TW201417822A - Topical compositions for the treatment of acne - Google Patents

Topical compositions for the treatment of acne Download PDF

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TW201417822A
TW201417822A TW102133208A TW102133208A TW201417822A TW 201417822 A TW201417822 A TW 201417822A TW 102133208 A TW102133208 A TW 102133208A TW 102133208 A TW102133208 A TW 102133208A TW 201417822 A TW201417822 A TW 201417822A
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topical formulation
formulation
extract
acne
topical
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Sharon Rozenblat
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Kamedis Ltd
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    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K36/70Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/708Rheum (rhubarb)
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    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/77Sapindaceae (Soapberry family), e.g. lychee or soapberry
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
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    • A61K8/342Alcohols having more than seven atoms in an unbroken chain
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    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
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    • AHUMAN NECESSITIES
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    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • AHUMAN NECESSITIES
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    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

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Abstract

The invention is directed to topical formulations comprising plant extracts together with additional ingredients. The invention is further directed to use of the formulations in treating acne. In particular, the invention is directed to a topical formulation comprising Portulaca oleracea extract, Rheum palmatum extract, Chrysanthemum indicum extract and Scutellaria baicalensis root extract or its active ingredient Baicalin, together with nordihydroguaiaretic acid and oleanolic acid.

Description

用於治療痤瘡的局部用組成物 Topical composition for treating acne 發明領域 Field of invention

本發明係有關包含植物萃取物連同額外之成分之局部用配方。本發明更有關該配方於治療痤瘡之用途。 The present invention relates to topical formulations comprising plant extracts together with additional ingredients. The invention is more related to the use of the formulation for the treatment of acne.

發明背景 Background of the invention

痤瘡(Acne vulgaris)(囊腫型痤瘡或"痤瘡")為常見之皮膚病,其特徵為皮膚發紅、粉刺(黑頭與白頭)、丘疹(針頭狀)、膿皰(疙瘩)、結節(大型丘疹)與疤痕。痤瘡大多影響皮膚毛囊皮脂腺最密集部位;這些區域包括臉部、胸部上方與背部。嚴重型痤瘡具有發炎性,不過痤瘡也有非發炎形式。此類病變之成因為毛囊皮脂腺單位、毛囊與其相關皮脂腺組成之皮膚結構之改變,以及該變化需要雄性激素刺激。痤瘡最常出現在青春期,且通常延續至成年期。痤瘡被認為是西方國家最普遍皮膚疾病之一。痤瘡於成年人之盛行率為約25%,而有90%青少年於12至24歲期間患有痤瘡。其症狀特徵為臉部、頸部、背部、胸部與肩部常出現腫塊。痤瘡之嚴重程度因人而異,且遺傳因素扮演重要角色。其致病因素包括皮脂分泌、毛囊角化、微生物族群, 以及免疫性與發炎過程。 Acne vulgaris (cyst-type acne or "acne") is a common skin disease characterized by redness of the skin, acne (blackheads and whiteheads), papules (needle-like), pustules (sputum), nodules (large papules). ) with scars. Acne mostly affects the most dense parts of the skin's hair follicle sebaceous glands; these areas include the face, upper chest and back. Severe acne is inflammatory, but acne also has a non-inflammatory form. The formation of such lesions is due to changes in the skin structure of the hair follicle sebaceous gland units, hair follicles and their associated sebaceous glands, and this change requires androgen stimulation. Acne most often occurs during puberty and usually continues into adulthood. Acne is considered to be one of the most common skin diseases in Western countries. The prevalence of acne in adults is about 25%, while 90% of adolescents suffer from acne during the 12 to 24 years of age. Symptoms are characterized by lumps in the face, neck, back, chest and shoulders. The severity of acne varies from person to person and genetic factors play an important role. Its pathogenic factors include sebum secretion, follicular keratosis, and microbial populations. And the process of immunity and inflammation.

依據廣泛之理論,痤瘡病變之初步發展階段為角質細胞異常脫落,其阻止正常皮脂排出。青少年體內循環之雄性激素增加,刺激了皮脂產生,導致周圍毛囊腫脹。這些情況之結合,於皮脂腺內產生有利於痤瘡桿菌(Propionibacterium acnes)增生之環境。滋生之痤瘡桿菌會分泌各種炎性分子與趨化因子,其啟動局部發炎反應,並可能同時誘發角質細胞過度增生。然而,證據顯示,發炎情況於病變形成之前出現,且堵塞情況在一定程度上,會受到痤瘡桿菌之發炎影響。 According to a broad theory, the initial stage of development of acne lesions is abnormal keratinocyte shedding, which prevents normal sebum discharge. An increase in circulating male hormones in adolescents stimulates sebum production, causing swelling of surrounding hair follicles. The combination of these conditions produces an environment conducive to the proliferation of Propionibacterium acnes in the sebaceous glands. The breeding acne bacteria secrete various inflammatory molecules and chemokines, which initiate local inflammatory reactions and may induce excessive proliferation of keratinocytes. However, evidence suggests that inflammatory conditions occur before the formation of the lesion, and that the occlusion is affected to some extent by the inflammation of the acne bacillus.

現行之痤瘡病變類型可分為發炎性與非發炎性病變。 Current types of acne lesions can be classified into inflammatory and non-inflammatory lesions.

非發炎性病變亦稱為粉刺。非發炎性病變為固體小型白色丘疹,一般直徑小於1mm,其含有由皮脂與角化碎片構成之白色碎片核心(封閉性粉刺),或暗灰色碎片核心,係因暴露於空氣與之後氧化(開放性粉刺)所致。 Non-inflammatory lesions are also known as acne. Non-inflammatory lesions are solid small white papules, typically less than 1 mm in diameter, containing a white debris core (closed acne) consisting of sebum and keratinized debris, or a dark gray debris core that is exposed to air and then oxidized (open Caused by sexual acne.

發炎性病變包括丘疹、膿皰與結節。發炎性病變之範圍可由高溫固化紅斑性丘疹、含化膿性材料之核心膿皰,至較大硬結性病變。後者若其直徑小於5mm,則被界定為結節。 Inflammatory lesions include papules, pustules, and nodules. Inflammatory lesions range from high-temperature solidified erythematous papules, core pustules containing purulent material, to larger induration lesions. The latter, if its diameter is less than 5 mm, is defined as a nodule.

鑑於習知之痤瘡治療之缺點,目前仍需要一種含草藥之局部用組成物,以用於治療。 In view of the shortcomings of conventional acne treatments, there is still a need for a topical composition containing herbs for use in therapy.

發明概要 Summary of invention

本發明之實施例係有關包含馬齒莧(Portulaca oleracea)萃取物、掌葉大黃(Rheum palmatum)萃取物、油菊(Chrysanthemum indicum)萃取物與黃芩(Scutellaria baicalensis)根萃取物,或其活性成分黃芩苷(Baicalin),結合去甲二氫癒創木酸(nordihydroguaiaretic acid)與齊墩果酸(oleanolic acid)之局部用配方。進一步之實施例係有關使用上述配方治療或預防痤瘡。依據一些實施例,該配方進一步包含甘草酸二鉀(dipotassium glycyrrhizate)、洋甘菊(母菊屬)(Chamomilla recutita(matricaria))花萃取物與北美金縷梅(金縷梅)(Hamamelis virginiana(witch hazel))之一或多者。 Embodiments of the present invention relate to extracts comprising Portulaca oleracea extract, Rheum palmatum extract, Chrysanthemum indicum extract and Scutellaria baicalensis root extract, or activity thereof Ingredients Baicalin, combined with a topical formulation of nordihydroguaiaretic acid and oleanolic acid. Further embodiments relate to the treatment or prevention of acne using the above formulations. According to some embodiments, the formulation further comprises dipotassium glycyrrhizate, Chamomilla recutita (matricaria) flower extract and Hamamelis virginiana (witch hazel) )) One or more.

