KR102494289B1 - 활성 혼합물 - Google Patents
활성 혼합물 Download PDFInfo
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- KR102494289B1 KR102494289B1 KR1020150038828A KR20150038828A KR102494289B1 KR 102494289 B1 KR102494289 B1 KR 102494289B1 KR 1020150038828 A KR1020150038828 A KR 1020150038828A KR 20150038828 A KR20150038828 A KR 20150038828A KR 102494289 B1 KR102494289 B1 KR 102494289B1
- Authority
- KR
- South Korea
- Prior art keywords
- acid
- derivatives
- oil
- agent
- hydroxy
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 125
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Abstract
(a) 1,2-헥산다이올 및
(b) 1,2-옥탄다이올을 포함하는 활성 혼합물이 제안된다.
(b) 1,2-옥탄다이올을 포함하는 활성 혼합물이 제안된다.
Description
본 발명은 화장품 분야에 속하고 두 개의 선택된 1,2-알칸다이올로 구성된 활성 혼합물, 상기 활성성분(active)들을 포함하는 조성물 및 이들의 구체적 적용에 관한 것이다.
에멀젼은 다양한 적용과 함께 모든 종류의 피부 관리(skin care) 제품에 대한 가장 중요한 종류의 제형이다. 그러므로, 우수한 물리적(physical) 및 미생물 안정성을 가진 제형을 개발하는 것은 화장품 산업에서 주된 도전과제이다.
법적 제한 또는 부정적 언론 때문에 미생물 안정화(stabilization)를 위한 허용 물질의 수는 제한되어 있다. 그러므로 더욱더 전통적 보존제들이 항미생물 물성을 가진 다기능 성분들로 전적으로 또는 부분적으로 대체되고 있다.
항미생물 효과와 함께 에멀젼의 물리화학적 안정성은 제품 개발을 위하여 아직 중요한 요소이다.
마지막으로, 화장품 제품의 감각 프로파일(sensorial profile)은 고객에 의해 받아들여지기(acceptance) 위하여 가장 중요하다. 특히, 퍼짐성(spreadability), 흡수 및 피부 느낌은 피부에 적용후 화장품 제형의 전반적인 퍼포먼스에 기여하는 중요한 파라메터들이다. 에멀젼의 오일 바디가 피부에 빨리 퍼지면 퍼질수록 더 좋다는 것이 소비자의 인식이다. 제형의 퍼짐성 양상 - 및 그러므로 이의 감각 프로파일은 조성물 중 액적의 평균 입자 크기에 연관되어 있다. 액적이 더 작으면 작을수록 퍼짐은 더 빨라진다. 그 결과, 평균 입자 크기 분포를 더 작은 값으로 만들기 위한 첨가제에 대한 수요가 여전히 있다 또한, 입자 크기는 에멀젼 안정성을 위해 중요한 파라메터이다. 분산된 상의 액적이 더 작을수록 물리화학적 안정성이 더 좋아진다.
국제특허출원 WO 2003 069994 A1에 따르면 상이한 변화(change) 길이의 알칸 다이올 혼합물은 순수한 1,2-알칸 다이올과 비교하여 상승적으로(synergistically) 개선된 항미생물 효과를 가진다는 것이 알려져 있다. 그러나, 상기 문헌은 에멀전 중의 입자 크기 분포를 더 작은 액적으로 변경시키기 위하여 다이올을 사용하는 것에 대한 어떠한 내용도 시사 또는 암시하고 있지 않다.
그러므로, 본 발명의 목적은 동시에
· 항미생물 안정성을 제공하고
· 조성물 중의 평균 입자 크기를 더 작은 액적으로 변경시키고, 및
· 특히 퍼짐성, 흡수 및 피부 느낌에 관한 감각 프로파일을 개선하는 화장품, 약학적 또는 피부과(dematological) 에멀젼에 사용하기 위한 활성성분(actives)을 제공하는 것이다.
본 발명의 목적은
(a) 1,2-헥산다이올 및
(b) 1,2-옥탄다이올을 포함하는 활성 혼합물이다.
놀랍게도, 1.2-헥산다이올 및 1,8-옥탄다이올의 혼합물이, 특히 동일한 양일 때, 상기 기술된 복잡한 문제를 완전히 해결한다는 것이 관찰되었다. 특히 상기 이원혼합물은 항미생물학적 활성과 관련하여 상승적 행동을 보이고, 평균 방울 크기를 감소시키고 화장료, 피부과학적 또는 약학적 조성물에 첨가되었을 때 감각적 프로파일을 보여준다.
1,2-알칸다이올(1,2-
ALKANEDIOLS
)
1,2-알칸다이올은 예를 들어 말단 올레핀(olefin)의 에폭시화 및 이어지는 물을 사용한 고리 절단에 의해 수득될 수 있는 잘 알려진 화장료 성분이다. 상승적 활성과 관련하여 (a) 및 (b)의 2가지 구성요소가 약 25:75 내지 약 75:25의 중량에 의한 비율로, 보다 바람직하게는 약 40:60 내지 약 60:40의 중량에 의한 비율로, 특히 약 50:50의 중량에 의한 비율로 존재할 때 혼합물의 최고의 결과가 얻어졌다.
에멀전
본 발명의 또 다른 목적은 상기 기술된 바와 같이 1.2-헥산다이올 및 1,2-헥산다이올의 상승적 혼합물을 포함하는 화장료 또는 약학적 조성물과 관련된다. 바람직하게는 상기 조성물은 피부 관리, 모발 관리, 자외선 차단 또는 개인적 관리(personal care) 조성물이다.
바람직하게는 상기 조성물은 에멀전이고, 특히 상기 에멀전은 유중수(o/w) 에멀전, 수중유(w/o) 에멀전 또는 다상(w/o/w 또는 o/w/o) 에멀전이다.
전형적으로, 상기 에멀전은
● 10 부피%(Vol.-%)가 2 ㎛보다 작은 지름을 보이고(바람직하게는 0.5 ㎛ 미만),
● 50 부피%가 5 ㎛보다 작은 지름을 보이고(바람직하게는 2 ㎛ 미만),
● 90 부피%가 15 ㎛보다 작은 지름을 보이는(바람직하게는 12 ㎛ 미만), 평균 입자 크기 분포를 나타낸다.
화장품 또는 개인 관리 조성물(COSMETIC OR PERSONAL CARE COMPOSITION)
본 발명의 다른 목적은 1,2-알칸다이올의 상기 두 부분으로 이루어진(binary) 혼합물을 포함하는 화장품 또는 개인 관리 조성물을 아우른다. 화장품 또는 개인 관리 조성물은 예를 들어 화장품 크림, 로션, 스프레이, 에멀젼, 연고, 겔 또는 무스(mousse) 등과 같은 피부 관리, 모발 관리 및/또는 자외선 차단(sun care) 제품이 대표적일 수 있다. 통상적인 예는 피부 크림 및 모발 샴푸, 발한억제제(antiperspirants) 및 비누이다.
본 발명에 따른 제형은 추가적인 보조제(auxiliary) 및 첨가제(additive)로서 연마제(abrasive), 항-여드름제(anti-acne agent), 보존제(preservatives), 피부노화방지제(agent against ageing of the skin), 항-봉와직염제(anti-cellulitis agent), 항비듬제(antidandruff agent), 항-염증제(anti-inflammatory agent), 자극-방지제(irritation-preventing agent), 자극-억제제(irritation-inhibiting agent), 항산화제(antioxidant), 수렴제(astringent), 냄새 제거제(deodorant agents), 땀-억제제(perspiration-inhibiting agent), 살균제(antiseptic agent), 대전 방지제(anti-statics), 결합제(binder), 버퍼(buffer), 담체 물질(carrier material), 킬레이트제(chelating agent), 세포자극제(cell stimulant), 세정제(클린징제; cleansing agent), 관리제(케어제; care agent), 제모제(depilatory agent), 표면활성물질(surface-active substance), 탈취제(deodorizing agent), 발한억제제(antiperspirant), 연화제(softener), 유화제(emulsifier), 효소(enzyme), 에센셜 오일(essential oil), 섬유(fibre), 필름-형성제(film-forming agent), 고정제(fixative), 거품-형성제(foam-forming agent), 거품안정제(foam stabilizer), 거품 방지물질(substances for preventing foaming), 거품촉진제(foam booster), 겔링제(gelling agent), 겔-형성제(gel-forming agent), 모발관리제(모발케어제; hair care agent), 모발-세팅제(hair-setting agent), 모발-스트레이트너제(hair-straightening agent), 보습제(moisture-donating agent), 보습물질(moisturizing substance), 수분-유지 물질(moisture-retaining substance), 표백제(bleaching agent), 강화제(strengthening agent), 얼룩제거제(stain-removing agent), 시각적으로 광택제(optically brightening agent), 주입제(impregnating agent), 더트-기피제(dirt-repellent agent), 마찰감소제(friction-reducing agent), 윤활제(lubricant), 보습크림(moisturizing cream), 연고(ointment), 불투명화제(opacifying agent), 가소제(plasticizing agent), 커버제(covering agent), 연마제(polish), 광택제(gloss agent), 중합체(polymer), 파우더(분말; powder), 단백질(protein), 리-오일링제(re-oiling agent), 마모제(abrading agent), 실리콘(silicone), 피부-진정제(skin-soothing agent), 피부-클렌징제(skin-cleansing agent), 피부 관리제(피부 케어제; skin care agent), 피부-치유제(skin-healing agent), 피부 라이트닝제(skin-lightening agent), 피부-보호제(skin-protecting agent), 피부-유연제(skin-softening agent), 모발 촉진제(hair promotion agent), 냉각제(cooling agent), 피부-냉각제(skin-cooling agent), 온감제(warming agent), 피부-온감제(skin-warming agent), 안정화제(stabilizer), UV-흡수제(UV-absorbing agent), UV 필터(UV filter), 세제(detergent), 섬유유연제(fabric conditioning agent), 서스펜션화제(suspending agent), 피부 태닝제(skin-tanning agent), 점증제(thickener), 비타민(vitamina), 오일(oil), 왁스(wax), 지방(fat), 인지질(phospholipid), 포화지방산(saturated fatty acid), 모노- 또는 폴리불포화 지방산, α-히드록시산(α-hydroxy acid), 폴리히드록시지방산(polyhydroxyfatty acid), 액화제(liquefier), 염료(dyestuff), 색보호제(colour-protecting agent), 색소(pigment), 항-부식제(anti-corrosive), 아로마(aroma), 향미 물질(flavouring substance), 향기 물질(odoriferous substance), 폴리올(polyol), 계면활성제(surfactant), 전해질(electrolyte), 유기용매(organic solvent) 또는 실리콘 유도체(silicone derivative) 등을 포함할 수 있다.
계면활성제(SURFACTANTS)
바람직한 보조제 및 첨가제는 음이온성 및/또는 양쪽성 또는 쌍성이온(zwitterionic) 계면활성제이다. 음이온 계면활성제의 일반적인 예로는 비누, 알킬 벤젠설포네이트, 알칸설포네이트, 올레핀 설포네이트, 알킬에테르 설포네이트, 글리세롤 에테르 설포네이트, 메틸 에스테르 설포네이트, 설포지방산, 알킬 설페이트, 지방 알코올 에테르 설페이트, 글리세롤 에테르 설페이트, 지방산 에테르 설페이트, 하이드록시 혼성 에테르 설페이트(hydroxy mixed ether sulfate), 모노글리세라이드 (에테르) 설페이트, 지방산 아마이드 (에테르) 설페이트, 모노- 및 다이알킬(dialkyl) 설포숙시네이트(sulfosuccinate), 모노- 및 다이알킬 설포숙시나메이트(sulfosuccinamate), 설포트리글리세라이드, 아마이드 비누(amide soap), 에테르 카복실산 및 이의 염, 지방산 이세치오네이트(isethionate), 지방산 사르코시네이트(sarcosinate), 지방산 타우라이드(tauride), N-아실아미노 산, 예컨대, 예를 들어, 아실 락틸레이트, 아실 타르트레이트, 아실 글루타메이트 및 아실 아스파테이트, 알킬 올리고글루코사이드 설페이트, 단백질 지방산 응축액 (특히 밀 기반 식물성 제품) 및 알킬(에테르)포스페이트가 있다. 만약 음이온성 계면활성제가 폴리글리콜 에테르 사슬을 포함하면, 비록 그것들이 좁은 범위의 호모로그(homolouge) 분포를 가지는 것이 바람직하지만 통상의 호모로그 분포를 가질 수 있다. 양쪽성 또는 쌍성이온 계면활성제의 일반적인 예로는 알킬베타인, 알킬아미도베타인, 아미노프로피오네이트, 아미노글리시네이트, 이미다졸리니움 베타인 및 설포베타인이 있다. 언급된 계면활성제는 모두 알려진 화합물들이다. 이들의 구조 및 제조 정보는 관련 개요, 예를 들어, J. Falbe (ed.), "Surfactants in Consumer Products", Springer Verlag , Berlin, 1987, pages 54 to 124 또는 J. Falbe (ed.), "Katalysatoren, Tenside und Mineraloladditive , pages 123-217에서 찾아볼 수 있다. 제제의 계면활성제의 퍼센트(백분율; percentage) 함량은 제제에 대하여(기초하여) 0.1 내지 10 중량% 및 바람직하게는 0.5 내지 5 중량%일 수 있다.
오일
바디
(OIL BODIES)
O/W 에멀전의 성분을 형성하는 적절한 오일 바디는, 예를 들어, 6 내지 18, 바람직하게는 8 내지 10 탄소원자를 가지는 지방 알코올에 기초한 게르벳 알코올(Guerbet alcohol), 직쇄 또는 분지 C6-C22-지방 알코올과 직쇄 C6-C22-지방산의 에스테르 또는 직쇄 또는 분지 C6-C22-지방 알코올과 분지 C6-C 13-카르복시산의 에스테르, 예컨대, 예를 들어, 미리스틸 미리스테이트(myristyl myristate), 미리스틸 팔미테이트(myristyl palmitate), 미리스틸 스테아레이트(myristyl stearate), 미리스틸 이소스테아레이트(myristyl isostearate), 미리스틸 올레이트(myristyl oleate), 미리스틸 베헤네이트(myristyl behenate), 미리스틸 에루케이트(myristyl erucate), 세틸 미리스테이트(cetyl myristate), 세틸 팔미테이트(cetyl palmitate), 세틸 스테아레이트(cetyl stearate), 세틸 이소스테아레이트(cetyl isostearate), 세틸 올레이트(cetyl oleate), 세틸 베헤네이트(cetyl behenate), 세틸 에루케이트(cetyl erucate), 스테아릴 미리스테이트(stearyl myristate), 스테아릴 팔미테이트(stearyl palmitate), 스테아릴 스테아레이트(stearyl stearate), 스테아릴 이소스테아레이트(stearyl isostearate), 스테아릴 올레이트(stearyl oleate), 스테아릴 베헤네이트(stearyl behenate), 스테아릴 에루케이트(stearyl erucate), 이소스테아릴 미리스테이트(isostearyl myristate), 이소스테아릴 팔미테이트(isostearyl palmitate), 이소스테아릴 스테아레이트(isostearyl stearate), 이소스테아릴 이소스테아레이트(isostearyl isostearate), 이소스테아릴 올레이트(isostearyl oleate), 이소스테아릴 베헤네이트(isostearyl behenate), 이소스테아릴 올레이트(isostearyl oleate), 올레일 미리스테이트(oleyl myristate), 올레일 팔미테이트(oleyl palmitate), 올레일 스테아레이트(oleyl stearate), 올레일 이소스테아레이트(oleyl isostearate), 올레일 올레이트(oleyl oleate), 올레일 베헤네이트(oleyl behenate), 올레일 에루케이트(oleyl erucate), 베헤닐 미리스테이트(behenyl myristate), 베헤닐 팔미테이트(behenyl palmitate), 베헤닐 스테아레이트(behenyl stearate), 베헤닐 이소스테아레이트(behenyl isostearate), 베헤닐 올레이트(behenyl oleate), 베헤닐 베헤네이트(behenyl behenate), 베헤닐 에루케이트(behenyl erucate), 에루실 미리스테이트(erucyl myristate), 에루실 팔미테이트(erucyl palmitate), 에루실 스테아레이트(erucyl stearate), 에루실 이소스테아레이트(erucyl isostearate), 에루실 올레이트(erucyl oleate), 에루실 베헤네이트(erucyl behenate) 및 에루실 에루케이트(erucyl erucate)이다. 또한 적절한 것은 분지 알코올, 특히 2-에틸헥산올(2-ethylhexanol)과 직쇄 C6-C22-지방산의 에스테르, 직쇄 또는 분지 C6-C22-지방 알코올, 특히 다이옥틸 말레이트(dioctyl malate)와 C18-C38-알킬히드록시 카르복시산(C18-C38-alkylhydroxy carboxylic acid)의 에스테르, 다가 알코올(polyhydric alcohol){예컨대, 예를 들어, 프로필렌 글리콜(propylene glycol), 다이머다이올(dimerdiol) 또는 트라이머트라이올(trimertriol)} 및/또는 게르벳 알코올(Guerbet alcohol)과 직쇄 및/또는 분지 지방산의 에스테르, C6-C10-지방산에 기초한 트라이글리세라이드(triglyceride), C6-C18-지방산에 기초한 액체 모노-/다이-/트라이글리세라이드 혼합물, 방향족 카르복시산(aromatic carboxylic acid), 특히 벤조산(benzoic acid)과 C6-C22-지방 알코올 및/또는 게르벳 알코올의 에스테르, 1 내지 22 탄소원자를 가지는 직쇄 또는 분지 알코올 또는 2 내지 10 탄소원자 및 2 내지 6 히드록실기를 가지는 폴리올(polyol)과 C2-C12-다이카르복시산(C2-C12-dicarboxylic acid)의 에스테르, 식물성 오일(vegetable oil), 분지 일차 알코올(branched primary alcohol), 치환된 사이클로헥산(cyclohexane), 직쇄 및 분지 C6-C22-지방 알코올 카르보네이트(C6-C22-fatty alcohol carbonate), 예컨대, 예를 들어, 디카프릴릴 카르보네이트(Dicaprylyl Carbonate){세티올®CC(Cetiol®CC)}, 6 내지 18, 바람직하게는 8 내지 10 탄소원자를 가지는 지방 알코올에 기초한 게르벳 카보네이트, 직쇄 및/또는 분지 C6-C22-알코올과 벤조산의 에스테르{예를 들어, 핀솔브®TN(Finsolv®TN)}, 알킬기 당 6 내지 22 탄소원자를 가지는 직쇄 또는 분지, 대칭 또는 비대칭 다이알킬 에테르(dialkyl ether), 예컨대, 예를 들어, 디카프릴릴 에테르{세티올®OE(Cetiol®OE)}, 폴리올과 에폭시화된 지방산 에스테르의 고리열림 생성물(ring-opening products of epoxidized fatty acid esters with polyol), 실리콘 오일(silicone oil){사이클로메치콘(cyclomethicone), 실리콘 메치콘 등급(silicone methicone grade), 등} 및/또는 지방족 또는 나프텐 탄화수소(naphthenic hydrocarbon), 예컨대, 예를 들어, 스쿠알란(squalane), 스쿠알렌(squalene) 또는 다이알킬사이클로헥산(dialkylcyclohexane)이다.
유화제(EMULSIFIER)
다른 계면활성제는 또한 다음의 예를 포함하여, 유화제로서 제제에 추가될 수 있다:
·알킬기에 8 내지 15개의 탄소원자를 포함한 직쇄 C8 -22 지방알코올, C12 -22 지방산 및 알킬페놀에 2 내지 30 몰의 에틸렌 옥사이드 및/또는 0 내지 5 몰의 프로필렌 옥사이드 첨가 제품;
·글리세롤에 1 내지 30 몰의 에틸렌 옥사이드의 추가제품의 C12 /18 지방산 모노에스테르 및 다이에스테르;
·글리세롤 모노- 및 다이에스테르 및 6 내지 22 의 탄소원자를 포함하는 포화 및 불포화 지방산의 솔비탄 모노- 및 다이에스테르 및 이의 에틸렌 옥사이드 첨가 제품;
·캐스터 오일 및/또는 하이드로지네이트된 캐스터 오일에 15 내지 60 몰의 에틸렌 옥사이드의 첨가 제품;
·폴리올 에스테르 및, 특히, 폴리글리세롤 에스테르로, 예를 들어, 폴리글리세롤 폴리리시놀레이트, 폴리글리세롤 폴리-12-하이드록시스테아레이트 또는 폴리글리세롤 다이머레이트 이소스테아레이트. 이러한 종류의 몇몇의 화합물의 혼합물 또한 적합하다;
·캐스터 오일 및/또는 하이드로지네이트된 캐스터 오일에 2 내지 15 몰의 에틸렌 옥사이드 첨가 제품;
·직쇄, 분지, 불포화 또는 포화 C6 /22 지방산, 리시놀레산(ricinoleic acid) 및 12-하이드록시스테아르산 및 글리세롤, 폴리글리세롤, 펜타에리스리톨, 다이펜타에리스리톨, 당 알코올(예 : 소비톨), 알킬 글루코사이드 (예: 메틸 글루코사이드, 부틸 글루코사이드, 라우릴 글루코사이드) 및 폴리글루코사이드 (예: 셀룰로오즈)에 기초한 부분 에스테르;
·모노- 다이- 및 트라이알킬 포스페이트 및 모노-, 다이 및/또는 트라이-PEG-알킬 포스페이트 및 이들의 염;
·울 왁스 알코올;
·폴리실옥세인/폴리알킬 폴리에테르 공중합체 및 상응하는 유도체;
·펜타에리스리톨, 지방산, 시트르산 및 지방 알코올의 혼합된 에스테르 및/또는 C6 -22 지방산, 메틸 글루코스 및 폴리올, 바람직하게는 글리세롤 또는 폴리 글리세롤의 혼성 에스테르,
·폴리알킬렌 글리콜 및
·글리세롤 카보네이트.
