KR20110029800A - Composition containing coffee berry extracts or biter orange flower extracts - Google Patents

Abstract

PURPOSE: A composition containing coffee berry extract or biter orange flower extract is provided to prevent edema and lipoxygase. CONSTITUTION: A composition for preventing edema contains coffee berry extract or biter orange flower extract as an active ingredient. A composition for suppressing lipoxygenase contains the coffee berry extract or biter orange flower extract as an active ingredient. The extract is contained in 0.01-80 weight% based on total composition.

Description

Composition containing coffee berry extracts or biter orange flower extracts}

The present invention relates to a composition containing a coffee berry extract or a beater orange flower extract as an active ingredient.

If you develop swelling, you may feel swollen, gain weight, sleep when you wake up, swell your eyes, pinch your fingers, and feel unpleasant. Edema is also known to cause local excess moisture in the skin, promoting impaired blood circulation and skin aging. In general, skin problems have been reported to exacerbate the condition of people with impaired lymphatic system and overloaded lymphedema.

Therefore, many people are worried about edema, but the countermeasures are insufficient. In particular, these symptoms can cause extreme popularity in social life. Drugs are used to alleviate these symptoms, but often have side effects.

Therefore, it is necessary to develop a material that is excellent in suppressing or preventing edema, has no side effects, and is inexpensive.

The present invention finds that when using one or more selected from the group consisting of coffee berry extract and bitter orange flower extract, excellent edema suppression or prevention, lipoxygenase inhibition and lipid inhibition promoting effect are achieved, thereby coffee berry extract and It is to provide a composition for inhibiting or preventing edema, inhibiting lipoxygenase and promoting lipid inhibition, which contains at least one selected from the group consisting of bitter orange flower extract as an active ingredient.

The present invention provides edema inhibition or prevention, lipoxygenase inhibition, lipid inhibition promoting composition containing as an active ingredient at least one selected from the group consisting of coffee berry extract and beater orange flower extract.

The composition of the present invention contains at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract as an active ingredient to have edema inhibition or prevention, lipoxygenase inhibition and lipid inhibition promoting effect.

The present invention relates to edema inhibition or prevention, lipoxygenase inhibition and lipid inhibition promoting composition containing as an active ingredient at least one selected from the group consisting of coffee berry extract and beater orange flower extract.

As used herein, the term "extract" includes any material obtained by extracting a component therefrom from a natural product, regardless of the method of extraction or the kind of the component. For example, it is a broad concept that includes all components obtained by extracting a component dissolved in a solvent from a natural product using water or an organic solvent, and those obtained by extracting only a specific component such as an oil such as oil.

Edema refers to a condition in which excess fluid, such as lymphatic fluid or tissue exudates, is present in tissues and is simply a symptom of swelling. Edema in the skin and soft tissues causes swelling, a sloppy feeling, and when pressed, the skin temporarily dents.

Edema may appear temporarily if you consume too much water or salt, or if you are tired or not able to get a good night's sleep, but in most cases it will go away on its own. In addition, heart disease, kidney disease, or blood circulation disorders in any part of the body may occur, and in women, edema may occur during normal pregnancy or pregnancy addiction. When the permeability of capillaries increases, local edema may also occur, for example, in the case of burns, trauma, local inflammation, and allergic reactions.

On the other hand, since the skin around the eyes is thinner than other parts, it is easy to feel swollen if there is excess liquid such as lymphatic fluid or tissue exudates and / or excessive accumulation of lipids.

Coffee berry belongs to the nectarine and is also called coffee cherry. Due to the large crossroads and fertile land, well-drained and well-grown dry and wet seasons, they are cultivated mainly in tropical rainfalls and produce good varieties in high altitudes from 1000m to 3000m above sea level. Tropical and subtropical regions between 28 and 30 degrees north latitude are suitable for cultivation.

Biter orange is a plant fruit tree belonging to the dicotyledonous rats and the citrus tree family. It is known to be resistant to cold and to adapt to climate climate such as high temperature, dryness and low humidity. The size of the fruit is slightly larger than orange, and it is used as a fragrance or food flavor or as a herbal medicine.

