WO2017003080A1 - Solution de dispersion contenant des microparticules lipidiques solides d'un système exempt de tensioactif, et composition cosmétique l'utilisant - Google Patents

Solution de dispersion contenant des microparticules lipidiques solides d'un système exempt de tensioactif, et composition cosmétique l'utilisant Download PDF

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Publication number
WO2017003080A1
WO2017003080A1 PCT/KR2016/004399 KR2016004399W WO2017003080A1 WO 2017003080 A1 WO2017003080 A1 WO 2017003080A1 KR 2016004399 W KR2016004399 W KR 2016004399W WO 2017003080 A1 WO2017003080 A1 WO 2017003080A1
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temperature
solid lipid
dispersion
wax
oil
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PCT/KR2016/004399
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English (en)
Korean (ko)
Inventor
최수정
김도훈
박승한
박성일
채병근
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(주)아모레퍼시픽
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Priority to CN201680038579.8A priority Critical patent/CN107735074B/zh
Publication of WO2017003080A1 publication Critical patent/WO2017003080A1/fr
Priority to HK18103369.7A priority patent/HK1243920A1/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • 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
    • A61K8/34Alcohols
    • 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

Definitions

  • the present invention relates to a dispersion comprising a solid lipid microparticles of a surfactant-free system and a cosmetic composition using the same, and to a dispersion comprising a solid lipid microparticles having high stability and excellent appearance quality even at high temperatures and a cosmetic composition using the same.
  • Solid lipid nanoparticles and nanostructures lipid carriers (NLCs) have been developed as alternative carrier systems for emulsions, liposomes, and polymeric nanoparticles and are active It can increase the chemical stability of ingredients, increase skin hydration through occlusive effect, increase the bioavailability of active ingredients in skin, and physical stability of topical preparations. Due to the advantage that can increase, has recently gained great popularity in the cosmetic field. However, since the SLN and NLC are too stable to take a long time to release the drug, there is a need for a method that can effectively release the drug in order to overcome this, and when applied to the oil-in-water formulation, Due to the imbalance of the wax-lipid combination, it is difficult to secure stability.
  • the present inventors search for a dispersion containing solid lipid particles of a specific combination with a small change in structure according to temperature change, and when the crystal melting temperature and the recrystallization temperature satisfy a specific range, The present invention has been completed by discovering that dispersions containing solid lipid particulates with excellent stability can be prepared.
  • the present invention provides a dispersion comprising solid lipid microparticles including wax, lipids and oils, and satisfying the following formulas 1 and 2
  • Tm 1 is the maximum temperature value of the crystal melting temperature at heating
  • Tm 2 is the maximum temperature value of the recrystallization temperature at reduced temperature
  • the present invention provides a cosmetic composition that is excellent in high temperature stability including a dispersion that satisfies the formula 1 and formula 2.
  • the dispersion including the solid lipid particles according to the present invention is a surfactant-free system, it has excellent emulsion stability and excellent formulation stability according to temperature, so that it can be effectively applied to a water gel base, and excellent skin stability and trouble generation are minimized. It has the advantage of being able to.
  • the dispersion containing the solid lipid particles according to the present invention effectively inhibits coalescence or aggregation, which not only has a differentiated appearance, but also provides excellent moisture with a smooth application while melting at skin temperature, and is excellent when applied to the skin.
  • Occlusion effect has the advantage of providing a high moisturizing power and skin suppleness.
  • the dispersion containing the solid lipid particles according to the present invention has the advantage of providing a high moisture feeling of the solubilization formulation and the oiliness of the emulsified formulation, moisturizing sustainability at the same time.
  • the cosmetic composition using the dispersion including the solid lipid fine particles according to the present invention has a function of enhancing or decreasing skin absorption by a change in phase, thereby providing a cosmetic composition with optimized skin absorption tendency.
  • FIG. 1 shows an analysis result using differential scanning calorimetry (DSC) of solid lipid particles in Example 1 composition.
  • Figure 2 shows the analysis results using differential scanning calorimetry (DSC) of the solid lipid particles in the composition of Example 7.
  • FIG. 3 shows an analysis result using differential scanning calorimetry (DSC) of solid lipid particles in Example 9 composition.
  • Figure 4 shows the analysis results using differential scanning calorimetry (DSC) of the solid lipid particles in the composition of Example 10.
  • Figure 5 shows the results of analysis using differential scanning calorimetry (DSC) of the solid lipid particles in the composition of Example 11.
  • FIG. 6 shows the results of analysis using differential scanning calorimetry (DSC) of solid lipid particles in the composition of Example 12.
  • FIG. 7 shows an analysis result using differential scanning calorimetry (DSC) of solid lipid particles in Example 13 composition.
  • FIG. 8 shows an analysis result using differential scanning calorimetry (DSC) of solid lipid particles in Comparative Example 1 composition.
