KR102120416B1 - Composition comprising high concentration caffeines - Google Patents

Abstract

The composition according to the present invention can provide a composition having high stability by containing caffeine with low solubility together with niacinamide and vanillin, thereby increasing the solubility of caffeine and preventing precipitation of niacinamide and vanillin. Moreover, the composition according to the present invention can provide a synergistic effect of significantly increasing the solubility of caffeine while using a smaller amount than when treating niacinamide or vanillin to caffeine by including niacinamide and vanillin together.
Thus, the composition according to the present invention can provide excellent lipolysis promotion or cellulite removal effect, and thus can be usefully used in the cosmetic field as well as in the cosmetic field.

Description

Composition comprising high concentration caffeines

The content described herein relates to a composition in which a high concentration of caffeine is stably dissolved.

As caffeine is known to have not only blood circulation but also the effect of lipolysis, customers' needs for products containing high concentrations of caffeine are increasing in various fields such as cosmetics and medicine in addition to the food field. However, when caffeine is applied to the skin, in order to obtain pharmacological effects such as lipolysis, cellulite decomposition or relief, caffeine must penetrate the skin, and in order to do this, caffeine must be dissolved in water. That is, even if the composition contains a large amount of caffeine, it is difficult to absorb the skin if not dissolved. However, since caffeine has a very low solubility of about 2% in water at room temperature, there is a problem that the content that can be added to the product is actually limited. Even if dissolved, there is a problem that the use of the caffeine precipitates is limited in terms of stability because the temperature is lowered.

Although a technique of using a solubilizer together to contain a high concentration of caffeine has been developed, if the solubilizer is also included in a certain amount or more to increase the solubility of caffeine, there are limitations in applying to the skin such as skin irritation caused by the solubilizer Therefore, it is necessary to develop a technology capable of substantially containing high concentrations of caffeine in cosmetics.

Republic of Korea Patent Publication No. 10-2012-0119874

One aspect of the present invention is to provide a composition having excellent formulation stability by stably dissolving high concentrations of caffeine.

In order to achieve the above object, an aspect of the present invention provides a composition comprising caffeine, niacinamde and vanillin.

The composition according to the present invention can provide a composition having high stability by containing caffeine with low solubility together with niacinamide and vanillin, thereby increasing the solubility of caffeine and preventing precipitation of niacinamide and vanillin. Moreover, the composition according to the present invention can provide a synergistic effect of significantly increasing the solubility of caffeine while using a smaller amount than when niacinamide or vanillin is included in caffeine by including niacinamide and vanillin together.

In addition, since niacinamide and vanillin also have lipolysis promotion and cellulite removal ability, the composition according to the present invention may not only contain caffeine at a high concentration, but also provide excellent lipolysis promotion or cellulite removal effect. Therefore, it can be usefully used not only in the food field but also in the cosmetic and pharmaceutical fields.

1 is a graph showing the results of a comparative experiment of caffeine skin permeation (cumulative skin permeation of caffeine) of a composition further comprising vanillin or vanillin and niacinamide in caffeine.
Figure 2 is a graph showing the results of a comparative experiment with the case of mixing the fat-decomposing effect (Glycerol release) with caffeine according to the content of vanillin.

In the present specification, the term "skin" means a tissue that covers the body surface of an animal, and is the broadest concept that includes not only the tissue that covers the body surface, such as a face or body, but also the scalp and hair.

Hereinafter, the present invention will be described in detail.

One aspect of the present invention provides a composition comprising caffeine, niacinamide and vanillin.

The caffeine (caffeine) has a xanthine structure (C ₈ H ₁₀ O ₂ N ₄ ) having three methyl groups (see Formula 1 below).

[Formula 1]

Caffeine has pharmacological effects such as central nervous system stimulants, cardiac agents, and diuretics, and has a decomposition effect of fat, particularly cellulite.

Fat is accumulated in the body in the form of triacylglycerol (adiacocyte), the main fat reservoir in the body. The triacylglycerol lipase, a fat-degrading enzyme, is activated by cyclic adenosine monophosphate (cAMP), which breaks down fat into triglyceride and fatty acid. In addition, cellulite (Cellulite) is a major cause of the decrease in lymphatic circulation, and waste products and toxins emitted from the body's metabolic processes cannot be excreted outside and remain in the skin tissue. By connecting the tissue layer of the core and the core, a compartment containing cells containing fat is formed, and the cells containing fat are formed as the size increases.

The caffeine increases the amount of cAMP by inhibiting the activity of the nucleotide phosphodistease, thereby enhancing the activity of triacylglycerol lipase, thereby promoting lipolysis and cellulite. It can be effectively removed.

