JPS6136210A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To obtain the titled composition having excellent storage stability, especially hydrolysis resistance in the high-temperature storage of a tocopherol (derivative), by adding a nonionic surfactant to a composition containing tocopherol or its ester derivative and an anionic surfactant. CONSTITUTION:A nonionic surfactant is added in an amount of 0.1-5(wt)% to a composition composed of (A) 0.01-5%, especially 0.05-2% tocopherol or its ester derivative effective as a preventive or remedy for periodontosis by its pharmacological activity such as the blood flow promoting effect, etc. and (B) 0.1-5%, especially 0.3-3% anionic surfactant (especially a 8-18C alkylsulfuric acid ester) used as a frothing agent to improve the feeling to the oral cavity. The nonionic surfactant is preferably a fatty acid alkonolamide (e.g. lauric acid diethanolamide) having 8-18C fatty acid group and 2-3C alkanol group. The weight ratio of the nonionic surfactant to the anionic surfactant is preferably 1:5-5:1.

Description

[Detailed Description of the Invention] The present invention provides tocopherol (vitamin E) 5? 1: This invention relates to an oral composition such as a toothpaste containing an ester derivative thereof, and more specifically, to an oral composition having excellent storage stability of tocopherol or a derivative thereof.

Conventionally, it has been proposed to incorporate tocopherol (vitamin E) or ester derivatives such as tocopherol acetate into oral compositions such as toothpaste, and to prevent and treat periodontal diseases through its pharmacological effects such as blood circulation promoting effects. ing.

However, according to studies conducted by the present inventors, oral compositions using an anionic active agent as a foaming agent, especially oral compositions using alkyl sulfate salts such as sodium lauryl sulfate, sodium lauroyl sarcosine, etc., contain tocopherol. When tocopherol or its ester derivative is blended, the tocopherol or its ester derivative tends to be hydrolyzed, resulting in a decrease in its storage stability. In particular, this tendency is remarkable when oral compositions are stored at high temperatures, and there is a problem in that the residual rate of tocopherols becomes extremely low after long-term storage at high temperatures.

In this case, tocopherols are relatively stable if no anionic active agent is blended, but it may be necessary to incorporate an anionic active agent from the viewpoint of the usability of the oral composition, especially foaming. Therefore, it is desirable to stably incorporate tocopherol or its ester derivatives into oral compositions such as toothpastes containing anionic activators.

Features of the Invention In view of the above circumstances, the present inventors have developed a method to prevent tocopherol or its ester derivative from being hydrolyzed when tocopherol or its ester derivative is blended into an oral composition containing an anionic activator, and to As a result of various studies to improve storage stability, we incorporated a nonionic active agent, particularly a fatty acid alkanolamide such as lauric acid jetanolamide, into an oral composition containing an anionic active agent and tocopherol or its ester derivative. In this case, the present inventors have surprisingly found that the hydrolysis of tocopherols, especially during high-temperature storage, is effectively suppressed, and the above object is effectively achieved, leading to the present invention.

The present invention will be explained in more detail below.

Structure of the Invention The oral composition according to the present invention is formed by blending a nonionic active agent into an oral composition containing tocopherol or an ester derivative thereof and an anionic active agent, and is suitable for use in toothpastes and moisturized toothpastes. It is used as dentifrice such as liquid toothpaste, mouthwash, etc.

The type of anionic activator used in the present invention is not limited, and for example, one or more of the following may be used.

(1) Fatty acid soaps, sodium laurate, sodium myristate, potassium oleate, sodium stearate, etc. (2) Higher alcohol sulfate salts, sodium lauryl sulfate, sodium octyl sulfate, sodium oleyl sulfate, etc. (3m secondary higher alcohols) Sulfate ester salt Arosl
n-type, Tgrgitol type-Teapal type 1 hegetadecane-2-sulfate, henotadecane-8-sulfate, etc. (4) Sulfate salts (5) Sulfate ester salts of higher fatty acid esters (6)
Sulfuric ester salts of higher fatty acid alkylolamides (7) Nonionic ether sulfuric ester salts (8) Higher alkyl sulfonates (9) Alkylaryl sulfonates Alkylbenzene sulfonates, alkylnaphthalene sulfonates, etc., α1 higher fatty acid amides Alkylated sulfonate 0 and sulfonate of higher fatty acid ester (6)
Diargyl sulfo moss <acid acid (to) higher alkyl phosphate ester Q4 Other In this case, in the present invention, the number of carbon atoms in the alkyl group is 8
Water-soluble salts of higher alkyl sulfate esters ranging from 1 to 18, particularly sodium lauryl sulfate and sodium lauroyl sarcosine, can be effectively used. The amount of the anionic activator to be added is preferably 0.1 to 5% (weight %, same hereinafter), particularly 0.3 to 3%, based on the total composition, and preferably 0.3 to 3%.
If it is less than 1%, the foaming of the composition may become poor, while if it is more than 5%, problems may arise in the stability and safety of the composition.

