TW520286B - Skin whitening composition - Google Patents
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五、發明說明(1) 、 相關申請案 本申請案係為1998年6月30日提出及目前審理令之美 國申請序號09/⑽,107之部分延續申請案,其係以1998年 4月29日提出之美國臨時中請序號6議3,為基礎及就其優 先權申請專利。 發明之技術領域 本發明係有關-種新的皮膚美白摻合物,其係為一種 低色素沈著的組成成份與一種抗氧化劑之協同組合物。將 f皮膚美白摻合物進_步地納人—適宜的局部載劑中,以 提供-皮膚美白組成物。選擇性地,該皮膚美白摻合物亦 可包含一種防曬劑及/或一種皮膚細胞更新速率之促進劑 發明之目標 本發明之一目標係提供一種有效的皮膚美白摻合物, 其包含一種低色素沈著的組成成份與一種抗氧化劑。 本發明之另一目標係提供一種有效的皮膚美白摻合物 ,其進一步包含一種防曬劑及/或一種皮膚細胞更新速率 之促進劑。 本發明之另一目標係提供一種有效的皮膚美白組成物 ,其係將本發明的皮膚美白摻合物納於一藥學上極佳的局 部載劑中。 本發明之另一目標係提供一種有效的皮膚美白組成物 ’其係為一乳霜。 4 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297 ^7 ^0286 A7 B7 經 濟 部 智 慧 財 產 局 員 工 消 費 合 作 社 印 製 五、發明說明(2) 本發明之另一目標係提供二種有效的皮膚美白組成物 ,其係為一乳液、溶液、水醇液體、粉末、潤膚膏或皮膚 貼布。 較佳具體例之說明 本發明係有關一種皮膚美白摻合物(此後稱作”皮膚 美白摻合物),其係納於一適宜的局部載劑中,以構成 本發明之整體的皮膚美白組成物。除非另外界定,在此所 揭路之百分比係為整體的皮膚美白組成物(此後稱作,,組 成物”)之重量百分比。 適用於本發明之局部載劑包括乳霜、乳液、溶液、水 醇液體、潤膚膏、粉末與皮膚貼布。 該組成物之活性/功效在此係界定為淡化膚色、均勻 化膚色/色澤、減少日曬斑(老年斑)或汗斑(雀斑)之 出現、減少黑斑病、減少褐黃斑、減少發炎後之過度色素 沈著作用、減少色素沈著型角質化病、及/或減少日曬所 引發的任何損傷。 本發明的第-具體例,係為具有一皮膚美白換合物之 -種組成物。該皮膚美白摻合物具有_種低色素沈著的組 成成份與一種抗氧化劑。在本發明的第二具體例中,該皮 膚美白摻合物具有-種增強或加速皮膚細胞更新速率之組 成成份(此後稱作,,促進劑”)。在本發明的第三具體例中 ,該皮膚美白摻合物具有低色素沈著的組成成份、抗氧化 劑與-種防曬劑,而第四具體例具有所有三種成份再加上 本紙張尺度適用中國國家標準(CNSM_4規格⑵〇 x 297公着丁 --------------裝--------訂---------線 (請先閱讀背面之注意事項再填寫本頁) 520286V. Description of the Invention (1) Relevant Application This application is a partial continuation application of the US application serial number 09 / ⑽, 107 filed on June 30, 1998 and the current trial order, which is based on April 29, 1998. The US Provisional Chinese Serial No. 6 and 3 filed on the basis of Japan and applied for a patent based on its priority. TECHNICAL FIELD OF THE INVENTION The present invention relates to a new skin lightening blend, which is a synergistic composition of a low pigmentation component and an antioxidant. The f skin whitening blend is incorporated into a stephena-a suitable topical vehicle to provide-a skin lightening composition. Optionally, the skin whitening blend may also include a sunscreen and / or a skin cell regeneration rate promoter. An object of the present invention is to provide an effective skin whitening blend comprising a low Pigmented ingredients with an antioxidant. Another object of the present invention is to provide an effective skin lightening blend, which further comprises a sunscreen agent and / or a skin cell regeneration rate promoting agent. Another object of the present invention is to provide an effective skin-whitening composition which incorporates the skin-whitening blend of the present invention in a pharmaceutically excellent local carrier. Another object of the present invention is to provide an effective skin lightening composition 'which is a cream. 4 This paper size applies to China National Standard (CNS) A4 specifications (210 X 297 ^ 7 ^ 0286 A7 B7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (2) Another object of the present invention is to provide two An effective skin whitening composition, which is an emulsion, solution, hydroalcoholic liquid, powder, moisturizer or skin patch. DESCRIPTION OF PREFERRED EMBODIMENTS The present invention relates to a skin lightening blend (hereinafter referred to as " Skin lightening blend), which is contained in a suitable topical vehicle to form the overall skin lightening composition of the present invention. Unless otherwise defined, the percentages disclosed herein are the overall skin lightening composition (Hereinafter referred to as "composition") by weight. Topical carriers suitable for use in the present invention include creams, lotions, solutions, hydroalcoholic liquids, body creams, powders, and skin patches. The activity of the composition / Efficacy is defined here as lightening skin tone, homogenizing skin tone / color, reducing the appearance of sun spots (age spots) or sweat spots (freckles), reducing dark spots, reducing brown spots, reducing Excessive hyperpigmentation after inflammation, reducing pigmentation-type keratosis, and / or reducing any damage caused by sun exposure. The first specific example of the present invention is a composition having a