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WO2020190015A1 - Composition s'appliquant par voie cutanée présentant un point de fusion contrôlé et une température de transition de phase de molécules de graisse, son procédé de préparation et sa méthode d'application - Google Patents

Composition s'appliquant par voie cutanée présentant un point de fusion contrôlé et une température de transition de phase de molécules de graisse, son procédé de préparation et sa méthode d'application Download PDF

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Publication number
WO2020190015A1
WO2020190015A1 PCT/KR2020/003669 KR2020003669W WO2020190015A1 WO 2020190015 A1 WO2020190015 A1 WO 2020190015A1 KR 2020003669 W KR2020003669 W KR 2020003669W WO 2020190015 A1 WO2020190015 A1 WO 2020190015A1
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Prior art keywords
melting point
composition
fat
phase transition
transition temperature
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Ceased
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PCT/KR2020/003669
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English (en)
Korean (ko)
Inventor
최성현
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Lipobiomed Corp
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Lipobiomed Corp
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Filing date
Publication date
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

Definitions

  • the present invention relates to a composition for application to the skin in which the melting point and the phase transition temperature of fat molecules are controlled, and a method of manufacturing the same.
  • Oil thickeners themselves are sometimes used as external preparations or cosmetics for skin protection, and in cosmetics and pharmaceuticals, they are mainly used as a method for imparting formulation stability and maintaining effective active substances on the skin surface for a long time.
  • petrolatum can be obtained by purifying an ointment-like substance obtained by solvent dewaxing the residual oil of vacuum distillation of crude oil, and its main component is a C24-C43 hydrocarbon, which is an amorphous substance.
  • White petrolatum which is highly purified and can be used in cosmetics and pharmaceuticals, is on the market.
  • Vaseline is frequently used in skin care cosmetics, makeup cosmetics, and skin external medicines to impart formulation stability and achieve target viscosity and hardness.
  • petrolatum has an excellent thickening effect, but generally has a low hardness, so that an excessively sticky formulation may be made, which has little stickiness and hinders the implementation of a formulation having an appropriate hardness.
  • petrolatum is a material obtained from the vacuum distillation residual oil of crude oil, and it is well known that it has the potential of environmental pollution and has toxicity that is unsuitable for application to sensitive skin or wounds.
  • the present invention has been conceived by the above necessity, and an object of the present invention is to provide a formulation of an external preparation or moisturizer that is structurally stable and physiologically safe in the epidermis.
  • the present invention is a melting point of a fat molecule prepared by mixing a composition of a neutral fat composition having a melting point of 37 °C ⁇ 44 °C and a polar fat composition having a melting point of 37 °C ⁇ 44 °C It provides a skin application composition with a controlled phase transition temperature.
  • the neutral fat composition having a melting point of 37°C to 44°C is prepared by mixing fat having a melting point lower than 36°C and fat having a melting point higher than ⁇ 44°C. It is preferable, but is not limited thereto.
  • the fat having a melting point lower than 36°C is shea butter, and the fat having a melting point higher than 44°C is preferably tripalmitin, but all fats having a corresponding temperature range are seen. It is included in the scope of the invention.
  • the mixing weight ratio of the shea butter and tripalmitin is preferably 4 to 16% of tripalmitin in the shea butter, but is not limited thereto.
  • the polar fat composition having a melting point of 37°C to 44°C is prepared by mixing a phospholipid having a melting point lower than 36°C and a phospholipid having a melting point higher than ⁇ 44°C. It is preferable, but is not limited thereto.
  • the phospholipid having a melting point lower than 36° C. is soy lecithin
  • the phospholipid having a melting point higher than 44° C. is preferably hydrogenated soy lecithin. All fats having a range are included in the scope of the present invention.
  • the weight ratio of the soybean lecithin and hydrogenated soybean lecithin is preferably mixed with soybean lecithin and hydrogenated soybean lecithin by 0.07% to 0.13%, but is not limited thereto.
  • the mixing weight ratio of the composition of the neutral fat composition having a melting point of 37 °C ⁇ 44 °C and the polar fat composition having a melting point of 37 °C ⁇ 44 °C is the polar fat in the triglyceride composition It is preferable to mix 4 to 8% of the composition, but is not limited thereto.
