TW201422249A - Maesa japonica extracts and methods of use - Google Patents

Maesa japonica extracts and methods of use Download PDF

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TW201422249A
TW201422249A TW102135899A TW102135899A TW201422249A TW 201422249 A TW201422249 A TW 201422249A TW 102135899 A TW102135899 A TW 102135899A TW 102135899 A TW102135899 A TW 102135899A TW 201422249 A TW201422249 A TW 201422249A
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skin
extract
composition
osmanthus
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TWI637751B (en
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Siming W Chen
Qian Zheng
John W Lyga
Uma Santhanam
Russell J Wyborski
Leeson Daniel Thorn
Permanan Raaj Khusial
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Avon Prod Inc
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Abstract

Methods of using extracts of Maesa japonica to impart anti-aging benefits to skin and/or improve skin conditions resulting from aging or damaged skin.

Description

山桂花(MAESA JAPONICA)萃取物及使用方法 MAESA JAPONICA extract and method of use 相關申請案Related application

本申請案主張於2011年12月13日提出申請之美國專利申請案第13/324,150號之優先權。本申請案亦與以下申請案同時申請並主張其優先權:於2012年12月11日提出申請且將Qian Zheng指定為最先發明者之標題為「Serissa japonica extracts and methods of use」的PCT申請案第PCT/US12/68858號;及於2012年12月11日提出申請且將Permanan Raaj Khusial列舉為最先發明者之標題為「Stephanotis jasminoides extracts and methods of use」的PCT申請案第PCT/US12/68866號。上述申請案之每一者之全部內容出於所有目的皆以引用方式併入本文中。 The present application claims priority to U.S. Patent Application Serial No. 13/324,150, filed on Dec. 13, 2011. This application also applies and claims its priority at the same time as the following application: PCT application filed on December 11, 2012 and designated by Qian Zheng as the first inventor entitled " Servissa japonica extracts and methods of use"PCT/US12/68858; and PCT Application No. PCT/US12, filed on December 11, 2012, and which listed Permanan Raaj Khusial as the first inventor entitled " Stephanotis jasminoides extracts and methods of use" /68866. The entire content of each of the above applications is hereby incorporated by reference in its entirety for all purposes.

本發明概言之係關於納入山桂花萃取物之化妝品組合物及其用途,其藉由增加表皮厚度、減少黑色素產生及/或刺激膠原及/或玻尿酸產生用於減少細紋及皺紋、改善皮膚色調並使皮膚變色光亮及改善皮膚之整體外觀。 SUMMARY OF THE INVENTION The present invention relates to a cosmetic composition for incorporation of an osmanthus extract and use thereof for reducing fine lines and wrinkles and improving skin by increasing epidermal thickness, reducing melanin production and/or stimulating collagen and/or hyaluronic acid production. The color tone makes the skin discolored and brightens and improves the overall appearance of the skin.

消費者愈來愈多地關注治療、減少或延遲正老化或已老化皮膚之體徵的化妝品。正老化或已老化皮膚之體徵自身表現為紋及皺紋、下垂、暗沉、變色、不均勻色調及/或粗糙膚質。此外,已老化皮膚缺乏強度及彈性且因此較脆。化妝品工業正積極追尋可用於減少正老 化或已老化皮膚之體徵且藉此提供抗皺紋、復原及亮膚效益的產品(抗老化化合物)。 Consumers are increasingly focusing on cosmetics that treat, reduce or delay signs of aging or aging skin. The signs of positively aged or aged skin manifest themselves as wrinkles, wrinkles, sagging, dullness, discoloration, uneven tones, and/or rough skin. In addition, aged skin lacks strength and elasticity and is therefore brittle. The cosmetics industry is actively pursuing the use of reducing the age A product of the aging or aging skin and thereby providing a product that is resistant to wrinkles, rejuvenation and skin lightening (anti-aging compounds).

人類皮膚廣泛分成兩層:為外來元素提供解剖障壁且維持體內環境之表面表皮、以及為表皮提供營養及結構支撐之下伏真皮。表皮主要由角質形成細胞組成且包括若干子層(自最內向外):生髮層/基底層、棘皮層、顆粒層及角質層。藉由角質形成細胞幹細胞之有絲分裂產生之角質形成細胞起源於基底層中且隨後穿過層推進。在該等細胞移動至皮膚表面時,其經歷逐漸分化,從而變無核、平坦化且高度角質化。在此過程期間,角質形成細胞經高度組織化。其經由角蛋白及脂質之排泄彼此之間形成橋粒、細胞接合,形成強化皮膚之細胞外基質。角質形成細胞最終死亡並形成角質層。在健康皮膚中,角質形成細胞脫落並每30天連續更換。 Human skin is broadly divided into two layers: providing an anatomical barrier to foreign elements and maintaining the surface epidermis of the internal environment, as well as providing nutrients and structural support to the epidermis. The epidermis consists primarily of keratinocytes and includes several sub-layers (from the innermost to the outer): the germinal/basal layer, the echinoderma, the granular layer, and the stratum corneum. Keratinocytes produced by mitosis of keratinocyte stem cells originate in the basal layer and then advance through the layer. As the cells move to the surface of the skin, they undergo a gradual differentiation that becomes non-nuclear, flattened, and highly keratinized. During this process, keratinocytes are highly organized. It forms a desmosome and a cell junction between keratin and lipid excretion to form an extracellular matrix that strengthens the skin. The keratinocytes eventually die and form the stratum corneum. In healthy skin, keratinocytes shed and were replaced continuously every 30 days.

儘管角質形成細胞在基底層內,但其需要黑色素,一種來自黑色素細胞之黑色紫外光吸收色素。黑色素細胞在稱作黑色素小體之細胞器內產生黑色素且隨後經由其樹突將含有黑色素之黑色素小體轉移至相鄰角質形成細胞。在每一角質形成細胞內,黑色素小體形成黑色素蓋,其保留於角質形成細胞內直至角質形成細胞自皮膚脫落為止。黑色素蓋減輕對人類表皮及下伏細胞及組織之紫外線誘導之DNA損害。黑色素提供皮膚具有其顏色且因此皮膚顏色之強度與數目、大小、黑色素含量、含有黑色素之黑色素小體之形成速率、含有黑色素之黑色素小體轉移至角質形成細胞之速率及黑色素在角質形成細胞內降解之速率相關。對於關於黑色素之更詳細背景,參見G.Costin及V.Hearing,「Human skin pigmentation:melanocytes modulate skin color in response to stress」,The FASEB Journal第21卷,第976-994頁,2007年4月,其揭示內容之全文以引用方式併入本文中。 Although keratinocytes are within the basal layer, they require melanin, a black ultraviolet light absorbing pigment from melanocytes. Melanocytes produce melanin in an organelle called melanin bodies and then transfer melanin bodies containing melanin to adjacent keratinocytes via their dendrites. Within each keratinocyte, the melanin bodies form a melanin cap that remains in the keratinocytes until the keratinocytes are detached from the skin. Melanin caps reduce UV-induced DNA damage to human epidermis and underlying cells and tissues. Melanin provides the skin with its color and therefore the intensity and number of skin colors, the size, the melanin content, the rate of formation of melanin-containing melanin bodies, the rate at which melanin-containing melanin bodies are transferred to keratinocytes, and melanin in keratinocytes The rate of degradation is related. For a more detailed background on melanin, see G. Costin and V. Hearing, "Human skin pigmentation: melanocytes modulate skin color in response to stress", The FASEB Journal, Vol. 21, pp. 976-994, April 2007, The disclosure of which is incorporated herein by reference in its entirety.

玻尿酸(HA)(一種膠狀胺基聚糖)亦在正常表皮中起重要作用。 HA係基底角質形成細胞之細胞外基質的組成部分,從而維持細胞外空間並為營養素之通過提供開口及水合結構。HA亦可用作自由基清除劑,促使表皮抵抗太陽輻射。HA亦可用作角質形成細胞增殖及遷移之調節劑。 Hyaluronic acid (HA), a colloidal aminoglycan, also plays an important role in normal epidermis. The HA is a component of the extracellular matrix of the basal keratinocytes, thereby maintaining extracellular space and providing an opening and hydration structure for the passage of nutrients. HA can also be used as a free radical scavenger to promote the epidermis against solar radiation. HA can also be used as a modulator of keratinocyte proliferation and migration.

真皮係位於表皮與皮下組織之間之皮膚之下伏層。由於表皮無血管,故表皮之細胞的營養素及氧依賴於真皮中之血管。真皮-表皮接合(DEJ)係維持緻密板(即上皮位於其上之細胞外基質之層)與真皮之下伏結締組織之間緊密接觸的專門結構。DEJ主要包括膠原及彈性蛋白且結構化為自表皮及真皮層之聯鎖指狀突出物,稱作表皮突。表皮突增加DEJ處暴露於真皮之表皮之表面區域,以使必需營養素/氧之轉移更有效,且皮膚之兩個層形成抵抗機械應力(剪切)之強鍵。另外,真皮係最厚之皮膚層且包含皮膚之細胞外基質,其由成纖維細胞維持。成纖維細胞藉由連續分泌細胞外基質之前體維持結締組織之結構完整性。真皮之主要結構組份係稱作膠原之蛋白質。膠原分子束貫穿真皮堆疊在一起,佔皮膚之乾燥重量之四分之三。膠原具有大的抗拉強度;以及軟角蛋白,其負責皮膚強度及彈性。對於關於膠原之詳細背景,參見Lodish等人,Molecular Cell Biology,W.H.FREEMAN,New York,NY,第4版,2000,其揭示內容之全文以引用方式併入本文中。 The dermis is located beneath the skin between the epidermis and the subcutaneous tissue. Since the epidermis has no blood vessels, the nutrients and oxygen of the cells of the epidermis depend on the blood vessels in the dermis. The dermis-epidermal junction (DEJ) is a specialized structure that maintains a close contact between the dense plate (i.e., the layer of the extracellular matrix on which the epithelium is located) and the connective tissue beneath the dermis. DEJ mainly consists of collagen and elastin and is structured as an interlocking finger protrusion from the epidermis and dermis, called the epidermal process. The epidermal process increases the surface area of the epidermis exposed to the dermis at DEJ to make the transfer of essential nutrients/oxygen more effective, and the two layers of the skin form strong bonds against mechanical stress (shear). In addition, the dermis is the thickest skin layer and contains the extracellular matrix of the skin, which is maintained by fibroblasts. Fibroblasts maintain the structural integrity of connective tissue by continuously secreting the extracellular matrix precursor. The main structural component of the dermis is called collagen protein. Collagen molecular bundles are stacked across the dermis, accounting for three-quarters of the dry weight of the skin. Collagen has a large tensile strength; and soft keratin, which is responsible for skin strength and elasticity. For a detailed background on collagen, see Lodish et al, Molecular Cell Biology, W. H. FREEMAN, New York, NY, 4th edition, 2000, the disclosure of which is incorporated herein in its entirety by reference.

皮膚之組織學研究顯示在老化發生時,皮膚經歷與其他體器官之老化及變性變化並行之結構、功能及代謝變化。儘管年齡性及/或激素老化在皮膚老化中起明顯作用,但環境應力(例如太陽暴露)亦可起始及/或加速皮膚老化,此部分係由於於紫外(UV)日光中之過暴露。在已老化及/或正老化皮膚中,細胞補充起來耗時更長、數目較少及/或分解更快速。具體而言,在發生老化時,膠原之產生減少,同時降解加速,此乃因膠原酶(即分解膠原之蛋白酶)之過度產生。所 產生之膠原缺乏可導致皮膚強度及彈性降低。此外,由於膠原係DEJ之主要組份,故DEJ隨著老化變平,以使皮膚更脆且更可能剪切。隨著DEJ變平,轉移至表皮之營養素/氧之量減少,此乃因與表皮接觸之表面區域收縮。表皮細胞外基質內之HA之減少會降低將表皮有用營養素/氧轉移至其細胞之能力。此無效營養素/氧運輸影響表皮之角質形成細胞及黑色素細胞。角質形成細胞更新速率降低且因此,角質層損失其保留水份能力且皮膚脫水。此外,黑色素細胞之數目變少且剩餘黑色素細胞可產生更大量之黑色素,從而導致皮膚變色/色素沉著過度及/或太陽斑痣、「老人斑」。在皮膚表面處,已老化或正老化皮膚可呈現紋及皺紋、下垂、暗沉、變色、不均勻色調、粗糙膚質及諸如此類。另外,已老化或正老化皮膚呈現較小強度及撓性且更脆。老化之該等體徵可因常見藥劑(例如彼等指示用於治療帕金森氏病(Parkinson’s disease)(即左旋多巴(Levodopa)或停經(即激素療法)者))加劇。 Histological studies of the skin have shown that when aging occurs, the skin undergoes structural, functional, and metabolic changes in parallel with changes in aging and degeneration of other body organs. Although age and/or hormonal aging plays a significant role in skin aging, environmental stress (eg, sun exposure) may also initiate and/or accelerate skin aging due to overexposure in ultraviolet (UV) sunlight. In aged and/or aging skin, cells are added longer, less frequently, and/or decomposed faster. Specifically, when aging occurs, the production of collagen is reduced, and the degradation is accelerated, which is caused by the excessive production of collagenase (ie, collagen-decomposing protease). Place The lack of collagen produced can result in reduced skin strength and elasticity. Furthermore, due to the major component of collagen-based DEJ, DEJ flattens with aging to make the skin more brittle and more likely to shear. As the DEJ flattens, the amount of nutrients/oxygen transferred to the epidermis decreases, due to shrinkage of the surface area in contact with the epidermis. A decrease in HA in the extracellular matrix of the epidermis reduces the ability to transfer the epidermis with useful nutrients/oxygen to its cells. This ineffective nutrient/oxygen transport affects the keratinocytes and melanocytes of the epidermis. The rate of keratinocyte renewal is reduced and, therefore, the stratum corneum loses its ability to retain moisture and dehydrate the skin. In addition, the number of melanocytes is reduced and the remaining melanocytes can produce a greater amount of melanin, resulting in skin discoloration/hypigmentation and/or sunburn, "old age spots". At the surface of the skin, aged or aging skin can exhibit wrinkles and wrinkles, sagging, dullness, discoloration, uneven tones, rough skin and the like. In addition, aged or positively aged skin exhibits less strength and flexibility and is more brittle. Such signs of aging may be exacerbated by common agents (e.g., those indicated for use in the treatment of Parkinson's disease (i.e., Levodopa or menopause (i.e., hormonal therapy)).

一種用於抗老化皮膚護理之熟知產品係視黃醇,已證明其可有效減少臉部皮膚上之可視老化體徵。視黃醇具有副作用,包括引起皮膚刺激之趨勢或在暴露於氧或UV時分解之趨勢,藉此損害其效率。 A well-known product for anti-aging skin care is retinol, which has been shown to be effective in reducing visible signs of aging on the skin of the face. Retinol has side effects, including a tendency to cause skin irritation or a tendency to decompose upon exposure to oxygen or UV, thereby impairing its efficiency.

山桂花(亦稱作杜莖山(du jing shan)或日本山桂花(izo-senryo))係原產於中國南部、越南及日本之多年生植物。該植物具有葉,其係硬紙質或幾乎革樣;橢圓形、窄橢圓形披針形或長方形卵圓形;6cm至9cm長及3cm至5cm寬;頂點尖形、銳利或鈍的;基底圓形或圓頭;很少楔形;頂部上幾乎整個或鋸齒形;側脈5至8對;莖長5mm至15mm。花通常係腋生總狀花序或圓錐花序。單生花有時聚集;花長度為3mm至5mm;腎形小苞片,具有突出腺狀條紋;花萼,覆瓦狀,卵圓形至球形;鐘狀花冠,白色,3mm至4mm長,具有腺狀形狀及寬卵圓形葉片。山桂花葉已用於傳統中藥以治癒疥瘡。仍需要解決老 化體徵、具體而言皺紋、紋及變色區域之外觀的化妝品組合物。因此,本發明之目標係提供新組合物及治療、改善及/或預防已老化或正老化皮膚之體徵的方法。本發明之又一目標係改善正老化或已老化皮膚之整體外觀。 Osmanthus fragrans (also known as du jing shan or izo-senryo) is a perennial plant native to southern China, Vietnam and Japan. The plant has leaves which are hard paper or almost leather-like; elliptical, narrow elliptical lanceolate or oblong oval; 6 cm to 9 cm long and 3 cm to 5 cm wide; apex pointed, sharp or blunt; base circular Or rounded; rarely wedge-shaped; almost entirely or serrated on the top; 5 to 8 pairs of lateral veins; stem length 5 mm to 15 mm. Flowers are usually axillary racemes or panicles. Single flower sometimes gathers; flower length 3mm to 5mm; kidney-shaped bracteoles, with glandular streaks; calyx, imbricate, ovoid to spherical; bell-shaped corolla, white, 3mm to 4mm long, glandular Shaped and wide oval leaves. The osmanthus leaves have been used in traditional Chinese medicine to cure acne. Still need to solve the old A cosmetic composition that modifies signs, particularly wrinkles, lines, and the appearance of discolored areas. Accordingly, it is an object of the present invention to provide new compositions and methods of treating, ameliorating and/or preventing signs of aged or aging skin. Yet another object of the invention is to improve the overall appearance of aged or aged skin.

以上論述僅為該技術所面臨問題之本質提供更佳之理解且不應以任何方式理解為對先前技術之認同,亦不應將本文任何參考文獻之引用理解為認同該參考文獻構成本發明之「先前技術」。 The above discussion is only to provide a better understanding of the nature of the problems faced by the technology and should not be construed as an admission of the prior art in any way. Prior art."

根據上述目標及其他,已發現山桂花萃取物係體內膠原、玻尿酸及黑色素合成之調節劑且因此係抵抗皮膚內老化及變色之體徵的有益試劑。 In accordance with the above objectives and others, it has been found that the extract of osmanthus fragrans is a beneficial agent for the synthesis of collagen, hyaluronic acid and melanin in the body and is therefore a sign of resistance to aging and discoloration in the skin.

本發明概言之係關於改善有需要之老化皮膚美觀的方法,其係藉由以下方式達成:向皮膚局部施用存於化妝品上可接受之媒劑中的組合物,該組合物包含有效賦予皮膚美觀改善之量的山桂花萃取物。在一個實施例中,皮膚係敏感性皮膚。在本發明之又一實施例中,至少每日一次將組合物局部施用至皮膚至少一週。 SUMMARY OF THE INVENTION The present invention relates to a method for improving the aesthetic appearance of aged skin in need thereof by topically applying to the skin a composition in a cosmetically acceptable vehicle, the composition comprising an effective application to the skin. A beautifully improved amount of osmanthus extract. In one embodiment, the skin is sensitive to the skin. In yet another embodiment of the invention, the composition is topically applied to the skin at least once a day for at least one week.

在某些實施例中,老化可係由於年齡性、激素或環境效應。在其他實施例中,美觀之改善係選自以下之群:(a)治療、減輕及/或預防細紋或皺紋;(b)減小皮膚毛孔大小;(c)改善皮膚厚度、豐滿度及/或緊實度;(d)改善皮膚柔順度及/或柔軟度;(e)改善皮膚色調、光彩及/或透明度;(f)改善原膠原及/或膠原產生;(g)改善彈性蛋白之維持及重塑;(h)改善膚質及/或促進煥膚;(i)改善皮膚障壁修復及/或功能;(j)改善皮膚輪廓之外觀;(k)恢復皮膚光澤及/或亮度;(l)補充皮膚中之必需營養素及/或成份;(m)改善因老化及/或停經而衰減之皮膚外觀;(n)改善皮膚濕潤性及/或水合;(o)增加及/或預防損失皮膚彈性及/或回彈性;(p)治療、減少及/或預防皮膚下 垂;(q)治療、減少及/或預防皮膚變色;及(r)其任何組合。在本發明之其他實施例中,皮膚改善可係由於膠原合成增加、玻尿酸合成增加、表皮厚度增加、黑色素合成減少;或其任何組合。 In certain embodiments, aging can be due to age, hormonal, or environmental effects. In other embodiments, the improvement in aesthetics is selected from the group consisting of: (a) treating, reducing, and/or preventing fine lines or wrinkles; (b) reducing skin pore size; (c) improving skin thickness, fullness, and / or firmness; (d) improve skin suppleness and / or softness; (e) improve skin tone, brilliance and / or transparency; (f) improve procollagen and / or collagen production; (g) improve elastin (h) improve skin texture and/or promote skin rejuvenation; (i) improve skin barrier repair and/or function; (j) improve the appearance of skin contours; (k) restore skin shine and/or brightness (l) replenish essential nutrients and/or ingredients in the skin; (m) improve the appearance of the skin attenuated by aging and/or menopause; (n) improve skin moistness and/or hydration; (o) increase and / or Prevent loss of skin elasticity and/or rebound; (p) treat, reduce and/or prevent under the skin (q) treating, reducing and/or preventing skin discoloration; and (r) any combination thereof. In other embodiments of the invention, skin improvement may be due to increased collagen synthesis, increased hyaluronic acid synthesis, increased epidermal thickness, decreased melanin synthesis, or any combination thereof.