지방알코올, 지방산, 알킬페놀, 글리세롤 모노- 및 다이에스테르 및 지방산의 솔비탄 모노- 및 다이에스테르, 또는 캐스터 오일에 에틸렌 옥사이드 및/또는 프로필렌 옥사이드 첨가 제품이 상업적으로 이용가능한 제품으로 알려져있다. 그들은 알콕시화의 평균 정도가 에틸렌 옥사이드 및/또는 프로필렌 옥사이드와 첨가반응이 수행되는 기질 간의 비율에 상응하는 균질한 혼합물이다. 글리세롤에 에틸렌 옥사이드의 첨가 제품의 C12 /18 지방산 모노에스테르 및 다이에스테르는 화장품 포뮬레이션용(제형용) 지질층 개선제(enhancer)로 알려져있다. 바람직한 유화제가 하기에 더 상세히 기재된다:
부분 글리세라이드 . 적절한 부분 글리세라이드의 일반적인 예는 하이드록시 스테아르산 모노글리세라이드, 하이드록시 스테아르산 다이글리세라이드, 이소스테아르산 모노글리세라이드, 이소스테아르산 다이글리세라이드, 올레산 모노글리세라이드, 올레산 다이글리세라이드, 리시놀레산 모노글리세라이드, 리시놀레산 다이글리세라이드, 리놀레산 모노글리세라이드, 리놀레산 다이글리세라이드, 리놀렌산 모노글리세라이드, 리놀렌산 다이글리세라이드, 에루신산 모노글리세라이드, 에루신산 다이글리세라이드, 타르타르산 모노글리세라이드, 타르타르산 다이글리세라이드, 시트르산 모노글리세라이드, 시트르산 다이글리세라이드, 말산 모노글리세라이드, 말산 다이글리세라이드 및 제조 공정으로부터 트라이글리세라이드 소량을 여전히 포함할 수 있는 이들의 기술적 혼합물이 있다. 언급된 부분 글리세라이드에 1 내지 30몰, 바람직하게는 5 내지 10몰의 에틸렌 옥사이드 첨가 제품 또한 바람직하다.
솔비탄 에스테르. 적절한 솔비탄 에스테르는 솔비탄 모노이소스테아레이트, 솔비탄 세스퀴이소스테아레이트, 솔비탄 다이이소스테아레이트, 솔비탄 트라이소스테아레이트, 솔비탄 모노올레이트, 솔비탄 세스퀴올레이트, 솔비탄 다이올레이트, 솔비탄 트라이올레이트, 솔비탄 모노에루케이트, 솔비탄 세스퀴에루케이트, 솔비탄 다이에루케이트, 솔비탄 트라이에루케이트, 솔비탄 모노리시놀레이트, 솔비탄 세스퀘리시놀레이트, 솔비탄 다이리시놀레이트, 솔비탄 트라이리시놀레이트, 솔비탄 모노하이드록시 스테아레이트, 솔비탄 세스퀴 하이드록시 스테아레이트, 솔비탄 다이하이드록시 스테아레이트, 솔비탄 트라이하이드록시 스테아레이트, 솔비탄 모노타르트레이트, 솔비탄 세스퀘타르트레이트, 솔비탄 다이타르트레이트, 솔비탄 트라이타르트레이트, 솔비탄 모노시트레이트, 솔비탄 세스퀴시트레이트, 솔비탄 다이시트레이트, 솔비탄 트라이시트레이트, 솔비탄 모노말레이트, 솔비탄 세스퀴말레이트, 솔비탄 다이말레이트, 솔비탄 트라이말레이트 및 이들의 기술적 혼합물이 있다. 언급된 솔비탄 에스테르에 1 내지 30몰, 및 바람직하게 5 내지 10 몰의 에틸렌 옥사이드 첨가 제품도 바람직하다.
폴리글리세롤 에스테르. 적절한 폴리글리세롤 에스테르의 일반적인 예는 폴리글리세릴-2 다이폴리하이드록시 스테아레이트 (Dehymuls® PGPH), 폴리글리세린-3-다이이소스테아레이트 (Lameform® TGI), 폴리글리세릴-4 이소스테아레이트 (Isolan® GI 34), 폴리글리세릴-3 올레이트, 다이이소스테아로일 폴리글리세릴-3 다이이소스테아레이트 (Isolan® PDI), 폴리글리세릴-3 메틸글루코스 다이스테아레이트 (Tego care® 450), 폴리글리세릴-3 비즈왁스 (Cera Bellina®), 폴리글리세릴-4 카프레이트 (폴리글리세롤 카프레이트 T2010/90), 폴리글리세릴-3 세틸 에테르 (Chimexane® NL), 폴리글리세릴-3 다이스테아레이트 (Cremophor® GS 32) 및 폴리글리세릴 폴리리시놀레이트 (Admul® WOL 1403), 폴리글리세릴 다이머레이트 이소스테아레이트 및 이들의 혼합물이다. 다른 적절한 폴리에스테르의 예는 선택적으로 1 내지 30몰의 에틸렌 옥사이드와 반응하는 라우르산, 코코(coco) 지방산, 델로(tallow) 지방산, 팔미트산, 스테아르산, 올레산, 또는 베헨산 등과 트라이메틸올 프로페인 또는 펜타에리스리톨의 모노-, 다이- 및 트라이에스테르이다.
음이온성 유화제. 일반적인 음이온 유화제는 지방족 C12 -22 지방산으로 예를 들어, 팔미트산, 스테아르산 또는 베헨산, 및 C12 -22 다이카르복실산으로 예를 들어 아젤라산 또는 세바스산이 있다.
양쪽성 유화제. 다른 적절한 유화제는 양쪽성 또는 쌍성이온 계면활성제이다. 쌍성이온 계면활성제는 분자에 적어도 하나의 4차 암모늄기 및 적어도 하나의 카르복실레이트 및 하나의 설포네이트기를 포함하는 표면 활성 화합물이다. 특히 적절한 쌍성이온 계면활성제는 소위 베타인으로서, 예컨대 N-알킬-N,N-다이메틸 암모늄 글리시네이트로 예를 들어, 코코알킬 다이메틸 암모늄 글리시네이트, N-아실아미노프로필-N,N-다이메틸 암모늄 글리시네이트로 예를 들어, 코코아실아미노프로필 다이메틸 암모늄 글리시네이트, 및 알킬 또는 아실기에 8 내지 18의 탄소원자를 포함하는 2-알킬-3-카르복시메틸-3-하이드록시에틸 이미다졸린 및 코코아실아미노에틸 하이드록시에틸 카르복시메틸 글리시네이트이다. 코카미도프로필 베타인의 CTFA 명칭에 따라 알려진 지방산 아마이드 유도체가 특히 선호된다. 양쪽성 계면활성제도 적절한 유화제이다. 양쪽성 계면활성제는 C8 /18 알킬 또는 아실기 뿐만 아니라, 분자 내에 적어도 하나의 유리 아미노기 및 적어도 하나의 -COOH- 또는 -SO3H 기를 포함하고 염을 형성할 수 있는 표면 활성 화합물이다. 적절한 양쪽성 계면활성제의 예로는 N-알킬 글라이신, N-알킬 프로피온산, N-알킬아미노부티르산, N-알킬이미노다이프로피온산, N-하이드록시에틸-N-알킬아미도프로필 글리신, N-알킬 타우린, N-알킬 사르코신, 알킬기에 약 8 내지 18의 탄소원자를 포함하는 2-알킬아미노프로피온산 및 알킬아미노아세트산이 있다. 특히 바람직한 양쪽성 계면활성제는 N-코코알킬아미노프로피오네이트, 코코아실아미노에틸 아미노프로피오네이트 및 C12/18 아실 사르코신이 있다.
슈퍼팻팅제
(
SUPERFATTING
AGENT) 및
컨시스턴시
인자(CONSISTENCY FACTOR)
슈퍼팻팅제는 예를 들어, 라놀린 및 레시틴뿐만 아니라 폴리에톡시화 또는 아실화 라놀린 및 레시틴 유도체, 폴리올 지방산 에스테르, 모노글리세라이드 및 지방산 알카놀아마아드와 같은 물질로부터 선택될 수 있고, 지방산 알카놀아마이드는 또한 거품 안정화제 역할을 한다.
컨시스턴시 인자는 주로 12 내지 22 및 바람직하게는 16 내지 18 개의 탄소원자를 포함한 지방 알코올 또는 하이드록시지방 알코올뿐만 아니라 부분 글라이세라이드, 지방산 또는 하이드록시지방산이다. 알킬 올리고글루코사이드 및/또는 같은 사슬 길이의 지방산 N-메틸 글루카마이드 및/또는 폴리글리세롤 폴리-12-하이드록시스테아레이트와의 이들 물질의 조합이 바람직하게 이용된다.
증점제
(THICKENING AGENT) 및 유동 첨가물(RHEOLOGY ADDITIVE)
적절한 증점제는 폴리머릭 증점제로 예컨대 Aerosil® 타입 (친수성 실리카), 폴리사카라이드, 보다 특별하게, 잔탄검, 구아-구아(guar-guar), 아가-아가(agar-agar), 알기네이트 및 타일로스(tylose), 카르복시메틸 셀룰로오스 및 하이드록시에틸 셀룰로오스, 또한 상대적으로 높은 분자량의 폴리에틸렌 글리콜 모노에스테르 및 지방산의 다이에스테르, 폴리아크릴레이트(예를 들어 Carbopols® [Goodrich] 또는 Synthalens® [Sigma]), 폴리크릴아마이드, 폴리비닐 알코올 및 폴리비닐 피롤리돈, 계면활성제로, 예를 들어, 에톡시화 지방산 글리세라이드, 폴리올과 지방산의 에스테르, 예를 들어 펜타에리스리톨 또는 트라이메틸올 프로판, 좁은 범위 지방 알코올 에톡시레이트 및 염화나트륨 및 염화암모늄과 같은 전해질이 있다.
폴리머
(중합체; POLYMER)
예를 들어, 적절한 양이온성 폴리머로는, 양이온성 셀룰로오스 유도체로 예를 들어, 폴리머 JR 400®의 명칭으로 Amerchol에서 얻을 수 있는 4차(quaternized) 하이드록시에틸 셀룰로오스, 양이온성 전분, 다이알릴 암모늄 염과 아크릴아마이드의 공중합체, 4차 비닐 피롤리돈/비닐 이미다졸 폴리머로 예를 들어, Luviquat®(BASF), 폴리글리콜 및 아민의 축합 생성물, 4차 콜라겐 폴리펩타이드로 예를 들어, 라우릴디모늄 하이드록시프로필 가수분해된 콜라겐(Lamequat® L, Grunau), 4차 밀 폴리펩타이드, 폴리에틸렌이민, 양이온성 실리콘 폴리머로 예를 들어, 아모디메치콘, 아디프산 및 다이메틸아미노하이드록시프로필 다이에틸렌트라이아민(Cartaretine®, Sandoz)의 공중합체, 다이메틸 다이알릴 염화 암모늄과 아크릴산의 공중합체(Merquat® 550, Chemviron), 폴리아미노폴리아마이드 및 이의 가교 수용성 폴리머, 양이온 키틴 유도체로 예를 들어, 선택적으로 미정질에 분산된 4차 키토산, 비스-다이알킬아민으로 예를 들어 비스-다이메틸아미노-1,3-프로판과 다이할로알킬로 예를 들어 다이브로모부탄의 축합 생성물, 양이온성 구아검으로 예를 들어, 셀라니즈(Celanese)사의 Jaguar® CBS, Jaguar® C-17, Jaguar® C-16, 4차 암모늄 염 폴리머로 예를 들어, 미라놀(Miranol)사의 Mirapol® A-15, Mirapol® AD-1, Mirapol® AZ-1 및 상품명 Rheocare® CC 또는 Ultragel® 300 하에 판매되는 것을 알 수 있는 다양한 폴리쿼터니움 타입(예를 들어 6, 7, 32 또는 37)이 있다.
적절한 음이온성, 쌍성이온, 양쪽성 및 비이온성 폴리머는, 예를 들어, 비닐 아세테이트/크로톤산 공중합체, 비닐 피롤리돈/비닐 아크릴레이트 공중합체, 비닐 아세테이트/부틸 말레이트/이소보닐 아크릴레이트 공중합체, 메틸 비닐에테르/말레익 무수물 공중합체 및 이들의 에스테르, 가교되지 않고 폴리올-가교된 폴리아크릴 산, 아크릴아미도프로필 트라이메틸암모늄 염화물/아크릴레이트 공중합체, 옥틸아크릴아마이드/메틸 메타크릴레이트/tert-부틸아미노에틸 메타크릴레이트/2-하이드록시프로필 메타크릴레이트 공중합체, 폴리비닐 피롤리돈, 비닐 피롤리돈/비닐 아세테이트 공중합체, 비닐 피롤리돈/다이메틸아미노에틸 메타크릴레이트/비닐 카프로락탐 터폴리머(terpolymer) 및 선택적으로 유도된 셀룰로오스 에테르 및 실리콘이다.
펄화
왁스(
PEARLISING
WAX)
적절한 펄화(pearlising) 왁스는 예를 들어, 알킬렌 글리콜 에스테르, 특히 에틸렌 글리콜 다이스테아레이트; 지방산 알카놀아마이드, 특히 코코지방산 다이에탄올아마이드; 부분 글리세라이드, 특히 스테아르 산 모노글리세라이드; 다염기성 에스테르, 6 내지 22 탄소 원자를 포함하는 지방 알코올과 선택적으로 하이드록시-치환된 카르복실산, 특히, 타르타르 산의 긴 사슬 에스테르; 지방 화합물로 예를 들어 적어도 24개의 탄소원자를 포함하는 지방 알코올, 지방 케톤, 지방 알데하이드, 지방 에테르 및 지방 카보네이트, 특히 라우론(laurone) 및 다이스테아릴에테르; 지방 산으로 스테아르산, 하이드록시 스테아르산 또는 베헨산, 12 내지 22의 탄소 원자를 포함하는 지방 알코올 및/또는 2 내지 15의 탄소원자 및 2 내지 10의 하이드록시기를 포함하는 폴리올과 12 내지 22의 탄소원자를 포함하는 올레핀 에폭사이드의 개환형 생산물 및 이들의 혼합물이다.
실리콘(SILICONE)
적절한 실리콘 화합물로, 예를 들어, 다이메틸 폴리실록산, 메틸페닐 폴리실록산, 고리형 실리콘 및 상온에서 액체와 수지-유사체 모두로 존재할 수 있는 변형된 아미노-, 지방산-, 알코올-, 폴리 에테르-, 에폭시-, 플루오린-, 글리코사이드- 및/또는 알킬-변형 실리콘 화합물이 있다. 다른 적절한 실리콘 화합물은 수소화된 실리케이트와 평균 사슬 길이 200 내지 300의 다이메틸실록산 단위를 가지는 다이메치콘의 혼합물인 시메치콘이 있다. 적절한 휘발성 실리콘의 자세한 개요는 Todd 외, in Cosm . Toil. 91 , 27 (1976)에서 찾을 수 있다.
왁스(WAX) 및
안정화제
(STABILIZER)
천연오일의 사용 외에도 왁스 또한 제제에서 존재할 수 있고, 보다 특별하게 천연왁스로, 예를 들어, 칸드릴라(candelilla) 왁스, 카나우바(carnauba) 왁스, 일본 왁스, 아프리카띠(espartograss) 왁스, 코르크 왁스, 구아루마(guaruma) 왁스, 쌀 오일 왁스, 사탕 수수 왁스, 오우리큐리(ouricury) 왁스, 몬탄(montan) 왁스, 비즈 왁스 (beeswax), 셀락(shellac) 왁스, 경랍(spermaceti), 라놀린(양모(wool) 왁스), 우지(uropygial) 지방, 세라신(ceresine), 지랍(ozocerite, earth wax), 페트로라텀(petrolatum), 파라핀 왁스 및 마이크로왁스가 있고; 화학적으로 변형된 왁스(하드 왁스)로 예를 들어, 몬탄 에스테르 왁스, 사솔 왁스, 수소화된 호호바(jojoba) 왁스 및 합성 왁스로 예를 들어, 폴리알킬렌 왁스 및 폴리에틸렌 글리콜 왁스가 있다.
지방산의 금속염으로, 예를 들어, 마그네슘, 알루미늄 및/또는 아연 스테아레이트 또는 리시놀레이트가 안정화제로 사용될 수 있다.
제1 자외선 차단 인자(PRIMARY SUN PROTECTION FACTOR)
본 발명의 명세서 내에서 제1 자외선 차단 인자는 예를 들어, 상온(room temperature)에서 액체 또는 결정이고, 자외선을 흡수할 수 있고 더 긴 파장, 예를 들어 열의 형태로 흡수된 에너지를 방출할 수 있는 유기 물질(광 필터)이다.
본 발명에 따른 제형은 유리하게는 적어도 하나의 UV-A 필터 및/또는 적어도 하나의 UV-B 필터 및/또는 광대역 필터 및/또는 적어도 하나의 무기 색소를 함유한다. 본 발명에 따른 제형은 바람직하게는 적어도 하나의 UV-B 필터 또는 광대역 필터, 보다 특히 바람직하게는 적어도 하나의 UV-A 필터 및 적어도 하나의 UV-B 필터를 함유한다.
바람직한 화장품 조성물, 바람직하게는 본 발명에 따른 국소 제형은 4-아미노벤조산(4-aminobenzoic acid) 및 유도체, 살리실산(salicylic acid) 유도체, 벤조페논(benzophenone) 유도체, 다이벤조일메탄(dibenzoylmethane) 유도체, 다이페닐 아크릴레이트(diphenyl acrylates), 3-이미다졸-4-일 아크릴산(3-imidazol-4-yl acrylic acid) 및 이의 에스테르, 벤조퓨란(benzofuran) 유도체, 벤질리덴 말로네이트(benzylidene malonate) 유도체, 하나 이상의 오르가노실리콘(organosilicon) 라디칼을 함유하는 폴리머성 UV 흡수제, 신남산(cinnamic acid) 유도체, 캠퍼(camphor) 유도체, 트라이아닐리노-s-트라이아진(trianilino-s-triazine) 유도체, 2-하이드록시페닐벤조트라이아졸(2-hydroxyphenylbenzotriazole) 유도체, 페닐벤즈이미다졸 설폰산(phenylbenzimidazole sulfonic acid) 유도체 및 이의 염, 안트라닐산 멘틸(anthranilic acid menthyl) 에스테르, 벤조트라이아졸(benzotriazole) 유도체 및 인돌 유도체로 이루어진 군으로부터 선택된 하나, 둘, 셋 또는 그 이상의 자외선 차단 인자를 포함한다.
또한, 피부를 통과하고 자외선-유도된 손상에 대해 내부로부터의 피부 세포를 보호하고 피부의 매트릭스 메탈로프로테아제(cutaneous matrix metalloprotease)의 수준을 감소시키는 활성성분과 화학식 (I)의 화합물을 배합하는 것이 유리하다. 소위 아릴탄화수소(arylhydrocarbon) 수용체 길항제로 불리는 바람직한 각각의 성분은 참고로서 본원에 병합되는 WO 2007/128723에 기술된다. 바람직한 것은 2-벤질리덴-5,6-다이메톡시-3,3-다이메틸인단-1-온(2-benzylidene-5,6-dimethoxy-3,3-dimethylindan-1-one)이다.
본원 발명의 내용 내에서 사용될 수 있는 하기 열거된 UV 필터가 바람직하나 당연히 이에 제한되지 않는다.
