JP2000256152A - Oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an oral composition capable of preventing the discoloration of ascorbic acid or a derivative thereof with time. SOLUTION: This oral composition is obtained by formulating an oil and fat or an oil-soluble antioxidant dissolved in the oil and fat with an oral composition containing ascorbic acid or a derivative thereof. A sesame oil, an olive oil, a soybean oil, a corn oil, a safflower oil, a cotton seed oil, a grape seed oil, a peanut oil, a macadamia nut oil, a palm oil, a lard, a horse oil, a whale oil and the like are usable as the oil and fat used in the composition. The oil and fat can be used singly or in combination of two or more kinds, and the amount to be formulated is preferably 0.05-15%, especially 0.5-5% based on the whole composition.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition containing ascorbic acid or a derivative thereof, and more particularly, to an oral composition in which discoloration of ascorbic acid or a derivative thereof over time is prevented.

[0002]

2. Description of the Related Art It has been known that ascorbic acid or a derivative thereof is blended as an active ingredient in oral compositions such as dentifrices.
An oral composition containing ascorbic acid or a derivative thereof has a problem that discoloration easily occurs over time. For this reason, various proposals have been made for a method of suppressing discoloration, but the discoloration suppression effect has a limit,
Further measures were desired. The preparation containing ascorbic acid or a derivative thereof as described above causes discoloration over time and causes a practical problem such as turning a white preparation into brown.However, the strength of the discoloration is ascorbic acid or its derivative. The degree of decrease in the residual ratio of the derivative does not always coincide with the degree, and the cause is not clear.

[0003]

Means for Solving the Problems and Embodiments of the Invention The present inventors have conducted intensive studies on a method for preventing discoloration of an oral composition containing ascorbic acid or a derivative thereof with the passage of time. It is found that the compounding is effective in preventing discoloration, and furthermore, the discoloration preventing effect is further improved when an oil-soluble antioxidant is dissolved in this oil or fat and added to an oral composition containing ascorbic acid or a derivative thereof. Thus, the present invention has been accomplished.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains ascorbic acid or a derivative thereof. In this case, as the ascorbic acid derivative,
1 or 2 of the 2,3,5,6-positioned hydroxyl group of ascorbic acid
Above can be esters of phosphoric acid, polyphosphoric acid, sulfuric acid, fatty acids, and other pharmaceutically acceptable compounds. For example, ascorbic acid-2-phosphate,
Ascorbic acid-3-phosphate, ascorbic acid-6-phosphate, ascorbic acid-2-polyphosphate, ascorbic acid-2-sulfate, ascorbic acid-2-palmitate, ascorbic acid-6-palmitin Acid ester, ascorbic acid-2-
Stearic acid ester, ascorbic acid-6-stearic acid ester, ascorbic acid-2,6-dibutyl ester, ascorbic acid-2,6-dipalmitic acid ester and the like can be mentioned. Examples of the salts include sodium salts, potassium salts, calcium salts, magnesium salts and the like.

[0005] These ascorbic acids or derivatives thereof are
One type may be used alone or two or more types may be used in combination.
Alternatively, a derivative in which the hydroxyl group at the 3-position is esterified is preferably used.

[0006] The amount of ascorbic acid or a derivative thereof in the oral composition of the present invention is 0.000% of the total composition.
1 to 5% (% by weight, the same applies hereinafter), particularly 0.01 to 3%
Is desirable.

In the present invention, fats and oils are blended in order to prevent discoloration of the oral composition due to the above ascorbic acid or a derivative thereof over time.

The fats and oils used in the present invention include:
Sesame oil, olive oil, soybean oil, corn oil, safflower oil, cottonseed oil, grape seed oil, peanut oil, macadamia nut oil, palm oil, lard, horse oil, whale oil, etc. can be used. It can be added by dissolving warm.

