KR20010096065A - Oral composition containing minocycline HCL - Google Patents

Abstract

PURPOSE: An oral composition containing minocycline HCL capable of expressing a sustained antibacterial activity and having an excellent efficacy and practical effect on oral diseases as a core component is provided, which can prevent and treat periodontitis. CONSTITUTION: This oral composition comprises 0.0001 to 0.01% by weight of minocycline HCL, 0.1 to 20% by weight of a flavonoid component, 0.01 to 5% by weight of a titrated extract of Centella asiatica, 10 to 30% by weight of an abrasive, 20 to 60% by weight of water, 1 to 10% by weight of a swelling agent, 2 to 10% by weight of a binding agent, 5 to 10% by weight of a preserving agent, 0.1 to 5% by weight of perfume and 2 to 10% by weight of a surfactant.

Description

Oral composition for preventing and treating periodontitis containing minocycline HCL {Oral composition containing minocycline HCL}

The present invention relates to an oral composition, and more particularly, by using a minocycline HCL as a key component that is susceptible to periodontitis-related bacteria and can be adsorbed to calcium on the tooth surface and exhibit a continuous antimicrobial action, gum disease It relates to an oral composition that can effectively prevent and treat.

The main cause of oral disease is dental plaque (also called plaque). Among them, acid produced as a by-product is produced by the growth of bacteria such as Streptococcus mutans and Lactobacillus attached to dental plaque. It is known to cause tooth decay by corroding it.

In addition, long-term without removing the bacteriostatic bacterium, it is combined with the components of calcium, magnesium and phosphorus in the saliva of the oral cavity to form sparingly soluble salts, thereby forming tartar having a hardness similar to that of teeth. As it progresses, it penetrates the interface between the gum and teeth, causing bleeding easily when brushing teeth, and also causing inflammation of the oral bacteria to cause gingivitis and periodontal disease. Inflammation of gingivitis may include redness of the gingival redness, swelling, and bleeding. If the gingivitis progresses, it may cause periodontal disease.

The most important part for the prevention of gingivitis or periodontitis is to individually remove calculus through oral hygiene to reduce the infectious diseases caused by microorganisms, and even if gingivitis or periodontitis occurs, it is treated with antimicrobial agents.

Several antimicrobials have been developed to treat gingivitis and periodontitis, but few of them can control tartar. Potential drugs include plant extracts, metal salts, phenols and bisbiguanides (Lander, PE Newcomb, GM, Seymour, GJ, Powell, RN (1986) The antimacrobial and clinlical effects of a single subgingival irrigation of chlorohexidine in advanced periodontal lesions, J. clin.periodontal. 13: 74-80)

In an effort to prevent periodontal disease, chlorohexidine gluconate, cetylpyridium chloride, sanguinarine, and triclosan can kill periodontal disease bacteria in a short time. ) Has been developed and applied to oral products such as toothpaste and toothpaste, but the occurrence of gingivitis is not yet prevented fundamentally.

U.S. Patent No. 52,308,895 has suggested that a periodontal disease can be treated by developing a system in which a drug containing tetracycline is continuously delivered to inhibit the enzyme activity of collagenase, which breaks down periodontal tissue.

EP-A 528468 A1 suggests that toothpaste and oral cleaning agents containing Triclosan can be developed to inhibit periodontal disease by inhibiting the production of prostaglandins, which are gingival inflammation-causing agents.

Fresh guinea extract (see US Patent No. 4,689,216), sage and unflavored extract (see Japanese Patent No. 58-134013), toothpaste composition containing bamboo salt (Korean Patent Publication No. 94-64) and the like, extracts of medicinal plants have been used. Herbal medicines, which are extracts of plants than other drugs, are considered to be excellent substances that can minimize various side effects caused by the use of chemicals, such as tooth discoloration, irritation and prolonged use. Symptoms of periodontal disease such as or edema have been reported (Yankell, LL, Dolan, MM, Emling, RC (1988) Efficacy of therapeutic agent against gingivitis and periodontal disease.J. Antibact.Antifung.Angsts 11: 451 -61).

However, toothpaste compositions containing such natural extracts are not good in terms of compatibility with other components have a severe limitation in the content and has a disadvantage in that the process for removing a specific smell is complicated.

The present invention has been made to solve the conventional problems as described above, the object of the present invention is the susceptibility of periodontitis associated bacteria and adsorption to calcium of the tooth surface can exhibit a continuous antibacterial action and to prevent periodontitis compared to other antibiotics and It is to prepare oral compositions that can prevent and treat periodontitis using Minocycline HCL, an antibiotic that has superior efficacy and effectiveness in treatment.

In order to achieve the above object, the present invention,

Minocycline HCL 0.0001 ~ 0.01% by weight, flavonoid component 0.1-20% by weight, Centala asiatica quantitative extract component 0.01-5% by weight, abrasive 10-30% by weight, water 20-60% by weight, wetting agent 1- Provided is an oral composition for preventing and treating periodontitis, comprising 10 wt%, 2-10 wt% binder, 5-10 wt% preservative, 0.1-5 wt% fragrance, and 2-10 wt% surfactant. .