바람직하게 사용되는 UV 필터는 하기로 이루어진 군으로부터 선택된다:
·p-아미노벤조산(p-aminobenzoic acid)
·에톡실화된 p-아미노벤조산 에틸 에스테르(p-aminobenzoic acid ethyl ester) (25 mol) (INCI 명칭: PEG-25 PABA)
·p-다이메틸아미노벤조산-2-에틸헥실 에스테르(p-dimethylaminobenzoic acid-2-ethylhexyl ester)
·N-프로폭실화된 p-아미노벤조산 에틸 에스테르(p-aminobenzoic acid ethyl ester) (2 mol)
·p-아미노벤조산 글리세롤 에스테르(p-aminobenzoic acid glycerol ester)
·살리실산 호모멘틸 에스테르 (호모살레이트) {salicylic acid homomenthyl ester (homosalates)} (Neo Heliopan®HMS)
·살리실산-2-에틸헥실 에스테르(salicylic acid-2-ethylhexyl ester) (Neo Heliopan®OS)
·트라이에탄올아민 살리실레이트(triethanolamine salicylate)
·4-이소프로필 벤질 살리실레이트(4-isopropyl benzyl salicylate)
·안트라닐산 멘틸 에스테르(anthranilic acid menthyl ester) (Neo Heliopan®MA)
·다이이소프로필 신남산 에틸 에스테르(diisopropyl cinnamic acid ethyl ester)
·p-메톡시신남산-2-에틸헥실 에스테르(p-methoxycinnamic acid-2-ethylhexyl ester) (Neo Heliopan®AV)
·다이이소프로필 신남산 메틸 에스테르(diisopropyl cinnamic acid methyl ester)
·p-메톡시신남산 이소아밀 에스테르(p-methoxycinnamic acid isoamyl ester) (Neo Heliopan®E 1000)
·p-메톡시신남산 다이에탄올아민 염(p-methoxycinnamic acid diethanolamine salt)
·p-메톡시신남산 이소프로필 에스테르(p-methoxycinnamic acid isopropyl ester)
·2-페닐벤즈이미다졸 설폰산 및 염(2-phenylbenzimidazole sulfonic acid and salts) (Neo Heliopan®Hydro)
·3-(4'-트라이메틸암모늄) 벤질리덴 보르난-2-온 메틸 설페이트(3-(4'-trimethylammonium) benzylidene bornan-2-one methyl sulfate)
·베타-이미다졸-4(5)-아크릴산(우로칸산){beta-imidazole-4(5)-acrylic acid (urocanic acid)}
·3-(4'-설포)벤질리덴 보르난-2-온 및 염(3-(4'-sulfo)benzylidene bornan-2-one and salts)
·3-(4'-메틸 벤질리덴)-D,L-캠퍼(3-(4'-methyl benzylidene)-D,L-camphor) (Neo Heliopan®MBC)
·3-벤질리덴-D,L-캠퍼(3-benzylidene-D,L-camphor)
·N-[(2 및 4)-[2-(옥소보론-3-일리덴) 메틸]벤질] 아크릴아미드 폴리머{N-[(2 and 4)-[2-(oxoborn-3-ylidene) methyl]benzyl] acrylamide polymer}
·4,4'-[(6-[4-(1,1-다이메틸)아미노카보닐)페닐아미노]-1,3,5-트라이아진-2,4-다이일)다이이미노]-비스-(벤조산-2-에틸헥실 에스테르){4,4'-[(6-[4-(1,1-dimethyl)aminocarbonyl)phenylamino]-1,3,5-triazine-2,4-diyl)diimino]-bis-(benzoic acid-2-ethylhexyl ester)} (Uvasorb®HEB)
·벤질리덴 말로네이트 폴리실록산(benzylidene malonate polysiloxane) (Parsol®SLX)
·글리세릴 에틸헥사노에이트 다이메톡시신나메이트(glyceryl ethylhexanoate dimethoxycinnamate)
·다이프로필렌 글리콜 살리실레이트(dipropylene glycol salicylate)
·트리스(2-에틸헥실)-4,4',4''-(1,3,5-트라이아진-2,4,6-트라이일트라이이미노)트라이벤조에이트 (= 2,4,6-트라이아닐리노-(p-카보-2'-에틸헥실-1'-옥시)-1,3,5-트라이아진){tris(2-ethylhexyl)-4,4',4''-(1,3,5-triazine-2,4,6-triyltriimino)tribenzoate (= 2,4,6-trianilino-(p-carbo-2'-ethylhexyl-1'-oxy)-1,3,5-triazine)} (Uvinul®T150).
본 발명에 따른 제제 내에서 바람직하게는 하나 이상의 화학식 (I)의 화합물과 배합되는 광대역 필터는 하기로 이루어진 군으로부터 선택된다:
·2-에틸헥실-2-시아노-3,3-다이페닐 아크릴레이트(2-ethylhexyl-2-cyano-3,3-diphenyl acrylate) (Neo Heliopan®303)
·에틸-2-시아노-3,3'-다이페닐 아크릴레이트(ethyl-2-cyano-3,3'-diphenyl acrylate)
·2-하이드록시-4-메톡시벤조페논(2-hydroxy-4-methoxybenzophenone) (Neo Heliopan®BB)
·2-하이드록시-4-메톡시벤조페논-5-설폰산(2-hydroxy-4-methoxybenzophenone-5-sulfonic acid)
·다이하이드록시-4-메톡시벤조페논(dihydroxy-4-methoxybenzophenone)
·2,4-다이하이드록시벤조페논(2,4-dihydroxybenzophenone)
·테트라하이드록시벤조페논(tetrahydroxybenzophenone)
·2,2'-다이하이드록시-4,4'-다이메톡시벤조페논(2,2'-dihydroxy-4,4'-dimethoxybenzophenone)
·2-하이드록시-4-n-옥톡시벤조페논(2-hydroxy-4-n-octoxybenzophenone)
·2-하이드록시-4-메톡시-4'-메틸 벤조페논(2-hydroxy-4-methoxy-4'-methyl benzophenone)
·소듐 하이드록시메톡시벤조페논 설포네이트(sodium hydroxymethoxybenzophenone sulfonate)
·다이소듐-2,2'-다이하이드록시-4,4'-다이메톡시-5,5'-다이설포벤조페논(disodium-2,2'-dihydroxy-4,4'-dimethoxy-5,5'-disulfobenzophenone)
·페놀, 2-(2H-벤조트라이아졸-2-일)-4-메틸-6-(2-메틸-3(1,3,3,3-테트라메틸-1-(트라이메틸실릴)옥시)다이실록시아닐)프로필){phenol, 2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(1,3,3,3-tetramethyl-1-(trimethylsilyl)oxy)disiloxyanyl) propyl)} (Mexoryl®XL)
·2,2'-메틸렌 비스-(6-(2H-벤조트라이아졸-2-일)-4-1,1,3,3-테트라메틸부틸) 페놀){2,2'-methylene bis-(6-(2H-benzotriazol-2-yl)-4-1,1,3,3-tetramethylbutyl) phenol)} (Tinosorb®M)
·2,4-비스-[4-(2-에틸헥실옥시)-2-하이드록시페닐]-1,3,5-트라이아진(2,4-bis-[4-(2-ethylhexyloxy)-2-hydroxyphenyl]-1,3,5-triazine)
·2,4-비스-[{(4-(2-에틸헥실옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{(4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine) (Tinosorb®S)
·2,4-비스-[{(4-(3-설포네이토)-2-하이드록시프로필옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진 소듐 염(2,4-bis-[{(4-(3-sulfonato)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine sodium salt)
·2,4-비스-[{(3-(2-프로필옥시)-2-하이드록시프로필옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{(3-(2-propyloxy)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine)
·2,4-비스-[{4-(2-에틸헥실옥시)-2-하이드록시}페닐]-6-[4-(2-메톡시에틸 카보닐) 페닐아미노]-1,3,5-트라이아진(2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-[4-(2-methoxyethyl carbonyl) phenylamino]-1,3,5-triazine)
·2,4-비스-[{4-(3-(2-프로필옥시)-2-하이드록시프로필옥시)-2-하이드록시}페닐]-6-[4-(2-에틸카복실) 페닐아미노]-1,3,5-트라이아진(2,4-bis-[{4-(3-(2-propyloxy)-2-hydroxypropyloxy)-2-hydroxy}phenyl]-6-[4-(2-ethylcarboxyl) phenylamino]-1,3,5-triazine)
·2,4-비스-[{4-(2-에틸헥실옥시)-2-하이드록시}페닐]-6-(1-메틸피롤-2-일)-1,3,5-트라이아진(2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(1-methylpyrrol-2-yl)-1,3,5-triazine)
·2,4-비스-[{4-트리스-(트라이메틸실록시실릴프로필옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{4-tris-(trimethylsiloxysilylpropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine)
·2,4-비스-[{4-(2''-메틸프로페닐옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{4-(2''-methylpropenyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine)
·2,4-비스-[{4-(1',1',1',3',5',5',5'-헵타메틸실록시-2''-메틸프로필옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{4-(1',1',1',3',5',5',5'-heptamethylsiloxy-2''-methylpropyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine).
상기 조성물은 UV-A 필터와 같은 추가적인 일반 세제 및 세정 조성물 성분을 포함할 수 있다. 본 발명에 따른 제제 내에서 바람직하게는 하나 이상의 화학식 (I)의 화합물과 배합되는 필터는 하기로 이루어진 군으로부터 선택된다:
·4-이소프로필 다이벤조일 메탄(4-isopropyl dibenzoyl methane)
·테레프탈리덴 다이보르난 설폰산 및 염(terephthalylidene dibornane sulfonic acid and salts) (Mexoryl®SX)
·4-t-부틸-4'-메톡시다이벤조일 메탄 (아보벤존){4-t-butyl-4'-methoxydibenzoyl methane (avobenzone)} / (Neo Heliopan®357)
·페닐렌 비스-벤즈이미다질 테트라설폰산 다이소듐 염(phenylene bis-benzimidazyl tetrasulfonic acid disodium salt) (Neo Heliopan®AP)
·2,2'-(1,4-페닐렌)-비스-(1H-벤즈이미다졸-4,6-다이설폰산), 모노소듐 염{2,2'-(1,4-phenylene)-bis-(1H-benzimidazole-4,6-disulfonic acid), monosodium salt}
·2-(4-다이에틸아미노-2-하이드록시벤조일) 벤조산 헥실 에스테르(2-(4-diethylamino-2-hydroxybenzoyl) benzoic acid hexyl ester) (Uvinul®A Plus)
·DE 100 55 940 A1(= WO 2002 038537 A1)에 따른 인다닐리덴(indanylidene) 화합물.
상기 조성물은 UV 필터와 같은 추가적인 일반 세제 및 세정 조성물 성분을 포함할 수 있고, 본 발명에 따른 제제 내에서 바람직하게는 하나 이상의 화학식 (I)의 화합물과 배합되는 UV 필터는 하기로 이루어진 군으로부터 선택된다:
·p-아미노벤조산(p-aminobenzoic acid)
·3-(4'-트라이메틸암모늄) 벤질리덴 보르난-2-온 메틸 설페이트(3-(4'-trimethylammonium) benzylidene bornan-2-one methyl sulfate)
·살리실산호모멘틸 에스테르(salicylic acid homomenthyl ester) (Neo Heliopan®HMS)
·2-하이드록시-4-메톡시벤조페논(2-hydroxy-4-methoxybenzophenone) (Neo Heliopan®BB)
·2-페닐벤즈이미다졸 설폰산(2-phenylbenzimidazole sulfonic acid) (Neo Heliopan®Hydro)
·테레프탈리덴 다이보르난 설폰산 및 염(terephthalylidene dibornane sulfonic acid and salts) (Mexoryl®SX)
·4-tert-부틸-4'-메톡시다이벤조일 메탄(4-tert-butyl-4'-methoxydibenzoyl methane) (Neo Heliopan®357)
·3-(4'-설포)벤질리덴 보르난-2-온 및 염(3-(4'-sulfo)benzylidene bornan-2-one and salts)
·2-에틸헥실-2-시아노-3,3-다이페닐 아크릴레이트(2-ethylhexyl-2-cyano-3,3-diphenyl acrylate) (Neo Heliopan®303)
·N-[(2 및 4)-[2-(옥소보른-3-일리덴) 메틸]벤질] 아크릴아미드 폴리머(N-[(2 and 4)-[2-(oxoborn-3-ylidene) methyl]benzyl] acrylamide polymer)
·p-메톡시신남산-2-에틸헥실 에스테르(p-methoxycinnamic acid-2-ethylhexyl ester) (Neo Heliopan®AV)
·에톡실화된 p-아미노벤조산 에틸 에스테르(p-aminobenzoic acid ethyl ester) (25 mol) (INCI 명칭: PEG-25 PABA)
·p-메톡시신남산 이소아밀 에스테르(p-methoxycinnamic acid isoamyl ester) (Neo Heliopan®E1000)
·2,4,6-트라이아닐리노-(p-카보-2'-에틸헥실-1'-옥시)-1,3,5-트라이아진(2,4,6-trianilino-(p-carbo-2'-ethylhexyl-1'-oxy)-1,3,5-triazine) (Uvinul®T150)
·페놀, 2-(2H-벤조트라이아졸-2-일)-4-메틸-6-(2-메틸-3(1,3,3,3-테트라메틸-1-(트라이메틸실릴)옥시)다이실록시아닐)프로필){phenol, 2-(2H-benzotriazol-2-yl)-4-methyl-6-(2-methyl-3(1,3,3,3-tetramethyl-1-(trime-thylsilyl)oxy)-disiloxyanyl) propyl)} (Mexoryl®XL)
·4,4'-[(6-[4-(1,1-다이메틸)아미노카보닐)페닐아미노]-1,3,5-트라이아진-2,4-다이일)다이이미노]-비스-(벤조산-2-에틸헥실 에스테르) {4,4'[(6-[4-(1,1-dimethyl)aminocarbonyl)phenylamino]-1,3,5-triazine-2,4-diyl)diimino]-bis-(benzoic acid-2-ethylhexyl ester)} (Uvasorb HEB)
·3-(4'-메틸 벤질리덴)-D,L-캠퍼(3-(4'-methyl benzylidene)-D,L-camphor) (Neo Heliopan®MBC)
·3-벤질리덴 캠퍼(3-benzylidene camphor)
·살리실산-2-에틸헥실 에스테르(salicylic acid-2-ethylhexyl ester) (Neo Heliopan®OS)
·4-다이메틸아미노벤조산-2-에틸헥실 에스테르(4-dimethylaminobenzoic acid-2-ethylhexyl ester) (Padimate O)
·하이드록시-4-메톡시벤조페논-5-설폰산 및 Na 염(hydroxy-4-methoxybenzophenone-5-sulfonic acid and Na salt)
·2,2'-메틸렌 비스-(6-(2H-벤조트라이아졸-2-일)-4-1,1,3,3-테트라메틸부틸) 페놀){2,2'-methylene bis-(6-(2H-benzotriazol-2-yl)-4-1,1,3,3-tetramethylbutyl) phenol)} (Tinosorb®M)
·페닐렌 비스-벤즈이미다질 테트라설폰산 다이소듐 염(phenylene bis-benzimidazyl tetrasulfonic acid disodium salt) (Neo Heliopan®AP)
·2,4-비스-[{(4-(2-에틸헥실옥시)-2-하이드록시}페닐]-6-(4-메톡시페닐)-1,3,5-트라이아진(2,4-bis-[{(4-(2-ethylhexyloxy)-2-hydroxy}phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine) (Tinosorb®S)
·벤질리덴 말로네이트 폴리실록산(benzylidene malonate polysiloxane) (Parsol®SLX)
·멘틸 안트라닐레이트(menthyl anthranilate) (Neo Heliopan®MA)
·2-(4-다이에틸아미노-2-하이드록시벤조일) 벤조산 헥실 에스테르(2-(4-diethylamino-2-hydroxybenzoyl) benzoic acid hexyl ester) (Uvinul® A Plus)
·DE 100 55 940 (= WO 02/38537)에 따른 인다닐리덴(indanylidene) 화합물.
유리한 제1 및 또한 제2 자외선 차단 인자가 WO 2005 123101 A1에 언급된다. 유리하게, 이들 제제는 적어도 하나의 UVA 필터 및/또는 적어도 하나의 UVA/UVB 필터 및/또는 적어도 하나의 무기 색소를 함유한다. 상기 제제는 자외선 차단 제제에서 통상적으로 사용되는 것과 같은 다양한 형태로 존재할 수 있다. 따라서, 그들은 용액, 유-중-수 타입 (W/O) 또는 수-중-유 타입 (O/W)의 에멀젼 또는 다중 에멀젼, 예를 들어, 수-중-유-중-수 타입 (water-in-oil-water, W/O/W), 젤, 수분산액, 고체 스틱 또는 에어로졸의 형태일 수 있다.
추가의 바람직한 구체예에서, 본 발명에 따른 제형은 본 발명에 따른 제형이 2 또는 그 이상의 (바람직하게는 5 또는 그 이상의) 광 차단 지수(light protection factor)를 갖도록 썬스크린제, 즉 특히 UV 필터 및/또는 무기 색소 (UV 필터 색소)의 총량을 함유한다. 본 발명에 따른 그러한 제형은 피부 및 모발의 보호를 위해 특히 적합하다.
제2 자외선 차단 인자 (SECONDARY SUN PROTECTION FACTOR)
상기 언급된 제1 자외선 차단 인자 이외에, 항산화 타입의 제2 자외선 차단 인자는 또한 사용될 수 있다. 항산화 타입의 제2 자외선 차단 인자는 자외선이 피부를 통과할 때 개시되는 광화학 연쇄 반응을 방해한다. 전형적인 예는 아미노산(예를 들어, 글라이신, 히스티딘, 티로신, 트립토판) 및 이의 유도체, 이미다졸 {예컨대 우로칸산(urocanic acid)} 및 이의 유도체, 펩타이드, 예컨대 D,L-카르노신(D-carnosine), D-카르노신, L-카르노신 및 이의 유도체 (예컨대 안세린), 카로티노이드(carotinoid), 카로텐(carotenes)(예컨대 알파-카로텐, 베타-카로텐, 리코펜) 및 이의 유도체, 클로로겐산(chlorogenic acid) 및 이의 유도체, 리폰산(liponic acid) 및 이의 유도체{예컨대 다이하이드로리폰산(dihydroliponic acid)}, 아우로티오글루코스(aurothioglucose), 프로필 티오우라실(propylthiouracil) 및 기타 티올 (예컨대 티오레독신(thioredoxine), 글루타치온(glutathione), 시스테인(cysteine), 시스틴(cystine), 시스타민(cystamine) 및 글리코실, N-아세틸, 메틸, 에틸, 프로필, 아밀, 부틸 및 라우릴(lauryl), 팔미토일(palmitoyl), 올레일(oleyl), 알파-리놀레일(alpha-linoleyl), 콜레스테릴(cholesteryl) 및 이의 글리세릴(glyceryl) 에스테르) 및 이의 염, 다이라우릴티오다이프로피오네이트(dilaurylthiodipropionate), 다이스테아릴티오다이프로피오네이트(distearylthiodipropionate), 티오다이프로피온산(thiodipropionic acid) 및 이의 유도체 (에스테르, 에테르, 펩타이드, 리피드(lipid), 뉴클레오타이드, 뉴클레오사이드 및 염) 및 매우 작은 용인되는 투여량의 설폭시민(sulfoximine) 화합물 (예컨대 부티오닌 설폭시민(butionine sulfoximines), 호모시스테인 설폭시민(homocysteine sulfoximine), 부티오닌 설폰(butionine sulfones), 펜타-, 헥사- 및 헵타-티오닌 설폭시민), 또한 (금속) 킬레이터(예컨대 알파-하이드록시 지방산(alpha-hydroxyfatty acids), 팔미트산(palmitic acid), 피트산(phytic acid), 락토페린(lactoferrine)), 알파-하이드록시산 {예컨대 시트르산(citric acid), 락트산(lactic acid), 말산(malic acid)}, 흄산(humic acid), 담즙산, 담즙 추출물, 빌리루빈(bilirubin), 빌리베르딘(biliverdin), EDTA, EGTA 및 이의 유도체, 불포화 지방산 및 이의 유도체 {예컨대 리놀레산(linoleic acid), 올레산(oleic acid)}, 엽산(folic acid) 및 이의 유도체, 유비퀴논(ubiquinone) 및 유비퀴놀(ubiquinol) 및 이의 유도체, 비타민 C 및 이의 유도체 (예컨대 아스코르빌 팔미테이트(ascorbyl palmitate), Mg 아스코르빌 포스페이트(Mg ascorbyl phosphate), 아스코르빌 아세테이트), 토코페롤 및 유도체 (예컨대 비타민 E 아세테이트), 비타민 A 및 유도체 (비타민 A 팔미테이트) 및 벤조인 수지(benzoin resin)의 코니페릴 벤조에이트(coniferyl benzoate), 루틴산(rutinic acid) 및 이의 유도체, 글리코실 루틴(glycosyl rutin), 페룰산(ferulic acid), 퍼푸릴리덴 글루시톨(furfurylidene glucitol), 카르노신(carnosine), 부틸 하이드록시톨루엔(butyl hydroxytoluene), 부틸 하이드록시아니솔(butyl hydroxyanisole), 노르다이하이드로구아이악 수지산(nordihydroguaiac resin acid), 노르다이하이드로구아이아레트산(nordihydroguaiaretic acid), 트라이하이드록시부티로페논(trihydroxybutyrophenone), 요산(uric acid) 및 이의 유도체, 만노스(mannose) 및 이의 유도체, 슈퍼옥사이드 다이스뮤타아제(superoxide dismutase), 이산화티타늄(titanium dioxide) (예컨대 에탄올 내의 분산), 징크 및 이의 유도체 (예컨대 ZnO, ZnSO4), 셀레늄(selenium) 및 이의 유도체 (예컨대 셀레늄 메티오닌), 스틸벤(stilbenes) 및 이의 유도체{예를 들면, 스틸벤 옥사이드(stilbene oxide), 트랜스-스틸벤 옥사이드} 및 본 발명의 목적에 적합한 이들 활성 물질의 유도체(염, 에스테르, 에테르, 당(sugar), 뉴클레오타이드, 뉴클레오사이드, 펩타이드 및 리피드)이다.