  • the final temperature of the composition is preferably 37 °C ⁇ 45 °C, but is not limited thereto.
  • the composition is preferably used for cosmetics or pharmaceuticals, but is not limited thereto.
  • the cosmetic composition described above is, for example, a solution, a gel, a solid or anhydrous product, an emulsion obtained by dispersing an oil phase in an aqueous phase, a suspension, a microemulsion, a microcapsule, a microgranular sphere or an ionic (liposome), a nonionic vesicle
  • a dispersant cream, skin, lotion, powder, ointment, spray or conceal stick.
  • it may be prepared in the form of a foam or an aerosol composition further containing a compressed propellant.
  • the above cosmetic composition may further include a solubilizing agent, a thickening agent and a gelling agent, an emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic or nonionic emulsifier, and a filler.
  • a solubilizing agent emollient
  • an antioxidant emollient
  • a suspending agent e.g., a suspending agent
  • a stabilizer e.g., a foaming agent
  • a fragrance e.g., emollient, emollient, emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, an ionic or nonionic emulsifier, and a filler.
  • Sequestering and chelating agents preservatives, vitamins, blockers, wetting agents, essential oils, dye
  • a solubilizing agent When used as an external skin preparation according to the present invention, additionally a solubilizing agent, a thickening agent and a gelling agent, an emollient, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, a surfactant, water, ionic or nonionic Type emulsifiers, fillers, sequestering and chelating agents, preservatives, vitamins, blockers, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic actives, lipid vesicles or any other ingredients commonly used in external preparations for skin and It may contain adjuvants commonly used in the same dermatological field. In addition, the above ingredients may be introduced in an amount generally used in the field of dermatology.
  • the present invention provides a composition for skin application in which the melting point of the fat molecule and the phase transition temperature are controlled by mixing a composition of a neutral fat composition having a melting point of 37°C to 44°C and a polar fat composition having a melting point of 37°C to 44°C.
  • a composition for skin application in which the melting point of the fat molecule and the phase transition temperature are controlled by mixing a composition of a neutral fat composition having a melting point of 37°C to 44°C and a polar fat composition having a melting point of 37°C to 44°C.
  • melting point When explaining the change in the properties of fat molecules according to temperature rise, neutral fat is called the melting point, and polar fat is called the phase transition temperature.
  • Two fats with different properties, polar fats and neutral fats, can be expressed as melting points in a comprehensive sense from the viewpoint that the distance and movement of the molecules at the tail (hydrocarbon region) of the molecules change as the temperature increases. Therefore, the two phenomena are referred to here as melting points.
  • Each body fat has its own melting temperature.
  • the melting point of visceral fat is 35°C
  • the fat extracted from the foot of the human body has a melting point of 0 to 10°C (Knut Schmidt-Nielsen Acta Physiologica Scandinavica, Volume 12, Issue 2-3 June 1946 Pages 123-129).
  • the melting point of phospholipids constituting the cell membrane is 10-20°C, much lower than body temperature (Heimburg T1, Jackson AD. Proc Natl Acad Sci U S A. 2005 Jul 12;102(28):9790-5.).
  • fat in the cell membrane has such a low melting point is to maintain the activity of fat molecules and membrane fluidity at a body temperature of 36.5°C, and visceral fat is in a semi-liquid state at normal body temperature. ), it can be interpreted as having the purpose of maintaining the fat storage form while suppressing the dispersion of fat molecules.
  • the fat coating the surface of the lungs has a high melting point of 41°C. This is interpreted as the purpose of obtaining a crystallized structure of the hydrocarbons of fat molecules at a temperature much higher than body temperature at 36.5°C. In other words, it is interpreted for the purpose of maintaining the intrinsic physiological function of finely coating the surface of the lungs by maintaining a planar structure without disturbance of fat molecules at body temperature, suppressing moisture evaporation, and reducing surface tension. In addition, it is interpreted that it is designed to protect the lung surface without being disturbed even at a temperature higher than the normal body temperature in preparation for excessive heat generation due to infection or inflammation.
  • Fats that make up the stratum corneum of the skin are mostly solid-crystalline or gel state at body temperature.
