JPH1112144A - Liquid oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare the subject composition excellent in retention of active ingredient and sustainability of efficacy of the medicine, hardly causing sticky feeling and having a thick feeling by formulating a specific nonionic water-soluble high molecular compound with the liquid oral composition containing the active ingredient. SOLUTION: This liquid oral composition is obtained by formulating an active ingredient in combination with polyvinylpyrrolidone and polyvinyl alcohol and/or polyethylene oxide, which are nonionic water-soluble high molecular compound. The formulating amount of the active ingredient is 0.01-5 wt.%. The formulating amount of the polyvinylpyrrolidone is 0.1-10 wt.%, and that of the polyvinyl alcohol and polyethylene oxide is 0.1-10 wt.%. Further, the total formulating amount of the before water-soluble high molecular compounds is 0.2-10 wt.%. Further, the composition preferably contains 1-15 wt.% one or more kinds of polyhydric alcohols selected from polypropylene glycol, polyethylene glycol and glycerol.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for a liquid oral cavity which has an excellent retention property of a medicinal ingredient in the oral cavity, can maintain the medicinal effect for a long time, and has a practical feeling of stickiness and thickness. About.

[0002]

2. Description of the Related Art
Various medicinal ingredients are blended in the oral composition. In an oral composition containing this medicinal ingredient, it is important that the preparation can be easily spread to every corner of the oral cavity, and a highly dispersible liquid dosage form is effectively used for this purpose. Furthermore, in consideration of prevention of oral diseases, it is also important that a drug that has penetrated into every corner stays for a long time and exhibits a medicinal effect.

[0003] However, the medicinal components incorporated in the oral composition generally have low retention in the oral cavity. Particularly, in the case of liquid dosage forms such as mouth rinses, they are exhaled or swallowed after oral rinse. However, it is difficult for the drug to remain sufficiently, and therefore, there has been a problem in improving the sustainability of the drug effect.

Accordingly, the retention of the above-mentioned medicinal ingredients in the oral cavity is as follows:
Although it depends on the intrinsic properties of the components, there has been a demand for the development of a technique capable of maintaining the active ingredients in the liquid dosage form for a longer time.

[0005]

Means for Solving the Problems and Embodiments of the Invention The present inventor has conducted intensive studies to meet the above-mentioned demands. As a result, a nonionic water-soluble polymer was added to a liquid oral composition containing a medicinal ingredient. By compounding a compound of polyvinylpyrrolidone and polyvinyl alcohol and / or polyethylene oxide in combination, these water-soluble polymer compounds act as anchor components, and a medicinal component for making the medicinal component easily remain in the oral cavity. Tooth, bridging the gingiva, the medicinal component stays in the oral cavity for a long time even after exhalation and swallowing, and it is possible to sufficiently bring out the medicinal effect, even though the water-soluble polymer compound is blended, The viscosity at the time of use, the feeling of use such as stickiness can be easily adjusted, there is no sticky feeling, and the actual feeling of thickening can be obtained, To, propylene glycol, by blending one or more polyhydric alcohols selected from polyethylene glycol and glycerin, and finding that the effect described above is further improved, leading to the completion of the present invention.

Accordingly, the present invention provides a liquid oral composition containing a medicinal ingredient and a combination of polyvinylpyrrolidone and polyvinyl alcohol and / or polyethylene oxide. The above-mentioned composition for liquid oral cavity containing one or more polyhydric alcohols selected from propylene glycol, polyethylene glycol and glycerin is provided.

Hereinafter, the present invention will be described in more detail. The liquid oral composition of the present invention can be prepared as a liquid dentifrice, a mouthwash and the like, and has a medicinal component, polyvinylpyrrolidone, polyvinyl alcohol and / or polyethylene oxide. And is used in combination.