As mentioned above, according to the present invention, since the sensitivity of periodontitis-related bacteria is large and adsorbed on the calcium of the tooth surface, it is used for the prevention and treatment of periodontitis by using Minocycline HCL, which can exhibit a continuous antibacterial action, as a key ingredient. To prepare oral compositions having superior efficacy and efficacy.

Hereinafter, the oral composition for preventing and treating periodontitis according to the present invention will be described in detail.

Since ancient times, teeth have been counted as one of the five folds, and as important as the teeth are the gums that surround and support the teeth. Among gum diseases, periodontitis is an infectious disease caused by anaerobic bacteria present in plaque or periodontal sac, so removal of these bacteria is the basis of prevention and treatment of periodontitis.

Minocycline HCL is a semi-synthetic tetracycline antibiotic, especially because it is susceptible to periodontitis-related bacteria and is adsorbed by calcium on the surface of the tooth, and can exhibit continuous antimicrobial activity and activity of the enzyme collagenase involved in the formation of periodontal pocket It is an antibiotic that has superior efficacy and effectiveness in preventing and treating periodontitis compared to other antibiotics.

In addition, Bacteroides gingivalis, Bacteroides intermedius, Bacteroided melaninogenicus, Eikenellacorrodens, Fusobacterium nucleatrm, Capnocytophaga spp, and Haemophilus actinomycetemcomitans, which are susceptible to Minocycline HCL, have been shown to exhibit excellent efficacy of ameliorating the following diseases.

Therefore, the present invention uses oral minocycline (Minocycline) HCL having such an effect to make a composition for oral cavity that can prevent and treat gingivitis, periodontitis, wherein the composition for oral cavity is Minocycline HCL component 0.0001 ~ 0.01 weight %, Flavonoid component 0.1-20 wt%, abrasive 10-30 wt%, water 20-60 wt%, wetting agent 1-10 wt%, binder 2-10 wt%, preservative 5-10 wt%, perfume 0.1-5 It contains weight%, 0.1-2 weight% of dyes, and 2-10 weight% of surfactant.

The composition for oral cavity according to the present invention contains a substance selected from precipitated silica, precipitated calcium carbonate, calcium phosphate, sodium hydrogen carbonate and the like as an abrasive component.

In addition, the composition for oral cavity according to the present invention contains a substance selected from crystalline silica, xanthan gum or carboxymethyl cellulose as a binder component.

In addition, the composition for oral cavity according to the present invention contains a substance selected from sodium benzoate, methyl paraben or propyl paraben as a preservative component.

In addition, the composition according to the present invention contains a substance selected from menthol, peppermint, spearmint, fresh mint, or a combination thereof as the perfume component.

Wetting agents used in the present invention should be compatible with other agents and have no peculiar irritating odor, using propylene glycol, glycerin, sorbitol, polyethylene glycol, polypropylene glycol, mannitol, xyitol or combinations thereof do.

In addition, the composition according to the present invention is an alpha-olefin sulfonate (α-OLEFFIN SULFONATE), sodium dodecyl sulfate (SODIUM DODECYL SULFATE), sodium dodecyl benzene sulfonate (SODIUM DODECYL BENZENE SULFONATE), polyoxyethylene alkyl POLYOXYETHYLENE ALKYL ARYL ETHER, SECONDARY-ALCOHOL ETHOXYLATE having 11-13 carbon atoms and 5-20 moles of EO, 1 having 8-20 carbon atoms and 8-20 moles of EO PRIMARY-ALCOHOL ETHOXYLATE, POLYOXYETHYLENE ALKYL ARYL ETHER, wherein the ALKYL group represents a straight chain having 8-12 carbon atoms, and the ARYL group is aromatic having 6-12 carbon atoms Group), sodium dioctyl sulfosuccinate (trade name AEROSOL OT or CR-DOC70), twins (TWEEN), sorbitan mono oleate (SORBITAN MONO OLEATE (SPAN 80)), sorbitan mono la Rate (SORBITAN MONO LAURATE (SPAN 20)), glycerol monooleate (GLYCERIN MONO OLEATE (GMO)), was used alone or in combination with glycerol monolaurate (GLYCERIN MONO LAURATE (GML)) and the like.

The following briefly describes the composition of the embodiments according to the present invention.

<Example 1>

Minocycline HCL 0.0001 ~ 0.01g

10-20 g of precipitated silica

Sorbitol 1-10g

Saccharin Sodium 1-10g

Sodium benzoate 5-10g

1 to 5 g of pigment

0.1-5g fragrance

Xanthan gum 0.5-3g

1-5 g of sorbitan mono oleate

1 to 5 g glycerin monolaurate

1 to 3 g of propylene glycol

Water quantity

100 g in total

By the composition as in Example 1 can be made for preventing gum disease and tooth whitening composition.

