TW201340991A - Composition for improving skin defensive power - Google Patents

Composition for improving skin defensive power Download PDF

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TW201340991A
TW201340991A TW102108990A TW102108990A TW201340991A TW 201340991 A TW201340991 A TW 201340991A TW 102108990 A TW102108990 A TW 102108990A TW 102108990 A TW102108990 A TW 102108990A TW 201340991 A TW201340991 A TW 201340991A
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composition
compound
skin
weight
protopanaxadiol
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TW102108990A
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TWI597068B (en
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Hyeon-Chung Kim
Yong-Joo Na
Eun-Hye Kim
Sung-Il Park
Youn-Joon Kim
Sang-Hoon Han
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Amorepacific Corp
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/13Coniferophyta (gymnosperms)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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)
    • A61K36/25Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258Panax (ginseng)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics 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
    • A61K8/9755Gymnosperms [Coniferophyta]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

Abstract

Disclosed is a composition for improving skin defensive power containing at least one of a protopanaxadiol compound and a Japanese nutmeg extract as an active ingredient.

Description

增進皮膚防護力的組成物a composition that enhances skin protection

本發明有關一種增進皮膚防護力的組成物。
The present invention relates to a composition for enhancing skin protection.

茶樹油、水楊酸、三氯沙(triclosan)、果酸等本身具有抗菌活性的物質早已用來預防或改善面皰或皮膚問題。然而,由於這些物質的抗菌活性可能造成皮膚刺激,並有相關法規限制許可濃度,因此這些物質所使用的濃度無法展現效用且難以達到實質成效。因此,需要研發一種展現出卓越抗菌及抗發炎效果又不會刺激皮膚的物質。Tea tree oil, salicylic acid, triclosan, fruit acid and the like which have antibacterial activity itself have long been used to prevent or ameliorate acne or skin problems. However, since the antibacterial activity of these substances may cause skin irritation and there are regulatory restrictions on the permitted concentration, the concentrations used by these substances are not effective and difficult to achieve substantial results. Therefore, there is a need to develop a substance that exhibits excellent antibacterial and anti-inflammatory effects without irritating the skin.

【引用之相關技術】[Related technology]

【專利文獻】[Patent Literature]

(專利文獻1) 韓國專利案第10-0884616號(2009年2月12日);
(專利文獻2) 韓國專利申請案公開號第10-2006-0043067號(2006年5月15日)。


(Patent Document 1) Korean Patent No. 10-0884616 (February 12, 2009);
(Patent Document 2) Korean Patent Application Publication No. 10-2006-0043067 (May 15, 2006).


【技術問題】
本發明旨在提供一種能增進皮膚防護力的組成物。
【technical problem】
The present invention aims to provide a composition capable of enhancing skin protection.

【技術方案】
在一大體態樣中,提供一種增進皮膚防護力的組成物,該組成物包含原人參二醇(protopanaxadiol)化合物及日本榧樹(Torreya nucifera)萃取物之其中至少一者作為活性成份。
【Technical solutions】
In a large aspect, a composition for enhancing skin protection is provided, which comprises at least one of a protopanaxadiol compound and a Torreya nucifera extract as an active ingredient.

在另一大體態樣中,提供一種增進皮膚防護力的組成物,該組成物包含原人參二醇(protopanaxadiol)化合物及日本榧樹(Torreya nucifera)萃取物之其中至少一者;以及表沒食子兒茶素沒食子酸酯(epigallocatechin gallate)作為活性成份。In another general aspect, a composition for enhancing skin protection is provided, the composition comprising at least one of a protopanaxadiol compound and a Japanese eucalyptus extract (Torreya nucifera); Epigallocatechin gallate is used as an active ingredient.