skin-whitening exchange agent The skin whitening blend has a low pigmentation component and an antioxidant. In a second specific example of the present invention, the skin whitening blend has a component that enhances or accelerates the rate of skin cell regeneration (Hereinafter referred to as "accelerator".) In the third specific example of the present invention, the skin whitening blend has a low pigmentation component, an antioxidant, and a sunscreen, and the fourth specific example has all The three ingredients plus this paper size are applicable to Chinese national standards (CNSM_4 specifications ⑵〇x 297 public Ding -------------- installed -------- order ---- ----- Line (Please read the precautions on the back before filling this page) 520286
第二具體例之促進劑。 用於所有四個具體例之低色素沈著的組成成份包括下 列的成份:⑴一種甘草萃取物;(ii)包含至少一種下列萃 取物之一天然萃取物:金縷梅丹寧、桑椹、虎耳草、黃芩 、葡萄、小球藻、熊莓、越桔、歐洲越橘、糖蜜、梨、蕃 石榴或其混合物;及(iii)如⑴中所界定之甘草萃取物與如 (11)中所界定之一天然萃取物摻合物(此後稱作,,天然萃取 換合物)之一種換合物。 有關天然卒取物(ii) ’若單獨使用,則任一天然萃取 物皆具有低色素沈著的活性。然而,為達到使用者所需之 淡化膚色的程度,該天然萃取物較佳為選自下列群中的至 少二種萃取物之混合物:金縷梅丹寧、桑椹、虎耳草、黃 芩、葡萄、小球藻、熊莓、越桔、歐洲越橘、糖蜜、梨及 蕃石榴(此後稱作”天然萃取混合物”)。在第二個較佳的 具體例中,天然萃取混合物具有梨及蕃石榴萃取物。在一 個更佳的具體例中,天然萃取混合物具有所有的下列萃取 物:金縷梅丹寧、桑椹、虎耳草、黃芩、葡萄、小球藻、 能每、越桔、歐洲越橘及糖蜜。在一個最佳的具體例中, 天然萃取混合物具有下列的萃取物:金縷梅丹寧、桑椹、 虎耳草、黃芩、葡萄及熊莓。當萃取物係為桑椹萃取物或 虎耳卓卒取物時’較佳至少*部份的萃取物係取自其根部 〇 當低色素沈著的組成成份具有一種甘草萃取物時,可 本纸張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) -----------I ^--- (請先閱讀背面之注咅?事項再填寫本頁} 二. 經濟部智慧財產局員工消費合作社印製 6 520286 A7 ^---- B7 ------------ 五、發明說明(4) 、使用一水溶性(或含水的)或一油溶性甘草萃取物。 (請先閱讀背面之注意事項再填寫本頁) 適宜的水溶性甘草萃取物之實例為羥基式甘草萃取物 、醇式甘草萃取物及其組合物。若使用水溶性甘草萃取物 ’甘卓卒取物的》辰度係南於約0.001重量%至3〇重量%。 油溶性甘草萃取物係為較佳的甘草萃取物。較佳,油 溶性甘草萃取物係為粉末形式,及約為組成物之〇 〇〇1重 量%至5.0重量%,更佳約為〇.0〇2重量%至1〇重量%。甚至 更佳係油溶性甘草萃取物約為組成物之〇 重量%至〇.2 重量%。最佳係該油溶性組成物約為組成物之〇〇5重量% 至0· 1重量%。該油溶性甘草萃取物可具有一或多種下列 成份·葛拉柏鍵(glabridin)、葛拉賓(giabrene)、7-經基-4,-曱氧異黃酮、葛拉柏拉(glabrol)及其他相關的酚式化合物 。紛式化合物的實例可包括依斯帕葛拉柏錠 (hisPaglabridin)-A、4,-鄰-甲基葛拉柏錠(glabridin)及3,_羥 基-4’-鄰·甲基葛拉柏旋(giabfidin)。 經濟部智慧財產局員工消費合作社印制农 低色素沈著的組成成份較佳係為甘草萃取物⑴。用於 該組成物之低色素沈著的組成成份更佳為天然萃取摻合物 (iii)(其包括甘草萃取物⑴與天然萃取物(ii)二者)。然而 ,該低色素沈著的組成成份甚至更佳為甘草萃取物⑴的較 佳具體例與天然萃取混合物(Π)的更佳的第一具體例之組 合物。該低色素沈著的組成成份最佳為甘草萃取物⑴的最 佳具體例與天然萃取混合物(ii)的最佳的第一具體例之組 合物。 本紙張尺度適用中國國家標準(CNS)A4規格(210 x 297公釐) 經濟部智慧財產局員工消費合作社印製 520286 A7 _ B7 五、發明說明(5) 若該低色素沈著的組成成份係為如(ii)所界定之天然 萃取物的混合物,該天然萃取混合物具有約佔混合物〇1 重量%至99重量%之至少二種下列的萃取物··金縷梅丹寧 (維吉尼亞金縷梅(Hamamelis virginiana))、桑椹、虎 耳草、黃答、葡萄、小球藻(Chlorella vulgaris )、熊莓 (Arctostaphylos uva ursi) '越桔(Vaccinium vitiQ )、歐洲越橘(Vaccinium myrtillns)、糖蜜(黑糖)。 天然萃取混合物之第二實例具有約0.1重量%至99重 量%之金縷梅丹寧萃取物,及約〇.〇1重量%至99重量%之 下列各萃取物:桑椹、虎耳草、黃芩、葡萄及熊莓。更佳 ,天然萃取混合物之第二實例具有約5重量%至30重量% 之金縷梅丹寧萃取物,及約0.1重量%至1〇重量%之下列各 萃取物··桑椹、虎耳草、黃芩、葡萄及熊莓。 天然萃取混合物之第三實例具有約〇· 1重量%至99重 量%之金縷梅丹寧萃取物,及約〇.〇1重量%至99重量%之 下列各萃取物:桑椹、虎耳草、黃芩、葡萄、小球藻、熊 莓、越桔、歐洲越橘及糖蜜。更佳,天然萃取混合物之第 三實例具有約5重量%至30重量%之金縷梅丹寧萃取物,及 約0·1重量%至1〇重量%之下列各萃取物:桑椹、虎耳草、 黃芩、葡萄、小球藻、熊莓、越桔、歐洲越橘及糖蜜。 天然萃取混合物之第四實例具有約0.01重量%至99重 量%之梨萃取物,及約0.01重量%至99重量%之蕃石榴萃 取物。更佳,天然萃取混合物之第四實例具有約〇· 1重量 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) (請先閱讀背面之注意事項再填寫本頁)Accelerator of the second specific example. The low-pigmentation ingredients used in all four specific examples include the following: ⑴ a licorice extract; (ii) a natural extract containing at least one of the following extracts: witch hazel tannin, mulberry, tiger ear Grass, Scutellaria baicalensis, grapes, chlorella, bilberry, bilberry, bilberry, molasses, pear, guava or mixtures thereof; and (iii) licorice extract as defined in ⑴ and as described in (11) One of the definitions is a natural extract blend (hereinafter referred to as, natural extraction permeate). Concerning natural extracts (ii) ’When used alone, any natural extract has low pigmentation activity. However, in order to reduce the skin tone desired by the user, the natural extract is preferably a mixture of at least two extracts selected from the group consisting of witch hazel tannin, mulberry, saxifraga, scutellaria baicalensis, grapes , Chlorella, bearberry, bilberry, bilberry, molasses, pear, and guava (hereinafter referred to as "natural extract mixture"). In a second preferred embodiment, the natural extract mixture has pear and guava extracts. In a more specific embodiment, the