依據一些實施例,該配方進一步包含水楊酸、尿囊素(allantoin)與沒藥醇(α-bisabolol)之一或多者。依據一些實施例,該配方進一步包含高嶺土(kaolin)、氧化鋅、沙棘油(hippophae rhamnoides oil)、松蘿酸(usnic acid)、羥苯基丙醯胺基苯甲酸(hydroxyphenyl propamidobenzoic acid)、二氧化鈦之一或多者。依據一些實施例,該配方進一步包含咪唑啶基尿素(imidazolidinyl urea)、甲基氯異噻唑啉酮(methylchloroisothiazolinone)與甲基異噻唑啉酮(methylisothiazolinone)之一或多者。 According to some embodiments, the formulation further comprises one or more of salicylic acid, allantoin, and a-bisabolol. According to some embodiments, the formulation further comprises kaolin, zinc oxide, hippophae rhamnoides oil, usnic acid, hydroxyphenyl propamidobenzoic acid, titanium dioxide One or more. According to some embodiments, the formulation further comprises one or more of imidazolidinyl urea, methylchloroisothiazolinone, and methylisothiazolinone.

本發明之一些實施例係有關包含馬齒莧萃取物、無患子(Sapindus mukorossi)果萃取物與月桂醇聚醚硫酸銨(ammonium laureth sulfate)、椰油醯胺基丙基甜菜鹼(cocamidopropyl betaine)、椰油醯胺MEA(cocamide MEA)、 椰油醯胺DEA(cocamide DEA)之至少一者之局部用配方。依據一些實施例,上述配方係用於治療或預防痤瘡。 Some embodiments of the present invention relate to a purslane extract, a Sapindus mukorossi fruit extract, an ammonium laureth sulfate, a cocamidopropyl betaine, A topical formulation of at least one of cocoamide MEA (cocamide MEA) and cocamide DEA (cocamide DEA). According to some embodiments, the above formulations are used to treat or prevent acne.

依據一些實施例,該配方提供涵蓋皮脂分泌減少、皮膚油類吸收、抗發炎活性、抗菌活性、傷口癒合特性、抗氧化活性、皮膚刺激減少、配方之皮膚吸收,或其任何結合之協同效用。 According to some embodiments, the formulation provides a synergistic effect that encompasses reduced sebum secretion, skin oil absorption, anti-inflammatory activity, antibacterial activity, wound healing characteristics, antioxidant activity, reduced skin irritation, skin absorption of the formula, or any combination thereof.

本發明之進一步實施例係有關治療痤瘡之方法,其包含以本文詳述之局部用配方,局部施加至有需要之個體。 A further embodiment of the invention is a method of treating acne comprising topically applying to a subject in need thereof, in a topical formulation as detailed herein.

本發明於此以附圖說明,但僅用於示範。可具體參考詳細之圖示說明,必須強調的是,以範例方式之詳盡描述,目的僅在於說明本發明之較佳實施例,並提供被認為最適用與易於理解之闡述,以呈現本發明之原則與觀點。在此方面,除了本發明所需之基本理解之外,並未試圖以更詳盡方式呈現本發明之構成細節,而用於體現本發明之各種形式之圖示與說明,對於本領域之技術人員而言將是顯而易見。 The invention is illustrated herein with reference to the drawings, but only for purposes of illustration. The detailed description of the present invention is intended to be illustrative of the preferred embodiments of the invention Principles and opinions. In this regard, the detailed description of the invention is not intended to It will be obvious.

圖1A、1B、1C與1D為比較結果之圖示說明,其於患有痤瘡之個體中,比較本發明示範性實施例之面霜與先前較差療效之配方之治療功效。特別的是,圖1A與1B圖示說明本發明實施例之面霜之結果,而圖1C與1D圖示說明先前較差療效之配方之結果。 1A, 1B, 1C and 1D are graphical representations of comparison results comparing the therapeutic efficacy of a cream of an exemplary embodiment of the present invention with a previously poorly curative formulation in an individual suffering from acne. In particular, Figures 1A and 1B illustrate the results of a face cream of an embodiment of the present invention, while Figures 1C and 1D illustrate the results of a previously poorly formulated formula.

圖2A、2B、2C與2D為比較結果之圖示說明,其 於患有痤瘡之個體中,比較了本發明示範性實施例之遮瑕處理配方,與先前較差療效之配方之治療功效。圖2A與2B圖示說明本發明實施例之遮瑕處理之結果,而圖2C與2D圖示說明先前較差療效之遮瑕處理配方之結果。 2A, 2B, 2C and 2D are graphical illustrations of comparison results, In an individual suffering from acne, the concealer treatment formulation of an exemplary embodiment of the present invention was compared to the therapeutic efficacy of a previously poorly formulated formulation. Figures 2A and 2B illustrate the results of concealing treatments in accordance with embodiments of the present invention, while Figures 2C and 2D illustrate the results of concealing treatment formulations of previously poorer efficacy.

圖3係圖示說明以水楊酸單獨,及以水楊酸結合草藥混合物治療後,病患之痤瘡發炎性病變減少。 Figure 3 is a graphical representation of the reduction in acne inflammatory lesions in patients treated with salicylic acid alone and with a mixture of salicylic acid and herbal extracts.

較佳實施例之詳細說明 Detailed description of the preferred embodiment

本發明之一實施例為包含馬齒莧萃取物、掌葉大黃萃取物、油菊萃取物與黃芩根萃取物,或其活性成分黃芩苷,結合去甲二氫癒創木酸與齊墩果酸之局部用配方。本發明之一些實施例係有關使用包含馬齒莧萃取物、掌葉大黃萃取物、油菊萃取物與黃芩根萃取物,或其活性成分黃芩苷,結合去甲二氫癒創木酸與齊墩果酸之局部用配方,治療及/或預防痤瘡。 An embodiment of the present invention comprises a purslane extract, a rhubarb extract, a chrysanthemum extract and a xanthium root extract, or an active ingredient baicalin, combined with nordihydroguaiaretic acid and Qi Dun A topical formula for fruit acids. Some embodiments of the present invention relate to the use of a extract comprising purslane extract, rhubarb extract, oil daisy extract and xanthium root extract, or an active ingredient baicalin, in combination with nordihydroguaiaretic acid A topical formulation of oleanolic acid for the treatment and/or prevention of acne.

依據一些實施例,該局部用配方進一步包含一或多個下列試劑:氧化鋅、高嶺土、二氧化鈦、沙棘油、羥苯基丙醯胺基苯甲酸、松蘿酸、甘草酸二鉀、洋甘菊(母菊屬)花萃取物、水楊酸、甘油、北美金縷梅(金縷梅)水、尿囊素、沒藥醇,或其任何之結合物。 According to some embodiments, the topical formulation further comprises one or more of the following agents: zinc oxide, kaolin, titanium dioxide, sea buckthorn oil, hydroxyphenyl propylamino benzoic acid, usnic acid, dipotassium glycyrrhizinate, chamomile (mother Chrysanthemum) flower extract, salicylic acid, glycerin, witch hazel (witch hazel) water, allantoin, bisabolol, or any combination thereof.

依據一些實施例,該局部用配方進一步包含氧化鋅、高嶺土、二氧化鈦、沙棘油、羥苯基丙醯胺基苯甲酸與松蘿酸,或其任何結合物之一或多者。 According to some embodiments, the topical formulation further comprises one or more of zinc oxide, kaolin, titanium dioxide, sea buckthorn oil, hydroxyphenyl propylaminobenzoic acid and usnic acid, or any combination thereof.

依據一些實施例,該局部用配方進一步包含甘草 酸二鉀、洋甘菊(母菊屬)花萃取物、水楊酸、甘油、北美金縷梅(金縷梅)水、尿囊素與沒藥醇,或其任何結合物之一或多者。 According to some embodiments, the topical formulation further comprises licorice One or more of dipotassium, chamomile (Matricaria) flower extract, salicylic acid, glycerin, witch hazel (witch hazel) water, allantoin and bisabolol, or any combination thereof.