【有利功效】
本發明之組成物含有原人參二醇化合物及日本榧樹萃取物之其中至少一者以及視需要選用的表沒食子兒茶素沒食子酸酯(epigallocatechin gallate),該化合物能藉由促進抗菌胜肽的活性且增進皮膚自我防護力而展現出卓越的皮膚抗菌和抗發炎活性。

[Beneficial effect]
The composition of the present invention contains at least one of a protopanaxadiol compound and an extract of Japanese eucalyptus, and optionally an epigallocatechin gallate, which can be promoted by the compound The antibacterial peptide is active and promotes skin self-protection to exhibit excellent skin antibacterial and anti-inflammatory activity.

no

第1圖比較化合物K、日本榧樹籽油、表沒食子兒茶素沒食子酸酯、上述物質之混合物以及茶樹油對於皮膚中之抗菌胜肽表現的影響。
Figure 1 compares the effects of Compound K, Japanese eucalyptus seed oil, epigallocatechin gallate, a mixture of the above, and the performance of tea tree oil on the antibacterial peptide in the skin.

【最佳實施例】
當用於本文中,「皮膚(skin)」一詞意指覆蓋動物體表的組織,並且以最廣含義而言,其不僅包括臉部或身體,還包括頭皮和頭髮。當用於本文中,「萃取物(extract)」一詞廣義上包括任何從天然產物萃取而得的物質,而不論所使用之萃取方法、萃取溶劑、所萃取之成份或萃取物類型。例如,該萃取物可為萃取自天然產物的油類成份。當用於本文中,「皮膚防護力(skin defensive power)」一詞意指保護皮膚不受外來刺激或毒素侵害的能力。該刺激廣義上包括任何對皮膚有害的刺激,包括細菌、病毒、紫外線(UV)、乾燥、損傷,等等。
[best embodiment]
As used herein, the term "skin" means the tissue that covers the surface of an animal and, in its broadest sense, includes not only the face or body, but also the scalp and hair. As used herein, the term "extract" broadly includes any material extracted from a natural product, regardless of the extraction method employed, the extraction solvent, the extracted component, or the type of extract. For example, the extract can be an oil component extracted from a natural product. As used herein, the term "skin defensive power" means the ability to protect the skin from external stimuli or toxins. The stimulus broadly includes any irritating effects on the skin, including bacteria, viruses, ultraviolet light (UV), dryness, damage, and the like.

以下詳細說明本發明。The invention is described in detail below.

皮膚是藉由分泌抗菌胜肽來對抗細菌侵襲。因此,能促進皮膚中抗菌胜肽活性的物質可藉由增進皮膚的防護力而提高皮膚的抗菌和抗發炎能力又不會刺激皮膚。The skin resists bacterial attack by secreting antibacterial peptides. Therefore, a substance which can promote the activity of the antibacterial peptide in the skin can enhance the antibacterial and anti-inflammatory ability of the skin without irritating the skin by enhancing the protective effect of the skin.

另一方面,本發明提供一種增進皮膚防護力的組成物,該組成物包含原人參二醇化合物和日本榧樹萃取物其中至少一者作為活性成份。原人參二醇化合物或日本榧樹萃取物可藉由促進皮膚中的抗菌胜肽表現而提高皮膚防護力。因此,含有原人參二醇化合物及日本榧樹萃取物之其中至少一者的組成物可提高皮膚防護力,特別是提高皮膚的抗菌和抗發炎活性,且可進一步改善面皰和其他皮膚問題。在本發明的示例性實施例中,抗菌胜肽是一種回應外來刺激而誘發表現並且能控制入侵病原體的胜肽。代表性的實例包括hBD1、hBD2、LL37或RNA水解酶7(RNase7),但不僅限於此。In another aspect, the present invention provides a composition for enhancing skin protection comprising at least one of a protopanaxadiol compound and a Japanese eucalyptus extract as an active ingredient. The protopanaxadiol compound or the Japanese eucalyptus extract can enhance skin protection by promoting the performance of the antibacterial peptide in the skin. Therefore, the composition containing at least one of the protopanaxadiol compound and the Japanese eucalyptus extract can improve skin protection, particularly, enhance the antibacterial and anti-inflammatory activity of the skin, and can further improve the acne and other skin problems. In an exemplary embodiment of the invention, the antibacterial peptide is a peptide that induces expression in response to external stimuli and is capable of controlling invading pathogens. Representative examples include hBD1, hBD2, LL37 or RNA hydrolase 7 (RNase7), but are not limited thereto.