natural extract mixture has all of the following extracts: witch hazel tannin, mulberry, saxifraga, scutellaria baicalensis, grapes, chlorella, canola, bilberry, bilberry, and molasses . In a preferred embodiment, the natural extraction mixture has the following extracts: Witch Hazel Tannin, Mulberry, Saxifraga, Scutellaria baicalensis, Grape and Bearberry. When the extract is a mulberry extract or tiger ear extract, it is preferred that at least part of the extract is taken from its root. When the low pigmentation component has a licorice extract, this paper can be used. Standards are applicable to China National Standard (CNS) A4 (210 X 297 mm) ----------- I ^ --- (Please read the note on the back? Matters before filling out this page} 2. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 6 520286 A7 ^ ---- B7 ------------ 5. Description of the invention (4), use of a water-soluble (or water-containing) or a Oil-soluble licorice extract. (Please read the notes on the back before filling out this page) Examples of suitable water-soluble licorice extracts are hydroxy-licorice extract, alcohol-type licorice extract, and combinations thereof. If water-soluble licorice is used The extract of "Ganzhuo extract" is about 0.001% to 30% by weight. The oil-soluble licorice extract is a better licorice extract. Preferably, the oil-soluble licorice extract is a powder Form, and about 0.001% to 5.0% by weight of the composition, more preferably about 0.02% to 1% by weight 0% by weight. Even more preferably, the oil-soluble licorice extract is about 0% to 0.2% by weight of the composition. The most preferable is that the oil-soluble composition is about 0.05% by weight to 0.1 of the composition. % By weight. The oil-soluble licorice extract may have one or more of the following ingredients: glabridin, giabrene, 7-Cyclo-4,-oxo-isoflavone, glabra ( glabrol) and other related phenolic compounds. Examples of the compounds may include hisPaglabridin-A, 4, -o-methylglabridin and 3, _hydroxy- 4'-o-methyl gabfidin. The low-pigmentation component of the printed agricultural product printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs is preferably licorice extract. The low-pigmentation used for this composition The composition is more preferably natural extract blend (iii) (which includes both licorice extract ⑴ and natural extract (ii)). However, the composition with low pigmentation is even more preferably licorice extract ⑴ Preferred specific example and better first specific example of natural extract mixture (Π) Composition. The composition of the low pigmentation is preferably the combination of the best specific example of the licorice extract ⑴ and the best first specific example of the natural extract mixture (ii). This paper size applies the Chinese national standard (CNS ) A4 size (210 x 297 mm) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 520286 A7 _ B7 V. Description of the invention (5) If the composition of the low pigmentation is a natural extract as defined in (ii) The natural extract mixture has at least two types of the following extracts, which are about 0.01% to 99% by weight of the mixture: witch hazel tannin (Hamamelis virginiana), mulberry , Saxifraga, yellow answer, grape, Chlorella vulgaris, Arctostaphylos uva ursi 'Vaccinium vitiQ, Vaccinium myrtillns, molasses (black sugar). The second example of the natural extraction mixture has about 0.1% to 99% by weight of witch hazel tannin extract, and about 0.01% to 99% by weight of each of the following extracts: mulberry, saxifraga, scutellaria , Grapes and bear berries. More preferably, the second example of the natural extraction mixture has about 5% to 30% by weight of witch hazel tannin extract, and about 0.1% to 10% by weight of each of the following extracts: mulberry, saxifraga , Scutellaria baicalensis, grapes and bear berries. The third example of the natural extraction mixture has a witch hazel tannin extract of about 0.1% to 99% by weight, and about 0.01 to 99% by weight of each of the following extracts: mulberry, saxifraga , Scutellaria baicalensis, grapes, chlorella, bearberry, bilberry, bilberry