유리한 무기 제2 광 차단 색소(light protection pigments)는 WO 2005 123101 A1에 또한 언급된 미세하게 분산된 금속 산화물(metal oxides) 및 금속염이다. 본 발명에 따른 최종 화장품 제제 내 무기 색소, 특히 소수성 무기 미세색소(micropigment)의 총량은, 제제의 총 중량에 기초하여 각각의 경우에서, 유리하게는 0.1 내지 30 중량%, 바람직하게는 0.5 내지 10.0 중량%이다.
또한, 바람직하게는 티타늄의 산화물(TiO2), 징크의 산화물 (ZnO), 철의 산화물(Fe2O3), 지르코늄의 산화물 (ZrO2), 실리콘의 산화물 (SiO2), 망간의 산화물 (예컨대 MnO), 알루미늄의 산화물 (Al2O3), 세륨의 산화물 (예컨대 Ce2O3) 및/또는 이들의 혼합물과 같은 선택적으로 소수성화될 수 있는 미립자 UV 필터 또는 무기 색소가 사용될 수 있다.
피부 및/또는 모발 색소를 조절하는 활성제 (ACTIVES MODULATING SKIN AND/OR HAIR PIGMENTATION)
피부 및/또는 모발 라이트닝에 대한 바람직한 활성 성분은 하기로 구성된 군으로부터 선택된다:
코지산 (5-하이드록시-2-하이드록시메틸-4-피라논) {kojic acid (5-hydroxy-2-hydroxymethyl-4-pyranone)}, 코지산 유도체, 바람직하게는 코지산 다이팔미테이트(kojic acid dipalmitate), 알부틴(arbutin), 아스코르브산(ascorbic acid), 아스코르브산 유도체, 바람직하게는 마그네슘 아스코르빌 포스페이트(ascorbyl phosphate), 하이드로퀴논(hydroquinone), 하이드로퀴논 유도체, 레조르시놀(resorcinol), 레조르시놀 유도체, 바람직하게는 4-알킬레조르시놀 및 4-(1-페닐에틸)1,3-다이하이드록시벤젠(페닐에틸 레조르시놀), 사이클로헥실 카바메이트(바람직하게는 WO 2010/122178 및 WO 2010/097480에 개시된 하나 또는 그 이상의 사이클로헥실 카바메이트), 황-함유 분자(sulfur-containing molecules), 바람직하게는 글루타치온(glutathione) 또는 시스테인(cysteine), 알파-하이드록시산(alpha-hydroxy acids){바람직하게는 시트르산(citric acid), 락트산(lactic acid), 말산(malic acid)}, 이의 염 및 에스테르, N-아세틸 티로신(N-acetyl tyrosine) 및 유도체, 운데세노일 페닐알라닌(undecenoyl phenylalanine), 글루콘산(gluconic acid), 크로몬(chromone) 유도체, 바람작하게는 알로에신(aloesin), 플라보노이드(flavonoids), 1-아미노에틸 포스핀산(1-aminoethyl phosphinic acid), 티오우레아(thiourea) 유도체, 엘라그산(ellagic acid), 니코틴아미드 (니아신아미드), 징크(아연) 염, 바람직하게는 징크 클로라이드(zinc chloride) 또는 징크 글루코네이트(zinc gluconate), 투자플리신(thujaplicin) 및 유도체, 트라이터펜(triterpenes), 바람직하게는 마슬린산(maslinic acid), 스테롤(sterols), 바람직하게는 에르고스테롤(ergosterol), 벤조퓨라논(benzofuranones), 바람직하게는 센큐놀라이드(senkyunolide), 비닐 구이아콜(vinyl guiacol), 에틸 구이아콜(ethyl guiacol), 다이온산(dionic acids), 바람직하게는 옥토데센다이온산(octodecene dionic acid) 및/또는 아젤라산(azelaic acid), 질소 산화물(산화질소) 합성의 억제제, 바람직하게는 L-니트로아르기닌(L-nitroarginine) 및 이의 유도체, 2,7-다이니트로인다졸(2,7-dinitroindazole) 또는 티오시트룰린(thiocitrulline), 메탈 킬레이터 (바람직하게는 알파-하이드록시 지방산, 피트산(phytic acid), 흄산(부식산, humic acid), 담즙산(bile acid), 담즙 추출물(bile extracts), EDTA, EGTA 및 이의 유도체), 레티노이드(retinoids), 두유 및 추출물, 세린 프로테아제 억제제(serine protease inhibitors) 또는 리포산(lipoic acid) 또는 피부 및 모발 라이트닝을 위한 다른 합성 또는 천연 활성 성분, 후자는 바람직하게는 식물 추출물 형태로 사용되는 것으로서, 바람직하게는 베어베리(bearberry) 추출물, 쌀 추출물, 파파야 추출물, 터메릭(강황, turmeric) 추출물, 멀베리(오디, mulberry) 추출물, 벵코앙(bengkoang) 추출물, 넛그래스(nutgrass, 향부자) 추출물, 리코리스(감초, liquorice) 뿌리 추출물 또는 이로부터 농축 또는 분리된 구성성분, 바람직하게는 글라브리딘(glabridin) 또는 리코찰콘 A(licochalcone A), 아르토카르푸스(artocarpus) 추출물, 루멕스(rumex) 및 라물루스(ramulus) 종의 추출물, 파인(소나무, pine) 종(pinus)의 추출물, 비티스(vitis) 종의 추출물, 또는 이로부터 분리 또는 농축된 스틸벤(stilbene) 유도체, 삭시프리지(saxifrage) 추출물, 스쿠텔레리아(scutelleria) 추출물, 포도 추출물 및/또는 미세조류(microalgae) 추출물, 특히, 테트라셀미스 수에시카(Tetraselmis suecica) 추출물.
바람직한 성분 (b)의 피부 라이트너(skin lightener)는 티로시나제 억제제로 코지산 및 페닐에딜 레소르시놀, 베타- 및 알파-알부틴(arbutin), 하이드로퀴논, 니코틴아미드, 다이오 산(dioic acid), Mg 아스코르빌 포스페이트 및 비타민 C 및 이의 유도체, 멀베리 추출물, 벵코앙 추출물, 파파야 추출물, 터메릭(termeric) 추출물, 넛그래스 추출물, 감초 추출물{글리시리진(glycyrrhizin) 함유}, 알파-하이드록시-산, 4-알킬레조르시놀, 4-하이드록시아니솔(4-hydroxyanisole)이다. 이러한 피부 라이트너는 매우 좋은 활성 때문에 특히, 본 발명에 따른 스클라레올라이드(sclareolide)와 조합하여, 선호된다. 또한, 상기 바람직한 피부 라이트너는 쉽게 이용가능하다.
이러한 관점에서 이로운 피부 및 모발 태닝 활성 성분은 티로시나제의 기질 또는 기질 유사체로 예컨대 L-티로신, N-아세틸 티로신, L-DOPA 또는 L-다이하이드록시페닐알라닌, 잔틴 알킬로이드(xanthine alkaloid)로 예컨대, 카페인, 테오브로민(theobromine) 및 테오필린(theophylline) 및 이들의 유도체, 프로오피오멜라노코르틴(proopiomelanocortin) 펩티드로 예컨대, ACTH, 알파-MSH, 이들의 펩티드 유사체 및 멜라노코르틴 수용체에 결합하는 다른 물질, 펩티드로 예컨대, Val-Gly-Val-Ala-Pro-Gly, Lys-lle- Gly-Arg-Lys 또는 Leu-lle-Gly-Lys, 퓨린, 피리미딘, 엽산(folic acid), 구리염으로 예컨대 글루콘산 구리, 염화 구리 또는 피롤리돈산 구리, 1,3,4-옥사다이아졸-2-티올(1,3,4-oxadiazole-2-thiol)로 5-피라진-2-일-1,3,4-옥사다이아졸-2-티올(5-pyrazin-2-yl-1,3,4-oxadiazole-2-thiol), 커큐민(curcumin), 징크 다이글리시네이트[zinc diglycinate, (Zn(GIy)2)], EP 0 584 178에 예를 들어 기술된 탄산수소 마그네슘(ll) 복합체 (manganese(ll) bicarbonate complex) ("가성카탈라제(pseudocatalases)"), WO 2005/032501에 예를 들어 기술된 사중치환 사이클로헥센 유도체, WO 2005/102252 및 WO 2006/010661에 기술된 이소프레노이드(isoprenoid), 멜라닌 유도체로 예컨대, 멜라신-100(Melasyn-100) 및 멜라제(MelanZe), 다이아실 글리세롤, 지방족 또는 고리형 다이올, 소랄렌(psoralens), 프로스타글란딘 및 이의 유사체, 아데닐산고리화 효소의 활성체 및 케라티노사이트에 대한 멜라노좀의 전이를 활성화화는 세린 프로테아제 또는 PAR-2 수용체의 아고니스트와 같은 화합물, 국화(chrysanthemum) 종, 오이풀(sanguisorba) 종, 호두 추출물, 우루쿰(urucum) 추출물, 루바브(rhubarb) 추출물, 미세조류 추출물, 특히 아이소크라이시스 갈바나(Isochrysis galbana), 트레할로스(trehalose), 에리스롤로스(erythrulose) 및 다이하이드로옥시아세톤(dihydroxyacetone)의 식물 및 식물 일부의 추출물이다. 또한, 피부 및 모발의 변색 또는 갈색화를 가져오는 플라보노이드(예를 들어, 퀘르세틴, 람네틴(rhamnetin), 캠프페롤, 피세틴(fisetin), 제니스테인(genistein), 다이드제인(daidzein), 크리신(chtysin) 및 아피제닌(apigenin), 에피카테킨(epicatechin), 다이오스민(diosmin) 및 다이오스메틴(diosmetin), 모린(morin), 퀘르시트린(quercitrin), 나린제닌(naringenin), 헤스페리딘(hesperdin), 플로리진(phloridzin) 및 플로레틴(phloretin))가 사용될 수 있다.
본 발명에 따른 제품 내 피부 및 모발 색소의 조절을 위한 추가적인 활성성분(하나 이상의 화합물)의 앞서 언급된 예들의 양은 제제의 총 중량을 기초로 바람직하게 0.00001 내지 30 중량 %(wt. %), 보다 바람직하게 0.0001 내지 20 중량 %(wt. %), 특히 바람직하게 0.001 내지 5 중량 %(wt. %)이다.
항-노화 활성제(ANTI-
AGEING
ACTIVES)
본 발명의 내용상, 항노화 또는 생체제는, 예를 들어, 항산화제, 매트릭스-메탈로프로테이나제 억제제(MMPI), 피부 보습제, 글리코사민글리칸 자극제, 항-면역제, TRPV1 길항제 및 식물 추출물이다.
항산화제(Antioxidants). 적합한 항산화제는 아미노산 (바람직하게는 글라이신, 히스티딘, 티로신, 트립토판) 및 그의 유도체, 이미다졸 {바람직하게는 우로칸산(urocanic acid)} 및 그의 유도체, 펩타이드, 바람직하게는 D,L-카르노신(D,L-carnosine), D-카르노신(D-carnosine), L-카르노신(L-carnosine) 및 그의 유도체 (바람직하게는 안세린(anserine)), 카르니틴(carnitine), 크레아틴(creatine), 마트리킨 펩타이드(matrikine peptides) {바람직하게는 라이실-트레오닐-트레오닐-라이실-세린(lysyl-threonyl-threonyl-lysyl-serine)} 및 팔미토일화 펜타펩타이드(palmitoylated pentapeptides), 카로티노이드(carotenoid), 카로텐(carotenes) {바람직하게는 알파-카로텐, 베타-카로텐, 리코펜(lycopene)} 및 그의 유도체, 리포산(lipoic acid) 및 그의 유도체 {바람직하게는 다이하이드로리포산(dihydrolipoic acid)}, 아우로티오글루코스(aurothioglucose), 프로필 티오우라실 및 기타 티올 (바람직하게는 티오레독신, 글루타티온, 시스테인, 시스틴, 시스타민 및 그의 글리코실, N-아세틸, 메틸, 에틸, 프로필, 아밀, 부틸 및 라우릴, 팔미토일, 올레일, 감마-리놀레일, 콜레스테릴, 글리세릴 및 올리고글리세릴 에스테르) 및 그의 염, 다이라우릴 티오다이프로피오네이트, 다이스테아릴 티오다이프로피오네이트, 티오다이프로피온산 및 그의 유도체 (바람직하게는 에스테르, 에테르, 펩타이드, 리피드, 뉴클레오타이드, 뉴클레오사이드 및 염) 및 매우 작게 허용된 투여량 (예컨대 pmol 내지 μmol/kg)의 설폭시민(sulfoximine) 화합물 (바람직하게는 부티오닌 설폭시민, 호모시스테인 설폭시민, 부티오닌 설폰, 펜타-, 헥사-, 헵타티오닌 설폭시민), 또한 (금속) 킬레이터 {바람직하게는 알파-하이드록시 지방산, 팔미트산(palmitic acid), 피트산(phytic acid), 락토페린(lactoferrin), 알파-하이드록시산 (바람직하게는 시트르산(citric acid), 락트산(lactic acid), 말산(malic acid)), 흄산(humic acid), 담즙산(bile acid), 담즙(bile) 추출물, 탄닌(tannins), 빌리루빈(bilirubin), 빌리베르딘(biliverdin), EDTA, EGTA 및 그의 유도체}, 불포화 지방산 및 그의 유도체 {바람직하게는 감마-리놀렌산, 리놀레산(linoleic acid), 올레산(oleic acid)}, 엽산(folic acid) 및 그의 유도체, 유비퀴논(ubiquinone) 및 그의 유도체, 유비퀴놀(ubiquinol) 및 그의 유도체, 비타민 C 및 유도체 (바람직하게는 아스코르빌 팔미테이트, Mg 아스코르빌 포스페이트, 아스코르빌 아세테이트, 아스코르빌 글루코사이드), 토코페롤 및 유도체 (바람직하게는 비타민 E 아세테이트), 비타민 A 및 유도체 (비타민 A 팔미테이트) 및 벤조익 수지(benzoic resin)의 코니페릴 벤조에이트, 루틴산(rutinic acid) 및 그의 유도체, 플라보노이드 및 그의 글리코실화된 전구체, 특히 퀘르세틴(quercetin) 및 그의 유도체, 바람직하게는 알파-글루코실 루틴, 로즈마린산(rosmarinic acid), 카르노솔(carnosol), 카르노솔산(carnosolic acid), 레스베라트롤(resveratrol), 카페인산(caffeic acid) 및 그의 유도체, 시납산(sinapic acid) 및 그의 유도체, 페룰산(ferulic acid) 및 그의 유도체, 커큐미노이드(curcuminoid), 클로로겐산(chlorogenic acid) 및 그의 유도체, 레티노이드(retinoid), 바람직하게는 레티닐 팔미테이트, 레티놀 또는 트레티노인(tretinoin), 우르솔산(ursolic acid), 레불린산(levulinic acid), 부틸 하이드록시톨루엔, 부틸 하이드록시아니솔, 노르다이하이드로구아이악산(nordihydroguaiac acid), 노르다이하이드로구아이아레트산(nordihydroguaiaretic acid), 트라이하이드록시부티로페논, 요산(uric acid) 및 그의 유도체, 만노스 및 그의 유도체, 징크(아연) 및 그의 유도체 (바람직하게는 ZnO, ZnSO4), 셀레늄 및 그의 유도체 (바람직하게는 셀레늄 메티오닌), 슈퍼옥사이드 디스뮤타아제(superoxide dismutase), 스틸벤(stilbenes) 및 그의 유도체 (바람직하게는 스틸벤 옥사이드, 트랜스-스틸벤 옥사이드) 및 본 발명에 따른 적합한 이들 인용된 활성 성분의 유도체(염, 에스테르, 에테르, 당, 뉴클레오타이드, 뉴클레오사이드, 펩타이드 및 리피드), 또는 항산화 효과를 갖는 식물의 추출물 또는 분획물, 바람직하게는 녹차, 루이보스(rooibos), 허니부쉬(honeybush), 포도, 로즈마리, 세이지(sage), 멜리사(melissa), 타임(thyme), 라벤더, 올리브, 오트(oats), 코코아, 은행(ginkgo), 인삼(ginseng), 감초(liquorice), 인동(honeysuckle), 괴화(sophora), 갈근(pueraria), 소나무(pinus), 시트러스(citrus), 필란터스 엠브리카(Phyllanthus emblica) 또는 세이트존스워트(고추나물, 성요한초, St. John's wort), 포도 종자(grape seeds), 맥아(wheat germ), 필란터스 엠브리카(Phyllanthus emblica), 코엔자임, 바람직하게는 코엔자임 Q10, 플라스토퀴논(plastoquinone) 및 메나퀴논(menaquinone)을 포함한다. 바람직한 항산화제는 비타민 A 및 유도체, 비타민 C 및 유도체, 토코페롤 및 유도체, 바람직하게는 토코페릴 아세테이트, 및 유비퀴논으로 이루어진 군에서 선택된다.
만일 비타민 E 및/또는 그의 유도체가 항산화제로서 사용되는 경우, 그 농도는 제형(formulation)의 총 중량에 대하여 약 0.001 내지 약 10 중량 % (% b.w.)의 범위로부터 선택되는 것이 유리하다. 만일 비타민 A 또는 비타민 A 유도체 또는 카로텐 또는 그의 유도체가 항산화제로서 사용되는 경우, 그 농도는 제형의 총 중량에 대하여 약 0.001 내지 약 10 중량 % (% b.w.)의 범위로부터 선택되는 것이 유리하다.
매트릭스- 메탈로프로테이나제 억제제 ( MMPI ). 바람직한 조성물은 매트릭스-메탈로프로테이나제 억제제(matrix-metalloproteinase inhibitors), 특히, 효소로 콜라겐을 쪼개어 매트릭스-메탈로프로테이나제를 억제하는 것을 함유하고, 상기 억제제는 다음으로 이루어진 군에서 선택된다: 우르솔산(ursolic acid), 레티닐 팔미테이트(retinyl palmitate), 프로필 갈레이트(propyl gallate), 프리코센(precocenes), 6-하이드록시-7-메톡시-2,2-디메틸-1(2H)-벤조피란(6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)-benzopyran), 3,4-다이하이드로-6-하이드록시-7-메톡시-2,2-다이메틸-1(2H)-벤조피란(3,4-dihydro-6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)-benzopyran), 벤즈아미딘 하이드로클로라이드(benzamidine hydrochloride), 시스테인 프로테이나제 억제제 N-에틸말레이미드(N-ethylmalemide) 및 세린 프로테아제 억제제의 엡실론-아미노-n-카프로산(epsilon-amino-n-caproic acid): 페닐메틸설포닐플루오라이드(phenylmethylsufonyl-fluoride), 콜히빈(collhibin) {Pentapharm 사; INCI: 가수분해된 쌀 단백질(hydrolysed rice protein)}, 오에노테롤(oenotherol) {Soliance 사; INCI: 프로필렌 글리콜, 수분(aqua), 큰달맞이꽃(oenothera biennis) 뿌리 추출물, 예를 들어 석류(pomegranate)로부터의 엘라그산(ellagic acid) 및 엘라기타닌(ellagitannins)}, 포스포라미돈 히노키티올(phosphoramidone hinokitiol), EDTA, 갈라딘(galardin), 에퀴스탓(EquiStat) {Collaborative Group 사; 사과 열매 추출물, 콩씨앗 추출물, 우르솔산(ursolic acid), 콩 이소플라본 및 콩 단백질}, 세이지(sage) 추출물, MDI {Atrium 사; INCI: 글리코사미노글리칸(glycosaminoglycans)}, 페르미스킨(fermiskin) {Silab/Mawi 사; INCI: 물 및 표고버섯(lentinus edodes) 추출물), 엑팀프 1.9.3(actimp 1.9.3) {Expanscience/Rahn 사; INCI: 가수분해된 루핀 단백질(hydrolysed lupine protein)}, 리포벨 소야글리콘(lipobelle soyaglycone) {Mibelle 사; INCI: 알코올, 폴리소르베이트 80(polysorbate 80), 레시틴 및 콩 이소플라본}, 녹차 및 홍차의 추출물 및 WO 02 069992 A1 (상기 문헌의 표 1-12 참조, 본원에서 참조로 병합)에 열거된 기타 식물 추출물, 콩으로부터의 단백질 또는 당단백질, 쌀로부터의 가수분해된 단백질, 완두콩(pea) 또는 루핀(lupine), MMPs를 억제하는 식물 추출물, 바람직하게는 표고버섯(shitake mushroom) 추출물, 장미과(Rosaceae), 장미과 아류의 잎의 추출물, 보다 바람직하게는 예를 들면 SymMatrix {Symrise 사, INCI: 말토덱스트린(Maltodextrin), 블랙베리(Rubus Fruticosus) 잎 추출물}과 같은 블랙베리 잎 추출물(바람직하게는 본원에서 참조로 병합된, WO 2005 123101 A1에서 개시된 바와 같은). 바람직한 활성제는 레티닐 팔미테이트, 우르솔산, 장미과와 장미과 아류의 잎의 추출물, 제니스테인(genistein) 및 다이제인 (daidzein)으로 이루어진 군으로부터 선택된다.
