JPS63267714A - Drug for dental oral cavity - Google Patents

Abstract

PURPOSE:To obtain a drug the for dental oral cavity, containing an extract of Krameria trianara Ruiz et Pavon as a principal ingredient, capable of exhibiting excellent antimicrobial activity against periodontal pathogenic germs and high safety and useful for preventing and treating periodontosis. CONSTITUTION:A drug for the dental oral cavity, obtained by blending an extract of Krameria trianara Ruiz et Pavon which is the name of the original crude drug of the family (Leguminosae-Caesalpinioideae) with water or an organic solvent, such as methanol, ethanol, acetone, n-hexane or benzene, or a mixture or water with the organic solvent, such as water-ethanol, as a principal ingredient in a dental composition, capable of exhibiting a wide antimicrobial spectrum and powerful antimicrobial activity against pathogenic germs for periodontosis and carious pathogenic germs and usable even with antibiotics together.

Description

[Detailed Description of the Invention] [Industrial Application Field] The present invention relates to a dental and oral drug containing a Latania extract having bactericidal properties, and more specifically, to a drug for the prevention and treatment of periodontal diseases using a Latania extract. The present invention relates to an oral composition.

[Prior art]

Canker sores in oral diseases are caused by Streptococcus mutans.
) is an infectious disease mainly caused by bacteria. On the other hand, periodontal diseases typified by alveolar pyorrhea are caused by Bacteroides sp.
It is thought to be a mixed infection caused by several obligate anaerobic bacteria such as P. roides 5pecies).

Actinomyces viscosus (A), which causes periodontal disease
ctinosyces viscosus), Actinomyces naeslundi 4- (A, naeslundi
i), Bacteroides gingivalis
Bacteroides gingivalis), Bacteroides melaninogenicus subspecies melaninogenicus (Bact,
melanogenicus s, s melan
inog-enicus), Eikanella corrodens, Actipacillus actinomycetemcomitans (Actino
bacillus actinomycetem-co
sitans), Capnocytophaga ocracea
and Selenomonas sputigena (Selenoa+on
The pathogenicity of causative bacteria such as As sputigena has been confirmed using germ-free animals.

Actinomyces viscosus (A, viscosus)
) −.

Actinomyces naeslundii (A, naeslu)
Durham-positive bacteria such as ndii) inhabit dental plaque and gingivitis. Pathological periodontal pockets that form between teeth and gums as periodontal disease symptoms progress are infected with Eikenella corrodens (Eik, corroden).
s), Actipacillus actinomycetemcomitans (Ac t , acti non+ycste
mcom i tans) and Capnocytophaga ocr.
acea) proliferates and local bleeding symptoms occur, Bacteroides gingivalis (Bact, gtn
Bact, melani-nogenicus and Fusobacterium nucleatum.
Durham-negative obligate anaerobes such as Rium nucleatum) grow. Some of these pathogenic bacteria produce various enzymes and endotoxins that destroy periodontal tissue, leading to tooth loss.

Today, the medicines for treating gingivitis and pyorrhea on the market are so-called gingival pine surge agents, and their efficacy is to stop bleeding,
Astringent, anti-inflammatory, bad breath removal, etc. have been mentioned, but since periodontal disease is an infectious disease, it is necessary to consider its antibacterial effect as well as these pharmacological and chemical effects.

[Purpose of the invention]

The present inventors searched for substances that have antibacterial effects specifically against periodontal pathogens from about 200 types of highly safe natural herbal medicines and Chinese herbal medicines that have been used after thousands of years of selection, and found that Latania extract It was found that it has particularly excellent antibacterial activity.

That is, the present invention aims to prevent and treat periodontal diseases using a composition containing an extract of Latania.

[Structure of the invention]

The present invention is a dental or oral drug formulated with Latania water and Latania extract, generally in an organic solvent.