and molasses. More preferably, the third example of the natural extraction mixture has about 5% to 30% by weight of witch hazel tannin extract, and about 0.1% to 10% by weight of each of the following extracts: mulberry, tiger ear Grass, Scutellaria baicalensis, Grape, Chlorella, Bearberry, Bilberry, European Bilberry and Molasses. A fourth example of the natural extraction mixture has a pear extract of about 0.01% to 99% by weight, and a pomegranate extract of about 0.01% to 99% by weight. More preferably, the fourth example of the natural extract mixture has a weight of about 0.1. The paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) (Please read the precautions on the back before filling this page)
520286520286
經濟部智慧財產局員工消費合作社印製 %至10重1%之梨萃取物,及約〇1重量%至1〇重量%之蕃 石榴萃取物。 本發明的所有四個具體例中之第二組成成份,係為一 抗氧化劑。該抗氧化劑可包括下列萃取物··綠茶、逑迭香 (此後稱作,,迷迭香 ”)、^穀 維素、生育酚或生育酚衍生物、四氫薑黃色素或其混合物 。雖然當個別使用時,前述的抗氧化劑皆具有活性,該抗 氧化劑較佳係為至少二種抗氧化劑萃取物。該抗氧化劑最 佳為所有四種抗氧化劑之混合物。組成物中之抗氧化劑總 量約為0.0001重量%至50重量%。 綠茶萃取物可為含水式、醇式、羥基式、油可混溶的 粉末,或其組合物。若綠茶萃取物係為含水式、醇式或羥 基式’則該綠茶萃取物約為該組成物之〇 〇〇〇1重量%至3〇 重量%。 该綠茶萃取物較佳為一種綠茶萃取粉末,其中多盼的 最低含量約為綠茶萃取粉末的65重量%,及該多盼含量包 含表兒茶酸沒食子酸酯(ECG)與表掊兒茶素沒食子酸酯 (EGCG )。然而,多酚含量中可包含其他附加的成份。 當使用上所界定具有多酚含量之綠茶萃取粉末時,該組成 物約為綠茶萃取粉末之〇.〇〇〇1重量%至5.0重量%,更佳約 為綠茶萃取粉末之0.0001重量%至1 ·〇重量〇/〇。 迷迭香卒取物可為含水式、醇式、經基式、油可混溶 的粉末’或其組合物。迷迭香萃取物約為0 001重量%至30 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐)Printed by the Consumers' Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs from 10% to 10% by weight of 1% pear extract and about 0.01% by weight to 10% by weight of pomegranate extract. The second component in all four specific examples of the present invention is an antioxidant. The antioxidant may include the following extracts: green tea, rosemary (hereafter, rosemary), oryzanol, tocopherol or tocopherol derivatives, tetrahydroturmeric pigment or mixtures thereof. When used individually, the aforementioned antioxidants are all active. The antioxidant is preferably at least two antioxidant extracts. The antioxidant is preferably a mixture of all four antioxidants. The total amount of antioxidants in the composition is about 0.0001% to 50% by weight. The green tea extract may be an aqueous, alcoholic, hydroxy, oil-miscible powder, or a combination thereof. If the green tea extract is an aqueous, alcoholic, or hydroxy type ' Then, the green tea extract is about 0.001% to 30% by weight of the composition. The green tea extract is preferably a green tea extract powder, and the lowest content of Dopan is about 65 weight of the green tea extract powder. %, And the polyphenol content includes epicatechin gallate (ECG) and epigallocatechin gallate (EGCG). However, other additional ingredients may be included in the polyphenol content. When used As defined above When the green tea extract powder has a polyphenol content, the composition is about 0.0001% to 5.0% by weight of the green tea extract powder, and more preferably about 0.0001% to 1.0% by weight of the green tea extract powder. 〇. Rosemary extract can be water-based, alcohol-based, base-based, oil-miscible powder 'or a combination thereof. Rosemary extract is about 0 001% by weight to 30 This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm)
9 量/〇約為92重虿%至98重量%乾燥粉末之油可混溶的 迟迭香萃取物,係為較佳。當使用該油可混溶的迷迭香萃 取粉末時,該組成物約為迷迭香萃取粉末之0.001重量% 至15重里彳,更佳約為迷迭香萃取粉末之〇.〇5重量%至5重 量% 〇 抗氧化劑亦可具有約0.001重量%至15重量%,更佳約 0·01重量%至5重量%之丫·穀維素。抗氧化劑組成物進一步 包括約0.01重量%至10重量%,更佳約〇1重量%至5重量% 之生育酚或生育酚衍生物。適宜的生育酚衍生物的實例為 維他命Ε乙酸酯、他命Ε菸酸酯及他命Ε亞油酸酯。 四氫薑黃色素係為較佳的抗氧化劑。在一個較佳具體 例中’四氫薑黃色素係以約〇〇〇1重量%至2〇重量%之一量 存在。在一個更佳具體例中,四氫薑黃色素係以約01重 量%至1〇重量%之一量存在,及最佳係以約〇.5重量%至5 重置%之一量存在。本發明的抗氧化劑較佳包括四氫薑黃 色素。 發現當分別相較於四氫薑黃色素或一種天然萃取物之 低色素沈著摻合物時,本發明之皮膚美白組成物,其同時 具有四氫薑黃色素及一種天然萃取物之低色素沈著摻合物 ’展現一未預期的協同性美白/去色素沈著之活性。 進行三種皮膚美白組成物之活體比較測試,測量在暴 露於1 MED (最低紅斑劑量)光照之後,皮膚色素沈著作 用之產生。試樣A、B與C之活性組成成份如下所列。 10 本紙張尺度適用中國國家標準(CNS)A4規格(2〗〇 x 297公爱) 520286 . Α7 Β7 經濟部智慧財產局員工消費合作社印製 五、發明說明(8) 試樣A 3.6.9- 三氧雜十一烷二酸 維他命E乙酸酯 γ-穀維素 迷迭香萃取粉末 甘草萃取物(油可混溶的粉末) 綠茶萃取粉末 桑椹萃取粉末 熊莓萃取粉末 金縷梅丹寧萃取物 虎耳草萃取物 葡萄萃取物 桑椹根部萃取物 黃芩根部萃取物 試樣Β 3.6.9- 三氧雜十一烷二酸 維他命Ε乙酸酯 γ-榖維素 迷迭香萃取粉末 甘草萃取物(油可混溶的粉末) 綠茶萃取粉末 桑椹萃取粉末 熊莓萃取粉末 (請先閱讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 11 520286 A7 B7 五、發明說明(9) 葡萄萃取物 _ 桑椹根部萃取物 黃芩根部萃取物 四氫薑黃色素 試樣C 四氫薑黃色素 對照組 未經處理的皮膚 以試樣A、B或C處理一人類古倉 貝皮膚區域,然後暴露於相 當於1刪(最低紅斑劑量)之光照。