在本發明的示例性實施例中,該原人參二醇化合物是一種人參皂苷(ginsenoside),其為一種人參皂素(ginseng saponin)。在本發明的另一示例性實施例中,可利用酵素處理人參提取物,尤其是紅參提取物而獲得原人參二醇化合物。在本發明的另一示例性實施例中,該原人參二醇化合物包括化合物K。化合物K亦稱為人參皂苷M1,其係如化學式1所表示的20-O-(b-d-吡喃葡萄糖苷)-20(S)-原人參二醇 (20-O-(beta-d-glucopyranosyl)-20(S)-protopanaxadiol)。In an exemplary embodiment of the invention, the protopanaxadiol compound is a ginsenoside which is a ginseng saponin. In another exemplary embodiment of the present invention, the ginseng diol compound may be obtained by treating the ginseng extract, especially the red ginseng extract, with an enzyme. In another exemplary embodiment of the invention, the protopanaxadiol compound comprises Compound K. Compound K is also known as ginsenoside M1, which is a 20-O-(bd-glucopyranoside)-20(S)-protopanaxadiol represented by Chemical Formula 1 (20-O-(beta-d-glucopyranosyl) )-20(S)-protopanaxadiol).

[化學式1]

[Chemical Formula 1]

以該組成物的總重量計,根據本發明示例性實施例之組成物可包含0.001~10重量%、較佳0.01~5重量%、更佳為0.1~3重量%的原人參二醇化合物。當含有上述範圍的原人參二醇化合物時,可適當地達到本發明之期望效果,同時兼符合該組成物的安定性和安全性。此外,上述範圍亦可取得適當的成本效益。特別是,若該組成物的原人參二醇化合物含量少於0.001重量%,則其增進皮膚防護力的效果可能微不足道。又若該組成物的原人參二醇化合物含量超過10重量%,該組成物可能因原人參二醇化合物對溶劑的溶解度下降,而使該組成物的安定性降低。The composition according to an exemplary embodiment of the present invention may comprise 0.001 to 10% by weight, preferably 0.01 to 5% by weight, more preferably 0.1 to 3% by weight, based on the total weight of the composition, of the protopanaxadiol compound. When the protopanaxadiol compound of the above range is contained, the desired effects of the present invention can be suitably attained while satisfying the stability and safety of the composition. In addition, the above range can also be obtained with appropriate cost-effectiveness. In particular, if the composition has a protopanaxadiol compound content of less than 0.001% by weight, the effect of enhancing skin protection may be negligible. Further, if the content of the original panaxadiol compound of the composition exceeds 10% by weight, the composition may lower the solubility of the composition due to a decrease in the solubility of the original panaxadiol compound in the solvent.

在本發明之示例性實施例中,日本榧樹萃取物包含日本榧樹(Torreya nucifera)之樹實的萃取物,尤其是日本榧樹籽的萃取物。在本發明的另一示例性實施例中,日本榧樹萃取物包括油類及脂肪成份,例如藉由壓榨或使用有機溶劑萃取日本榧樹所取得的日本榧樹油,特別是日本榧樹籽油。該有機溶劑包括選自下述群組中的一或多種有機溶劑:乙醇、己烷、丙酮、乙酸乙酯、乙醚(diethyl ether)、甲乙酮(ethyl methyl ketone)及氯仿(chloroform),但不僅限於此。In an exemplary embodiment of the invention, the Japanese eucalyptus extract comprises a dendritic extract of Japanese eucalyptus (Torreya nucifera), especially an extract of Japanese eucalyptus seed. In another exemplary embodiment of the present invention, the Japanese eucalyptus extract includes oils and fat components, such as Japanese eucalyptus oil obtained by pressing or using an organic solvent to extract Japanese eucalyptus, especially Japanese eucalyptus seeds. oil. The organic solvent includes one or more organic solvents selected from the group consisting of ethanol, hexane, acetone, ethyl acetate, diethyl ether, ethyl methyl ketone, and chloroform, but is not limited thereto. this.