  • Example 9 is a photograph confirming the restoring force of the dispersion prepared in Example 7 and Comparative Example 1.
  • the dispersion including the solid lipid fine particles of the surfactant-free system according to the present invention and the cosmetic composition using the same are described below, but unless otherwise defined in the technical terms and scientific terms used at this time, the present invention generally includes The person skilled in the art has a general understanding, and in the following description, descriptions of well-known functions and configurations that may unnecessarily obscure the subject matter of the present invention will be omitted.
  • SSN solid lipid nanoparticles
  • NLC nanostructured lipid carriers
  • the present applicant has further intensified research on the structural change according to the temperature change of each component included in the solid lipid microparticles through DSC, and as a result, the thermal stability of the solid lipid microparticles in certain combinations significantly lowers the stability. It has been found that the eggplant can be prepared a dispersion, the dispersion satisfies the following formulas 1 and 2, and includes solid lipid particles having a wax, a lipid and an oil.
  • Tm 1 Is the maximum temperature value of the crystal melting temperature at heating
  • Tm 2 is the maximum temperature value of the recrystallization temperature at reduced temperature
  • the solid lipid microparticles according to an embodiment of the present invention may give a visual cognitive effect through appearance discrimination and visualization in which skin active ingredients are absorbed as a stable dispersion having a stable stability, and as a conventional surfactant as a surfactant-free system. It can minimize the skin irritation or troubles caused, it can be applied to sensitive skin products.
  • lipid refers to a single-chain lipid, and may be one or more selected from linear saturated alcohols and linear saturated fatty acids, but is not limited thereto.
  • full width at half maximum means the range of temperature change ( ⁇ T) based on the half height with respect to the peak of the melting temperature and recrystallization temperature by DSC analysis. do.
  • Tm 1 warm-up crystal melting temperature
  • Tm 1 the warm-up crystal melting temperature according to the present invention
  • Tm 1 it shows a soft coating feeling while melting at the skin temperature, preferably in the range of the following Equation 3 in terms of imparting an excellent moisture and moisture to the skin But it is not limited thereto.
  • the improved high temperature stability, and due to the fast recovery force may be in the range of the following Equation 4 preferably in terms of transparency of the trauma, but is not limited thereto. no.
  • the crystal melting temperature and the recrystallization temperature of the dispersion according to an embodiment of the present invention each have one peak, it is advantageous that the dispersion of the crystal melting temperature and recrystallization temperature range is low.
  • the low dispersion of the crystal melting temperature and the recrystallization temperature range may mean that the structural change according to the temperature change is small, and thus the low temperature and high temperature stability of the solid lipid particles may be remarkably improved.
  • the full width at half maximum ( ⁇ T m 1 ) of the crystal melting temperature at heating is in the range of 1 to 5 ° C. or at the full width at the temperature of recrystallization at low temperature.
  • half maximum, ⁇ T m 2 ) is a low dispersion that satisfies the range of 1 to 5 °C is good in terms of stability of the high dispersion according to the temperature change, the resilience of the solid lipid particles when the temperature is lowered to room temperature at a high temperature (above 45 °C)
  • the half-height width value of the recrystallization temperature at low temperature must satisfy the range of 1 to 5 ° C.
  • the solid lipid particles according to an embodiment of the present invention may be one containing one or more waxes selected from vegetable waxes, animal waxes, mineral waxes and synthetic waxes, non-limiting example of the wax candelilla Wax, Carnauba Wax, Rice Wax, Cotton Wax, Berry Berry Wax, Chinese Insect Wax, Sugar Cane Wax, Jojoba Wax, Shea Butter, Sunflower Wax, Hydrogenated Vegetable Oil, Hydrogenated Olive Vegetable waxes including oil stearyl esters, hydrogenated olive oil dodecyl esters, and the like; Animal waxes including beeswax, lanolin and the like; Mineral waxes including ozokerite, ceresin wax, microcrystalline wax, multi wax, paraffin wax and the like; Synthetic waxes including polyethylene wax, POE (polyoxyethylene) lanolin alcohol ether wax, POE lanolin alcohol acetate wax, POE cholesterol ether wax, lanolin fatty acid polyethylene glycol wax
  • the oil may be one or more oils selected from hydrocarbon oils, ester oils, triglyceride oils, vegetable oils and silicone oils.
  • oils include squalane, mineral oil, hydrogenated polydecene ( hydrocarbon-based oils including hydrogenated polydecene), hydrogenated polyisobutene, and the like; Isopropyl palmitate, 2-octyldodecyl myristate, isopropyl myrister, butyloctyl salicylate, cetyl octanoate, cetyl octyl hexanoate, coco caprylate / caprate, decyl cocoate, isostere Ester oils including arylisostearate, pentaerythritol tetraethylhexanoate, dicaprylylcarbonate, and the like; Vegetable oils including castor oil, olive oil, jojoba oil, avocado oil, macadamia oil, meadowfo
  • the lipid may be one or more selected from higher fatty alcohols of C10-C30 and higher fatty acids of C10-C30, and has a high solubility in the oil and may be high in C10-C30 in terms of melting at skin temperature and showing a soft coating. Preference is given to using fatty alcohols.
  • a non-limiting example of the higher fatty alcohol may include one or more lipids selected from cetyl alcohol, stearyl alcohol, cetostearyl alcohol, behenyl alcohol and the like, but is not limited thereto.
