JPS5857320A - Plaque formation inhibitor - Google Patents

Abstract

PURPOSE:The titled inhibitor that contains, as active ingredients, a variety of herb medicines such as BOI, SHINKYU, TANSHIN, NANTEN seeds or their essences. CONSTITUTION:A variety of herb medicines such as BOI (Aristalochiaceae fangchi Wu), KANZO (Glycyrrhiza gleabra-L. var. glandulfiere), NINZIN (Panax), CHIMO (Anemarrhena), HOKOEI root (Taraxacum), JUYAKU (Houttuynia) and others are subjected to heat extraction with water, 50% methanol or methanol for 3hr to get an essence. The resultant essence is used to prepare the objective preparation for inhibiting plaque formation. The preparation may be used directly in an oral cavity, however, it may be mixed with tooth paste. The dose is preferably a little excessive, in consideration of the loss during the use.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a dental calculus formation inhibitor, and more specifically to a dental calculus formation inhibitor comprising extracts and/or active ingredients of various herbal medicines as described in the claims. The purpose is to provide an effective oral preparation for preventing dental caries or inhibiting its progression by suppressing tartar formation on tooth surfaces. It is a disease that causes localized and progressive destruction of teeth, and the morbidity rate is extremely high, making it an important public health problem.

This phenomenon of eclipse is caused by oral streptococcus.
sptococcus mutanθ uses sucrose in food as a substrate.

The first step is to produce a sticky polysaccharide (glucan), which allows the bacteria to colonize the smooth surface of the tooth.

This aggregate of bacteria that aggregates and colonizes on the tooth surface is called dental calculus f Pl.
aque). And, in order to prevent wrinkles, it is sufficient to suppress the above-mentioned tartar formation. There are various ways to suppress the formation of such tartar.

The first thing that comes to mind is 8treptococcus mu
This is a method of exterminating cariogenic bacteria from the oral cavity by administering a drug that has a bactericidal or bacteriostatic effect on T. tans, and has actually been tried to some extent. However, these drugs disturb the bacterial flora in the oral cavity and intestines, disrupting the balance of natural bacteria, and are associated with other side effects.

It has not yet been widely used.

Next VC #i There is a mechanical method for removing tartar. 1. Although toothpaste is used on a daily basis, this is a physical cleaning using the hands and does not completely remove tartar. It is difficult to do so.0 The present inventor has conducted various studies regarding the appropriate method for suppressing tartar formation, and has extensively investigated means for preventing the adhesion of cariogenic bacteria to the smooth surfaces of teeth. , t'') It was very unexpected that we discovered that extracts of certain herbal medicines had such effects, and as a result of further research, we finally completed the present invention. Experimental methods and results demonstrating the effects of the present invention will be explained in detail.

Hot water, 50% methanol and methanol extracts of various Japanese and Chinese herbal medicines were prepared, and 8trθ was prepared in the presence of sucrose.
The inhibitory reactions of various extracts to the adhesion of heat-treated bacterial cells to glass surfaces due to glucan production by crude glucosyltransferase derived from Ptococcus mutan were investigated.

The extracts used were prepared by heating and extracting crude drugs with water, 50 timethanol, or methanol for 3 hours. In addition, the glucosyltransferase of the bacterial cells and the heat-killed bacteria were purified as follows. i.e. S, mutans OM
After culturing Z 176 at 37°C for 24 hours using BE culture medium, it was centrifuged at 12,000g for 20 minutes, and the resulting supernatant was adjusted to the ammonium sulfate concentration of sob to precipitate glucosyltransferase.9 Then, this was incubated overnight. 9 using the next phase #ligature obtained by dialysis. Manen fungal body dloO
The heat-killed bacteria were used after being heat-treated for 20 minutes at "C" and then freeze-dried.

1(K) The inhibitory effect on tartar formation using these extracts was assayed as follows.

That is, to the crude glucosyltransferase and heat-killed bacteria as described above, the extract concentration was o, xq/111. The extract was added to give a concentration of g, 5++ILi/iu, and 1η/d, and this was cultured in a tissue culture test tube at 37°C for 16 hours at an angle of 3o0 in the presence of sucrose. The test tube was then gently rotated to remove floating microbial cells, washed three times, and stained with methylene blue to compare the number of microbial cells attached to the glass wall. The results of testing the ability of these two methods to prevent heat-killed bacteria from adhering to a glass surface are shown below.

(a) Completely inhibited bacterial adhesion at a concentration of 0.1 u:9/rxl (methanol extract) Sachiboshi 9M Satsuma (completely inhibited bacterial adhesion at a concentration of 10.51 ng/il) Methanol extract) Shikon, Boar, Reishi, Juyaku, Gobai, Urushi, Bai Xun.