在本發明之再一實施例中,萃取物可以基於組合物之總重量約0.0001wt%至約90wt%之量存在,且在又一實施例中,可以組合物之總重量之約0.01wt%至約10wt%之量存在。在某些實施例中,山桂花植物萃取物可源自山桂花植物之花。 In still another embodiment of the present invention, the extract may be present in an amount of from about 0.0001% by weight to about 90% by weight based on the total weight of the composition, and in yet another embodiment, may be about 0.01% by weight based on the total weight of the composition. It is present in an amount of up to about 10% by weight. In certain embodiments, the osmanthus plant extract may be derived from the flower of a osmanthus plant.

本發明之另一實施例係關於改善皮膚之障壁功能及活力的方法,其係藉由以下方式達成:向皮膚局部施用存於化妝品上可接受之媒劑的組合物,該組合物包含可有效增加膠原合成、增加玻尿酸合成、增加表皮厚度、減少黑色素合成或其任何組合之量之山桂花萃取物。在此方法之特定實施例中,萃取物係源自山桂花之花。在該方法之其他實施例中,植物萃取物係以基於組合物之總重量約0.0001wt%至約90wt%之量存在,且在又一些實施例中,植物萃取物係以基於組合物之總重量約0.01wt%至約10wt%之量存在。 Another embodiment of the present invention relates to a method for improving barrier function and vitality of the skin by topically applying to the skin a composition for a cosmetically acceptable vehicle, the composition comprising an effective A sweet-scented osmanthus extract that increases collagen synthesis, increases hyaluronic acid synthesis, increases epidermal thickness, reduces melanin synthesis, or any combination thereof. In a particular embodiment of this method, the extract is derived from the flower of the osmanthus flower. In other embodiments of the method, the plant extract is present in an amount from about 0.0001 wt% to about 90 wt%, based on the total weight of the composition, and in still other embodiments, the botanical extract is based on the total composition It is present in an amount of from about 0.01% by weight to about 10% by weight.

本發明方法之又一實施例係關於治療皺紋、細紋或下垂皮膚,其係藉由以下方式達成:向皮膚局部施用存於化妝品上可接受之媒劑的組合物,該組合物包含可有效治療有需要之皮膚之量的山桂花萃取物。 A further embodiment of the method of the present invention relates to the treatment of wrinkles, fine lines or sagging skin by topically applying to the skin a composition for a cosmetically acceptable vehicle, the composition comprising an effective A sweet-scented osmanthus extract that treats the amount of skin needed.

使有需要之亮膚之方法係本發明之另一實施例。該方法涉及向有需要之皮膚局部施用存於化妝品上可接受之媒劑中的光亮組合物,該組合物包含可有效達成光亮效益之量的山桂花萃取物之。在此方法之其他實施例中,植物萃取物係以基於組合物之總重量約0.01wt%至約10wt%之量存在。 A method of making a skin light in need is another embodiment of the present invention. The method involves topically applying to a skin in need thereof a brightening composition in a cosmetically acceptable vehicle, the composition comprising an extract of osmanthus fragrans in an amount effective to achieve a luminous benefit. In other embodiments of this method, the plant extract is present in an amount from about 0.01% to about 10% by weight, based on the total weight of the composition.

在某些實施例中,光亮效益可選自由以下組成之群:(a)漂白色素沉著過度之毛髮、皮膚、唇及/或指甲;(b)減少老人斑;(c)使皮 膚變色均勻或最佳化;(d)改善眼下暗圈之外觀;(e)治療黑斑病、黃褐斑、雀斑、燒傷後疤痕及損傷後色素沉著過度;(f)漂白頭皮、腿、臉部及其他期望漂白及顏色減少之區域上之毛髮;(g)漂白指甲染色;及(h)其組合。光亮效益可係由於黑色素合成減少,且在某些實施例中,黑色素合成減少可為約20-100%,且在其他實施例中可為約40-100%。 In certain embodiments, the luminous benefit can be selected from the group consisting of: (a) bleaching hyperpigmented hair, skin, lips, and/or nails; (b) reducing age spots; (c) making skin (d) improving the appearance of the dark circles under the eyes; (e) treating black spot, chloasma, freckles, scars after burns and hyperpigmentation after injury; (f) bleaching the scalp, legs, Hair on the face and other areas where bleaching and color reduction are desired; (g) bleaching nail staining; and (h) combinations thereof. The brightening benefit may be due to reduced melanin synthesis, and in certain embodiments, the melanin synthesis reduction may be about 20-100%, and in other embodiments may be about 40-100%.

又一實施例係關於藉由向有需要之皮膚區域局部施用有效量之調節皮膚生物標記之山桂花萃取物來治療皮膚的方法,其中藉由量測選自包含以下之群之皮膚生物標記之變化量的分析來測定山桂花萃取物調節皮膚生物標記之能力:表皮變厚、總膠原、原膠原、及與山桂花萃取物接觸之皮膚細胞及/或皮膚細胞分化前前體中之玻尿酸結合蛋白。 A further embodiment relates to a method of treating skin by topically applying to the skin area in need thereof an effective amount of a skin biomarker-regulating osmanthus extract, wherein the skin biomarker selected from the group consisting of: Analysis of the amount of change to determine the ability of the extract of Osmanthus fragrans to regulate skin biomarkers: thickening of the epidermis, total collagen, procollagen, and hyaluronic acid in skin cells and/or pre-differentiation precursors of skin cells in contact with osmanthus extract protein.

參照以下詳細說明及附圖,將更佳地理解本發明之該等及其他態樣。 These and other aspects of the present invention will be better understood from the following detailed description and drawings.

圖1係山桂花萃取物之HPLC概況。 Figure 1 is an HPLC overview of the extract of Osmanthus fragrans.

本文中揭示本發明之詳細實施例;然而,應理解,所揭示實施例僅具本發明之闡釋性,本發明可以各種形式來體現。另外,結合本發明之各個實施例給出之每一實例意欲具有闡釋性而非限制性。此外,該等圖不必按比例,且一些特徵可放大以顯示實施例組份之詳情。另外,圖中顯示之任何量測、說明及諸如此類意欲具有闡釋性而非限制性。因此,本文中揭示之具體結構及功能詳情不應揭示為具有限制性,而是用作教示所屬技術領域之技術人員不同地利用本發明之代表性基礎。 The detailed embodiments of the present invention are disclosed herein; however, it is understood that the disclosed embodiments are only illustrative of the invention, and the invention may be embodied in various forms. In addition, each of the examples given in connection with the various embodiments of the invention is intended to be illustrative and not restrictive. In addition, the figures are not necessarily to scale, and some features may be exaggerated to show the details of the embodiments. In addition, any measurement, description, and the like in the figures are intended to be illustrative and not limiting. Therefore, the specific structural and functional details disclosed herein are not to be construed as limiting, but as a representative basis of the teachings of those skilled in the art.

年輕皮膚之成功恢復必須解決多個關鍵問題,其包括:成纖維 細胞及角質形成細胞之活力、表皮及真皮中之細胞-細胞黏著、對表皮之細胞營養、角質形成細胞之間之細胞-細胞錨固及黏著、真皮與表皮之間之通信、膠原酶過度產生、膠原更換及皮膚之機械性質。本發明經由使用納入山桂花萃取物之化妝品組合物解決該等關鍵問題。具體而言,可使用本發明組合物減少細紋及皺紋、改善皮膚色調及減少變色並改善皮膚之整體外觀。山桂花萃取物可增加表皮厚度、減少黑色素合成、刺激膠原合成、刺激玻尿酸合成及/或促進其任何組合。 Successful recovery of young skin must address several key issues, including: Fibrillation Cell and keratinocyte viability, cell-cell adhesion in the epidermis and dermis, cell nutrition to the epidermis, cell-cell anchorage and adhesion between keratinocytes, communication between the dermis and epidermis, overproduction of collagenase, Collagen replacement and mechanical properties of the skin. The present invention addresses these critical issues via the use of cosmetic compositions incorporating osmanthus extract. In particular, the compositions of the present invention can be used to reduce fine lines and wrinkles, improve skin tone and reduce discoloration and improve the overall appearance of the skin. The osmanthus extract can increase epidermal thickness, reduce melanin synthesis, stimulate collagen synthesis, stimulate hyaluronic acid synthesis, and/or promote any combination thereof.

本發明提供用於局部施用之組合物,其包含有效量之山桂花萃取物以治療、逆轉、改善及/或預防皮膚損害或皮膚老化之體徵。該等效益包括(但不限於)以下:(a)治療、減輕及/或預防細紋或皺紋,(b)減小皮膚毛孔大小,(c)改善皮膚厚度、豐滿度及/或緊實度;(d)改善皮膚柔順度及/或柔軟度;(e)改善皮膚色調、光彩及/或透明度;(f)改善原膠原及/或膠原產生;(g)改善彈性蛋白之維持及重塑;(h)改善膚質及/或促進煥膚;(i)改善皮膚障壁修復及/或功能;(j)改善皮膚輪廓之外觀;(k)恢復皮膚光澤及/或亮度;(l)補充該皮膚中之必需營養素及/或成份;(m)改善因老化及/或停經而衰減之皮膚外觀;(n)改善皮膚濕潤性及/或水合;(o)增加及/或預防損失皮膚彈性及/或回彈性; (p)治療、減少及/或預防皮膚下垂;及/或(q)治療、減少及/或預防皮膚變色。 The present invention provides compositions for topical administration comprising an effective amount of osmanthus extract to treat, reverse, ameliorate and/or prevent signs of skin damage or skin aging. These benefits include, but are not limited to, the following: (a) treating, reducing and/or preventing fine lines or wrinkles, (b) reducing skin pore size, and (c) improving skin thickness, fullness and/or firmness (d) improving skin suppleness and/or softness; (e) improving skin tone, brilliance and/or transparency; (f) improving procollagen and/or collagen production; (g) improving elastin maintenance and remodeling (h) improve skin texture and / or promote skin rejuvenation; (i) improve skin barrier repair and / or function; (j) improve the appearance of skin contours; (k) restore skin shine and / or brightness; (l) supplement Essential nutrients and/or ingredients in the skin; (m) improving the appearance of the skin attenuated by aging and/or menopause; (n) improving skin moisturization and/or hydration; (o) increasing and/or preventing loss of skin elasticity And/or rebound flexibility; (p) treating, reducing and/or preventing sagging of the skin; and/or (q) treating, reducing and/or preventing discoloration of the skin.

實際上,可將本發明組合物施用至需要治療之皮膚。亦即,患有任何上述屬性之缺失或損失或否則將受益於任何上述皮膚屬性之改善的皮膚。 In fact, the compositions of the invention can be applied to the skin in need of treatment. That is, suffering from any loss or loss of any of the above attributes or otherwise would benefit from any of the above-described skin attributes.

在另一實施例中,使用納入山桂花萃取物之組合物來使毛髮、皮膚、唇及/或指甲光亮、即減少其色素沉著以達成以下光亮效益:(a)漂白色素沉著過度之毛髮、皮膚、唇及/或指甲;(b)減少老人斑;(c)使皮膚變色均勻或最佳化;(d)改善眼下暗圈之外觀;(e)治療黑斑病、黃褐斑、雀斑、燒傷後疤痕及損傷後色素沉著過度;(f)漂白頭皮、腿、臉部及其他期望漂白及顏色減少之區域上之毛髮;及/或(g)漂白指甲染色。 In another embodiment, the composition incorporating the osmanthus extract is used to brighten, ie, reduce, pigmentation of the hair, skin, lips and/or nails to achieve the following luminous benefits: (a) bleaching hyperpigmented hair, (b) reducing age spots; (c) making skin discoloration uniform or optimal; (d) improving the appearance of the underlying dark circles; (e) treating black spot, chloasma, freckles , post-burn scars and hyperpigmentation after injury; (f) bleaching of scalp, legs, face and other areas of bleaching and color reduction; and/or (g) bleaching nail staining.

在一個實施例中,組合物意欲用作非治療性治療。在另一實施例中,組合物係根據US FD&C Act,sec.201(i)意欲擦拭、傾倒、噴灑或噴霧於人體上、引入人體中或以其他方式施用至人體用於清潔、美化、促進吸引力或改變外觀之物件。 In one embodiment, the composition is intended for use as a non-therapeutic treatment. In another embodiment, the composition is intended to be wiped, poured, sprayed or sprayed onto the human body, introduced into the human body, or otherwise applied to the human body for cleaning, beautification, promotion, according to the US FD&C Act, sec. 201(i). An object that appeals or changes its appearance.

實際上,可將本發明組合物施用至需要治療之皮膚。亦即,患有任何上述屬性之缺失或損失或否則將受益於任何上述皮膚屬性之改善的皮膚。 In fact, the compositions of the invention can be applied to the skin in need of treatment. That is, suffering from any loss or loss of any of the above attributes or otherwise would benefit from any of the above-described skin attributes.

除非另有規定,否則本文使用之所有術語均意欲具有其普通含義。 Unless otherwise stated, all terms used herein are intended to have their ordinary meaning.

術語「活性量」係指在無稀釋劑、溶劑、載劑、填充劑或任何 其他成份下之山桂花萃取物之量。為皮膚提供特定抗老化效益之「有效量」(「amount effective」或「effective amount」)係指提供老化之特定表現(即在施用或投與足以提供老化之特定表現之臨床上可量測之改善時,與老化有關之不期望特徵)之臨床上可量測之改善所需之萃取物之「活性量」。 The term "activity amount" means no diluent, solvent, carrier, filler or any The amount of osmanthus extract under other ingredients. An "effective amount" ("amount effective" or "effective amount") is used to provide a specific indication of aging (ie, clinically measurable in the administration or administration of a specific performance sufficient to provide aging) The clinically measurable improvement in the "activity amount" of the extract required for the improvement of the undesired characteristics associated with aging.

本文所用術語「有需要之人」係指由於老化具有不期望皮膚症狀、不期望特徵(例如紋及皺紋、下垂、暗沉、變色、不均勻色調、粗糙膚質等)之個體或在不存在顯著且不期望之皮膚症狀下選擇以降低老化之效應(即防止性或預防性)之個體。 The term "person in need" as used herein refers to an individual who has undesired skin symptoms due to aging, undesirable characteristics (such as wrinkles and wrinkles, sagging, dullness, discoloration, uneven color tone, rough skin, etc.) or does not exist. Individuals selected to reduce the effects of aging (ie, preventive or prophylactic) under significant and undesirable skin conditions.

本文所用術語「基本上由......組成」意欲將本發明限於指定材料或步驟及彼等不會顯著影響所主張本發明之基本及新穎特徵者,如自閱讀本說明書所瞭解。 The term "consisting essentially of" is used herein to mean that the invention is limited to the specified materials or steps and that they do not significantly affect the basic and novel characteristics of the claimed invention.

「化妝品上可接受」意指通常將特定組份視為在所用量下安全且無毒。 "Cosmetically acceptable" means that a particular component is generally considered safe and non-toxic at the dosage employed.

本文所用術語「變色」包括分散色素沉著及有斑點之色素沉著。分散色素沉著係較深色素之不同均勻區域且可看似皮膚上之褐色斑點或雀斑且可包括太陽雀斑痣、由老化及太陽引起之皮膚上之變深斑點,亦稱作「壽斑」、「老年性雀斑」或「老人斑」或雀子斑、雀斑。有斑點之色素沉著係大小及形狀較分散色素沉著更大且更不規則之深色斑點且可包括諸如由激素(即由於懷孕、避孕藥或雌激素替換療法)引起之黃褐斑、黑斑病、皮膚變色等症狀。變色可係由於外部因素(其包括但不限於UV-R、皮膚曬黑及光老化、藥物及/或化學品)或內部因素(其包括但不限於遺傳、激素影響及/或發炎)。在本發明之某些實施例中,變色可不包括由於因座瘡或皮炎引起之發炎的色素沉著過度。 The term "discoloration" as used herein includes disperse pigmentation and speckle pigmentation. Disperse pigmentation is a different uniform area than dark pigment and can appear as brown spots or freckles on the skin and can include sun-spotted ticks, dark spots on the skin caused by aging and the sun, also known as "life spots", "Old age freckles" or "old age spots" or freckles, freckles. Spotted pigmentation systems are larger in size and shape than discolored pigmentation and more irregular dark spots and may include chloasma, dark spots such as those caused by hormones (ie, due to pregnancy, birth control pills or estrogen replacement therapy). Symptoms such as illness and skin discoloration. Discoloration can be due to external factors including, but not limited to, UV-R, skin tanning and photoaging, drugs and/or chemicals, or internal factors including, but not limited to, heredity, hormonal effects, and/or inflammation. In certain embodiments of the invention, discoloration may not include hyperpigmentation due to inflammation due to acne or dermatitis.

皮膚彈性係指皮膚在變形後重新獲得其初始形狀及大小之能力 的彈性及回彈性。可藉由捏指測試評價皮膚彈性,該捏掐測試可藉由拉伸或擠壓皮膚引起變形。 Skin elasticity refers to the ability of the skin to regain its original shape and size after deformation. Flexibility and resilience. Skin elasticity can be evaluated by a pinch test which can be deformed by stretching or squeezing the skin.

本文所用術語「精油」係指藉由物理分離過程(例如蒸餾或層析分離)自植物或植物部分獲得之揮發性醚性部分。精油通常係經常包含單萜之類萜且具有萃取其之植物之味道及香味。 The term "essential oil" as used herein refers to a volatile etheric moiety obtained from a plant or plant part by a physical separation process such as distillation or chromatographic separation. Essential oils often contain a cockroach such as a cockroach and have the taste and aroma of the plant from which they are extracted.

