JPH10245329A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition, high in adhesivity to the affected part, especially in local persistence in the affected part, and showing an excellent treatment effect for an extended period, by including a hydrophobic ointment base, water-soluble polymer, medicine and light silicic anhydride. SOLUTION: This composition comprises (A) 40 to 90wt.% of a hydrophobic ointment base (e.g. liquid paraffin), (B) 5 to 50wt.% of a water-soluble polymer (e.g. sodium carboxymethylcellulose), (C) 0.05 to 10wt.% of a medicine (e.g. hydrocortisone), and (D) 1 to 10wt.% of light silicic anhydride (e.g. brand name: Aerosil). Preferably, the component B/component A weight ratio is (3:2) to (1:25) and the component D/component B weight ratio is (2:1) to (1:30).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a composition for the oral cavity, and more particularly to an improvement in its retention in the oral cavity.

[0002]

2. Description of the Related Art In general, a base such as an ointment must have good adhesion to an application site. In the case of a base such as an oral ointment, the oral mucosa is always in a wet state. The composition must be capable of adhering well to the affected area for a long time after application without being easily dispersed by saliva or the like, and capable of maintaining the efficacy.

[0003] For this reason, an ointment base conventionally applied to the oral mucosa is based on a hydrophobic ointment base so as not to be easily dissolved and dispersed. A compound containing a water-soluble polymer is widely used. Examples of the water-soluble polymer to be blended include polyacrylic acid (salt), carboxymethylcellulose (salt), alginic acid (salt), polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropylcellulose, gum arabic, karaya gum, tragacanth gum, xanthan gum, and locust. Bean gum, guar gum, carrageenan, galactomannan, gelatin, agar, pullulan, pectin, starch, methacrylic acid-based copolymers, cellulose derivatives and the like are known. The water-soluble polymer blended in an appropriate amount absorbs water and becomes tacky, and serves to strongly adhere the oral ointment base to the local area, and at the same time, to reduce irritation and discomfort to the local area. Have. For example, as examples in which sodium polyacrylate is blended as the water-soluble polymer, there are the compositions described in JP-A-51-38412 and JP-A-53-86011. The aim of these oral compositions is to gradually supply the compounded drug to the affected area and perform treatment as the composition gradually dissolves locally.

[0004]

However, in the oral composition of the type in which the above-mentioned conventional water-soluble polymer is dispersed in a hydrophobic ointment base, the water-soluble polymer absorbs and thickens on the surface of the wet mucous membrane. However, the viscosity of the paste increases with time, but on the other hand, the paste starts to disintegrate in a relatively short time and the local retention is not sufficient, so that the protection of the affected mucous membrane and the continuous supply of the drug to the affected area are reduced. It was not always satisfactory. The present invention has been made in view of the above-mentioned problems of the prior art, and an object of the present invention is to provide a novel oral cavity which has a high adhesiveness to an affected area, particularly a high local retention property of a composition, and provides an excellent therapeutic effect over a long period of time. To provide a composition for use.

[0005]

Means for Solving the Problems The present inventors have conducted intensive studies in order to solve the above-mentioned problems, and as a result, in addition to the hydrophobic ointment base, the water-soluble polymer and the drug conventionally used in oral compositions, Further, they have found that an oral composition containing light anhydrous silicic acid not only has excellent adhesion to oral mucosa, but also significantly increases local retention. Furthermore, it was also found that the composition for oral cavity of the present invention had little discomfort when used and was not irritating. That is, the oral composition according to the present invention is characterized by containing a hydrophobic ointment base, a water-soluble polymer, a drug, and light anhydrous silicic acid.

It is preferable that the composition according to the present invention contains sodium carboxymethylcellulose as a water-soluble polymer. Further, in the composition containing sodium carboxymethylcellulose according to the present invention, as the water-soluble polymer, a composition further containing one or more selected from sodium alginate, hydroxypropylcellulose, agar, and sodium hyaluronate may also be used. It is suitable.

Further, in the composition according to the present invention, it is preferable that the average particle size of the light anhydrous silicic acid is 0.1 μm or less. Further, in the composition according to the present invention, it is preferable that the blending amount of the light silicic anhydride is 1 to 10% by weight. In the composition according to the present invention, the mixing ratio of light anhydrous silicic acid to the water-soluble polymer is 2: 1 to 1: 3.
It is preferably 0.

