JP2008074814A - Lipolysis promoter - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide medicines and external preparations, excellent in effects of promoting lipolysis in cells. <P>SOLUTION: The lipolysis promoter comprises ingredients (A) and (B): (A) extracts of Rubus plants, and (B) extracts of a plant selected from Aesculus plants, Hamamelis plants, rutaceous family plants and Ruscus plants. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

  The present invention relates to a lipolysis promoter and a skin external preparation for squeezing that promote intracellular lipolysis, reduce systemic or local adipose tissue, and are excellent in convergence and slimming effects.

  The living body always maintains the homeostasis by adjusting the balance between the intake energy and the consumption energy. However, due to various factors such as lifestyle and diet, fat metabolism in the living body is not performed well, and fat accumulation and so-called obesity occur.

  In the living body, fat cells exist, and not only the excessively consumed energy is stored in the cells as fat droplets but also a biological function regulating substance is secreted. When the accumulation of visceral fat is large, various diseases such as arteriosclerosis are likely to be caused, and therefore prompt improvement is required. Further, when the accumulation of subcutaneous fat is large, it is a big problem from the viewpoint of beauty regardless of gender. In particular, due to the recent increase in interest in health and beauty, there is an increasing number of people who want to make their bodies healthy and slim regardless of age or gender. Interested in.

Conventionally, in order to suppress, prevent, and improve obesity, people perform dietary restrictions such as dietary restrictions and health food intake. There are also people who work on aerobic whole body exercise such as aerobics.
In addition, xanthine derivatives such as caffeine, various drugs having a lipolysis-promoting action such as capsaicin, dihydrocapsaicin, nordihydrocapsaicin contained in red pepper, or external preparations containing those related substances as active ingredients have been developed. .
However, in any of the above methods, obesity prevention, improvement effect, and squeezing effect are not always sufficient, and there are problems that individual differences are large and that it is difficult to accept as a habit.

On the other hand, some plant extracts have various pharmacological actions. For example, the raspberry extract has a blood circulation promoting action (Patent Document 1), a melanin production inhibitory action (Patent Document 2), an antiallergic action (Patent Document 3), an acne improvement, and a smoothness / moistness imparting action to the skin ( Patent Document 4) and matrix protease inhibitory action (Patent Document 5) have been reported to be effective.
JP 2001-048740 A JP-A-11-335233 JP-A-9-124498 Japanese Patent Laid-Open No. 3-188008 JP 2003-160433 A

  An object of the present invention is to provide a lipolysis promoter and a skin external preparation for squeezing which are excellent in intracellular lipolysis promotion effect.

  Therefore, the present inventor paid attention to the raspberry extract and examined its physiological action, and surprisingly had an excellent lipolysis promoting effect, and further, the raspberry extract and the genus Tochinoki, witch hazel, citrus or It has been found that the combined use with a plant extract of the genus Nagiikada significantly enhances its lipolysis promoting effect, and the present invention has been completed.

That is, the present invention includes the following components (A) and (B):
(A) extract of raspberry plant,
(B) an extract of a plant selected from the genus Tochinoki, the witch genus plant, the citrus family plant and the genus Nigida
The present invention provides a lipolysis promoter containing, and a skin external preparation for squeezing.

  Since the use of the preparation for accelerating lipolysis and squeezing the skin according to the present invention significantly promotes the degradation of fat in the cells, it is useful as a medicament and cosmetic for improving obesity, squeezing and slimming.

  The component (A) used in the present invention is an extract of the genus Rubus. The extract of the genus Rubus can be obtained from the whole plant, leaves, stems, flowers, fruits, pericarps, seeds, and roots of the plant, and is preferably an extract of the roots. Examples of the raspberry genus plant include raspberry, oni strawberry, blackberry, wedge strawberry, and the like, more preferably an extract of oni strawberry (Rubus elipticus) or raspberry, particularly preferably an extract of oni strawberry root.

  The component (B) used in the present invention is an extract of a plant selected from the genus Planta, the witch plant, the citrus plant, and the genus Nigida. An extract of the genus Amanita can be obtained from leaves, flowers, fruits, fruit skins, seeds, roots, and bark of the plant, and is preferably an extract of the seeds and leaves. Examples of the plant belonging to the genus Tochinoki include horse chestnut, cypress, and the like. More preferred is an extract of horse chestnut (Aesculus hippocastanum), and particularly preferred is an extract of seed or leaf of horse chestnut.

