KR100687037B1 - Composition for nano carrier comprising extract of licorice, tocopherol and balsam, oral care product using it - Google Patents

Abstract

The present invention relates to a nanocarrier composition containing licorice extract, tocopherol and balsam and oral care products using the same, more specifically 1-5.00 wt% lecithin, 1-20.00 wt% ethanol, capric / caprylic trigly 1-5.00% ceride, 1-20.00% balsam extract, 1-20.00% tocopherol acetate, 0.001-1.00% oil soluble licorice extract, 0.01-1.00% cetylphosphate, 0.001-1.00% vitamin C, BHT 0.1 Nanocarrier composition comprising -0.5% by weight, purified water, and it is applied to the use of oral hygiene products.

When using the nanocarrier according to the present invention, it is possible to improve the oral penetration ability of licorice extract, tocopherol, balsam, etc., which are effective medicinal ingredients in the oral cavity. It is possible to obtain a periodontal disease prevention effect.

Nano Carrier, Licorice, Tocopherol, Balsam, Oral Hygiene

Description

Nano Carrier Composition Containing Licorice Extract, Tocopherol and Balsam, Oral Hygiene Products Using the Same {Opposite for NANO CARRIER COMPRISING EXTRACT OF LICORICE, TOCOPHEROL AND BALSAM, ORAL CARE PRODUCT USING IT}             

1 is a graph showing the particle size distribution of the nanocarriers produced by the present invention.

2 is a frozen electron micrograph of the nanocarrier particles produced by the present invention.

The present invention relates to a composition containing an oral medicinal ingredient and an oral hygiene product using the same, and more particularly, to an oral composition and an oral hygiene product using the same oral mucosa penetration of the active ingredient.

In general, when the composition for promoting oral hygiene is mainly used, except for pharmaceuticals, toothpaste, oral cleaning liquid, chewing gum and the like can be mentioned. These compositions may appear differently depending on the characteristics of the product, but the development of the composition for promoting oral hygiene is basically focused on preventing caries, preventing periodontal disease, and removing bad breath.

Therefore, oral hygiene products are also manufactured using various compositions containing ingredients that are effective in preventing tooth decay, periodontal disease, etc. In addition to xylitol, fluorine, green tea extract, licorice extract, and the like, various compositions containing various herbal ingredients are used. It is becoming a trend.

However, conventionally, oral hygiene products containing ingredients effective for oral hygiene, even though they contain ingredients effective for periodontal disease, etc., the composition is often used as it is, so it is hardly absorbed by the living body, such as periodontal disease actually The preventive effect could not be greatly expected. That is, even if the toothpaste contains licorice extract, for example, there is a problem that the effect by the active ingredient is hardly seen unless it is absorbed into the body for a short time while brushing teeth.

 In addition, Korean Laid-Open Patent Publication No. 1999-0053087 published on July 15, 1999, discloses a composition for oral hygiene enhancement encapsulated in 200 to 2,000 micrometers sized extract of the complex extracted five times gall, licorice, gold in a certain ratio However, this is only a method for improving the stability and usability of the toothpaste over time, and is not a method for increasing the bioabsorption rate of the herbal preparations. As a result, in the case of encapsulating and using various active ingredients, there is still a problem that the bioabsorption rate of the active ingredients is low.

Therefore, there has been a continuous need for a method of increasing the stability of the substance itself that can prevent periodontal disease and the like in the composition for promoting oral hygiene and a method of increasing the effect of increasing the biological penetration of the substance.

In order to solve the above problems, the present invention has a severe discoloration and does not dissolve well in oil-soluble oils, oil-soluble licorice extract with low absorption of the body, skin or gums, tocopherol acetate and late balm extracts effective against caries bacteria, oral mucosal penetration ability The purpose is to increase the stability in the oral hygiene products at the same time.

In order to achieve the above object, the present invention is 1-5.00% by weight of lecithin, 1-20.00% by weight of ethanol, 1-5.00% by weight of capric / caprylic triglycerides, 1-20.00% by weight of balsam extract, tocopherol acetate Nanocarrier composition comprising 1-20.00 wt%, oil-soluble licorice extract 0.001-1.00 wt%, cetylphosphate 0.01-1.00 wt%, vitamin C 0.001-1.00 wt%, BHT 0.1-0.5 wt%, purified water Provide oral hygiene products used.