術語「光亮」在本文中意欲指任何可檢測之毛髮、皮膚、唇及/或指甲之皮膚顏色/色素沉著之減輕,例如裸眼可見之減輕,其在個體皮膚與包含山桂花萃取物之治療方案接觸後發生。作為實例,此可係指使皮膚變色均勻或最佳化(即漂白老人斑、雀斑等)以降低或消除變色皮膚與周圍皮膚之間之顏色差異;及/或使個體之正常色素沉著/皮膚顏色整體光亮,使亮膚。術語減少色素沉著、光亮、漂白或顏色減少在本文中可互換使用。不希望受限於特定理論,申請者相信本發明之草藥萃取物藉由損害黑色素合成、藉此減少黑色素產生而達成此光亮效應。術語「減少黑色素產生」在本文中用於意指與在無山桂花萃取物下合成之黑色素之量相比,可檢測地降低由暴露於該抑制化合物之黑色素細胞合成之黑色素之量。在本文中關於黑色素使用之術語「減少」分別意指完全預防、控制分泌或一定程度地減少黑色素形成。在一個實施例中,術語「降低」係指藉此合成之黑色素之量減少約10%至約100%。在一個實施例中,術語「降低」係指所合成黑色素之量減少約25%至約100%。在一個實施例中,術語「降低」係指所合成黑色素之量減少約35%至約100%。在一個實施例中,術語「降低」係指所合成黑色素之量減少約40%至約100%。術語降低、減輕、減少、阻抑及抑制在關於黑色素產生使用時意欲互換使用。可主觀或藉由使用包括但不限於彼等熟習此項技術者已知之活體外、離體、動物模型及/或臨床模型的分析評價該黑色素產生減少。舉例而言,可使用彼等熟習此項技術者已知之方法(包括但不限於人類黑色素細胞培 養、黑色素瘤培養(參見下文實例3及美國專利7,189,419,其全部內容出於所有目的皆以引用方式併入本文中)、HRM2毛髮較少小鼠模型(參見Chung等人之「Evaluation of in vitro and in vivo anti-melanogenic activity of a newly synthesized strong tyrosinase inhibitor(E)-3-(2,4 dihydroxybenzylidene)pyrrolidine-2,5-dione(3-DBP),」Biochim Biophys Acta.2012年7月;1820(7):962-9,其全部內容出於所有目的皆以引用方式併入本文中)、斑馬魚模型(參見Choi,T.Y.;Kim,J.H.;Ko,D.H.;Kim,C.H.;Hwang,J.S.;Ahn,S.;Kim,S.Y.;Kim,C.D.;Lee,J.H.;Yoon,T.J.Zebrafish as a new model for phenotype-based screening of melanogenic regulatory compounds.Pigment Cell Res.2007,20,120-127,其全部內容出於所有目的皆以引用方式併入本文中)及MelanoDermTM皮膚模型(MatTek公司,Ashland,MA))確立黑色素合成減少。 The term "bright" is used herein to mean any measurable reduction in skin color/pigmentation of the hair, skin, lips and/or nails, such as reduction of visible to the naked eye, in the treatment of individual skin and treatments containing osmanthus extract. Occurs after contact. By way of example, this may mean that the skin is discolored or optimized (ie, bleaching age spots, freckles, etc.) to reduce or eliminate color differences between the color-changing skin and the surrounding skin; and/or to cause normal pigmentation/skin color in the individual. overall bright, even skin lightening. The term reducing pigmentation, lightening, bleaching or color reduction is used interchangeably herein. Without wishing to be bound by a particular theory, Applicants believe that the herbal extract of the present invention achieves this luminous effect by impairing melanin synthesis, thereby reducing melanin production. The term "reducing melanin production" is used herein to mean a detectable decrease in the amount of melanin synthesized by melanocytes exposed to the inhibitory compound compared to the amount of melanin synthesized under the extract of osmanthus fragrans. The term "reduction" as used herein with respect to melanin means to completely prevent, control secretion or to some extent reduce melanin formation. In one embodiment, the term "reduced" means that the amount of melanin synthesized thereby is reduced by from about 10% to about 100%. In one embodiment, the term "reduced" means that the amount of melanin synthesized is reduced by from about 25% to about 100%. In one embodiment, the term "reduced" means that the amount of melanin synthesized is reduced by from about 35% to about 100%. In one embodiment, the term "reduced" means that the amount of melanin synthesized is reduced by from about 40% to about 100%. The terms reduction, alleviation, reduction, suppression, and inhibition are intended to be used interchangeably when used with respect to melanin production. This reduction in melanin production can be assessed subjectively or by analysis using, for example, but not limited to, in vitro, ex vivo, animal models, and/or clinical models known to those skilled in the art. For example, methods known to those skilled in the art (including, but not limited to, human melanocyte culture, melanoma culture (see Example 3 below and U.S. Patent No. 7,189,419, the disclosure of which is incorporated herein by reference in entirety Incorporated herein, HRM2 hairless mouse model (see Chung et al. "Evaluation of in vitro and in vivo anti-melanogenic activity of a newly synthesized strong tyrosinase inhibitor (E)-3-(2,4 dihydroxybenzylidene) Pyrrolidine-2,5-dione(3-DBP),"Biochim Biophys Acta. July 2012; 1820(7): 962-9, the entire contents of which are hereby incorporated by reference for all purposes), Zebra Fish model (see Choi, TY; Kim, JH; Ko, DH; Kim, CH; Hwang, JS; Ahn, S.; Kim, SY; Kim, CD; Lee, JH; Yoon, TJZebrafish as a new model for phenotype -based screening of melanogenic regulatory compounds. Pigment Cell Res. 2007,20,120-127, in its entirety for all purposes begin incorporated herein by reference) and MelanoDerm TM skin model (the MatTek Corporation, Ashland, MA)) established melanoma The synthesis is reduced.

本文所用「預防(prevention)」以及相關術語(例如「預防」(「prevent」或「preventing」)係指為尚未受症狀侵襲之皮膚提供如下效益:用於避免、延遲、對抗、最小化或減少一或多個與欲預防之皮膚症狀有關之不期望特徵的復發/發作。該等預防效益包括(例如)延遲症狀之發育及/或復發、或降低一或多個與症狀(若其最終發育)有關之不期望特徵之持續時間、嚴重程度或強度。使用術語「預防」並不意欲暗指投與化妝品組合物之個體群體中之所有個體皆絕不會受化妝品或皮膚病學症狀、損害、效應或症候侵襲或發育該等病狀,而是個體群體將呈現化妝品或皮膚病學損害、效應或症候之減輕。舉例而言,許多流感疫苗在彼等投與疫苗者中進行預防時並非100%有效。 預防老化係指為尚未受侵襲之皮膚提供如下效益:用於避免、延遲、對抗或最小化一或多個與老化有關之不期望特徵,例如降低最終在所治療區域中形成之紋及皺紋、下垂、暗沉、變色、不均勻色調、粗糙 膚質及/或脆性之程度。 As used herein, "prevention" and related terms (such as "prevent" or "preventing") mean the following benefits for skin that has not been affected by symptoms: for avoiding, delaying, confronting, minimizing or reducing One or more recurrence/onset of undesired characteristics associated with skin symptoms to be prevented. Such prophylactic benefits include, for example, delaying the development and/or recurrence of symptoms, or reducing one or more symptoms (if their development is ultimately The duration, severity or intensity of the undesired characteristics associated with it. The use of the term "prevention" is not intended to imply that all individuals in the individual group of the cosmetic composition will never suffer from cosmetic or dermatological symptoms or damage. , effects or symptoms invade or develop such conditions, but the individual population will present a reduction in cosmetic or dermatological damage, effects or symptoms. For example, many influenza vaccines are not prevented when they are administered vaccines. 100% effective. Preventing aging means providing the unaffected skin with the benefit of avoiding, delaying, combating or minimizing one or more undesirable characteristics associated with aging, such as reducing the lines and wrinkles that ultimately form in the treated area, Drooping, dull, discolored, uneven tones, rough The extent of skin and/or fragility.

本文所用術語「皮膚」包括臉部、口、頸、胸、背、臂、手、腿及頭皮上或其中之皮膚。「薄皮膚」意欲包括由於年齡性老化、停經或光損害而變薄之皮膚。 The term "skin" as used herein includes skin on or in the face, mouth, neck, chest, back, arms, hands, legs and scalp. "Thin skin" is intended to include skin that is thinned by ageing, menopause or light damage.

如本文所用之「治療(treatment)」以及相關術語(例如「治療」(「treat」或「treating」)係指根除、減輕、改善或逆轉一或多個與所治療皮膚症狀有關之不期望特徵,以使消費者發覺皮膚外觀改善或關於症狀之其他治療效益。治療皮膚老化或損害係指根除、減輕、改善或逆轉一或多種與老化有關之不期望特徵。與老化皮膚有關之不期望特徵,例如,紋及皺紋、下垂、暗沉、不均勻色調、變色、粗糙膚質等。與變色有關之不期望特徵,例如,老人斑、雀斑、黃褐斑、黑斑、發炎後色素沉著過度等。治療效益包括(例如)減輕紋、皺紋及/或下垂之外觀、使皮膚恢復光澤、使皮膚色調均勻、使膚質軟化及/或使變色光亮。本發明組合物及方法適用於治療許多身體區域(包括但不限於臉部、前額、唇、頸、臂、手、腿、膝、足、胸、背部、腹股溝、臀部及諸如此類)中皮膚之皮膚病學症狀。在另一實施例中,將組合物施用至臉部。 As used herein, "treatment" and related terms (eg "treat" or "treating") refers to eradication, alleviation, amelioration or reversal of one or more undesirable characteristics associated with the skin condition being treated. To cause the consumer to notice an improvement in the appearance of the skin or other therapeutic benefit with regard to the symptoms. Treatment of skin aging or damage means eradicating, mitigating, ameliorating or reversing one or more undesirable characteristics associated with aging. Undesirable characteristics associated with aged skin For example, wrinkles and wrinkles, sagging, dullness, uneven hue, discoloration, rough skin, etc. Undesirable features associated with discoloration, such as age spots, freckles, melasma, dark spots, post-inflammatory hyperpigmentation The therapeutic benefits include, for example, reducing the appearance of wrinkles, wrinkles and/or sagging, restoring the skin, making the skin tone uniform, softening the skin and/or brightening the color. The compositions and methods of the present invention are suitable for treating many Body area (including but not limited to face, forehead, lips, neck, arms, hands, legs, knees, feet, chest, back, groin, buttocks, etc.) Dermatological symptoms of the skin. In another embodiment, the composition is applied to the face.

術語「皺紋」或「起皺」係指細皺紋及粗皺紋二者。細皺紋或細紋係指皮膚表面上之淺表紋及皺紋。粗皺紋係指深皺紋,特別是臉部上及眼周圍之深紋/皺紋,包括表情紋,例如皺眉紋及皺紋、前額紋及皺紋、魚尾紋及皺紋、法令及木偶紋及皺紋。前額紋及皺紋係指前額皮膚上之淺表紋及/或深皺紋。魚尾紋及皺紋係指眼區域周圍皮膚上之淺表紋及/或深皺紋。木偶紋及皺紋係指嘴周圍皮膚上之淺表紋及/或深皺紋。可針對紋之數目、長度及深度評定皺紋。 The term "wrinkle" or "wrinkle" refers to both fine wrinkles and coarse wrinkles. Fine wrinkles or fine lines refer to superficial lines and wrinkles on the surface of the skin. Rough wrinkles are deep wrinkles, especially deep lines/wrinkles on the face and around the eyes, including expression lines such as frown lines and wrinkles, forehead lines and wrinkles, crow's feet and wrinkles, ritual and puppet lines and wrinkles. Forehead lines and wrinkles refer to superficial lines and/or deep wrinkles on the forehead skin. Crow's feet and wrinkles refer to superficial and/or deep wrinkles on the skin surrounding the area of the eye. Puppet lines and wrinkles are shallow lines and/or deep wrinkles on the skin around the mouth. Wrinkles can be assessed for the number, length and depth of the lines.

除非另外指明,否則所有百分比皆係基於組合物之總重量。 All percentages are based on the total weight of the composition unless otherwise indicated.

化妝品組合物Cosmetic composition

本發明方法中所用之化妝品組合物包含源自山桂花植物之植物組份。山桂花植物可呈任何形式,包括(但不限於)整株植物、乾燥植物、磨碎的植物或其部分(包括,但不限於,種子、針葉、葉子、根、樹皮、球花、莖、根莖、癒傷組織細胞、原生質體、器官及器官系統及分生組織),或於植物及/或植物之部分中發現或分離的萃取物、乾燥萃取物、合成萃取物或組份及/或成份,或直接源自植物或自植物合成之萃取物,或其任何組合。在一個實施例中,本發明植物組份中所用之化妝品組合物係直接源自山桂花植物。該植物組份可呈純形式、半純形式或未純化形式。山桂花植物組份可呈液體、半固體或固體稠度形式。在一個實施例中,植物組份可為精油。 The cosmetic composition used in the method of the present invention comprises a plant component derived from a osmanthus plant. The osmanthus plant may be in any form including, but not limited to, whole plants, dried plants, ground plants or parts thereof (including, but not limited to, seeds, needles, leaves, roots, bark, spherules, stems , rhizomes, callus cells, protoplasts, organs and organ systems and meristems, or extracts, dried extracts, synthetic extracts or components found in or isolated from parts of plants and/or plants and/or Or ingredients, or extracts derived directly from plants or from plants, or any combination thereof. In one embodiment, the cosmetic composition used in the plant component of the invention is derived directly from the osmanthus plant. The plant component can be in pure form, semi-pure form or unpurified form. The osmanthus plant component can be in the form of a liquid, semi-solid or solid consistency. In one embodiment, the plant component can be an essential oil.

在一個實施例中,原材料係自山桂花植物之莖、葉及/或花收集,且在某些實施例中,原材料主要或僅自山桂花之花獲得。在某些實施例中,將收集自山桂花植物之原材料研磨成小粒徑。另外,原材料可經乾燥以減少水含量。原材料可經風乾,烘箱乾燥,在真空下旋轉蒸發,凍乾,或藉由業內已知之任何其他適宜方法乾燥。 In one embodiment, the raw material is collected from the stems, leaves, and/or flowers of the osmanthus plant, and in certain embodiments, the raw material is obtained primarily or exclusively from the flowers of the osmanthus flower. In certain embodiments, the raw materials collected from the osmanthus plants are ground to a small particle size. In addition, the raw materials can be dried to reduce the water content. The raw materials can be air dried, oven dried, rotary evaporated under vacuum, lyophilized, or dried by any other suitable method known in the art.

可藉由用剝除劑蒸餾原材料獲得山桂花萃取物。剝除劑可為與山桂花之期望萃取物混溶、不混溶或部分混溶之液體。適宜剝除劑包括(但不限於)以下:水;醇(例如甲醇、乙醇、丙醇、丁醇及諸如此類);二醇;醚(例如二乙醚、二丙醚及諸如此類);酯(例如乙酸丁酯、乙酸乙酯及諸如此類);酮(例如丙酮、乙基甲基酮及諸如此類);二甲亞碸;乙腈;其他有機溶劑;及其組合。在一個實施例中,剝除劑與山桂花之期望萃取物不混溶。山桂花萃取物可藉由自剝除劑相分離來收集。據信剝除劑會增加蒸餾系統之整體蒸氣壓用以獲得山桂花萃取物且藉此降低期望產物山桂花萃取物之沸點。 The osmanthus extract can be obtained by distilling the raw material with a stripping agent. The stripping agent can be a liquid that is miscible, immiscible or partially miscible with the desired extract of osmanthus. Suitable stripping agents include, but are not limited to, the following: water; alcohols (eg, methanol, ethanol, propanol, butanol, and the like); glycols; ethers (eg, diethyl ether, dipropyl ether, and the like); esters (eg, acetic acid) Butyl ester, ethyl acetate and the like; ketones (such as acetone, ethyl methyl ketone and the like); dimethyl hydrazine; acetonitrile; other organic solvents; In one embodiment, the stripper is immiscible with the desired extract of osmanthus. The osmanthus extract can be collected by phase separation from the stripper. It is believed that the stripping agent increases the overall vapor pressure of the distillation system to obtain the osmanthus extract and thereby lowers the boiling point of the desired product, the osmanthus extract.

在其他實施例中,山桂花植物組份可呈藉由溶劑萃取獲得、在一個實施例中藉由有機溶劑萃取獲得之萃取物形式。簡言之,有機溶 劑萃取方法涉及使用有機溶劑洗滌並萃取原材料,該等原材料可為整株或將其研磨成小粒徑。有機溶劑之非限制性實例包括甲醇、乙醇、異丙醇、二氯甲烷、氯仿、己烷、二甲苯及石油醚。可使用萃取機進行有機溶劑萃取,如業內所熟知。可藉由推進器將原材料緩慢推至萃取機中。可經由廢物排放出口之頂部處之溶劑入口向機器中添加有機溶劑(例如,乙醇)。由於重力及平衡差別,溶劑向前流至原材料入口,浸泡該等材料並自溶劑入口之相對側流出。由於植物材料及溶劑以彼此相對方向移動,故植物材料始終浸沒於含有低濃度萃取物之溶液中。由於平衡結果,可藉由以低濃度溶液連續萃取植物材料達成植物成份之高產率。 In other embodiments, the osmanthus plant component may be in the form of an extract obtained by solvent extraction, in one embodiment by organic solvent extraction. In short, organic dissolution The agent extraction method involves washing and extracting a raw material using an organic solvent, which may be a whole plant or ground to a small particle size. Non-limiting examples of organic solvents include methanol, ethanol, isopropanol, dichloromethane, chloroform, hexane, xylene, and petroleum ether. Organic solvent extraction can be performed using an extractor, as is well known in the art. The raw material can be slowly pushed into the extraction machine by the pusher. An organic solvent (eg, ethanol) can be added to the machine via a solvent inlet at the top of the waste discharge outlet. Due to gravity and equilibrium differences, the solvent flows forward to the raw material inlet, soaking the materials and flowing out from the opposite side of the solvent inlet. Since the plant material and the solvent move in opposite directions to each other, the plant material is always immersed in the solution containing the low concentration extract. Due to the equilibrium result, a high yield of plant ingredients can be achieved by continuously extracting plant material in a low concentration solution.

所用適於萃取山桂花植物成份之萃取時間通常介於約1-10小時,更經常在一個實施例中介於約2-8小時,且最經常在另一實施例中介於約3-6小時。萃取溫度介於約30℃至100℃,在一個實施例中介於約40℃至70℃,且更經常在一個實施例中介於約50℃至60℃。隨後將所收集萃取物微細過濾以移除碎片,且其可直接使用,或藉由(例如)蒸餾溶劑或藉由其他習用處理法進行濃縮。可在真空下旋轉蒸發萃取物活性物之溶液或進行冷凍乾燥。典型萃取物之活性物含量高於約25%,在一個實施例中其高於50%,且萃取物亦可呈精油或具有半固體或固體稠度之濃縮物形式提供。 The extraction time suitable for extracting the components of the osmanthus plant is typically between about 1-10 hours, more often between about 2-8 hours in one embodiment, and most often between about 3-6 hours in another embodiment. The extraction temperature is between about 30 ° C and 100 ° C, in one embodiment between about 40 ° C and 70 ° C, and more often between about 50 ° C and 60 ° C in one embodiment. The collected extract is then finely filtered to remove debris and it can be used directly or concentrated by, for example, distillation of the solvent or by other conventional treatments. The solution of the extract active can be rotated or vacuum dried under vacuum. Typical extracts have an active level of greater than about 25%, in one embodiment greater than 50%, and the extract may also be provided as an essential oil or as a concentrate having a semi-solid or solid consistency.

類似地,水性-有機溶劑萃取法涉及先自山桂花植物收集原材料,該等山桂花植物可為整株或將其研磨成小粒徑。端視期望萃取物在酸性或鹼性(鹼)條件下之溶解度及穩定性而定,將磨碎之植物材料浸泡於酸性或鹼性水溶液中。對於酸性條件下之萃取,向水中添加(例如)約3%(w/v)濃度之諸如鹽酸或硫酸等酸類。對於鹼性條件下之萃取,向水中添加諸如氫氧化鈉或碳酸鈉等鹼。萃取之萃取時間及溫度通常類似於上述有機溶劑萃取方法中所用者。 Similarly, aqueous-organic solvent extraction involves the collection of raw materials from the osmanthus plants, which may be whole plants or ground to small particle sizes. Depending on the solubility and stability of the desired extract under acidic or basic (base) conditions, the ground plant material is immersed in an acidic or basic aqueous solution. For extraction under acidic conditions, an acid such as hydrochloric acid or sulfuric acid is added to the water at a concentration of, for example, about 3% (w/v). For the extraction under alkaline conditions, a base such as sodium hydroxide or sodium carbonate is added to the water. The extraction time and temperature of the extraction are generally similar to those used in the above organic solvent extraction methods.

隨後收集萃取物並精細過濾以移除碎片。端視所收集萃取物之酸性或鹼性而定,可向萃取物中添加鹼性劑(例如,氨)或酸化劑(例如,硫酸)以藉由調節pH中和該溶液。水性萃取物可直接使用、呈濃縮或乾燥形式使用。或者,隨後可向中和溶液中添加有機溶劑,以將萃取物自水相轉移至有機相。該等有機溶劑之實例包括(但不限於)乙醇、異丙醇、丁醇、戊醇、己醇及二甲苯。包含溶解於有機溶劑中之轉移萃取物活性物的萃取物可直接呈精油或濃縮物形式使用,或藉由若干不同方式乾燥,例如風乾、烘箱乾燥、在真空下旋轉蒸發或凍乾成半固體或固體稠度。 The extract was then collected and finely filtered to remove debris. Depending on the acidity or basicity of the collected extract, an alkaline agent (for example, ammonia) or an acidulant (for example, sulfuric acid) may be added to the extract to neutralize the solution by adjusting the pH. The aqueous extract can be used directly, in concentrated or dried form. Alternatively, an organic solvent can then be added to the neutralizing solution to transfer the extract from the aqueous phase to the organic phase. Examples of such organic solvents include, but are not limited to, ethanol, isopropanol, butanol, pentanol, hexanol, and xylene. The extract comprising the transfer extract active dissolved in an organic solvent can be used directly in the form of an essential oil or concentrate, or dried by several different means, such as air drying, oven drying, rotary evaporation under vacuum or lyophilization to a semisolid. Or solid consistency.

亦應注意,含有不同成份之不同植物可與山桂花混合並萃取在一起。在一個實施例中,混合萃取之此過程用於萃取彼等含有與山桂花於用於萃取之溶劑(例如乙醇)中之溶解度類似之成份的植物。可在適當溶劑中濃縮並儲存萃取物之混合物。 It should also be noted that different plants containing different ingredients can be mixed and extracted with osmanthus. In one embodiment, the process of mixed extraction is used to extract plants which contain ingredients similar to those of osmanthus fragrans in a solvent for extraction (e.g., ethanol). The mixture of extracts can be concentrated and stored in a suitable solvent.