  • the epidermis maintains 32 degrees Celsius during active daytime and 35-36 degrees Celsius during sleep time. That is, fat present in the stratum corneum can be dissolved at a body temperature of 36.5°C, but it can be determined that it is mostly crystallized at an actual epidermal temperature.
  • fat accumulated in cells or intestines has a melting point lower than body temperature
  • fat present on or outside the body is composed of fat having a melting point higher than body temperature. That is, fat inside the human body maintains high fluidity for replacement, circulation, and metabolism of fat molecules, and fat outside the body uses less fluid fat with little to no disturbance of fat molecules.
  • This patent is a dual combination composition of a composition of triglycerides combined to have a melting point higher than body temperature and a composition of polar fats combined to have a melting point higher than body temperature, and is a structurally stable and physiologically safe external preparation or moisturizer in the epidermis.
  • Fat molecules can be arranged on the skin by the physical action of rubbing for a very long time, but by heating to an appropriate temperature and converting to a liquid state or a gel state of the fat structure, the fat molecules are uniformly applied and arranged. can do.
  • Fat heated slightly higher than its melting point temporarily has a random structure, but it has a solid or crystallin state in which the tail of the fat is neatly aligned as it is cooled at a somewhat lower epidermal temperature after application to the skin. do. That is, a structurally stable fat protective film in which the hydrocarbon portions of fat molecules are well aligned can be formed on the epidermis.
  • compositions for skin application are prepared according to the following basic principles: triglycerides with high melting points (palm stearin, tripalmitin, etc.) and triglycerides with low melting points (triolein, shea butter, cacao butter, etc.) )
  • triglycerides with high melting points palm stearin, tripalmitin, etc.
  • low melting points triolein, shea butter, cacao butter, etc.
  • the temperature is limited to 45°C, which does not cause skin burns. That is, the range of the melting point of the fat composition targeted in this patent is higher than the temperature of the body and lower than the temperature that causes burns. In other words, it means that it is above 37°C and below 45°C.
  • the composition of the present invention can be used as a moisturizer or external application because it can provide excellent skin protection while being safe for the human body.
  • FIG. 1 is a diagram showing a device for measuring the melting point of fat.
  • a fat mixture is filled in a Pasteur pipette with a sealed tip, and a metal ball is placed on it.
  • the temperature at the point when the temperature of the Pasteur pipette containing the sample was raised with a water bath, and the temperature at the time when the fat liquefied and the metal spheres settled on the floor was set as the melting point.
  • Figure 2 is a figure showing the measurement of the melting point of a combination of shea butter and tripalmitin (above) a picture showing the measurement of the melting point of a combination of cacao butter and tripalmitin, in the figure, shea butter with a low melting point and trypalmitin with a high melting point, two neutrals By mixing the fat, the composition ratio of the combination having a melting point lower than body temperature and lower than 45°C was confirmed.
  • Figure 3 is a picture showing the measurement of the melting point of a combination of soy lecithin and hydrogenated soy lecithin, in the figure, soy lecithin with a low melting point and hydrogenated soy lecithin with a high melting point, and two polar fats are mixed, so that it is higher than body temperature. It was confirmed the composition ratio of the combination of melting point less than 45 °C Celsius.
  • FIG. 4 is a diagram showing an example of application to dry skin, in the figure, before application (left), application 2 days (middle), application 3 days (right). It was confirmed that the composition has an effect of immediately suppressing the oozing phenomenon caused by skin damage.
  • FIG. 5 and 6 are photographs showing the result of improving dry skin after (Fig. 6) compared to before (Fig. 5) applying the composition of the present invention to the arm of a 64-year-old man for 3 days,
  • FIG. 7 and 8 are photographs showing the result of improving dry skin after (Fig. 8) compared to before (Fig. 7) applying the composition of the present invention to the ankle of a 59-year-old woman for 4 days,
  • FIG. 9 and 10 are photographs showing the results of relieving skin troubles after (FIG. 10) compared to before (FIG. 9) applying the composition of the present invention to the lips and around the lips of a 16-year-old man for 2 days.
  • composition of polar fat having a melting point in the same temperature range as that of a neutral fat composition having a melting point between 37-44°C is prepared, and the two compositions are mixed again to make a final composition.