In addition, tocopherol ester derivative Toshiteha Vinegar 1f
f) Copherol, tocopherol nicotinate, and the like. In the present invention, one kind of tocopherol and its ester derivative can be used alone or in combination of two or more kinds.

The blending amount is 0.01 to 5% of the total composition, especially 0.0
The amount is preferably 5 to 2%; if it is less than 0.01%, sufficient pharmacological effects may not be exhibited, and if it is more than 5%, the flavor of the composition may be adversely affected.

Further, the type of nonionic activator is not particularly limited, and for example, one or more of the following may be used.

(1)/+7 Oxyethylene alkyl ether The number of moles of ethylene oxide added is 10 to 100 and the alkyl group is cetyl, oleoyl, hydroabiethyl, tridecyl alcohol, etc., f2), telJ oxyethylene alkyl phenol ether carbon of the alkyl group (3) / such as those with a number of 10 to 20
'J oxyethylene alkylphenol formalin condensate Triton WR-1339■ etc., (4) polyoxyethylene fatty acid ester fatty acid has 10 or more carbon atoms
20 (e.g. lauric acid, myristic acid, oleic acid) etc. (5), f? Lyoxyethylene alkylamide (6) Fatty acid alkanolamide (7) Polyoxyethylene algylamine (8)
Furkyl mercaptan ether (9) & dioxyethylene lanolin alcohol 00 Higher fatty acid glycerin esters lauroyl monoglyceride, stearyl monoglyceride, etc., alpha higher fatty acid sorbitan esters sorbitan monostearate, sorbitan trilaurate, sorbitan similistate, etc., alpha simisaccharide Fatty acid ester silica mononoe lumitate, silica monostearate,
Sucrose dilaurate, etc. (To) Polyoxyethylene sorbitan fatty acid ester α
◆ Polyoxyethylene glycerol monofatty acid ester 0 Polyoxyethylene zolopylene glycol monofatty acid ester (1 (e / lyoxyethylene sorbitol fatty acid ester aη Prioxyethylene oxyfatty acid triglyceride derivative Polyoxyethylene hydrogenated castor oil derivative etc., 0II
Polyoxyethylene lanolin derivative Lanogel ■
, 5olan■, etc. Block polymer type pluronic, tetronic, those containing alkyl groups, etc. (a) Others In this case, in the present invention, the fatty acid group has 8 to 1 carbon atoms.
8, and a fatty acid alkanolamide in which the alkanol group has 2 or 3 carbon atoms is preferably used. The fatty acid may be saturated or unsaturated, linear or branched, and may be a mixed fatty acid. Specifically, capric acid modiethanolamide, lauric acid jetanolamide, myristic acid jetanolamide, thujarumitic acid jetanolamide, coconut oil fatty acid jetanolamide, beef tallow fatty acid jetanolamide, lauric acid monoisonolamide and nolamide, etc. However, it is particularly preferable to use diuric acid diethanolamide and myristic acid jetanolamide from the viewpoint of improving the stability of tocopherols and the usability and stability of the composition. In addition, the amount of nonionic surfactant added is 0.00% of the total composition.
It is preferable that the amount is 1 to 5%, and if it is less than 0.1%, problems may arise in the storage stability of the toco7 alcohols, and if it is more than 5%, the foaming speed of the composition will be reduced. If it is slow, it may feel uncomfortable to use.

In addition, in the present invention, the anionic activator and the nonionic activator are mixed at a ratio of 10:1 to 1:10. In particular, it is preferable to use them together at a weight ratio of 5:1 to 1:5, thereby further enhancing the storage stability of cytocopherols.

As other components of the present invention, appropriate components commonly used may be blended depending on the type of oral composition, purpose of use, etc.

For example, in the case of toothpaste, dibasic calcium phosphate
Hydrates and anhydrides, monocalcium phosphate, tertiary calcium phosphate, calcium carbonate, calcium pyrophosphate,
titanium oxide, alumina, hydrated alumina, precipitated silica,
One type of other silica-based abrasives, aluminum silicate, insoluble sodium metaphosphate, insoluble potassium metaphosphate, tertiary magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, synthetic resin, etc. or 2s or more (compounding amount usually 10% to 99%, in the case of toothpaste 1
0eI6-75ch).

