JPS61130210A - Pasta containing stabilized chlorhexidine - Google Patents

Abstract

PURPOSE:A pasta for oral cavity that contains chlorhexidine hydrochloride or chlorhexidine gluconate, citric acid and carrageenan, thus being suitable for prevention or treatment for periodontosis, because it shows high stability with the passage of time and causes no discoloration. CONSTITUTION:The pasta for oral cavity contains 0.01-0.2wt% of chlorhexidine, or chlorhexidine gluconate, 0.1-1wt% of citric acid and 1-5wt% of carrageenan as a binder. The resultant pasta causes no problems on deterioration or discoloration of the chlorhexidine, even after it is stored at 40 deg.C for more than 3 months.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to pasta stably formulated with the antibacterial agent chlorhexidine, particularly for oral applications.

BACKGROUND OF THE INVENTION Traditionally, various medicinal agents have been incorporated into oral medicines and used for the prevention and treatment of periodontal diseases, etc.
It is also said that chlorhexidine antibacterial agent 1 is a medicinal agent suitable for application in the oral cavity. However, when chlorhexidine is added to pasta, there are problems in that the stability over time is poor and the pasta is colored.

Conventionally, it has been considered very difficult to incorporate chlorhexidine into pasta without these problems.

In view of these circumstances, the present inventors conducted extensive studies in order to obtain pasta that stably contains chlorhexidine. As a result, it was unexpectedly discovered that chlorhexidine in pasta can be specifically stabilized and prevented from discoloration by combining citric acid with carrageenan as a binder in a specific manner.1 This led to the completion of the present invention. reached.

Summary of the Invention The present invention comprises chlorhexidine hydrochloride or chlorhexidine gluconate 0.01 to 0.2% (weight %, same hereinafter), citric acid 0.1 to 1%, and carrageenan 1 to 5% as a binder. % of chlorhexidine is stably mixed therein. According to the present invention, only a specific combination of citric acid and carrageenan among various organic acids and binders, and in a specific amount of B, exhibits the excellent stabilizing effect of chlorhexidine and the effect of preventing discoloration of pasta. As a result, it is possible to obtain oral pasta containing chlorhexidine, which does not have the problems of chlorhexidine instability or coloring even when stored at 40°C for 3 months or more.

DETAILED DESCRIPTION OF THE INVENTION The pasta of the invention thus contains as essential ingredients the medicinal agent chlorhexidine hydrochloride or gluconate, citric acid and the binding agent carrageenan.

Chlorhexidine hydrochloride or gluconate should be added at 0.0% to the whole pasta from the viewpoint of its blending effect and economical efficiency.
01 to 0.2%.

If the amount of citric acid is too small, the effect of stabilizing chlorhexidine and preventing the coloring of pasta cannot be expected, and if it is too large, the acidity will become too strong and cause problems with the flavor.
．． Add 1 to 1%.

If the amount of carrageenan is too small, the stabilizing effect of chlorhexidine and the effect of preventing coloring of pasta cannot be expected;
The properties of the pasta cannot be maintained and too much will cause problems in production, so it should be used in a range of 1 to 5%.

The pasta of the present invention can be produced in the same manner as ordinary oral pasta, and the other ingredients are not particularly limited and may be any of those normally used for this type of pasta. Furthermore, the obtained pasta can be used for the prevention and treatment of periodontal diseases and the like in the same manner as ordinary pasta for intraoral application.

Example Next, the present invention will be explained in more detail with reference to Examples.

Example 1 Pasta containing stable chlorhexidine was obtained by a conventional method according to the following recipe.

Ingredients Polychlorhexidine hydrochloride 0.05 Methyl paraoxybenzoate 0.05 Carrageenan 3.00 Glycerin 30.00 Glyceryl monostearate 8.00 Polyoxyethylene sorbitan 2.00 Monooleate (20E
, O,) Citric acid 0.30 Saccharin sodium o, i.

Purified water adjusted to ioo% Example 2 Pasta stably blended with chlorhexidine was obtained by a conventional method according to the following recipe.

Ingredients % Chlorhexidine gluconate 0.01 Methyl paraoxybenzoate 0.10 Carrageenan
2.50 Glyceryl Monostearate 10.00 Polyoxyethylene Rubitan 4.00 Monooleate (20E, 0.
) Sodium lauryl sulfate 0.10 Citric acid 0.10 Sodium saccharin 0.10 Sorbitol 20.00 Purified water
Adjustment to 100% Example 3 Pasta in which chlorhexidine was stably blended was obtained according to the following recipe.

Ingredients Polychlorhexidine gluconate 0.05 Glythyl paraoxybenzoate 0.10 Carrageenan
2.50 Glycerin Monostearate 10.00 Polyoxyethylene Rubitan
4.00 Monooleate (20E, 0.) Citric Acid 0.30D-
Xylose 0.10 Sorbitol 20.00 Sodium lauroyl sarcosine 0.10 Purified water
100% L Coordination Example 4 Pasta stably mixed with chlorhexidine was obtained according to the following recipe.