在另一實施例中,如本文所用山桂花萃取物亦包括「合成」萃取物,即已知山桂花植物組份及/或成份之各種組合,其經組合以實質上模擬天然來源之山桂花植物萃取物之組成及/或活性。在一個實施例中,合成萃取物與天然山桂花植物材料具有實質上相同數目之活性組份。合成萃取物與天然山桂花植物材料間之以數值表示之活性物的一致性亦可在「共同性百分比」方面加以描述。合成萃取物與植物或天然萃取物之化學組成具有約50%或更大共同性。換言之,合成萃取物具有植物或天然萃取物中發現之活性成份的約50%或更多。在一個實施例中,合成萃取物之化學組成與植物或天然萃取物之化學組成具有約70%或更大共同性。最佳地,合成萃取物與植物或天然萃取物之化學組成具有約90%或更大共同性。 In another embodiment, the osmanthus extract used herein also includes a "synthetic" extract, i.e., various combinations of known osmanthus plant components and/or ingredients that are combined to substantially mimic the natural source of osmanthus Composition and/or activity of plant extracts. In one embodiment, the synthetic extract has substantially the same number of active components as the native osmanthus plant material. The consistency of the active substance between the synthetic extract and the natural osmanthus plant material can also be described in terms of "common percentage". The synthetic extract has a chemical composition of about 50% or greater with the chemical composition of the plant or natural extract. In other words, the synthetic extract has about 50% or more of the active ingredient found in the plant or natural extract. In one embodiment, the chemical composition of the synthetic extract has a commonality of about 70% or greater with the chemical composition of the plant or natural extract. Most preferably, the synthetic extract has a chemical composition of about 90% or greater with the chemical composition of the plant or natural extract.

本發明之組合物可以多種形式調配用於局部施用且將包含約0.0001重量%至約90重量%山桂花萃取物,且在一個實施例中將包含 約0.0005重量%至約25重量%,在一個實施例中約0.001重量%至約10重量%。在更佳範圍內,該組合物可包含佔總組合物介於約0.005重量%、0.01重量%、0.05重量%、0.1重量%、0.25重量%、0.5重量%、0.75重量%或1重量%高達5重量%、7.5重量%或10重量%範圍內之山桂花萃取物。組合物將包含有效量之山桂花萃取物,此意指在給定皮膚區域中局部施加時足以減輕及/或抑制該區域中之老化或損害之體徵之外觀的量。上述量係指山桂花萃取物之「活性量」。 The compositions of the present invention may be formulated for topical application in a variety of forms and will comprise from about 0.0001% to about 90% by weight of the osmanthus extract, and in one embodiment will comprise From about 0.0005 wt% to about 25 wt%, in one embodiment from about 0.001 wt% to about 10 wt%. In a more preferred range, the composition may comprise between about 0.005%, 0.01%, 0.05%, 0.1%, 0.25%, 0.5%, 0.75%, or 1% by weight of the total composition. Osmanthus fragrans extract in the range of 5% by weight, 7.5% by weight or 10% by weight. The composition will comprise an effective amount of osmanthus extract, which means an amount sufficient to reduce and/or inhibit the appearance of signs of aging or damage in the area when applied topically in a given area of the skin. The above amount refers to the "activity amount" of the extract of Osmanthus fragrans.

根據本發明,包含山桂花植物之組份之組合物包括(但不限於)局部施用調配物、抗氧化劑、抗發炎劑、防曬劑、化妝品(包括裝扮品)、個人護理產品(例如,止汗劑或用於控制體臭之除臭劑)、外敷劑、皮膚促滲劑及諸如此類。亦根據本發明,包含山桂花植物組份及額外成份之該等組合物可以多種產品形式調配。組合物可在靶遞送系統(例如乳霜、洗劑、凝膠、調色劑、漿液、經皮貼片及諸如此類)製備,尤其用於局部投與。亦可藉由電離子透入法達成靶遞送及/或滲透增強。 According to the present invention, compositions comprising components of osmanthus plants include, but are not limited to, topical formulations, antioxidants, anti-inflammatory agents, sunscreens, cosmetics (including dressings), personal care products (eg, antiperspirant) Agent or deodorant for controlling body odor), external application agent, skin penetration enhancer and the like. Also in accordance with the present invention, such compositions comprising osmanthus plant components and additional ingredients can be formulated in a variety of product forms. The compositions can be prepared in a target delivery system (e.g., creams, lotions, gels, toners, serums, transdermal patches, and the like), especially for topical administration. Target delivery and/or penetration enhancement can also be achieved by iontophoresis.

本發明進一步提供包含山桂花植物組份之組合物,其在一個實施例中用於本發明方法以局部投與用於靶遞送。本發明方法適於所有皮膚類型,例如敏感性、正常、油性或組合皮膚。在特定實施例中,在一個實施例中,可將組合物施用至敏感性皮膚或毛髮類型。將組合物施用至皮膚或毛髮達足以改善皮膚相關性症狀(包括與老化有關之不期望特徵,例如,紋及皺紋、下垂、暗沉、不均勻色調、變色、粗糙膚質等)之美觀的時間段。組合物可每日局部施用一次、兩次或更多次,且在一個實施例中每天一次。每日施用可施用1週、2週、4週或更長之時段。 The invention further provides compositions comprising a plant component of osmanthus fragrans, which in one embodiment are used in the methods of the invention for topical administration for target delivery. The method of the invention is suitable for all skin types, such as sensitive, normal, oily or combination skin. In a particular embodiment, in one embodiment, the composition can be applied to a sensitive skin or hair type. Applying the composition to the skin or hair for aesthetics sufficient to improve skin-related symptoms, including undesirable features associated with aging, such as wrinkles, wrinkles, sagging, dullness, uneven hue, discoloration, rough skin, and the like period. The composition can be administered topically, once or twice daily, and once per day in one embodiment. Daily administration can be administered for a period of 1 week, 2 weeks, 4 weeks or longer.

可將組合物調配成脂質體,該等脂質體可包含其他添加劑或物質,及/或其可經改質以在投與後更特定地到達或保留於位點處。本 發明組合物可藉由治療至少一個皮膚老化或損害相關性不期望特徵改善美觀。 The compositions may be formulated as liposomes, which may contain other additives or substances, and/or which may be modified to more specifically arrive or remain at the site after administration. this The compositions of the present invention can improve aesthetics by treating at least one skin aging or damaging undesirable undesirable characteristics.

本發明方法之另一實施例涵蓋包含化妝品或皮膚病學上可接受之調配物的組合物,該調配物適於接觸活的動物組織(包括人類組織),而對使用者無實質上不利之生理效應。本發明涵蓋之組合物可以任何化妝品及/或皮膚病學適宜形式(在一個實施例中,例如洗劑或乳霜)、而且亦於無水或水性基質中以及以可噴霧液體形式提供。本發明中所用組合物之其他適宜化妝產品形式包括(例如)乳液、乳霜、香膏、上光膏、洗劑、面膜、漿液、調色劑、軟膏、摩絲、貼片、潤髮油、溶液、噴霧、蠟基棒或濕紙巾。在一個實施例中,組合物並非面膜。另外,組合物可包括熟習此項技術者常用且已知之一或多種相容之化妝品上可接受之佐劑,例如著色劑、芳香劑、潤膚劑、潤濕劑、防腐劑、維他命、螯合劑、增稠劑、紫蘇油或紫蘇籽油(WO 01/66067,「Method of Treating a Skin Condition」,出於所有目的其全部內容併入本文中)及諸如此類,以及其他植物藥,例如蘆薈、春黃菊及諸如此類,且如下文所進一步闡述。 Another embodiment of the method of the invention encompasses a composition comprising a cosmetically or dermatologically acceptable formulation adapted to contact live animal tissue, including human tissue, without substantial disadvantage to the user. Physiological effects. The compositions encompassed by the present invention may be provided in any cosmetically and/or dermatologically suitable form (in one embodiment, such as a lotion or cream), but also in an anhydrous or aqueous base, and in the form of a sprayable liquid. Other suitable cosmetic product forms of the compositions used in the present invention include, for example, lotions, creams, balms, glazes, lotions, masks, serums, toners, ointments, mousses, patches, pomades , solution, spray, wax-based sticks or wet wipes. In one embodiment, the composition is not a mask. Additionally, the compositions may include one or more compatible cosmetically acceptable adjuvants commonly used by those skilled in the art, such as coloring agents, fragrances, emollients, wetting agents, preservatives, vitamins, chelating agents. Mixtures, thickeners, perilla oil or perilla seed oil (WO 01/66067, "Method of Treating a Skin Condition", all of which is incorporated herein for all purposes) and the like, as well as other botanicals, such as aloe vera, Chamomile and the like, and as further explained below.

本發明亦涵蓋經皮遞送模式,例如貼片及諸如此類,其具有或無適宜促滲劑。由本發明實施之方法及提供可在經皮系統中有效地投與山桂花組份之方式。因此,向皮膚遞送組合物或調配物(經常具有滲透增強組合物)之經皮方式係經皮貼片或如業內已知且闡述之類似裝置。經皮貼片經設計以橫跨使用者之皮膚遞送有效量之化合物。經皮貼片通常涉及其中可納入山桂花萃取物之液體、凝膠、固體基質或壓感黏著載劑。貼片調配物及製劑已為業內所熟知。參見(例如)「Dermatological and Transdermal Formulations」(Drugs and the Pharmaceutical Sciences,第119卷),Kenneth A Walters(編輯),Marcel Dekker及「Transdermal Drug Delivery」(Drugs & the Pharmaceutical Sciences),Richard H.Guy(編輯),Jonathan Hadgraft(編輯),原版第2修訂版,Marcel Dekker及「Mechanisms of Transdermal Drug Delivery」(Drugs & the Pharmaceutical Sciences,第83卷),由Russell O.Potts及Richard H.Guy編輯(1997)。該等裝置之實例揭示於美國專利第5,146,846號、第5,223,262號、第4,820,724號、第4,379,454號及第4,956,171號;及美國專利公開案第US20110300198號中,所有該等案件之全部內容皆以引用方式併入本文中且該等說明並不意欲具有限制性。儲存及遞送組合物至皮膚(包括毛髮)上及形成活性組合物之經皮模式係方便的且充分適於本發明之實施例之目的。在另一方法中,經由持續釋放媒劑、載劑或稀釋劑(例如局部施用持續釋放貼片)進行施用。在一個實施例中,在使用局部貼片時,將貼片施用至期望區域達延長時間段。在一個實施例中,延長時間段大於1小時,在一個實施例中,延長時間段係過夜,即,在使用者睡眠時。另外,經皮貼片可經調配以提供延長效益約1-7天之時段,在一個實施例中約2至7天,且在一個實施例中約3-7天。該等延長佩戴貼片可尤其充分適於治療、改善及/或預防變色。此外,由於許多使皮膚色素沉著/顏色光亮之化合物係UV敏感性,故可使用經皮貼片允許以在佩戴者暴露於日光時繼續治療,藉此為佩戴者提供更大自由。在該等情況下,在一個實施例中,經皮貼片之外部係肉色的,且在一個實施例中,貼片應緊密匹配佩戴者之皮膚顏色以提供謹慎治療。 The invention also encompasses transdermal delivery modes, such as patches and the like, with or without a suitable penetration enhancer. The method of the present invention and the manner in which the osmanthus component can be effectively administered in a transdermal system. Thus, transdermal means of delivering a composition or formulation to a skin (often having a penetration enhancing composition) is a transdermal patch or a similar device as is known and described in the art. Transdermal patches are designed to deliver an effective amount of the compound across the skin of the user. Transdermal patches typically involve a liquid, gel, solid matrix or pressure sensitive adhesive carrier into which the osmanthus extract can be incorporated. Patch formulations and formulations are well known in the art. See, for example, "Dermatological and Transdermal Formulations" (Drugs and the Pharmaceutical Sciences, vol. 119), Kenneth A Walters (editor), Marcel Dekker, and "Transdermal Drug Delivery" (Drugs & the Pharmaceutical Sciences), Richard H. Guy (ed.), Jonathan Hadgraft (editor), original revision 2, Marcel Dekker and "Mechanisms of Transdermal Drug Delivery" (Drugs & the Pharmaceutical Sciences, Volume 83), by Russell O. Edited by Potts and Richard H. Guy (1997). Examples of such devices are disclosed in U.S. Patent Nos. 5,146,846, 5,223,262, 4,820, 724, 4, 379, 454, and 4, 956, 171, and U.S. Patent Publication No. US Pat. This description is incorporated herein by reference. The transdermal mode of storing and delivering the composition onto the skin (including hair) and forming the active composition is convenient and well suited for the purposes of the examples of the present invention. In another method, administration is via a sustained release vehicle, vehicle or diluent (eg, topical sustained release patch). In one embodiment, when a topical patch is used, the patch is applied to the desired area for an extended period of time. In one embodiment, the extended period of time is greater than one hour, and in one embodiment, the extended period of time is overnight, ie, while the user is asleep. Additionally, the transdermal patch can be formulated to provide a prolonged benefit for a period of about 1-7 days, in one embodiment about 2 to 7 days, and in one embodiment about 3-7 days. Such extended wear patches may be particularly well suited for treating, ameliorating and/or preventing discoloration. In addition, because many compounds that make skin pigmentation/color brightening are UV sensitive, transdermal patches can be used to allow continued treatment while the wearer is exposed to sunlight, thereby providing greater freedom to the wearer. In such cases, in one embodiment, the exterior of the transdermal patch is flesh-colored, and in one embodiment, the patch should closely match the skin color of the wearer to provide discreet treatment.

局部組合物可包括一或多種化妝品上可接受之媒劑。該等媒劑可採取業內已知適於施用至皮膚之任何形式且可包括水(例如,去離子水);植物油;礦物質油;酯,例如棕櫚酸辛酯、肉豆蔻酸異丙酯及棕櫚酸異丙酯;醚,例如二辛醚及二甲基異山梨糖醇;醇,例如乙醇及異丙醇;脂肪醇,例如十六烷醇、鯨蠟硬脂醇、硬脂醇及聯苯 醇;異鏈烷烴,例如異辛烷、異十二烷及異十六烷;聚矽氧油,例如環甲聚矽氧烷、二甲聚矽氧烷、二甲聚矽氧烷交聯聚合物、聚矽氧烷及其衍生物,在一個實施例中有機改質衍生物;烴油,例如礦物質油、礦脂、異二十烷及聚異丁烯;多元醇,例如丙二醇、甘油、丁二醇、戊二醇及己二醇;蠟,例如蜂蠟及植物蠟;或上述之任何組合或混合物。 The topical composition can include one or more cosmetically acceptable vehicles. The vehicles may take any form known in the art to be suitable for application to the skin and may include water (eg, deionized water); vegetable oils; mineral oils; esters such as octyl palmitate, isopropyl myristate and palm. Isopropyl acrylate; ethers such as dioctyl ether and dimethyl isosorbide; alcohols such as ethanol and isopropanol; fatty alcohols such as cetyl alcohol, cetearyl alcohol, stearyl alcohol and biphenyl Alcohol; isoparaffin, such as isooctane, isododecane and isohexadecane; polyfluorene oxide, such as cyclomethicone, dimethylpolyoxane, dimethicone cross-polymerization , polyoxyalkylene and derivatives thereof, in one embodiment organically modified derivatives; hydrocarbon oils, such as mineral oils, petrolatum, isodecane and polyisobutylene; polyols such as propylene glycol, glycerin, butyl Glycols, pentanediols and hexanediols; waxes, such as beeswax and vegetable waxes; or any combination or mixture of the foregoing.

媒劑可包含水相、油相、醇、聚矽氧相或其混合物。化妝品上可接受之媒劑亦可包含乳液。適宜乳液之非限制性實例包括油包水乳液、水包油乳液、水包聚矽氧乳液、聚矽氧包水乳液、水包蠟乳液、水-油-水三重乳液或具有乳霜、凝膠或微乳液外觀之類似物。該乳液可包括乳化劑,例如非離子型、陰離子型或兩性表面活性劑。 The vehicle may comprise an aqueous phase, an oil phase, an alcohol, a polyoxo phase or a mixture thereof. Cosmetically acceptable vehicles may also contain an emulsion. Non-limiting examples of suitable emulsions include water-in-oil emulsions, oil-in-water emulsions, water-in-oil emulsions, water-in-water emulsions, water-in-wax emulsions, water-oil-water triple emulsions or creams, condensation An analog of the appearance of a gel or microemulsion. The emulsion may include an emulsifier such as a nonionic, anionic or amphoteric surfactant.

在一個實施例中,乳液之油相具有一或多種有機化合物,包括潤膚劑;潤濕劑(例如丁二醇、丙二醇、甲基葡糖醇聚醚-20及甘油);其他水可分散或水溶性組份,包括增稠劑,例如矽酸鎂鋁(veegum)或羥基烷基纖維素;膠凝劑,例如高MW聚丙烯酸,即CARBOPOL 934;及其混合物。乳液可具有能夠乳化組合物中存在之各種組份的一或多種乳化劑。 In one embodiment, the oil phase of the emulsion has one or more organic compounds, including emollients; wetting agents (eg, butylene glycol, propylene glycol, methyl glucosamine-20, and glycerin); other waters are dispersible Or a water soluble component, including a thickening agent, such as veegum or hydroxyalkyl cellulose; a gelling agent, such as high MW polyacrylic acid, namely CARBOPOL 934; and mixtures thereof. The emulsion may have one or more emulsifiers capable of emulsifying the various components present in the composition.

適用於油相中之化合物包括(但不限於)植物油;酯,例如棕櫚酸辛酯、肉豆蔻酸異丙酯及棕櫚酸異丙酯;醚,例如二辛基醚;脂肪醇,例如十六烷醇、硬脂醇及山萮醇;異鏈烷烴,例如異辛烷、異十二烷及異十六烷;聚矽氧油,例如二甲聚矽氧烷、環狀聚矽氧及聚矽氧烷;烴油,例如礦物質油、礦脂、異二十烷及聚異丁烯;天然或合成蠟;及諸如此類。適宜疏水性烴油可為飽和或不飽和的,具有脂肪族特徵且為直鏈或具支鏈或含有脂環族或芳香族環。含油相可由單一油或不同油之混合物構成。 Suitable compounds for use in the oil phase include, but are not limited to, vegetable oils; esters such as octyl palmitate, isopropyl myristate and isopropyl palmitate; ethers such as dioctyl ether; fatty alcohols such as hexadecane Alcohols, stearyl alcohols and behenyl alcohols; isoparaffins such as isooctane, isododecane and isohexadecane; polyoxygenated oils such as dimethylpolyoxane, cyclic polyoxane and polyfluorene Oxane; hydrocarbon oils such as mineral oils, petrolatum, isoicosane and polyisobutylene; natural or synthetic waxes; and the like. Suitable hydrophobic hydrocarbon oils may be saturated or unsaturated, have aliphatic character and are linear or branched or contain alicyclic or aromatic rings. The oil-containing phase may consist of a single oil or a mixture of different oils.

烴油包括彼等具有6-20個碳原子、在一個實施例中10-16個碳原 子者。代表性烴包括癸烷、十二烷、十四烷、十三烷及C8-20異鏈烷烴。鏈烷烴可以商標ISOPARS自Exxon購得並可自Permethyl公司購得。另外,預期C8-20鏈烷烴(例如Permethyl公司製造之商品名Permethyl 99ATM之C12異烷烴(異十二烷))亦適宜。諸如異十六烷(商品名為Permethyl®)等多種市售C16異鏈烷烴亦適宜。較佳揮發性烴之實例包括聚癸烷,例如,異十二烷及異癸烷,其包括(例如)Permethyl-99A(Presperse公司)及C7-C8至C12-C15異鏈烷烴,例如,可自Exxon Chemicals購得之Isopar系列。代表性烴溶劑係異十二烷。 Hydrocarbon oils include those having from 6 to 20 carbon atoms, and in one embodiment from 10 to 16 carbon atoms. Representative hydrocarbons include decane, dodecane, tetradecane, tridecane, and C8-20 isoparaffins. Paraffins are commercially available from Exxon under the trademark ISOPARS and are commercially available from Permethyl Corporation. Further, a C 8-20 paraffin (for example, a C 12 isoalkane (isododecane) manufactured by Permethyl Corporation under the trade name Permethyl 99A TM ) is also suitable. Such as isohexadecane (trade name Permethyl®) and other commercially available C 16 isoparaffins are also suitable. Examples of preferred volatile hydrocarbons include polydecane, for example, isododecane and isodecane, which include, for example, Permethyl-99A (Presperse) and C 7 -C 8 to C 12 -C 15 isoparaffins. For example, the Isopar series available from Exxon Chemicals. A representative hydrocarbon solvent is isododecane.