在本發明之示例性實施例中,以該組成物的總重量計,該組成物可含有0.001~99重量%、較佳0.1~80重量%、更佳為10~50重量%的日本榧樹萃取物。當含有上述範圍內的日本榧樹萃取物時,可適當地達到本發明之期望效果,同時兼符合該組成物的安定性和安全性。此外,上述範圍亦可取得適當的成本效益。特別是,若該組成物的日本榧樹萃取物含量少於0.001重量%,則其增進皮膚防護力的效果可能極小。In an exemplary embodiment of the present invention, the composition may contain 0.001 to 99% by weight, preferably 0.1 to 80% by weight, more preferably 10 to 50% by weight, of Japanese eucalyptus, based on the total weight of the composition. Extracts. When the Japanese eucalyptus extract in the above range is contained, the desired effects of the present invention can be suitably attained while satisfying the stability and safety of the composition. In addition, the above range can also be obtained with appropriate cost-effectiveness. In particular, if the Japanese eucalyptus extract content of the composition is less than 0.001% by weight, the effect of enhancing skin protection may be extremely small.

根據本發明示例性實施例之增進皮膚防護力的組成物可進一步包含表沒食子兒茶素沒食子酸酯。當本發明之增進皮膚防護力的組成物進一步含有表沒食子兒茶素沒食子酸酯時,該組成物可能由於具有較高的皮膚抗菌和抗發炎活性提升作用,因而具有更佳的皮膚防護力增進效果。
在本發明中,表沒食子兒茶素沒食子酸酯是一種多酚化合物且主要是存在綠茶中的兒茶素,且亦以(-)-表沒食子兒茶素-3-沒食子酸酯((-)-epigallocatechin-3-gallate)的化學式來表示。在本發明之示例性實施例中,可從綠茶中萃取出表沒食子兒茶素沒食子酸酯。
The composition for enhancing skin protection according to an exemplary embodiment of the present invention may further comprise epigallocatechin gallate. When the skin-protecting composition of the present invention further contains epigallocatechin gallate, the composition may have a better effect due to a higher skin antibacterial and anti-inflammatory activity enhancing effect. Skin protection enhances the effect.
In the present invention, epigallocatechin gallate is a polyphenolic compound and is mainly present in catechins in green tea, and is also (-)-epigallocatechin-3- The chemical formula of gallic acid ester ((-)-epigallocatechin-3-gallate) is shown. In an exemplary embodiment of the invention, epigallocatechin gallate can be extracted from green tea.

以化合物的總重量計,根據本發明示例性實施例之化合物可含有0.00001~10重量%、較佳0.0001~5重量%、更佳為0.001~1重量%的表沒食子兒茶素沒食子酸酯。當含有上述範圍內的表沒食子兒茶素沒食子酸酯時,可適當地達到本發明之期望效果,同時兼符合該組成物的安定性和安全性。此外,上述範圍亦可取得適當的成本效益。特別是,若該組成物的表沒食子兒茶素沒食子酸酯含量少於0.00001重量%,則其增進皮膚防護力的效果可能極微小。又若該組成物的表沒食子兒茶素沒食子酸酯含量超過10重量%,由於容易發生氧化反應,而難以確保調配物(formulation)的安定性。The compound according to an exemplary embodiment of the present invention may contain 0.00001 to 10% by weight, preferably 0.0001 to 5% by weight, more preferably 0.001 to 1% by weight, based on the total weight of the compound, of epigallocatechin. Acid ester. When the epigallocatechin gallate is contained in the above range, the desired effects of the present invention can be suitably attained while satisfying the stability and safety of the composition. In addition, the above range can also be obtained with appropriate cost-effectiveness. In particular, if the epigallocatechin gallate content of the composition is less than 0.00001% by weight, the effect of enhancing skin protection may be extremely small. Further, if the epigallocatechin gallate content of the composition exceeds 10% by weight, the oxidation reaction tends to occur, and it is difficult to ensure the stability of the formulation.

另一方面,本發明提供一種化妝品組成物,該化妝品組成物包含原人參二醇化合物及日本榧樹萃取物之其中至少一者;以及視需要選用的表沒食子兒茶素沒食子酸酯作為活性成份。該化妝品組成物可展現皮膚防護力增進效果,特別是展現卓越的抗菌和抗發炎活性,並且該化妝品組成物可進一步改善或預防面皰或其他皮膚問題。In another aspect, the present invention provides a cosmetic composition comprising at least one of a protopanaxadiol compound and an extract of Japanese eucalyptus; and an epigallocatechin gallate, optionally selected The ester acts as an active ingredient. The cosmetic composition exhibits a skin-protecting effect, particularly exhibiting excellent antibacterial and anti-inflammatory activity, and the cosmetic composition can further improve or prevent acne or other skin problems.