The niacinamide (niacinamide) has a structure of the molecular formula C ₆ H ₆ N ₂ O (see Formula 2 below), it is usually used in the cosmetic field mainly to obtain a whitening effect.

[Formula 2]

The vanillin (vanillin) has a structure of the molecular formula C ₈ H ₈ O ₃ (see Formula 3 below), it is usually used in the food field as a raw material that gives a vanilla flavor.

[Formula 3]

The caffeine used as an embodiment of the present invention has a very low solubility of about 2% with respect to water at room temperature, so when applied to the skin, the skin permeability is very low, and there is a risk of caffeine precipitation at low temperatures, which is stable. There is a problem that this is very low, the present invention can significantly increase the solubility of caffeine by containing caffeine in the composition together with the niacinamide and vanillin as an example.

The niacinamide is a notice component of a whitening functional cosmetic, which has a notification standard of 2 to 5%, and when used in excess, causes irritation to the skin, so that it cannot be contained above a certain concentration, vanillin is difficult to steer when used in excess and discolors by pH There is a problem in that it is not suitable for use in a composition for a cosmetic, etc., but the present invention found that the solubility of caffeine can be sufficiently increased even with a small amount when used together without containing niacinamide and vanillin, respectively. , The above problems of niacinamide and vanillin do not occur.

Accordingly, the composition according to an aspect of the present invention may include the caffeine in an amount of 1 to 40% by weight, more specifically 2 to 20% by weight based on the total weight of the composition. When the content of caffeine is less than 1% by weight, a composition that maintains caffeine in a dissolved state within a range conceivable as a conventional composition for external application for skin may be used, and the effect on fat decomposition and cellulite decomposition is not large. If it exceeds 40% by weight, caffeine cannot be maintained in a stable dissolving state, and in the container opened state, it is preferable to contain 20% by weight because crystal nuclei are generated due to local moisture evaporation.

As an example, the composition of the present invention may include the niacinamide and vanillin in a weight ratio of more than 0 and less than 0.5 and more specifically, more than 0.1 and less than 0.3, respectively, based on the weight of caffeine included in the composition. In addition, the composition of the present invention as an embodiment may include the niacinamide and vanillin in a weight ratio of 1: 0.1 to 10, more specifically 1: 0.5 to 1.5. When the weight ratio of the niacinamide to vanillin component to caffeine is less than 0.1, caffeine may be precipitated at room temperature and low temperature depending on the concentration of caffeine, and when the weight ratio exceeds 0.3, it may cause irritation or disadvantages in steering, etc.

The weight ratio of niacinamide and vanillin to caffeine is significantly less than the content previously used as a solubilizing agent for niacinamide and vanillin, respectively, and the present invention is due to their synergistic effect by using niacinamide and vanillin together. It means that it can provide excellent caffeine solubility increase effect while including the total amount of ingredients in a significantly reduced amount.

Therefore, the composition as described above according to an embodiment of the present invention may contain a high content of caffeine stably dissolved, thereby providing a composition for promoting fat decomposition or cellulite removal that exhibits excellent effects. In addition, at this time, since vanillin and the like contained in the composition also have a fat decomposition or cellulite removal effect, it is possible to provide a more elevated fat decomposition or cellulite removal effect.

In addition, another aspect of the present invention provides a cosmetic, health food or pharmaceutical composition comprising the composition as described above.

The formulation of the cosmetic composition is not particularly limited, and may be appropriately selected according to the purpose. For example, skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisture lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, foundation, essence, nutrition essence, pack, soap, cleansing Foam, cleansing lotion, cleansing cream, body lotion and body cleanser may be prepared in any one or more formulations selected from the group consisting of, but is not limited thereto.

More specifically, the cosmetic composition may be used for promoting fat breakdown, slimming, or cellulite removal. The cosmetic composition can be applied directly to the subcutaneous fat-rich areas such as the face or the abdomen, thighs, buttocks, arms, etc., to reduce the fat at these areas locally, and is formulated in the form of an external preparation for skin suitable for this purpose. It may be, but the formulation is not particularly limited.

In addition, when the formulation of the present invention is a paste, cream, or gel, animal fibers, plant fibers, wax, paraffin, starch, trakant, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide are used as carrier components. Can be used. When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component, and in particular, in the case of a spray, additionally chlorofluorohydrocarbon, propane /Propellant such as butane or dimethyl ether. When the formulation of the present invention is a solution or emulsion, a solvent, solvating agent or emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid ester. When the formulation of the present invention is a suspension, liquid diluents such as water, ethanol or propylene glycol as carrier components, suspensions such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline Cellulose, aluminum metahydroxide, bentonite, agar or trakant, etc. can be used. When the formulation of the present invention is a surfactant-containing cleansing, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivatives, methyltaurate, sarcosinate, fatty acid amide as a carrier component Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linoline derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

The content of the active ingredient is not particularly limited, but may be included in 0.001 to 100% by weight based on the total weight of the composition. When the active ingredient satisfies the content range, it may exhibit excellent efficacy without side effects.