In addition, in the case of one-shot oral compositions such as toothpaste, caradanan, caladan, etc. are used as binders. Sodium oxymethylcellulose, methylcellulose, hydroxyethylcellulose, sodium hydroxymethylcellulose, natonocellulose derivatives, alkali metal alginates such as sodium alginate, nolopylene glycol alginate, gums such as xanthan gum, tragacanthum, karaya gum, gum arabic, polyvinyl alcohol, sodium polyacrylate,
Cal? Xyvinyl? 1. Synthetic binders such as remer, polyvinyl♂rolidone, inorganic binders such as silica silica, aluminum silica silica, peame, laponite, etc.
species or two or more species may be blended (compounding amount usually 0.5 to 5
blood).

Furthermore, in the production of dentifrices and other oral compositions,
As a thickening agent, one or more of sorbitol, glycerin, ethylene glycol, propylene glycol, 1,3-ethylene glycol, polyethylene glycol, polypropylene glycol, kinlit, marnat, lafutit, etc. may be blended (the amount usually ranges from 10 to 70chi).

In this case, in the present invention, primary amine salt, quaternary
There is no problem in blending one or more surfactants other than cationic surfactants such as amine salts, anionic surfactants such as amphoteric surfactants such as betaine type and amino acid type, and nonionic surfactants.

In addition, sweeteners (0 to 1%, preferably 0.01 to 0.51), and further optionally p-hydroxymethylbenzoic acid, p-hydroxyethylbenzoic acid, p-hydroxybutylbenzoic acid, p-hydroxybutylbenzoic acid, benzoic acid Preservatives such as acid sodium, lower fatty acid monoglycerides, fragrances such as wintergreen oil, spearmint oil, peppermint oil, satsafras oil, clove oil, and eucalyptus oil, whitening agents such as gelatin, peptone, arginine hydrochloride, aldimine, and casei Y1. , silicones, pigments, fungicides, and other ingredients. Furthermore, in addition to tocopherols, active ingredients include allantoin, epsilonamitsukazolonic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, lytic enzyme, sodium monofluorophosphate, monofluorophosphate, etc. Alkali metal monofluorophosphates such as potassium phosphate, fluoride chlorhexinone salts such as sodium fluoride, ammonium fluoride, and stannous fluoride;
One or more of dihydrocholesterol, glycyrrhetinic salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, caro(sitide, water-soluble inorganic phosphoric acid compounds, other vitamins, tartar inhibitors, plaque inhibitors, etc.) may be blended.

Effects of the Invention As explained above, the oral composition according to the present invention is obtained by blending a nonionic active agent into an oral composition containing tocopherol or its ester derivative and an anionic active agent. Tocopherol or its ester derivative has high storage stability, and even when stored at high temperatures, the hydrolysis of the tocopherols is well suppressed, and the pharmacological effects of tocopherols are fully and effectively exhibited. [Experimental Example] For a toothpaste with the following composition containing sodium lauryl sulfate and sodium lauroyl sarcosine as anionic activators and tocopherol acetate, laurin as a nonionic activator was added. Sample toothpastes containing acid jetanolamide at 0.34%, 0.5% or 1.0% of the total composition are prepared and filled into tubes. next,
The residual rate of tocopherol acetate was measured after these toothpastes were stored in a constant temperature room at 50° C. for one month. Furthermore, for comparison purposes, a similar experiment was conducted using a toothpaste that did not contain lauric acid jetanolamide. Results first
Shown in the table. Incidentally, the residual rate of tocopherol acetate was measured by the following method.

Toothpaste composition Dicalcium phosphate dihydrate 45 Silicic anhydride 2.0 Norobile/Dalicol 2.5 Sorbit
25 Cal? Sodium oxymethylcellulose 0.5 cara rnan
0.5 sodium lauryl sulfate
0.7 Sodium lauroyl sarcosine
0.3 Lauric acid diethanolamide Amount shown in Table 1 Tocopherol acetate 01 Fragrance
1.0 Saccharin Sodium 01 Total
100.0 sample toothpaste 2. O? was dispersed in 1001 nl of methanol and centrifuged for 10 minutes at 11,000 Orp. Ten volumes of the supernatant were collected and subjected to liquid chromatography to determine the amount of tocopherol acetate in the supernatant to calculate the residual rate.

Table 1 The results in Table 1 show that when lauric acid jetanolamide is added to a toothpaste containing tocopherol acetate and an anionic activator, the toothpaste is stored at high temperature for a long period of time;
It was observed that the decomposition of tocopherol acetate was well suppressed even when the tocopherol acetate was used, and the storage stability of tocopherol acetate was high.