所提供的本發明之化妝品組成物可為任何適用於外用藥的調配物。例如,該化妝品組成物可製備成溶液、水包油乳化液、油包水乳化液、懸浮液、固體、凝膠、粉末、膏狀物、泡沫或氣溶膠(aerosol)的形式。可根據所屬技術領域中常用的方法製備出此種調配物。The cosmetic composition of the present invention provided may be any formulation suitable for external use. For example, the cosmetic composition can be prepared in the form of a solution, an oil-in-water emulsion, a water-in-oil emulsion, a suspension, a solid, a gel, a powder, a paste, a foam or an aerosol. Such formulations can be prepared according to methods commonly used in the art.

本發明之化妝品組成物可進一步包含保溼劑、潤敷劑(emollient)、界面活性劑、紫外線(UV)吸收劑、防腐劑、殺菌劑、抗氧化劑、酸鹼度(pH)控制劑、有機或無機顏料、香料、清涼劑或止汗劑。所屬技術領域中熟悉該項技藝者可輕易地決定此等成份在該化妝品組成物中的含量,且該等成份的含量範圍不會對本發明的目的及效果造成不良影響。以組成物的總重量計,該等成份的含量可為0.01~5重量%、較佳為0.01~3重量%。The cosmetic composition of the present invention may further comprise a humectant, an emollient, a surfactant, an ultraviolet (UV) absorber, a preservative, a bactericide, an antioxidant, a pH control agent, an organic or inorganic A pigment, a fragrance, a cooling agent or an antiperspirant. Those skilled in the art can readily determine the amount of such ingredients in the cosmetic composition, and the range of such ingredients will not adversely affect the objects and effects of the present invention. The content of the components may be from 0.01 to 5% by weight, preferably from 0.01 to 3% by weight, based on the total weight of the composition.

在另一方面,本發明提供一種藥學組成物,該藥學組成物包含原人參二醇化合物及日本榧樹萃取物之其中至少一者以及視需要選用的表沒食子兒茶素沒食子酸酯作為活性成份。該藥學組成物可展現皮膚防護力增進效果,特別是展現卓越的抗菌和抗發炎活性,且該藥學組成物可進一步改善或預防面皰及其他皮膚問題。In another aspect, the present invention provides a pharmaceutical composition comprising at least one of a protopanaxadiol compound and an extract of Japanese eucalyptus, and optionally epigallocatechin gallate. The ester acts as an active ingredient. The pharmaceutical composition exhibits a skin-protecting effect, particularly exhibiting excellent antibacterial and anti-inflammatory activity, and the pharmaceutical composition can further improve or prevent blistering and other skin problems.

可使用口服或非腸胃道(例如,直腸用藥、外敷用藥、經皮膚用藥、靜脈注射、肌肉注射、腹腔內注射或皮下注射)的方式施用根據本發明一態樣所做之藥學組成物。The pharmaceutical composition according to one aspect of the present invention can be administered orally or parenterally (for example, rectal, topical, transdermal, intravenous, intramuscular, intraperitoneal or subcutaneous).

用於口服用藥的調配物包括錠劑、片劑、硬膠囊或軟膠囊、顆粒、粉末、細粒、液體、乳劑或丸粒(pellet),但不僅限於此。此等調配物除活性成份之外還可含有稀釋劑(例如,乳糖、右旋糖、蔗糖、甘露醇、山梨醇、纖維素或甘胺酸)、潤滑劑(例如,氧化矽(silica)、滑石粉、硬脂酸或聚乙二醇)或黏合劑(例如,矽酸鋁鎂、澱粉糊、明膠、黃耆樹膠(tragacanth)、甲基纖維素、羥甲基纖維素鈉或聚乙烯吡咯烷酮)。如偶有需要,該藥學組成物亦可含有藥學添加物,例如,崩散劑、吸收劑、著色劑、香料、甜味劑,等等。可利用常用的混合、造粒或塗膜方法製備錠劑。Formulations for oral administration include, but are not limited to, tablets, tablets, hard or soft capsules, granules, powders, granules, liquids, emulsions or pellets. These formulations may contain, in addition to the active ingredient, diluents (for example, lactose, dextrose, sucrose, mannitol, sorbitol, cellulose or glycine), lubricants (for example, silica, Talc, stearic acid or polyethylene glycol) or binder (for example, aluminum magnesium citrate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose or polyvinylpyrrolidone ). The pharmaceutical composition may also contain pharmaceutical additives such as disintegrating agents, absorbents, coloring agents, perfumes, sweeteners, and the like, as occasion demands. Tablets can be prepared by conventional mixing, granulating or film coating methods.