依據一些實施例,該局部用配方包含馬齒莧萃取物、掌葉大黃萃取物、油菊萃取物與黃芩根萃取物,或其活性成分黃芩苷,結合去甲二氫癒創木酸與齊墩果酸,以及水楊酸、尿囊素、沒藥醇、甘草酸二鉀、洋甘菊(母菊屬)花萃取物與北美金縷梅(金縷梅)之一或多者。依據一些實施例,該局部用配方不含對羥苯甲酸酯(paraben)。依據一些實施例,該配方之pH值為介於約3.5-4.5之間。依據一些實施例,該配方之pH值為介於約3.0-5.0之間。依據一些實施例,該配方之pH值為介於約3.0-5.5之間。在一些實施例中,該配方為面霜形式。 According to some embodiments, the topical formulation comprises a purslane extract, a palm leaf rhubarb extract, a nectarine extract and a scutellaria root extract, or an active ingredient baicalin, in combination with nordihydroguaiaretic acid Oleanolic acid, and one or more of salicylic acid, allantoin, bisabolol, dipotassium glycyrrhizinate, chamomile (Matricaria) flower extract and North American witch hazel (Witch Hazel). According to some embodiments, the topical formulation is free of parabens. According to some embodiments, the pH of the formulation is between about 3.5 and 4.5. According to some embodiments, the pH of the formulation is between about 3.0 and 5.0. According to some embodiments, the pH of the formulation is between about 3.0 and 5.5. In some embodiments, the formulation is in the form of a cream.

依據一些實施例,該局部用配方包含馬齒莧萃取物、掌葉大黃萃取物、油菊萃取物與黃芩根萃取物,或其活性成分黃芩苷,結合去甲二氫癒創木酸與齊墩果酸。依據一些實施例,該配方進一步包含高嶺土、氧化鋅、二氧化鈦、沙棘油與羥苯基丙醯胺基苯甲酸之一或多者。依據進一步之實施例,該配方進一步包含咪唑啶基尿素、甲基氯異噻唑啉酮與甲基異噻唑啉酮之一或多者。依據一些實施例,該局部用配方不含對羥苯甲酸酯。依據一些實施例,該配方之pH值為介於約7.0-8.0之間。在一些實施例中,該配方為遮瑕處理配方形式。 According to some embodiments, the topical formulation comprises a purslane extract, a palm leaf rhubarb extract, a nectarine extract and a scutellaria root extract, or an active ingredient baicalin, in combination with nordihydroguaiaretic acid Oleanolic acid. According to some embodiments, the formulation further comprises one or more of kaolin, zinc oxide, titanium dioxide, sea buckthorn oil, and hydroxyphenyl acrylamidobenzoic acid. According to further embodiments, the formulation further comprises one or more of imidazolidinyl urea, methylchloroisothiazolinone and methylisothiazolinone. According to some embodiments, the topical formulation is free of parabens. According to some embodiments, the pH of the formulation is between about 7.0 and 8.0. In some embodiments, the formulation is in the form of a concealer treatment formulation.

本發明之一些實施例係有關包含馬齒莧萃取 物、無患子果萃取物與月桂醇聚醚硫酸銨、椰油醯胺基丙基甜菜鹼、椰油醯胺MEA、椰油醯胺DEA之至少一者之局部用配方。本發明之其他實施例係有關使用包含馬齒莧萃取物、無患子果萃取物與月桂醇聚醚硫酸銨、椰油醯胺基丙基甜菜鹼、椰油醯胺MEA、椰油醯胺DEA之至少一者之局部用配方,治療痤瘡。依據一些實施例,該配方不含十二基硫酸鈉(SLS)。依據一些實施例,該配方為潔淨凝膠形式。 Some embodiments of the invention relate to the extraction of purslane A topical formulation of at least one of a substance, a fruit extract, and a lauryl ammonium sulfate, cocoamidopropyl betaine, cocoamine MEA, cocoamine DEA. Other embodiments of the invention relate to the use of a purslane extract, sapindus extract and ammonium laureth sulfate, cocoamidopropyl betaine, cocoamine MEA, cocoamine DEA At least one of the partial formulas for treating acne. According to some embodiments, the formulation does not contain sodium dodecyl sulfate (SLS). According to some embodiments, the formulation is in the form of a clean gel.

依據一些實施例,該局部用配方包括抗發炎成分、抗菌成分、調節皮脂分泌成分、皮膚保濕成分、止痛劑、抗刺激劑、抗氧化劑,及其任何之結合物之一或多者。 According to some embodiments, the topical formulation comprises one or more of an anti-inflammatory component, an antimicrobial component, a conditioning sebum secreting component, a skin moisturizing component, an analgesic, an anti-irritant, an antioxidant, and any combination thereof.

依據一些實施例,該局部用配方之活性成分提供協同效用,以治療及/或預防痤瘡。依據進一步之實施例,配方中活性成分之至少一者與其他成分之至少一者之結合物,係提供協同效用,以治療及/或預防痤瘡。協同效用可為直接性,以治療/預防病症、間接性,如藉由增進配方/活性成分之穿透進入皮膚或減少皮膚刺激,或同時為直接性與間接性。 According to some embodiments, the active ingredient of the topical formulation provides a synergistic effect for the treatment and/or prevention of acne. According to further embodiments, a combination of at least one of the active ingredients in the formulation with at least one of the other ingredients provides a synergistic effect for the treatment and/or prevention of acne. Synergistic utility can be direct, to treat/prevent a condition, indirect, such as by enhancing penetration of the formulation/active ingredient into the skin or reducing skin irritation, or both direct and indirect.

氧化鋅之使用有助於降低皮脂量。高嶺土可用於吸收油性皮膚之過多油脂與滲出液。黃芩苷與掌葉大黃可減少雄性激素受體表達,因此,可用於減少雄性激素媒介之皮脂腺活性刺激,導致皮脂量下降。因此,掌葉大黃與黃芩,或其活性成分黃芩苷,之結合物,連同氧化鋅及/或高嶺土,或任何其他同等成分,可協同地減少皮膚之皮脂 分泌與油吸收。 The use of zinc oxide helps to reduce the amount of sebum. Kaolin can be used to absorb excess oil and exudate from oily skin. Baicalin and palm leaf rhubarb can reduce androgen receptor expression and, therefore, can be used to reduce the sebaceous gland activity stimulating by androgen mediators, resulting in decreased sebum content. Therefore, the combination of palm leaf rhubarb and scutellaria, or its active ingredient baicalin, together with zinc oxide and/or kaolin, or any other equivalent ingredient, can synergistically reduce sebum of the skin. Secretion and oil absorption.

羥苯基丙醯胺基苯甲酸,一種合成之燕麥蒽醯胺(avenanthramide),可增進草藥混合物之抗發炎活性。此外,掌葉大黃萃取物亦具有特異於痤瘡之抗發炎活性,係因其抑制細胞介素如IL-1α。因此,依據一些實施例,羥苯基丙醯胺基苯甲酸,或任何同等成分,以及掌葉大黃可協同地增進配方之抗發炎活性。 Hydroxyphenyl acrylamide benzoic acid, a synthetic avenanthramide, enhances the anti-inflammatory activity of herbal mixtures. In addition, the palm leaf rhubarb extract also has anti-inflammatory activity specific for acne because it inhibits interleukins such as IL-1α. Thus, according to some embodiments, hydroxyphenyl prolyl benzoic acid, or any equivalent component, and palm rhubarb can synergistically enhance the anti-inflammatory activity of the formulation.