  The extract of the genus plant can be obtained from the leaves, flowers, fruits, fruit skin, seeds, roots, and bark of the plant, and is preferably an extract of the leaves and bark. Examples of the plants belonging to the genus are Clam squirrel, Atezmansaku and Sinamansaku. More preferred is an extract of Hamamelis virginiana, and particularly preferred is an extract of a leaf or bark of Hamelis.

  Citrus plant extracts can be obtained from the leaves, flowers, fruits, peels, seeds, roots, and bark of the plants, but are preferably extracts of the fruits (mature, immature, pulp, peel, etc.). . Citrus plants include citrus, mandarin orange, orange, lemon, kumquat, karatachi, salamander and the like. More preferred is an extract of citrus junos, and particularly preferred is an extract of a fruit body of citron.

  An extract obtained from a plant belonging to the genus Nagiida can be obtained from leaves, flowers, fruits, fruit skins, seeds, roots, and bark of the plant, and is preferably an extract of the roots. As the plant belonging to the genus Nagiida, there is Nagiikada. More preferably, it is an extract of Nagi Ikada (Ruscus acculeatus), and particularly preferably an extract of Nagi Ikada root.

  As the component (B), an extract of a genus Toxinaceae plant, a witch genus plant, a citrus family plant or a genus genus plant may be used alone, or two or more of these may be used in combination.

  In the present invention, the plant extract is an extract obtained by pulverizing or pulverizing various parts of these plants without drying or drying, and extracting them with a solvent, or the extract. Non-volatile components obtained by evaporating the extraction solvent from lyophilized or lyophilized. The extraction solvent is not particularly limited, but water, alcohol (lower alcohols such as methanol and ethanol, polyhydric alcohols such as ethylene glycol, propylene glycol, and 1,3-butylene glycol), acetone, methyl ethyl ketone, and the like. Various solvents such as ketones, ethers such as diethyl ether and tetrahydrofuran, aromatics such as toluene, higher alcohols and the like can be mentioned, and these can be used alone or in combination of two or more. Of these extraction solvents, water and / or alcohol are preferred.

  The content of the component (A) in the lipolysis accelerator and the skin external preparation for squeezing of the present invention is 0.0001 to 50% by mass, further 0.001 to 10% in terms of solid matter, from the viewpoint of the effect of promoting lipolysis. % By mass, particularly 0.001 to 5% by mass is preferred. In addition, the content of the component (B) is 0.0001 to 50 mass in terms of solid content from the viewpoint of the lipolysis promoting effect, particularly the enhancing effect of the lipolysis promoting effect by the combined use of the component (A) and the component (B). %, More preferably 0.001 to 10% by mass, and particularly preferably 0.001 to 5% by mass. Further, the content ratio (mass ratio) of the component (A) and the component (B) is 1: 100 to 100: 1, more preferably 1:50 to 50: in terms of solid content, from the viewpoint of enhancing the effect of promoting lipolysis. 1, especially 1:10 to 10: 1 is preferred.

  As shown in the Examples below, the Raspberry genus plant extract alone has a lipolysis promoting action of adipocytes, and is an extract of Raspberry genus plants, Toxinaceae plants, Witch genus plants, Citrus plants, or Nagiidae plants When used together, the lipolysis promoting action is remarkably enhanced. Therefore, when the lipolysis promoter of the present invention is used, systemic or local cell lipolysis is promoted, and it is useful as a medicament and cosmetic for improving obesity, tightening and slimming. The lipolysis promoter may be administered orally or externally applied to the skin, but is preferably applied externally to the skin. It is particularly preferable to use it as a skin external preparation for tightening.

  The dosage form of the skin external preparation for squeezing of the present invention is not particularly limited, and includes solutions, emulsions, creams, gels, ointments, liquids, powders, pastes, poultices, plasters, aerosols, etc. Various dosage forms applicable for external use can be obtained.