[0008]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will be described below in detail. Examples of the hydrophobic ointment base used in the present invention include petroleum jelly, solid paraffin, liquid paraffin, and gelled hydrocarbons such as microcrystalline wax. Preferably, liquid paraffin [trade name: Plastibase, manufactured by Bristol-Myers Squibb Co., Ltd.] in which 4% of a polyethylene resin having low temperature dependence of hardness is dispersed is good.

The amount of the hydrophobic ointment base used in the present invention is preferably 40 to 90% by weight, more preferably 50 to 90% by weight.
It is 85% by weight, particularly preferably 60 to 80% by weight.
If the blending amount of the hydrophobic ointment base is too small, the local retentivity as a preparation is undesirably reduced.

The water-soluble polymer used in the present invention has been conventionally used in oral compositions, and is not particularly limited, but sodium carboxymethylcellulose is preferred. Further, a composition containing one or more selected from sodium alginate, hydroxypropyl cellulose, agar, and sodium hyaluronate in addition to sodium carboxymethylcellulose is also suitable.

The amount of the water-soluble polymer used in the present invention is 5 to 50% by weight, preferably 10 to 40% by weight, particularly preferably 20 to 30% by weight. If the amount of the water-soluble polymer is small, sufficient adhesiveness to the affected part may not be obtained. In addition, if the amount of the water-soluble polymer is too large, water absorption from the mucous membrane becomes too large to give pain to the affected area, and the oral composition may be easily dissolved and dispersed, resulting in poor local retention, which is preferable. Absent.

The mixing ratio of the water-soluble polymer to the hydrophobic ointment base used in the oral composition of the present invention is 3: 2 to 1: 2.
5, preferably 1: 1 to 1:15, more preferably 1: 2 to 1:10. The light anhydrous silicic acid used in the present invention is an extremely fine powdered anhydrous silica represented by SiO ₂ , and need not have an internal surface area.

The average particle size of the light anhydrous silicic acid used in the present invention is 0.1 μm or less, more preferably 7 to 10 μm.
40 nm [Example: trade name Aerosil, manufactured by Nippon Aerosil Co., Ltd.]. As the particle size increases, the local retentivity of the oral composition becomes inferior. Therefore, the particle size is preferably as small as possible.

The amount of light anhydrous silicic acid used in the oral composition of the present invention is preferably 1 to 10% by weight, more preferably 2 to 8% by weight, and particularly preferably 3 to 6% by weight. If the amount of light anhydrous silicic acid is small, sufficient local retentivity to the oral mucosa cannot be obtained, and if the amount of light anhydrous silicic acid is too large, the preparation becomes too hard and does not cause discomfort during use. It is not preferable because it involves irritation.

The mixing ratio of the light anhydrous silicic acid to the water-soluble polymer used in the oral composition of the present invention is 2: 1 to 1: 3.
0 is suitable, preferably 1: 1 to 1:20, more preferably 1: 2 to 1:10. If the ratio is out of these ranges, the composition may not be able to obtain excellent retention, usability, and tackiness, which is not preferable.

The drug used in the oral composition of the present invention is not particularly limited as long as it is used in the oral cavity. Examples thereof include hydrocortisone, triamcinolone, dexamethasone, prednisolone, triamcinolone acetonide, hydrocortisone acetate, and acetate. Examples include steroidal anti-inflammatory drugs such as dexamethasone, local anesthetics such as lidocaine hydrochloride, dibucaine hydrochloride, and procaine hydrochloride, and bactericides such as chlorhexidine hydrochloride, cetylpyridinium chloride, berzarkonium chloride, benzethonium chloride, and the like.

The compounding amount of the drug used in the present invention is 0.1.
It is from 0.05 to 10% by weight, preferably from 0.1 to 5% by weight, particularly preferably from 0.5 to 3% by weight. If the compounding amount of the drug is small, sufficient pharmacological action on the affected area cannot be obtained, and if the compounding amount of the drug is too large, other components relatively decrease and the intended effect may not be obtained. is there. Also,
Some drugs are not preferable because they cause side effects.