去甲二氫癒創木酸與齊墩果酸,係藉由抑制5α-還原酶作用,以及控制細菌生長,而減少過度角化(hyperkeratosis)、抑制發炎與減少皮脂分泌。此外,松蘿酸已知具有抗菌活性,而北美金縷梅(金縷梅)水已知具有抗發炎特性。此類成分,或同等物,可以協同方式,結合具有抗發炎活性之草藥萃取物,如馬齒莧萃取物、掌葉大黃萃取物、油菊萃取物與黃芩根萃取物或黃芩苷,以治療痤瘡。當結合調節皮脂分泌之萃取物,如掌葉大黃萃取物及黃芩根萃取物或黃芩苷使用時,亦可協同地治療痤瘡。依據一些實施例,當結合馬齒莧萃取物使用時,上述成分或其同等物可協同地增進對於痤瘡桿菌之抗菌活性。值得注意的是,痤瘡桿菌之減少,與發炎媒介物之減少及痤瘡之臨床上改進有相關性。當結合馬齒莧萃取物與掌葉大黃萃取物使用時,上述成分可進一步協同地增進傷口癒合能力。 Nordihydroguaiaretic acid and oleanolic acid reduce hyperkeratosis, inhibit inflammation and reduce sebum secretion by inhibiting 5α-reductase action and controlling bacterial growth. In addition, Usnic acid is known to have antibacterial activity, while Witch Hazel (Witch Hazel) water is known to have anti-inflammatory properties. Such ingredients, or equivalents, may be combined in a synergistic manner with herbal extracts having anti-inflammatory activity, such as purslane extract, palmetto rhubarb extract, oil daisy extract, and astragalus root extract or baicalin, Treating acne. Acne can also be treated synergistically when combined with an extract that regulates sebum secretion, such as palm leaf rhubarb extract and Astragalus root extract or baicalin. According to some embodiments, the above ingredients or their equivalents synergistically enhance the antibacterial activity against Acne bacillus when used in combination with a purslane extract. It is worth noting that the reduction in acne bacilli is associated with a reduction in inflammatory mediators and clinical improvement in acne. When combined with a purslane extract and a palm leaf rhubarb extract, the above ingredients can further synergistically enhance wound healing ability.

沙棘油(沙棘籽油)可作為傷口癒合之用。因此,其結合物,或任何其他之同等成分,結合具有傷口癒合能力之草藥萃取物,如馬齒莧萃取物與掌葉大黃萃取物,可 提供協同效用,以舒緩痤瘡發生與減少疤痕形成。沙棘油與北美金縷梅(金縷梅)水更為已知之抗氧化劑。因此,其結合物,或任何其他之同等成分,可協同地增進草藥萃取物之抗氧化劑活性,其降低了痤瘡之嚴重性與症狀。 Sea buckthorn oil (sea buckthorn seed oil) can be used as a wound for healing. Therefore, the combination, or any other equivalent component, combined with herbal extracts with wound healing capabilities, such as purslane extract and palmatum rhubarb extract, Provide synergistic effects to soothe acne and reduce scarring. Sea buckthorn oil and North American Witch Hazel (Witch Hazel) water are more known antioxidants. Thus, the combination, or any other equivalent ingredient, synergistically enhances the antioxidant activity of the herbal extract, which reduces the severity and symptoms of acne.

洋甘菊(母菊屬)花萃取物具有抗發炎活性,並可減少皮膚刺激。因此,其結合物,或任何其他之同等成分,結合草藥萃取物混合物,可協同地減少痤瘡病患之發炎與皮膚刺激。此外,依據一些實施例,該配方進一步包含水楊酸,其可能會引起皮膚刺激。洋甘菊(母菊屬)花萃取物之添加可同時減少此種皮膚刺激。亦可添加尿囊素與沒藥醇,以減少皮膚刺激,包括加入水楊酸造成之刺激。 Chamomile (Matricaria) flower extract has anti-inflammatory activity and can reduce skin irritation. Thus, the combination, or any other equivalent component, in combination with the herbal extract mixture, synergistically reduces inflammation and skin irritation in acne sufferers. Further, according to some embodiments, the formulation further comprises salicylic acid, which may cause skin irritation. The addition of a chamomile (Matricaria) flower extract can simultaneously reduce such skin irritation. Allantoin and bisabolol can also be added to reduce skin irritation, including irritation caused by the addition of salicylic acid.

依據進一步之實施例,該局部用配方進一步包含水楊酸。依據進一步之實施例,該局部用配方進一步包含至少0.3% w/w水楊酸。依據進一步之實施例,該局部用配方進一步包含至少0.4% w/w水楊酸。依據進一步之實施例,該局部用配方進一步包含至少0.5% w/w水楊酸。依據進一步之實施例,該局部用配方進一步包含約1.0% w/w水楊酸。依據進一步之實施例,該局部用配方進一步包含範圍為0.4-2.5% w/w之水楊酸。依據進一步之實施例,該局部用配方進一步包含範圍為0.5-2.0% w/w之水楊酸。依據進一步之實施例,該局部用配方進一步包含範圍為0.5-1.5% w/w之水楊酸。依據進一步之實施例,該局部用配方進一步包含範圍為0.5-1.0% w/w之水楊酸。依據進一步之實施例,該局部用配方進一步包含範圍為1.25-2% w/w之水楊酸。 According to a further embodiment, the topical formulation further comprises salicylic acid. According to a further embodiment, the topical formulation further comprises at least 0.3% w/w salicylic acid. According to a further embodiment, the topical formulation further comprises at least 0.4% w/w salicylic acid. According to a further embodiment, the topical formulation further comprises at least 0.5% w/w salicylic acid. According to further embodiments, the topical formulation further comprises about 1.0% w/w salicylic acid. According to a further embodiment, the topical formulation further comprises salicylic acid in the range of from 0.4 to 2.5% w/w. According to a further embodiment, the topical formulation further comprises salicylic acid in the range of from 0.5 to 2.0% w/w. According to a further embodiment, the topical formulation further comprises salicylic acid in the range of from 0.5 to 1.5% w/w. According to a further embodiment, the topical formulation further comprises salicylic acid in the range of from 0.5 to 1.0% w/w. According to further embodiments, the topical formulation further comprises salicylic acid in the range of 1.25-2% w/w.

依據進一步之實施例,該局部用配方進一步包含過氧化苯。依據進一步之實施例,該局部用配方進一步包含至少1.5% w/w過氧化苯。依據進一步之實施例,該局部用配方進一步包含至少2.0% w/w過氧化苯。依據進一步之實施例,該局部用配方進一步包含至少2.5% w/w過氧化苯。依據進一步之實施例,該局部用配方進一步包含範圍為1.5-12.0% w/w之過氧化苯。依據進一步之實施例,該局部用配方進一步包含範圍為2.0-11.0% w/w之過氧化苯。依據進一步之實施例,該局部用配方進一步包含範圍為2.5-10.0% w/w之過氧化苯。 According to a further embodiment, the topical formulation further comprises benzoyl peroxide. According to a further embodiment, the topical formulation further comprises at least 1.5% w/w benzoyl peroxide. According to a further embodiment, the topical formulation further comprises at least 2.0% w/w benzoyl peroxide. According to a further embodiment, the topical formulation further comprises at least 2.5% w/w benzoyl peroxide. According to a further embodiment, the topical formulation further comprises benzoic acid in the range of from 1.5 to 12.0% w/w. According to a further embodiment, the topical formulation further comprises benzoic acid in the range of from 2.0 to 11.0% w/w. According to a further embodiment, the topical formulation further comprises benzoic acid in the range of from 2.5 to 10.0% w/w.

依據一些實施例,該局部用配方之pH值為介於約3.0-5.0之間。依據進一步之實施例,該局部用配方之pH值為介於約3.5-4.5之間。依據進一步之實施例,該局部用配方之pH值為介於約2.5-6.0之間。依據一些實施例,該局部用配方之pH值為介於約6.0-9.0之間。依據進一步之實施例,該局部用配方之pH值為介於約7.0-8.0之間。依據進一步之實施例,該局部用配方之pH值為介於約6.5-8.5之間。 According to some embodiments, the topical formulation has a pH between about 3.0 and 5.0. According to a further embodiment, the topical formulation has a pH between about 3.5 and 4.5. According to a further embodiment, the topical formulation has a pH between about 2.5 and 6.0. According to some embodiments, the topical formulation has a pH between about 6.0 and 9.0. According to a further embodiment, the topical formulation has a pH between about 7.0 and 8.0. According to a further embodiment, the topical formulation has a pH between about 6.5 and 8.5.