油相可包含一或多種蠟,其包括(例如)米糠蠟、巴西棕櫚蠟、小冠椰子蠟、堪地里拉蠟(candelilla wax)、褐煤蠟、甘蔗蠟、地蠟、聚乙烯蠟、Fischer-Tropsch蠟、蜂蠟、微晶蠟、聚矽氧蠟、氟化蠟及其任一組合。 The oil phase may comprise one or more waxes including, for example, rice bran wax, carnauba wax, small crown coconut wax, candelilla wax, montan wax, sugar cane wax, ozokerite wax, polyethylene wax, Fischer- Tropsch wax, beeswax, microcrystalline wax, polyoxynized wax, fluorinated wax, and any combination thereof.

非限制性乳化劑包括乳化蠟、乳化多羥基醇、聚醚多元醇、聚醚、多元醇之單酯或二酯、乙二醇單硬脂酸酯、甘油單硬脂酸酯、甘油二硬脂酸酯、含有聚矽氧之乳化劑、大豆固醇、脂肪醇(例如十六烷醇)、丙烯酸酯、脂肪酸(例如硬脂酸)、脂肪酸鹽及其混合物。較佳乳化劑包括大豆固醇、十六烷醇、硬脂酸、乳化蠟、丙烯酸酯、含有聚矽氧之乳化劑及其混合物。可用於本發明組合物中之其他具體乳化劑包括(但不限於)以下中之一或多者(僅列舉幾個例子):丙烯酸C10-30烷基酯交聯聚合物;二甲聚矽氧烷PEG-7異硬脂酸酯、丙烯醯胺共聚物;礦物質油;山梨醇酐酯;聚甘油-3-二異硬脂酸酯;山梨醇酐單硬脂酸酯、山梨醇酐三硬脂酸酯、山梨醇酐倍半油酸酯、山梨醇酐單油酸酯;丙三醇酯,例如丙三醇單硬脂酸酯及丙三醇單油酸酯;聚氧乙烯酚,例如聚氧乙烯辛基酚及聚氧乙烯壬基酚;聚氧乙烯醚,例如聚氧乙烯十六烷基醚及聚氧乙烯硬脂基醚;聚氧乙烯二醇酯;聚氧乙烯山梨醇酐酯;二甲聚矽氧烷共聚醇;聚甘油酯,例如聚甘油-3-二 異硬脂酸酯;月桂酸甘油酯;硬脂醇聚氧乙烯醚-2、硬脂醇聚氧乙烯醚-10及硬脂醇聚氧乙烯醚-20。額外乳化劑係提供於INCI成份詞典及手冊,第11版,2006中,其揭示內容以引用方式併入本文中。 Non-limiting emulsifiers include emulsifying waxes, emulsified polyhydric alcohols, polyether polyols, polyethers, monoesters or diesters of polyhydric alcohols, ethylene glycol monostearate, glyceryl monostearate, glycerol Fatty acid esters, emulsifiers containing polyoxyxides, soy sterols, fatty alcohols (e.g., cetyl alcohol), acrylates, fatty acids (e.g., stearic acid), fatty acid salts, and mixtures thereof. Preferred emulsifiers include soy sterol, cetyl alcohol, stearic acid, emulsifying wax, acrylate, polyoxymethane-containing emulsifier, and mixtures thereof. Other specific emulsifiers useful in the compositions of the present invention include, but are not limited to, one or more of the following (to name a few): C 10-30 alkyl acrylate crosspolymer; dimethyl fluorene Oxylkane PEG-7 isostearate, acrylamide copolymer; mineral oil; sorbitan ester; polyglyceryl-3-diisostearate; sorbitan monostearate, sorbitan Tristearate, sorbitan sesquioleate, sorbitan monooleate; glycerol esters, such as glycerol monostearate and glycerol monooleate; polyoxyethylene phenol For example, polyoxyethylene octylphenol and polyoxyethylene nonylphenol; polyoxyethylene ethers such as polyoxyethylene cetyl ether and polyoxyethylene stearyl ether; polyoxyethylene glycol ester; polyoxyethylene sorbitol Alkyd ester; dimethoxane copolyol; polyglycerol ester, such as polyglyceryl-3-diisostearate; lauric acid glyceride; stearyl polyoxyethylene ether-2, stearyl alcohol Vinyl ether-10 and stearyl polyoxyethylene ether-20. Additional emulsifiers are provided in the INCI Ingredient Dictionary and Handbook, 11th Edition, 2006, the disclosure of which is incorporated herein by reference.

該等乳化劑通常可以約0.001重量%至約10重量%之量、在一個實施例中約0.01重量%至約5重量%、在一個實施例中約0.1重量%至約3重量%之量存在於組合物中。 The emulsifiers may generally be present in an amount from about 0.001% to about 10% by weight, in one embodiment from about 0.01% to about 5% by weight, and in one embodiment from about 0.1% to about 3% by weight. In the composition.

油相可包含一或多種揮發性及/或不揮發性聚矽氧油。揮發性聚矽氧包括環狀及直鏈揮發性二甲基矽氧烷聚矽氧。在一個實施例中,揮發性聚矽氧可包括環二甲聚矽氧烷,其包括四聚物(D4)、五聚物(D5)及六聚物(D6)環甲基聚矽氧烷或其混合物。尤其可提及揮發性環甲聚矽氧烷-六甲基環三矽氧烷、八甲基-環四矽氧烷及十甲基-環五矽氧烷。適宜二甲聚矽氧烷係以名稱Dow Corning 200® Fluid自Dow Corning購得且具有介於0.65至600,000厘斯托克斯範圍內或更高之黏度。適宜的非極性揮發性液體聚矽氧油揭示於美國專利第4,781,917號中,該案件之全文以引用方式併入本文中。其他揮發性聚矽氧材料闡述於Todd等人,「Volatile Silicone Fluids for Cosmetics」,Cosmetics and Toiletries,91:27-32(1976)中,該文件之全文以引用方式併入本文中。直鏈揮發性聚矽氧在25℃下通常具有小於約5厘斯托克斯之黏度,而環狀聚矽氧在25℃下具有小於約10厘斯托克斯之黏度。各種黏度之揮發性聚矽氧的實例包括Dow Corning 200、Dow Corning 244、Dow Corning 245、Dow Corning 344及Dow Corning 345(Dow Corning公司);SF-1204及SF-1202 Silicone Fluids(G.E.Silicones)、GE 7207及7158(General Electric公司);及SWS-03314(SWS Silicones公司)。直鏈揮發性聚矽氧包括低分子量聚二甲基矽氧烷化合物,例如(僅列舉幾個例子)六甲基二矽氧烷、八甲基三矽氧烷、十甲基四矽氧烷及十二甲基五矽氧烷。 The oil phase may comprise one or more volatile and/or non-volatile polyoxyphthalic oils. Volatile polyfluorene oxides include cyclic and linear volatile dimethyl oxa oxide polyoxyl. In one embodiment, the volatile polyoxo can include a cyclomethicone comprising tetramer (D 4 ), pentamer (D 5 ), and hexamer (D 6 ) cyclomethine A siloxane or a mixture thereof. Mention may in particular be made of the volatile cyclomethicone-hexamethylcyclotrioxane, octamethyl-cyclotetraoxane and decamethyl-cyclopentaoxane. Suitable dimethoxane is commercially available from Dow Corning under the name Dow Corning 200® Fluid and has a viscosity in the range of from 0.65 to 600,000 centistokes or higher. Suitable non-polar, volatile liquid polyoxyxides are disclosed in U.S. Patent No. 4,781,917, the disclosure of which is incorporated herein in its entirety by reference. Other volatile polyoxo materials are described in Todd et al., "Volatile Silicone Fluids for Cosmetics", Cosmetics and Toiletries, 91: 27-32 (1976), the entire disclosure of which is incorporated herein by reference. Linear volatile polyoxyxene typically has a viscosity of less than about 5 centistokes at 25 °C, while cyclic polyfluorene has a viscosity of less than about 10 centistokes at 25 °C. Examples of volatile polyoxins of various viscosities include Dow Corning 200, Dow Corning 244, Dow Corning 245, Dow Corning 344, and Dow Corning 345 (Dow Corning); SF-1204 and SF-1202 Silicone Fluids (GE Silicones), GE 7207 and 7158 (General Electric); and SWS-03314 (SWS Silicones). Linear volatile polyoxymethylene includes low molecular weight polydimethyl methoxy hydride compounds, for example (only a few examples) hexamethyldioxane, octamethyltrioxane, decamethyltetraoxane And dodecamethylpentaoxane.

不揮發性聚矽氧油通常會包含聚烷基矽氧烷、聚芳基矽氧烷、聚烷基芳基矽氧烷或其混合物。聚二甲基矽氧烷係較佳不揮發性聚矽氧油。不揮發性聚矽氧油在25℃下之黏度通常可為約10厘斯托克斯至約60,000厘斯托克斯,在一個實施例中介於約10厘斯托克斯與約10,000厘斯托克斯之間,且仍更佳介於約10厘斯托克斯與約500厘斯托克斯之間;且在大氣壓下具有高於250℃之沸點。非限制性實例包括二甲基聚矽氧烷(二甲聚矽氧烷)、苯基三甲聚矽氧烷及二苯基二甲聚矽氧烷。揮發性及不揮發性聚矽氧油可視情況經各種官能基(例如,僅列舉幾個例子)烷基、芳基、胺基、乙烯基、羥基、鹵代烷基、烷基芳基及丙烯酸酯基團)取代。 Non-volatile polyoxyxides typically comprise a polyalkyl siloxane, a polyaryl siloxane, a polyalkylaryl oxane or a mixture thereof. Polydimethylsiloxane is preferably a non-volatile polyoxyxene oil. The viscosity of the non-volatile polyoxyxene oil at 25 ° C can generally range from about 10 PCT Stokes to about 60,000 PCT Stokes, and in one embodiment between about 10 PCT Stokes and about 10,000 cc. Between the toxes, and still more preferably between about 10 centistokes and about 500 centistokes; and having a boiling point above 250 °C at atmospheric pressure. Non-limiting examples include dimethyl polyoxyalkylene (dimethyl polyoxyalkylene), phenyl trimethyl polyoxyalkylene, and diphenyl dimethyl polyoxyalkylene. Volatile and non-volatile polyoxyxides may optionally be subjected to various functional groups (for example, to name a few) alkyl, aryl, amine, vinyl, hydroxy, haloalkyl, alkylaryl and acrylate groups. Replaced by the regiment).

可利用非離子型表面活性劑(乳化劑)(例如,聚二有機矽氧烷-聚氧基伸烷基嵌段共聚物,包括彼等闡述於美國專利第4,122,029號中者,該揭示內容以引用方式併入本文中)乳化聚矽氧包水乳液。該等乳化劑通常包含具有包含-(EO)m-及/或-(PO)n-基團之側鏈之聚二有機矽氧烷骨架,通常聚二甲基矽氧烷,其中EO係伸乙氧基且PO係1,2-伸丙氧基,側鏈通常經氫或低碳數烷基(例如,C1-6,通常為C1-3)封端或終止。其他適宜聚矽氧包水乳化劑揭示於美國專利第6,685,952號中,該案件之揭示內容以引用方式併入本文中。市售聚矽氧包水乳化劑包括彼等可以商標名3225C及5225C FORMULATION AID自Dow Corning購得者、自General Electric購得之SILICONE SF-1528、自Goldschmidt Chemical公司(Hopewell,Va.)購得之ABIL EM 90及EM 97及由OSI Specialties(Danbury,Conn.)出售之SILWET系列乳化劑。 Nonionic surfactants (emulsifiers) may be utilized (e.g., polydiorganotoxioxane-polyoxyalkylene alkyl block copolymers, including those described in U.S. Patent No. 4,122,029, the disclosure of which is incorporated herein by reference. The manner of incorporation herein is an emulsified polyoxynionic water-in-water emulsion. The emulsifiers generally comprise a polydiorganotoxioxane skeleton having a side chain comprising -(EO)m- and/or -(PO)n- groups, typically polydimethyloxane, wherein the EO stretching Ethoxy and PO are 1,2-propenoxy, and the side chain is typically terminated or terminated by hydrogen or a lower alkyl group (e.g., C1-6 , typically C1-3 ). Other suitable polyoxynium emulsifiable emulsifiers are disclosed in U.S. Patent No. 6,685,952, the disclosure of which is incorporated herein by reference. Commercially available polyoxynized water emulsifiers include those available from Dow Corning under the trade names 3225C and 5225C FORMULATION AID, SILICONE SF-1528 available from General Electric, and from Goldschmidt Chemical Company (Hopewell, Va.). ABIL EM 90 and EM 97 and SILWET series emulsifiers sold by OSI Specialties (Danbury, Conn.).

聚矽氧包水乳化劑之實例包括(但不限於)二甲聚矽氧烷PEG 10/15交聯聚合物、二甲聚矽氧烷共聚醇、十六烷基二甲聚矽氧烷共聚醇、PEG-15月桂基二甲聚矽氧烷交聯聚合物、月桂基甲聚矽氧烷 交聯聚合物、環甲聚矽氧烷及二甲聚矽氧烷共聚醇、二甲聚矽氧烷共聚醇(及)辛酸/癸酸甘油三酸酯、聚甘油-4異硬脂酸酯(及)十六烷基二甲聚矽氧烷共聚醇(及)月桂酸己基酯、及二甲聚矽氧烷共聚醇(及)環五矽氧烷。聚矽氧包水乳化劑之較佳實例包括(但不限於)PEG/PPG-18/18二甲聚矽氧烷(商品名5225C,Dow Corning)、PEG/PPG-19/19二甲聚矽氧烷(商品名BY25-337,Dow Corning)、十六烷基PEG/PPG-10/1二甲聚矽氧烷(商品名Abil EM-90,Goldschmidt Chemical公司)、PEG-12二甲聚矽氧烷(商品名SF 1288,General Electric)、月桂基PEG/PPG-18/18矽酮(商品名5200 FORMULATION AID,Dow Corning)、PEG-12二甲聚矽氧烷交聯聚合物(商品名9010及9011聚矽氧彈性體摻合物,Dow Corning)、PEG-10二甲聚矽氧烷交聯聚合物(商品名KSG-20,Shin-Etsu)、二甲聚矽氧烷PEG-10/15交聯聚合物(商品名KSG-210,Shin-Etsu)及二甲聚矽氧烷PEG-7異硬脂酸酯。 Examples of polyoxynegated water emulsifiers include, but are not limited to, dimethoxane PEG 10/15 crosslinked polymer, dimethicone copolyol, cetyl dimethoxane copolymer Alcohol, PEG-15 lauryl dimethoxane cross-linked polymer, lauryl polyoxymethane Crosslinked polymer, cyclomethicone and dimethoxane copolyol, dimethoxane copolyol (and) caprylic/capric triglyceride, polyglycerol-4 isostearate (and) cetyl dimethoxane copolyol (and) hexyl laurate, and dimethyl polyoxyn copoly alcohol (and) cyclopentaoxane. Preferred examples of polyoxyxyl alcohol emulsifiers include, but are not limited to, PEG/PPG-18/18 dimethylpolyoxane (trade name 5225C, Dow Corning), PEG/PPG-19/19 dimethyl hydrazine. Oxyalkane (trade name BY25-337, Dow Corning), cetyl PEG/PPG-10/1 dimethylpolyoxane (trade name Abil EM-90, Goldschmidt Chemical), PEG-12 dimethyl fluorene Oxyalkane (trade name SF 1288, General Electric), lauryl PEG/PPG-18/18 fluorenone (trade name 5200 FORMULATION AID, Dow Corning), PEG-12 dimethylpolyoxane cross-linked polymer (trade name) 9010 and 9011 polyoxyxene elastomer blends, Dow Corning), PEG-10 dimethylpolyoxyalkylene crosspolymer (trade name KSG-20, Shin-Etsu), dimethylpolyoxane PEG-10 /15 crosslinked polymer (trade name KSG-210, Shin-Etsu) and dimethoxane PEG-7 isostearate.

聚矽氧包水乳化劑通常可依約0.001重量%至約10重量%之量、在一個實施例中依約0.01重量%至約5重量%、在一個實施例中依低於1重量%之量存在於組合物中。 The polyoxynoxa emulsifiable emulsifier can generally be present in an amount from about 0.001% to about 10% by weight, in one embodiment from about 0.01% to about 5% by weight, and in one embodiment from less than 1% by weight. The amount is present in the composition.

乳液之水相可包括一或多種其他溶劑,包括低碳數醇,例如乙醇、異丙醇及諸如此類。揮發性溶劑亦可為化妝品上可接受之酯,例如乙酸丁酯或乙酸乙酯;酮,例如丙酮或乙基甲基酮;或諸如此類。 The aqueous phase of the emulsion can include one or more other solvents, including lower alcohols such as ethanol, isopropanol, and the like. The volatile solvent may also be a cosmetically acceptable ester such as butyl acetate or ethyl acetate; a ketone such as acetone or ethyl methyl ketone; or the like.

含油相通常可佔乳液之總重量之約10重量%至約99重量%,在一個實施例中約20重量%至約85重量%,且在一個實施例中約30重量%至約70重量%,且水相通常可佔總乳液之約1重量%至約90重量%,在一個實施例中約5重量%至約70重量%,且更經常在一個實施例中約20重量%至約60重量%。水相通常可包含約25重量%至約100重量%、更通常約50重量%至約95重量%水。 The oil-containing phase can generally comprise from about 10% to about 99% by weight, in one embodiment from about 20% to about 85% by weight, and in one embodiment from about 30% to about 70% by weight, based on the total weight of the emulsion. And the aqueous phase can generally comprise from about 1% to about 90% by weight of the total emulsion, in one embodiment from about 5% to about 70% by weight, and more often from about 20% to about 60 in one embodiment. weight%. The aqueous phase can generally comprise from about 25% to about 100% by weight, more typically from about 50% to about 95% by weight water.

組合物可包括脂質體。脂質體可包含其他添加劑或物質及/或可 經改質以在投與後更特定地到達或保留於位點處。 The composition can include liposomes. Liposomes may contain other additives or substances and/or may It is modified to arrive or remain more specifically at the site after administration.

遵照本發明推薦之日劑量介於0.5mg/天至2600mg/天且在一個實施例中5mg/天至1200mg/天山桂花萃取物之範圍內。本發明組合物可服用若干天、週或月。治療方案可在一年內重複多次且甚至可連續。 The recommended daily dose in accordance with the present invention ranges from 0.5 mg/day to 2600 mg/day and in one embodiment from 5 mg/day to 1200 mg/day of the osmanthus extract. The compositions of the invention may be administered for several days, weeks or months. The treatment regimen can be repeated multiple times a year and can even be continuous.

在一個實施例中,組合物意欲用作非治療性治療。在另一實施例中,組合物係根據US FD&C Act,sec.201(i)意欲擦拭、傾倒、噴灑或噴霧於人體上、引入人體中或以其他方式施用至人體用於清潔、美化、促進吸引力或改變外觀之物件。 In one embodiment, the composition is intended for use as a non-therapeutic treatment. In another embodiment, the composition is intended to be wiped, poured, sprayed or sprayed onto the human body, introduced into the human body, or otherwise applied to the human body for cleaning, beautification, promotion, according to the US FD&C Act, sec. 201(i). An object that appeals or changes its appearance.

該組合物可視情況包含對彼等熟習此項技術者顯而易見之其他化妝品活性物及賦形劑,其包括(但不限於)填充劑、乳化劑、抗氧化劑、表面活性劑、膜形成劑、螯合劑、膠凝劑、增稠劑、潤膚劑、潤濕劑、保濕劑、維他命、礦物質、黏度及/或流變性改良劑、防曬劑、去角質劑、色素脫失劑、類視色素、激素化合物、α-羥基酸、α-酮基酸、抗分枝桿菌劑、抗真菌劑、抗微生物劑、抗病毒劑、鎮痛劑、脂質化合物、抗過敏劑、H1或H2抗組胺劑、抗發炎劑、抗刺激劑、抗腫瘤劑、免疫系統加強劑、免疫系統抑制劑、祛痘劑、麻醉劑、防腐劑(antiseptics)、驅蟲劑、冷膚化合物、護膚劑、皮膚促滲劑、磨砂劑、潤滑劑、芳香劑、著色劑、色素脫失劑、色素淡化劑、防腐劑(preservative)(例如,DMDM己內醯脲/碘丙炔丁基碳酸酯)、穩定劑、醫藥劑、光穩定劑、中和劑(例如,三乙醇胺)及其混合物。除上述外,本發明之化妝品組合物亦可含有用於治療皮膚病症之任何其他化合物。 The compositions may optionally include other cosmetic actives and excipients which are apparent to those skilled in the art including, but not limited to, fillers, emulsifiers, antioxidants, surfactants, film formers, chelating agents. Mixture, gelling agent, thickener, emollient, moisturizer, moisturizer, vitamin, mineral, viscosity and / or rheology modifier, sunscreen, exfoliating agent, pigment loss agent, retinoid , hormone compound, α-hydroxy acid, α-keto acid, antimycobacterial agent, antifungal agent, antimicrobial agent, antiviral agent, analgesic, lipid compound, antiallergic agent, H1 or H2 antihistamine , anti-inflammatory, anti-irritant, anti-tumor, immune system enhancer, immune system inhibitor, acne, anesthetic, antiseptics, insect repellent, skin care, skin care, skin penetration enhancer , sanding agents, lubricants, fragrances, colorants, pigment loss agents, pigment lightening agents, preservatives (for example, DMDM caprolactam / iodopropynyl butyl carbonate), stabilizers, pharmaceutical agents , light stabilizer, neutralizer (example , Triethanolamine) and mixtures thereof. In addition to the above, the cosmetic composition of the present invention may also contain any other compound for treating a skin condition.