用於非腸胃道用藥的調配物包括注射液、藥用滴劑、乳液(lotion)、油膏、凝膠、乳膏、懸浮液、乳化液、塞劑、貼布或噴霧,但不僅限於此。Formulations for parenteral administration include, but are not limited to, injections, pharmaceutical drops, lotions, ointments, gels, creams, suspensions, emulsions, stoppers, patches or sprays. .

根據本發明一態樣所做之藥學組成物的活性成份施用劑量將可隨著病患的年齡、性別、體重、欲進行治療的特殊疾病或病理狀態、疾病或病理狀態的嚴重程度、用藥途徑及診斷者的考量而改變。考量這些因素來決定用藥劑量是屬於所屬技術領域中熟悉該項技藝者的能力水平。每日用藥劑量可例如為0.1~100毫克/公斤/每日,較佳為5~50毫克/公斤/每日,但不僅限於此。The active ingredient of the pharmaceutical composition according to one aspect of the present invention may be administered in a dose corresponding to the age, sex, weight of the patient, the particular disease or pathological condition to be treated, the severity of the disease or pathological condition, and the route of administration. And the doctor's considerations change. Taking these factors into account to determine the dosage is a level of competence of those skilled in the art. The daily dose may be, for example, 0.1 to 100 mg/kg/day, preferably 5 to 50 mg/kg/day, but is not limited thereto.

[發明實施方式]
以下將藉由實施例和試驗例來詳細描述本發明。然而,下述實施例僅做為示範目的之用,所屬技術領域中具有通常技藝者將明白本發明範圍不受限於該等實施例。
[Inventions]
The invention will be described in detail below by way of examples and test examples. However, the following examples are for illustrative purposes only, and it is apparent to those skilled in the art that the scope of the invention is not limited by the embodiments.

[實施例]
利用酵素使紅參水解而獲得化合物K。藉由壓榨日本榧樹籽或使用有機溶劑對日本榧樹籽進行萃取以獲得日本榧樹籽油。
[Examples]
Compound K is obtained by hydrolyzing red ginseng with an enzyme. Japanese eucalyptus seed is extracted by pressing Japanese eucalyptus seeds or using an organic solvent to obtain Japanese eucalyptus seed oil.

依據下述方法獲得表沒食子兒茶素沒食子酸酯(EGCG)。首先,使用10倍體積的純水以熱水回流方式於30~70°C下對綠茶葉進行萃取1~24小時。經過濾後,去除殘餘物,並再次過濾餘留的濾液而分離出水溶性成份。從所分離出的水溶性成份中,利用結晶法選擇性地僅沈澱和濃縮表沒食子兒茶素沒食子酸酯。利用過濾法去除未沈澱的殘留濾液後,利用色層分析法(chromatography)純化該沈澱物。隨後,使溶劑蒸發,最後獲得高純度的表沒食子兒茶素沒食子酸酯。Epigallocatechin gallate (EGCG) was obtained according to the following method. First, the green tea leaves were extracted by hot water reflux at 10 to 70 ° C for 1 to 24 hours using 10 volumes of pure water. After filtration, the residue was removed, and the remaining filtrate was filtered again to separate the water-soluble component. From the separated water-soluble components, only epigallocatechin gallate is selectively precipitated and concentrated by crystallization. After the unprecipitated residual filtrate was removed by filtration, the precipitate was purified by chromatographic analysis. Subsequently, the solvent was evaporated, and finally high-purity epigallocatechin gallate was obtained.

