JPH10298073A - Therapeutic agent for inflammatory stomatopathy - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a safe therapeutic agent for inflammatory stomatopathy having high effects. SOLUTION: This therapeutic agent for inflammatory stomatopathy has >10 wt.% and <95 wt.% of vitamin E and >5 wt.% and <95 wt.% of squalane.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an agent for treating inflammatory oral disease.

[0002]

2. Description of the Related Art Conventionally, steroids (for example, dexamethasone) and azulene have been used for treating inflammatory oral diseases. However, steroids have problems such as local pigmentation, increased susceptibility to infection, and the occurrence of systemic side effects. In addition, azulene does not have a strong effect. Therefore, for oral diseases with inflammation,
There is a need for safe and effective therapeutic agents.

An oral composition containing vitamin E, vitamin C, lysozyme chloride and lecithin has been disclosed (JP-A-62-273910).
Since the content of vitamin E is 10% or less, it is difficult to expect a strong inflammation-suppressing action, and there is a concern that irritation by vitamin C and sensitization by lysozyme chloride may occur.

[0004]

The object of the present invention is to solve the above-mentioned problems, and an object of the present invention is to provide a safe and highly effective agent for treating inflammatory oral diseases.

[0005]

Means for Solving the Problems The agent for treating inflammatory oral diseases of the present invention is characterized by containing vitamin E and squalane.

[0006] The above-mentioned vitamin E refers to tocopherol (vitamin E) and derivatives thereof. Examples of those listed in the Japanese Pharmacopoeia include tocopherol acetate (vitamin E acetate), tocopherol succinate (vitamin E succinate). Acid ester). Those not listed in the Japanese Pharmacopoeia include, for example, α-tocopherol, β-tocopherol, γ-tocopherol, δ-
Tocopherol, tocopherol nicotinate (vitamin E nicotinic acid ester), tocopherol phosphate (vitamin E phosphate), natural vitamin E, and the like, but are not limited thereto, and monosaccharides and oligosaccharides of tocopherol Or, a conjugate with a polysaccharide or water-soluble vitamin E is also included. It is generally known that vitamin E has no side effects due to excessive intake and is extremely safe.

[0007] The above-mentioned squalane refers to fish in the deep sea, especially in shark liver oil or vegetable oil such as olive oil,
It is a saturated hydrocarbon obtained by reducing squalene which is an unsaturated hydrocarbon present in rice bran oil, wheat germ oil, sesame oil, cottonseed oil and the like. Further, a synthetic squalane obtained by using geranylacetone and an acetylene compound as raw materials is also included. In addition, squalane is contained in a large amount in foods as described above, and is also recognized as a pharmaceutical additive. Therefore, its safety is extremely high.

When the content of vitamin E in the therapeutic agent for inflammatory oral diseases of the present invention is reduced, the effect of suppressing inflammation is not sufficient, and even when it is increased, the effect of suppressing inflammation is significantly increased according to the content. Therefore, the content is preferably more than 10% by weight and less than 95% by weight, more preferably 20 to 50% by weight.

When the content of squalane in the agent for treating inflammatory oral diseases of the present invention is reduced, the effect of suppressing inflammation becomes insufficient, and even if it is increased, the effect of suppressing inflammation becomes significantly higher according to the content. Therefore, it is preferably more than 5% by weight and less than 90% by weight, more preferably 10 to 50% by weight.

The dosage form of the therapeutic agent for inflammatory oral disease according to claims 1 and 2 of the present invention is not particularly limited. For example, the above-mentioned drug is dissolved or mixed and dispersed in a base, Examples include pastes, creams, jellies, gels, emulsions, tablets, troches, chewing gums and the like.

As the base, any pharmaceutically acceptable base may be used, and any bases such as liquids and ointments which are conventionally known can be used. Examples thereof include sodium alginate, gelatin, corn starch, tragacanth gum and the like. , Methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, dextrin, xanthan gum, carrageenan, mannan, agarose, polyvinyl alcohol, sodium polyacrylate, methoxyethylene-maleic anhydride copolymer, polyvinyl ether,
Polymers such as polyvinylpyrrolidone; beeswax, olive oil, cacao oil, sesame oil, soybean oil, camellia oil, peanut oil, beef oil, pork oil, chicken oil, lanolin, and other oils; white petrolatum, yellow petrolatum; paraffin; Hydrogen (eg, Plastibase, manufactured by Bristol-Myers Squibb); higher fatty acids such as stearic acid; higher alcohols such as cetyl alcohol, octyldodecanol, stearyl alcohol; polyethylene glycol (eg, Macrogol 400, Macrogol 4000)
Glycerin monostearate; polyoxyethylene cetyl ether; self-emulsifying propylene glycol monostearate; triethanolamine; monooleic acid ester; glyceride stearate; water, physiological saline, phosphate buffer and the like. However, the present invention is not limited to these.