피부-보습제(Skin-moisturizing agent). 바람직한 피부 보습제는 3 내지 12개의 탄소원자를 포함하는 알칸 다이올 또는 알칸 트라이올, 바람직하게는 C3-C10-알칸 다이올 및 C3-C10-알칸 트라이올로 이루어진 군에서 선택된다. 보다 바람직하게는 피부 보습제는 다음으로 이루어진 군에서 선택된다: 글리세롤, 1,2-프로필렌 글리콜, 1,2-부틸렌 글리콜, 1,3-부틸렌 글리콜, 1,2-펜탄다이올, 1,2-헥산다이올, 1,2-옥탄다이올 및 1,2-데칸다이올.
글리코사미노글리칸 자극제( Glycosaminoglycan stimulators). 바람직한 조성물은, 히알루론산(hyaluronic acid) 및 유도체 또는 염, 서브리스킨(Subliskin) {Sederma, INCI: 시노리조비움 멜리로티(Sinorhizobium Meliloti) 효모 여과액, 세틸 하이드록시에틸셀룰로오스(Cetyl Hydroxyethylcellulose), 레시틴}, 히알루픽스(Hyalufix) {BASF, INCI: 물, 부틸렌 글리콜, 월도(alpinia galanga) 잎 추출물, 잔탄 검, 카프릴릭/카프릭 트리글리세라이드}, 스티뮬히알(Stimulhyal) {Soliance, INCI: 칼슘 케토글루코네이트(Calcium ketogluconate)}, 신-글리칸(Syn-Glycan) {DSM, INCI: 테트라데실 아미노부티로일발릴아미노부티릭 우레아 트리플루오로아세테이트(Tetradecyl Aminobutyroylvalylaminobutyric Urea Trifluoroacetate), 글리세린, 마그네슘 클로라이드), 칼파리안(Kalpariane) {Biotech Marine}, DC 업레귤렉스(DC Upregulex) {Distinctive Cosmetic Ingredients, INCI: 물, 부틸렌 글리콜, 포스포리피드, 가수분해된 세리신(Hydrolyzed Sericin)}, 글루코사민, N-아세틸 글루코사민, 레티노이드, 바람직하게는 레티놀 및 비타민 A, 우엉(Arctium lappa) 열매 추출물, 비파나무(Eriobotrya japonica) 추출물, 겐크와닌(Genkwanin), N-메틸-L-세린, (-)-알파-비사볼롤((-)-alpha-bisabolol) 또는 합성 알파-비사볼롤로, 예를 들어 Symrise의 드라고산톨(Dragosantol) 및 드라고산톨 100(Dragosantol 100), 오트 글루칸, 에키네시아 푸르푸레아(Echinacea purpurea) 추출물 및 콩 단백질 가수분해물로 이루어진 군으로부터 선택된 글리코사미노글리칸의 합성을 자극하는 물질을 포함한다. 바람직한 활성제는 히알루론산 및 유도체 또는 염, 레티놀 및 유도체, (-)-알파-비사볼롤 또는 합성 알파-비사볼롤로 예를 들어 시므라이즈(Symrise)의 드라고산톨(Dragosantol) 및 드라고산톨(Dragosantol) 100, 오트 글루칸, 에키네시아 푸르푸레아 추출물, 시노리조비움 멜리로티 효모 여과액, 칼슘 케토글루코네이트, 월도(Alpinia galanga) 잎 추출물 및 테트라데실 아미노부티로일발릴아미노부티릭 우레아 트리플루오로아세테이트로 이루어진 군에서 선택된다.
항- 염증제 (Anti-inflammatory agent). 조성물은 또한 항-염증 및/또는 발적 및/또는 가려움증 완화 성분, 특히 하이드로코티손(hydrocortisone), 덱사메타손(dexamethasone), 덱사메타손 포스페이트(dexamethasone phosphate), 메틸 프레드니솔론(methyl prednisolone) 또는 코티손(cortisone)으로 이루어진 군에서 선택된 코르티코스테로이드 타입의 스테로이드성 물질을 포함할 수 있고, 이들은 항-염증 활성 성분 또는 발적 및 가려움을 완화시키는 활성 성분으로 유리하게 사용되며, 그것들의 목록은 다른 스테로이드성 항-염증제의 추가에 의해 확장될 수 있다. 비-스테로이드성 항-염증제 또한 사용될 수 있다. 여기에서 인용될 수 있는 예는 피록시캄(piroxicam) 또는 테녹시캄(tenoxicam)과 같은 옥시캄(oxicam); 아스피린, 다이살시드(disalcid), 솔프린(solprin) 또는 펜도살(fendosal)과 같은 살리실레이트; 다이클로페낙(diclofenac), 펜클로페낙(fenclofenac), 인도메타신(indomethacin), 설린닥(sulindac), 톨메틴(tolmetin) 또는 클린다낙(clindanac)과 같은 아세트산 유도체; 메페나믹(mefenamic), 메클로페나믹(meclofenamic), 풀루페나믹(flufenamic) 또는 니플루믹(niflumic)과 같은 페나메이트; 이부프로펜(ibuprofen), 나프록센(naproxen), 베녹사프로펜(benoxaprofen)과 같은 프로피온산 유도체 또는 페닐부타존(phenylbutazone), 옥시페닐부타존(oxyphenylbutazone), 페브라존(febrazone) 또는 아자프로파존(azapropazone)과 같은 피라졸이다. 안트라닐산 유도체, 특히 WO 2004/047833 A1에 기재된 아베난스라미드(avenanthramide)가 본 발명에 따른 조성물에서 바람직한 항-가려움증 성분이다.
또한, 천연 또는 천연적으로 발생한 항-염증성 물질들의 혼합물 또는 발적 및/또는 가려움증을 완화시켜주는 물질들의 혼합물이 유용하고, 특히 카모마일, 알로에 베라, 콤미포라(Commiphora) 종, 루비아(Rubia) 종, 윌로우(willow), 윌로우-허브, 오트, 카렌듈라(calendula), 아르니카(arnica), 성요한초(St John's wort), 허니서클(honeysuckle), 로즈마리, 시계초(Passiflora incarnata), 풍년화(witch hazel), 생강 또는 에키네시아(Echinacea); 바람직하게는 카모마일, 알로에 베라, 오트, 카렌듈라, 아르니카, 허니서클, 로즈마리, 풍년화, 생강 또는 에키네시아로부터의 추출물 또는 분획물 로 이루어진 군에서 선택되는것의 추출물 또는 분획물, 및/또는 순수 물질, 바람직하게는 알파-비사볼롤(alpha-bisabolol), 아피제닌(apigenin), 아피제닌-7-글루코사이드, 진저롤(gingerol), 쇼가올(shogaol), 진저다이올(gingerdiol), 디하이드로진저다이온(dehydrogingerdione), 파라돌(paradol), 천연 또는 천연적으로 발생한 아베난스라미드, 바람직하게는 트라닐라스트(tranilast), 아베난스라미드 A, 아베난스라미드 B, 아베난스라미드 C, 비-천연 또는 비-천연적으로 발생한 아베난스라미드, 바람직하게는 디하이드로아베난스라미드 D, 디하이드로아베난스라미드 E, 아베난스라미드 D, 아베난스라미드 E, 아베난스라미드 F, 보스웰산(boswellic acid), 피토스테롤(phytosterol), 글리시리진(glycyrrhizin), 글라브리딘(glabridin) 및 리코찰콘 A(licochalcone A); 바람직하게는 알파-비사볼롤, 천연 아베난스라미드, 비-천연 아베난스라미드, 바람직하게는 디하이드로아베난스라미드 D (WO 2004/047833 A1에서 기재), 보스웰산, 피토스테롤, 글리시리진, 및 리코찰콘 A로 이루어진 군으로부터 선택되는 것, 및/또는 알란토인(allantoin), 판테놀(panthenol), 라놀린(lanolin), (슈도-)세라미드 [바람직하게는 세라미드 2, 하이드록시프로필 비스팔미타미드 MEA, 세틸옥시프로필 글리세릴 메톡시프로필 미리스타미드, N-(1-헥사데카노일)-4-하이드록시-L-프롤린 (1-헥사데실) 에스테르, 하이드록시에틸 팔미틸 옥시하이드록시프로필 팔미타미드], 글리코스핑고리피드, 피토스테롤, 키토산, 만노스, 락토스 및 β-글루칸, 특히 오트로부터의 1,3-1,4-β-글루칸이 유용하다.
본 발명에 있어서 비사볼롤이 사용될 때, 그것은 천연 또는 합성 유래일 수 있으며, 바람직하게는 "알파-비사볼롤"이다. 바람직하게는, 사용되는 비사볼롤은 합성적으로 제조되거나 천연의 (-)-알파-비사볼롤 및/또는 합성의 혼합된 이성체 알파-비사볼롤이다. 만일 천연의 (-)-알파-비사볼롤이 사용되는 경우, 이것은 또한 에센셜 오일 또는 식물 추출물 또는 그의 분획물의 구성성분, 예를 들어, 카모마일 또는 바닐로스몹시스(Vanillosmopsis) {특히 바닐로스몹시스 에리쓰로파파(Vanillosmopsis erythropappa) 또는 바닐로스몹시스 아르보레아(Vanillosmopsis arborea)}의 오일(의 분획물) 또는 추출물의 구성성분으로서 사용될 수 있다. 합성 알파-비사볼롤은, 예를 들어, Symrise 사의 "드라고산톨(Dragosantol)"이라는 명칭의 제품으로부터 입수할 수 있다.
본 발명에 있어서 생강 추출물이 사용되는 경우, 바람직하게는 신선한 또는 건조된 생강 뿌리의 추출물이 사용되며, 이러한 추출물은 메탄올, 에탄올, 이소-프로판올, 아세톤, 에틸 아세테이트, 이산화탄소 (CO2), 헥산, 메틸렌 클로라이드, 클로로포름 또는 다른 용매 또는 견줄만한 극성의 용매 혼합물로 추출하여 제조된다. 상기 추출물은 예컨대 진저올, 쇼가올, 진저다이올, 디하이드로진저다이온 및/또는 파라돌과 같은 구성성분의 활성 피부 자극을 감소시키는 양의 존재에 의해 특정된다.
TRPV1 길항제( TRPV1 antagonists). 피부 신경의 과민증을 감소시키는 적절한 화합물은 예를 들어, WO 2009/087242 A1에 개시된 바와 같은 트랜스-4-터트-부틸시클로헥사놀을 포함하는 TRVP1 길항제로서의 작용, 또는 μ-수용체의 활성에 의한 TRPV1의 간접적 조절제로서, 예를 들어 아세틸 테트라펩티드-15의 작용에 기초하는것이 바람직하다.
박리제( Desquamating agent). 조성물은 또한 박리제(성분 b5)를 제제의 총 중량에 대하여 약 0.1 내지 약 30 중량 % (% b.w.), 바람직하게는 약 0.5 내지 약 15 중량 % (% b.w.), 보다 바람직하게는 약 1 내지 약 10 중량 % (% b.w.)으로 포함할 수 있다. "박리제"라는 표현은 하기의 작용을 할 수 있는 임의의 화합물을 의미하는 것으로 이해된다:
각질제거(exfoliation)를 촉진하여 직접적으로 박리(desquamation) 작용, 예를 들어, β-하이드록시산, 특히 살리실산 및 그의 유도체(5-n-옥타노일살리실산 포함); α-하이드록시산, 예를 들어 글리콜산(glycolic acid), 시트르산(citric acid), 락트산(lactic acid), 타르타르산(tartaric acid), 말산(malic acid)이나 만델산(mandelic acid); 우레아; 겐티스산(gentisic acid); 올리고푸코스; 신남산(cinnamic acid); 회화나무(sophora japoniea)의 추출물; 레스베라트롤(resveratrol) 및 자스몬산(jasmonic acid)의 일부 유도체;
또는 박리 또는 코르네오데스모좀(corneodesmosomes), 글리코시데이즈(glycosidases), 각질층 키모트립 효소(stratum corneum chymotryptic enzyme; SCCE) 또는 다른 단백질 분해효소(트립신, 키모트립신 유사체)의 분해에 관여하는 효소에서의 작용. 이에는 하기 무기염 킬레이트제가 언급될 수 있다: EDTA; N-아실-N,N',N'-에틸렌디아민트리 아세트산; 아미노설폰 화합물 및 특히 (N-2-하이드록시에틸피페라진-N-2-에탄)설폰산 (HEPES); 2-옥소티아졸리딘-4-카르복시산(프로시스테인)의 유도체; 글리신 유형의 알파-아미노산의 유도체 (EP 0852949에 기재, 및 BASF에 의해 상품명 TRILON M으로 판매되는 메틸글리신 다이아세테이트 나트륨); 꿀; O-옥타노일-6-D-말토스 및 N-아세틸글루코사민과 같은 당 유도체; SILAB 사에 의해 Recoverine® 명칭으로 판매되는 것과 같은 체스트넛(chestnut) 추출물, SILAB사에 의해 Exfolactive® 명칭으로 판매되는 것과 같은 프리클리 피어(prickly pear) 추출물, 또는 Degussa 사에 의해 판매되는 Phytosphingosine SLC®(살리실산으로 그라프트된 피토스핑고신).
본 발명에 적합한 박리제는, 술폰산, 칼슘 킬레이트제, 글리콜산, α-하이드록시산, 예컨대 글리콜산, 시트르산, 락트산, 타르타르산, 말산 또는 만델산; 아스코르브산 및 그의 유도체, 예컨대 아스코르빌 글루코시드 및 마그네슘 아스코르빌 포스페이트; 니코틴아미드; 우레아; (N-2-하이드록시에틸피페라진-N-2-에탄)설폰산 (HEPES), β-하이드록시산, 예컨대 살리실산 및 그의 유도체, 레티노이드, 예컨대 레티놀 및 그의 에스테르, 레티날, 레티노산(retinoic acid) 및 그의 유도체, FR 2570377 A1, EP 0199636 A1, EP 0325540 A1, EP 0402072 A1에 개시된 것들, 체스트넛 또는 프리클리 피어 추출물, 특히 SILAB에 의해 판매되는 것; 시스테인 또는 시스테인 전구체와 같은 환원시키는 화합물을 포함하는 군에서 특히 선택될 수 있다.
또한, 사용될 수 있는 박리제는, 소위 비타민 B3 또는 비타민 PP라 불리는, 니코틴산 및 그의 에스테르 및 니코틴아미드, 특히 EP 1529522 A1 출원에 개시된 바와 같은, 아스코르브산 및 그의 전구체이다.
항- 셀룰라이트제 (Anti-cellulite agent). 항-셀룰라이트제 및 지질분해제는 바람직하게는 WO 2007/077541에 개시된 것들, 및 베타-아드레날린 수용체 작용제, 예컨대 시네프린(synephrine) 및 그의 유도체, 및 WO 2010/097479에 개시된 시클로헥실 카바메이트로 이루어진 군에서 선택된다. 항-셀룰라이트제의 활성을 개선시키거나 촉진하는 제제(agent), 특히 C 신경섬유를 자극 및/또는 감극시키는 제제는, 바람직하게는 캡사이신 및 이의 유도체, 바닐릴-노닐아미드 및 이의 유도체, L-카르니틴, 코엔자임 A, 이소플라보노이드, 콩 추출물, 아나나스(ananas) 추출물 및 공액 리놀레산으로 이루어진 군으로부터 선택된다.
지방개선제(Fat enhancing agent). 본 발명에 따르면 제형 및 제품은 또한 지방 개선제의 활성을 개선시키거나 촉진하는 제제(agent) 뿐만 아니라 하나 이상의 지방개선제 및/또는 지방형성제를 포함할 수도 있다. 지방개선제는 예를 들어 하이드록시메톡시페닐 프로필메틸메톡시벤조퓨란(상품명: Sym3D®)이다.
모발 성장 활성제 또는 억제제(HAIR GROWTH ACTIVATOR OR INHIBITORS)
본 발명에 따른 제형 및 제품은 또한 하나 이상의 모발 성장 활성제, 즉, 모발 성장을 자극하기 위한 제제(agent)를 포함할 수 있다. 모발 성장 활성제는 바람직하게 피리미딘 유도체, 예컨대 2,4-다이아미노피리미딘-3-옥사이드 {아미넥실(Aminexil)}, 2,4-다이아미노-6-피페리디노피리미딘-3-옥사이드 {미녹시딜(Minoxidil)} 및 이의 유도체, 6-아미노-1,2-다이하이드로-1-하이드록시-2-이미노-4-피페리디노피리미딘 및 이의 유도체, 잔틴 알칼로이드(xanthine alkaloids), 예컨대 카페인, 테오브로민(theobromine) 및 테오필린(theophylline) 및 이의 유도체, 퀘르세틴 및 유도체, 다이하이드로퀘르세틴 {탁시폴린(taxifolin)} 및 유도체, 포타슘 채널 오프너, 항안드로겐제, 합성 또는 천연 5-환원효소 억제제, 니코틴산 에스테르, 예컨대 토코페릴 니코티네이트, 벤질 니코티네이트 및 C1-C6 알킬 니코티네이트, 단백질, 예컨대 트리펩타이드 Lys-Pro-Val, 다이펜시프렌(diphencypren), 호르몬, 피나스테라이드(finasteride), 두타스테라이드(dutasteride), 프루타마이드(flutamide), 바이칼루타마이드(bicalutamide), 프레그난(pregnane) 유도체, 프로게스테론 및 이의 유도체, 사이프로테론 아세테이트, 스피로노락론 및 다른 이뇨제, 칼신우린(calcineurin) 억제제, 예컨대 FK506 {타크롤리무스(Tacrolimus), 후지마이신(Fujimycin)} 및 이의 유도체, 사이클로스포린 A 및 이의 유도체, 아연 및 아연 염, 폴리페놀, 프로시아니딘(procyanidin), 프로안토시아니딘(proanthocyanidin), 피토스테롤(phytosterol), 예컨대 베타-시토스테롤(beta-sitosterol), 비오틴(biotin), 유제놀(eugenol), (±)-베타-시트로넬롤((±)-beta-citronellol), 판테놀(panthenol), 예를 들어 근육으로부터의 글리코겐, 미생물, 조류(algae) 추출물, 식물 및 식물 부분의 추출물, 예컨대 민들레 (Leontodon 또는 Taraxacum 속), 오르토시폰(Orthosiphon), 바이텍스(Vitex), 커피(Coffea), 파우리니아(Paullinia), 테오브로마(Theobroma), 족두리풀(Asiasarum), 호박(Cucurbita) 또는 괴화(Styphnolobium), 톱야자 나무(Serenoa repens, saw palmetto), 고삼(Sophora flavescens), 파이지움 아프리카눔(Pygeum africanum), 기장(Panicum miliaceum), 승마(Cimicifuga racemosa), 글리신맥스(Glycine max), 정향나무(Eugenia caryophyllata), 안개나무(Cotinus coggygria), 하와이 무궁화(Hibiscus rosa-sinensis), 차나무(Camellia sinensis), 마테(Ilex paraguariensis), 아이소크라이시스 갈바나(Isochrysis galbana), 감초(licorice), 포도, 사과, 보리(barley) 또는 홉(hop)의 추출물, 또는/및 쌀 또는 밀로의 가수분해물의 추출물로 이루어진 군으로부터 선택된다.