(1) Method for producing extract using water: 100 g of dry Latania powder was extracted under reflux under heating in 2000 cc of water for 3 hours, and filtered. The obtained filtrate was heated to 1200O
rpm+, after cooling centrifugation for 10 minutes, the supernatant was concentrated to dryness,
The obtained extract was freeze-dried to obtain a water extract.

(2) Method for producing extract using methanol, ethanol or acetone: 100 g of dried Latania powder was extracted under reflux under heating for 3 hours in 2000 cc of methanol, ethanol or acetone, and filtered. The obtained filtrate was heated to 1200 rpm, 1
After cooling and centrifuging for 0 minutes, the supernatant was concentrated to dryness, and the resulting extracts were freeze-dried to obtain a methanol extract, an ethanol extract, and an acetone extract, respectively.

(3) Method for producing extract of Latania using n-hexane: 100g of dry Latania powder and 2000cc of tohexane
was added, stirred and extracted at room temperature for 24 hours, and then filtered.

The filtrate was concentrated to dryness to obtain an n-hexane extract.

(4) Method for producing an extract of Latania using benzene: Add 2000 cc of benzene to 100 g of dry Latania powder, stir and extract at room temperature for 3 hours, and then filter the filtrate.
The mixture was concentrated to dryness to obtain a benzene extract.

(5) Method for producing a water-ethanol extract of Latania: 100 g of dry Latania powder and 2 ml of a 50% ethanol aqueous solution
000 cc was added, and the mixture was stirred and extracted at room temperature for 3 hours, followed by filtration. The filtrate was concentrated to dryness to obtain an aqueous ethanol extract.

[Method of evaluating effectiveness]

(1) Measurement of minimum inhibitory concentration For each of these extracts, the antibacterial activity against periodontal pathogens was determined by measuring the minimum inhibitory concentration (MIG).

As comparative examples, old C was measured for extracts from licorice, sagebrush, and homica, and berberine chloride, which were crude drugs that had relatively strong antibacterial effects against periodontal pathogens among the many crude drugs searched.

Determination of minimum inhibitory concentration: Add GAM Agar assay medium to the sample and solvent,
A diluted medium was prepared using the 2-fold dilution method.

The bacterial solution for inoculation was subcultured in GAM Broth for 3 generations, and the number of bacteria was adjusted to 10'-'cells/-.

Bacteria inoculation into the diluted medium is performed in the glove box of the anaerobic culture device (mixed gas N2:II□:CO□=80:10:10)
After culturing at 37°C for 120 hours, the growth of the fungus was determined by comparing it with a control.

The measurement results are shown in Table 1.

Water extract of Latania contains bacteria 1, 2.5.9.12 and 1
It showed an MIC of 400 μg/lan against A. 3, and although its antibacterial activity was weaker than extracts using organic solvents, it showed much stronger activity than the aqueous extracts of licorice, staghorn vine, and Vomica.

Regarding methanol and ethanol extracts of Latania,
When we examined the antibacterial activity against all periodontal disease pathogens and caries pathogens, we found that M of 3.13 to 50.0 μg/ml
It showed IC, and a wide antibacterial spectrum and strong antibacterial activity were recognized. The former C against bacteria 1.2, 5°9.12 and 13 for acetone, hexane and benzene extracts of Latania is 1.56 to 50.0 μg/all, which is almost the same or slightly stronger than that of methanol and ethanol extracts. showed that.

(2) Comparison test with antibiotics Bacteroides gingival is considered to be the most important pathogen in periodontal diseases among dental and oral diseases.
Regarding the antibacterial activity against is, a comparative test with various antibiotics was conducted and the results are shown in Table 2. As a result, the ethanol extract of Latania had the same effect as polymyxin B.

Old CM [1C Cephalexin O, 6251, 25)
NovobiocLn O,040,15
6 Polymyxin B 6.25
12.5 Tutracycline TeLrac, ycline O, 1250,
313 Rifaa*picin O,01
560,125Nalidixic acid 100
400 Number of inoculated bacteria 10'cell/d
MBC" (Minimum Bactericidal Concentration) (3) Combination Effect Test with Antibiotics Furthermore, we investigated the combined effect of Latania extract with various antibiotics. For the test method and its evaluation method, please refer to D.
arrel+J, H,; L, I', Garrod &
P.M.