Lipoxygenase is an enzyme related to lipid and arachidonic acid metabolism, and is known to exhibit hyperlipidation inhibition, lipid inhibition, antioxidant, anti-inflammatory, and anti-allergic effects when inhibited.

The composition containing one or more selected from the group consisting of coffee berry extract and beater orange flower extract according to the present invention as an active ingredient has the effect of reducing edema and inhibiting the activity of lipoxygenase to inhibit or prevent edema and promote lipid inhibition. . In particular, it may have an effect of reducing edema and an effect of inhibiting hyperlipidation, and thus may be effective in alleviating or preventing symptoms of swelling of the eyes. The composition can further inhibit blood circulation disorders and skin aging by inhibiting or preventing edema. Inhibiting lipids can also inhibit obesity, cholesterol-related diseases including hyperlipidemia, high blood pressure, and other cardiovascular diseases. This effect is even better when it contains a coffee berry extract and a bitter orange flower extract. The composition according to the present invention has the advantage that it is safe to the human body and can be continuously used as an active ingredient extracted from natural plants. It is also less accessible than other drugs, making it more accessible.

The coffee berry extract or the beater orange flower extract of the composition according to the present invention may be obtained by extracting the coffee berry or the beater orange flower at a room temperature with a low molecular weight extraction method under ultrahigh pressure (1000 atm, 100 MPa) using only water as a pressure medium. This method can penetrate water into plant cells to extract very low-molecular (nano) -enriching substances, which not only extract a large amount of low-molecular amino acids and peptides, but also reduce nutrient destruction using low-temperature methods. It has the advantage of maintaining the natural color. Meanwhile, the coffee berry extract or the bitter orange flower extract used in the present invention may be prepared by a conventional method known in the art by extracting the coffee berry or the bitter orange flower with an organic solvent such as water or ethanol, and commercially available in the form of an extract. You can also use the product.

In a composition containing at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract according to an embodiment of the present invention, the at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract is a total composition It may be contained in 0.01 to 30% by weight based on the weight of water, respectively. In a composition containing at least one selected from the group consisting of a coffee berry extract and a bitter orange flower extract according to another embodiment, at least one selected from the group consisting of a coffee berry extract and a bitter orange flower extract is added to the total composition weight It may be contained in 0.01 to 40% by weight, respectively. In a composition containing at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract according to another embodiment, the at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract is the total composition weight It may be contained in an amount of 0.01 to 50% by weight, respectively. When the active ingredient is contained in less than 0.01% by weight relative to the total weight of the composition, it is difficult to obtain the expected effect, when contained in more than 50% by weight may cause problems of skin irritation.

On the other hand, in a composition containing the coffee berry extract and the beater orange flower extract according to an embodiment of the present invention as an active ingredient, the coffee berry extract and the beater orange flower extract may be contained in an amount of 0.01 to 80% by weight based on the total weight of the composition have. If the active ingredient is contained in less than 0.01% by weight based on the total weight of the composition, it is difficult to obtain the expected effect, when contained in more than 80% by weight may cause problems in formulation stability. In a composition containing at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract according to another embodiment of the present invention as an active ingredient, when the coffee berry extract and the beater orange flower extract are included together, the coffee berry When the weight ratio of the extract and the beater orange flower extract is 1-10: 1-10, the edema suppression effect is better. In a composition containing at least one selected from the group consisting of a coffee berry extract and a beater orange flower extract according to another embodiment of the present invention as an active ingredient, the coffee berry extract and the beater orange flower extract together, the coffee The weight ratio of the berry extract and the bitter orange flower extract may be 1: 1.