As a result, the biopermeability of licorice extract, balsam, tocopherol components and the like is improved to maximize the effect of the active ingredient.

Hereinafter, the configuration of the present invention to be described in more detail.

In particular, the nanocarrier composition of the present invention contains 1-20.00% by weight of balsam extract, 1-20.00% by weight of tocopherol acetate, and 0.001-1.00% by weight of oil-soluble licorice extract.

Balsam is a sticky liquid secreted from conifers and is one of natural resins. Balsam has antiseptic, anti-inflammatory, and antibacterial effects, especially against caries. Nanocarrier composition in the present invention contains 1-20.00% by weight of balsam extract having the above-described efficacy.

The nanocarrier composition of the present invention also includes an oil-soluble licorice extract, which is the root of licorice, a perennial plant belonging to the legume, which is reddish brown or dark brown, tastes sweet and nonpoisonous. Licorice has the detoxification effect, helps the function and energy of the spleen, removes boils, and evenly harmonizes various medicines. The nanocarrier composition of the present invention contains 0.001-1.00% by weight of an oil-soluble licorice extract having the above-described efficacy.

In addition, the nanocarrier composition of the present invention contains 1-20.00% by weight of tocopherol acetate. Tocopherol is a vitamin E, which is contained in vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, and palm oil. . Tocopherol acts as an antioxidant that inhibits the production of free radicals and lipid peroxide by scavenging free radicals in vivo. Tocopherol itself is unstable to use a lot of its derivatives, in particular vitamin acetate, vitamin palmitate, etc. are mainly used, the tocopherol acetate is used in the nanocarrier composition of the present invention. Vitamin E is also effective in severe periodontal disease. In particular, animal studies have shown that tocopherol reduces silver toxicity, so if the tooth is silver plated, the antioxidant effect of tocopherol is essential.

In the present invention, the oral effective substance as described above, that is, licorice extract which is effective in various inflammations, such as stomatitis, upper respiratory tract, bronchitis, anti-inflammatory, antibacterial balsam, and antioxidant action, immune function enhancement, wound healing promoting action And tocopherol component that is effective in periodontal disease, such as caries, gingivitis, periodontal disease is effective, but low bio-absorption useful material is used by nano-carrier.

Nanocarriers in the present invention mainly consists of two forms, liposomes and nanoemulsions. Among them, phosphatidyl choline (PC), phosphatidyl ethanolamine (PE), phosphatidyl serine (PS), sphingomyelins, cardiolipids, plasmalogens (plasmalogens) Liposomes in equilibrium with water are formed by forming a bilayer closed membrane composed of phospholipids such as phosphatidic acid and cerebroside. Lipid components have amphiphilic properties in themselves and thus have polar (hydrophilic) hydrophilic sites and nonpolar (lipophilic) lipophilic sites. Therefore, liposomes, when dispersed in water, form a bilayer, rather than a spherical form, to capture the aqueous phase. In contrast, nanoemulsions collect oily components. Therefore, the nano-carrier is used to prepare a poorly soluble substance (eg, tocopherol, retinol, etc.) inside the nanoemulsion, and a material having low bioavailability (eg, licorice extract, balsam, etc.) using liposomes. It will be able to enhance their bioavailability by collecting. In addition, by utilizing this through the product, the biologically active material is selectively absorbed into the mucous membranes of the mouth, gums and other skin, thereby increasing the effects of caries prevention, gingivitis prevention, and periodontal disease prevention.

However, the nanocarriers are so small in particle size that they cannot be measured by a general optical microscope. Therefore, as shown in Figure 2 it can be confirmed by taking a picture by using a Photo Graphing Freeze-Fracture Scanning Electron Microscopy. In FIG. 2, the protruding part is a nanoemulsion part in monolayer, and the part is a liposome that is a bilayer. That is, it can be seen that the nanocarrier is a combination of nanoemulsion and liposome.

As can be seen in Figure 1, the nanocarrier prepared by the composition of the nano-carrier of the present invention, the particle size of the nano-carrier was measured using a Zeta Potential Analyzer (Malvern, Zetasizer 1000HS) results in a particle size of 20- It was found that it is 300nm. Therefore, since the intercellular lipids are 200-300nm and the nanocarriers according to the present invention are 20-300nm, when the nanocarriers according to the present invention are used, the active ingredient collected in the nanocarriers can be rapidly penetrated to the gums and the like. will be.

The present invention also provides an oral care product comprising a nano carrier prepared by the nano carrier composition.