  • the solid lipid microparticles according to one embodiment of the present invention may include 50 to 150 parts by weight of lipids and 100 to 500 parts by weight of oil, based on 100 parts by weight of wax, preferably based on wax 1
  • the oil should be mixed in a 1: 2 ratio and 1: 5 ratio.
  • the aqueous phase of the trauma of the dispersion may further include an aqueous phase thickener for stable dispersion of the solid lipid particles.
  • the water thickener is not limited as long as it is a substance used to improve the viscosity of the water phase in the art, polyacrylic acid, polyacrylamide, polymethacrylic acid, polyhydroxyethyl methacrylate, polyacrylic acid-polymetha Krylic acid copolymer, polyacrylic acid-polyacrylamide copolymer, polymethacrylic acid-polyacrylamide copolymer, polyethylene glycol, poly (N, N-ethylaminoethyl methacrylate), hyaluronic acid, agar, chitosan, ammonium May include one or more aqueous thickeners selected from acryloyldimethyltorate-VPicopolymers, xanthan gums, celluloses, cellulose ethers, polyviny
  • the viscosity of the dispersion according to an embodiment of the present invention is preferably in the range of 10,000 to 50,000 cps, preferably in the range of 10,000 to 30,000 cps in terms of stable dispersibility and excellent spreadability of the solid lipid particles, but is not limited thereto. It is not.
  • the average diameter of the solid lipid particles may range from 10 nm to 20 mm, may range from 50 nm to 10 mm, and may range from 100 nm to 10 mm in terms of phase stability and optimum stability according to temperature. However, it is not limited thereto.
  • the present invention provides a cosmetic composition comprising a dispersion that satisfies the following formula 1 and formula 2.
  • Tm 1 Is the maximum temperature value of the crystal melting temperature at heating
  • Tm 2 is the maximum temperature value of the recrystallization temperature at reduced temperature
  • the cosmetic composition may contain a dispersion that satisfies the above range, may give a good moisture while melting at the skin temperature, and can provide high moisturizing power and skin suppleness through excellent occlusion effect when applied to the skin. .
  • the cosmetic composition may have a function of enhancing or decreasing skin absorption by a change of phase, thereby providing a cosmetic composition with optimized skin absorption tendency.
  • the cosmetic composition according to an embodiment of the present invention may further include fragrances, pigments, preservatives, fungicides, oxidative stabilizers, pearls and the like within a range that does not inhibit the effect of the dispersion.
  • the waxes, lipids, and oils were completely dissolved at 85 ° C. according to the compositions of Tables 1 to 2 to form an oil phase, and then a thickener of the following composition was added to form an aqueous phase (water gel base) having a viscosity of 15,000 cps (centi poise). After the addition, the mixture was stirred at room temperature with an azi mixer to prepare a dispersion including solid lipid particles (average diameter: 3 mm).
  • DSC was used as CSC (4100DSC, Calorimetry Science Corporation, Lindon, Utah, United States).
  • One pan was used as a reference material without filling a sample, and each sample was filled with a sample of each of the solid lipid fine particles prepared in Examples 1 to 15 and Comparative Example 1, respectively.
  • the reference pan, which did not fill the sample, became the reference material, which was set as the baseline, and the thermal flow of the remaining samples was compared and analyzed.
  • the temperature range to be measured was measured at 5 ° C./min from 25 ° C. to 85 ° C., and the results are shown in FIGS. 1 to 8 and Table 3 below.
  • Example Comparative Example 1 One 7 9 10 11 12 13 Tm 1 42 42.5 42.5 41 37.5 43 38 43 Tm 2 35 36 34 32.5 29 33 29 36 ⁇ Tm 2 2.5 2.0 1.8 4.8 2.5 3.0 2.0 7.0
  • the solid lipid particles according to the present invention each has a single peak crystal melting temperature value, the half-height width of the recrystallization temperature at reduced temperature according to the present invention
  • the crystallization rate was fast and the resilience of the solid lipid fine particles in the formulation was excellent.
  • the solid lipid particles satisfying the formulas 1 and 2 according to the present invention has a low dispersion crystal melting temperature range and recrystallization temperature range by minimizing thermal behavior and suppressing structural changes due to temperature changes, thereby further improving. Emulsification stability and excellent temperature stability can be represented.
  • each of the dispersion prepared in Examples 1 to 15 and Comparative Example 1 was put in a vial having a content of 20 g room temperature (25 ⁇ 2 °C), cold and thermostat (4 ⁇ 2 °C ), High temperature thermostat (45 ⁇ 2 °C) and cycle chamber (Freeze-Thaw Chamber, cycle from -20 °C to 45 °C once a day) and store and check the formulation stability of each sample at weekly interval.
  • the results are shown in Table 4 below.
  • Example 1 Example 5
  • Example 7 Comparative Example 1 Room temperature (1 week / 2 weeks / 3 weeks / 4 weeks) ⁇ / ⁇ / ⁇ / ⁇ ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ Cold and Hot Tub ⁇ / ⁇ / ⁇ / ⁇ / ⁇ ⁇ / ⁇ / / ⁇ / / ⁇ / / / / / High Temperature Bath ⁇ / ⁇ / / ⁇ / ⁇ / ⁇ / / ⁇ / ⁇ / ⁇ / ⁇ / / / Cycle chamber ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / ⁇ / / ⁇ / / / / / / / / Cycle chamber ⁇
  • the dispersion containing the solid lipid microparticles having a specific composition according to the present invention can have a significantly improved low temperature and high temperature stability compared to the dispersion containing the solid lipid microparticles in the prior art, and have a smooth feeling of use, smooth appearance with excellent appearance quality It is possible to provide an excellent skin cosmetic composition capable of imparting skin feel and improved moisture.