Furthermore, it has been found that tocopherol acetate can be stabilized more reliably by blending lauric acid jetanolamide with a content of 0.51 or more. On the other hand, in line drawing brushes containing no lauric acid jetanolamide, tocopherol acetate was hydrolyzed when stored at high temperatures for long periods of time, resulting in poor storage stability.

Examples are shown below.

[Example 1] Toothpaste dicalcium phosphate dihydrate 50 tcal-oxymethylcellulose sodium 0.5 caradanan 0.5 sorbitol 15 glycerin
15 globylene glycol
2 Sodium lauryl sulfate
1 Lauric acid diethanolamide 0.3 Myrist/acid diethanolamide 0.3 Tocopherol acetate 0.05 Epsilonamicazolonic acid 0.017 Lantoinate Q,
01 β-glycyrrhetinic acid 0.01 Chlorhexidine gluconate 0.01 Methylnolaben 0.05 Sodium benzoate 0.3 Saccharin sodium 0.1 Flavor
1 [Example 2] Toothpaste dicalcium phosphate dihydrate 50q6 silicic anhydride
3 cal-xymethylcellulose sodium 1 sorbitol
15 Glycerin 1
0 Propylene glycol 2 Ethanol 0.5 Sodium higher alkyl sulfate (C1G-C16) "" Sodium lauroyl sarcosine 0.2 Zoethanolamide lauric acid 1 Tocopherol acetate
0.1 tranexamic acid
0.05β-glycyrrhetinic acid 0.
01 Chlorhexinone Hydrochloride 0.01 Licorice Extract 0.05 Methyl Lapen 0.1 Sodium Benzoate 0.1 Saccharin Sodium 0.1 Flavor
1 total
100.0 Ch*Higher alkyl sodium sulfate (CLO-016) The above is 9 of the total carbon number distribution
Items of 8 or more [Example 3] Toothpaste aluminum hydroxide 4o Chikara rnan l sodium alginate 0.5glycerin
25 Propylene Glycol 3
Sodium lauryl sulfate 0.3 Sodium lauroyl sarcosine 0.3 Myristate zoethanolamide 0.5 Tocopherol nicotinate 0.3 Tranexamic acid
0.05 Glycyrrhizinate dipotassium salt 0
．． 01 Sodium chloride 5 Chlorhexidine hydrochloride 0.01 Butylparaben 0.05 Sodium benzoate 0.3 Saccharin sodium
0.1 fragrance
1 [Example 4] Toothpaste Aluminum hydroxide 40 Calcium carbonate 2 Caradanan
1 sorbitol
30 higher alkyl sodium sulfate (C1°~C1
6) 1 Lauric acid diethanolamide 1.5 Myristic acid diethanolamide 0.5 Tocopherol nicotinate 0.1 Dextranase
, 2000U/g Toothpaste Chlorhexidine Gluconate 0.001 Sodium Monofluorophosphate 0.76 Butylno9 Lapen
0.02 Sodium benzoate
0.5 Stevioside 0
．． 1 Fragrance 1 [Example 5] Toothpaste Calcium Carbonate 45% Sodium Calxymethyl Cellulose 1.5 Sorbit 20 Glycerin
5 Propylene glycol 2 Sodium lauryl sulfate 2 Lauric acid diethanolamide 0.3 Myristic acid diethanolamide 0.3 No? Lumitic acid diethanolamide
0.3 Tocopherol acetate 0.1 Tranexamic acid 0.03 Chlorhexinone hydrochloride 0.001 Butylparaben 0.1 Sodium benzoate
0.57 Spartame
0.1 fragrance
1 [Example 6] Toothpaste calcium carbonate 45 Silicic anhydride 3 Caradanan
1 sorbitol
30 propylene glycol 2
Sodium higher alkyl sulfate (C1o-C46) 3 coconut oil fatty acid diethanolamide 0.3 mother rumitic acid diethanolamide 0.3 tocopherol nicotinate 0.1 tocopherol acetate
0.1 epsilon aminocaproic acid
0.01 Chlorhexinone gluconate 0.
001 Petyl no arm laben 0.0
2 Sodium benzoate 1 Stevioside 0.1 Flavor
1 [Example 7] Toothpaste Silicic anhydride 30 Sodium methylcellulose 1 Sorbit 10 Glycerin
25 polyethylene glycol
5 Sodium lauryl sulfate 0.3
Sodium lauroyl sarcosine 0.5 Lauric acid diethanolamide 0.5 Ristic acid jetanolamide' 0.5 Sucrose lauric acid monoester 1 Tocopherol nicotinic acid 0.
05 Alantoine) 0.01
Chlorhexidine hydrochloride 0.0017 Stannous trouside 0.4 Ethylparaben 0.02 Sodium benzoate 0.3 Saccharin sodium
0.1 fragrance