Side oak leaf 1 pomegranate root bark, dandelion palm, saiko (50 timethanol extract), cinnamon bark, osteoclast repair, good tatami, dry tatami, rhubarb, ephedra, urajirogashi.

Danko (Waterworks kiss) Bone fracture supplement, Gobako, Light bamboo leaf, X leaf, Summer dry grass, Danko palm (C1
l 11f/111 concentration that completely inhibits bacterial adhesion (methanol extract) Hu Huanglian, Mokhang Y4. Ibarami, Jibo, Han Hobok, and Cordyceps sinensis.

Oga 9 losses, soy sauce, horse teeth 1. White skin, side leaves 1 pomegranate root bark, 4
11 coconut, 0 ginseng, yuan zhi (50 timethanol extract), elm, boar, defense, 10 medicines, 5x, camellia leaf, word kako, light bamboo leaf.

Wu Laiying, Urajirogashi 9 pomegranate root bark, dandelion palm, licorice.

(Suikokiss) Jingyangpi, ten medicines, mountain bean root, hanhoboku, rhubarb, and mulberry root. 9 pomegranate root bark of Red Xuan, and 1il of Zan palm, which showed a particularly remarkable effect in the above experiment.
Regarding the methanol extract of iii, Sephadex L
The action of the fractions developed on a H20 column and eluted with 90 timemethanol was investigated, and it was found that the fractions exhibiting reactions with capillarycins and flavones exhibited bacterial adhesion inhibiting activity. Furthermore, when we conducted a precise experiment using a standard compound, we found that 2-(p-hydroxyphenoxy)
The product of the present invention is extremely useful as a tartar formation inhibitor, as shown by the experiments above C in which -5,7-cyhydroxychromone and G-2 (flavone) were found to exhibit bacterial adhesion inhibiting activity. Certain 1° tartar formation inhibitors of the present invention may be used alone or in combination. For example, the methanol extract of H. medicinale may be used alone, or it may be used in combination with other crude drug extracts.

If necessary, it may be used in combination with other tartar formation inhibitors, general oral preparations, and drugs that exhibit bactericidal or bacteriostatic activity against s'treptococcus and smutans.

These are naturally also included within the scope of the present invention.

In addition, water, 5O1s methanol, and methanol are cited as examples of the solvent for producing the extract, but other solvents and solvent mixtures may also be widely used as long as they do not interfere with the structure and purpose of the present invention. The tartar formation inhibitor may be applied directly into the oral cavity as it is, or may be mixed with other oral preparations such as toothpaste. Lozenges as needed,
Sublingual tablets or other appropriate dosage forms may be used.

It is best to use an appropriate amount based on the EIKEN data mentioned above, but please be aware that the amount lost during use, for example when mixed with toothpaste, may be washed away by rinsing. It is advisable to use consideration and extra-shun.

Some examples are given below as illustrations of embodiments of the invention.

Of course, these are merely illustrative examples, and therefore do not mean that the present invention is limited only to these examples.

Example 1 Green onion leaves are heated with methanol for 3 hours, and the resulting extract is pressed and kneaded into a commercially available paste-like toothpaste product.

Example 2゜Example 1. Mix the methanol extract with water and a small amount of i-lysis aid and fragrance in a container with an atomizer to make an intracavitary spray.

Example 3 Water and a solubilizing agent are added to the methanol extract of Example 1 to prepare a hoeing agent.
Above, Example 4: To the methanol extract of Example 1, an appropriate amount of an antibacterial agent against 5 treptococcus mutans, which was determined by the present inventors from the extracts or active ingredients of nine various herbal medicines, was added. Toothpaste 1 should be an intracavity spray or a rutting agent.

that's all Patent applicant: Tsurui Pharmaceutical Co., Ltd.

Claims (1)

[Scope of Claims] 1. Houki, Hata brother, Tanqin, Nantenji, Chimo, Gamagoheikon, Juyaku, Gobaiko, Yamabean root, Gennoshoko, white fruit, camellia leaf, arrowroot, bellflower, frankincense. Summer dried grass, horse-toothed grass, southern sky leaves, ephedra, peony bark, white bark, wubai, Wu Ceying, lianchu, schisandra, Chenpi, Xinyi 9th block, gold and silver flowers,
Chrysanthemum, half summer. Jiyu, mshin, huhuanglian, hyakubekon, toki, weirishian, cinnamon, purple root, sawara, shiraki, sogu, bone crushing, hyakuo 9sho hemp, ryoyo,
Inui, Kika. Qinpi, Irei, Ogirei, Reishi, Calyx, Capsicum, Shotai, Sofukijin,
Power i skin. Setsui, side leaf, Urajirogashi 1 pomegranate root bark, dandelion palm, segusa, saiko. Tartar formation inhibitor consisting of extracts and/or active ingredients of ginseng, ginseng, and/or ginseng