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Abstract

La présente invention concerne une solution de dispersion contenant des microparticules lipidiques solides d'un système exempt de tensioactif, et une composition cosmétique l'utilisant, et fournit une solution de dispersion contenant des microparticules lipidiques solides présentant une meilleure stabilité thermique et une excellente qualité d'aspect en conséquence de la remarquable dégradation du comportement thermique des microparticules lipidiques solides dans une combinaison spécifique, ainsi qu'une composition cosmétique les utilisant.
PCT/KR2016/004399 2015-06-30 2016-04-27 Solution de dispersion contenant des microparticules lipidiques solides d'un système exempt de tensioactif, et composition cosmétique l'utilisant WO2017003080A1 (fr)

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CN201680038579.8A CN107735074B (zh) 2015-06-30 2016-04-27 无表面活性剂体系的含有固体脂质微粒的分散液及使用其的化妆品组合物
HK18103369.7A HK1243920A1 (zh) 2015-06-30 2018-03-09 無表面活性劑體系的含有固體脂質微粒的分散液及使用其的化妝品組合物

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KR1020150093463A KR102406641B1 (ko) 2015-06-30 2015-06-30 무계면활성제 시스템의 고형 지질 미립자를 포함하는 분산액 및 이를 이용한 화장료 조성물
KR10-2015-0093463 2015-06-30

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EP3655108A4 (fr) * 2017-07-19 2021-01-27 Henkel AG & Co. KGaA Composition de conditionnement de cheveux ayant un effet de fonte de neige

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KR102224314B1 (ko) 2017-07-31 2021-03-09 (주)아모레퍼시픽 구형 입자를 포함하는 분산 제형 화장료 조성물
CN110585070A (zh) * 2019-09-12 2019-12-20 北京植物医生生物科技有限公司 含有悬浮粒子的化妆品及其制备方法
KR102462350B1 (ko) * 2020-07-13 2022-11-03 주식회사 알엠사이언스 이데베논 또는 이의 약학적으로 허용가능한 염을 함유하는 지질 비드 및 이의 제조방법

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KR102406641B1 (ko) 2022-06-08
KR20170003163A (ko) 2017-01-09
TW201702315A (zh) 2017-01-16
CN107735074B (zh) 2021-07-20
CN107735074A (zh) 2018-02-23
HK1243920A1 (zh) 2018-07-27

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