These fats and oils may be used alone or in combination of two or more. The amount of the fat or oil is 0.05 to 15% of the total composition, particularly 0.5 to 5%. %. If the amount is too small, the effect is not sufficiently exhibited, and if the amount is too large, a problem in usability may occur.

It is preferable that the oral composition of the present invention further contain an oil-soluble antioxidant in addition to the fat or oil. However, it is recommended that the oil-soluble antioxidant be dissolved in the fat or oil and blended. You. In this case, as the oil-soluble antioxidant, retinol or a derivative thereof, tocopherol or a derivative thereof, carotene, dibutylhydroxytoluene, guaiac, nordihydroguaiaretic acid (NDG)
A), butylhydroxyanisole (BHA), dibutylhydroxytoluene (BHT), propyl gallate and the like, and one or more of these can be used in combination.

The amount of the oil-soluble antioxidant to be added is appropriately selected, but is preferably 0.001 to 5% of the total composition, particularly 0.03%.
Preferably it is 1 to 3%.

The oral composition of the present invention can be made into various dosage forms such as dentifrice such as toothpaste, gum massage cream, topical application, mouthwash, troche, chewing gum and the like. In this case, in addition to the above-mentioned components, various base components used in ordinary oral compositions can be blended with the oral composition of the present invention. For example, in the case of a dentifrice, an abrasive, a binder, a thickener, a sweetener, a flavor, and the like can be blended in a usual amount.

For example, abrasives include calcium hydrogen phosphate dihydrate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, silicic anhydride, aluminum silicate, insoluble sodium metaphosphate, tertiary phosphorus Magnesium acid, magnesium carbonate,
Calcium sulfate, bentonite, zirconium silicate,
One or more of polymethyl methacrylate, other synthetic resins, and the like may be blended within a range that does not impair the effects of the present invention.

Examples of the binder include cellulose derivatives such as carrageenan, sodium carboxymethylcellulose, methylcellulose and hydroxyethylcellulose; alginic acid derivatives such as sodium alginate and propylene glycol alginate; gums such as xanthan gum, gellan gum, tragacanth gum, and karaya gum; One or more kinds of synthetic binders such as alcohol, sodium polyacrylate and carboxyvinyl polymer, and inorganic binders such as silica gel, veegum and laponite may be blended.

As the humectant, one or more polyhydric alcohols such as glycerin, sorbitol, propylene glycol, polyethylene glycol, xylitol, maltitol and lactitol can be blended.

As the surfactant, an anionic surfactant such as sodium lauryl sulfate, a nonionic surfactant such as decaglyceryl laurate and diethanolamide myristate, and an amphoteric surfactant such as betaine can be blended. .

As the fragrance component, menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, cineol, linalool, ethyl linalool, crocodile, thymol, peppermint oil, spearmint oil, wintergreen oil, T-shaped oil, fragrances such as eucalyptus oil can be blended alone or in combination, saccharin sodium,
Sweetening agents such as stevioside, glycyrrhizin, perillartin, thaumatin and the like can be added.

Further, in the present invention, cationic fungicides such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, decanium chloride, phenolic compounds such as triclosan, hinokitiol and biosol, dextranase, mutanase, lysozyme, amylase, protease, lytic enzymes, enzymes such as superoxide dismutase, vitamin E, vitamins such as vitamin B _6, sodium monofluorophosphate, alkali metal monofluorophosphate salts such as potassium monofluorophosphate, Sodium fluoride, fluorides such as stannous fluoride, tranexamic acid, epsilon aminocaproic acid,
One or more known active ingredients such as aluminum chlorohydroxyl allantoin, dihydrocholestanol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, sodium chloride, and a water-soluble inorganic phosphate compound can be blended.

The composition of the present invention can be used by filling it into a container usually used for an oral composition. Specifically, such a container comprises a polyethylene layer, an ethylene methacrylic acid copolymer layer, a polyethylene terephthalate layer, an aluminum layer, a glass deposition layer, a polyvinyl alcohol layer, an ethylene vinyl alcohol copolymer layer, a recycled plastic layer, and the like. A laminate container, a polyethylene container, a polyethylene terephthalate container, a polypropylene container and the like can be mentioned.

