abrasive, a thickener, a binder other than sodium alginate and xanthan gum, a surfactant, a sweetener, a preservative, a coloring agent, various active ingredients other than the above triclosan, and the like can be added. Here, as the polishing agent, silica-based polishing agents such as precipitated silica, silica gel, aluminosilicate, and zirconosilicate, dicalcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, Magnesium carbonate, tribasic magnesium phosphate, zeolite, zirconium silicate, synthetic resin-based abrasives and the like are preferably used.

As the thickener, glycerin, sorbit, propylene glycol, polyethylene glycol,
Xylit, maltite, lactit, etc., as binders, sodium carboxymethyl cellulose, hydroxyethyl cellulose, carrageenan, carbopol, guar gum, montmorillonite, gelatin, etc.As surfactants, anionic surfactants, cationic surfactants, nonionics A surfactant may be added, and specifically, sodium lauryl sulfate, sodium α-olefinsulfonate, N-acyl sarcosinate, N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethyl. Imidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, pluronic, polyoxyethylene sorbitan monosteare DOO, etc., as the sweetener, sodium saccharin, stevioside, stevia extract, para-methoxy cinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine, etc., as the preservative,
Paraoxybenzoic acid ester, sodium benzoate, etc.
Various active ingredients include fluorides such as sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride and sodium monofluorophosphate, and water-soluble phosphate compounds such as potassium orthophosphoric acid salts and sodium salts. , Allantoin chlorhydroxy aluminum, hinokitiol,
Ascorbic acid, lysozyme chloride, glycyrrhizic acid and its salts, sodium chloride, tranexamic acid, epsilon aminocaproic acid, dl-tocopherol acetate, α
-Bisabolol, isopropylmethylphenol, chlorohexidine salts, cetylpyridinium chloride, azulene, glycyrrhetinic acid, copper chlorophyllin sodium,
Copper compounds such as copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, dextranase, mutanase, amylase,
Such as methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterin, benzethonium chloride, dihydrocholesterol, trichlorocarbanilide, zinc citrate, soft extract of Japanese persimmon extract, cabbage extract, clove, rosemary, sardine, safflower, etc. Examples of fragrances such as extracts include terpenes such as 1-menthol, carvone, anethole, and limonene, or derivatives thereof, and examples of colorants include Blue No. 1, Yellow No. 4, and titanium dioxide. In addition, the compounding amounts of these components can be set to normal amounts as long as the effects of the present invention are not impaired.

[0013]

INDUSTRIAL APPLICABILITY The composition for oral cavity of the present invention has excellent retention of triclosan in the oral cavity and can exhibit a high bactericidal effect.
It also has good formulation stability and can be widely used by preparing it in various formulations.

[0014]

EXAMPLES The present invention will be specifically described below by showing experimental examples and examples, but the present invention is not limited to the following examples. In addition,% in each example is% by weight.

[Experimental Example 1] The following experiment was conducted as a model experiment for investigating the adsorption and retention of triclosan on the teeth.

Hydroxyapatite (HAp) 10m
After washing g with a phosphate buffer (PBS), it was immersed in human saliva for 1 hour. The saliva-coated HAp was washed with PBS and then stirred with 100 ml of the following composition liquid for 30 minutes.
After treatment, triclosan is extracted with ethanol and HPLC
(High performance liquid chromatography) was used to quantify the residual amount of triclosan (TC). The results are shown in Table 1. Test liquid composition: propylene glycol 4.0% sorbit 20.0 sodium lauryl sulfate 1.5 triclosan 0.1 compound shown in Table 1 0.5 water balance 100.0% From the results in Table 1, xanthan gum and alginic acid were added to triclosan. It was found that the combined use of sodium with xanthan gum and sodium alginate significantly increases the adsorption and retention properties of triclosan on HAp as compared with the case of individually compounding other compounds and other compounds. did.