  • a method of heating the mixture to 45°C and applying it to the skin is suggested.
  • Example 1 Method for measuring the melting point of fat
  • Slip melting point measurement method (Ismail Hakk ⁇ Boyac ⁇ Ihsan Karabulut Semra Turan 2003 Journal of Food Lipids 10(3):193-202Slip) and its own method of measuring the melting point of fat to prepare a fat mixture having a melting point of 37°C ⁇ 44°C Was developed and used.
  • the developed method will be called the metal ball sinking point measurement method.
  • the Slip melting point measurement method is to fill the inside of one end of a glass capillary with a fat of 10 mm, and seal the other end of the capillary.
  • the capillary tube filled with fat is bathed in distilled water. It is a method of measuring the temperature at which the fat filled in the capillary tube comes out of the capillary tube as the melting point. At this time, the increase in the water bath temperature is 1°C/minute or less.
  • the measurement method developed to measure the melting point of fat is more convenient and less variation in measured values, and is as follows. Briefly, cut the pointed end of a glass Pasteur pipette (inner diameter 5.6mm), melt it with a gas torch, and seal it, and put 1ml of the melted fat mixture inside Pasteur. Put a Pasteur pipette containing fat in the refrigerator for 12 hours to sufficiently harden the fat. Place a bearing metal ball (diameter 4.76mm, average 0.4411 ⁇ 0.00047g) on the hardened fat sample inside the Pasteur pipette and bathe in water. The increase in the water bath temperature is 1°C/min or less. As the temperature rises, when the hardened fat melts, the bearing metal balls placed on top sink into the fat. The temperature at the point when the ball closes on the floor (the average depth of fat is 2.8 cm) is measured as the melting point (FIG. 1).
  • Example 2 Primary composition of triglycerides
  • Example 3 Primary composition of polar fat
  • a composition having a required melting point was prepared by mixing a phospholipid having a melting point higher than 44°C and a phospholipid lower than 36°C. Soybean lecithin (melting point, -5°C) was used as a low-temperature phospholipid, and hydrogenated soy lecithin (melting point, 50-60°C) was used as a high-temperature phospholipid.
  • the melting point of the composition obtained by combining the two fats is shown in the figure (Fig. 3).
  • Example 4 Secondary composition of a combination of triglycerides and polar fats for skin application
  • a formulation that can be applied to the human body was prepared by mixing the neutral fat and polar fat with the melting point adjusted as described above. Triglycerides and polar fats whose melting point was set to 39°C were selected and mixed. Polar fat was mixed in a ratio of 4% and 8% to the weight of neutral fat, respectively. The mixture was hydrated by adding 30% (weight ratio) of water to the mixture. The moisture of 30% is imitated from the fact that the human stratum corneum generally has a moisture content of 20-30%, which has the purpose of improving the spreadability of a high triglyceride composition. In addition, it has the purpose of preventing excessive movement of moisture from the epidermis toward the fat composition. The final formulation was found to have a melting point of 38.4°C.
  • fat molecules are used as energy, it is very important that the molecules are evenly arranged and have a certain structure for the intrinsic function of fat in vivo. In other words, in order to apply fat molecules to a living body as an external application, molecular diffusion must be performed well, and molecules must have a solid structure in which they are properly aligned.
  • the factor necessary for the diffusion of fat compositions with melting points higher than body temperature is temperature. In other words, by heating above the melting point, the molecules are spread over the skin, and the molecules are arranged as they cool down.
  • composition of this patent is provided to the user using a small sealed container containing 2 ml each, and the user immersed the sealed container in hot water to warm the contents.
  • a sealed container of the same size containing the cacao butter mixed fat having a clear point at 45°C so that the user can bathe the composition in water at an appropriate temperature was provided.
  • a small dry heating device that can heat a container containing the composition to 45°C is designed to consider user convenience.
  • Fig. 4 shows an example of application to dry skin. As can be seen from FIG. 4, it was confirmed that the composition of the present invention has an effect of immediately inhibiting oozing from skin damage.
  • the composition of the present invention was distributed to 14 volunteers, and participants were asked to take pictures of improvement after use and skin improvement. Although the applicants who participated in the experience evaluated the satisfaction level after use as very good, it was judged that the objectivity of the evaluation could not be secured because most of the applicants were composed of acquaintances, and the result was omitted here.