依據一些實施例,該配方之草藥萃取物之結合濃度為至少0.75%。依據一些實施例,該配方之草藥萃取物之結合濃度為至少0.9%。依據一些實施例,該配方之草藥萃取物之結合濃度為至少1.0%。依據一些實施例,該配方之草藥萃取物之結合濃度為介於約0.8-1.2%之間。依據一些實施例,該配方之草藥萃取物之結合濃度為至少8.0%。依據一些實施例,該配方之草藥萃取物之結合濃度為至少 9.0%。依據一些實施例,該配方之草藥萃取物之結合濃度為至少10.0%。依據一些實施例,該配方之草藥萃取物之結合濃度為介於約9.0-11%之間。 According to some embodiments, the herbal extract of the formulation has a combined concentration of at least 0.75%. According to some embodiments, the herbal extract of the formula has a combined concentration of at least 0.9%. According to some embodiments, the herbal extract of the formulation has a combined concentration of at least 1.0%. According to some embodiments, the herbal extract of the formulation has a combined concentration of between about 0.8 and 1.2%. According to some embodiments, the herbal extract of the formulation has a combined concentration of at least 8.0%. According to some embodiments, the herbal extract of the formula has a combined concentration of at least 9.0%. According to some embodiments, the herbal extract of the formulation has a combined concentration of at least 10.0%. According to some embodiments, the herbal extract of the formula has a combined concentration of between about 9.0 and 11%.

依據一些實施例,該配方之草藥萃取物之每一者之量為約0.3%。依據一些實施例,該配方之草藥萃取物之每一者之量之範圍為約0.25-0.35%。依據一些實施例,該配方之草藥萃取物之每一者之量之範圍為約0.2-0.4%。 According to some embodiments, the amount of each of the herbal extracts of the formula is about 0.3%. According to some embodiments, the amount of each of the herbal extracts of the formula ranges from about 0.25 to 0.35%. According to some embodiments, the amount of each of the herbal extracts of the formula ranges from about 0.2 to 0.4%.

依據一些實施例,該配方包含至少0.075%黃芩苷。依據一些實施例,該配方包含至少0.085%黃芩苷。依據一些實施例,該配方包含至少0.095%黃芩苷。依據進一步之實施例,依據進一步之實施例,該面霜配方包含至少0.1%黃芩苷。依據一些實施例,該遮瑕處理配方包含至少1.0%黃芩苷。依據一些實施例,該面霜之草藥萃取物濃度為約1.0-1.6%。依據一些實施例,該遮瑕膏之草藥萃取物濃度為約9.0-11.0%。利用常規方法,本發明之配方可配製成多種製備物,其取決於預期之用途。這些製備物包括但不侷限於,醫療用之局部用皮膚組成物,以及局部用皮膚化妝品組成物。 According to some embodiments, the formulation comprises at least 0.075% baicalin. According to some embodiments, the formulation comprises at least 0.085% baicalin. According to some embodiments, the formulation comprises at least 0.095% baicalin. According to a further embodiment, according to a further embodiment, the cream formulation comprises at least 0.1% baicalin. According to some embodiments, the concealer treatment formulation comprises at least 1.0% baicalin. According to some embodiments, the cream extract has a herbal extract concentration of from about 1.0% to about 1.6%. According to some embodiments, the concealer has a herbal extract concentration of about 9.0 to 11.0%. The formulations of the present invention can be formulated into a variety of preparations depending on the intended use, using conventional methods. These preparations include, but are not limited to, topical skin compositions for medical use, and topical skin cosmetic compositions.

在醫療用之局部用皮膚組成物與局部用皮膚化妝品組成物方面,可使用凝膠、軟膏、肥皂、面霜與乳液之多種形式。可以任何適用之方式施加配方,亦即,經由手、刮勺、噴霧或墊。 Gels, ointments, soaps, creams and lotions can be used in the form of topical skin compositions for medical use and topical skin cosmetic compositions. The formulation can be applied in any suitable manner, i.e., via hand, spatula, spray or pad.

本發明之配方可為面霜、遮瑕處理,或潔淨凝膠形式。本發明之配方可施加至經痤瘡感染之全部皮膚區域, 或局部針對各個瘡。當施加至人體皮膚時,本發明之配方具有高度皮膚相容性與低刺激性。依據一些實施例,該配方係施加至人體並隨後以,如清水洗滌方式,將其移除。 The formulation of the invention may be in the form of a face cream, concealer treatment, or a clean gel. The formulation of the present invention can be applied to all skin areas infected with acne, Or partial for each sore. The formulations of the present invention have high skin compatibility and low irritation when applied to human skin. According to some embodiments, the formulation is applied to the human body and subsequently removed, such as by a water wash.

以本發明之局部用組成物作為化妝品組成物使用時,化妝品或皮膚病學上可接受成分,可任擇地以所希望之任意組合併入,並依據本領域之習知技術測定。依據一些實施例,該組成物可包括油類、脂肪、蠟、清潔劑、調和劑、pH值調節劑、防腐劑、溶劑、黏度調節劑、著色劑、香料、染料及其類似物。 When the topical composition of the present invention is used as a cosmetic composition, a cosmetic or dermatologically acceptable ingredient may optionally be incorporated in any desired combination and determined according to techniques well known in the art. According to some embodiments, the composition may include oils, fats, waxes, detergents, blending agents, pH adjusters, preservatives, solvents, viscosity modifiers, colorants, perfumes, dyes, and the like.

該組成物可為水包油、油包水、水包油包水,以及矽膠包水包油乳液、霜劑、軟膏、水性溶液、洗劑、肥皂、糊劑、泡沫劑、乳液、凝膠、油膏、油液、洗液、調理劑或氣霧形式。 The composition may be oil-in-water, water-in-oil, water-in-oil-in-water, and water-in-oil emulsion, cream, ointment, aqueous solution, lotion, soap, paste, foam, emulsion, gel , ointments, oils, lotions, conditioners or aerosols.

依據本發明之一實施例,本發明之組成物係每日投予一次。依據其他實施例,該組成物之投予為每日兩次、每日三次或以上。 According to an embodiment of the invention, the composition of the invention is administered once a day. According to other embodiments, the composition is administered twice daily, three times daily or more.

依據本發明之一實施例,該組成物為長期投予。 According to an embodiment of the invention, the composition is administered chronically.

依據本發明之一些實施例,該組成物之投予為約10天或以上、20天、30天、60天、90、120天或以上。 According to some embodiments of the invention, the composition is administered for about 10 days or more, 20 days, 30 days, 60 days, 90 days, 120 days or more.

在本發明之一些實施例中,該組成物進一步包含清潔劑或界面活性劑,其典型上為陰離子、陽離子、非離子或兩性界面活性劑。典型之陰離子界面活性劑為羧酸鹽類、磺酸鹽類、硫酸鹽類或磷酸鹽類,如脂肪酸皂類、月桂基硫酸鹽類與月桂基醚硫酸鹽類。陽離子界面活性劑之 範例為衍生自脂肪酸與松香酸之脂族單、二與多胺類、胺氧化物類、乙氧基化烷基胺類與咪唑啉類。非離子界面活性劑之範例為聚氧乙烯界面活性劑、烷基酚乙氧基化物、羧酸酯類,如單與二甘油酯、聚氧乙烯酯類與脂肪酸二乙醇胺縮合物。兩性界面活性劑為那些含有上述陰離子與陽離子基團之結合物者,特別是那些同時含有酸性羧基與鹼性氮基者。典型之兩性界面活性劑為咪唑啉類與甜菜鹼,如月桂酸與肉荳蔻咪唑啉及甜菜鹼,以及醯胺丙基甜菜鹼。 In some embodiments of the invention, the composition further comprises a detergent or surfactant, which is typically an anionic, cationic, nonionic or amphoteric surfactant. Typical anionic surfactants are carboxylates, sulfonates, sulfates or phosphates such as fatty acid soaps, lauryl sulfates and lauryl ether sulfates. Cationic surfactant Examples are aliphatic mono-, di- and polyamines, amine oxides, ethoxylated alkylamines and imidazolines derived from fatty acids and rosin acids. Examples of nonionic surfactants are polyoxyethylene surfactants, alkylphenol ethoxylates, carboxylates such as mono- and diglycerides, polyoxyethylene esters and fatty acid diethanolamine condensates. Amphoteric surfactants are those which contain a combination of the above anionic and cationic groups, especially those which contain both an acidic carboxyl group and a basic nitrogen group. Typical amphoteric surfactants are imidazolines and betaines such as lauric acid and myristic imidazoline and betaine, and amidinopropyl betaine.