To the oral composition of the present invention, an acidic substance such as an organic acid may be added to the system as a pH adjuster for stabilizing the above-mentioned main drug and the like. Examples of the acidic substance used herein include citric acid, adipic acid, tartaric acid, maleic acid, isocitric acid, fumaric acid, malic acid, succinic acid, gluconic acid, lactic acid, malonic acid, glutaric acid, glutaconic acid, and aspartic acid. , Glutamic acid, pimelic acid, oxalic acid, glycolic acid, glyceric acid, pyruvic acid, acrylic acid, methacrylic acid, suberic acid, azelaic acid, mevalonic acid, ethylenediaminetetraacetic acid, phthalic acid, terephthalic acid, oxyacetic acid, phenylsuccinic acid, Ethylmalonic acid, pivalic acid, undecanoic acid, lauric acid, myristic acid, valmitic acid, stearic acid,
Behenic acid, N-palmitoyl-L-glutamic acid, ascorbic acid, pyrrolidonecarboxylic acid, sulfamic acid,
Glucono delta lactone, phosphoric acid, monopotassium phosphate,
Monosodium phosphate, carbonic acid, boric acid and the like can be mentioned, and if necessary, one or more kinds can be used in combination.

The oral composition of the present invention may further contain, if necessary, drugs other than the above-mentioned main drugs and pH adjusters (eg, vitamins, antipruritics), excipients (absorption enhancers, fresheners). , Antioxidants, gelling agents, chelating agents, oils,
Surfactants, fragrances, coloring agents, etc.) can be added as long as the effects of the present invention are not impaired.

[0020]

EXAMPLES Next, the present invention will be described in more detail with reference to Examples, Comparative Examples and Test Examples of the oral composition of the present invention, but these do not limit the present invention in any way. In the following examples, “%” indicates “% by weight” unless otherwise specified, and numerical values in the composition table also indicate “% by weight”.

The method of producing each composition is not particularly limited. For example, the desired composition is obtained by kneading and kneading other components in order with the hydrophobic ointment base component of the compounding component. Was. First, the present inventors conducted the following tests in the process of examining an oral composition containing light anhydrous silicic acid.

Comparison of the present invention with the prior art [Examples 1 and Comparative Examples] Preparations having the compositions shown in Table 1 were prepared and used as Examples 1 and Comparative Examples.

[0023]

Table 1 ──────────────────────────────────── Ingredients (ointment base) Comparative Example ヒ ド ロ Hydrocortisone acetate 0.5 0.5 Chlorhexidine hydrochloride 0. 2 0.2 Lidocaine hydrochloride 0.5 0.5 Sodium carboxymethylcellulose 25 25 Citric acid 11 Light silicic anhydride ^{* 1} 3- Plastibase ^{* 2} qs qq計 Total (%) 100 100 ────────────────────── * * 1: Aerosil 200 (average particle size about 12nm, manufactured by Nippon Aerosil Co., Ltd.) * 2: Liquid paraffin with 4% polyethylene resin dispersed (Pristol Myers Squif Co., Ltd.)

Next, in order to examine the mucoadhesiveness of the oral composition of the present invention, the preparations of Example 1 and Comparative Example were subjected to a mucoadhesive test. [Method of mucoadhesion test] The test method was an acrylic cylinder (upper part of 3 cm in diameter) equipped with freeze-dried pork skin [Aloask D: manufactured by Taiho Pharmaceutical Co., Ltd.] moistened with physiological saline and excess water was removed with filter paper. 100 μl of physiological saline solution only on the lower part of a cylinder, a lower cylinder having a diameter of 4 cm, and a silicone sponge sheet having a thickness of 5 mm attached to the surface of each acrylic cylinder.
Was instilled into the mouth. Approximately 0.1 g of a sample is weighed on the upper part of the acrylic cylinder, and one saline solution is placed on the lower part.
After dropping 00 μl, immediately put the upper and lower acrylic cylinders into 300
g and left for 5 minutes. After this, the upper and lower acrylic cylinders are separated at a constant speed (20 mm / min),
The maximum tensile stress was determined from the peak of the stress versus time curve at this time, and this was regarded as the mucoadhesive force. Thereby, the mucosal adhesion of the preparation was evaluated.

The test results are shown in FIG. As can be seen from the results, the oral composition of the present invention (Example 1) was compared with a conventional preparation of a type in which a water-soluble polymer was blended with a hydrophobic ointment base having excellent tackiness (Comparative Example). However, even better mucosal adhesion was observed.