Mate-rworth: J, Cl1n, Path, 2
1:202-209.1968. The results are shown in Table 3.

Various antibiotics and the ethanol extract of Latania did not have antagonistic effects, but showed additive effects. This indicates that even when antibiotics are used in combination with the Latania ethanol extract, they act additively without deactivating each other and can be used in combination.

As shown above, the antibacterial activity test results show that Latania extract has antibacterial activity against various periodontal pathogens, and its antibacterial activity is higher than that of the extracts from licorice, staghorn vine, and homica taken as comparative examples. It was also much stronger, showing a tendency to be slightly stronger than berberine chloride, which is used as a bactericidal and intestinal regulation agent.

In addition, it shows the same effect as polymyxin B in comparison with various antibiotics, and can be used in combination with antibiotics, and is used as a dental oral drug with bactericidal properties to treat oral diseases such as periodontal disease and caries-causing pathogens. showed superior antibacterial activity.

Based on these facts, it is expected that by incorporating Latania extract into oral preparations, it will have an antibacterial effect against periodontal pathogens and enhance the effects of these preparations.

[Production method and examples]

Oral preparations containing Latania extract include gingival surge agents, dentifrices, troches, and impregnation agents.

Possible agents include oral mucosal or gingival adhesive preparations, gums, etc., and can be appropriately selected depending on the purpose of use. Examples of formulations containing latania extract will be described below, but it goes without saying that the present invention is not limited to these examples in any way.

(Example 1) Mouthwash Latania extract 0.4g Peppermint oil 2.0g Sodium lauryl sulfate 1.0g Propylene glycol
30.0g Total: 100.0ml A mouthwash containing the ethanolic extract of Latania was produced according to the above recipe using a conventional method.

(Example 2) Dentifrice Latania extract 1.25g Sodium bicarbonate 70.0g Sodium lauroylsarcosinate 1.5g Peppermint oil
2.0g glycerin
Appropriate amount total: too, og A dentifrice containing an ethanol extract of Latania was prepared according to the above formulation by a conventional method.

(Example 3) Dentifrice Latania extract 1.0g Calcium monophosphate 85.0g Sodium lauryl sulfate 1.0g Orange oil
1.0g lemon oil
0.5g Propyl paraoxybenzoate 0
．． 02g saccharin sodium 0.01
g Glycerin appropriate amount total 100.
0g A dentifrice containing an ethanol extract of Latania was prepared according to the above recipe using a conventional method.

In contrast to Examples 1.2 and 3 above, as a comparative example, the minimum inhibitory concentration of the antibacterial activity of commercially available oral preparations (pharmaceuticals) A-D was measured. The main ingredients of A to D are added to the fourth
Table 5 shows the MIC measurement results. The test method was based on the method described above.

Table 4 [Effects of the invention] In the oral cavity, it is desired to develop a drug that is effective against obligate anaerobes, mainly Bogingivalis, and ABPC (
Antibiotics such as ampicillin are under clinical investigation. However, its use is limited to short-term administration for acute diseases;
Currently, it is not applicable to products that are used continuously, such as general toothpastes and gingival pine surgers, due to the impact on intestinal bacteria or the prevention of the emergence of resistant bacteria.

This substance extracted from latania, a natural herbal medicine, has shown excellent antibacterial activity in antibacterial activity tests, and is considered to be an antibacterial substance that can be expected to prevent and treat infectious diseases in the oral cavity.

Claims (2)

[Claims] (1) A dental or oral drug characterized by containing Latania extract as a main component. (2) Latania is a Fabaceae (Leguminosae-C).
aesal-pinioideae) and its original drug name is (Krameria Lyandra Ruiz e
2. The dental and oral cavity drug according to claim 1, characterized in that the pharmaceutical composition is t Pavon).