[0020]

The oral composition containing ascorbic acid or a derivative thereof according to the present invention is one in which discoloration over time is prevented.

[0021]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to experimental examples and examples, but the present invention is not limited to the following examples. In the following examples,% indicates% by weight.

[Experimental Example] A dentifrice was prepared by mixing the following fats and oils and an oil-soluble antioxidant with the following dentifrice base (blank preparation). These dentifrices were stored in a thermostat at 60 ° C., and the discoloration of the preparations after one month was visually determined. As a control, a product stored at −5 ° C. having the same composition was used as an undiscolored product. Table 1 shows the results. Dentifrice base Propylene glycol 3% Carboxymethyl cellulose 2% Paraben 0.08% Ascorbic acid phosphate magnesium salt 0.1% Sodium saccharin 0.2% Sorbit 30% Silicic anhydride 15% Fragrance 1% Sodium lauryl sulfate 1.2 % Purified water Residual oil Olive oil 2% Safflower oil 2% Oil-soluble antioxidant β-carotene 0.005% Tocopherol acetate 0.01%

[0023]

[Table 1] Discoloration judging criteria- : No discoloration is observed ±: Discoloration is noticeable compared to control +: Discoloration is apparent at a glance ++: Discoloration is strong

From the above results, it can be seen that the discoloration of the dentifrice due to ascorbic acid can be effectively suppressed by blending the fats and oils, and in particular, an excellent discoloration preventing effect is obtained by dissolving and blending the oil-soluble antioxidant in fats and oils. It is recognized that.

Next, examples will be shown. In the following examples, all oil-soluble antioxidants were dissolved in fats and oils and blended.

Example 1 Toothpaste Propylene glycol 5% Sorbit 40 Carrageenan 1.2 Saccharin sodium 0.2 Sodium lauryl sulfate 1.2 Ethyl parahydroxybenzoate 0.1 Ascorbic acid-2-phosphate magnesium salt 0.2 Olive oil 2 Sodium hydroxide 0.05 Silicic anhydride 15 Fragrance 0.9 Purified water Balance 100%

Example 2 Toothpaste Polyethylene glycol 400 5% Glycerin 20 Xanthan gum 1.1 Xylit 10 Sodium lauryl sulfate 0.9 Myristic acid diethanolamide 0.6 Palmitic acid 0.5 Cottonseed oil 1 Ascorbic acid phosphate sodium salt 0.1 Ethyl parahydroxybenzoate 0.1 Aluminum hydroxide 40 Fragrance 1.2 Purified water Balance 100%

Example 3 Toothpaste Propylene glycol 4% Sorbite 40 Carboxymethylcellulose 2 Saccharin sodium 0.15 Sodium lauryl sulfate 1 Lauroyl sarcosine sodium 0.2 Sodium benzoate 0.8 Sodium hydroxide 0.05 Tranexamic acid 0.1 Ascorbic acid fatty acid ester 0.05 Grape seed oil 4 β-carotene 0.02 Sodium myristate 0.2 Titanium-binding silica 20 Fragrance 1 Purified water Balance 100%

Example 4 Toothpaste Propylene glycol 5% Sorbite 35 Sodium alginate 3 Sodium saccharin 0.15 Sodium lauryl sulfate 1 Butyl paraoxybenzoate 0.5 Sodium hydroxide 0.05 Triclosan 0.1 Ascorbic acid-3-phosphate Acid ester 0.05 Tocopherol acetate 0.01 Olive oil 0.5 β-carotene 0.005 Sodium myristate 0.2 Silicic anhydride 20 Fragrance 1 Purified water Balance 100%