  The skin external preparation for squeezing according to the present invention can enhance the moist feeling of the skin by using various oil components together. Examples of the oil component used in the present invention include, but are not limited to, fats and oils, waxes, hydrocarbons, higher fatty acids, higher alcohols, esters, essential oils, silicone oils, and the like. Examples of the fats and oils include soybean oil, nutka oil, jojoba oil, avocado oil, almond oil, olive oil, cacao oil, sesame oil, persic oil, castor oil, coconut oil, mink oil, beef fat, pork fat and the like, and these Hardened oil obtained by hydrogenation of natural fats and oils and synthetic triglycerides such as myristic acid glyceride and 2-ethylhexanoic acid triglyceride; waxes include, for example, carnauba wax, whale wax, beeswax, lanolin and the like; hydrocarbons For example, liquid paraffin, petrolatum, paraffin microcrystalline wax, ceresin, squalane, bristan etc .; higher fatty acids include, for example, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, linoleic acid, Linolenic acid, lanolinic acid, isostearic acid, etc .; Examples of the class alcohols include lauryl alcohol, cetyl alcohol, stearyl alcohol, oleyl alcohol, lanolin alcohol, cholesterol, 2-hexyldecanol, etc .; examples of the esters include cetyl octanoate, triglyceride octanoate, myristyl lactate, cetyl lactate, Examples of essential oils include mint oil, jasmine, isopropyl myristate, myristyl myristate, octyldodecyl myristate, isopropyl palmitate, isopropyl adipate, butyl stearate, decyl isoleate, cholesterol isostearate, POE sorbite fatty acid ester, etc. Oil, pepper brain oil, cypress oil, spruce oil, ryu oil, turpentine oil, cinnamon oil, bergamot oil, mandarin oil, ginger oil, pine , Lavender oil, bay oil, clove oil, hiba oil, rose oil, eucalyptus oil, lemon oil, thyme oil, peppermint oil, rose oil, sage oil, menthol, cineole, eugenol, citral, citronellal, borneol, linalool, geraniol, Camphor, thymol, spirantol, pinene, limonene, terpene compounds, etc .; examples of silicone oils include dimethylpolysiloxane. These oily components described above can be used alone or in combination of two or more. In the present invention, among these, myristic acid glyceride, 2-ethylhexanoic acid triglyceride, lanolin, liquid paraffin, petrolatum, paraffin microcrystalline wax, squalane, lauric acid, myristic acid, palmitic acid, linoleic acid, linolenic acid, isostearic acid , Cetyl alcohol, stearyl alcohol, oleyl alcohol, cholesterol, cetyl octanoate, triglyceride octanoate, isopropyl myristate, octyldodecyl myristate, cholesterol isostearate, POE sorbite fatty acid ester, peppermint oil, spruce oil, cinnamon oil, rose Oil, menthol, cineol, eugenol, citral, citronellal, geraniol, pinene, limonene, dimethylpolysiloxane It is preferable to use.

  The content of the oil component can be appropriately selected according to the dosage form (form) of the skin external preparation for squeezing, and can usually be 0.1 to 95% by mass in the total amount of the composition.

  In addition, the skin external preparation for squeezing of the present invention includes surfactants, solvents, humectants, astringents, lipolysis accelerators, polymer compounds used in various pharmaceutical and cosmetic preparations in addition to the oily components described above. UV absorbers, anti-inflammatory agents, bactericides, antioxidants, sequestering agents, preservatives, vitamins, pigments, fragrances and the like can be blended.

  As the surfactant, any of anionic, cationic, nonionic, natural, and synthetic surfactants can be used, but it is preferable to use a nonionic surfactant in consideration of irritation to the skin. Nonionic surfactants include, for example, glycerin fatty acid ester, propylene glycol fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, tetraoleic acid polyoxyethylene sorbitol, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene Examples include glycol, polyoxyethylene polyoxypropylene alkyl ether, polyethylene glycol fatty acid ester, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and alkyl glycoside.

The following components can be further blended in the skin external preparation for squeezing of the present invention, but the components are not limited to these.
(A) Dyes: recognized as food additives such as tar dyes I and II dyes, chlorophyll, riboflavin, crocin, safflower, anthraquinone, etc. stipulated in the Ordinance of the Ministry of Health and Welfare such as Yellow No. 4, Blue No. 1, Yellow No. 202, etc. Natural pigments that are used.
(B) Vitamins; vitamin A, vitamin C, vitamin D, vitamin E, and various derivatives thereof.
(C) Others: bactericides, preservatives, other ingredients necessary for the preparation, etc.

  EXAMPLES Hereinafter, although an Example is given and this invention is demonstrated in detail, this invention is not limited to these Examples. The extracts 1 to 6 used in the examples are as follows.

Extract 1
100 g of dried fruits of Rubus Idaeus were extracted with a 50% aqueous ethanol solution by a conventional method, concentrated under reduced pressure, and then freeze-dried. This was a raspberry extract.