1 [Example 8] Toothpaste silicic anhydride 2 o Sodium xymethylcellulose 1 caradanan 0.5 sorbitol
40 glopylene glycol
3 Sodium lauryl sulfate
0.5 myristic acid diethanolamide 1-H sugar i4 lumitic acid monoester 0.3 tocopheryl acetate 0.3 β-glycyrrhetinic acid 0.01 chlorhexinone gluconate 0.017 sodium tsunide
0.2 ethyl arm lap pen
0.05 Sodium benzoate 0.5
Satucharin sodium 0.1 fragrance
1 [Example 9] Toothpaste calcium pyrophosphate 50% xanthan gum 1 sorbitol
30 propylene glycol
Sodium 2 higher alkyl sulfate (C1°~C
16) 1.5 lauric acid diethanolamide 0
．． 3-myristic acid zoethanolamide 0.5PO
E-hydrogenated castor oil 1.0 Tocopherol acetate 0.1 Dipotassium glycyrrhizinate 0.01 Sodium monofluorophosphate 0.76 Methyl nogurapen
0.2 Sodium benzoate
0.5 Satucalin sodium 0.1
Fragrance 1 [Example 10
] Toothpaste Monocalcium phosphate 50 Insoluble sodium metaphosphate 3 Hydroxyethyl cellulose 1 Rubit
10 Glycerin 15
Propylene glycol 2 Sodium lauryl sulfate 1 Lauric acid diethanolamide 0.5 Coconut oil fatty acid diethanolamide
2POE sorbitan monolaurate 0.3
Tocopherol acetate 0.5 Chlorhexidine hydrochloride 0.017 Sodium fluoride 0.2 Methylnoya laben
0.1 Sodium benzoate
0.3 Satucalin Sodium
0.1 fragrance 1 [
Example 11 Toothpaste Insoluble Sodium Metaphosphate 50% Sodium Calxymethylcellulose 1 Sorbit 20 Glycerin
5 Zoropyrene glycol 3 Ethanol 0.5 Sodium higher alkyl sulfate (C4゜~c, 6) 1.5 Noya lumitic acid jetanolamide 3 Lactitol monolaurate 0.5 Tocopherol acetate
1 Izosilone aminocaproic acid o
, oi sodium monofluorophosphate 0.76
Ethylparaben 0.1 Sodium benzoate 1 Sodium saccharin 0.1 Fragrance
1 Remaining purified ice
Example 12] Junsei Toothpaste Calcium Carbonate 7o Thisolbit 3 Glycerin
7 Sodium lauryl sulfate
1,5 lauric acid diethanolamide 1
Tocopherol acetate 0.1 Epsilon aminocaproic acid 0.03 Sacchulin sodium 0.1 Flavor
1 purified water
Remaining [Example 13] Liquid toothpaste glycerin 35 Tipropylene glycol 5 Sodium polyacrylate 3 Sodium lauryl sulfate
1 Lauric acid diethanolamide 2 Saccharin sodium 0.2 Fragrance
5-tocopherol acetate
0.5 purified water
Remaining [Example 14] Mouthwash ethanol (96 yen) 20 Eusaccharin sodium 0.3 POE hydrogenated castor oil 0.5 Sodium lauryl sulfate 0.5 Lauric acid diethanolamide 1 Fragrance 3
．． 5 Tocopherol acetate 0.1 Purified ice Remainder Examples 1-
All of the 140 oral compositions contained tocopherols stably even when stored at high temperatures.

Claims (1)

[Scope of Claims] 1. An oral composition comprising a nonionic active agent added to an oral composition containing tocopherol or an ester derivative thereof and an anionic active agent. 2. The oral composition according to claim 1, wherein the nonionic active agent is a fatty acid alkanolamide. 3. Claim 2, wherein the fatty acid alkanolamide is one or more selected from lauric acid diethanolamide, myristic acid diethanolamide, palmitic acid diethanolamide, coconut oil fatty acid diethanolamide, and beef tallow fatty acid diethanolamide. Oral composition as described. 4. The oral composition according to any one of claims 1 to 3, wherein the amount of tocopherol or its ester derivative is 0.01 to 5% by weight of the entire composition. 5. The amount of anionic activator is 0.1 to 5 of the total composition.
The oral composition according to any one of claims 1 to 4, which is % by weight. 6. The amount of nonionic activator is 0.1 to 5 of the total composition.
The oral composition according to any one of claims 1 to 5, which is % by weight.