In addition to nanocarriers, oral care products may include abrasives, humectants, binders, foaming agents, sweeteners, preservatives, fragrances, pH adjusters, brighteners, and the like.

Hereinafter, the present invention will be described in more detail with reference to preferred embodiments of the present invention. However, the scope of the present invention is not determined accordingly, but is presented by way of example only.

EXAMPLE

Example 1 Preparation of Nanocarriers Using Balsam Extract, Tocopherol Acetate and Oil-Soluble Licorice

1-5.00% lecithin, 1-20.00% ethanol, 1-5.00% capric / caprylic triglyceride, 1-20.00% balsam extract, 1-20.00% tocopherol acetate, oil-soluble licorice extract 0.001-1.00 100% by weight of purified water is added to the weight%, cetyl phosphate 0.01 to 1.00% by weight, vitamin C 0.001-1.00% by weight, BHT 0.1-0.5% by weight. The nanocarrier was prepared by mixing and stirring the nanocarrier composition, and passing the high pressure fine homogenizer, followed by cooling and defoaming.

As can be seen in Figure 1, the particle size distribution of the nano-carriers prepared above was measured using a Zeta Potential Analyzer (Malvern, Zetasizer 1000HS), the particle size was 20-300nm, especially at 50-100nm Many distributions were found.

Example 2 Preparation of Nanocarrier-Containing Toothpaste

As a preparation step, the components of a) were introduced into the production unit at a temperature of 70 to 75 ° C. and stirred for 20 minutes to completely dissolve the powder and then cooled to room temperature. Subsequently, as a dissolving step of the moisturizer, sweetener and useful ingredient, b) components including the nanocarrier obtained in Example 1 were added to the preparation unit at 25 to 35 ° C., followed by stirring for 15 minutes to dissolve. The following is a powder and viscous mixing process, in which c) components were mixed at 25 to 35 ° C. and added stepwise. Thereafter, as the foaming agent mixing and primary defoaming step, d) component is added to complete the primary defoaming during the 40 minute process at 25-35 ° C. Finally, as a fragrance mixing process, the nanocarrier-containing toothpaste was prepared by adding e) component and performing secondary degassing at 25 to 35 ° C.

Nanocarrier-containing toothpaste (1)

a) Make total weight of purified water 100%

b) 6.00% by weight glycerin

  Sorbitol 35.00 wt%

  Zaccarin Sodium 0.10% by weight

  Nano Carrier 1.00-20.00% by weight

c) 7.00 wt% silica

  Precipitated Calcium Carbonate 39.00% by weight

d) 2.00% by weight of sodium lauryl sulfate

e) menthol 0.40% by weight

  Peppermint oil 0.10% by weight

 Nanocarrier-containing toothpaste (2)

a) 0.75% by weight sodium monofluorophosphate

  Makes 100% by weight of purified water in total

b) 0.10% by weight of aminocaproic acid

  4.50 wt% sodium chloride

  Glycerin 4.00 wt%

  Sorbitol 35.00 wt%

  Nano Carrier 1.00-20.00% by weight

c) 15.00 wt% colloidal silicon oxide

d) polyethylene glycol 1500 4.00% by weight

Nanocarrier-containing toothpaste (3)

a) 0.75% by weight sodium monofluorophosphate

  Makes 100% by weight of purified water in total

b) sorbitol 30.00 wt%

  Glycerin 5.00 wt%

  Zaccarin Sodium 0.20% by weight

  Sodium chloride 0.20 wt%

  Nano Carrier 1.00-20.00% by weight

c) 15.00 wt% of silicon dioxide

  6.00% by weight of silica

  1.00% by weight of carboxymethyl cellulose

d) 2.00% by weight of sodium lauryl sulfate

Nanocarrier-containing toothpaste (4)