[測驗例] 增進皮膚中之抗菌胜肽表現效果的評估[Test Example] Evaluation of the effect of improving the performance of antibacterial peptides in the skin

使用化合物K、日本榧樹籽油、表沒食子兒茶素沒食子酸酯(EGCG)、化合物K+日本榧樹籽油、化合物K+日本榧樹籽油+表沒食子兒茶素沒食子酸酯或茶樹油對HaCaT角質細胞 (HaCaT keratinocytes,由德國海德堡之德國癌症研究中心的N.E. Fusenig博士所提供)進行處理24小時之後,使用即時聚合酶鏈鎖反應法(real-time PCR)測量代表性皮膚抗菌胜肽hBD1、hBD2、LL37和RNA水解酶7(RNase7)的基因表現變化情形。第1圖(平均值)與表1(平均值±標準偏差值)中顯示經過處理之各個群組與未經處理之控制組的基因表現變化情形。Use compound K, Japanese eucalyptus seed oil, epigallocatechin gallate (EGCG), compound K + Japanese eucalyptus seed oil, compound K + Japanese eucalyptus seed oil + epigallocatechin Gallate or tea tree oil was treated with HaCaT keratinocytes (provided by Dr. NE Fusenig of the German Cancer Research Center in Heidelberg, Germany) for 24 hours, using real-time PCR. The changes in gene expression of representative skin antibacterial peptides hBD1, hBD2, LL37 and RNA hydrolase 7 (RNase7) were measured. Fig. 1 (average value) and Table 1 (mean ± standard deviation value) show changes in gene expression of each of the treated groups and the untreated control group.

[表1][Table 1]

可看出,化合物K、日本榧樹籽油、表沒食子兒茶素沒食子酸酯(EGCG)、化合物K+日本榧樹籽油、化合物K+日本榧樹籽油+表沒食子兒茶素沒食子酸酯皆能提高皮膚抗菌胜肽hBD1、hBD2、LL37和RNase7的表現,而來自天然產物且常用於抗菌化妝品中的茶樹油則會抑制此四種基因的表現。也就是說,儘管茶樹油不能增進皮膚防護力,但化合物K、日本榧樹籽油、表沒食子兒茶素沒食子酸酯(EGCG)及其混合物能夠藉由活化皮膚中的抗菌胜肽而增進皮膚防護力。It can be seen that compound K, Japanese eucalyptus seed oil, epigallocatechin gallate (EGCG), compound K + Japanese eucalyptus seed oil, compound K + Japanese eucalyptus seed oil + table gallop The tea gallate can enhance the performance of the skin antibacterial peptides hBD1, hBD2, LL37 and RNase7, while the tea tree oil from natural products and commonly used in antibacterial cosmetics inhibits the expression of these four genes. That is, although tea tree oil does not enhance skin protection, compound K, Japanese eucalyptus seed oil, epigallocatechin gallate (EGCG), and mixtures thereof can be achieved by activating antibacterial in the skin. Peptides enhance skin protection.

以下將詳細說明根據本發明示例性實施例所做之組成物的調配物實例,然而,該實例可應用於各種不同類型的調配物。且下述調配物實例並非意欲用於限制本發明範圍,而是僅作為解說之用。
[調配物實例1] 乳液
An example of a formulation of a composition according to an exemplary embodiment of the present invention will be described in detail below, however, the example can be applied to various different types of formulations. The following examples of formulations are not intended to limit the scope of the invention, but are merely illustrative.
[Formulation Example 1] Emulsion

根據常用方法以表2中所載的組成物製備乳液。The emulsion was prepared according to the composition contained in Table 2 according to a usual method.

[表2][Table 2]

[調配物實例2] 乳膏[Formulation Example 2] Cream

根據常用方法以表3中所載的組成物製備乳膏。Creams were prepared according to the compositions contained in Table 3 according to the usual methods.

[表3][table 3]

[調配物實例3] 面膜[Formulation Example 3] Mask

根據常用方法以表4中所載的組成物製備面膜。The mask was prepared according to the composition contained in Table 4 according to a usual method.