Next, in order to examine the local retentivity of the oral composition of the present invention, the retentivity of the preparations of Example 1 and Comparative Example was evaluated. <Method of Retentivity Test> The test method is as follows. A freeze-dried pork skin (Aloask D) is mounted on a polypropylene disk with the skin side facing up, and at a fixed distance (2 cm) from the center of the rotating shaft.
Approximately 100 mg of sample is applied evenly within a 15 mmφ circle,
The sample was rotated at 100 rpm in 1000 ml of physiological saline at 37 ° C., and it was determined with time (measured from 30 minutes to 12 hours) whether or not the sample had disappeared from the circular frame. In this way, the local retention of the oral composition was evaluated, and the results are shown in Table 2. The evaluation criteria for retention are as follows. [Evaluation criteria for retention] ○ The sample stayed in the circle △ The sample partially stayed in the circle × The sample completely disappeared from the circle

[0027]

[Table 2] ──────────────────────────────────── 30 minutes 1 hour 2 hours 3 hours 6 hours 12 hours ──────────────────────────────────── Example 1 ○ ○ ○ ○ ○ ○ Comparative example △ × − − − − ────────────────────────────────────

As can be seen from the results in Table 2, the composition for the oral cavity of the present invention (Example 1) was compared with a preparation of a type in which a water-soluble polymer was added to a conventional hydrophobic ointment base (Comparative Example). Excellent local retention was observed.

Formulation of Light Silicic Anhydride [Test Examples 1 to 6] Test Example 1 was used in Example 1, and Formulations in which other powders were mixed in place of the light silica used in Example 1 were used in Test Example 2. As No.-6, a mucoadhesion test and a retention test were performed. The mucoadhesion test and the retention test were performed in accordance with Example 1 and Comparative Example. Table 3 shows the results.

Next, evaluation criteria for mucoadhesive force and retention are shown. [Evaluation Criteria for Mucoadhesion] ◎ The mucoadhesion is 600 g or more. -Mucoadhesive force is 450g-600g. △ Mucoadhesion is 300 g to 450 g. X Mucoadhesive force is 300 g or less. [Evaluation Criteria for Retention] ◎ The sample remained in the circle for 12 hours or more ○ The sample disappeared leaving a part of the circle in 6 to 12 hours, and the sample was in the circle in 1 hour to 6 hours. × completely disappeared from within × 1 hour, the sample completely disappeared from within the circle

[0031]

[Table 3] ──────────────────────────────────── Ingredients (ointment base) Test example No. 1 2 3 4 5 6 ヒ ド ロ Hydrocortisone acetate 0.5 0.5 0.5 0.5 0.5 0.5 Chlorhexidine hydrochloride 0.2 0.2 0.2 0.2 0.2 0.2 Lidocaine hydrochloride 0.5 0.5 0.5 0.5 0.5 0.5 Sodium carboxymethyl cellulose 25 25 25 25 25 25 25 Citric acid 1 1 1 1 1 1 Light anhydrous silicic acid ^{* 1} 3 Synthetic aluminum silicate 3 Silicic acid Magnesium aluminate 3 Calcium carbonate 3 Aluminum hydroxide 3 Magnesium stearate 3 Plastibase ^{* 2} Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Total (%) 100 100 100 100 100 100 ────────────────粘膜 Mucoadhesion ◎ × × × × × Retention ◎ ◎ ◎ ◎ ◎ ◎

From the results shown in Table 3, it can be seen that the preparation containing Light Silicic Anhydride (Test Example 1) has good mucosal adhesion and retention. On the other hand, in the preparations using powders other than light anhydrous silicic acid (Test Examples 2 to 6), it can be seen that the retentivity is obtained but the adhesion to the mucous membrane is significantly inhibited.

Average particle size of light anhydrous silicic acid [Test Examples 7 to 10] Compounds obtained by changing the average particle size of light anhydrous silicic acid of Example 1 to 0.007 to 10 μm are referred to as Test Examples 7 to 10, Table 4 shows the evaluation of the retention.
In addition, the method of the retention test was as described in Example 1 and Comparative Example.
In addition, the evaluation criteria of the retention were performed according to Test Examples 1 to 6.

[0034]

[Table 4] 配合 Ingredients (ointment base) Test example Number 7 8 9 10 ヒ ド ロ Hydrocortisone acetate 0.5 0.5 0.5 0.5 Chlorhexidine hydrochloride 0.2 0.2 0.2 0.2 Lidocaine hydrochloride 0.5 0.5 0.5 0.5 Sodium carboxymethyl cellulose 25 25 25 25 Citric acid 11 1 1 Light anhydrous silicate average particle size 0.007 ^* 3 3 average particle size 0.03 .mu.m ^* 4 3 average particle size 2 [mu] m ^* 5 3 average particle diameter 10 [mu] m ^* 6 3 plastibase ^{* 2} qs qs qs qs Total (%) 100 100 100 100 ──────────────────────────────────── Detention ◎ ◎ △ × ──────────────────────────────────── * 3: Aerosil 300CF (Average particle size 7nm * 4: Aerosil 50 (average particle diameter 30 nm, manufactured by Nippon Aerosil Co., Ltd.) * 5: Silophyur 25 (average particle diameter 2 μm, manufactured by Fujitaison Chemical Co., Ltd.) * 6: SiloFur 30-S (Average particle size 10μm, manufactured by Fujita Wison Chemical Co., Ltd.)