Example 5 Toothpaste Sodium polyacrylate 0.5% Xanthan gum 0.5 Propylene glycol 5 70% sorbite solution 20 Saccharin sodium 0.1 Sodium benzoate 0.3 Sodium lauryl sulfate 1.5 Tranexamic acid 0. Reference Signs List 1 ascorbic acid-2-phosphate sodium salt 0.5 dl-α-tocopherol 0.2 horse oil 1 oak extract 0.05 sodium fluoride 0.2 silicic anhydride 20 fragrance 1 purified water balance 100%

Example 6 Liquid Dentifrice Silicic Anhydride 10% Xanthan Gum 1 Saccharin Sodium 0.1 60% Sorbit Solution 40 Glycerin 20 Propylene Glycol 3 Sodium Lauryl Sulfate 1.2 Sodium Bicarbonate 2 Decaglyceryl Laurate 0.5 Fluoride Sodium chloride 0.2 Triclosan 0.1 Ascorbic acid-2-phosphate magnesium salt 1.5 Corn oil 4 Retinol 0.01 Flavor 0.8 Blue No. 1 0.001 Purified water Balance 100%

Example 7 Oral Pasta Cetanol 20% Squalane 5 Polyoxyethylene (40) Hydrogenated Castor Oil 0.1 Sorbitan Monooleate 1 Sodium Lauryl Sulfate 0.2 Glycyrrhetinic Acid 0.1 Saccharin Sodium 0.6 Ascorbin Acid phosphate 0.3 Palm oil 1 β-carotene 0.002 Calcium hydrogen phosphate 5 Fragrance 0.3 Purified water Balance 100%

Example 8 Mouthwash Ethanol 5% Sorbit 10 Sucrose monopalmitate 0.2 Polyoxyethylene (60) hydrogenated castor oil 0.1 Methyl parahydroxybenzoate 0.01 Saccharin sodium 0.7 Tranexamic acid 0 .5 Cetylpyridinium chloride 0.2 Ascorbic acid-2-sulfate sodium salt 0.2 Macadamia nut oil 2 Isopropyl citrate 0.1 Sodium monofluorophosphate 0.7 Oubaku extract 0.1 Perfume 1 Purified water Balance 100%

Example 9 Mouthwash Ethanol 10% Glycerin 10 Polyoxyethylene (60) hydrogenated castor oil 5 Saccharin sodium 0.7 Tranexamic acid 0.15 Ascorbic acid-2-phosphate magnesium salt 1 Olive oil 0.5 Acetic acid Tocopherol 0.1 Perfume 1 Purified water Balance 100%

Example 10 Chewing gum gum base 25% xylitol 10 sugar 15 isomaltose 20 corn syrup 16 starch syrup residual ascorbic acid fatty acid ester 0.2 lard 1 propyl gallate 0.05 palmitic acid 0.2 fragrance 0.6 total 100 %

 ──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Yuko Aratani 1-3-7, Honjo, Sumida-ku, Tokyo F-term in Lion Corporation (reference) 4B014 GB13 GG14 GK11 GL03 4C076 AA07 BB22 CC16 DD26Z DD38 DD41 DD45Q DD46 DD59A DD59Q DD61T DD63A DD69 EE03Q EE53Q EE54Q FF65 4C083 AA081 AA082 AA121 AA122 AB032 AB172 AB222 AB282 AB312 AB372 AB472 AC022 AC072 AC102 AC122 AC132 AC242 AC312 AC351 AC352 AC422 AC432 AC442 AC482 AC552 AC642 AC482 AC552 AC2 482 AD352 AD532 AD622 AD641 AD642 AD662 BB47 CC41 DD12 DD22 DD23 DD27 EE01 4C086 AA01 BA09 BA18 DA37 MA02 MA03 MA05 MA07 MA09 NA03 ZA67

Claims (2)

[Claims] 1. An oral composition comprising an oral composition containing ascorbic acid or a derivative thereof and an oil or fat. 2. The oral composition according to claim 1, wherein the oil-soluble antioxidant is dissolved in fats and oils and blended.