[表4][Table 4]

[調配物實例4] 軟膠囊[Formulation Example 4] Soft Capsules

根據常用方法將原人參二醇化合物(50毫克)、日本榧樹萃取物(200毫克)、表沒食子兒茶素沒食子酸酯(10毫克)、大豆萃取物(50毫克)、大豆油(180毫克)、棕櫚油(2毫克)、氫化棕櫚油(8毫克)、黃色蜂蠟(4毫克)及卵磷脂(6毫克)混合並製備成軟膠囊。The original ginseng diol compound (50 mg), Japanese eucalyptus extract (200 mg), epigallocatechin gallate (10 mg), soy extract (50 mg), large Soybean oil (180 mg), palm oil (2 mg), hydrogenated palm oil (8 mg), yellow beeswax (4 mg) and lecithin (6 mg) were mixed and prepared into soft capsules.

[調配物實例5] 錠劑[Formulation Example 5] Lozenges

混合化合物K(10毫克)、日本榧樹籽油(200毫克)、表沒食子兒茶素沒食子酸酯(10毫克)、大豆萃取物(50毫克)、葡萄糖(100毫克)、澱粉(96毫克)及硬脂酸鎂(4毫克),並於混合物中添加30%的乙醇(40毫克)以形成顆粒。待顆粒乾燥後,使用打錠機將該顆粒製備成錠劑。

Mixed compound K (10 mg), Japanese eucalyptus seed oil (200 mg), epigallocatechin gallate (10 mg), soy extract (50 mg), glucose (100 mg), starch (96 mg) and magnesium stearate (4 mg), and 30% ethanol (40 mg) was added to the mixture to form granules. After the granules were dried, the granules were prepared into tablets using a tablet machine.

no

Claims (10)

一種增進皮膚防護力的組成物,該組成物包含一原人參二醇化合物及一日本榧樹(Torreya nucifera)萃取物其中至少一者以作為活性成份。A composition for enhancing skin protection, comprising at least one of a proto-ginseng diol compound and a Japanese eucalyptus extract (Torreya nucifera) as an active ingredient. 如請求項1所述之組成物,其中該原人參二醇化合物包括化合物K(20-O-(b-d-吡喃葡萄糖苷)-20(S)-原人參二醇)。The composition of claim 1, wherein the protopanaxadiol compound comprises the compound K (20-O-(b-d-glucopyranoside)-20(S)-protopanaxadiol). 如請求項1所述之組成物,其中該日本榧樹萃取物包括日本榧樹籽油。The composition of claim 1, wherein the Japanese eucalyptus extract comprises Japanese eucalyptus seed oil. 如請求項1所述之組成物,其中以該組成物的總重量計,該組成物包含0.001~10重量%的該原人參二醇化合物。The composition of claim 1, wherein the composition comprises 0.001 to 10% by weight of the protopanaxadiol compound based on the total weight of the composition. 如請求項1所述之組成物,其中以該組成物的總重量計,該組成物包含0.001~99重量%的該日本榧樹萃取物。The composition of claim 1, wherein the composition comprises 0.001 to 99% by weight of the Japanese eucalyptus extract based on the total weight of the composition. 如請求項1所述之組成物,其中該組成物進一步包含表沒食子兒茶素沒食子酸酯(epigallocatechin gallate)。The composition of claim 1, wherein the composition further comprises epigallocatechin gallate. 如請求項6所述之組成物,其中以該組成物的總重量計,該組成物包含0.00001~10重量%的表沒食子兒茶素沒食子酸酯。The composition of claim 6, wherein the composition comprises 0.00001 to 10% by weight of epigallocatechin gallate, based on the total weight of the composition.  如請求項1所述之組成物,其中該組成物增進皮膚的抗菌和抗發炎活性。The composition of claim 1, wherein the composition enhances antibacterial and anti-inflammatory activity of the skin.  如請求項1所述之組成物,其中該組成物促進皮膚中之抗菌胜肽的表現。The composition of claim 1, wherein the composition promotes the performance of an antimicrobial peptide in the skin.  如請求項1至9中任一項所述之組成物,其中該組成物是一化妝品組成物。The composition of any one of claims 1 to 9, wherein the composition is a cosmetic composition.
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