From the results shown in Table 4, the average particle size was 0.1 μm.
Preparations containing the following light anhydrous silicic acid (Test Examples 7 and 8)
It can be seen that is excellent in retention. On the contrary,
It can be seen that the formulations containing light anhydrous silicic acid having an average particle size of more than 0.1 μm (Test Examples 9 and 10) have significantly reduced retention.

Blended amount of light silicic anhydride [Test Examples 11 to 16] The blended amount of light silicic anhydride of Example 1 was changed from 0 to 15% to Test Examples 11 to 16, respectively.
Table 5 shows the evaluation of the retention and useability. In addition, the test method of the retention property is as described in Example 1 and Comparative Example.
Moreover, the evaluation criteria of the retention property were performed according to Test Examples 1 to 6.

<Method of Usability Test> A method of examining the usability of each preparation of the test examples was performed as follows. Test Examples 11 to 1 previously prepared after washing the oral cavity by gargle with a group of 8 healthy normal adult male and female subjects
The formulation of No. 6 was applied to the buccal cavity of the subject. During the test,
The subject was prohibited from eating and drinking, and after 30 minutes, the subject was evaluated for usability in four steps. The evaluation criteria for usability are shown below. [Evaluation Criteria for Usability] ◎ No discomfort with the formulation ○ Slightly uncomfortable with the formulation △ Discomfort with the formulation × Notable discomfort with the formulation

[0038]

[Table 5] 配合 Ingredients (ointment base) Test Example No. 11 12 13 14 15 16 ヒ ド ロ Hydrocortisone acetate 0.5 0.5 0.5 0.5 0.5 0.5 Chlorhexidine hydrochloride 0.2 0.2 0.2 0.2 0.2 0.2 Lidocaine hydrochloride 0.5 0.5 0.5 0.5 0.5 0.5 Sodium carboxymethyl cellulose 25 25 25 25 25 25 25 Citric acid 1 1 1 1 1 1 Light anhydrous silicic acid ^{* 1} 0 0.5 1 5 10 15 Plastic base ^{* 2} qs q q q q q q q q qs (%) 100 100 100 100 100 100 ───────────────────────────────── ─── Retention × × ◎ ◎ ◎ ◎ Usability ◎ ◎ ◎ ◎ ◎ × ───────────────────────────── ──── ──

From the results shown in Table 5, it can be seen that the preparations containing 1 to 10% by weight of light silicic anhydride (Test Examples 13 to 15) have good usability and retention. On the other hand, in the preparations containing less than 1% of light anhydrous silicic acid (Test Examples 11 and 12), the retention was poor, and in the preparations exceeding 10% (Test Example 16), the usability was significantly deteriorated. I understand.

Blending ratio of light anhydrous silicic acid to water-soluble polymer [Test Examples 17 to 22] The light anhydrous silicic acid of Example 1 (LA
SA) and the water-soluble polymer (WBP) in a compounding ratio of about 3: 1
Table 6 shows the evaluations of the retentivity and the usability as Test Examples 17 to 22 in which the ratio was set to １ ： 1: 37. In addition, the method of the retentivity test was performed in Example 1 and Comparative Example, and the evaluation criteria were in accordance with Test Examples 1 to 6. In addition, the usability test method and its evaluation criteria were determined in Test Examples 11 to 16.
It went according to.

