JPS5812252B2 - toothpaste composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a dentifrice composition, and more particularly to a dentifrice composition with excellent plaque prevention effects.

Dental plaque is a major cause of diseases such as cavities and periodontal disease in the oral cavity.

The main component of this dental plaque is dextran, which is produced by polymerizing sugar from Strebutococcus mutans, a type of streptococcus found in the oral cavity.

Therefore, the use of the enzyme dextranase to decompose this dextran has been considered to prevent dental plaque, but it is not necessarily suitable as a medicinal agent to be incorporated into toothpaste from the viewpoint of stability.

On the other hand, in recent years, water-soluble acid addition salts of l,6-di(P-chlorophenylbiguanide)hexane, for example, have been developed and put into practical use as chemicals that prevent plaque due to their antibacterial properties. When this water-soluble salt is added to toothpaste, it is difficult to exist in an effective form due to interaction with toothpaste ingredients, and only about 30% of the amount of water-soluble salt is eluted from the toothpaste when used. A sufficient plaque prevention effect cannot be expected.

In view of the current situation, the present inventors have conducted various research and found that ■.
When phospholipids are used in combination with a dentifrice composition containing a water-soluble acid addition salt of 6-di(P-chlorophenylhycuanido)hexane, the amount of the water-soluble acid addition salt eluted during use is significantly increased. This discovery led to the completion of the present invention.

That is, the present invention provides a dentifrice composition characterized in that a phospholipid is blended into a dentifrice composition containing a water-soluble acid addition salt of l,6-di(P-chlorophenylbiguanide)hexane. During use, the dentifrice composition of the present invention exhibits excellent dissolution of the water-soluble acid addition salt of 1,6-di-(P-chlorophenylbiguanito)hexane and exhibits the desired antibacterial activity. It exhibits excellent plaque prevention effects.

Examples of water-soluble addition salts of 1,6-C-(P-chlorophenylbiguanidohexane) include diglucohebutanoate, diincyanate, diacetate, monogluconate, digluconate, diisobutyrate, Dilactate, dimethasulfonate, etc. are used.

Examples of phospholipids include lecithin, cephalin, phosphatidylserine, which are classified as phosphatides in the field of complex lipids.
Examples include inositol phosphatide, and phospholipids extracted from egg yolk, natural butter, wheat and corn germ, soybean, etc. may be used, and it is particularly preferred to use soybean phospholipids, which are easily available.

Next, the results of a test regarding the dissolution properties of 1,6-di(P-chlorophenylbiguanide)hexane water-soluble acid addition salts will be shown.

1,6-di(P-chlorphenylhycuanide)hexane digluconate extracted by varying the concentration using various phospholipids (lecithin, cephalin, phosphatidylserine) according to the recipe of Example 2. The amount of salt was measured.

The results are shown in the table below.

Measurement method: Precisely weigh 20 g of toothpaste into a 100 ml beaker, add 15 liters of water and disperse, then add 10% cetyl imide and 30 ml of isopropyl alcohol and stir for 20 minutes.

After stirring, centrifuge (10,000 rpm for 20 minutes) and transfer the supernatant to a 100 ml volumetric flask.

Inglovir alcohol 12mlN sodium hydroxide solution 51nl, sodium hypobromite solution (NaOH10.
Dissolve 5.5 ml of bromine in water and add 5 ml of Kashite 500 d) to develop color, and add water to the marked line 1.
00ml.

Immediately after color development, absorbance (480 nm) is measured.

As a control solution, a toothpaste containing no 1,6-di-(P-chlorophenylhycuanito)hexane digluconate was subjected to the same procedure.

The standard solution was 1,6-di-(P-chlorophenylbiguanito)hexane digluconate solution (1.07 g
/100ml), 30ml of 10% cetyl imide
, isopropyl alcohol 15Fd, INNaOH solution (5 ml), sodium hypobromite solution (5 ml), and the color was developed in the same manner as above.

As is clear from the above results, the blended concentration of phospholipids is 0.
．． It can be seen that when it exceeds 5%, the amount of elution increases significantly.

In particular, there is no upper limit to the concentration of phospholipids, but if it exceeds 4%, the toothpaste will become discolored and its marketability will be impaired.
Since there is not much difference in elution effect, it is usually 0.5 to 4.
It is preferable to blend phospholipids in a range of 0% by weight.