The present invention can provide a cosmetic composition comprising a composition containing at least one selected from the group consisting of coffee berry extract and beater orange flower extract as an active ingredient. The cosmetic composition may for example be a cosmetic, the appearance of which contains cosmetically or dermatologically acceptable media or bases. These are all formulations suitable for topical application, e.g. emulsions obtained by dispersing the oil phase in solutions, gels, solids, pasty anhydrous products, aqueous phases, emulsions obtained by dispersing the aqueous phase in oil phases, multiemulsions, suspensions, micro emulsions, micro It may be provided in the form of capsules, microgranules or ionic (liposomal) and nonionic vesicle dispersants, or in the form of creams, skins, lotions, powders, ointments, sprays, cleansers or concealed sticks. These compositions may be prepared according to conventional methods in the art. The composition according to the invention can also be used in the form of a foam or in the form of an aerosol composition further containing a compressed propellant.

Cosmetic compositions may include fatty substances, organic solvents, solubilizers, thickeners, gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, fillers Cosmetics or skin, such as metal ion sequestrants, chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or any other ingredients commonly used in cosmetics It may contain adjuvants commonly used in the scientific field. Such adjuvants are introduced in amounts generally used in the cosmetic or dermatological fields.

The cosmetic composition is not particularly limited in formulation, and may be appropriately selected in accordance with the desired purpose. The formulations may be prepared as eye care products including eye creams, eye essences, eye packs, izone bright formulations, eye shadows, eye foundations. Also, supple cosmetics (skin lotion and milk lotion), nourishing cream, essence, nourishing cream, massage cream, pack, gel, essence, cleansing cream, cleansing foam, cleansing water, pack, powder, cleanser, body lotion, body cream, body It may be prepared in one or more formulations selected from the group consisting of oils and body essences, but is not limited thereto.

In addition, the present invention may provide a pharmaceutical composition comprising a composition containing at least one selected from the group consisting of coffee berry extract and bitter orange flower extract as an active ingredient.

When the composition according to the present invention is applied to a medicament, the composition can be formulated into an oral or parenteral dosage form in the form of solid, semi-solid or liquid by adding a commercially available inorganic or organic carrier. If the active ingredient of the present invention is carried out according to the conventional method, it can be easily formulated, and it can be easily formulated with surfactants, excipients, colorants, spices, stabilizers, preservatives, preservatives, wetting agents, emulsifiers, suspending agents, salts for controlling osmotic pressure and / or Buffers and other commercial auxiliaries can be used as appropriate.

As the preparation for oral administration, tablets, pills, granules, soft and hard capsules, powders, fine granules, powders, solutions, emulsions, syrups, pellets, etc. Can be mentioned. These formulations contain, in addition to the active ingredient, diluents (e.g. lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and glycine), glidants (e.g. silica, talc, stearic acid and its magnesium or calcium salts and polyethylene glycols) It may contain. Tablets may also contain binders such as magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and polyvinylpyrrolidine, optionally starch, agar, alginic acid or its sodium salt Pharmaceutical additives such as disintegrants, absorbents, colorants, flavors, and sweeteners. The tablets can be prepared by conventional mixing, granulating or coating methods.

In addition, the parenteral administration agent may be, for example, an external preparation for skin, and may be an injection, drop, lotion, ointment, gel, cream, suspension, emulsion, suppository, patch or spray formulation. It is not limited to this.

The pharmaceutical composition according to the present invention may be administered orally, parenteral, rectal, topical, transdermal, intravenous, intramuscular, intraperitoneal, subcutaneous.

In addition, the dosage of the active ingredient will depend on the age, sex, weight of the subject to be treated, the specific disease or pathology to be treated, the severity of the disease or pathology, the route of administration and the judgment of the prescriber. Dosage determination based on these factors is within the level of skill in the art. Typical dosages are 0.001 mg / kg / day to 2000 mg / kg / day, more specifically 0.5 mg / kg / day to 2.5 mg / kg / day.

Hereinafter, the configuration and effects of the present invention will be described in more detail with reference to Examples, Comparative Examples and Experimental Examples. However, these Examples, Comparative Examples and Experimental Examples are provided only for the purpose of illustration in order to facilitate understanding of the present invention, and the scope and scope of the present invention is not limited by the following Examples, Comparative Examples and Experimental Examples.