[0017]

[Table 1]

[Experimental Example 2] As shown in Table 2, toothpaste having the following composition was prepared by changing the compounding ratio of xanthan gum and sodium alginate. The shape retention, spinnability and liquid separation of this toothpaste were evaluated by the following methods. The results are also shown in Table 2. Toothpaste composition: aluminum hydroxide 45% sorbit 30 xanthan gum + sodium alginate 1.0 in total in the proportions shown in Table 1.0 sodium lauryl sulphate 1.2 fragrance 1.3 myristic acid diethanolamide 2 triclosan 0.1 water balance 100.0% Evaluation method: The sample was filled in a laminate tube, and 5
After storing at 0 ° C. for 1 month, it was left at room temperature for 1 day. Then, the following items were evaluated. Shape retention When toothpaste is pushed onto the toothbrush ○: Stable on the toothbrush and does not lose its shape △: It loses its shape on the toothbrush or rolls more easily than the toothbrush ×: Runs down or falls off the toothbrush Spinnable toothpaste When extruded onto a toothbrush ○: No stringing and good kneading △: Some stringing is seen ×: Significant stringing and poor kneading Liquid separation When toothpaste is extruded onto paper ○ : Liquid separation is not observed at all Δ: Liquid separation is slightly observed at the mouth ×: Liquid separation is observed From the results of Table 2, the composition for oral cavity containing the three components of triclosan, xanthan gum, and sodium alginate is:
It was found to be pharmaceutically stable.

[0019]

[Table 2]

[Example 1] Toothpaste Aluminum hydroxide 45% Solbit 30 Propylene glycol 5 Xanthan gum 0.8 Sodium alginate 0.6 Sodium lauryl sulfate 0.8 Lauroyl sarcosinate 0.4 Perfume 1.3 Saccharin sodium 0.1 Lauroyldiethanolamide 1.6 Gelatin 0.2 Dextranase 2000 U / g Toothpaste Triclosan 0.02 Sodium monofluorophosphate 0.73 Butylparaben 0.01 Ethylparaben 0.02 Water Residual 100.0%

Example 2 Toothpaste Calcium phosphate 55% Solbit 23 Propylene glycol 2 Xanthan gum 0.3 Sodium alginate 0.6 Silica anhydride 3 Sodium lauryl sulfate 1.5 Perfume 0.7 Sodium saccharin 0.2 Triclosan 0.1 Benzoate Sodium acid 0.3 Methylparaben 0.2 Water Residual 100.0%

[Example 3] Toothpaste Silica 20% Solbit 35 Polyethylene glycol # 400 3 Sodium carboxymethyl cellulose 1 Xanthan gum 0.1 Sodium alginate 0.05 Hydroxyethyl cellulose 0.1 Silica anhydride 1 Sodium lauryl sulfate 1 Perfume 0.7 Saccharin sodium 0.1 Lauroyldiethanolamide 0.3 Triclosan 0.05 Sodium monofluorophosphate 0.73 Sodium sulfate 0.5 Water Residual 100.0%

[Example 4] Toothpaste Modified aluminum hydroxide 45% Glycerin 20 Polyethylene glycol # 400 2 Xanthan gum 0.1 Sodium alginate 0.05 Hydroxypropyl cellulose 0.1 Anhydrous silicic acid 2 Sodium lauryl sulfate 0.5 Lauroyl Sarcosinate 0.2 Perfume 0.75 Saccharin sodium 0.02 Triclosan 0.02 Dipotassium glycyrrhizinate 0.05 Tranexamic acid 0.05 Water Residual 100.0%

[Example 5] Toothpaste Calcium carbonate 40% Solbit 40 Propylene glycol 3 Xanthan gum 0.1 Sodium alginate 0.3 Carrageenan 0.2 Silicic anhydride 2 Lauroyl sarcosinate 0.5 Perfume 0.8 Saccharin sodium 0. 1 Lauroyl diethanol amide 1.5 Gelatin 0.2 Triclosan 0.5 Water Residual 100.0%

[Example 6] Liquid dentifrice Silica 9% Solbit 50 Glycerin 20 Propylene glycol 3 Xanthan gum 0.15 Sodium alginate 0.2 Perfume 1.1 Saccharin sodium 0.1 Lauroyl diethanolamide 0.5 Polyglycerin fatty acid ester 0.5 Alanine 0.5 Triclosan 0.1 Sodium fluoride 0.21 Water Residual 100.0%

[Example 7] troche gum arabic 6% xanthan gum 0.3 sodium alginate 0.1 fragrance 1 glucose 36 palatinose 36 triclosan 0.01 water balance 100.0%

[Example 8] Chewing gum Calcium carbonate 2% Gum base 20 Xanthan gum 0.1 Sodium alginate 0.1 Flavor 1 Syringe 15 Powdered sugar 58 Triclosan 0.01 Water Residual total 100.0%

[Procedure amendment]

[Submission date] March 16, 1994

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[0025]

Claims (1)

[Claims] 1. An oral composition comprising an oral composition containing triclosan and sodium alginate and xanthan gum in combination.