그 대신에, 본 발명에 따른 제형 및 제품은 하나 이상의 모발 성장 억제제(상기 기술됨), 즉, 모발 성장을 감소 또는 억제하기 위한 제제(agent)를 포함할 수 있다. 모발 성장 억제제는 바람직하게 액티빈(activin), 액티빈 유도체 또는 액티빈 작용제, 오르니틴 탈카르복실화효소 억제제, 예컨대 알파-다이플루오로메틸오르니틴 또는 펜타사이클릭 트리테르펜(pentacyclic triterpene) 예를 들어 우르솔산(ursolic acid), 베툴린(betulin), 베툴린산(betulinic acid), 올레아놀산(oleanolic acid) 및 이의 유도체, 5 알파-환원효소 억제제, 안드로겐 수용체 길항제, S-아데노실메티오닌 탈카르복실화효소 억제제, 감마-글루타밀 트랜스펩티다아제 억제제, 트랜스글루타미나아제 억제제, 소이빈-유래 세린 프로테아제 억제제, 미생물, 조류, 다른 미세조류 또는 식물 및 식물 부분으로부터의 추출물, 예를 들어 콩과(Leguminosae), 가지과(Solanaceae), 화본과(Graminae), 박주가리과(Asclepiadaceae) 또는 박과(Cucurbitaceae), 콘드러스속(Chondrus), 글로이오펠티스속(Gloiopeltis), 비단풀속(Ceramium), 더빌리아속(Durvillea), 글리신 맥스(Glycine max), 오이풀속(Sanguisorba officinalis), 금잔화(Calendula officinalis), 조롱나무속(Hamamelis virginiana), 아니카(Arnica montana), 흰버드나무(Salix alba), 물레나물(Hypericum perforatum) 또는 김네마 실베스터(Gymnema sylvestre)의 추출물로 구성된 군으로부터 선택된다.
냉각제 (COOLING AGENTS)
조성물은 또한 바람직하게 하기 리스트로부터 선택되는 생리적인 냉각효과를 가지는 하나 이상의 물질(냉각제)을 포함할 수 있다: 멘톨 및 멘톨 유도체 (예를 들면 L-멘톨, D-멘톨, 라세믹 멘톨, 이소멘톨, 네오이소멘톨, 네오멘톨), 멘틸에테르 (예를 들면 (l-멘톡시)-1,2-프로판다이올, (l-멘톡시)-2-메틸-1,2-프로판다이올, l-멘틸-메틸에테르), 멘틸에스테르 (예를 들면 멘틸포미에이트, 멘틸아세테이트, 멘틸이소뷰티레이트, 멘틸락테이트, L-멘틸-L-락테이트, L-멘틸-D-락테이트, 멘틸-(2-메톡시)아세테이트, 멘틸-(2-메톡시에톡시)아세테이트, 멘틸피로글루타메이트), 멘틸카보네이트 (예를 들면 멘틸프로필렌글리콜카보네이트, 멘틸에틸렌글리콜카보네이트, 멘틸글리세롤카보네이트 또는 이의 혼합물), 디카르복실산 또는 이의 유도체를 갖는 멘톨의 세미-에스테르 (예를 들면 모노-멘틸숙시네이트, 모노-멘틸글루타레이트, 모노-멘틸말로네이트, O-멘틸 숙신산 에스테르-N,N-(디메틸)아미드, O-멘틸 숙신산에스테르 아미드), 멘탄카르복실산 아미드 (이 경우에는 바람직하게는 US 4,150,052에 개시된 멘탄카르복실산-N-에틸아미드 [WS3] 또는 Nα-(멘탄카보닐)글리신에틸에스테르 [WS5], WO 2005/049553 A1에 개시된 멘탄카르복실산-N-(4-시아노페닐)아미드 또는 멘탄카르복실산-N-(4-시아노메틸페닐)아미드, 메탄카르복실산-N-(알콕시알킬)아미드), 멘톤 및 멘톤 유도체 (예를 들면 L-멘톤 글리세롤 케탈), 2,3-다이메틸-2-(2-프로필)-부티르산 유도체 (예를 들면 2,3-다이메틸-2-(2-프로필)-부티르산-N-메틸아미드 [WS23]), 이소풀레골(isopulegol) 또는 이의 에스테르 (I-(-)-이소풀레골, I-(-)-이소풀레골아세테이트), 멘탄 유도체 (예를 들면 p-멘탄-3,8-다이올), 큐베볼(cubebol) 또는 큐베볼을 함유하는 합성 또는 천연의 혼합물, 사이클로알킬다이온 유도체의 피롤리돈 유도체 (예를 들면 3-메틸-2(1-피롤리디닐)-2-사이클로펜텐-1-온) 또는 테트라하이드로피리미딘-2-온 (예를 들면 WO 2004/026840에 개시된 이실린(iciline) 또는 관련 화합물), 더 나아가 카르복스아미드 (예를 들면 N-(2-(피리딘-2-일)에틸)-3-p-멘탄카르복사미드 또는 관련 화합물), (1R,2S,5R)-N-(4-메톡시페닐)-5-메틸-2-(1-이소프로필)사이클로헥산-카르복사미드 [WS12], 옥사메이트 (바람직하게는 EP 2033688 A2에 개시된 것들).
항미생물제
(ANTI-MICROBIAL AGENTS)
적절한 항미생물제는 원칙적으로 그람 양성균에 대하여 효과가 있는 모든 물질이고, 예를 들어 4-하이드록시벤조산 및 이의 염 및 에스테르, 4-메틸벤질 알코올, 트로플론(troplone), 히노키티올(hinokitiol), N-(4-클로로페닐)-N'-(3,4-디클로로페닐)우레아, 2,4,4'-트라이클로로-2'-하이드록시-디페닐 에테르 (트리클로산), 4-클로로-3,5-다이메틸-페놀, 2,2'-메틸렌비스(6-브로모-4-클로로페놀), 3-메틸-4-(1-메틸에틸)페놀, 2-벤질-4-클로로-페놀, 3-(4-클로로페녹시)-1,2-프로판다이올, 3-아이오도-2-프로피닐 부틸카바메이트, 클로르헥시딘, 3,4,4'-트라이클로로카르바닐리드 (TTC), 항균 향수, 티몰, 타임 오일(thymere oil), 유제놀, 정향 오일(clove oil), 멘톨, 민트 오일, 파르네솔(farnesol), 페녹시에탄올, 글리세롤 모노카프레이트, 글리세롤 모노카프릴레이트, 글리세롤 모노라우레이트 (GML), 다이글리세롤 모노카프레이트 (DMC), 살리실산 N-알킬아미드, 예컨대 n-옥틸살리실아미드 또는 n-데실살리실아미드이다. 추가적으로, 항미생물제는 일반적으로, 그중에서도 암냄새, 발냄새, 여드름 또는 비듬 형성에 대하여 사용되는, 키토산(chitosan), 토타롤(totarol), 아릴알킬 알코올, 예를 들어, 4-메틸-4-페닐-2-펜타놀 및 이의 유도체(DE 101 43 434, 특히 4-메틸-4-페닐-2-펜타놀), 뮤게 알코올(muguet alcohol, 2,2-dimethyl-3-phenylpropanol), 다른 아릴알킬 알코올(예를 들어, DE 44 47 361, DE 103 30 697, US 4,110,430 또는 EP 1 157 687에 개시되어 있는 것), 2-부틸옥타노산, 2-헥실데카노산, p-아니스산, 항미생물 활성이 있는 향수 오일 또는 단일 아로마 화학물질(aroma chemical), 폴리글리세롤 에스테르, 예를 들어 폴리글리세릴 3-카프릴레이트, 또는 상기 언급된 물질들의 조합이다.
효소 억제제(ENZYME INHIBITORS)
적절한 효소 억제제는 예를 들어 에스테라제 억제제이다. 이들은 바람직하게 트라이알킬 시트레이트로, 예컨대 트라이메틸 시트레이트, 트라이프로필 시트레이트, 트라이이소프로필 시트레이트, 트라이부틸 시트레이트 및, 특히 트라이에틸 시트레이트 (Hydagen CAT)이다. 상기 물질은 효소 활성을 억제함으로 악취의 형성을 감소시킨다. 적절한 에스테라제 억제제인 다른 물질은 스테롤 설페이트 또는 포스페이트로, 예컨대 라노스테롤(lanosterol), 콜레스테롤(cholesterol), 캠페스테롤(campesterol), 스티그마스테롤(stigmasterol) 및 시토스테롤(sitosterol) 설페이트 또는 포스페이트, 다이카르복실산 및 이의 에스테르, 예컨대 글루타르산(glutaric acid), 모노에틸 글루타레이트, 다이에틸 글루타레이트, 아디프산(adipic acid), 모노에틸 아디페이트, 다이에틸 아디페이트, 말론산(malonic acid) 및 다이에틸 말로네이트, 하이드록시카르복실산 및 이의 에스테르, 예컨대 시트르산(citiric acid), 말산(malic acid), 타르타르산(tartaric acid) 또는 다이에틸 타르트레이트 및 아연 글리시네이트이다.
악취 흡수제(
ODOUR
ABSORBERS) 및 발한억제 활성제(ANTIPERSPIRANT ACTIVE AGENTS)
적절한 악취 흡수제는 악취-형성 화합물을 흡수하고 대량으로 함유할 수 있는 물질이다. 이들은 각각의 성분의 부분압을 낮춤으로써, 확산비율도 감소시킨다. 향수가 이러한 과정에서 손상되지 않고 유지되는 것이 중요하다. 악취 흡수제는 박테리아에 대하여 효과적이지 않다. 이들은 예를 들어, 주성분으로, 리시놀레산(ricinoleic acid)의 아연 염 착물을 포함하거나 또는 "고정제(fixative)"로 당업자에게 알려져 있는 특정 악취-중화 향수, 예컨대 랍다넘(labdanum) 또는 때죽나무(styrax)의 추출물 또는 특정 아비에트산(abietic acid) 유도체를 대량으로 포함한다. 악취 차폐제(odour masking agent)는, 악취 차폐제로서의 기능뿐만 아니라, 탈취제(deodorant)에 각각의 향(fragrance note)을 부여하는 향수(fragrance) 또는 향수 오일(perfume oil)이다. 언급될만한 향수 오일은, 예를 들어, 천연 및 합성 향기의 혼합물이다. 천연 향수는 꽃, 줄기와 잎, 열매, 열매 껍질, 뿌리, 나무, 허브와 풀, 니들과 가지, 및 레진과 발삼으로부터의 추출물이다. 또한 적합한 것은 동물의 생산물로, 예를 들어, 사향액(civet)과 해리향(castoreum)이 있다. 일반적인 합성 향수 화합물은 에스테르, 에테르, 알데하이드, 케톤, 알코올 및 탄화수소 유형의 생산물이다. 상기 에스테르 유형의 향수 화합물은, 예를 들어, 벤질 아세테이트, p-터트-부틸사이클로헥실 아세테이트, 리날릴 아세테이트, 페닐에틸 아세테이트, 리날릴 벤조에이트, 벤질 포르메이트, 알릴 사이클로헥실프로피오네이트, 스티랄릴프로피오네이트 및 벤질 살리실레이트가 있다. 상기 에테르는 예를 들어 벤질 에틸 에테르를 포함하고, 상기 알데하이드는 예를 들어 8 내지 18개의 탄소원자를 가지는 직쇄 알칸알, 시트랄(citral), 시트로넬랄(citronellal), 시트로넬릴오시아세트알데하이드(citronellyloxyacetaldehyde), 사이클라멘 알데하이드(cyclamen aldehyde), 하이드록시시트로넬랄(hydroxycitronellal), 릴리알(lilial) 및 부르지오날(bourgeonal)을 포함하며, 상기 케톤은 예를 들어 이오논(ionone) 및 메틸 세드릴 케톤(methyl cedryl ketone)을 포함하며, 상기 알코올은 아네톨(anethole), 시트로넬롤(citronellol), 유제놀(eugenol), 이소유제놀(isoeugenol), 제라니올(geraniol), 리날로올(linaool), 페닐에틸 알코올 및 테르피네올(terpineol)을 포함하며, 상기 탄화수소는 주로 테르펜과 발삼을 포함한다. 그러나, 선호되는 것은 다른 향수들을 섞어서 사용하여 만족스러운 향을 생성하는 것이다. 대부분 아로마 성분으로 사용되는 상대적으로 낮은 휘발성의 에센셜 오일도 향수 오일로 적합하며, 예를 들어, 세이지 오일, 카모마일 오일, 정향(clove)의 오일, 멜리사(melissa) 오일, 민트 오일, 시나몬 잎 오일, 린든(linden) 꽃 오일, 주니퍼베리(juniperberry) 오일, 베티버(vetiver) 오일, 유향(olibanum) 오일, 갈바넘(galbanum) 오일, 랍다넘(labdanum) 오일과 라반딘(lavandin) 오일이 있다. 선호되는 것은 베르가못(bergamot) 오일, 다이하이드로미르세놀(dihydromyrcenol), 릴리알, 라이랄(lyral), 시트로레놀, 페닐에틸 알코올, α-헥실신남알데하이드, 제라니올, 벤질아세톤, 시클라멘 알데히드, 리날로올, 보이삼브렌 포르테(boisambrene forte), 암브록산(ambroxan), 인돌, 헤디온(hedione), 산데라이스(sandelice), 레몬 오일, 만다린 오일, 오렌지 오일, 알릴 아밀 글리코레이트, 사이클로베르탈(cyclovertal), 라반딘 오일, 클라리 세이지 오일, β-다마스콘(β-damascone), 제라늄 오일 버번, 사이클로헥실 살리실레이트, 베르토픽스 코에우르(Vertofix coeur), 이소-E-슈퍼, 픽솔라이드 NP(Fixolide NP), 에버닐(evernyl), 이랄데인 감마(iraldein gamma), 페닐아세트산, 제라닐 아세테이트, 벤질 아세테이트, 장미 산화물, 로밀랫(romilat), 이로틸(irotyl) 및 플로라맷(floramat) 단독 또는 혼합물을 사용하는 것이다.
적절한 수렴성 발한억제 활성 성분은 주로 알루미늄, 지르코늄 또는 아연의 염이다. 이러한 적절한 발한 활성 성분으로는 예를 들어, 알루미늄 클로라이드, 알루미늄 클로로하이드레이트, 알루미늄 다이클로로하이드레이트, 알루미늄 세스퀴클로로하이드레이트 및 예를 들어 1,2-프로필렌 글리콜과의 이들의 복합체 화합물, 알루미늄 하이드록시알란토이네이트(hydorxyallantoinate), 알루미늄 클로라이드 타르트레이트, 알루미늄 지르코늄 트라이클로로하이드레이트, 알루미늄 지르코늄 테트라클로로하이드레이트, 알루미늄 지르코늄 펜타클로로하이드로레이트 및 예를 들어 글리신과 같은 아미노산과의 이의 복합체 화합물이다.
필름
형성제
(FILM FORMERS) 및 항-
비듬제
(ANTI-DANDRUFF AGENTS)
일반적인 필름 형성제는, 예를 들어 키토산, 미정질(microcrystalline) 키토산, 4차 키토산, 폴리비닐 피롤리돈, 비닐 피롤리돈/비닐 아세테이트 공중합체, 아크릴산 계열의 고분자, 4차 셀룰로오스 유도체, 콜라겐, 히알루론산 및 이들의 염 및 이들과 유사한 화합물이다.
적절한 항비듬제로 피록톤 올라민(Piroton Olamin)(1-하이드록시-4-메틸-6-(2,4,4-트라이메틸펜틸)-2-(1H)-피리디논 모노에탄올아민 염), Baypival®(클림바졸; Climbazole), Ketoconazol®(4-아세틸-1-{4-[2-(2,4-다이클로로페닐) r-2-(1H-이미다졸-1-일메틸)-1,3-다이옥실란-c-4-일메톡시페닐}-피페라진, 케토코나졸(ketoconazole), 엘루비올(elubiol), 이황화 셀레늄, 콜로이드성 황, 황 폴리에틸렌 글리콜 솔비탄 모노올레이트, 황 리시놀 폴리에톡시레이트, 황 타르 증류액, 살리실산 (또는 헥사클로로펜과의 조합), 운데실렌산(undecylenic acid), 모노에탄올아미드 설포숙시네이트 Na 염, Lamepon® UD (단백질/운데실렌산 응축액), 아연 피리티온, 알루미늄 피리티온 및 마그네슘 피리티온/다이피리티온 마그네슘 설페이트가 있다.
담체
(CARRIERS) 및 하이드로트로프(
HYDROTROPES
)
바람직한 화장품 담체 물질은 25 ℃ 및 1013 mbar에서 고체 또는 액체(고점도 물질 포함)이며, 예를 들어 글리세롤, 1,2-프로필렌글리콜, 1,2-부틸렌글리콜, 1,3-프로필렌글리콜, 1,3-부틸렌글리콜, 에탄올, 물 및 물과 상기 액체 담체 물질의 둘 이상의 혼합물이다. 선택적으로, 본 발명에 따른 이러한 제제는 방부제(preservative) 또는 가용화제(solubilizer)를 사용하여 제조될 수 있다. 본 발명에 따른 제제의 성분이 될 수 있는 다른 바람직한 액체 담체 물질은 식물성 오일, 중성 오일 및 미네랄 오일과 같은 오일로 구성된 군으로부터 선택된다.
본 발명에 따른 제제의 성분이 될 수 있는 바람직한 고체 담체 물질은 하이드로클로이드이고, 예컨대 전분, 분해된 전분, 화학적 또는 물리적으로 개질된 전분, 덱스트린, (파우더) 말토덱스트린 (바람직하게는 5 내지 25, 바람직하게는 10 내지 20의 당량치의 덱스트로스 포함), 락토스, 이산화규소, 글루코오스, 개질된 셀룰로오스, 검 아라빅(gum arabic), 가티검(ghatti gum), 트라간트(tranganth), 카라야(karaya), 카라기난(carrageenan), 풀루란(pullulan), 커들란(curdlan), 잔탄검(xanthan gum), 젤란검(gellan gum), 구아가루(guar flour), 캐롭콩가루(carob bean flour), 알지네이트(alginate), 아가(agar), 펙틴(pectin) 및 이눌린(inulin) 및 이들 고체의 둘 이상의 혼합물이고, 특히 말토덱스트린 (바람직하게는 15 내지 20의 당량치의 덱스트로스 포함), 락토스, 이산화규소 및/또는 글루코오스이다.
또한, 하이드로트로프, 예를 들어 에탄올, 이소프로필 알코올 또는 폴리올은, 유동 작용을 향상시키기 위해 사용할 수 있다. 적합한 폴리올은 바람직하게 2 내지 15개의 탄소 원자와 적어도 두 개의 하이드록시기를 포함한다. 상기 폴리올은 다른 작용기, 특히 아미노기를 포함할 수 있으며, 또는 질소로 개질될 수 있다. 일반적인 예로는 다음이 있다.
자가-축합도(degree of self-condensation)가 1.5 내지 10인 테크니컬 올리고글리세롤 혼합물, 예컨대 40 내지 50 중량%의 양으로 다이글리세롤을 포함하는 테크니컬 다이글리세롤 혼합물;
방부제(PRESERVATIVES)
적절한 방부제는 예를 들어, 페녹시에탄올, 포름알데하이드 용액, 파라벤(parabene), 펜탄다이올 또는 소르브산(sorbic acid) 및 Kosmetikverordnung {"화장품 지침(cosmetic directive)"}의 파트 A와 B의 부록 6에 나와있는 화합물의 다른 클래스이다.