局部用醫藥組成物,亦可包含適用之乳化劑,意指可增進或促進水包油或油包水之混合與懸浮者。本文所使用之乳化劑可由單一乳化劑,或可由非離子、陰離子、陽離子或兩性界面活性劑,或二或多個此類界面活性劑之摻合物組成;用於本文者較佳為非離子與離子乳化劑。此類界面活性劑係描述於“McCutcheon's Detergent and Emulsifiers,”North American Edition,1980 Annual published by the McCutcheon Division,MC Publishing Company,175 Rock Road,Glen Rock,N.J.07452,USA。 The topical pharmaceutical composition may also contain a suitable emulsifier, meaning that it may enhance or promote the mixing and suspension of oil-in-water or water-in-oil. The emulsifier used herein may be a single emulsifier, or may be composed of a nonionic, anionic, cationic or amphoteric surfactant, or a blend of two or more such surfactants; preferably used herein as a nonionic With ionic emulsifiers. Such surfactants are described in "McCutcheon's Detergent and Emulsifiers," North American Edition, 1980 Annual published by the McCutcheon Division, MC Publishing Company, 175 Rock Road, Glen Rock, N.J. 07452, USA.

CTFA Cosmetic Ingredient Handbook,Second Edition(1992)中,描述了多種皮膚保養產業中常見之非侷限性化妝品成分,其適合本發明組成物使用。這些成分類別之範例包括:研磨劑、吸收劑、美觀成分,如香料、顏料、增色劑/著色劑、精油、皮膚增感劑、收斂劑等(例如,丁香油、薄荷醇、樟腦、桉葉油、丁香酚、乳酸薄荷酯、金縷梅餾出物)、抗痤瘡劑、防結塊劑、消泡劑、抗菌劑(例 如,碘化丙基丁基胺甲酸酯)、抗氧化劑、黏合劑、生物添加劑、緩衝劑、填充劑、熬合劑、化學添加劑、著色劑、化妝品收斂劑、化妝品生物滅除劑、變性劑、藥物收斂劑、外用止痛劑、成膜劑或材料,如聚合物,有助於組成物之成膜特性與持久性(例如,二十碳烯與乙烯基吡咯啶酮之共聚合物)、遮光劑、pH值調節劑、推進劑、還原劑、螯合劑、皮膚調理劑(例如,濕潤劑,包括混雜型與封閉型)、皮膚舒緩劑及/或癒合劑(例如,泛醇及衍生物(例如,乙基泛醇)、蘆薈、泛酸及衍生物、尿囊素、沒藥醇,與甘草酸二鉀)、皮膚治療劑、增稠劑,與維生素,及其衍生物。 In the CTFA Cosmetic Ingredient Handbook, Second Edition (1992), a variety of non-limiting cosmetic ingredients commonly found in the skin care industry are described which are suitable for use in the compositions of the present invention. Examples of these ingredient classes include: abrasives, absorbents, aesthetic ingredients such as perfumes, pigments, colorants/colorants, essential oils, skin sensitizers, astringents, etc. (eg, clove oil, menthol, camphor, cilantro Oil, eugenol, menthyl lactate, witch hazel distillate), anti-acne agent, anti-caking agent, antifoaming agent, antibacterial agent For example, iodide propyl butyl carbamate), antioxidants, binders, biological additives, buffers, fillers, chelating agents, chemical additives, colorants, cosmetic astringents, cosmetic biocides, denaturing agents a drug astringent, a topical analgesic, a film former or a material, such as a polymer, contributes to the film forming properties and durability of the composition (for example, a copolymer of eicosene and vinylpyrrolidone), Sunscreens, pH adjusters, propellants, reducing agents, chelating agents, skin conditioning agents (eg, wetting agents, including promiscuous and blocked), skin soothing agents and/or healing agents (eg, panthenol and derivatives) (eg, ethyl panthenol), aloe vera, pantothenic acid and derivatives, allantoin, bisabolol, and dipotassium glycyrrhizinate), skin therapeutics, thickeners, and vitamins, and derivatives thereof.

可由配方之實施例進行治療或預防之其他皮膚病為例如,不限於,頭皮屑與油性皮膚狀況。 Other skin conditions that may be treated or prevented by embodiments of the formulation are, for example, without limitation, dandruff and oily skin conditions.

術語“約”意指±10%。術語% w/w,係指特定成分之重量於整體製劑重量中之百分比。 The term "about" means ±10%. The term % w/w refers to the percentage of the weight of a particular ingredient in the weight of the overall formulation.

術語“皮膚學上可接受載體”,使用於此,意指相容於皮膚、頭皮、毛髮、指甲及其類似物之載體。 The term "dermatologically acceptable carrier", as used herein, means a carrier which is compatible with the skin, scalp, hair, nails and the like.

術語“預防”意指確保個體不發生疾病、異常或症狀。在某些情況下,個體可能有發展為疾病之風險,但未被診斷出患有該疾病。在某些情況下,術語"預防"意指預防下一循環之疾病發生。 The term "prevention" means ensuring that the individual does not develop a disease, disorder or symptom. In some cases, an individual may have a risk of developing a disease but has not been diagnosed with the disease. In some cases, the term "prevention" means preventing the occurrence of a disease of the next cycle.

本文所使用之植物萃取物可由極性溶劑,例如乙基醇(乙醇)、丁基醇(丁醇)、甲醇、水,或丙醇、丙二醇、丁二醇、甘油,純化(亦即,極性萃取物)。本發明之極性萃取物可包含任何百分比之極性溶劑。 The plant extract used herein may be purified by a polar solvent such as ethyl alcohol (ethanol), butyl alcohol (butanol), methanol, water, or propanol, propylene glycol, butylene glycol, glycerol (ie, polar extraction). ()). The polar extract of the present invention may comprise any percentage of polar solvent.

或者,植物萃取物可由非極性溶劑,例如但不侷限於異辛烷純化(亦即,非極性萃取物)。本發明之非極性萃取物可包含任何百分比之非極性溶劑。 Alternatively, the plant extract can be purified by a non-polar solvent such as, but not limited to, isooctane (i.e., a non-polar extract). The non-polar extract of the present invention may comprise any percentage of non-polar solvent.

典型而言,疏水性分子趨向於非極性,因此使用非極性溶劑。親水性分子趨向於極性,並可由水及/或其他極性物質溶解。 Typically, hydrophobic molecules tend to be non-polar, so non-polar solvents are used. Hydrophilic molecules tend to be polar and can be dissolved by water and/or other polar substances.

活性成分可由萃取物中濃縮出,係使用親和層析法、質量層析法,及其類似方法。 The active ingredient can be concentrated from the extract using affinity chromatography, mass chromatography, and the like.