The base is preferably a lipophilic substance having good compatibility with vitamin E and squalane, and examples thereof include gelled hydrocarbon and white petrolatum.

Further, if necessary, polysorbate 8
0, surfactants such as polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, and lecithin; solubilizers such as polyvinylpyrrolidone; inorganic fillers such as kaolin, bentonite, zinc oxide, and titanium oxide; methyl paraoxybenzoate; Stabilizers such as propyl paraoxybenzoate;
Antioxidants; pH regulators; Preservatives such as benzalkonium chloride, benzethonium chloride, citric acid and its sodium salt, paraoxybenzoic acids, boric acid, borax, camphor; xanthan gum, sodium chondroitin sulfate;
Viscosity agents such as liquid paraffin, glycerin, macrogol, and polyvinylpyrrolidone; thickeners; and the like may be added.

The amount of the agent for treating inflammatory oral disease of the present invention may be 1 to 4 times a day, 50 to 50 for a liquid per time.
0 μl, 50-500 mg for ointment.

The diseases to be treated by the agent for treating inflammatory oral diseases of the present invention include, for example, tonsillitis, stomatitis, intractable stomatitis with erosion and ulcer, inflammation of the wound site including the tooth extraction layer, glossitis, Examples include, but are not limited to, marginal periodontitis, acute gingivitis, alveolar pyorrhea, and the like.

[0016]

DESCRIPTION OF THE PREFERRED EMBODIMENTS Examples of the present invention and comparative examples will be described. (Examples 1 to 3 and Comparative Examples 1 and 2) Tocopherol acetate (manufactured by BASF), squalane (manufactured by Maruha), and gelled hydrocarbon (manufactured by Bristol-Myers Squibb) shown in Table 1 ) Was supplied to a mortar and kneaded until the whole became uniform to obtain an ointment.

Action on Experimental Stomatitis The ointment obtained above was evaluated for Yoshikawa (Japanese Society of Cosmetic Engineers, Vol. 12, No. 2, pp. 44-50, 1978).
) Was evaluated for the efficacy of experimental stomatitis. That is, a golden hamster (male, weight 70
-100 g), pentobarbital sodium (manufactured by Abbott Laboratories) was intraperitoneally administered, and a small amount of absorbent cotton was inserted into the cheek pouch under general anesthesia. Immediately 1m of 10% sodium lauryl sulfate (Wako Pure Chemical Industries) aqueous solution
was poured into the above absorbent cotton and allowed to contact for 30 minutes. Then, the absorbent cotton was taken out, and the site of the cheek pouch contacted with sodium lauryl sulfate was washed with 25 ml of distilled water.

Next, the ointment obtained in the above Examples and Comparative Examples, or an ointment base (gelled hydrocarbon) as a control substance
Was applied to the above sodium lauryl sulfate contact site and left for 24 hours. After the test animal was over-anaesthetized and killed with diethyl ether, the buccal pouch mucosa tissue was excised, a tissue section was prepared according to a conventional method, stained with hematoxylin-eosin, and observed with a microscope. Tissue findings were determined according to the following criteria (score). Table 1 shows the results. Normal 0 Stratum corneum swelling, vasodilation, partial epidermal hyperplasia 1 Epidermal hyperplasia, strong cell infiltration 2

The above-mentioned evaluation of the efficacy was carried out for each ointment and ointment base (control substance) for 5 golden hamsters. In the evaluation result column of Table 1, the number of cases corresponding to each score / 5 is shown.

[0020]

[Table 1]

From the results shown in Table 1, it was confirmed that the therapeutic agent for inflammatory oral diseases of the present invention has a remarkable inhibitory effect on stomatitis as compared with the preparation of vitamin E or squalane alone. It turns out that it is an effective preparation for diseases.

[0022]

The composition of the agent for treating inflammatory oral diseases according to claim 1 is as described above, and the effect of vitamin E and squalane exerts an effect of remarkably suppressing inflammation in the oral cavity. .

The composition of the therapeutic agent for inflammatory oral diseases according to claim 2 is as described above, and contains vitamin E and squalane in a specific range, so that it has a stronger effect of suppressing inflammation in the oral cavity. Demonstrate.

Therefore, the present invention can provide an agent for treating inflammatory oral diseases having a high clinical effect.

Claims (2)

[Claims] 1. An agent for treating inflammatory oral diseases, which comprises vitamin E and squalane. 2. The inflammatory composition according to claim 1, wherein the content of vitamin E is more than 10% by weight and less than 95% by weight, and the content of squalane is more than 5% by weight and less than 90% by weight. Agent for treating oral diseases.