Ingredients % Chlorhexidine hydrochloride 001 Methyl paraoxybenzoate 0.05 Butyl paraoxybenzoate 0.05 Carrageenan
3.00 Glycerin Monostearate 10.00 Polyoxyethylene Rubitan
4.00 Monooleate 1- (20E, 0.) Sodium lauryl sulfate 0.10 Citric acid 0.10 Sodium saccharin 0.10 Rubitol 20. OO spirit! summer water
Adjustment to 100% Example 5 Pasta stably blended with chlorhexidine was obtained according to the following recipe.

Ingredients Polychlorhexidine hydrochloride 0.10 Methyl paraoxybenzoate 0.10 Carrageenan 3.00 Glycerin 10.00 Glycerylmo/stearate 10.00 Polyoxyethylene rubitan
4.00 Monooleate (20E, O,) Sodium lauryl sulfate 0.10 Citric acid 0.500-Xylose 0.10 Rubitol 10.00 Purified water
Adjustment to 100% Example 6 Pasta in which chlorhexidine was stably blended was obtained according to the following recipe.

Ingredients % Chlorhexidine jtha salt 0.20 Gtyl paraoxybenzoate 0.10 Carrageenan 3.00 Glycerin 1.00 Glycerin monostearate 1- 10.00 Polyoxyethylene sorbitan 4.00 Mopooleate (2
0E, 0. ) Sodium lauryl sulfate 0.05 Citric acid 1.00 Sodium saccharin 0.05 D-xylose 0.05 Rubitol 10.00 Sodium lauroyl sarcosinate 0.05 Purified water
Adjusted to 100% (11 Coloration prevention effect of various organic acids) Pasta 2 of Example 1 and the pasta obtained by replacing the citric acid in its formulation with the same amount of other various organic acids were heated at 40"C. It was stored for one month, and the coloring state S and flavor were sensually compared, and the evaluation was 1'iI[iL,] based on the following criteria.

Coloration ○: No coloration observed visually.

X: Visually observed coloration.

Taste ○: Good flavor.

X: Poor flavor.

The results are shown in Table 1.

As is clear from Table 1, among the various organic acids, only citric acid specifically prevents the coloring of pasta and also satisfies the flavor.

(2) Discoloration prevention effect of binder In Pasta 2 of Example 1 and its formulation, carrageenan was added to the same amount of other various binders (pasta obtained by
"C" for one month, and the coloring state was evaluated in the same manner as above. The results are shown in Table 2.

As shown in Table 2, only when carrageenan is used as a binder, coloring of the specific pasta is prevented.

(3) Amount of citric acid and stabilization of chlorhexidine 2
Relationship between coloration and anti-coloring effect Pastas were prepared with various amounts of citric acid in the formulation of Example 1, and after each was stored at 40"C for 1 month, the coloring state 2 and flavor were evaluated in the same manner as above. In addition, the chlorhexidine content was measured and compared with the chlorhexidine content at the beginning of pasta kneading, and the stabilizing effect of chlorhexidine was evaluated according to the criteria set forth in the above.

○: When the chlorhexidine content at the beginning of kneading is 100, 40"C, the content after 1 month is 90% or more.

×: When the chlorhexidine content at the beginning of kneading is taken as 100%, the content after 11 months at 40°C is less than 90%.

The results are shown in Table 3.

Table 3 As shown in Table 3, flavor, chlorhexidine stabilization S
The amount of citric acid was 0 in order to satisfy all the requirements of coloring and color prevention.
．． 1% to 1%.

(41 Carrageenan content and pasta shape) Pasta was prepared with various amounts of carrageenan in the formulation of Example 1, and the properties of the pasta were evaluated. In addition, during kneading during production, it is not possible to knead cloudy dough without a certain degree of fluidity. Those having the above-mentioned conditions were evaluated as ○, and the others were evaluated as ×.The results are shown in Table 4.

Table 4 As is clear from Table 4, the amount of carrageenan is 1 to 5.
%.

(5) Prepared according to the pasta and togi recipe of Preservation Test Example 1,
Pasta without citric acid and carrageenan (control)
was stored at 40°C for 3 months and the stability of chlorhexidine3 and coloration were evaluated. Control pasta formulation ingredients Polychlorhexidine hydrochloride O,OS Methyl paraoxybenzoate 0.05 Sodium carboxymethyl cellulose 3. oO Glycerin 30.00 Glycerin monostearate 8.00 Polyoxyethylene rubitan 2.00 Monosdearate (20E, O,) Sodium saccharin 0.10 Purified water 100%L The adjustment results are shown in Table 5. In Table 5, stability is expressed as the relative proportion (%) of chlorhexidine remaining after storage to the chlorhexidine content during pasta kneading, and coloring is expressed on the same basis as above.

Table 5 As is clear from Table 5, the combination of citric acid and carrageenan can specifically stabilize chlorhexidine and prevent it from sticking to pasta.

Special liver applicant Sunstar Co., Ltd.

Claims (1)

[Claims] (1) Chlorhexidine hydrochloride or chlorhexidine gluconate 0.01-0.2% by weight, citric acid 0.1
~1% by weight and 1 to 5 carrageenan as a binder
A pasta stably containing chlorhexidine, which is characterized by containing chlorhexidine at % by weight.