향수 오일(PERFUME OILS) 및 향수(FRAGRANCES)
적절한 향수 오일은 천연 및 합성 향수의 혼합물이다. 천연 향수는 꽃 {백합, 라벤더, 장미, 자스민, 네롤리(neroli), 일랑-일랑(ylang-ylang)}, 줄기와 잎{제라늄(geranium), 패출리(patchouli), 페티그레인(petitgrain)}, 열매{아니스(anise), 코리앤더(coriander), 캐러웨이(caraway), 주니퍼(juniper)}, 열매 껍질 {베르가못(bergamot), 레몬, 오렌지), 뿌리 {육두구(nutmeg), 안젤리카(angelica), 셀러리, 카다몸(cardamom), 코스투스(costus), 창포(iris), 칼무스(calmus)}, 나무 {소나무목(pine wood), 백단향(sandal wood), 유창목(guaiac wood), 백향목(cedarwood), 자단(rosewood)}, 허브와 풀 {타라곤(tarragon), 레몬 글라스, 세이지, 백리향(thyme)}, 니들 및 가지 {가문비 나무(spruce), 전나무(fir), 소나무(pine), 잣나무(dwarf pine)}, 레진 및 발삼 {갈바넘(galbanum), 엘레미(elemi), 벤조인, 몰약(myrrh), 유향(olibanum), 오포포낙스(opoponax)}의 추출물을 포함한다. 동물 원료는 예를 들어, 사향액과 비버 향이 또한 사용될 수 있다. 일반적인 합성 향수 화합물로는 에스테르, 에테르, 알데하이드, 케톤, 알코올 및 탄화수소 유형의 제품이다. 상기 에스테르 유형의 향수 화합물의 예로, 벤질 아세테이트, 페녹시에틸 이소부틸레이트, p-터트-부틸사이클로헥실 아세테이트, 리날릴 아세테이트, 다이메틸 벤질 카비닐 아세테이트, 페닐 에틸 아세테이트, 리날릴 벤조에이트, 벤질 포르메이트, 에틸메틸 페닐 글리시네이트, 알릴 사이클로헥실 프로피오네이트, 스티랄릴 프로피오네이트 및 벤질 살리실레이트가 있다. 에테르는 예를 들어, 벤질 에틸 에테르를 포함하고, 한편 알데하이드는 예를 들어, 8 내지 18개의 탄소원자를 가지는 직쇄 알칸알, 시트랄, 시트로넬랄, 시트로넬릴옥시아세트알데하이드, 사이클라멘 알데하이드, 하이드록시시트로넬랄, 릴리알 및 부르지오날을 포함한다. 적절한 케톤의 예로 이오논, -이소메틸이오논 및 메틸 세드릴 케톤을 포함한다. 적절한 알코올은 아네톨, 시트로넬롤, 유제놀, 이소유제놀, 제라니올, 리날로올, 페닐에틸 알코올 및 테르피네올을 포함한다. 상기 탄화수소로 테르펜과 발삼을 주로 포함한다. 그러나, 함께 기분 좋은 향수를 생성할 수 있는 다른 향수 화합물의 혼합물을 사용하는 것이 선호된다. 다른 적절한 향수 오일은 대부분 아로마 성분으로 사용되는 상대적으로 낮은 휘발성의 에센셜 오일이다. 예를 들어, 세이지 오일, 카모마일 오일, 정향 오일, 멜리사 오일, 민트 오일, 시나몬 잎 오일, 라임 블라섬 오일, 주니퍼 베리 오일, 베티버 오일, 유향 오일, 갈바넘 오일, 랍다넘 오일 및 라반딘 오일이 있다. 다음은 바람직하게 개별적으로 또는 혼합물의 형태로 사용된다: 베르가못 오일, 다이하이드로미르세놀(dihydromyrcenol), 릴리알, 라이랄, 시트로넬롤, 페닐에틸 알코올, 헥실신남알데하이드, 제라니올, 벤질 아세톤, 사이클라멘 알데하이드, 리날로올, 보이삼브렌 포르테, 암브록산, 인돌, 헤디온, 산데라이스, 시트러스 오일, 만다린 오일, 오렌지 오일, 알릴아밀 글리코레이트, 사이클로베르탈, 라반딘 오일, 클라리 오일, 다마스콘, 제라늄 오일 버번, 사이클로헥실 살리실레이트, 베르토픽스 코에우르, 이소-E-슈퍼, 픽솔라이드 NP, 에버닐, 이랄데인 감마, 페닐아세트산, 제라닐 아세테이트, 벤질 아세테이트, 장미 산화물, 로밀랫, 이로틸 및 플로라맷.
염료(DYES)
적절한 염료는 화장품 목적으로 적합하고 승인된 물질의 어느 것으로, 예를 들어, 출판물 Farbstoff-kommission der Deutschen Forschungsgemeinschaft, Verlag Chemie , Weinheim , 1984, 81 내지 106면의 "Kosmetische Fabemittel"에 기재된 것이다. 그 예로 코치닐 레드 A {cochineal red A (C.I. 16255)}, 페턴트 블루 V {patent blue V (C.I. 42051)}, 인디고틴 {indigotin (C.I. 73015)}, 클로로필린 {chlorophyllin (C.I. 75810)}, 퀴놀린 엘로우 {quinoline yellow (C.I. 47005)}, 티타늄 다이옥사이드 {titanium dioxide (C.I. 77891)}, 인단트렌 블루 RS {indanthrene blue RS (C.I. 69800)} 및 메더 레이크 {madder lake (C.I. 58000)}를 포함한다. 루미놀은 또한 발광성 염료로 존재할 수 있다. 바람직한 착색 색소는 예를 들어 티타늄 다이옥사이드, 미카(mica), 산화철 {예를 들어 Fe2O3, Fe3O4, FeO(OH)} 및/또는 산화 주석이다. 바람직한 염료는 예를 들어 카민(carmine), 베를린 블루, 산화 크로늄 그린, 울트라마린 블루 및/또는 망간 바이올렛이다.
제제(PREPARATIONS)
본 발명에 따른 바람직한 조성물은 피부 및/또는 모발의 치료, 보호, 케어 및 세정을 위한 제품 또는 메이크업 제품, 바람직하게는 리브-온(leave-on) 제품(씻어내는 제제와 비교하여 하나 이상의 화학식 (I)의 화합물이 장시간 동안 피부 및/또는 모발에 남아있게 됨으로써, 보습 및/또는 항-노화 및/또는 상처 치료를 증진하는 이들의 역할을 더 현저하게 하는 것을 의미함) 군으로부터 선택된다.
본 발명에 따른 제형은 바람직하게는, 에멀젼, 예컨대 W/O (water-in-oil), O/W (oil-in-water), W/O/W (water-in-oil-in-water), O/W/O (oil-in-water-in-oil) 에멀젼, PIT 에멀젼, 피커링 에멀젼, 오일 함량이 낮은 에멀젼, 마이크로- 또는 나노 에멀젼, 용액, 예컨대 오일 (지방유 또는 지방산 에스테르, 특히 C6-C32 지방산 C2-C30 에스테르) 또는 실리콘 오일, 디스퍼젼, 서스펜션, 크림, 로션 또는 유액, 제조방법 및 성분에 따라, 겔 (하이드로겔, 하이드로디스퍼젼 겔, 올레오겔 포함), 스프레이 (예를 들어, 펌프 스프레이 또는 추진제를 갖는 스프레이) 또는 거품 또는 화장품 제거용 함침 용액, 세제(detergent), 예컨대 비누, 합성세제, 세정액, 샤워 및 목욕 제제, 목욕 용품 (캡슐, 오일, 정제, 염, 목욕염, 비누, 등), 발포성 제제, 스킨 케어 제품, 예컨대 에멀젼 (앞에서 언급함), 연고, 페이스트, 겔 (앞에서 언급함), 오일, 발삼, 세럼, 파우더 (예를 들어, 얼굴 파우더, 바디 파우더), 마스크, 펜슬, 스틱, 롤-온(roll-on), 펌프, 에어로졸 (포밍, 비-포밍 또는 포스트(post)-포밍), 데오도란트 및/또는 발한억제제, 구강청결제(mouth wash) 및 구강세정제(mouth rinse), 풋케어 용품 (각질용해제, 데오도란트 포함), 방충제, 선스크린, 애프터선 제제, 면도 용품, 애프터셰이브 밤, 프리(pre)- 및 애프터셰이브 로션, 탈모제, 헤어 케어 제품, 예컨대 샴푸 (2-인-1 샴푸, 항-비듬 샴푸, 베이비 샴푸, 건성 두피용 샴푸, 농축 샴푸 포함), 컨디셔너, 헤어 토닉, 헤어 워터, 헤어 린스, 스타일링 크림, 포마드, 펌 및 셋팅 로션, 헤어 스프레이, 스타일링 보조제 (예를 들어, 젤 또는 왁스), 헤어 스무딩제 (엉킴 방지제, 릴랙서), 헤어 염료, 예컨대 일시적인 직접-염색용 헤어 염료, 반-영구 헤어 염료, 영구 헤어 염료, 헤어 컨디셔너, 헤어 무스, 눈 케어 용품, 메이크업, 메이크업 리무버 또는 베이비 용품의 형태이다.
본 발명에 따른 제형은 특히 바람직하게는, 에멀젼 형태, 특히 W/O, O/W, W/O/W, O/W/O 에멀젼, PIT 에멀젼, 피커링 에멀젼, 오일 함량이 낮은 에멀젼, 마이크로- 또는 나노 에멀젼, 겔 (하이드로겔, 하이드로디스퍼젼겔, 올레오겔 포함), 용액, 예컨대 오일 (지방유 또는 지방산 에스테르, 특히 C6-C32 지방산 C2-C30 에스테르) 또는 실리콘 오일, 또는 스프레이 (예를 들어, 펌프 스프레이 또는 추진제를 갖는 스프레이)이다.
보조제 및 첨가제는 제형의 총 중량에 대하여 5 내지 99 중량 % (% b.w.), 바람직하게는 10 내지 80 중량 % (% b.w.)의 양으로 포함될 수 있다. 각각의 경우에 사용되는 화장료 또는 피부학적 보조제 및 첨가제 및 향수의 양은 특정 제품의 성질에 따라 간단한 시도 및 오류를 통하여 통상의 기술자에 의해 쉽게 결정될 수 있다.
상기 제제는 또한 제제의 총 중량에 대하여 최대 99 중량 % (% b.w.), 바람직하게는 5 내지 80 중량 % (% b.w.)까지 물을 함유할 수 있다.
약제학적 조성물 (PHARMACEUTICAL COMPOSITIONS)
본 발명에 따른 약제학적 조성물은 화장료 적용에서 이미 설명된 바와 유사한 첨가제로 예컨대, 예를 들어 오일바디 또는 유화제 및 특히 신규한 생강 추출물의 이로운 특성을 보충하는 공동-활성제를 포함할 수 있다. 하기 인용되는 다양한 활성제는 화장료 제형, 소위 "코스메슈티컬(cosmeceuticals)"에 또한 통합될 수 있는 것이 또한 언급되어야 한다. 그러므로, 화장료 및 약제학적 조성물 간의 경계는 이어지고 이는 다른 적용에 인용된 구성요소가 문자로 반복없이 필요한 부분만 약간 수정하여 다른 쪽에 추천되는 것으로 이해되어야 한다.
항-자극제(Anti-irritation agents)
공동-활성의 중요한 그룹은 항-자극제로 예컨대, 예를 들어 코르티코스테로이드 유형의 스테로이드계 항-염증성 물질로, 예컨대 예를 들어, 하이드로코르티손, 하이드로코르티손 유도체로, 예컨대 하이드로코르티손 17-부틸레이트, 덱사메타손, 덱사메타손 포스페이트, 메틸프레드니솔론 또는 코르티손; 비-스테로이드계 항 염증성과 같은 옥시캄으로 예컨대 피로옥시캄(piroxicam) 또는 텐옥시캄(tenoxicam); 살리실레이트로 예컨대 아스피린, 디스알시드(Disalcid), 솔프린 또는 펜도살; 아세트산 유도체로 예컨대 디클로페낙, 펜클로페낙(fenclofenac), 인도메타신, 술인닥, 톨메틴 또는 클린다낙(clindanac); 페나메이트로 예컨대 메페나믹, 메클로페나믹, 플루페나믹 또는 니플루믹; 프로피온산 유도체로 예컨대 이부프로펜, 나프로센 또는 베노사프로펜(benoxaprofen) 또는 피라졸로 예컨대 페닐부타존, 옥시페닐부타존, 페브라존 또는 아자프로파존을 포함한다. 또한, 천연 항-염증성 물질 또는 발적-및/또는 가려움 경감 물질이 사용될 수 있다. 식물 추출물, 특히 식물 추출물로부터 분리된 높은 활성 식물 추출 분획물 및 고순도 활성 물질은 알로에 베라, 콤미포라(Commiphora) 종, 루비아(Rubia) 종, 루버스(Rubus) 종, 버드나무, 로즈-베이, 분홍바늘 꽃(willowherb), 오트, 금잔화(calendula), 아르니카, 세인트 존스 워트(St.John's wort), 허니서클(honeysuckle), 생강, 카모마일, 로즈마리, 세이지, 멜리사, 시계초(passiflora), 회화나무(Sophora japonica), 풍년화(witch hazel), 갈근(Pueraria), 패랭이(Dianthus) 또는 에키네이셔(Echinacea)로부터 추출물, 분획물 및 활성 물질과 같은 것이 사용될 수 있을 뿐만 아니라 정제 물질로 예컨대, 그 중에서도, 비사보롤, 아피제닌, 아피제닌-7-글루코시드, 로스마리 산, 보스웰 산, 피토스테롤, 글리시리직 산, 글라브리딘, 리코찰콘 A, [6]-파라돌, 및 안트라닐 산 아마이드, 예컨대 특히 아베난스라미드(avenanthramides) 또는 다이안스라미드가 바람직하게 선호된다. 본 발명에 따른 제형 또는 제품 내 항-자극제의 총 함량은 각각의 제형 또는 제품의 총 중량을 기초로 바람직하게 0.0001 내지 20 중량 %, 바람직하게 0.0001 내지 10 중량%, 특히 0.001 내지 5 중량%의 범위이다.
특히 유용한 공동-활성제는 항-진균 및 통증 완화제로 구성된 그룹, 보다 바람직하게 에리스로마이신(erythromycin), 디메틴덴(dimetindene), 베타메타손(betamethasone), 이부프로펜(ibuprofen), 케토프로펜(ketoprofene), 디클로페낙(diclofenac), 메트로니다졸(metronidazole), 아시클로비르(acyclovir), 이미쿼모드(imiquimod), 테르비나핀(terbinafine), 도코사놀(docosanol), 사이클로피록솔사민(cyclopyroxolamine), 및 이들의 혼합물로 구성된 그룹으로부터 선택된다.
에리스로마이신(Erythromycin)은 페니실린의 항미생물 스펙트럼과 유사하거나 약간 넓은 항미생물 스펙트럼을 가지는 매크로라이드(macrolide) 항생제이고, 페니실린에 알러지를 가지는 사람들에게 종종 사용된다.
최근 연구는 이것이 가벼운 항-억제제로 사용될 수 있음을 또한 보여주고 있다. 호흡 기관 감염에 대하여, 이것은 마이코플라즈마(mycoplasma) 및 레지오넬라증(legionellosis)을 포함한 이례적 미생물의 범위를 더 가진다. 이것은 Eli Lilly 및 Company에 의해 처음 시판되었고, 이는 EES로 흔히 오늘날 알려져 있다(에리스로마이신 에틸숙시네이트, 일반적으로 투여되는 에스테르 프로드러그). 구조에서, 이 매크로사이클릭 화합물은 10개의 비대칭 중심과 두개의 당(L-클라디노스 및 D-데소사민)을 가지는 14 개의 락톤 링을 포함하기 때문에, 합성 방법을 통해 생산하기 매우 어렵다. 에리스로마이신은 방사균인 Saccharopolyspora erythraea의 균주로부터 생산된다(US 2,653,899 Eli Lily 참조).
또한 페니스틸 (RS-다이메틸(2-(3-[피리딘-2-일)에틸]-1H-인덴-2-일)에틸)아민) (RS-dimethyl(2-(3-[pyridin-2-yl)ethyl]-1H-inden-2-yl)ethyl)amine)으로 알려진 디메틴덴(Dimetindene)은 항가려움제로 경구 또는 국소로 사용되는 항히스타민/항콜린제이다.
베타메타손 ( Betamethasone ) (8S,9R,10S.11S,13S,14S,16S,17R)-9-플루오로-11,17-(2-하이드록시아세틸)-10,13,16-트라이메틸-6,7,8,9,10,11,12,13,14,15,16,17-도데카하이드로-3H-사이클로펜타(알파)-페난트렌-3-온 {(8S,9R,10S.11S,13S,14S,16S,17R)-9-fluoro-11,17-(2-hydroxyacetyl)-10, 13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta(alpha)-phenanthren-3-one)}은 항-염증 및 염증 억제 특성을 가진 잠재적 글루코코르티코이드 스테로이드이다.
이러한 효과를 가진 다른 약물과 다르게, 베타메타손은 수분 보유(water retention)가 발생하지 않는다. 이는 가려움을 치료하기 위해 국소 크림, 연고, 거품, 로션 또는 젤로 적용될 수 있다. 베타메타손 소듐 포스페이트는 덩굴 옻나무(poison ivy) 및 유사 식물에 대한 알러지 반응을 포함하여 다양한 질병으로부터 가려움에 대한 근육 내 주사로 때때로 처방된다(US 3,053,865-Merck 참조).
명명법 이소-부틸-프로판오익-페놀산(iso-butyl-propanoic-phenolic acid)으로부터 이부프로펜(Ibuprofen) (RS)-2-(4-(2-메틸프로필)페닐)프로피온 산) {(RS)-2-(4-(2-methylpropyl)phenyl)propanoic acid)}은 진통제(통증 경감), 특히, 염증 요소가 있는 곳에서 관절염, 열 및 월경통 증상의 경감을 위해 사용되는 비-스테로이드계 항-염증 약물(NSAID)이다.
이부프로펜은 이것이 아스피린 또는 다른 더 잘 알려진 항혈소판 약물과 대비되었을 때 상대적으로 약하고 다소 단수명임에도 불구하고, 항혈소판 효과를 가지는 것으로 알려져 있다. 일반적으로 이부프로펜은 이것이 주로 사이클로옥시제나제 2 효소에 의해 생산되는 혈관 확장 프로스타사이클린을 억제하기 때문에 관상 동맥 및 일부 다른 혈관을 수축하는 것을 보여 또한 혈관수축제로써 작용한다. 이부프로펜은 1960년대 동안 Boots 그룹의 연구 목적에 의해 프로피온 산으로부터 유래하였고 1961년에 특허되었다. Brufen으로 최초 시판된 이부프로펜은 Motrin, Nurofen, Advil, 및 Nuprin을 포함하여 다양한 유명 상표 하에 이용할 수 있다 (US 3,385,886 -Boots 참조).
케토프로펜 ( Ketoprofen ) (RS)2-(3-벤조일페닐)-프로피온 산은 진통 및 해열 효과를 가지는 비-스테로이드계 항-염증 약물(NSAID)의 또다른 프로피온 산 종류 중 하나이다.
이는 프로스타글란딘의 인체 생성을 억제함으로써 작용한다(US 3,641,127 - Rhone-Poulenc 참조).
디클로페낙( Diclofenac )은 또한 특정 상태에서 고통을 경감시키는 진통제로써 염증을 경감하기 위한 비-스테로이드계 항-염증 약물(NSAID)이다.
이름은 이의 화합물 명칭 : 2-(2,6-다이클로로아닐리노)페닐아세트산으로부터 유래된다. 영국, 인도, 브라질, 미국에서, 이는 소듐 또는 포타슘 염으로도 공급될 수 있으며, 중국에서는 대부분 소듐 염으로써, 일부 다른 국가에서는 오직 포타슘 염으로 공급될 수 있다. 디클로페낙은 다수의 제형으로 제네릭 약물로써 이용가능하다. 처방전 없이(Over-the-counter) 이용은 약간의 아픔 및 고통 및 일반적인 감염과 연관된 열에 대해 일부 국가에서 승인된다 (US 3,558,690-Ciba-Geigy 참조).
메트로니다졸( Metronidazole ) (2-(2-메틸-5-니트로-1H-이미다졸-1-일)에탄올)은 혐기성 박테리아와 원충에 대해 특히 사용되는 니트로이미다졸 항생제 약물이다.
메트로니다졸은 항생제, 항아메바제 및 항원충제이다. 이는 경도 내지 중등도의 클로스트리듐 디피실리균(Clostridium difficile) 감염의 첫 단계에 대해 선택되는 약물이다. 이는 Pfizer에 의해 미국에, 상표 Flagyl로 Sanofi에 의해 전세계로, Star laboratories에 의해 Nidagyl로 또한 파키스탄 및 방글라데시에, Thai Nakhorn Patana에 의해 Mepagyl로 태국에 시판된다. 이는 또한 Milpharm Limited 및 Almus Pharmaceuticals에 의해 영국에 시판된다. 메트로니다졸은 1960년에 개발되었다. 메트로니다졸은 또한 주사비(rosaceae) 및 진균 종양과 같은 피부 상태의 치료에 겔 제제로써 사용된다 (US 2,944,061-Rhone Poulenc 참조).
(VIII) ACV로 축약되는 화합물명 아시클로구아노신 (2-아미노-1,9-다이하이드로-9-((2-하이드록시에톡시)메틸)-6H-푸린-6-온){(2-Amino-1,9-dihydro-9-((2-hydroxyethoxy)methyl)-6H-Purin-6-one)}, 아시클로비르 ( Acyclovir ) 또는 아시클로비르 (USAN, former BAN)는 Cyclovir, Herpex, Acivir, Acivirax, Zovirax, 및Xovir와 같은 상표하에 시판되는 구아노신 유사체 항바이러스 약물이다. 고체 활성제는 20 ℃, 물 (20°dH)에서 5 g/L 보다 이하의 용해도를 가진다.