典型而言,本發明之植物萃取物為水性萃取物。欲取得經純化之植物萃取物(例如,植物萃取物之有機鹽類,及/或重金屬,及/或澱粉之含量減少),水性植物萃取物一般係進一步以樹脂層析法,如巨孔型樹脂或其他層析方法純化。將甘油、丙二醇、丁二醇或丙二醇加入水性萃取物中,以評估萃取物之溶解度、評估其皮膚穿透能力,並進一步保存該萃取物。萃取物亦可包含防腐劑。 Typically, the plant extract of the invention is an aqueous extract. In order to obtain purified plant extracts (for example, organic salts of plant extracts, and/or heavy metals, and/or reduced starch content), aqueous plant extracts are generally further subjected to resin chromatography, such as macroporous Purified by resin or other chromatography methods. Glycerin, propylene glycol, butylene glycol or propylene glycol is added to the aqueous extract to assess the solubility of the extract, assess its skin penetration ability, and further preserve the extract. The extract may also contain a preservative.

因此,依據另一實施例,係提供一種製備含有經濃縮草藥萃取物之組成物之方法,以治療及/或預防痤瘡,該方法包含:(a)將植物置於1-10倍體積之水中,以產生植物萃取物;以及(b)以巨孔型樹脂減少植物萃取物之雜質含量,使植物萃取物之活性成分含量提高。 Thus, according to another embodiment, there is provided a method of preparing a composition comprising a concentrated herbal extract for treating and/or preventing acne comprising: (a) placing the plant in 1-10 volumes of water To produce a plant extract; and (b) reducing the impurity content of the plant extract with a macroporous resin to increase the active ingredient content of the plant extract.

依據一些實施例,該配方包含任何額外之成分,包括溶劑、潤膚劑、保濕劑、調和劑、黏度劑、皮膚鎮靜劑、乳化劑、pH值調節劑、防腐劑、抗氧化劑、增黏劑、香料、濕潤劑、抗痤瘡劑、穩定劑與界面活性劑。 According to some embodiments, the formulation comprises any additional ingredients including solvents, emollients, humectants, blenders, viscosifiers, skin sedatives, emulsifiers, pH adjusters, preservatives, antioxidants, tackifiers, Perfumes, humectants, anti-acne agents, stabilizers and surfactants.

範例example 範例1Example 1 治療/預防痤瘡(遮瑕膏)之配方Formula for treating/preventing acne (concealer)

範例2Example 2 治療/預防痤瘡(面霜)之配方Formula for treating/preventing acne (cream)

上述面霜之pH值範圍為介於約3.5-4.5之間。 The pH of the above cream ranges from about 3.5 to 4.5.

範例3Example 3 治療/預防痤瘡(面霜)之配方Formula for treating/preventing acne (cream)

範例4Example 4 治療/預防痤瘡(潔淨凝膠)之配方Formulation for treating/preventing acne (clean gel)

範例5Example 5 治療/預防痤瘡(遮瑕處理)之配方Formula for treating/preventing acne (concealing treatment)

範例6Example 6 兩種面霜配方之比較Comparison of two cream formulas

進行兩種面霜處理之比較。第一種面霜之成分詳述於上表II,而第二種療效較差之面霜詳述於下表VI: Compare the two cream treatments. The ingredients of the first cream are detailed in Table II above, while the second cream with poor efficacy is detailed in Table VI below:

表VI之面霜之pH值範圍為介於約6.0-7.5之間。 The pH of the cream of Table VI ranges from about 6.0 to 7.5.

以面霜施加至六位年齡28.7±7.7之病患臉部六至七天,其中第一種面霜施加至一半臉上,而第二種面霜施加至另一半臉上。 The face cream was applied to six faces of six patients aged 28.7 ± 7.7 for six to seven days, with the first cream applied to half of the face and the second cream applied to the other half of the face.

參與者於受試期結束時填寫評量問卷,其中該問卷涵蓋下列標準:1.產品對於丘疹數量之影響;2.產品對於丘疹嚴重性之影響;3.產品對於油性皮膚之影響;4.產品對於皮膚發紅之影響;5.產品對於黑頭粉刺之影響;6.整體外觀;7.產品之整體評估;以及8.產品質地。 Participants fill out the assessment questionnaire at the end of the trial period, which covers the following criteria: 1. the impact of the product on the number of papules; 2. the impact of the product on the severity of papules; 3. the impact of the product on oily skin; The effect of the product on skin redness; 5. The effect of the product on blackheads; 6. Overall appearance; 7. Overall evaluation of the product; and 8. Product texture.

準則1-5可評價為具有:無影響、最小影響或顯著影響;以及準則6-8可評價為:不良、尚可、良好與極佳。 Guidelines 1-5 can be evaluated as having: no impact, minimal impact, or significant impact; and criteria 6-8 can be evaluated as: poor, acceptable, good, and excellent.

治療研究之結果圖示於圖1A、1B、1C與1D。 The results of the treatment studies are shown in Figures 1A, 1B, 1C and 1D.

圖1A與1C之間,以及圖1B與1D之間的比較顯示,相較於以第二種面霜治療(詳述於表VI且圖示於圖1C與1D),以第一種面霜治療(詳述於表II且圖示於圖1A與1B),在所有標準中皆較具有療效與滿意度,但產品對於黑頭粉刺之影響除外,因兩種產品之情況類似。 A comparison between Figures 1A and 1C, and between Figures 1B and 1D, shows treatment with a first cream compared to treatment with a second cream (described in detail in Table VI and illustrated in Figures 1C and 1D) Details are shown in Table II and are shown in Figures 1A and 1B), which are more effective and satisfactory in all standards, except for the effects of the product on blackheads, which are similar for both products.

範例7Example 7 兩種遮瑕處理配方之比較Comparison of two concealer treatment formulas

進行兩種遮瑕處理配方之比較。第一種遮瑕處理配方之成分詳述於上表I,而第二種面霜詳述於下表VII: A comparison of the two concealer treatment recipes. The ingredients of the first concealer treatment formulation are detailed in Table I above, while the second cream is detailed in Table VII below:

表VII所列配方之pH值為介於約6-7之間。 The pH of the formulations listed in Table VII is between about 6 and 7.

以一天兩次施加遮瑕處理配方至五位年齡44.8±10.3之病患臉部七天,其中第一種面霜施加至一半臉上,而第二種面霜施加至另一半臉上。遮瑕處理配方被視為厚面霜或軟膏。 The concealing treatment formula was applied twice a day to five faces of five patients aged 44.8 ± 10.3 for seven days, with the first cream applied to half of the face and the second cream applied to the other half of the face. The concealer treatment formula is considered a thick cream or ointment.

參與者於受試期結束時填寫評量問卷,其中該問卷涵蓋下列標準:1.產品對於丘疹數量之影響;2.產品對於丘疹嚴重性之影響;3.產品對於皮膚發紅之影響;4.整體外觀;5.產品之整體評估;以及6.產品質地。 Participants fill out the assessment questionnaire at the end of the trial period, which covers the following criteria: 1. The effect of the product on the number of papules; 2. The effect of the product on the severity of papules; 3. The effect of the product on the redness of the skin; Overall appearance; 5. overall evaluation of the product; and 6. product texture.

標準1-3可評價為具有:無影響、最小影響或顯著影響;以及準則4-6可評價為:不良、尚可、良好與極佳。 Standards 1-3 can be evaluated as having no effect, minimal impact, or significant impact; and criteria 4-6 can be evaluated as: poor, acceptable, good, and excellent.

治療研究之結果圖示於圖2A、2B、2C與2D。圖2A與2C之間,以及圖2B與2D之間的比較顯示,相較於以第二種面霜治療(詳述於表VII且圖示於圖2C與2D),以第一種面霜治療(詳述於表I且圖示於圖2A與2B),在所有標準中皆較具有療效與滿意度,但產品對於皮膚發紅之影響除外,因兩種產品之情況類似。 The results of the treatment studies are shown in Figures 2A, 2B, 2C and 2D. A comparison between Figures 2A and 2C, and between Figures 2B and 2D, shows treatment with a first cream compared to treatment with a second cream (described in detail in Table VII and illustrated in Figures 2C and 2D) Details are shown in Table I and shown in Figures 2A and 2B), which are more effective and satisfactory in all criteria, except for the effect of the product on skin redness, as the two products are similar.