[Examples 1-3 and Comparative Example 1]

(1) Preparation of Extract

First, 300 g of coffee berry was extracted using a low molecular weight extraction method under ultrahigh pressure (1000 atm, 100 MPa) using only water as a pressure medium at room temperature. Vita orange flower 300g, and 150g coffee berry and 150g mixed with a mixture of 150g each of the methanol was cut into 3g methyl alcohol and boiled at 100 ℃ in an extractor with a cooling condenser for 8 hours to obtain an extract.

(2) Preparation of Examples and Comparative Examples

In Examples 1 to 3 and Comparative Example 1 were prepared in the same content composition as Table 1. Example 1 is a coffee berry extract, Example 2 is a bitter orange flower extract, Example 3 is a coffee berry extract and a bitter orange flower extract at 1.0% by weight, respectively, Comparative Example 1 is added the active ingredient Not prepared as a control.

First, stearic acid, hydrogenated oil, pentaerythritol tetraethylhexanoate as an oil phase were dissolved after heating at 75 ° C., and the remaining components were mixed in an aqueous phase. The oil phase was slowly added to the aqueous phase and homomixed at 7000 rpm for 3 minutes to prepare Examples 1 to 3 and Comparative Example 1.

ingredient Example 1 Example 2 Example 3 Comparative Example 1 Purified water Balance Balance Balance Balance Stearic acid 1.0 1.0 1.0 1.0 Hydrogenated Oil 0.5 0.5 0.5 0.5 Pentaerythritol tetraethylhexanoate 2.0 2.0 2.0 2.0 Coffee Berry Extract 1.0 - 1.0 - Bitter Orange Flower Extract - 1.0 1.0 - Spices a very small amount a very small amount a very small amount a very small amount antiseptic a very small amount a very small amount a very small amount a very small amount Polyacrylamide, C ₁₃ -C ₁₄ Isoparaffin, Laureth-7 2.5 2.5 2.5 2.5

Experimental Example 1 Evaluation of Edema Suppression and Prevention Effect

Edema inhibition and prevention effect of the composition according to the present invention was evaluated through experiments using Examples 1 to 3 and Comparative Example 1 prepared above. Among women between 20 and 40 years old, 120 women with idiopathic edema were randomly divided into 4 groups, and each of Examples 1 to 3 and Comparative Example 1 was washed twice daily each evening, followed by an appropriate amount for facial and limbs for 8 weeks. Corrected. The improvement effect of the edema was evaluated as a very effective, effective, slightly effective, and invalid phase by observing the improvement of facial and limbs after the end of the use experiment.

The eight-week experimental results are shown in Table 2 below. In the evaluation results by dividing each step, scores of 3 points for very effective, 2 points for validity, 1 point for validity, and 0 points for invalidity were calculated.

Effectiveness (%) = [{(Sum of each step × number of people in each step)} / (3 × number of people)] × 100

For example, the effective rate of Example 1 may be calculated as {(3 × 3 + 15 × 2 + 10 × 1 + 2 × 0) / (3 × 30)} × 100 = 54.4%, and Example 2 The effective rate of {(4 × 3 + 13 × 2 + 9 × 1 + 4 × 0) / (3 × 30)} × 100 = 52.2%, and the effective rate of Example 3 was {(8 × 3 + 16 × 2 + 6 × 1 + 0 × 0) / (3 × 30)} × 100 = 68.9%, and the effective rate of Comparative Example 1 is {(0 × 3 + 1 × 2 + 3 × 1 + 26 × 0) / ( 3 × 30)} × 100 = 5.6%.

step Example 1 Example 2 Example 3 Comparative example Very effective 3 4 8 0 Valid (persons) 15 13 16 One Slightly effective 10 9 6 3 Invalid (persons) 2 4 0 26 Effective rate (%) 54.4 52.2 68.9 5.6

As can be seen in Table 2, Examples 1 to 3 was found to be overwhelmingly high effective rate compared to Comparative Example 1 was able to confirm the excellent edema suppression and prevention effect, of which both coffee berry extract and bitter orange flower extract It was the most excellent in suppressing and preventing the edema of Example 3 containing. Therefore, it was confirmed that the composition containing one or more selected from the group consisting of coffee berry extract and beater orange flower extract of the present invention as an active ingredient has an effect of inhibiting or preventing edema. On the other hand, no skin irritation was observed at the sites where Examples 1 to 3 were applied.