In addition to the caffeine, vanillin, and niacinamide, the cosmetic composition may further include functional additives and components included in the general cosmetic composition. The functional additive may include a component selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids, and seaweed extract. In addition, the cosmetic composition according to an embodiment of the present invention may be combined with the functional additives, and components included in the general cosmetic composition, if necessary. Other ingredients included include oils and fats, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavors, blood circulation Accelerators, cooling agents, limiting agents, purified water, and the like. Moreover, the present invention relates to an external preparation for skin comprising the composition for promoting fat breakdown or cellulite removal, and the external preparation for skin is a generic term that may include anything applied from outside the skin, and cosmetics of various formulations may be included therein. Can be.

In addition, the formulation of the health food composition according to an aspect of the present invention is not particularly limited, for example, tablets, granules, powders, liquids such as drinks, caramels, gels, bars, etc. may be formulated. The food composition of each formulation may be formulated by appropriately selecting the ingredients commonly used in the field in addition to the active ingredients according to the formulation or purpose of use without difficulty, and synergistic effects may occur when applied simultaneously with other raw materials.

The pharmaceutical composition according to one aspect of the present invention may be administered orally, parenteral, rectal, topical, transdermal, intravenous, intramuscular, intraperitoneal, subcutaneous, and the like. Formulations for oral administration may be, but are not limited to, tablets, pills, soft and hard capsules, granules, powders, granules, liquids, emulsions or pellets. Formulations for parenteral administration may be, but are not limited to, solutions, suspensions, emulsions, gels, injections, drops, suppositories, patches or sprays. The formulations can be readily prepared according to conventional methods in the art, surfactants, excipients, hydrating agents, emulsifying accelerators, suspending agents, salts or buffers for controlling osmotic pressure, colorants, spices, stabilizers, preservatives, preservatives or Other commercial adjuvants can be used as appropriate.

In addition, the active ingredient of the pharmaceutical composition may vary depending on the age, gender, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber, and the determination of the application amount based on these factors is within the level of those skilled in the art. Its daily dosage may be, for example, 0.1 mg/kg/day to 100 mg/kg/day, more specifically 5 mg/kg/day to 50 mg/kg/day, but is not limited thereto.

Hereinafter, the present invention will be described in more detail through the following examples, experimental examples and manufacturing examples. However, the following examples, experimental examples and manufacturing examples are provided for the purpose of illustration only to aid understanding of the present invention, and the scope and scope of the present invention are not limited thereto.

[Experimental Example 1] Caffeine crystal precipitation experiment 1

Caffeine has very low solubility at low temperature, so crystals are precipitated. Therefore, in order to compare the effect of caffeine precipitation at low temperature, that is, the effect of increasing caffeine solubility, depending on the combination of vanillin and niacinamide included in the composition according to an embodiment of the present invention , The following experiment was carried out.

With the composition shown in Table 1, each component was blended in a mixer for stirring while heating to 50-70°C. After filling each object, leave it at room temperature for 1 hour Cooled. Thereafter, to reduce the stability observation time, it was stored in refrigerated (4°C), a harsh condition, and observed whether caffeine precipitated every day. The crystal precipitation properties were observed and are shown in Table 2 below.

Comparative Example 1 Comparative Example 2 Example 1 Caffeine 10.0 10.0 10.0 vanillin 3.0 0.0 1.5 Niacinamide 0.0 3.0 1.5 Purified water Balance Balance Balance

(weight%)

Comparative Example 1 Comparative Example 2 Example 1 Precipitation date 4 days 1 day 8 days

As a result, as shown in Table 1 and Table 2, when the total amount in Example 1 in which the two substances and Comparative Examples 1 and 2 using niacinamide and vanillin, respectively, were the same, an example using niacinamide and vanillin together In the case of 1, caffeine precipitated after 8 days, whereas in Comparative Examples 1 and 2 used, caffeine precipitated after 4 and 1 days, respectively. This means that the present invention comprising niacinamide and vanillin in caffeine can increase the solubility and stability of caffeine by 2 to 8 times or more than when niacinamide or vanillin is included in caffeine, respectively.