<Example 2>

Minocycline HCL 0.0001 ~ 0.01g

Precipitated Calcium Carbonate 10-20g

Centala asiatica fixed extract 5-100mg

Xyitol 1-10 g

Saccharin Sodium 1-10g

Sodium benzoate 5-10g

1 to 5 g of pigment

0.1-5g fragrance

Xanthan gum 0.5-3g

Sodium Dodecyl Sulfate 1-5g

1 to 5 g glycerin monolaurate

Glycerin 1-3g

Water quantity

100 g in total

A composition for treating tooth whitening and gum disease can be made with the same composition as in Example 2.

<Example 3>

Minocycline HCL 0.0001 ~ 0.01g

Precipitated Calcium Carbonate 10-15g

Flavonoids 0.1-10g

Xyitol 1-10 g

Saccharin Sodium 1-10g

Propyl paraben 5-10 g

1 to 5 g of pigment

0.1-5g fragrance

Carboxymethyl Cellulose 0.5 ~ 3g

Sodium Dodecyl Sulfate 1-5g

1 to 5 g glycerin monolaurate

Glycerin 1-3g

Water quantity

100 g in total

The composition for oral cavity of gum disease, tooth whitening and bad breath removal effect can be made with the same composition as in Example 3.

As mentioned above, the composition for oral cavity according to the present invention, by containing Minocycline HCL 0.0001 ~ 0.01g, is effective in periodontal diseases such as gingivitis, periodontitis, as well as reducing the inflammation of the gums It strengthens the gums, giving it the ability to resist bacterial infections. In addition, it contains the plant extracts flavonoids and panesol to remove the bad smell in the mouth and to remove the bad smell, and to provide the effect of treating the wound in the mouth by containing the quanta extract of Centala asiatica, It is prepared by mixing excipients such as abrasives, wetting agents, sweeteners, binders, diluents, preservatives, flavoring agents, pigments, surfactants, water and the like.

Therefore, when brushing teeth using the oral composition according to the present invention, unlike the existing composition for oral gum disease, tooth whitening effect and tartar removal, bad breath removal, periodontitis prevention and treatment, weak gum health Can be obtained simultaneously.

Although described above with reference to a preferred embodiment of the present invention, those skilled in the art will be variously modified and changed within the scope of the invention without departing from the spirit and scope of the invention described in the claims below. I can understand that you can.

Claims (3)

Minocycline HCL 0.0001 ~ 0.01% by weight, flavonoid component 0.1-20% by weight, Centala asiatica quantitative extract component 0.01-5% by weight, abrasive 10-30% by weight, water 20-60% by weight, wetting agent 1- An oral composition for preventing and treating periodontitis, which comprises 10% by weight, 2-10% by weight of binder, 5-10% by weight of preservative, 0.1-5% by weight of perfume, and 2-10% by weight of surfactant. The method of claim 1, wherein the abrasive is a substance selected from the group consisting of precipitated silica, precipitated calcium carbonate, calcium phosphate and sodium bicarbonate, and the wetting agent is propylene glycol, glycerin, sorbitol, polyethylene glycol, polypropylene glycol, mannitol Oral composition for preventing and treating periodontitis, characterized in that the material is selected from the group consisting of xyitol and combinations thereof, the binder is selected from the group consisting of precipitated silica, xanthan gum and carboxy methyl cellulose. The method of claim 1, wherein the preservative is a material selected from the group consisting of sodium benzoate, methyl paraben and propyl paraben, the fragrance is a material selected from the group consisting of menthol, peppermint, spearmint, freshmint and combinations thereof Surfactants include alpha-olefin sulfonate, sodium dodecyl sulphate, sodium dodecyl benzene sulfonate, polyoxyethylene alkyl aryl ether, polyoxyethylene alkyl aryl ether Secondary-alcohol ethoxylates having 11 to 13 carbon atoms and 5 to 20 moles of EO, primary alcohols having 8 to 14 moles of carbon atoms and 8 to 20 moles of EO (PRIMARY) -ALCOHOL ETHOXYLATE), POLYOXYETHYLENE ALKYL ARYL ETHER (where the ALKYL group represents a straight chain having 8-12 carbon atoms) ARYL group represents an aromatic group having 6 to 12 carbon atoms, SODIUM DIOCTYL SULFOSUCCINATE (trade name AEROSOL OT or CR-DOC70), TWEEN, sorbitan monooleate (SORBITAN MONO) OLEATE (SPAN 80)), SORBITAN MONO LAURATE (SPAN 20), GLYCERIN MONO OLEATE (GMO), GLYCERIN MONO LAURATE (GML) and their Oral composition for preventing and treating periodontitis, characterized in that the material selected from the group consisting of a combination.