觀察該測試區域達 8天的期間,及自第4至8天進行每日觀察。測試結果示於 下列的第1表。 第1表 作用之程;t * * (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 對照組 0.5 試樣A 0.2 試樣B 0.1 試樣C 0.3 **所觀察到的色素沈著作用之程度隨著數值之減小而降低 ,亦即0.3的色素沈著程度係低於〇.5。 如第1表所示的結果顯示,相較於未具有四氫薑黃色 素之皮膚美白組成物或四氫薑黃色素本身而言,存在於本 發明的皮膚美白組成物中之四氫薑黃色素,產生一未預期 表紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公爱 ϋ I ^OJ1 ϋ n I «I ϋ n I I 一 520286 .經濟部智慧財產局員工消費合作社印製 A7 B7 五、發明說明(1¾ 的協同性美白效應。 包含==第:具體例中,該皮膚美白摻合物進-步 率 A 4促進劑有助於增加皮膚細胞之更新速 率=強化本發明的第—具體例之皮膚美白活性。 稱作,,氧雜r,,rM之實例係為氧雜酸、氧雜二酸(此後亦 類視色素與類視色素衍生物,其較佳為 1見:醇衍生物。較佳,該組成物具有約。篇重 里二至10重里之促進劑。若該促進劑係為視黃醇或一種 視百醇衍生物’則該組成物具有物Q1重量%至5重量% ^見讀或視黃醇射物。若該促進劑係為-種類視色素 ϋ見色讀生物,職㈣色錄佳為視料或-種視 * 丁生物;^促進劑係為—種氧雜酸或氧雜酸之一电 合物,該組成物較佳具有約0.5重量%至1〇重量%之氧雜酸 。適用於本發明之氧雜酸揭露於共審查中之美國專利申請 案序號_6,54Q與_58,_。前述各專利中請案之整 個揭路内合,在此併入本案以為參考資料。若使用一種氧 雜酸,則該組成物較佳具有約0.5重量%至1〇重量%之3,6,9_ ,氧雜十m此外,若該促進劑麵_種氧雜酸或 氧雜酸之-組合物’則該組成物之酸驗值最佳約為3·5至 4.5。 、皮膚美白摻合物之第三具體例具有低色素沈著的組成 成伤、抗氧化劑及進-步地包含_種防曬劑。該防暖劑可 為技藝中已知適用於局物組成物之任一種防曬劑或二或多 本纸張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐)9 Amount / 〇 About 92% by weight to 98% by weight of dry powder oil-miscible oils of late rosemary is preferred. When the oil-miscible rosemary extract powder is used, the composition is about 0.001% to 15% by weight of the rosemary extract powder, and more preferably about 0.05% by weight of the rosemary extract powder. The antioxidant may also have about 0.001% to 15% by weight, more preferably about 0.01% to 5% by weight of oryzanol. The antioxidant composition further comprises about 0.01 to 10% by weight, more preferably about 0.01 to 5% by weight of tocopherol or tocopherol derivative. Examples of suitable tocopherol derivatives are vitamin E acetate, vitamin E nicotinate, and vitamin E linoleate. Tetrahydrocurcumin is a preferred antioxidant. In a preferred embodiment, ' tetrahydrocurcumin is present in an amount of about 0.001% to 20% by weight. In a more specific embodiment, the tetrahydrocurcumin is present in an amount of about 01% to 10% by weight, and the most optimal is present in an amount of about 0.5% to 5% by weight. The antioxidant of the present invention preferably includes a tetrahydroturmeric pigment. It was found that the skin lightening composition of the present invention has both a low-pigmentation blend of tetrahydroturmeric pigment and a natural extract when compared to a low-pigmentation blend of tetrahydroturmeric pigment or a natural extract, respectively. It exhibits an unexpected synergistic whitening / depigmentation activity. A live comparison test of three skin whitening compositions was performed to measure the production of skin pigmentation after exposure to 1 MED (minimum erythema dose). The active components of Samples A, B, and C are listed below. 10 This paper size applies the Chinese National Standard (CNS) A4 specification (2) 0x 297 public love) 520286. Α7 Β7 Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 5. Description of the invention (8) Sample A 3.6.9- Trioxundecanoic acid vitamin E acetate γ-oryzanol rosemary extract powder licorice extract (oil-miscible powder) green tea extract powder mulberry extract powder bearberry extract powder witch hazel tannin extract Saxifraga extract Grape extract Mulberry root extract Scutellaria baicalensis root extract sample B 3.6.9- Trioxaundecane diacid vitamin E acetate γ-Ivytin rosemary extract powder licorice extract (Oil-miscible powder) Green tea extract powder, mulberry extract powder, bearberry extract powder (please read the precautions on the back before filling out this page) This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 11 520286 A7 B7 V. Description of the invention (9) Grape extract _ Mulberry root extract Scutellaria baicalensis root extract Tetrahydrocurcumin sample C Tetrahydrocurcumin control group Take samples A, B or C Organize the skin area of human Gu Cangbei, and then expose it to light equivalent to 1 (lowest erythema dose). The test area was observed for a period of 8 days, and daily observations were performed from days 4 to 8. The