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Abstract

La présente invention concerne une composition pouvant être appliquée par voie cutanée présentant des points de fusion contrôlés et des températures de transition de phase de molécules de graisse, la composition contenant une composition de triglycérides dont le point de fusion est compris entre 37 °C et 44 °C et une composition de lipides polaires point de fusion est comprise entre 37 °C et 44 °C, un procédé de préparation de la composition, et une utilisation de celle-ci en tant que produit cosmétique ou médical. La composition de la présente invention, dont la température finale est comprise entre 37 °C et 45 °C, est sans danger pour le corps humain et peut protéger la peau de manière excellente et, à ce titre, peut être utilisée comme agent hydratant ou agent à usage externe.
PCT/KR2020/003669 2019-03-21 2020-03-18 Composition s'appliquant par voie cutanée présentant un point de fusion contrôlé et une température de transition de phase de molécules de graisse, son procédé de préparation et sa méthode d'application Ceased WO2020190015A1 (fr)

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Application Number Priority Date Filing Date Title
KR10-2019-0032125 2019-03-21
KR20190032125 2019-03-21

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WO2020190015A1 true WO2020190015A1 (fr) 2020-09-24

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990001323A1 (fr) * 1988-08-12 1990-02-22 Bernstein Joel E Procede et composition de traitement et de prevention des problemes de peau seche
KR20060114685A (ko) * 2003-09-11 2006-11-07 킴벌리-클라크 월드와이드, 인크. 보습 및 윤활 조성물
KR101455684B1 (ko) * 2014-04-29 2014-11-04 주식회사 씨엠에스랩 피부 장벽 개선 및 피부 재생 효과를 갖는 액정유화 화장료 조성물
KR20150108198A (ko) * 2014-03-17 2015-09-25 주식회사 엘지생활건강 생체 유사 화장료 조성물
KR20180109329A (ko) * 2017-03-27 2018-10-08 (주)에이씨티 보습 복합물을 함유하는 피부 보습용 화장료 조성물

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990001323A1 (fr) * 1988-08-12 1990-02-22 Bernstein Joel E Procede et composition de traitement et de prevention des problemes de peau seche
KR20060114685A (ko) * 2003-09-11 2006-11-07 킴벌리-클라크 월드와이드, 인크. 보습 및 윤활 조성물
KR20150108198A (ko) * 2014-03-17 2015-09-25 주식회사 엘지생활건강 생체 유사 화장료 조성물
KR101455684B1 (ko) * 2014-04-29 2014-11-04 주식회사 씨엠에스랩 피부 장벽 개선 및 피부 재생 효과를 갖는 액정유화 화장료 조성물
KR20180109329A (ko) * 2017-03-27 2018-10-08 (주)에이씨티 보습 복합물을 함유하는 피부 보습용 화장료 조성물

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