組合物可包含具有抗老化效益之其他活性成份,如預期可利用該等組合獲得協同改良。例示性抗老化組份包括(但不限於,列舉幾個例子)植物藥(例如紫鉚(Butea Frondosa)萃取物);硫二丙酸(TDPA) 及其酯;類視色素(例如,全反式視黃酸、9-順式視黃酸、植烷酸及其他);羥酸(包括α-羥酸及β-羥酸)、水楊酸及水楊酸酯;脫落劑(例如,乙醇酸、3,6,9-三氧雜十一烷二酸等);雌激素合成酶刺激化合物(例如咖啡因及衍生物);能夠抑制5α-還原酶活性之化合物(例如,次亞麻油酸、亞麻油酸、非那雄胺(finasteride)及其混合物);障壁功能增強劑(例如,神經醯胺、甘油、膽固醇及其酯、α-羥基及ω-羥基脂肪酸及其酯等);膠原酶抑制劑;及彈性蛋白酶抑制劑。 The compositions may contain other active ingredients with anti-aging benefits, as may be expected to achieve synergistic improvements using such combinations. Exemplary anti-aging components include, but are not limited to, a few examples of botanicals (eg, Butea Frondosa extract); thiodipropionic acid (TDPA) and its esters; retinoids (eg, total anti- Retinoic acid, 9-cis retinoic acid, phytanic acid and others); hydroxy acids (including alpha-hydroxy acids and beta-hydroxy acids), salicylic acid and salicylates; exfoliating agents (eg, ethanol) Acid, 3,6,9-trioxadecanedioic acid, etc.; estrogen synthase stimulating compounds (such as caffeine and derivatives); compounds capable of inhibiting 5α-reductase activity (eg, linoleic acid) , linoleic acid, finasteride and mixtures thereof; barrier function enhancers (eg, neuropterin, glycerol, cholesterol and its esters, alpha-hydroxy and ω-hydroxy fatty acids and their esters, etc.); collagen Enzyme inhibitors; and elastase inhibitors.

本發明組合物亦可包括皮膚美白劑。該等適宜皮膚美白劑之一些實例包括(但不限於)以下中之一或多者:抗壞血酸葡糖苷、維他命C、視黃醇及/或其衍生物、熊果苷(arbutin)、熊果萃取物、皺葉酸模(rumex crispus)萃取物、乳蛋白(包括水解乳蛋白)、N,N,S-叁(羧基甲基)半胱胺、齊墩果酸(oleanolic acids)、紫蘇油、胎盤萃取物、虎耳草(Saxifragia sarmentosa)、紫蘇萃取物、檜酸(juniperic acid)、TDPA、川芎(Ligusticum chiangxiong hart.)、紫其(Asmunda japonica thunb.)、繁縷(Stellaria medica(L.)cyr.)、垂盆草(Sedum sarmentosum bunge)、女貞(Ligusticum lucidum Ait.)、四季青(ilex purpurea hassk)、餘甘子(emblica)、芹黃素(apigenin)、抗壞血酸基棕櫚醇、長豆角(carruba)多酚、橙皮素(hesperitin)、稲畑(inabata)多酚、異甘草素(isoliquirtigenin)、山茶酚-7-新橙皮糖(kaempherol-7-neohesperidose)、L-含羞草鹼(L-mimosine)、木犀草素(luteolin)、油溶性甘草(licorice)萃取物P-T(40)、含氧酸(oxa acid)、異硫氰酸苯基酯、可可素(cococin)、水飛薊(silymarin)、T4CA、四氫薑黃素、由尼三醇(unitrienol)、熊果酸-齊墩果酸、UVA/URSI、對苯二酚、麴酸、洋甘草(Glycyrrhiza glabra)、普通小球藻(Chiarella vulgaris)萃取物、椰果萃取物、紫鉚(Butea frondosa)、補血草(Naringi crenulata)、烏蕨(Stenoloma chusana)、印楝(Azadirachta indicia)、檄樹(Morinda citrifolia),或其任何組合,參見美國專利7,189,419,其全文以引用方式併入本文中。 Compositions of the invention may also include skin lightening agents. Some examples of such suitable skin lightening agents include, but are not limited to, one or more of the following: ascorbyl glucoside, vitamin C, retinol and/or its derivatives, arbutin, bearberry extract , rumex crispus extract, milk protein (including hydrolyzed milk protein), N, N, S-叁 (carboxymethyl) cysteamine, oleanolic acids, perilla oil, placenta Extract, Saxifragia sarmentosa , Perilla extract, juniperic acid, TDPA, Ligusticum chiangxiong hart. , Asmunda japonica thunb. , Stellaria medica (L.) cyr .), Sedum sarmentosum bunge , Ligusticum lucidum Ait. , ilex purpurea hassk , emblica, apigenin, ascorbyl palmitol, long bean ( Carruba) polyphenols, hesperitin, inabata polyphenols, isoliquirtigenin, kaempferol-7-neohesperidose, L-mimosine (L) -mimosine), luteolin, oil-soluble licorice extract PT (40), oxa acid, phenyl isothiocyanate, cococin, silymarin, T4CA, tetrahydrocurcumin, unitrienol, bear AHA-oleanolic acid, UVA/URSI, hydroquinone, citric acid, Glycyrrhiza glabra , Chiarella vulgaris extract, coconut extract, butea frondosa , Naringi crenulata , Stenoloma chusana , Azadirachta indicia , Morinda citrifolia , or any combination thereof, see U.S. Patent No. 7,189,419, hereby incorporated by reference herein.

適宜羥基酸包括例如乙醇酸、乳酸、蘋果酸、酒石酸、檸檬酸、2-羥基烷酸、扁桃酸、水楊酸、及其烷基衍生物(包括5-正辛醯基水楊酸、5-正十二烷醯基水楊酸、5-正癸醯基水楊酸、5-正辛基水楊酸、5-正庚基氧基水楊酸、4-正庚基氧基水楊酸),及2-羥基-3-甲基苯甲酸或其烷氧基衍生物(例如2-羥基-3-甲氧基苯甲酸)。 Suitable hydroxy acids include, for example, glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, 2-hydroxyalkanoic acid, mandelic acid, salicylic acid, and alkyl derivatives thereof (including 5-n-octyl salicylic acid, 5-positive Dodecanedecyl salicylic acid, 5-n-decylsalicylic acid, 5-n-octylsalicylic acid, 5-n-heptyloxysalicylic acid, 4-n-heptyloxysalicylic acid) And 2-hydroxy-3-methylbenzoic acid or an alkoxy derivative thereof (for example 2-hydroxy-3-methoxybenzoic acid).

例示性類視色素包括(但不限於):視黃酸(例如全反式-或13順式)及其衍生物、視黃醇(維他命A)及其酯(例如視黃醇棕櫚酸酯、視黃醇乙酸酯及視黃醇丙酸酯)及其鹽。 Exemplary retinoids include, but are not limited to, retinoic acid (eg, all-trans- or 13-cis) and derivatives thereof, retinol (vitamin A) and esters thereof (eg, retinyl palmitate, Retinol acetate and retinyl propionate) and salts thereof.

在另一實施例中,本發明之局部組合物亦可包括以下中之一或多者:皮膚促滲劑、潤膚劑、皮膚豐滿劑、光散射劑、防曬劑、脫落劑及抗氧化劑。 In another embodiment, the topical compositions of the present invention may also include one or more of the following: skin penetration enhancers, emollients, skin plumping agents, light scattering agents, sunscreens, exfoliating agents, and antioxidants.

潤膚劑提供增強膚質(平滑性)及減少細紋及粗皺紋之外觀的功能效益。實例包括肉豆蔻酸異丙酯、礦脂、羊毛脂酸異丙酯、聚矽氧(例如,甲聚矽氧烷、二甲聚矽氧烷)、油、礦物質油、脂肪酸酯、己酸十六烷基乙基酯、苯甲酸C12-15烷基酯、異硬脂酸異丙酯、二異丙基二聚體二油酸酯或其任何混合物。在一個實施例中,潤膚劑可以組合物總重量之約0.1wt%至約50wt%存在。 Emollients provide functional benefits that enhance skin texture (smoothness) and reduce the appearance of fine lines and coarse wrinkles. Examples include isopropyl myristate, petrolatum, isopropyl lanolate, polyoxo (eg, polyoxyalkylene, dimethylpolyoxyalkylene), oils, mineral oils, fatty acid esters, Cetylethyl ethyl acrylate, C 12-15 alkyl benzoate, isopropyl isostearate, diisopropyl dimer dioleate or any mixture thereof. In one embodiment, the emollient may be present from about 0.1% to about 50% by weight of the total weight of the composition.

皮膚豐滿劑用作皮膚之膠原增強劑。適宜且較佳之皮膚豐滿劑之實例係棕櫚醯基寡肽。其他皮膚豐滿劑係膠原及/或其他糖胺聚糖(GAG)增強劑。皮膚豐滿劑(若存在)可佔組合物總重量之約0.1wt%至約20wt%。 A skin fullness agent is used as a collagen enhancer for the skin. An example of a suitable and preferred skin plump agent is palmitoyl oligopeptide. Other skin plump agents are collagen and/or other glycosaminoglycan (GAG) enhancers. The skin plumping agent, if present, can comprise from about 0.1% to about 20% by weight of the total weight of the composition.

光散射劑係改變皮膚之表面光學特徵之微粒,其可致使視覺模糊並可軟化(例如)紋及皺紋。可用於本發明中之光散射劑之實例包括(但不限於):氮化硼、雲母、耐綸、聚甲基丙烯酸甲酯(PMMA)、聚 胺基甲酸酯粉、絹雲母、二氧化矽、聚矽氧粉、滑石粉、特氟隆、二氧化鈦、氧化鋅或任何其混合物。光散射劑(若存在)可以組合物總重量之約0.01wt%至約20wt%存在。 Light scattering agents are microparticles that alter the optical characteristics of the surface of the skin, which can cause blurred vision and soften, for example, lines and wrinkles. Examples of light scattering agents that can be used in the present invention include, but are not limited to: boron nitride, mica, nylon, polymethyl methacrylate (PMMA), poly Aurethane powder, sericite, cerium oxide, polyoxyn powder, talc, Teflon, titanium dioxide, zinc oxide or any mixture thereof. The light scattering agent, if present, can be present from about 0.01% to about 20% by weight of the total weight of the composition.

亦可包括保護皮膚免受紫外線傷害之防曬劑。較佳防曬劑係彼等具有廣泛UVB及UVA保護者,例如氰雙苯丙烯酸辛酯、阿伏苯宗(avobenzone)(Parsol 1789)、甲氧基肉桂酸辛酯、水楊酸辛酯、氧苯酮、水楊酸三甲環己酯、二苯甲酮、樟腦衍生物、氧化鋅及二氧化鈦。防曬劑(若存在)可佔組合物之約0.01wt%至約70wt%。 It can also include sunscreens that protect the skin from UV rays. Preferred sunscreens are those with extensive UVB and UVA protection, such as octyl cyanoacrylate, avobenzone (Parsol 1789), octyl methoxycinnamate, octyl salicylate, oxybenzone , trimethylcyclohexyl salicylate, benzophenone, camphor derivatives, zinc oxide and titanium dioxide. The sunscreen, if present, can comprise from about 0.01% to about 70% by weight of the composition.

適宜脫落劑包括(例如)α-羥酸、β-羥酸、含氧酸、含氧二酸及其衍生物(例如其酯、酐及鹽)。適宜羥酸包括(例如)乙醇酸、乳酸、蘋果酸、酒石酸、檸檬酸、2-羥基烷酸、扁桃酸、水楊酸及其衍生物。另一脫落劑係乙醇酸。脫落劑(若存在)可佔組合物之約0.1wt%至約80wt%。 Suitable exfoliating agents include, for example, alpha-hydroxy acids, beta-hydroxy acids, oxo acids, oxydiacids and derivatives thereof (e.g., esters, anhydrides, and salts thereof). Suitable hydroxy acids include, for example, glycolic acid, lactic acid, malic acid, tartaric acid, citric acid, 2-hydroxyalkanoic acid, mandelic acid, salicylic acid, and derivatives thereof. Another exfoliating agent is glycolic acid. The exfoliating agent, if present, can comprise from about 0.1% to about 80% by weight of the composition.

抗氧化劑尤其起到自皮膚清除自由基以保護皮膚免受環境侵襲之作用。可用於本發明組合物中之抗氧化劑之實例包括含有酚類羥基官能基之化合物,例如抗壞血酸及其衍生物/酯類;α-羥酸;β-胡蘿蔔素;兒茶酚;薑黃素;阿魏酸衍生物(例如阿魏酸乙酯、阿魏酸鈉);沒食子酸衍生物(例如沒食子酸丙酯);番茄紅素;還原酸;迷迭香酸;丹寧酸;四氫薑黃素;生育酚及其衍生物(例如,乙酸生育酚酯);尿酸;或其任何混合物。其他適宜抗氧化劑係彼等具有一或多個硫醇官能基(-SH)者(呈還原形式或非還原形式),例如麩胱甘肽、硫辛酸、硫代乙醇酸及其他巰基化合物。抗氧化劑可係無機抗氧化劑,例如亞硫酸氫鹽、偏亞硫酸氫鹽、亞硫酸鹽或其他含硫無機鹽及酸。本發明組合物可包含佔組合物總重量之在一個實施例中約0.001wt%至約10wt%、在一個實施例中約0.01wt%至約5wt%之抗氧化劑。 Antioxidants especially act to scavenge free radicals from the skin to protect the skin from environmental attack. Examples of the antioxidant which can be used in the composition of the present invention include compounds containing a phenolic hydroxyl functional group such as ascorbic acid and derivatives/esters thereof; ?-hydroxy acid; ?-carotene; catechol; curcumin; Wei acid derivatives (such as ethyl ferulate, sodium ferulate); gallic acid derivatives (such as propyl gallate); lycopene; reducing acid; rosmarinic acid; tannic acid; Tetrahydrocurcumin; tocopherol and its derivatives (eg, tocopheryl acetate); uric acid; or any mixture thereof. Other suitable antioxidants are those having one or more thiol functional groups (-SH) (in reduced or non-reduced form), such as glutathione, lipoic acid, thioglycolic acid, and other sulfhydryl compounds. The antioxidant may be an inorganic antioxidant such as bisulfite, metabisulfite, sulfite or other sulfur-containing inorganic salt and acid. The compositions of the present invention may comprise from about 0.001% to about 10% by weight, and in one embodiment from about 0.01% to about 5% by weight, of the total weight of the composition of the antioxidant.

在一些實施例中,其他活性物可包括膠原刺激劑及/或彈性蛋白 刺激劑(例如,刺激彈性蛋白產生之物質)及/或糖胺聚糖增強劑。膠原、彈性蛋白及糖胺聚糖增強劑之實例包括(例如)茴香萃取物、胡蘿蔔萃取物及紫花苜蓿萃取物。在一些實施例中,其他活性物可包括膠原酶抑制劑及/或彈性蛋白酶抑制劑。在一些實施例中,本發明係關於本文所述一或多種組合物與紫蘇油協同作用以(例如)為皮膚提供增強抗脂肪團效益。 In some embodiments, other actives may include collagen stimulating agents and/or elastin A stimulating agent (for example, a substance that stimulates elastin production) and/or a glycosaminoglycan enhancer. Examples of collagen, elastin, and glycosaminoglycan enhancers include, for example, fennel extract, carrot extract, and alfalfa extract. In some embodiments, other actives can include collagenase inhibitors and/or elastase inhibitors. In some embodiments, the present invention relates to the synergistic effect of one or more of the compositions described herein with perilla oil to, for example, provide enhanced anti-cellulite benefits to the skin.

在一些實施例中,化妝品組合物可進一步包含至少一種膠原及/或彈性蛋白刺激劑。該等膠原或彈性蛋白刺激劑可有效(例如)改善原膠原及/或膠原產生及/或改善彈性蛋白之維持及重塑。 In some embodiments, the cosmetic composition can further comprise at least one collagen and/or elastin irritant. Such collagen or elastin stimulators are effective, for example, to improve procollagen and/or collagen production and/or to improve the maintenance and remodeling of elastin.

著色劑可包括(例如)有機及無機顏料及珠光劑。適宜無機顏料包括(但不限於)氧化鈦、氧化鋯及氧化鈰、以及氧化鋅、氧化鐵、氧化鉻及亞鐵藍。適宜有機顏料包括鋇、鍶、鈣、鋁色澱及炭黑。適宜珠光劑包括經氧化鈦、氧化鐵或天然顏料塗佈之雲母。 Colorants can include, for example, organic and inorganic pigments and pearlizing agents. Suitable inorganic pigments include, but are not limited to, titanium oxide, zirconium oxide and cerium oxide, as well as zinc oxide, iron oxide, chromium oxide and ferrous blue. Suitable organic pigments include strontium, barium, calcium, aluminum lakes and carbon black. Suitable pearlescent agents include mica coated with titanium oxide, iron oxide or natural pigments.

可添加各種填充劑及其他組份。填充劑通常以組合物總重量之約0重量%至約20重量%、在一個實施例中約0.1重量%至約10重量%之量存在。適宜填充劑包括(但不限於)以下:二氧化矽、經處理二氧化矽、滑石粉、硬脂酸鋅、雲母、高嶺土(kaolin)、耐綸粉末(例如,OrgasolTM)、聚乙烯粉末、TeflonTM、氮化硼、共聚物微球體(例如,ExpancelTM(Nobel Industries)、PolytrapTM(Dow Corning)及聚矽氧樹脂微珠粒(來自Toshiba之TospearlTM))及諸如此類。 Various fillers and other components can be added. The filler is typically present in an amount from about 0% to about 20% by weight, and in one embodiment from about 0.1% to about 10% by weight, based on the total weight of the composition. Suitable fillers include (but are not limited to) the following: silicon dioxide, treated silicon dioxide, talc, zinc stearate, mica, kaolin (Kaolin), nylon powder (e.g., Orgasol TM), polyethylene powder, Teflon TM, boron nitride, copolymer microspheres (e.g., Expancel TM (Nobel Industries), Polytrap TM (Dow Corning) and silicone polyethylene micro beads (from Toshiba of Tospearl TM)) and the like.

在本發明之一個實施例中,組合物可包括其他皮膚活性物,例如但不限於植物藥、去角質劑、脫皮劑、角質細胞增殖增強劑、膠原酶抑制劑、彈性蛋白酶抑制劑、色素脫失劑、抗發炎劑、類固醇、祛痘劑、抗氧化劑、水楊酸或水楊酸酯、抗脂質劑、抗脂肪團劑、硫二丙酸及其酯及晚期糖基化終產物(AGE)抑制劑。 In one embodiment of the invention, the composition may include other skin actives such as, but not limited to, botanicals, exfoliating agents, peeling agents, keratinocyte proliferation enhancers, collagenase inhibitors, elastase inhibitors, pigments. Loss agents, anti-inflammatory agents, steroids, acne agents, antioxidants, salicylic acid or salicylates, anti-lipids, anti-cellulite agents, thiodipropionic acid and its esters, and advanced glycation end products (AGE) ) inhibitors.

在一些實施例中,用於對抗老化體徵之化妝品組合物可進一步 包含抗脂質劑。舉例而言,包含可有效改善皮膚外觀之量之肉鹼棕櫚醯基轉移酶-1(CPT-1)刺激劑(例如楊桃(Averrhoa carambola)葉萃取物)的化妝品組合物可進一步包含至少一種其他抗脂質劑,包括一種其他抗脂肪團劑。 In some embodiments, the cosmetic composition for combating signs of aging may further comprise an anti-lipid agent. For example, a cosmetic composition comprising a carnitine palmitoyltransferase-1 (CPT-1) stimulating agent (eg, an Averrhoa carambola leaf extract) in an amount effective to improve skin appearance may further comprise at least one other Anti-lipid agents, including one other anti-cellulite agent.