[Experimental Example 2] Caffeine crystal precipitation experiment 2

In order to compare the degree of caffeine crystal precipitation inhibition according to the content ratio of vanillin and niacinamide contained in the composition according to an embodiment of the present invention, that is, the effect of increasing caffeine solubility, the following experiment was conducted.

With the composition shown in Table 3, each component was blended in a mixer for stirring while heating to 50-70°C. After each object to be inspected, it was allowed to stand at room temperature and cooled for 1 hour. Thereafter, to reduce the stability observation time, it was stored in refrigerated (4°C), a harsh condition, and observed whether caffeine precipitated every day. Crystal precipitation was observed and is shown in Table 4 below.

Example 2 Example 3 Example 4 Example 5 Example 6 Example 7 Caffeine 10.0 10.0 10.0 10.0 10.0 10.0 vanillin 0.5 1.0 1.5 1.7 2.0 2.5 Niacinamide 2.5 2.0 1.5 1.3 1.0 0.5 Purified water Balance Balance Balance Balance Balance Balance

(weight%)

Example 2 Example 3 Example 4 Example 5 Example 6 Example 7 Precipitation date 2 days 5 days 8 days 9 days 7 days 5 days

As a result, as shown in Table 3 and Table 4, the higher the content ratio of vanillin than the niacinamide, the higher the effect, but the closer the weight ratio to 1:1 (more preferably, the molar ratio is 1:1. The closer it was, the more effective it was. This is due to the influence of caffeine solubilization mechanism.

[Experimental Example 3] Caffeine skin penetration experiment

In order to compare the effect of increasing the skin permeability of caffeine depending on whether vanillin and niacinamide are used in the composition according to an embodiment of the present invention, the following experiment was conducted.

In the preliminary experiment using the artificial skin model (MCTT, Keraskin TM), in the case of the solution state, the skin absorption of caffeine was quickly made in a short period of time and the effect could not be observed. Prepared as a formulation and tested as follows. Specifically, caffeine, vanillin and niacinamide according to the composition of Table 5 below were dissolved in a mixer for stirring while heating to 50-70° C. using purified water as a dissolving agent, and then an aqueous phase with xanthan gum added to the dissolved phase was added. And stirred. After this, the remaining amount of purified water was added so that caffeine became 5% (w/w). After each object to be inspected, it was allowed to stand at room temperature and cooled for 1 hour.

Comparative Example 3 Comparative Example 4 Comparative Example 5 Example 8 Caffeine 5.00 5.00 5.00 5.00 vanillin 0.00 0.75 0.00 0.75 Niacinamide 0.00 0.00 0.75 0.75 Xanthan gum 2.00 2.00 2.00 2.00 Purified water Balance Balance Balance Balance

(weight%)

First, an artificial skin model (MCTT, Keraskin TM) was placed in a 6-well plate containing 0.9 ml per well of the medium warmed at 37°C, and then about 22±2 hours in a 37°C, 5% CO ₂ cell incubator. Stabilized for a while. After taking out the stabilized artificial skin model immediately before the test, 30 µl of each of Comparative Examples 3, 4, 5, and Example 8 of Table 5 above as a test substance was slowly dropped into the center of the artificial skin model and then inserted. After holding and returning it to be applied evenly, a nylon mesh was covered to prevent air bubbles. After the test substance was applied, it was placed in an incubator at 37°C and 5% CO ₂ conditions, and then sampled in a receptor compartment at 1 hour, 2.5 hours, and 5 hours, and the same amount of fresh medium was filled. (n=3). And the cumulative shin permeation of caffeine of caffeine at each time is shown in FIG. 1.

[Experimental Example 4] lipolysis experiment

The following experiment was carried out to confirm the lipolytic efficacy of vanillin contained in the composition according to an embodiment of the present invention.

First, primary human subcutaneous adipocytes (primary human subcutaneous preadipocyte) were differentiated into adipocytes over 2 weeks, and then treated with 10, 100, and 500 ppm of vanillin for 72 hours, respectively. After 72 hours, the concentration of glycerol released in the medium was measured. In addition, 10, 100, 500 ppm of vanillin and 500 μM caffeine were treated together in the same manner as above, and then the concentration of glycerol (Glycerol release, μg/μl) released in the medium after 72 hours was measured. And the results are shown in FIG. 2. In this case, in the horizontal axis of FIG. 2, (-) is a control in which caffeine and vanillin are not added, V10, V100, and V500, respectively, when vanillin is included in 10, 100, and 500 ppm, □(-caffeine) contains only vanillin without caffeine. If it is, ■(+caffeine) means that both caffeine and vanillin are included.