test results are shown in Table 1 below. Table 1 Process of action; t * * (Please read the notes on the back before filling out this page) Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs Control group 0.5 Sample A 0.2 Sample B 0.1 Sample C 0.3 ** The degree of pigmentation observed decreases with decreasing values, that is, the degree of pigmentation of 0.3 is less than 0.5. The results shown in Table 1 show that the tetrahydroturmeric pigment present in the skin whitening composition of the present invention produces more tetrahydroturmeric pigment than the skin whitening composition without tetrahydrocurcumin or the tetrahydrocurcumin itself, The paper size of the table is not expected to apply the Chinese National Standard (CNS) A4 specification (210 X 297 public love ϋ I ^ OJ1 ϋ n I «I ϋ n II 520286. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 B7 V. Description of the invention (1¾) Synergistic whitening effect. Include == No .: In the specific example, the skin whitening blend step-up rate A 4 promoter helps to increase the rate of skin cell renewal = strengthen the No. 1 -Specific of the invention Examples of skin whitening activity. Examples of oxa r ,, rM are oxa acids and oxa diacids (hereafter also retinoids and retinoid derivatives, which are preferably 1 see: alcohol derivative Preferably, the composition has an accelerator of about 2 to 10 weight. If the accelerator is a retinol or a retinol derivative, then the composition has a weight of 1 to 5 weight percent. % ^ See reading or retinol projectiles. If this promotes It is a kind of visual pigment, a color reading organism, and an occupational color record is preferably a visual material or a kind of spectroscopy; a promoter is a kind of oxa acid or an oxa acid complex. The material preferably has about 0.5 to 10% by weight of oxalic acid. The oxalic acid suitable for the present invention is disclosed in the co-examined US patent application serial numbers _6,54Q and _58, _. Each of the aforementioned patents The entire solution of the Chinese patent application is incorporated here, and is incorporated herein as reference material. If an oxa acid is used, the composition preferably has about 3,6,9_ of about 0.5% to 10% by weight of oxygen. In addition, if the surface of the accelerator is _ a kind of oxa acid or oxa acid-composition, the acid test value of the composition is preferably about 3.5 to 4.5. Three specific examples have a composition with low pigmentation, wounds, antioxidants, and further contain _ sunscreen agents. The warming agent may be any sunscreen agent or two or more sunscreen agents known in the art to be suitable for local composition. This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)
I I I I --- (請先閱讀背面之注意事項再填寫本頁) · -線· 13 520286 A7I I I I --- (Please read the notes on the back before filling out this page) · -line · 13 520286 A7
五、發明說明(11) 種防曬劑之組合物。該防曬劑約為組成物之0.001重量% 至40重量%,更佳約為3重量%至25重量%。 經濟部智慧財產局員工消費合作社印別农 適宜的防曬劑之實例及其適宜的濃度如下··約0.001 重量%至10重量%之肉桂酸乙基己基對-甲氧酯(適宜的肉 桂酸乙基己基對-曱氧酯之非限制性實例係為該等以商品 名”Parsol MCX” 自 Givaudan Corporation公司取得者、以商 品名”Escalol 557” 自 Van Dyk Incorporation公司取得者、 以商品名”Neo Heliopan Αν” 自 Haarman & Reimer Corporation公司取得者及以商品名”Uvinul MC80”自BASF 公司取得者);約〇.〇〇1重量%至1〇重量%之氧苯酮或二苯 甲酮-3 (適宜的氧苯酮之非限制性實例係為該等以商品名 ”Escalol 567,,自ISP Van Dyk公司取得者、以商品名”Uvinul M40”自BASF公司取得者、以商品名”Syntase 62”自Neville Synthese Chem.公司/Rhone Poulenc (Rhodia公司)取得者 及以商品名”Eusolex 4360”產品 #605376 自 Rona/EM Ind.公 司取得者);約0.001重量%至10重量%之磺異苯酮;約0.001 重量%至3.0重量%之二氧苯酮;約0.001重量%至5重量% 之鄰胺基苯曱酸蓋酯;約0.001重量%至25重量%之二氧化 鈦;約0.001重量%至20重量%之氧化鋅;約0.001重量%至 10重量%之類黃酮或其衍生物;約0.001重量%至10重量% 之丁基曱氧二苯甲醯基甲烷(適宜的丁基甲氧二苯甲醯基 甲烷之非限制性實例係以商品名”Pai:sol-1789”產品#64030 自Roche Inc.公司取得);約0.001重量%至10重量%之4- 14 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 520286 .