[0008] Here, as the medicinal component, various compounds which are usually blended in an oral composition can be used, for example, a fluorine source (sodium fluoride, sodium monofluorophosphate, stannous fluoride), a bactericide (Triclosan, cetylpyridinium chloride, chlorhexidine salts, benzethonium chloride, benzalkonium chloride, biosol, thymol, etc.), enzyme agents (dextranase, mutanase, etc.), anti-inflammatory agents (dipotassium glycyrrhizinate, sodium azulene sulfonate, allantoin, Glycyrrhetinic acid, tranexamic acid), deodorant components (sodium copper chlorophyllate, copper gluconate, etc.), vitamin E and the like can be added.

The compounding amount of the medicinal component can be a usual compounding amount according to each component, and is an effective amount.
The range is from 01 to 5% (% by weight, the same applies hereinafter).

Next, the average molecular weights of the water-soluble polymer compounds polyvinylpyrrolidone, polyvinyl alcohol, and polyethylene oxide are not particularly limited. In particular, polyvinyl pyrrolidone has a molecular weight of 200,000 to 1200,000, polyvinyl alcohol has a molecular weight of 40,000 to 200,000, and polyethylene oxide has a molecular weight of 40,000. ~ 1,000,000
Is suitable.

The amount of polyvinylpyrrolidone is preferably 0.1 to 10%, more preferably 0.1 to 5% of the whole composition.

The total amount of polyvinyl alcohol and polyethylene oxide is 0.1 to 10 in the total composition.
%, Particularly preferably 0.1 to 5%.

The total amount of the water-soluble polymer compound is preferably from 0.2 to 10%, especially from 0.2 to 5% of the whole composition. Is not sufficient, and if it exceeds 10%, the sticky feeling becomes strong and the usability deteriorates.

Preferably, the composition of the present invention further contains one or more polyhydric alcohols selected from propylene glycol, polyethylene glycol and glycerin. By adding a polyhydric alcohol, the retention of the medicinal ingredient in the oral cavity and the feeling of use are further improved.

The compounding amount of the polyhydric alcohol is preferably 1 to 15%, particularly 5 to 10% of the whole composition, and if it is less than 1%, a sufficient effect of addition may not be obtained.
If it exceeds 5%, there may be a sticky feeling or a warm feeling during use.

[0016] In addition to the above components, the liquid oral composition of the present invention may further comprise, as a surfactant, a sorbitan fatty acid ester,
Nonionic surfactants such as glycerin fatty acid ester, sucrose fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene / polyoxypropylene polymer, fatty acid diethanolamide, alkyl sulfate, alkyl ether sulfate, alkylbenzene sulfonate, N-acyl amino acid salts, N-acylmethyl taurine salts, anionic surfactants such as alkyl ether acetates,
Cationic surfactants such as alkyl ammonium salts and alkyl benzyl ammonium salts, and amphoteric surfactants such as alkyl betaines, imidazolinium betaines, and lecithin can be blended.

The amount of the surfactant is 0.1% of the whole composition.
1-5%, especially 0.5-3%, is preferred.

In the composition of the present invention, other optional components such as saccharin, flavoring agents such as flavors, citrate,
PH adjusters such as phosphates, preservatives such as parabens, coloring agents, ethanol and the like can be blended.

The viscosity of the liquid oral composition of the present invention is preferably 0.005 to 0.2 Pa · s at 25 ° C.

[0020]

EFFECT OF THE INVENTION The composition for liquid oral cavity of the present invention is excellent in the retention of medicinal ingredients in the oral cavity, can exert the medicinal effect for a long time, has no sticky feeling, and has a thick feeling. It has a real feeling.

[0021]

EXAMPLES The present invention will be specifically described below with reference to experimental examples and examples, but the present invention is not limited to the following examples. In the following examples, all percentages are weight percentages.

Experimental Example 1 A formulation having the following composition was prepared by mixing sodium fluoride as a medicinal ingredient and a water-soluble polymer compound shown in Table 1, and evaluated for fluorine adsorption by the following method. Table 1 shows the results. Formulation composition: Sodium fluoride 0.05% Glycerin (85%) 8.0 Water-soluble polymer compound shown in Table 1 0.1 POE hydrogenated castor oil 1.2 Citric acid 0.03 Sodium citrate 0.25 Fragrance 0. 2 Purified water balance meter 100.0%

Evaluation method of fluorine adsorptivity: Hydroxyapatite powder was used as a tooth model, and 0.1 g of this apatite powder was added with 5 ml of the above formulation solution and treated at 37 ° C for 3 minutes. After washing with distilled water, 0.5N perchloric acid 25m
The resulting solution was dissolved in 1 liter, a pH 5.3 acetate buffer was added, and the fluorine concentration was measured with a fluorine ion meter.