As a result, as shown in FIG. 2, it was confirmed that glycerol released from the medium (-caffeine) to which vanillin was added was measured, and that vanillin also had lipolytic effect. In addition, when both vanillin and caffeine are included, the concentration of released glycerol is significantly higher than when only vanillin is included, and it can be seen that vanillin can be used together without inhibiting the lipolysis efficacy of caffeine.

Hereinafter, a formulation example of the composition will be described, but not intended to limit the present invention, but to be specifically described.

[Formulation Example 1] Nutritional lotion (Milk Lotion)

A nutritional lotion (milk lotion) was prepared according to a conventional method using the composition according to an embodiment of the present invention in the composition shown in the table below.

Ingredients weight% Caffeine 5.0 Niacinamide 1.0 vanillin 1.0 Squalane 5.0 Wax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 1.5 Floating paraffin 0.5 Caprylic/Capric Triglyceride 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Triethanolamine 0.2 Preservatives, pigments, flavors Proper Purified water to 100

[Formulation Example 2] Flexible lotion (skin lotion)

The composition according to an embodiment of the present invention was prepared with a flexible lotion (skin lotion) according to a conventional method with the composition shown in the table below.

Ingredients weight% Caffeine 5.0 Niacinamide 1.0 vanillin 1.0 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 PEG 12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservatives, pigments, flavors Proper Purified water to 100

[Formulation Example 3] Nutrition Cream

The composition according to an embodiment of the present invention was prepared in a nutrient cream according to a conventional method with the composition shown in the table below.

Ingredients weight% Caffeine 5.0 Niacinamide 1.0 vanillin 1.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.5 PEG60 hardened castor oil 2.0 Floating paraffin 10 Squalane 5.0 Caprylic/Capric Triglyceride 5.0 glycerin 5.0 Butylene glycol 3.0 Propylene glycol 3.0 Triethanolamine 0.2 antiseptic Proper Coloring Proper Spices Proper Purified water to 100

[Formulation Example 4] Massage Cream

The composition according to an embodiment of the present invention was prepared in accordance with a conventional method with a composition described in the table below.

Ingredients weight% Caffeine 10.0 Niacinamide 1.5 vanillin 1.5 Wax 10.0 Polysorbate 60 1.5 PEG 60 hardened castor oil 2.0 Sorbitan sesquioleate 0.8 Floating paraffin 40.0 Squalane 5.0 Caprylic/Capric Triglyceride 4.0 glycerin 5.0 Butylene glycol 3.0 Propylene glycol 3.0 Triethanolamine 0.2 Preservatives, pigments, flavors Proper Purified water to 100

[Formulation Example 5] Pack

The composition according to one embodiment of the present invention was prepared according to a conventional method with the composition shown in the table below.

Ingredients weight% Caffeine 10.0 Niacinamide 1.5 vanillin 1.5 Polyvinyl alcohol 13.0 Sodium carboxymethylcellulose 0.2 glycerin 5.0 Allantoin 0.1 ethanol 6.0 PEG 12 nonylphenyl ether 0.3 Polysorbate 60 0.3 Preservatives, pigments, flavors Proper Purified water to 100

[Formulation Example 6] Gel

The composition according to an embodiment of the present invention was prepared according to a conventional method with the composition shown in the table below.

Ingredients weight% Caffeine 5.0 Niacinamide 1.0 vanillin 1.0 Sodium ethylenediamine acetate 0.05 glycerin 5.0 Carboxyvinyl polymer 0.3 ethanol 5.0 PEG 60 hardened castor oil 0.5 Triethanolamine 0.3 Preservatives, pigments, flavors Proper Purified water to 100

Since the specific parts of the present invention have been described in detail above, it is obvious that for those skilled in the art, this specific technique is only a preferred embodiment, and the scope of the present invention is not limited thereby. something to do. Accordingly, the substantial scope of the present invention will be defined by the appended claims and their equivalents.

Claims (9)

Caffeine, niacinamide and vanillin,
The composition contains the caffeine in 2 to 20% by weight relative to the total weight of the composition,
The niacinamide and vanillin in a weight ratio of 1: 1 to 2. delete The composition of claim 1 wherein the weight ratio of niacinamide to caffeine is greater than 0 and less than 0.5. The composition of claim 1, wherein the weight ratio of vanillin to caffeine is greater than 0 and less than 0.5. The composition of claim 1, wherein the weight ratio of niacinamide and vanillin is 1: 1 to 1.5. The composition according to any one of claims 1 and 3 to 5, wherein the composition is for decomposing fat or cellulite. 7. The composition of claim 6, wherein the composition is a cosmetic composition. delete 7. The composition of claim 6, wherein the composition is a food composition.

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