[0041]

[Table 6] 配合 Ingredients (ointment base) Test example No. 17 18 19 20 21 22 ヒ ド ロ Hydrocortisone acetate 0.5 0.5 0.5 0.5 0.5 0.5 chlorhexidine hydrochloride 0.2 0.2 0.2 0.2 0.2 0.2 lidocaine hydrochloride 0.5 0.5 0.5 0.5 0.5 0.5 carboxymethyl cellulose sodium 4.0 5.0 7.5 28 29 18.5 citric acid 1 1 1 1 1 1 light anhydrous silicic acid ^{* 1} 12 10 7.5 1.4 1.0 0.5 plastibase ^{* 2} qs qq qq qq qq qs Total (%) 100 100 100 100 100 100 ───────────────────────────────── ─── Compounding ratio (LASA: WBP) 3: 1 2: 1 1: 1 1:20 1:29 1:37 ───────────────────── ────────────── Retention ◎ ◎ ◎ ◎ ○ × Usability × ◎ ◎ ◎ ◎ ◎ ◎ ──────────────────────────────── ────

From the results in Table 6, it can be seen that the formulation ratio of light silicic anhydride to water-soluble polymer was 2: 1 to 1:30 (Test Example 1).
8 to 21) are preferable from the viewpoint of both the retention property and the usability. On the other hand, if the compounding ratio of light anhydrous silicic acid to the water-soluble polymer is more than 2: 1 and the amount of light anhydrous silicic acid is too large, the usability is remarkably reduced. It is understood that if the content is too small, sufficient retentivity cannot be obtained.

Next, further examples will be shown in order to make the oral composition of the present invention more specific. Of course, they do not limit the invention in any way. And these manufacturing methods are based on Example 1.

Example 2 (Ointment formulation) (Prescription) Compounding amount (%) (1) Triamcinolone acetonide 1 (2) Cetylpyridinium chloride 0.1 (3) Diphenhydramine hydrochloride 0.5 (4) Sodium carboxymethyl cellulose 15 ( 5) Sodium alginate 3 (6) Hydroxypropylcellulose 5 (7) Tartaric acid 0.5 (8) Light anhydrous silicic acid ^{* 7} 2 (9) Plastibase ^{* 2} qs 100 * 7: Aerosil 200V (average particle diameter about 12 nm, Manufactured by Nippon Aerosil Co., Ltd.)

Example 3 (Ointment preparation) (Prescription) Compounding amount (%) (1) Dexamethasone acetate 0.25 (2) Benzalkonium chloride 1.5 (3) Sodium carboxymethylcellulose 22 (4) Adipic acid 0 (5) Light anhydrous silicic acid ^{* 3} 5 (6) White petrolatum 8 (7) Plastic base ^{* 2} qs 100%

Example 4 (Ointment formulation) (Formulation) Compounding amount (%) (1) Prednisolone acetate 0.5 (2) Dibucaine hydrochloride 0.3 (3) Benzethonium chloride 0.2 (4) Sodium carboxymethyl cellulose 30 ( 5) Sodium alginate 6 (6) Sodium hyaluronate 5 (7) Citric acid 0.8 (8) Light anhydrous silicic acid ^* 84 (9) Plastic base ^{* 2} qs 100% * 8: Aerosil 300 (average particle size approx. 7 nm, manufactured by Nippon Aerosil Co., Ltd.)

Example 5 (Ointment preparation) (Prescription) Compounding amount (%) (1) Hydrocortisone acetate 1 (2) Cetylpyridinium chloride 0.5 (3) Sodium carboxymethylcellulose 17.5 (4) Sodium alginate 2.5 (5) Agar 3 (6) Tartaric acid 0.2 (7) Light anhydrous silicic acid ^* 15 (8) Plastibase ^{* 2} qs 100%

[0048]

EFFECTS OF THE INVENTION The oral composition of the present invention has better mucosal adhesion to the oral mucosa than conventional preparations, and has particularly high local retention. From this, sufficient sustained pharmacological action in the oral cavity can be obtained, and an excellent therapeutic effect on oral diseases can be expected.

[Brief description of the drawings]

FIG. 1 shows the mucoadhesive force of the oral compositions obtained in Example 1 and Comparative Example.

Claims (6)

[Claims] 1. An oral composition comprising a hydrophobic ointment base, a water-soluble polymer, a drug and light anhydrous silicic acid. 2. The composition for oral cavity according to claim 1, further comprising sodium carboxymethylcellulose as a water-soluble polymer. 3. The composition according to claim 2, further comprising one or more selected from the group consisting of sodium alginate, hydroxypropylcellulose, agar, and sodium hyaluronate as the water-soluble polymer. Composition. 4. The composition for oral cavity according to claim 1, wherein the light anhydrous silicic acid has an average particle size of 0.1 μm or less. 5. The composition for oral cavity according to claim 1, wherein the amount of light anhydrous silicic acid is 1 to 10% by weight. 6. The composition for oral cavity according to claim 1, wherein the mixing ratio of light anhydrous silicic acid to the water-soluble polymer is 2: 1 to 1:30. Composition.