The dentifrice composition of the present invention includes all conventional dosage forms such as toothpaste, toothpaste, dentifrice ointment, and water dentifrice.

In addition, other dentifrice base components may be those used in ordinary dentifrice compositions, such as abrasives such as dicalcium phosphate (dihydrate, anhydride), calcium carbonate, silicate, insoluble metaphosphoric acid. Sodium, etc.: As a binder, carboxymethyl cellulose sodium, carrageenan,
Sodium alginate, bentonite, silicic anhydride, etc. Wetting agents include glycerin, sorbitol, propylene glycol, sodium pyrrolidone carboxylate, polyethylene glycol, etc. Foaming agents include sodium lauryl, sucrose fatty acid ester, sodium N-acylsarcosine, etc. is used.

Furthermore, sweeteners, flavors, preservatives, etc. are also appropriately added.

Furthermore, the dentifrice composition of the present invention may contain various other medicinal agents, such as sodium monofluorophosphate, aluminum allantoinate, glycyrrhizinate, chlorhexidine, hinokitiol, and dextrose. Stranase, lysozyme, salt, tranexamic acid,
Examples include ε-aminocaproic acid.

According to the present invention, the antibacterial agent in toothpaste is present in an effective form even during use due to the combination of phospholipids as described above,
Moreover, since the dissolution property is increased, a dentifrice composition having an excellent plaque prevention effect can be obtained.

Next, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited thereto.

% in the examples indicates weight %.

Example 1 A toothpaste was prepared according to a conventional method using the following recipe.

Ingredients % Calcium phosphate dihydrate 42.0 Sodium carboxymethylcellulose 1.0 Carrageenan 0.5 Glycerin
5.0 Sorbitol
15.0 water
31.2 Sodium lauryl sulfate
2.0 fragrance
1.01.6-di-(P-chlorphenylvic o.i anido)hexane digluconate phospholipid 1.0
Sodium monofluorophosphate 0.8 Sodium saccharin 0.2 Preservatives
0.2 Example 2 A toothpaste was prepared according to a conventional method using the following formulation.

Ingredients % Calcium carbonate 45.0 Sodium carboxymethylcellulose 0.5 Carrageenan 0.5 Glycerin
15.0 Sorbitol
lO. 0 ingredients
% Water 24.0 Sodium lauryl sulfate 2.0 Fragrance
1.01・6
-di-(P-chlorphenylvic0.2anido)hexane digluconate phospholipid 1.5
Satucalin sodium 0.2 preservative.

．． 1 Example 3 A toothpaste was prepared according to a conventional method using the following recipe.

Ingredients % Calcium phosphate dihydrate 40.0 Sodium carboxymethyl cellulose 1.0 Carrageenan 0.5 Glycerin
10.0nlubitol
12.0 Propylene glycol
3.0 water
26.8 Sucrose fatty acid ester
1. ON-sodium lauroyl sarcosine 0.51・6--)-(P-chlorphenylbi' 0.1 anido)hexane/diacetate phospholipid 3.0
Sodium monofluorophosphate 0.8 Sodium saccharin 0.2 Flavoring
1.0 preservative
0.1 Example 4 A toothpaste was prepared according to a conventional method using the following recipe.

Ingredients % Dibasic calcium phosphate dihydrate 45.0 Sodium carboxymethylcellulose 0.5 Carrageenan
0.5 glycerin
10.0 Sorbitol
10.0 water
21.8N-Lauroylsulfucin sodium 0.51.6-di(P-chlorphenyl bi'0
．． 2 Anide) Hexane diacetate phospholipid 40 Sodium monofluorophosphate 0.8 Sasicaline sodium 0.1 Fragrance
0.9 preservative
0.2 Example 5 A toothpaste was prepared according to a conventional method using the following formulation.

Ingredients % Aluminum hydroxide 5.0 Sodium carboxymethyl cellulose 1.0 Carrageenan 0.5 Glycerin
10.0nlubitol
10.0 water
28.0 Sodium lauryl sulfate
2.0 fragrance
1.0 preservative
0.1 Satsukalin Sodium
0.21.6-G (P-chlorphenirbig)

Claims (1)

[Claims] A dentifrice composition comprising a dentifrice composition containing a water-soluble acid addition salt of 11,6-di-(p-chlorophenylbiguanide)hexane and 0.5 to 4.0% by weight of phospholipid. thing.