The evaluation criteria were as follows: control (composition not containing a water-soluble polymer compound): 100;
○: 110 to less than 130, Δ: 100 to less than 110, ×: less than 100.

[0025]

[Table 1]

From the results in Table 1, it can be seen that the addition of polyvinylpyrrolidone to the above-mentioned preparations significantly improved the fluorine adsorption property, and that the same tendency was observed even when polyvinyl alcohol and polyethylene oxide were added. I understood.

[Experimental Example 2] Triclosan and cetylpyridinium chloride (CPC) were used as active ingredients, respectively.
In addition, a formulation having the following composition containing the water-soluble polymer compound shown in Table 2 was prepared, and the adsorption of triclosan and CPC was evaluated by the following method. Table 2 shows the results. Formulation composition: Triclosan 0.02% Glycerin (85%) 8.0 Water-soluble polymer compound shown in Table 2 0.1 POE hydrogenated castor oil 1.2 Citric acid 0.03 Sodium citrate 0.25 Fragrance 0.2 Ethanol 2.0 Purified water Balance meter 100.0% Cetylpyridinium chloride 0.05% Glycerin (85%) 8.0 Water-soluble polymer compound shown in Table 2 0.1 POE hardened castor oil 0.5 Citric acid 0.03 Citric Sodium acid 0.25 Fragrance 0.2 Ethanol 5.0 Purified water Balance meter 100.0%

Evaluation method for triclosan and CPC adsorbability:
5 ml of the above formulation solution was added to 0.1 g of apatite powder and treated at 37 ° C. for 3 minutes. After washing with distilled water, ethanol was added and collected, and the amount of the drug was measured. The evaluation criteria were the same as in Experimental Example 1.

[0029]

[Table 2]

From the results in Table 2, it can be seen that triclosan, CPC were obtained by adding polyvinylpyrrolidone to the above preparation.
It was found that remarkable improvement in adsorbability was observed, and similar tendency was observed even when polyvinyl alcohol or polyethylene oxide was added.

[Examples 1 to 10, Comparative Examples 1 to 4] Mouthwashes having the following compositions were prepared, and the fluorine adsorption was evaluated in the same manner as in Experimental Example 1. After that, eight panelists put 10 ml of each preparation into the mouth. After the mouth was rinsed for 20 seconds, it was exhaled, and the feeling of use due to stickiness and thickening was evaluated according to the following evaluation criteria. Table 3 shows the results. Mouthwash composition: Sodium fluoride 0.05% Glycerin 5.0 Propylene glycol 1.0 Ethanol 5.0 Water-soluble polymer compound shown in Table 3 Amount shown in Table 3 POE (60) hydrogenated castor oil 1.2 Saccharin sodium 0 .1 Citric acid 0.03 Sodium citrate 0.25 Sodium benzoate 0.3 Fragrance 0.2 Purified water Balance meter 100.0% Evaluation criteria: Actual feeling of use due to thickening ○: Good actual feeling of use △: Somewhat good actual feeling of use ×: No real feeling of use

[0032]

[Table 3]

Examples 11 to 21 Liquid oral compositions having the compositions shown in Table 4 were prepared by an ordinary method.

[0034]

[Table 4]

Claims (2)

[Claims] 1. A liquid oral composition comprising a liquid oral composition containing a pharmaceutically active ingredient and a combination of polyvinylpyrrolidone and polyvinyl alcohol and / or polyethylene oxide. 2. The liquid oral composition according to claim 1, comprising one or more polyhydric alcohols selected from propylene glycol, polyethylene glycol and glycerin.