a) Make total weight of purified water 100%

b) sorbitol 20.00 wt%

  Glycerin 5.00 wt%

  Nano Carrier 1.00-20.00% by weight

c) calcium carbonate 30.00% by weight

  Calcium Dihydrogen Phosphate 12.00% by weight

  3.00 wt% silica

  Carboxymethyl cellulose 0.70 wt%

d) 1.50% by weight of sodium lauryl sulfate

Example 3:  Percutaneous absorption rate measurement experiment

Percutaneous absorption experiment using a toothpaste containing 5% by weight of the nanocarrier prepared in Example 2 and a general toothpaste containing 0.2% by weight of tocopherol, 0.001% by weight of useful oil licorice extract, and 0.50% by weight of balsam extract Was performed. Guinea pigs were used for this purpose. The skin of the guinea pig's buccal region was cut out and mounted in Frans-type diffusion cells (lab Fine Instruments). 5 ml of distilled water was put into a receptor vessel of a Franz-type permeation cell vessel, and the permeation cell was mixed and dispersed at 600 rpm while maintaining 32 ° C. 300 μl of each sample was placed in a donor vessel for 5 minutes. Maintained. Then, after adding 1ml of distilled water and maintaining for 2 minutes, the sample and the distilled water mixture was removed, and this process was repeated 10 times.

The area of skin where absorption and diffusion occurs is 0.64cm2. After the absorption diffusion of nanocarrier is finished, the skin surface is washed with 1 ml of distilled water, and 6 ml of ethanol is effective by using a tip type equalizer (Polytron PT2100, Switzerland). After the skin of which the components were absorbed and diffused was changed, the extract was filtered using a 0.45 µm nylon filtration membrane and the content was measured by high pressure liquid chromatography.

The skin permeability of the nanocarrier tocopherol, which indicates the degree of penetration into the skin, was 0.118% for the toothpaste, 0.189% for the toothpaste containing the nanocarrier, and the skin permeability of the nanocarrier was about 60%. As a result, it was confirmed that the nanocarrier promotes the absorption of buccal sac of tocopherol acetate.

Example 4 Measurement of Color Change by Heat and Light of General Toothpaste and Nanocarrier-containing Toothpaste

After changing the nanocarrier-containing toothpaste and the general toothpaste prepared in Example 2 under 25 ° C. + light shielding condition, 40 ° C., and light exposure conditions, color change was measured by a chroma meter.

As time passes, oil-soluble licorice changes color due to heat and light.In contrast, toothpaste containing nanocarrier is about 2 times under light exposure condition, about 1.5 times under 40 ℃, and 25 ℃ + shading compared to general toothpaste. It was found to be about three times stable under the conditions.

Example 5 Measurement of Gingivitis Mitigation Effect

To determine the gum disease prevention effect of the toothpaste containing the nanocarrier of the present invention was measured gingival index.

After selecting 20 subjects, the gingivitis index was measured according to Le's gingivitis rating criteria modified by Talbott, Mandel and Chilton.

(Le's gingivitis index, modified by Talbott, Mandel and Chilton)

Le Gingivitis Rating Criteria

0: no inflammation

1: Mild gingivitis (weak change of color and weak edema) No bleeding during periodontal cyst measurement

2: moderate gingivitis (redness, edema) bleeding during periodontal cyst measurement

3: tendency to bleed due to high gingivitis (ulcer)

Nano carrier-containing toothpaste Generic toothpaste Initial value 1.70 ± 0.18 1.69 ± 0.11 1 week 1.10 ± 0.18 1.51 ± 0.12 2 weeks 0.61 ± 0.14 1.10 ± 0.28

Table 1 shows the results of the gingivitis index measurement, as shown in Table 1, the toothpaste containing nanocarriers was found to have a very good gingivitis relieving effect as compared to the general toothpaste has a superior percutaneous absorption rate through the mucosa.

 According to the present invention, the composition containing licorice, tocopherol, balsam, etc., which have low absorption in the body despite being an effective ingredient in the oral cavity, is stabilized with a nanocarrier, thereby increasing the oral mucosal penetration of the active ingredients.

In addition, according to the present invention, even in the case of licorice that discolors well, it exhibits stability to heat and light.

Therefore, when the nanocarrier prepared according to the present invention is used in an oral hygiene product, not only can improve the stability of the oral medicinal components in the product, but also penetrates the skin, gums and body to increase the excellent gingivitis And periodontal disease prevention effect can be obtained.

Claims (2)

1-5.00% lecithin, 1-20.00% ethanol, 1-5.00% capric / caprylic triglyceride, 1-20.00% balsam extract, 1-20.00% tocopherol acetate, oil-soluble licorice extract 0.001-1.00 A nanocarrier composition comprising: wt%, cetylphosphate 0.01-1.00 wt%, vitamin C 0.001-1.00 wt%, BHT 0.1-0.5 wt%, purified water (balance). Toothpaste comprising a nanocarrier prepared by the nanocarrier composition of claim 1.

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