經濟部智慧財產局員工消費合作社印製5. Description of the invention (11) A combination of sunscreen agents. The sunscreen is about 0.001% to 40% by weight of the composition, and more preferably about 3% to 25% by weight. Examples of suitable sunscreens for employees of the Intellectual Property Bureau of the Ministry of Economic Affairs, Consumer Cooperatives, and their suitable concentrations are as follows: about 0.001% to 10% by weight of ethylhexyl p-methoxycinnamate (suitable ethyl cinnamate) Non-limiting examples of p-hexyl esters are those obtained under the trade name "Parsol MCX" from Givaudan Corporation, and under the trade name "Escalol 557" from Van Dyk Incorporation, under the trade name "Neo Heliopan Αν ”obtained from Haarman & Reimer Corporation and obtained from BASF under the trade name“ Uvinul MC80 ”); about 0.0001% to 10% by weight of oxybenzone or benzophenone- 3 (Non-limiting examples of suitable oxyphenones are those obtained under the trade name "Escalol 567, obtained from ISP Van Dyk, under the trade name" Uvinul M40 "from BASF, under the trade name" Syntase 62 "obtained from Neville Synthese Chem./Rhone Poulenc (Rhodia) and product under the trade name" Eusolex 4360 "# 605376 (from Rona / EM Ind.); Approximately 0.001% by weight 10% by weight of sulfoisophenone; about 0.001% by weight to 3.0% by weight of dioxophenone; about 0.001% by weight to 5% by weight of o-aminophenylbenzoic acid caprylate; about 0.001% by weight to 25% by weight Titanium dioxide; about 0.001% to 20% by weight of zinc oxide; about 0.001% to 10% by weight of flavonoids or derivatives thereof; about 0.001% to 10% by weight of butylphosphonium oxybenzoylmethane ( Non-limiting example of a suitable butylmethoxydibenzoylmethane is under the trade name "Pai: sol-1789" product # 64030 (available from Roche Inc.); from about 0.001% to 10% by weight of 4--14 copies Paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 520286. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs
--------------Μ ί (請先閱讀背面之注意事項再填寫本頁) · --線· A7 _____^L._ 五、發明說明(垮 異丙基二苯甲醯基甲烷;約〇〇Q1重量〇/〇至10重量%之辛基 三嗪酮;及約0.001重量%至25重量%之一種由二氧化鈦、 氧化鋅與美赛康(methicone)所組成之防曬劑,其係由 Miyoshi Kasei公司所生產及由u.S· Cosmetics公司以商品 名”TZ粉末第1(B)型”銷售。 一種較佳的防曬劑包括約7·5重量%之肉桂酸乙基己 基甲氧酯、約2重量%之丁基甲氧二苯甲醯基甲烷及約3重 量%至4重量%之氧苯酮或二苯甲酮。 在本發明之最佳的第四具體例中,該皮膚美白摻合物 具有低色素沈著的組成成份、抗氧化劑、促進劑與防曬劑 。就第四具體例而言,各組成成份之參數與上述相同。第 四具體例之所以為最佳,係因其藉由該促進劑而增加皮膚 細胞的更新速率,進而增強第一具體例之皮膚美白效果, 及所添加之防曬劑之作用係保護使用者免於紫外線照射之 傷害。 本發明之組成物具有一或多種其他成份,諸如醇類、 酸鹼值調節劑、螯合劑、潤膚劑、乳化劑、成膜劑、濕潤 劑、香料、掩蔽劑、色素、防腐劑、粉末、表面活性劑與 增稠劑。 該酸鹼值調節劑較佳係為一種鹼。該鹼較佳為氫氧化 銨、氫氧化鉀與氫氧化鈉。氫氧化鉀與氫氧化銨係為較佳 。理論而言,其他酸鹼值調節劑亦適用於本發明,若該酸 鹼值調節劑能提供一安定的組成物以及將該組成物之酸鹼 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 15 520286 A7 B7 五、發明說明(Θ 值調節至適於局部使用之一酸鹼值。如上述,當該促進劑 係為一氧雜酸時,組成物之酸鹼值最佳約為3·5至4.5。 本發明之較佳組成物可具有如下之成份: 經濟部智慧財產局員工消費合作社印製 成份_ 百分比 3,6,9-三氧雜十一烷二酸 0.001-10.0 氫氧化銨 0.001-4.0 濕潤劑(如乙二醇、甘油) 0.5-15.0 增稠劑(如樹膠、澱粉、聚合物) 0.1-4.0 螯合劑 0.001-0.5 潤膚劑 1.0-10.0 碎酮 0.1-15.0 防腐劑 0.01-2.0 脂族醇/乳化劑/蠟/脂肪酸 0.5-15.0 醇類 0-10.0 維他命Ε乙酸酯 1.0 y-穀維素 0.5 萃取物 12.35 肉桂酸乙基己基曱氧酯 7.5 丁基曱氧二苯曱醯基曱烷 2.0 二苯曱酮-3 3.5 去礦物質水 Q.S. 下列係本發明之一組成物,其經試管中之測試發現可 提供所需之有效的皮膚美白組成物。 本紙張尺度適用中國國家標準 X 297公釐)-------------- Μ ί (Please read the precautions on the back before filling out this page) · -line · A7 _____ ^ L._ 5. Description of the invention Benzamidine methane; octyltriazinone at about 0.001 to 10% by weight; and about 0.001 to 25% by weight of one consisting of titanium dioxide, zinc oxide, and memethone A sunscreen agent produced by Miyoshi Kasei and sold by uS Cosmetics under the trade name "TZ Powder Type 1 (B)". A preferred sunscreen agent comprises about 7.5% by weight of ethyl cinnamate Methylhexyl methoxyester, about 2% by weight of butylmethoxybenzophenamyl methane, and about 3 to 4% by weight of oxybenzone or benzophenone. In a preferred fourth embodiment of the present invention, The skin-whitening blend has low-pigmentation components, antioxidants, promoters, and sunscreens. As far as the fourth specific example is concerned, the parameters of each component are the same as above. The reason why the fourth specific example is the best , Because it increases the renewal rate of skin cells through the promoter, thereby enhancing the skin beauty of the first specific case The effect and the effect of the added sunscreen are to protect the user from the damage of ultraviolet radiation. The composition of the present invention has one or more other ingredients such as alcohols, pH adjusters, chelating