例示性抗脂肪團劑包括(但不限於)磷酸二酯酶抑制劑,例如黃嘌呤類似物、咖啡因、氨茶鹼(aminophylline)及茶鹼(theophylline);腺苷酸環化酶活化劑,例如福司柯林及毛喉鞘蕊花(Coleus forskohlii)萃取物;脂解刺激劑,例如山楂萃取物及可樂樹萃取物;β腎上腺素能受體激動劑,例如異丙腎上腺素;α-2-腎上腺素能拮抗劑,例如育亨賓(yohimbine)及銀杏萃取物;紫蘇油(例如,參見US 7,410,658);肉鹼及/或肌酸(例如,參見標題為「Cosmetic Composition having Carnitine Creatinate and Methods for Using」且全部內容以引用方式併入本文中之US 2007/0264205)。 Exemplary anti-cellulite agents include, but are not limited to, phosphodiesterase inhibitors, such as xanthine analogs, caffeine, aminophylline, and theophylline; adenylate cyclase activators, For example, extracts of forskolin and Coleus forskohlii ; lipolytic stimulators such as hawthorn extract and cola extract; beta adrenergic receptor agonists such as isoproterenol; - adrenergic antagonists, such as yohimbine and ginkgo extract; perilla oil (see, for example, US 7,410,658); carnitine and/or creatine (see, for example, "Cosmetic Composition having Carnitine Creatinate and Methods" For use" and the entire contents of which is hereby incorporated by reference herein in its entirety.

在具體實施例中,組合物可包含至少一種其他植物藥,例如植物萃取物、精油或植物自身。適宜植物藥包括(但不限於)來自以下之萃取物:印度冷杉(Abies pindrow)、兒茶(Acacia catechu)、寬葉榆綠木(Anogeissus latifolia)、紫萁(Asmunda japonica)、印楝(Azadirachta indica)、紫鉚(Butea frondosa)、紫礦(Butea monosperma)、雪松(Cedrus deodara)、餘甘果(Emblica officinalis)、孟加拉榕(Ficus benghalensis)、洋甘草、法國冬青(Ilex purpurea Hassk)、川木香(Inula racemosa)、川芎(Ligusticum chuangxiong)、女貞(Ligusticum lucidum)、粗糠柴(Mallotus philippinensis)、西班牙櫻桃(Mimusops elengi)、檄樹、辣木(Moringa oleifera)、補血草(Naringi crenulata)、夾竹桃(Nerium indicum)、補骨脂(Psoralea corylifolia)、烏蕨、毗黎勒(Terminalia bellerica)、番茄糖脂及其混合物。 In a particular embodiment, the composition may comprise at least one other botanical drug, such as a plant extract, an essential oil or the plant itself. Suitable botanicals include, but are not limited to, extracts from the following: Abies pindrow , Acacia catechu , Anogeissus latifolia , Asmunda japonica , Azadirachta Indica ), Butea frondosa , Butea monosperma , Cedrus deodara , Emblica officinalis , Ficus benghalensis , Licorice, French holly ( Ilex purpurea Hassk ), Sichuan Inula racemosa , Ligusticum chuangxiong , Ligusticum lucidum , Mallotus philippinensis , Mimusops elengi , eucalyptus , Moringa oleifera , Naringi crenulata ), Nerium indicum , Psoralea corylifolia , Fern, Terminalia bellerica , tomato glycolipid and mixtures thereof.

其他習用添加劑包括:維他命,例如生育酚及抗壞血酸;維他 命衍生物,例如單棕櫚酸抗壞血酯;增稠劑,例如羥基烷基纖維素;膠凝劑;結構化劑,例如膨潤土、膨潤石、矽酸鎂鋁及矽酸鋰鎂;金屬螯合劑,例如EDTA;顏料,例如氧化鋅及二氧化鈦;著色劑;潤膚劑;及潤濕劑。 Other conventional additives include: vitamins such as tocopherol and ascorbic acid; vitamins Derivatives such as ascorbyl monopalmitate; thickeners such as hydroxyalkyl cellulose; gelling agents; structuring agents such as bentonite, bentonite, magnesium aluminum silicate and lithium magnesium niobate; Mixtures such as EDTA; pigments such as zinc oxide and titanium dioxide; colorants; emollients; and wetting agents.

在一個實施例中,組合物基本上不含具有強氧化潛能之組份,其包括(例如)有機或無機過氧化物。「基本上不含」該等組份意指所存在之量不足以對山桂花萃取物之活性具有可量測之影響。在一些實施例中,相對於山桂花之量,此將小於1重量%。 In one embodiment, the composition is substantially free of components having strong oxidizing potential, including, for example, organic or inorganic peroxides. "Substantially free" of such components means that the amount present is not sufficient to have a measurable effect on the activity of the osmanthus extract. In some embodiments, this will be less than 1% by weight relative to the amount of osmanthus.

在一個實施例中,本發明包含山桂花萃取物之組合物的pH可介於約1與約8之間。在某些實施例中,組合物之pH將為酸性,即小於7.0,在一個實施例中可介於約2與約7之間,在一個實施例中介於約3.5與約5.5之間。 In one embodiment, the pH of the composition comprising the osmanthus extract of the present invention may be between about 1 and about 8. In certain embodiments, the pH of the composition will be acidic, i.e., less than 7.0, and in one embodiment may be between about 2 and about 7, and in one embodiment between about 3.5 and about 5.5.

治療正老化或已老化皮膚之方法Method of treating aging or aged skin

本發明提供治療老化皮膚之方法,其係藉由以下方式達成:在受侵襲區域上局部施用包含山桂花萃取物、在一個實施例中存於化妝品上可接受之媒劑中之組合物達足以減輕、改善、逆轉或預防老化之皮膚病學體徵的時間段。此方法尤其可用於治療皮膚光老化及內在老化之體徵。 The present invention provides a method of treating aged skin by topically applying a composition comprising a osmanthus extract, in one embodiment, to a cosmetically acceptable vehicle, on the affected area. The period of time to reduce, ameliorate, reverse or prevent dermatological signs of aging. This method is especially useful for treating signs of skin photoaging and intrinsic aging.

通常,症狀及/或美觀之改善係選自由以下組成之群:減輕年齡性老化、光老化、激素性老化及/或光化性老化之皮膚病學體徵;預防及/或減少紋及/或皺紋之外觀;減輕臉部紋及皺紋、面頰、前額上之臉部皺紋、介於眼睛之間的垂直皺紋、眼睛上面的水平皺紋、及圍繞口部之木偶紋、及尤其深皺紋或皺褶之顯著性;預防、減輕及/或減少紋及/或皺紋之外觀及/或深度;改善眶下紋及/或眼眶周圍紋之外觀;減輕眼角皺紋之外觀;復原及/或複新皮膚,尤其老化皮膚;減輕皮膚脆性;預防及/或逆轉葡萄糖胺聚糖及/或膠原之損失;改善雌 激素失調之效應;預防皮膚萎縮;預防、減輕及/或治療色素沉著過度;最小化皮膚變色;改善皮膚色調、光彩、透明度及/或緊實度;預防、減輕及/或改善皮膚下垂;改善皮膚堅實度、豐滿度、柔順度及/或柔軟度;改善原膠原及/或膠原產生;改善膚質及/或促進煥膚;改善皮膚障壁修復及/或功能;改善皮膚輪廓之外觀;恢復皮膚光澤及/或亮度;最小化疲勞及/或應激之皮膚病學體徵;抵抗環境應激;補充皮膚中因老化及/或更年期而減少的成份;改善皮膚細胞間之流通;增強細胞增殖及/或倍增;增強因老化及/或停經而減少的成份;改善皮膚細胞間之通信;增加細胞增殖及/或繁殖;增加因老化及/或停經而降低之皮膚細胞代謝;延緩細胞老化;改善皮膚濕潤性;增強皮膚厚度;增加皮膚彈性及/或回彈性;增強脫落;改善微循環;減少及/或預防脂肪團形成;及其任何組合。 Generally, the improvement in symptoms and/or aesthetics is selected from the group consisting of: dermatological signs that alleviate ageing, photoaging, hormonal aging, and/or actinic aging; prevention and/or reduction of streaks and/or The appearance of wrinkles; reduces facial lines and wrinkles, cheeks, facial wrinkles on the forehead, vertical wrinkles between the eyes, horizontal wrinkles above the eyes, and puppet lines around the mouth, and especially deep wrinkles or wrinkles Significant pleats; prevent, reduce and/or reduce the appearance and/or depth of creases and/or wrinkles; improve the appearance of underarms and/or around the eyelids; reduce the appearance of wrinkles around the eyes; restore and/or rejuvenate the skin , especially aging skin; reduce skin fragility; prevent and / or reverse the loss of glycosaminoglycan and / or collagen; improve female Effects of hormonal imbalance; prevention of skin atrophy; prevention, alleviation and/or treatment of hyperpigmentation; minimization of skin discoloration; improvement of skin tone, brilliance, transparency and/or firmness; prevention, reduction and/or improvement of sagging skin; improvement Skin firmness, fullness, suppleness and/or softness; improve procollagen and/or collagen production; improve skin texture and/or promote skin rejuvenation; improve skin barrier repair and/or function; improve skin contour appearance; Skin radiance and/or brightness; minimize dermatological signs of fatigue and/or stress; resist environmental stress; replenish ingredients in the skin that are reduced by aging and/or menopause; improve circulation between skin cells; enhance cell proliferation And/or multiplication; enhancing components that are reduced by aging and/or menopause; improving communication between skin cells; increasing cell proliferation and/or reproduction; increasing skin cell metabolism decreased by aging and/or menopause; delaying cell aging; Improve skin moisturization; enhance skin thickness; increase skin elasticity and / or resilience; enhance shedding; improve microcirculation; reduce and / or prevent cellulite Formed; and any combination thereof.

在另一實施例中,本發明提供治療變色皮膚之方法,其係藉由以下方式達成:在受侵襲區域上局部施用包含山桂花萃取物、在一個實施例中存於化妝品上可接受之媒劑中之組合物達足以減輕、改善、逆轉或預防皮膚變色的時間段。此方法尤其可用於治療由於光老化及內在老化引起之變色。通常,皮膚變色之症狀及/或美觀的改善係選自由以下組成之群:漂白色素沉著過度之毛髮、皮膚、唇及/或指甲;減少老人斑;使皮膚變色均勻或最佳化;改善眼下暗圈之外觀;治療黑斑病、黃褐斑、雀斑、燒傷後疤痕及損傷後色素沉著過度;漂白頭皮、腿、臉部及其他期望漂白及顏色減少之區域上之毛髮;減少黑色素產生及/或漂白指甲染色。 In another embodiment, the invention provides a method of treating discoloration of the skin by topically applying a flower comprising an extract of osmanthus fragrans on the affected area, in one embodiment a cosmetically acceptable medium The composition of the agent is in a period of time sufficient to reduce, ameliorate, reverse or prevent discoloration of the skin. This method is especially useful for treating discoloration due to photoaging and intrinsic aging. In general, the symptoms of skin discoloration and/or aesthetic improvement are selected from the group consisting of bleaching hyperpigmented hair, skin, lips and/or nails; reducing age spots; making skin discoloration uniform or optimal; improving under the eyes The appearance of dark circles; treatment of melasma, chloasma, freckles, scars after burns and hyperpigmentation after injury; bleaching of scalp, legs, face and other areas where bleaching and color reduction are desired; reducing melanin production and / or bleached nail stains.

在某些實施例中,可施用包含山桂花萃取物之組合物以對抗已知可加劇老化對皮膚之效應的各種醫藥物之副作用(具體而言彼等已知使皮膚變色者)。該等醫藥物包括(但不限於)抗生素(磺醯胺(sulfonamide)及四環素(tetracycline))、利尿劑、非類固醇抗發炎藥 物、止痛劑、精神活性醫藥、口服避孕劑、抗癲癇藥(乙內醯脲(hydantoin))、氯喹、DOPA療法(左旋多巴)、重金屬(含有砷、鉍、金或銀之藥物)及/或化學治療劑(環磷醯胺(cyclophosphamide)、5-氟尿嘧啶(5-fluorouracil)、多柔比星(doxorubicin)、柔紅黴素(daunorubicin)及博來黴素(bleomycin))。包含山桂花萃取物之組合物可在醫藥物投與之前、同時或之後施用。 In certain embodiments, a composition comprising an extract of osmanthus fragrans may be applied to combat the side effects of various pharmaceuticals known to exacerbate the effects of aging on the skin (specifically, those known to discolor the skin). Such pharmaceuticals include, but are not limited to, antibiotics (sulfonamide and tetracycline), diuretics, non-steroidal anti-inflammatory drugs Drugs, analgesics, psychoactive drugs, oral contraceptives, antiepileptic drugs (hydantoin), chloroquine, DOPA therapy (levodopa), heavy metals (drugs containing arsenic, antimony, gold or silver) and / or chemotherapeutic agents (cyclophosphamide, 5-fluorouracil, doxorubicin, daunorubicin and bleomycin). The composition comprising the osmanthus extract can be applied before, simultaneously or after administration of the medicinal agent.

通常每日一次、兩次或三次將組合物施用至皮膚,只要達成期望抗老化結果需要即可。治療方案可包含每日一次施用至少一週、至少兩週、至少四週、至少八週或至少十二週。亦涵蓋慢性治療方案。 The composition is typically applied to the skin once, twice or three times daily as long as the desired anti-aging results are achieved. The treatment regimen can include administration once a day for at least one week, at least two weeks, at least four weeks, at least eight weeks, or at least twelve weeks. Chronic treatment options are also covered.

將包含山桂花萃取物之組合物局部施用至「有需要之個體」,此意指獲益於減少皮膚損害或老化之可視體徵之個體。在具體實施例中,山桂花萃取物係於醫藥、生理、化妝品及皮膚病學可接受之媒劑、稀釋劑或載劑中提供,其中將組合物局部施用至受侵襲皮膚並以有效改善皮膚之症狀及美觀外觀之量留在受侵襲區域上。 The composition comprising the osmanthus extract is applied topically to the "individual in need", which means an individual who benefits from a visual sign that reduces skin damage or aging. In a specific embodiment, the osmanthus extract is provided in a pharmaceutically, physiologically, cosmetically and dermatologically acceptable vehicle, diluent or carrier, wherein the composition is topically applied to the affected skin to effectively improve the skin. The amount of symptoms and aesthetic appearance remains in the affected area.

在一個實施例中,治療細紋及皺紋之方法包含向有需要之個體皮膚局部施用包含山桂花萃取物之本發明組合物,例如以足以降低細紋及/或皺紋之嚴重程度或預防或抑制新細紋及/或皺紋形成之量及持續時間直接局部施用至細紋及/或皺紋。可藉由對皺紋形態(例如,每皮膚之單位面積之皺紋之數目、深度、長度、面積、體積及/或寬度)(例如)目視檢查定性地或藉由(例如)顯微鏡或電腦輔助之量測定量地評價組合物對細紋及皺紋之形成或外觀之效應。此實施例包括治療手、臂、腿、頸、胸及臉部(包括前額)之皮膚上之皺紋。 In one embodiment, a method of treating fine lines and wrinkles comprises topically applying a composition of the invention comprising an extract of osmanthus to the skin of an individual in need thereof, for example, to reduce the severity or prevent or inhibit the appearance of fine lines and/or wrinkles. The amount and duration of new fine lines and/or wrinkles are applied directly to the fine lines and/or wrinkles. By qualitatively examining the form of wrinkles (eg, number, depth, length, area, volume, and/or width of wrinkles per unit area of the skin), for example, by visual inspection or by, for example, microscopy or computer aided amounts The effect of the composition on the formation or appearance of fine lines and wrinkles was evaluated in quantitative amounts. This embodiment includes the treatment of wrinkles on the skin of the hands, arms, legs, neck, chest and face, including the forehead.

亦預計本發明組合物可用於向有需要之個體之薄皮膚局部施用該組合物來治療薄皮膚。在一些實施例中,治療係針對男性之薄皮膚,而其他實施例治療絕經前或絕經後女性之薄皮膚,據信皮膚隨男性及女性之年齡、且具體而言不同生命階段之女性而不同地薄化。 可以預防方式採用本發明方法以對抗包括尚未表現皮膚老化體徵之患者、最常見年齡為25歲以下個體中的老化。該方法亦可逆轉或治療表現後之老化體徵,如25歲以上患者中常見。 It is also contemplated that the compositions of the present invention can be used to topically apply the composition to thin skin of an individual in need thereof to treat thin skin. In some embodiments, the treatment is for thin skin of men, while other embodiments treat thin skin of premenopausal or postmenopausal women, which are believed to vary with the age of men and women, and specifically women of different life stages. The ground is thin. The method of the invention can be employed in a prophylactic manner against aging in patients including those who have not yet exhibited signs of skin aging, most commonly in individuals under the age of 25. This method can also reverse or treat signs of aging after performance, as is common in patients over 25 years of age.

實例 Instance

以下實例闡述本發明之具體態樣以闡釋本發明,但不應理解為限制本發明,此乃因該等實例僅提供可用於理解及實踐本發明及其多個態樣之具體方法。 The following examples are intended to illustrate the invention, but are not to be construed as limiting the scope of the invention.

實例1 山桂花萃取物之製備 Example 1 Preparation of Osmanthus fragrans Extract I. 純化植物萃取物之製備用於新生物分析篩選 I. Preparation of purified plant extracts for new bioassay screening 萃取方案 Extraction scheme

收集250g磨碎之山桂花之花且隨後於60℃下在電烘箱中乾燥2或3天。隨後將乾燥之花添加至容器中之1L 50%含水乙醇(EtOHIH2O 50-50 v/v;3×4體積)且藉由於37℃下將容器以150rpm振盪12h進行萃取。將此萃取重複三次以達成3L總萃取物。隨後於40℃至50℃之溫度下使用旋轉蒸發器使總萃取物經受真空濃縮直至體積減少至約150m為止。隨後將濃縮部分用純水稀釋至1500ml並於4℃下靜置12h(或更長時間)且隨後離心以移除任何殘餘物。將1500ml現在澄清之溶液用750ml己烷在分液漏斗中處理兩次並棄去有機層。藉由取150ml均質溶液試樣並將該試樣凍乾來確認剩餘均質水溶液之乾燥含量。將所得粉末稱重並使用其計算均質溶液中之乾物質之總量。隨後將所得粉末重新溶解於水(約100-150ml)中並與均質溶液彙集在一起。隨後向均質溶液中添加10重量%活性炭,約1500ml溶液為約17g活性炭。隨後將溶液於50℃下攪拌1小時且隨後在濾紙(類型,製造商)上過濾並重複該步驟。接下來,藉由利用水飽和之正丁醇液/液萃取對現在澄清之溶液進行分級分離。藉由在分液漏斗中向丁醇中添加相同體積之水製備飽和丁醇,在混合後收集有機上層並用於澄清溶液之液 /液萃取。製備約2250水飽和之丁醇用於1500ml澄清溶液。將水飽和之丁醇分成3個750ml部分且在分液漏斗中各自用於處理澄清溶液三次。單獨收集並彙集每次流經分液漏斗之所得有機層(丁醇萃取物)及水層。首先,向所彙集丁醇萃取物中添加相等體積之水並將溶液在真空下在旋轉蒸發器中濃縮。在停止蒸餾時,添加相等體積之水並重複濃縮。第三次重複濃縮且將所得溶液凍乾(第一純化萃取物)。其次,在真空下藉由旋轉蒸發器濃縮自每次流經分液漏斗產生之水層以移除丁醇(共沸沸點低於100℃,浴溫為60℃)。在停止蒸餾時,將水溶液凍乾(第二純化萃取物)。隨後合併並稱重第一及第二萃取物。 250 g of ground osmanthus flowers were collected and subsequently dried in an electric oven at 60 ° C for 2 or 3 days. The dried flowers were then added to 1 L of 50% aqueous ethanol (EtOHIH 2 O 50-50 v/v; 3 x 4 volumes) in a vessel and extracted by shaking the vessel at 150 ° C for 12 h at 37 °C. This extraction was repeated three times to achieve a total of 3 L of extract. The total extract was then subjected to vacuum concentration using a rotary evaporator at a temperature of 40 ° C to 50 ° C until the volume was reduced to about 150 m. The concentrated fraction was then diluted to 1500 ml with pure water and allowed to stand at 4 ° C for 12 h (or longer) and then centrifuged to remove any residue. 1500 ml of the now clarified solution were treated twice with 750 ml of hexane in a separatory funnel and the organic layer was discarded. The dry content of the remaining homogeneous aqueous solution was confirmed by taking 150 ml of a homogeneous solution sample and lyophilizing the sample. The resulting powder was weighed and used to calculate the total amount of dry matter in the homogeneous solution. The resulting powder is then redissolved in water (about 100-150 ml) and brought together with the homogeneous solution. Subsequently, 10% by weight of activated carbon was added to the homogeneous solution, and about 1500 ml of the solution was about 17 g of activated carbon. The solution was then stirred at 50 ° C for 1 hour and then filtered on filter paper (type, manufacturer) and the procedure repeated. Next, the now clarified solution was fractionated by liquid-liquid extraction using water-saturated n-butanol. Saturated butanol was prepared by adding the same volume of water to butanol in a separatory funnel, and after mixing, the organic upper layer was collected and used for liquid/liquid extraction of the clear solution. About 2250 water-saturated butanol was prepared for 1500 ml of clear solution. The water-saturated butanol was divided into three 750 ml portions and each was used to treat the clear solution three times in a separatory funnel. The resulting organic layer (butanol extract) and the aqueous layer each passed through a separatory funnel were separately collected and collected. First, an equal volume of water was added to the pooled butanol extract and the solution was concentrated under vacuum in a rotary evaporator. When the distillation was stopped, an equal volume of water was added and the concentration was repeated. The concentration was repeated a third time and the resulting solution was lyophilized (first purified extract). Next, the aqueous layer produced by each flow through the separatory funnel was concentrated by vacuum on a rotary evaporator to remove butanol (the azeotropic boiling point was less than 100 ° C and the bath temperature was 60 ° C). When the distillation was stopped, the aqueous solution was lyophilized (second purified extract). The first and second extracts are then combined and weighed.