가장 흔하게 사용되는 항 바이러스 약물 중 하나로; 이는 단순성 포진 바이러스 감염의 치료뿐만 아니라 수두(Varivella zoster)(수두, chickenpox) 및 포진(herpes zoster) (포진, Shingles)의 치료에 일차적으로 사용된다; 또한 US 4,199,574 (Wellcome) 참조.
이미쿼모드 ( Imiquimod ) (3-(2-메틸프로필)-3,5,8-트라이아자트라이사이클로[7.4.0.0.2,6]트라이데카-1(9),2(6),4,7,10, 12- 헥센-7-아민, INN) {(3-(2-methylpropyl)-3,5,8-triazatricyclo[7.4.0.0.2,6]trideca-1(9),2(6),4,7,10, 12- hexaen-7-amine, INN)}은 면역 반응 변형제로써 작용하는 처방약물이다.
이는 상표 Aldara 및 Zyclara 하에 Meda AB, Graceway Pharmaceuticals 및 iNova Pharmaceuticals에 의해, 및 Beselna로 Mochida에 의해 시판된다. 이는 R-837로 또한 언급된다 (US 4,689,338 - Riker 참조).
테르비나핀 ( terbinafine ), 보다 바람직하게 테르피나핀 하이드로클로라이드 [(2E)-6,6-다이메틸헵트-2-엔-4-인-1-일](메틸)(나프탈렌-1-일메틸)아민) {[(2E)-6,6-dimethylhept-2-en-4-yn-1-yl](methyl)(naphthalen-1-ylmethyl)amine)} 은 Novartis로부터의 합성 알릴아민 항진균제이다. 이는 천연에서 매우 친유성이고 피부, 손톱 및 지방 조직에 축적되는 경향이 있다.
이는 아르헨티나, 호주, 벨기에, 브라질, 캐나다, 칠레, 이집트, 핀란드, 프랑스, 독일, 그리스, 헝가리, 아이슬란드, 아일랜드, 이스라엘, 멕시코, 파키스탄, 페루, 뉴질랜드, 노르웨이, 루마니아, 러시아, 슬로베니아, 남아프리카 공화국, 스웨덴, 영국, 미국, 베네수엘라에서 Lamisil이라는 명칭으로써 판매되고, 터키에서 Corbinal 및 terbisil이라는 명칭으로써, 및 폴란드에서 "undofen cream" 라는 명칭으로써 판매된다. 제네릭으로써, 이는 호주에서 상표 Zabel로 판매된다. 이는 또한 미국, 영국, 벨기에, 스위스 및 브라질에서 제네릭 약물로써 이용가능하다. 인도에서, 테르비나핀 하이드로클로라이드는 브랜드명 Sebifin (Ranbaxy Labs), Zimig (GSK Pharma) 및 mycoCeaze (Progres Laboratories)로 국소제형으로 이용가능하다. Apricus Biosciences에 의해 개발된 MycoVa는 조갑진균증의 치료를 위해 3상 연구가 완료된 테르비나핀 및 DDAIP의 국소 손톱 용액이다.
또한 베헤닐 알코올로 알려진 도코사놀(Docosanol)은 전통적으로 화장료에서 피부연화제, 유화제 및 증점제로, 보다 최근에는, 약학적으로 승인되는 식품 의약품국(FDA)에서 식품 첨가물(개별 개체 및 또한 폴리코사놀의 구성요소로써)로, 단순성 포진 바이러스에 의해 야기되는 발진(cold sore)의 내성 감소를 위한 항바이러스제로 승인된 Abreva로 사용되는 포화 지방 알코올이다.
또한 Batrafen, Loprox, Mycoster, Penlac 및 Stieprox로 불리우는 사이클로피록솔사민( Cyclopiroxolamine ) (6-사이클로헥실-1-하이드록시-4-메틸피리딘-2(1H)-온){(clohexyl-1-hydroxy-4-methylpyridin-2(1H)-one)} 은 표면 진균증의 국소 피부 치료를 위한 합성 항진균 제제이다.
이는 어루러기(Tinea versicolor)에 대하여 가장 효과적이다 (US 3,883,545- Merck).
항-
셀룰라이트제
(Anti-cellulite agents)
항-셀룰라이트제의 활성을 개선시키거나 촉진하는 제제(agent), 특히 C 신경섬유를 자극 및/또는 감극시키는 제제는, 바람직하게는 캡사이신 및 이의 유도체, 바닐릴-노닐아미드 및 이의 유도체, L-카르니틴, 코엔자임 A, 이소플라보노이드, 콩 추출물, 아나나스(ananas) 추출물 및 공액 리놀레산으로 이루어진 군으로부터 선택된다.
지방개선제(Fat enhancing agents)
본 발명에 따르면 제형 및 제품은 또한 지방 개선제의 활성을 개선시키거나 촉진하는 제제(agent) 뿐만 아니라 하나 이상의 지방개선제 및/또는 지방형성제를 포함할 수도 있다. 지방개선제는 예를 들어 하이드록시메톡시페닐 프로필메틸메톡시벤조퓨란(상품명: Sym3D®)이다.
모발 성장 활성제 또는 억제제(Hair growth activator or inhibitors)
본 발명에 따른 제형 및 제품은 또한 하나 이상의 모발 성장 활성제, 즉, 모발 성장을 자극하기 위한 제제(agent)를 포함할 수 있다. 모발 성장 활성제는 바람직하게 피리미딘 유도체, 예컨대 2,4-다이아미노피리미딘-3-옥사이드 {아미넥실(Aminexil)}, 2,4-다이아미노-6-피페리디노피리미딘-3-옥사이드 {미녹시딜(Minoxidil)} 및 이의 유도체, 6-아미노-1,2-다이하이드로-1-하이드록시-2-이미노-4-피페리디노피리미딘 및 이의 유도체, 잔틴 알칼로이드(xanthine alkaloids), 예컨대 카페인, 테오브로민(theobromine) 및 테오필린(theophylline) 및 이의 유도체, 퀘르세틴 및 유도체, 다이하이드로퀘르세틴 {탁시폴린(taxifolin)} 및 유도체, 포타슘 채널 오프너, 항안드로겐제, 합성 또는 천연 5-환원효소 억제제, 니코틴산 에스테르, 예컨대 토코페릴 니코티네이트, 벤질 니코티네이트 및 C1-C6 알킬 니코티네이트, 단백질, 예컨대 트리펩타이드 Lys-Pro-Val, 다이펜시프렌(diphencypren), 호르몬, 피나스테라이드(finasteride), 두타스테라이드(dutasteride), 프루타마이드(flutamide), 바이칼루타마이드(bicalutamide), 프레그난(pregnane) 유도체, 프로게스테론 및 이의 유도체, 사이프로테론 아세테이트, 스피로노락론 및 다른 이뇨제, 칼신우린(calcineurin) 억제제, 예컨대 FK506 {타크롤리무스(Tacrolimus), Fujimycin} 및 이의 유도체, 사이클로스포린 A 및 이의 유도체, 아연 및 아연 염, 폴리페놀, 프로시아니딘(procyanidin), 프로안토시아니딘(proanthocyanidin), 피토스테롤(phytosterol), 예컨대 베타-시토스테롤(beta-sitosterol), 비오틴(biotin), 유제놀(eugenol), (±)-베타-시트로넬롤((±)-beta-citronellol), 판테놀(panthenol), 예를 들어 근육으로부터의 글리코겐, 미생물, 조류(algae) 추출물, 식물 및 식물 부분의 추출물, 예컨대 민들레 (Leontodon 또는 Taraxacum), 오르토시폰(Orthosiphon), 바이텍스(Vitex), 커피(Coffea), 파우리니아(Paullinia), 테오브로마(Theobroma), 족두리풀(Asiasarum), 호박(Cucurbita) 또는 괴화(Styphnolobium), 톱야자 나무(Serenoa repens, saw palmetto), 고삼(Sophora flavescens), 파이지움 아프리카눔(Pygeum africanum), 기장(Panicum miliaceum), 승마(Cimicifuga racemosa), 글리신맥스(Glycine max), 정향나무(Eugenia caryophyllata), 안개나무(Cotinus coggygria), 하와이 무궁화(Hibiscus rosa-sinensis), 차나무(Camellia sinensis), 마테(Ilex paraguariensis), 아이소크라이시스 갈바나(Isochrysis galbana), 감초(licorice), 포도, 사과, 보리(barley) 또는/및 홉(hop)의 추출물, 또는/및 쌀 또는 밀로부터의 가수분해 추출물로 이루어진 군으로부터 선택된다.
그 대신에, 본 발명에 따른 제형 및 제품은 하나 이상의 모발 성장 억제제(상기 기술됨), 즉, 모발 성장을 감소 또는 억제하기 위한 제제(agent)를 포함할 수 있다. 모발 성장 억제제는 바람직하게 액티빈(activin), 액티빈 유도체 또는 액티빈 아고니스트, 오르니틴 탈카르복실화효소 억제제, 예컨대 알파-다이플루오로메틸오르니틴 또는 펜타사이클릭 트라이페르펜으로 예를 들어 우르솔산(ursolic acid), 베툴린(betulin), 베툴린산(betulinic acid), 올레아놀산(oleanolic acid) 및 이의 유도체, 5 알파-환원효소 억제제, 안드로겐 수용체 길항제, S-아데노실메티오닌 탈카르복실화효소 억제제, 감마-글루타밀 트랜스펩티다아제 억제제, 트랜스글루타미나아제 억제제, 소이빈-유래 세린 프로테아제 억제제, 미생물, 조류, 다른 미세조류 또는 식물 및 식물 부분으로부터의 추출물, 예를 들어 콩과(Leguminosae), 가지과(Solanaceae), 화본(Graminae), 박주가리과(Asclepiadaceae) 또는 박과(Cucurbitaceae), 콘드러스속(Chondrus), 글로이오펠티스속(Gloiopeltis), 비단풀속(Ceramium), 더빌리아속(Durvillea), 글리신 맥스(Glycine max), 오이풀속(Sanguisorba officinalis), 금잔화(Calendula officinalis), 조롱나무속(Hamamelis virginiana), 아니카(Arnica montana), 흰버드나무(Salix alba), 물레나물(Hypericum perforatum) 또는 김네마 실베스터(Gymnema sylvestre)의 추출물로 구성된 군으로부터 선택된다.
용질 (Solutes)
본 발명에 따른 제형 및 제품은 하나 이상의 호환성 용질(compatible solutes)을 또한 포함한다. 바람직한 호환성 용질은 예컨대 WO 01/76572에 기술되어 있으며, 특히, EP 0 553 884, EP 0 671 161 및 WO 94/15923에 기술된 바와 같은 디미오-이노시톨포스페이트 (DIP), 디글리세린포스페이트 (DGP), 디-미오-이노시톨포스페이트(DIP), 사이클릭 2,3 디포스포글리세레이트 (cDPG), 1,1-디-글리세롤포스페이트 (DGP), 베타-만노실글리세레이트 (firoin), 베타-만노실글리세라마이드 (firoin-A) 및 디-만노실-디-이노시톨 포스페이트 (DMIP) 및 엑토인 및 엑토인-유도체, 특히 ((S)-1,4,5,6-테트라하이드로-2-메틸-4-피리미딘카르복시산) 및 하이드록시엑토인 ((S,S)-1,4,5,6-테트라하이드로-5-하이드록시-2-메틸-4-피리미딘카르복시산).
바람직하게, 호환성 용질의 총 함량은 본 발명에 따른 제형 또는 제품의 총 중량 에 기초하여 0.05 내지 10 중량 %, 바람직하게는 0.1 내지 5 중량 % 범위이다.
용매(Solvents)
약제학적 조성물은 예컨대 예를 들어 지방족 알코올 또는 1,2-알칸다이올 또는 물론 단순히 물을 포함할 수 있다.
1,2- 알칸다이올 . 적절한 1,2-알칸다이올은 1,2-부타다이올, 1,2-펜탄다이올, 1,2-헵탄다이올, 1,2-노난다이올, 1,2-데칸다이올, 1,2-운데칸다이올, 1,2-도데칸다이올, 및 이들의 혼합물을 포함한다. 바람직한 1,2-알칸다이올은 1,2-펜탄다이올이다.
지방족 알코올. 적절한 지방족 알코올은 에탄올, n-프로판올, 이소프로필알코올, 부탄올 이성질체 및 이들의 혼합물로 구성된 그룹으로부터 선택된다. 바람직한 종은 에탄올, 특히 적어도 95%의 순도를 가진 것이다.
본 발명의 추가적인 목적은, 1.2-헥산다이올 및 1,8-헥산다이올의 혼합물의 작용량을,
● 바람직하게는 약 25:75 내지 약 75:25의 중량에 의한 비율로, 보다 바람직하게는 약 40:60 내지 약 60:40의 중량에 의한 양으로 그리고 특히 약 50:50의 중량에 의한 양으로,
● 여기에서 상기 작용량(working amount)은 최종 에멀전 내에서 계산되었을 때 약 0.1 내지 약 1.0 중량%, 및 바람직하게는 약 0.2 내지 약 0.5 중량%를,
첨가함으로써,
(i) 에멀전의 안정성을 개선하고 및/또는
(ii) 에멀전 내 방울(droplet)의 평균 입자 분포를 감소시키고, 및/또는
(iii) 에멀전의 감각적 프로파일을 개선하는 것이다.
마지막으로, 본 발명의 또 다른 목적은 1,2-헥산다이올 및, 2-옥탄다이올의 이원혼합물을, 바람직하게는 상기 개시된 바와 같은 비율로 안정성을 개선시키면서 평균 입자 크기 분포를 감소시키는 동시에 에멀전의 감각적 프로파일을 개선하기 위해, 사용하는 것과 관련되며, 여기에서 이원혼합물은 바람직하게는 최종 에멀전에서 계산되었을 때 상기 에멀전에 대해 약 0.1 내지 약 1.0 중량%의 양이고 바람직하게는 약 0.2 내지 약 0.5 중량%의 양이다.
도 1은 실시예 2 및 비교예 C2 내지 C4의 입자 크기 분포를 나타난다.
도 2는 4가지 조성물의 현미경 이미지를 제공한다.
도 2는 4가지 조성물의 현미경 이미지를 제공한다.
실시예
1,
비교예
C1
내지
C2
항미생물학적
활성
1,2-헥산다이올 및, 1,2-옥탄다이올(1:1)의 항미생물학적 활성이 5가지 주요 미생물에 대하여 1,2-다이올 각각과 비교하여 조사되었다.
EC
에케리치아
콜라이(
Echerichia
coli
)
PA
슈도모나스 에루지노사(
Pseudomonas
aeruginosa
)
SA
스타필로코커스
아우레우스(Staphylococcus
aureus
)
CA
캔디다 알비칸스(
Candida
albicans
)
AN
아스퍼질러스
나이저
(
Aspergillus
niger)
결과는 표 1에 나타내었다. 최소 억제 농도(MIC)는 퍼센트로 보여진다.
[표 1]
항미생물학적
활성
상기 예는 본 발명에 따른 혼합물이 5가지 미생물 중 4가지의 성장을 억제하는 최소 농도에 대하여 상승작용을 보임을 증명한다. 오직 슈도모나스의 경우에 약간의 감소가 달성되었다.
실시예
2.
비교예
C3
내지
C5
입자 크기 분포
O/W 에멀전이 지질상 A 및 수상 B를 별도로 대략 80 ℃로 가열함으로써 제조되었다. 그 후 수상 B가 지질상 A에 첨가되고 6.000 rpm에서 2분간 울트라-투락스 교반기를 사용하여 균질화되었다. 이로써 수득된 에멀전은 바람개비형 교반기(vane stirrer)를 사용하여 150 rpm에서 10분 동안 식혔다. 마지막으로, 수성 소디움 하이드록사이드 용액을 첨가함으로써 pH 값이 약 6.0으로 조정되었다. 야기되는 에멀전의 입자 크기는 레이저 회절의 원리를 사용하는 마스터사이저 마이크로 MAF 500(Mastersizer Micro MAF 500) (Malvern)을 사용하여 결정되었다. 조성물 및 평균 입자 크기는 표 2에 보여진다. 비교예 C2는 위약이고, 비교예 C3 및 C4는 각각의 1,2-다이올을 사용하여 제조되었다. 실시예 2가 본 발명에 따른 것이다.
[표 2]
o/w 에멀전의 조성물(모든 양은 중량%임)
D(v, 0.5) 및 D(v, 0.9) 값과 관련하여 각각의 상승 지표(Sinergy Index, SI)가 쿨의 등식(Kull's equation)에 따라 계산되었다. 조성물 내의 상승은 상승 지표가 1 미만일 대 존재하는데, SI가 낮을수록 상승이 더 큰 것을 의미한다.
●D(v, 0.5) 값에 대한 SI = 0.337
●D(v, 0.9) 값에 대한 SI = 0.261
실시예 2 및 비교예 C2 내지 C4의 입자 크기 분포는 또한 도 1에 나타난다. 지표 "v"는 입자 크기 분포에 기초한 부피를 의미하며; 모든 값은 합계 분포 Qr로부터 취해졌다. 예를 들어, C2에 대한 값 1.7은 입자의 10%가 1.7 ㎛ 보다 작은 입자 크기를 보임을 의미하며 나머지도 마찬가지이다. 보이는 바와 같이, 1,2-헥산다이올 및 1,2-옥탄다이올의 혼합물 첨가는 평균 입자 크기를 상당히 더 작은 값으로 이동시키고 1,2-헥산다이올 및 1,2-옥탄다이올 단독과 비교하여 더 잘게 나누어진 에멀전으로 이어진다. 고도의 상승적 효과는 명확히 보여지고 계산될 수 있었다.
도 2는 4가지 조성물의 현미경 이미지를 제공한다. 시료들은 현미경을 통해 관찰되었다(올림푸스 IX 70, 600 배). 도 2B(=실시예 2)에서, 1,2-헥산다이올 및 1,2-옥탄다이올의 혼합물은 1,2-헥산다이올 및 1,2-옥탄다이올 단독(도 2C 및 도 2D)과 비교하여 상당히 더 작은 입자를 보였고 따라서 입자 크기 측정의 결과를 뒷받침한다.
Claims (15)
- (a) 1,2-헥산다이올 및
(b) 1,2-옥탄다이올을 포함하는 이원 활성 혼합물을 포함하는 조성물로서,
상기 조성물은 10 부피%(Vol.-%)가 2 ㎛보다 작은 지름을 보이고, 50 부피%가 5 ㎛보다 작은 지름을 보이고, 90 부피%가 15 ㎛보다 작은 지름을 보이는 평균 입자 크기를 가지는, 유중수(o/w) 에멀전, 수중유(w/o) 에멀전 또는 다상(w/o/w 또는 o/w/o) 에멀전이고,
최종 에멀전에서 계산된 상기 이원 활성 혼합물의 양은 0.2 내지 0.5 중량 %(wt.-%)인, 조성물. - 제1항의 조성물에 있어서, 상기 구성요소 (a) 및 (b)는 25:75 내지 75:25의 중량에 의한 비율로 존재하는 조성물.
- 제1항의 조성물에 있어서, 상기 구성요소 (a) 및 (b)는 40:60 내지 60:40의 중량에 의한 비율로 존재하는 조성물.
- 제1항의 조성물을 포함하는 화장료 조성물.
- 삭제
- 제4항에 있어서, 상기 조성물은 피부 관리, 모발 관리, 자외선 차단 (sun care) 또는 개인적 관리 조성물인 화장료 조성물.
- 삭제
- 삭제
- 삭제
- 삭제
- 제1항의 조성물을 최종 에멀전에서 계산된 0.2 내지 0.5 중량 %(wt.-%)의 함량으로 첨가함으로써 에멀전의 방울의 평균 입자 분포를 감소시키는 방법.
- 삭제
- 삭제
- 삭제
- 삭제
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BR102016000795A2 (pt) | 2016-08-02 |
BR102016000795B1 (pt) | 2021-04-13 |
JP2021176906A (ja) | 2021-11-11 |
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CN105902402B (zh) | 2021-10-15 |
KR20230019487A (ko) | 2023-02-08 |
MX2016000450A (es) | 2016-07-18 |
US20190247322A1 (en) | 2019-08-15 |
ZA201600079B (en) | 2017-09-27 |
JP2016132668A (ja) | 2016-07-25 |
EP3045161A1 (en) | 2016-07-20 |
JP7050407B2 (ja) | 2022-04-08 |
CN105902402A (zh) | 2016-08-31 |
US20160206571A1 (en) | 2016-07-21 |
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