agents, emollients, Emulsifier, film-forming agent, wetting agent, perfume, masking agent, pigment, preservative, powder, surfactant and thickener. The pH adjuster is preferably an alkali. The alkali is preferably hydroxide Ammonium, potassium hydroxide and sodium hydroxide. Potassium hydroxide and ammonium hydroxide are preferred. In theory, other pH regulators are also suitable for the present invention. If the pH regulator can provide a stable Composition and the acid and alkali of the composition The paper size of this composition is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 15 520286 A7 B7 V. Description of the invention (Θ value is adjusted to an acid and alkali suitable for local use As mentioned above, when the accelerator is monooxa acid, the pH value of the composition is preferably about 3.5 to 4.5. The preferred composition of the present invention may have the following components: Intellectual property of the Ministry of Economic Affairs Printed by Bureau Consumers Cooperative Ingredients_ Percentage 3,6,9-Trioxaundecane diacid 0.001-10.0 Ammonium hydroxide 0.001-4.0 Wetting agent (such as ethylene glycol, glycerin) 0.5-15.0 Thickener (such as gum, starch, polymer ) 0.1-4.0 chelating agent 0.001-0.5 emollient 1.0-10.0 crushed ketone 0.1-15.0 preservative 0.01-2.0 aliphatic alcohol / emulsifier / wax / fatty acid 0.5-15.0 alcohol 0-10.0 vitamin E acetate 1.0 y -Oryzanol 0.5 Extract 12.35 Ethylhexyl cinnamate cinnamate 7.5 Butyl oxydiphenyl fluorenyl oxane 2.0 Dibenzophenone-3 3.5 Demineralized water QS The following is one of the compositions of the present invention, It was tested in a test tube and found to provide the required effective skin whitening composition. This paper size applies Chinese National Standard X 297 mm)
520286 五、發明說明(β 第2例 成份 3,6,9-三氧雜十一燒二酸 氫氧化銨 濕潤劑(如乙二醇、甘油) 增稠劑(如樹膠、殿粉、聚合物) 螯合劑 潤膚劑 矽酮 防腐劑 脂族醇/乳化劑/壤/脂肪酸 醇類 維他命E乙酸酯 γ-穀維素 迷迭香萃取物 甘草萃取物(油可混溶的粉末) 綠茶萃取粉末 桑椹萃取粉末 熊莓萃取粉末 四氫薑黃色素 虎耳草、葡萄 芩根部萃取物之摻合物 肉桂酸乙基己基曱氧酯 丁基曱氧"一苯甲酿基曱烧 二苯曱酮-3 去礦物質水 百分比 桑椹根部萃取物與黃 0.001-10.0 0.001-4.0 0.5-15.0 〇.1-4.0 0.001-0.5 1.0-10.0 0.1-15.0 0.01-2.0 0.5-15.0 0-10.0 1.0 0.5 0.2 0.05 0.0004 0.1 1.0 1.0 1.0 7.5 2.0 3.5Q.S. --------------裝--------訂--------- (請先閱讀背面之注音?事項再填寫本頁} .經濟部智慧財產局員工消費合作社印製 經由查閱本申請案,將可瞭解本發明之各種改良與變 化。該等變化與附加部份係涵蓋於如下列申請專利範圍所 界定之本發明的範疇與精神之内。 卜纸張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐)520286 V. Description of the invention (β Example 2 Ingredient 3,6,9-trioxaundecyl diacid ammonium hydroxide wetting agent (such as ethylene glycol, glycerin) Thickener (such as gum, powder, polymer Chelating agents, emollients, silicone preservatives, aliphatic alcohols / emulsifiers / soils / fatty acid alcohols, vitamin E acetate, gamma-oryzanol, rosemary extract, licorice extract (oil-miscible powder), green tea extract Powder mulberry extract powder bear berry extract powder tetrahydroturmeric yellow saxifrage and grape root root extract blended with ethylhexyl oxycinnamate butyl oxyn cinnamate " monobenzoyl benzophenone -3 Demineralized water percentage Mulberry root extract with yellow 0.001-10.0 0.001-4.0 0.5-15.0 〇.1-4.0 0.001-0.5 1.0-10.0 0.1-15.0 0.01-2.0 0.5-15.0 0-10.0 1.0 0.5 0.2 0.05 0.0004 0.1 1.0 1.0 1.0 7.5 2.0 3.5QS -------------- Installation -------- Order --------- (Please read the note on the back first? Matters Refill this page}. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs. By reviewing this application, you will understand various improvements and changes to the present invention. The additions are within the scope and spirit of the invention as defined by the scope of the patent application below. The paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm)
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CN103083210A (en) * | 2013-01-25 | 2013-05-08 | 王恩瀚 | Medicine composition with skin whitening effect as well as preparation method and application thereof |
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CN103083210A (en) * | 2013-01-25 | 2013-05-08 | 王恩瀚 | Medicine composition with skin whitening effect as well as preparation method and application thereof |
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