EXAMPLE 4, 5, and 6

First, 300 g of the coffee berry was extracted with a low molecular weight extraction method under ultrahigh pressure (1000 atm, 100 MPa) using only water as a medium as a pressure medium at room temperature, and filtered with a 300 mesh filter paper. After standing for one week, the obtained precipitate was filtered twice with Edbentech No. 5 filter paper and Whatman GFC 47 mm filter paper. Then, the resultant was concentrated completely at 50 ° C. using a reduced pressure concentrator to obtain 125.4 g of dry weight.

Vita orange flower 300g, and coffee berry 150g and the mixture of 150g vita orange flower were cut into pieces and put into 3 kg of methyl alcohol, respectively, and extracted by boiling at 100 ° C for 8 hours in an extractor equipped with a cooling condenser. Each was then filtered through 300 mesh filter paper, left for 1 week, and then the precipitate was filtered twice with Edbentech No. 5 filter paper and Whatman GFC 47 mm filter paper. Then, the resultant was concentrated completely at 50 ° C. using a vacuum concentrator to obtain dry weights of 137.8 g and 136.0 g, respectively.

Table 3 below shows the results of each extraction by the extraction method described above.

Sample amount (g) Yield (g) Example 4 300 125.4 Example 5 300 137.8 Example 6 300 136.0

Experimental Example 2

The inhibitory effect on lipoxygenase of Examples 4, 5, and 6 was measured, and quercetin was used as a control.

The experiment was performed using the TBAS method, and linoleic acid, lipoxygenase, thiobabituric acid, and quercetin used in the experiment were those of SIGMA. First, 0.05 ml of Examples 4, 5, 6, and quercetin at various concentrations (5, 10, and 30 ppm) were added to 1 ml of 1 mM linoleic acid, and 0.95 ml of lipoxygenase was added, followed by stirring at 25 ° C. for 10 minutes. Thereafter, 0.5 ml of trichloroacetic acid was administered, 1 ml of thiobarbituric acid was added, and then heated for 10 minutes, and then cooled in ice water for 2 to 3 minutes to terminate the reaction. After the reaction was completed, 2 ml of butanol was added to the reaction solution, and centrifuged at 4000 rpm for 5 minutes, and the absorbance was measured at 535 nm. In this case, purified water was used instead of each test material as a blank test (0 ppm).

Equation 2 was used to determine the inhibitory effect of lipoxygenase activity and the results are shown in Table 4 below.

% Inhibitory effect of lipoxygenase activity = 100-{(reaction absorbance of each test substance / control absorbance of control) x100}

Concentration (ppm) Inhibitory effect of lipoxygenase activity (%) Example 4 Example 5 Example 6 Quercetin 0 0 0 0 0 5 18.71 10.42 24.02 27.64 10 40.78 36.62 62.14 61.49 30 80.13 76.89 93.98 94.64

As can be seen from Table 4, Examples 4, 5 and 6 were all recognized to have an inhibitory effect on lipoxygenase activity. All of them increased the inhibitory effect of lipoxygenase activity as the concentration, especially Example 6 showed a similar effect of lipoxygenase activity similar to quercetin, a positive control.

Based on the experimental results of Table 4, the free radical 50% scavenging concentration (IC ₅₀ ) is calculated and shown in Table 5.

Example 4 Example 5 Example 6 Quercetin IC ₅₀ (ppm) 17.12 18.66 12.93 12.63

Among them, the free radical 50% scavenging concentration (IC ₅₀ ) of Example 6 was almost the same as quercetin. Considering that quercetin is a single substance while Example is an extract, the lipoxygenase activity inhibitory effect of Example 6 is better than quercetin, and is considered to be more effective in terms of use and production cost.

Coffee berry extract and bitter orange flower extract having an excellent inhibitory effect of lipoxygenase activity as described above can inhibit hyperlipidation and promote lipid inhibition.