Extract 2
100 g of dried roots of oni strawberry (Rubus ellipticus) was extracted with a 50% aqueous ethanol solution by a conventional method, filtered, concentrated under reduced pressure, and then freeze-dried. This was used as the oni strawberry extract.

Extract 3
100 g of dried fruit peel of Citrus Junos was extracted with a 50% aqueous ethanol solution by a conventional method, filtered, concentrated under reduced pressure, and then lyophilized. This was used as a yuzu extract.

Extract 4
100 g of dried leaves of Hamamelis virginiana were extracted with a 50% aqueous ethanol solution by a conventional method, filtered, concentrated under reduced pressure, and then lyophilized. This was used as a Hamelis extract.

Extract 5
100 g of dried seeds of horse chestnut (Aesculus hippocastanum) was extracted with a 50% aqueous ethanol solution by a conventional method, filtered, concentrated under reduced pressure, and then freeze-dried. This was a horse chestnut extract.

Extract 6
100 g of dried rhizomes of Rubus aculeatas were extracted with a 50% aqueous ethanol solution by a conventional method, concentrated under reduced pressure, and then lyophilized. This was designated as Nagyakada extract.

Example 1
Using Compositions 1-5, Extracts 1-6 and Component 1, their lipolysis promoting action was examined by the following test method. The results are shown in Table 1.

Test Method Preparation of Adipocytes A free adipocyte solution was prepared from a testicular adipose tissue of Wistar male rats using a collagenase solution. This adipocyte solution was seeded on a 96-well plate, added to this so that the test substance concentration was 400 μg / mL, and cultured for 1.5 hours. After completion of the culture, the free fatty acid was measured with NEFA-C Test Wako (Wako Pure Chemical Industries, Ltd.).

The calculation method of the lipolysis promoting action is as follows.
Lipolysis promotion rate (%) = A / B × 100
A: Free fatty acid amount when test sample is added B: Free fatty acid amount when test sample is not added (control)

  From the above results, when 400 μg / mL of the test substance is allowed to act on the fat cells, the compositions 1 to 5 have a significant effect of enhancing lipolysis when compared with the case where the extracts 1 to 6 and component 1 are allowed to act. Was recognized.

  Although the example of the skin external preparation of this invention is shown below, it is not limited to these. In addition, the plant extract used below used what melt | dissolved the previous extracts 1-6 in 1% with 50% ethanol aqueous solution.

Example 2 (skin lotion)

  B was added to A while stirring, and C was added in order to mix well to obtain a lotion.

Example 3 (milky lotion)

  A and B are heated to 80 ° C. in separate containers. Add A to B and mix well. After adding C, it was cooled, and D was added to make it uniform to obtain an emulsion.

Example 4 (Cream)

  Heat A and B to 80 ° C. in separate containers. Mix B with A while stirring and cool. C was added to make a uniform cream.

Example 5 (Bath oil)

  Bath oil was obtained by adding B to A with thorough mixing.

Example 6 (a poultice)

  The above components were mixed thoroughly with a kneader, and this plaster was coated on a non-woven fabric by a conventional method to obtain a patch.

Example 7 (cleaning fee)

  A and B are heated to 80 ° C. in separate containers, and B is added to A. Cooling with stirring, C was added to obtain a cleaning material.

Example 8 (aerosol)

  Aerosol was obtained by filling A and B into a pressure-resistant container for aerosol.

Claims (6)

The following components (A) and (B):
(A) extract of raspberry plant,
(B) an extract of a plant selected from the genus Tochinoki, the witch genus plant, the citrus family plant and the genus Nigida
A lipolysis promoter containing   The lipolysis promoter according to claim 1, wherein the component (A) is an extract of Oni strawberry.   The lipolysis promoter according to claim 1 or 2, wherein the component (B) is an extract of a plant selected from horse chestnut, hamamelis, yuzu and nagiikada. The following components (A) and (B):
(A) extract of raspberry plant,
(B) an extract of a plant selected from the genus Tochinoki, the witch genus plant, the citrus family plant and the genus Nigida
A skin external preparation for squeezing.   The external preparation for skin tightening according to claim 4, wherein component (A) is an extract of Oni strawberry.   The skin external preparation for squeezing according to claim 4 or 5, wherein the component (B) is an extract of a plant selected from horse chestnut, hammamels, yuzu and nagiikada.