範例8Example 8 草藥混合物與0.5%水楊酸之結合物,與0.5%水楊酸之比較Comparison of herbal mixture with 0.5% salicylic acid and 0.5% salicylic acid

28位患有痤瘡個體之半邊臉部,以含有草藥混合物+0.5%水楊酸之配方處理12天,而另半邊臉上僅以0.5%水楊酸處理。該草藥混合物包含1.5%馬齒莧萃取物、1.5% 掌葉大黃萃取物、1.5%油菊萃取物與0.5%黃芩根萃取物(黃芩苷)。 The half face of 28 individuals with acne was treated with a herbal mixture + 0.5% salicylic acid for 12 days, while the other half was treated with only 0.5% salicylic acid. The herbal mixture contains 1.5% Portulaca oleracea extract, 1.5% Palmetto rhubarb extract, 1.5% oil lily extract and 0.5% Astragalus root extract (xanthine).

結果圖示於圖3,其顯示了僅以水楊酸處理,以及以上述之水楊酸與草藥混合物之結合物處理時,發炎性痤瘡病變減少之百分比。如圖3所示,單獨處理水楊酸僅減少約17%病變,而以草藥混合物連同水楊酸處理則減少32%發炎性病變。 The results are shown in Figure 3, which shows the percentage reduction in inflammatory acne lesions when treated with salicylic acid alone and with a combination of the above-described salicylic acid and herbal mixture. As shown in Figure 3, salicylic acid alone reduced only about 17% of the lesions, while treatment with the herbal mixture and salicylic acid reduced the inflammatory lesion by 32%.

Claims (20)

一種局部用配方,其包含馬齒莧(Portulaca oleracea)萃取物、掌葉大黃(Rheum palmatum)萃取物、油菊(Chrysanthemum indicum)萃取物與黃芩(Scutellaria baicalensis)根萃取物,或其活性成分黃芩苷(Baicalin),結合去甲二氫癒創木酸(nordihydroguaiaretic acid)與齊墩果酸(oleanolic acid)。 A topical formulation comprising Portulaca oleracea extract, Rheum palmatum extract, Chrysanthemum indicum extract and Scutellaria baicalensis root extract, or active ingredient thereof Baicalin, combined with nordihydroguaiaretic acid and oleanolic acid. 如請求項1之局部用配方,係用於治療或預防痤瘡。 The topical formulation of claim 1 is for the treatment or prevention of acne. 如請求項1之局部用配方,其更包含下列之一或多者:甘草酸二鉀(dipotassium glycyrrhizate)、洋甘菊(母菊屬)(Chamomilla recutita(matricaria))花萃取物,以及北美金縷梅(金縷梅)(Hamamelis virginiana(witch hazel)。 The topical formulation of claim 1 further comprising one or more of the following: dipotassium glycyrrhizate, chamomile ( Chamomilla recutita (matricaria)) flower extract, and witch hazel (金缕梅) ( Hamamelis virginiana (witch hazel). 如請求項1之局部用配方,其更包含下列之一或多者:水楊酸、尿囊素(allantoin),以及沒藥醇(α-bisabolol)。 The topical formulation of claim 1, which further comprises one or more of the following: salicylic acid, allantoin, and a-bisabolol. 如請求項1之局部用配方,其更包含下列之一或多者:高嶺土(kaolin)、氧化鋅、沙棘油(hippophae rhamnoides oil)、松蘿酸(usnic acid)、羥苯基丙醯胺基苯甲酸(hydroxyphenyl propamidobenzoic acid)、二氧化鈦。 The topical formulation of claim 1 further comprising one or more of the following: kaolin, zinc oxide, hippophae rhamnoides oil, usnic acid, hydroxyphenyl propylamine Hydroxyphenyl propamidobenzoic acid, titanium dioxide. 如請求項1之局部用配方,其更包含下列之一或多者:咪唑啶基尿素(imidazolidinyl urea)、甲基氯異噻唑啉酮(methylchloroisothiazolinone),以及甲基異噻唑啉酮(methylisothiazolinone)。 The topical formulation of claim 1 further comprising one or more of the following: imidazolidinyl urea, methylchloroisothiazolinone, and methylisothiazolinone. 如請求項3與4中任一項之局部用配方,其中該配方具有 pH值範圍為約3.5-4.5。 The topical formulation of any one of claims 3 and 4, wherein the formulation has The pH range is from about 3.5 to about 4.5. 如請求項5之局部用配方,該配方具有pH值範圍為約7.0-8.0。 The topical formulation of claim 5 has a pH in the range of from about 7.0 to about 8.0. 一種局部用配方,其包含馬齒莧萃取物、無患子(Sapindus mukorossi)果萃取物,以及下列之至少一者:月桂醇聚醚硫酸銨(ammonium laureth sulfate)、椰油醯胺基丙基甜菜鹼(cocamidopropyl betaine)、椰油醯胺MEA(cocamide MEA)、椰油醯胺DEA(cocamide DEA)。 A topical formulation comprising a purslane extract, a sapindus mukorossi fruit extract, and at least one of the following: ammonium laureth sulfate, cocoamidopropyl betaine (cocamidopropyl betaine), cocamide MEA (cocamide MEA), cocamide DEA (cocamide DEA). 如請求項9之局部用配方,其係用於治療或預防痤瘡。 A topical formulation according to claim 9 for use in the treatment or prevention of acne. 如請求項1至4中任一項之局部用配方,其中該水楊酸之含量範圍為0.5-2.0% w/w。 The topical formulation of any one of claims 1 to 4, wherein the salicylic acid is present in an amount ranging from 0.5 to 2.0% w/w. 如請求項1之局部用配方,其中該配方為面霜或遮瑕膏。 A topical formulation as claimed in claim 1, wherein the formulation is a cream or concealer. 如請求項9之局部用配方,其中該配方為潔淨凝膠。 A topical formulation as claimed in claim 9, wherein the formulation is a clean gel. 如請求項12之局部用配方,其中該局部用配方為面霜時,該等草藥萃取物之結合濃度為至少0.9% w/w。 The topical formulation of claim 12, wherein the topical formulation is a face cream, the combined concentration of the herbal extracts being at least 0.9% w/w. 如請求項12之局部用配方,其中該局部用配方為遮瑕膏時,該等草藥萃取物之結合濃度為至少9.0% w/w。 The topical formulation of claim 12, wherein the topical formulation is a concealer, the combined concentration of the herbal extracts is at least 9.0% w/w. 如請求項12之局部用配方,當該局部用配方為面霜時,含有至少0.075%黃芩苷,而當該配方為遮瑕膏時,含有至少0.9%黃芩苷。 A topical formulation according to claim 12, which contains at least 0.075% baicalin when the topical formulation is a face cream and at least 0.9% baicalin when the formula is a concealer. 如請求項12之局部用配方,其中當該配方為遮瑕處理配方時,每一草藥萃取物之量為約3%。 The topical formulation of claim 12, wherein the amount of each herbal extract is about 3% when the formulation is a concealing treatment formulation. 如請求項12之局部用配方,其中當該配方為面霜配方時,每一草藥萃取物之量為約0.3%。 The topical formulation of claim 12, wherein the amount of each herbal extract is about 0.3% when the formulation is a cream formulation. 如請求項1之局部用配方,其中該配方提供有關皮脂分泌減少、皮膚油類吸收、抗發炎活性、抗菌活性、傷口癒合特性、抗氧化活性、皮膚刺激減少、配方之皮膚吸收,或任何其等結合之協同效用。 A topical formulation according to claim 1, wherein the formulation provides for reduction in sebum secretion, absorption of skin oil, anti-inflammatory activity, antibacterial activity, wound healing characteristics, antioxidant activity, reduction of skin irritation, skin absorption of the formula, or any thereof The synergistic utility of the combination. 一種治療痤瘡之方法,其包含局部施用如請求項1之局部用配方於有需要之個體的步驟。 A method of treating acne comprising the step of topically applying a topical formulation of claim 1 to an individual in need thereof.
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