Hereinafter, a formulation example of a cosmetic composition and a pharmaceutical composition comprising a composition containing at least one selected from the group consisting of a coffee berry extract and a bitter orange flower extract according to the present invention as an active ingredient, but the cosmetic composition and the pharmaceutical composition Is applicable to various formulations, which are intended to explain in detail only, not to limit the invention.

[Formulation Example 1] Ointment in the external preparation for skin

The ointment was prepared in a conventional manner according to the composition described in Table 6.

ingredient Content (% by weight) Purified water Balance glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Coffee Berry & Bitter Orange Flower Extract 1.0 Caprylic / Capric Triglycerides 3.0 Squalane 1.0 Cetearyl Glucoside 1.5 Sorbitan stearate 0.4 Cetearyl Alcohol 1.0 antiseptic Quantity incense Quantity Pigment Quantity Beeswax 4.0

Formulation Example 2 Softening Cosmetic (Skin Lotion)

According to the composition described in Table 7 was prepared in a flexible method in a conventional manner.

Compounding ingredient Content (% by weight) Coffee Berry & Bitter Orange Flower Extract 0.1 glycerin 3.0 Butylene glycol 2.0 Propylene glycol 2.0 Carboxy Vinyl Polymer 0.1 Fiji-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 Preservative, coloring, fragrance Quantity Purified water Balance

Formulation Example 3 Nutrition Cream

Nutritional cream was prepared in a conventional manner according to the composition shown in Table 8.

ingredient Content (% by weight) Purified water Balance glycerin 3.0 Butylene glycol 3.0 Liquid paraffin 7.0 Beta Glucan 7.0 Carbomer 0.1 Coffee Berry & Bitter Orange Flower Extract 3.0 Caprylic / Capric Triglycerides 3.0 Squalane 5.0 Cetearyl Glucoside 1.5 Sorbitan stearate 0.4 Polysorbate 60 1.2 antiseptic Quantity incense Quantity Pigment Quantity Triethanolamine 0.1

Formulation Example 4 Massage Cream

To prepare a massage cream in a conventional manner according to the composition shown in Table 9.

ingredient Content (% by weight) Purified water Balance glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 45.0 Beta Glucan 7.0 Carbomer 0.1 Coffee Berry & Bitter Orange Flower Extract 1.0 Caprylic / Capric Triglycerides 3.0 Beeswax 4.0 Cetearyl Glucoside 1.5 Sesqui oleic acid sorbitan 0.9 Vaseline 3.0 antiseptic Quantity incense Quantity Pigment Quantity paraffin 1.5

[Formulation Example 5] Pack

To prepare a pack in a conventional manner according to the composition described in Table 10 below.

ingredient Content (% by weight) Purified water Balance glycerin 4.0 Polyvinyl alcohol 15.0 Hyaluronic acid extract 5.0 Beta Glucan 7.0 Allantoin 0.1 Coffee Berry & Bitter Orange Flower Extract 0.5 Nonyl Phenyl Ether 0.4 Polysorbate 60 1.2 antiseptic Quantity incense Quantity Pigment Quantity ethanol 6.0

Claims (7)

A composition for inhibiting or preventing edema containing at least one selected from the group consisting of coffee berry extract and beater orange flower extract as an active ingredient. A lipoxygenase inhibitory composition containing at least one selected from the group consisting of coffee berry extract and beater orange flower extract as an active ingredient. A lipid inhibition promoting composition comprising as an active ingredient at least one selected from the group consisting of coffee berry extract and bitter orange flower extract. 4. The method according to any one of claims 1 to 3, The composition comprises 0.01 to 50% by weight, respectively, of at least one selected from the group consisting of coffee berry extract and beater orange flower extract, based on the total weight of the composition. 4. The method according to any one of claims 1 to 3, The composition comprises a coffee berry extract and a bitter orange flower extract as an active ingredient. The method of claim 5, The composition comprises a coffee berry extract and a bitter orange flower extract in an amount of 0.01 to 80% by weight based on the total weight of the composition. The method of claim 5, The weight ratio of the coffee berry extract and the beater orange flower extract is a composition, characterized in that 1-10: 1-10.