萃取方案2(例示性) Extraction Scheme 2 (exemplary)

可收集並粉碎一定量(g)之磨碎之山桂花的花。隨後,可於100℃下使用8-10倍重量於粉碎之花的水使用彼等熟習此項技術者已知之方法實施回流萃取。可重複此步驟。可使用彼等熟習此項技術者已知之方法過濾並冷凝所得萃取物,其後可在彼等熟習此項技術者已知之適當條件下使萃取物經歷真空蒸餾。隨後,可將萃取物與適宜量之糊精混合並噴霧乾燥。 A certain amount (g) of the ground flower of the osmanthus fragrans can be collected and pulverized. Subsequently, refluxing extraction can be carried out using water of 8-10 times by weight of the pulverized flower at 100 ° C using methods known to those skilled in the art. This step can be repeated. The resulting extracts can be filtered and condensed using methods known to those skilled in the art, after which the extracts can be subjected to vacuum distillation under suitable conditions known to those skilled in the art. The extract can then be mixed with a suitable amount of dextrin and spray dried.

如剩餘說明書中所述,尤其在放大至較大體積用於生產期間,可對上述萃取製程進行修改及調節。 The above extraction process can be modified and adjusted, as described in the remainder of the specification, especially during amplification to a larger volume for production.

II. HPLC II. HPLC

隨後藉由高效液相層析表徵萃取方案1之萃取物。將約5mg/mL之試樣大小分配於25/75 MeOH/H2O中並進行超音波處理。在Zorbax SBC-18管柱(7.5cm×4.6mm,3.5um粒徑)上實施表徵且使用二極體陣列UV吸光度260nm、300nm及360nm達成檢測,圖1上之線以上升次序繪示且260nm在底部上。操作條件係流速1.5ml/min;溫度,40℃;試樣注射體積,20μL;及運行時間,19分鐘。所用流動相梯度係如下。 The extract of the extraction scheme 1 was then characterized by high performance liquid chromatography. A sample size of about 5 mg/mL was dispensed into 25/75 MeOH/H2O and subjected to ultrasonic treatment. Characterization was performed on a Zorbax SBC-18 column (7.5 cm x 4.6 mm, 3.5 um particle size) and detection was achieved using a diode array UV absorbance of 260 nm, 300 nm, and 360 nm. The lines in Figure 1 are shown in ascending order and 260 nm. On the bottom. Operating conditions were flow rate 1.5 ml/min; temperature, 40 ° C; sample injection volume, 20 μL; and run time, 19 minutes. The mobile phase gradient used is as follows.

萃取物之HPLC表徵展示於圖1中。在一個實施例中,本發明之實質上分離之萃取組合物呈現實質上類似於圖1中所繪示之HPLC概況之HPLC概況。 The HPLC characterization of the extract is shown in Figure 1. In one embodiment, the substantially isolated extraction composition of the present invention exhibits an HPLC profile substantially similar to the HPLC profile depicted in FIG.

實例2 Example 2 皮膚生物標記之活體內上調.Skin biomarkers are up-regulated in vivo.

測試山桂花之植物萃取物在活體內上調關鍵皮膚生物標記之能力。將年齡為30-65歲且具有II或III型皮膚及輕度至中度光損害之20名健康女性白人個體在前臂背側用成份處理3週(在半閉塞下連續的3輪5×24小時貼片)。在每一前臂上之5個位點上以隨機分配施用測試物件及媒劑。將每一個體用0.2%濃度下調配於丙二醇/乙醇/H2O(65:25:10)媒劑及媒劑對照中之山桂花萃取物處理。施用劑量係2mg/cm2。處理後,自每一處理位點獲得2mm衝壓活檢且將其固定於10%緩衝福爾馬林(formalin)中。隨後將組織試樣嵌入石蠟中,切片(5微米厚度),處理並染色用於以下皮膚標記-總膠原(藉由Masson Trichrome)、原膠原及玻尿酸結合蛋白(HABP)。另外,評價表皮厚度。對於每一標記,比較經處理位點與媒劑位點以測定標記強度之差別。若經處理位點中之標記強度相對於對照較高,則其指示生物標記改善。表2顯示在經山桂花萃取物治療3週後所測試皮膚生物標記具有改善之個體的百分比。 Test the ability of osmanthus plant extracts to upregulate key skin biomarkers in vivo. 20 healthy female white individuals aged 30-65 years with type II or III skin and mild to moderate photodamage were treated with ingredients for 3 weeks on the dorsal side of the forearm (3 x 24 in a row under a semi-occlusion) Hour patch). The test article and vehicle were applied at random at 5 sites on each forearm. Each individual was treated with 0.2% strength in propylene glycol/ethanol/H 2 O (65:25:10) vehicle and vehicle control in the osmanthus extract. The dose was applied at 2 mg/cm 2 . After treatment, a 2 mm punch biopsy was obtained from each treatment site and fixed in 10% buffer formalin. Tissue samples were then embedded in paraffin, sectioned (5 micron thickness), processed and stained for the following skin markers - total collagen (by Masson Trichrome), procollagen and hyaluronic acid binding protein (HABP). In addition, the thickness of the skin was evaluated. For each marker, the treated site and the vehicle site were compared to determine the difference in marker intensity. If the intensity of the marker in the treated site is higher relative to the control, it indicates an improvement in the biomarker. Table 2 shows the percentage of individuals with improved skin biomarkers tested after 3 weeks of treatment with osmanthus extract.

在活體內局部施用至皮膚時,山桂花之植物萃取物上調若干生物標記,例如表皮變厚(42.9%個體呈現增加)、膠原(55.9%個體呈現增加)、原膠原(61.3%個體呈現增加)及玻尿酸結合蛋白(63.9%個體呈現增加)。據信該等生物標記(其在老化皮膚中減少)之上調引起正老化或已老化皮膚之外觀改善。 When applied topically to the skin in vivo, the plant extract of osmanthus fragrans up-regulates several biomarkers, such as thickening of the epidermis (42.9% of individuals appearing increased), collagen (55.9% of individuals exhibiting an increase), and procollagen (61.3% of individuals exhibiting an increase) And hyaluronic acid binding protein (63.9% of individuals showed an increase). Up-regulation of such biomarkers, which are reduced in aged skin, is believed to cause an improvement in the appearance of aged or aged skin.

實例3 Example 3 活體外色素抑制活性之評價.Evaluation of in vitro pigment inhibition activity.

使B16小鼠黑色素瘤細胞(細胞系:ATCC,目錄號:CRL-6475)在96孔組織培養物處理之盤中的DMEM中生長。將細胞暴露於稀釋測試材料或媒劑對照中7天。在處理時段後,在培養基中使用分光光度計於540nm下對所產生色素之量進行定量。相對於媒劑對照,計算由測試活性物之色素產生之抑制百分比。山桂花(0.1%)抑制介於約0%至20%範圍內之色素產生。 B16 mouse melanoma cells (cell line: ATCC, catalog number: CRL-6475) were grown in DMEM in 96-well tissue culture treated dishes. Cells were exposed to dilution test material or vehicle control for 7 days. After the treatment period, the amount of the produced pigment was quantified in a medium using a spectrophotometer at 540 nm. The percent inhibition produced by the pigment of the test active was calculated relative to the vehicle control. Osmanthus fragrans (0.1%) inhibits pigment production in the range of about 0% to 20%.

實例4 Example 4 A.例示性抗脂肪團組合物 A. Exemplary anti-cellulite compositions

局部施用至呈現或處於呈現脂肪團風險下之皮膚的包含山桂花萃取物之化妝品組合物提供於表3中。 Cosmetic compositions comprising osmanthus extracts topically applied to the skin presented or at risk of presenting cellulite are provided in Table 3.

B.例示性抗老化組合物 B. Exemplary anti-aging composition

局部施用至呈現或處於呈現正老化或已老化皮膚風險下之皮膚的包含山桂花萃取物之化妝品組合物提供於表4中。 Cosmetic compositions comprising osmanthus extracts topically applied to the skin presenting or at risk of presenting aged or aged skin are provided in Table 4.

C.例示性亮膚組合物 C. Exemplary Brightening Composition

局部施用至呈現色素沉著過度體徵之皮膚之包含山桂花萃取物的化妝品組合物提供於表5中。 Cosmetic compositions comprising osmanthus extracts topically applied to the skin exhibiting hyperpigmentation signs are provided in Table 5.

據信該等組合物(上述抗脂肪團、抗老化及亮膚化妝品組合物)可 有效治療、逆轉、改善及/或預防老化體徵,特定而言,據信該等組合物可分別減輕皮膚中脂肪團、皺紋、紋及下垂之外觀及皮膚變色。可將表3至5之組合物施用至需要治療之皮膚,此意指需要抗脂肪團、抗老化或亮膚效益之皮膚。化妝品組合物可直接施用至需要治療之皮膚。 It is believed that the compositions (the above anti-cellulite, anti-aging and skin lightening cosmetic compositions) are Effectively treating, reversing, ameliorating and/or preventing signs of aging, in particular, it is believed that the compositions respectively reduce the appearance of cellulite, wrinkles, lines and sagging skin and discoloration of the skin. The compositions of Tables 3 to 5 can be applied to the skin in need of treatment, which means skin requiring anti-cellulite, anti-aging or skin lightening benefits. The cosmetic composition can be applied directly to the skin in need of treatment.

將該等化妝品組合物施用至老化或變色皮膚,每日兩次或三次,只要達成期望抗老化或亮膚結果所需即可,即可包含每日施用至少一週、至少兩週、至少四週、至少八週或至少十二週之治療方案。或者,例示性化妝品組合物可用於老化或變色皮膚之長期治療。 Applying the cosmetic compositions to aged or discolored skin twice or three times a day, as long as the desired anti-aging or skin lightening results are achieved, including daily administration for at least one week, at least two weeks, at least four weeks, Treatment regimen for at least eight weeks or at least twelve weeks. Alternatively, exemplary cosmetic compositions can be used for long-term treatment of aged or discolored skin.

包括專利申請案及公開案在內之本文所引用之所有參考文獻的全部內容出於所有目的皆以引用方式併入本文中,其併入程度就如同每一公開案或專利或專利申請案皆特別地且個別地指出其全部內容出於所有目的以引用方式併入本文中一般。彼等熟習此項技術者應瞭解,可在不背離本發明精神及範疇下對本發明實施多種修改及改變。本文所述之具體實施例僅以實例方式提供,且本發明僅受限於各項隨附申請專利範圍以及該等申請專利範圍所授權之等效物之全部範疇。 The entire contents of all of the references cited herein, including the patent application and the disclosure, are hereby incorporated by reference in entirety for all purposes in the same extent in In particular, and individually, all of its contents are hereby incorporated by reference in their entirety for all purposes. It will be appreciated by those skilled in the art that various modifications and changes can be made in the present invention without departing from the spirit and scope of the invention. The specific embodiments described herein are provided by way of example only, and the invention is limited by the scope of the accompanying claims and the scope of the equivalents.

Claims (21)

一種為有需要之老化皮膚改善美觀的方法,其包含向該皮膚局部施用於化妝品上可接受之媒劑中包含有效賦予改善皮膚美觀之量的山桂花(Maesa japonica)萃取物之組合物。 A method of improving the aesthetic appearance of an aging skin in need thereof, comprising topically applying to the skin a composition comprising a Maesa japonica extract effective to impart an aesthetically pleasing amount to a cosmetically acceptable vehicle. 如請求項1之方法,其中老化係由於年齡、激素或環境效應。 The method of claim 1, wherein the aging is due to age, hormone or environmental effects. 如請求項1之方法,其中該改善美觀係選自由以下組成之群:(a)治療、減少及/或預防細紋或皺紋,(b)減小皮膚毛孔大小,(c)改善皮膚厚度、豐滿度及/或緊實度;(d)改善皮膚柔順度及/或柔軟度;(e)改善皮膚色調、光彩(radiance)及/或透明度;(f)改善原膠原及/或膠原產生;(g)改善彈性蛋白之維持及重塑;(h)改善膚質及/或促進煥膚(re-texturization);(i)改善皮膚障壁修復及/或功能;(j)改善皮膚輪廓之外觀;(k)恢復皮膚光澤及/或亮度;(l)補充皮膚之必需營養素及/或成份;(m)改善因老化及/或停經而衰減之皮膚外觀;(n)改善皮膚濕潤性及/或水合;(o)增加及/或預防損失皮膚彈性及/或回彈性;(p)治療、減少及/或預防皮膚下垂;(q)治療、減少及/或預防皮膚變色;及其任何組合。 The method of claim 1, wherein the improving aesthetic is selected from the group consisting of: (a) treating, reducing and/or preventing fine lines or wrinkles, (b) reducing skin pore size, and (c) improving skin thickness, Fullness and/or firmness; (d) improved skin suppleness and/or softness; (e) improved skin tone, radiance and/or clarity; (f) improved procollagen and/or collagen production; (g) improving the maintenance and remodeling of elastin; (h) improving skin texture and/or promoting re-texturization; (i) improving skin barrier repair and/or function; (j) improving the appearance of skin contours (k) restore skin shine and/or brightness; (l) replenish essential nutrients and/or ingredients to the skin; (m) improve skin appearance attenuated by aging and/or menopause; (n) improve skin moistness and/or Or hydration; (o) increase and/or prevent loss of skin elasticity and/or rebound; (p) treat, reduce and/or prevent sagging of the skin; (q) treat, reduce and/or prevent skin discoloration; and any combination thereof . 如請求項1之方法,其中該皮膚係敏感性皮膚。 The method of claim 1, wherein the skin is sensitive to the skin. 如請求項1之方法,其中至少每日一次局部施用該組合物至少一週。 The method of claim 1, wherein the composition is topically applied at least once a day for at least one week. 如請求項1之方法,其中該萃取物係以基於該組合物之總重量約0.0001wt%至約90wt%之量存在。 The method of claim 1, wherein the extract is present in an amount of from about 0.0001% by weight to about 90% by weight based on the total weight of the composition. 如請求項6之方法,其中該萃取物係以該組合物之總重量之約0.01wt%至約10wt%之量存在。 The method of claim 6 wherein the extract is present in an amount from about 0.01% to about 10% by weight based on the total weight of the composition. 如請求項1之方法,其中該山桂花植物萃取物係源自該山桂花植物之花。 The method of claim 1, wherein the osmanthus plant extract is derived from the flower of the osmanthus plant. 如請求項1之方法,其中該皮膚改善歸因於膠原合成增加、玻尿酸合成增加、表皮厚度增加、黑色素合成減少;或其任何組合。 The method of claim 1, wherein the skin improvement is due to an increase in collagen synthesis, an increase in hyaluronic acid synthesis, an increase in epidermal thickness, a decrease in melanin synthesis, or any combination thereof. 一種改善皮膚之障壁功能及活力的方法,其包含向該皮膚局部施用於化妝品上可接受之媒劑中包含有效增加膠原合成、增加玻尿酸合成、增加表皮厚度、減少黑色素合成或其任何組合之量的山桂花萃取物之組合物。 A method of improving barrier function and vitality of the skin comprising topically applying to the skin a cosmetically acceptable vehicle comprising an amount effective to increase collagen synthesis, increase hyaluronic acid synthesis, increase epidermal thickness, reduce melanin synthesis, or any combination thereof. The composition of the mountain osmanthus extract. 如請求項10之方法,其中該萃取物係源自山桂花之花。 The method of claim 10, wherein the extract is derived from the flower of the osmanthus flower. 如請求項10之方法,其中該植物萃取物係以基於該組合物之總重量約0.0001wt%至約90wt%之量存在。 The method of claim 10, wherein the plant extract is present in an amount of from about 0.0001% by weight to about 90% by weight, based on the total weight of the composition. 如請求項12之方法,其中該植物萃取物係以基於該組合物之總重量約0.01wt%至約10wt%之量存在。 The method of claim 12, wherein the plant extract is present in an amount of from about 0.01% by weight to about 10% by weight based on the total weight of the composition. 一種治療皺紋、細紋或下垂皮膚之方法,其包含向該皮膚局部施用於化妝品上可接受之媒劑中包含有效治療該有需要皮膚之量的山桂花萃取物之組合物。 A method of treating wrinkles, fine lines or sagging skin comprising topically applying to the skin a cosmetically acceptable vehicle comprising a composition of an extract of osmanthus fragrans extract effective to treat the skin in need thereof. 一種使有需要之皮膚光亮之方法,其包含向該皮膚局部施用於化妝品上可接受之媒劑中包含有效達成光亮效益之量的山桂花萃取物之組合物。 A method of illuminating a skin in need thereof, comprising topically applying to the skin a composition comprising a osmanthus extract in an amount of a cosmetically acceptable vehicle comprising an amount effective to achieve a luminous benefit. 如請求項15之方法,其中該光亮效益係選自由以下組成之群:(a)漂白色素沉著過度之毛髮、皮膚、唇及/或指甲;(b)減少老人斑;(c)使皮膚變色均勻或最佳化;(d)改善眼下暗圈之外觀;(e)治療黑斑(melasma)、黃褐斑(cholasma)、雀斑、燒傷後疤痕及損傷後色素沉著過度;(f)漂白頭皮、腿、臉部及其他期望漂白及減少顏色之區域上之毛髮;(g)漂白指甲染色;及其組合。 The method of claim 15, wherein the luminous benefit is selected from the group consisting of: (a) bleaching hyperpigmented hair, skin, lips and/or nails; (b) reducing age spots; (c) discoloring the skin Uniform or optimized; (d) improve the appearance of the dark circles under the eyes; (e) treat melasma, chollas, freckles, scars after burns and hyperpigmentation after injury; (f) bleaching scalp , hair on the legs, face and other areas where bleaching and color reduction are desired; (g) bleaching nail staining; and combinations thereof. 如請求項15之方法,其中該光亮效益係由於黑色素合成減少。 The method of claim 15, wherein the luminous benefit is reduced due to melanin synthesis. 如請求項17之方法,其中該黑色素合成減少約20%至100%。 The method of claim 17, wherein the melanin synthesis is reduced by about 20% to 100%. 如請求項18之方法,其中該黑色素合成減少約40%至100%。 The method of claim 18, wherein the melanin synthesis is reduced by about 40% to 100%. 如請求項15之方法,其中該植物萃取物係以基於該組合物之總重量約0.01wt%至約10wt%之量存在。 The method of claim 15, wherein the plant extract is present in an amount of from about 0.01% by weight to about 10% by weight based on the total weight of the composition. 一種治療皮膚之方法,其包含向有需要之皮膚區域局部施用有效量之調節皮膚生物標記之山桂花萃取物,其中該山桂花萃取物調節皮膚生物標記之能力已藉由測量選自包含以下之群之皮膚生物標記之變化量的分析測定:表皮變厚、總膠原、原膠原、及已與該山桂花萃取物接觸之皮膚細胞及/或皮膚細胞分化前之前體中之玻尿酸結合蛋白。 A method of treating skin comprising topically applying an effective amount of a scented osmanthus extract to a skin area in need thereof, wherein the osmanthus extract has the ability to modulate a skin biomarker having been selected from the group consisting of Analysis of the amount of change in the skin biomarker of the group: thickening of the epidermis, total collagen, procollagen, and hyaluronic acid binding protein in the skin cells before and after differentiation of the skin cells and/or skin cells that have been in contact with the osmanthus extract.
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