TWI421098B - New use of new hesperidin - Google Patents
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- TWI421098B TWI421098B TW100130511A TW100130511A TWI421098B TW I421098 B TWI421098 B TW I421098B TW 100130511 A TW100130511 A TW 100130511A TW 100130511 A TW100130511 A TW 100130511A TW I421098 B TWI421098 B TW I421098B
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本發明涉及新橙皮苷的新用途，特別是在化妝品方面的新用途，更特別是新橙皮苷作為改善皮膚微循環的化學成分的作用，特別是在用於祛除眼部黑眼圈方面的新用途。The present invention relates to a novel use of new hesperidin, in particular for cosmetic use, and more particularly to the action of neohesperidin as a chemical component for improving skin microcirculation, particularly for removing dark circles of the eye. New use.
人體眼部皮膚的構造有別於人體肌膚的其它部位，首先眼部周圍的顴骨之上和鼻樑兩旁是血管和淋巴的“輸送位點”，該部位是面部微靜脈交匯的場所，並且血管非常幼細而豐富，若眼部微循環不足，將導致血液迴圈不暢或組織水腫造成血液瘀腫、水分固積；同時，眼部周圍的皮膚非常薄僅為其他部位皮膚厚度的1/10，通過光線折射後極易在眼周出現紫黑色，形成黑眼圈。而疲勞、壓力、睡眠不足等原因，是導致微循環障礙的重要因素，加之年歲漸長，肌膚每十年就會減少約6%的厚度，黑眼圈將更加明顯。因此無論短暫的或長期的，不同年齡的女性都曾經或一直有被黑眼圈問題所困擾的經歷，需通過改善眼周肌膚的微循環加以改善。The structure of the skin of the human eye is different from other parts of the human skin. First, above the humerus around the eye and on both sides of the bridge of the nose are the "transport sites" of blood vessels and lymph, which are the sites where the facial venules meet and the blood vessels Very fine and rich, if the eye microcirculation is insufficient, it will lead to poor blood circulation or tissue edema, resulting in blood swelling and water accumulation. At the same time, the skin around the eye is very thin only 1/ of the skin thickness of other parts. 10, after the light is refracted, it is easy to appear purple black in the eye, forming dark circles. Fatigue, stress, lack of sleep and other reasons are important factors leading to microcirculatory disorders. In addition, as the age grows, the skin will reduce thickness by about 6% every ten years, and dark circles will become more obvious. Therefore, regardless of the short-term or long-term, women of different ages have or have been plagued by dark circles problems, and need to improve by improving the microcirculation of the skin around the eyes.
文獻報導很多天然植物提取物經口服和靜脈等途徑應用後可以顯著改善皮膚的微循環，如：紅花提取物、丹參提取物、銀杏葉提取物、假葉樹提取物、金雀花提取物、柑橘提取物、人參提取物等。同時也有文獻報導了從上述植物提取物中提取純化到的一些單體成分如丹參酮、人參皂甙、β-七葉皂苷、魯斯可皂苷、銀杏黃酮等局部外用於人體皮膚後對微循環的作用，結果表明這些化學物質經局部施用於皮膚表面後均不能顯著改善皮膚微循環。The literature reports that many natural plant extracts can significantly improve skin microcirculation after oral and intravenous application, such as: safflower extract, salvia extract, ginkgo biloba extract, false leaf tree extract, gorse extract, Citrus extract, ginseng extract, etc. At the same time, there are also reports on the effects of some monomer components extracted from the above plant extracts such as tanshinone, ginsenoside, β-escin, saponin, ginkgo flavonoids, etc. on human skin after micro-circulation. The results showed that these chemicals did not significantly improve skin microcirculation after topical application to the skin surface.
目前市面上所售的改善皮膚微循環(例如改善眼部皮膚微循環，例如祛除黑眼圈)的眼部產品層出不窮，大多是添加了一些植物提取物，但是一方面這些提取物中是何種或何類成分發揮效果不明確，另一方面這些產品祛除黑眼圈的效果並不明顯，大多數改善皮膚微循環(例如用於祛黑眼圈)的產品經消費者使用後並未產生預期的效果(例如祛黑眼圈功效)。因此尋找經局部外用後能顯著改善皮膚微循環的化學物質，用以開發改善皮膚微循環(例如改善眼部皮膚微循環，例如祛除黑眼圈)的產品，特別是祛除黑眼圈的眼部護理產品，仍是本領域人員重點研究的方向。At present, the eye products sold on the market to improve skin microcirculation (for example, to improve eye microcirculation, such as removing dark circles) are endless, and most of them are added with some plant extracts, but on the one hand, what kind of extracts are or The effects of these ingredients are not clear. On the other hand, the effect of removing dark circles from these products is not obvious. Most products that improve skin microcirculation (for example, for dark circles) do not produce the desired results after being used by consumers. For example, dark circles effect). Therefore, looking for chemicals that can significantly improve skin microcirculation after topical application, to develop products that improve skin microcirculation (such as improving eye microcirculation, such as removing dark circles), especially eye care products that remove dark circles. It is still the focus of research in this field.
新橙皮苷是一種二氫黃酮，來源於芸香科枳屬植物枳(拉丁名：Poncirus trifoliate(L.) Raf.)的果實，其結構式如下：Neohesperidin is a dihydroflavonoid derived from the fruit of the genus Rutaceae (Poncirus trifoliate (L.) Raf.). Its structural formula is as follows:
分子式C28 H34 O15 ，分子量610.56。主要用於二氫查爾酮類新型甜味劑的製備。據文獻報導，新橙皮苷在抗過敏方面具有一定的療效，而關於新橙皮苷在改善皮膚微循環方面的用途尚未見有報導。開發新的具有改善皮膚微循環作用的產品特別是具有改善眼部皮膚微循環作用的產品，仍是本領域技術人員期待的。Molecular formula C 28 H 34 O 15 , molecular weight 610.56. Mainly used in the preparation of new sweeteners of dihydrochalcone. According to the literature, neohesperidin has a certain effect on anti-allergy, and the use of neohesperidin in improving skin microcirculation has not been reported. It is still desirable to those skilled in the art to develop new products having an effect of improving skin microcirculation, particularly products having an effect of improving microcirculation of the ocular skin.
本發明的目的在於提供新橙皮苷在改善皮膚微循環(例如改善眼部皮膚微循環，例如祛除黑眼圈)的方面的新用途。本發明令人意外地發現，使用新橙皮苷或者包含新橙皮苷的植物提取物可以有效地改善皮膚微循環，特別是改善眼部皮膚微循環，更特別是可以有效地祛除黑眼圈。本發明基於上述發現而得以完成。It is an object of the present invention to provide new uses of neohesperidin for improving skin microcirculation, such as improving ocular skin microcirculation, such as dark circles. The present inventors have surprisingly found that the use of neohesperidin or a plant extract comprising neohesperidin can effectively improve skin microcirculation, particularly to improve ocular skin microcirculation, and more particularly to effectively remove dark circles. The present invention has been completed based on the above findings.
為此，本發明第一方面提供了新橙皮苷或包含新橙皮苷的植物提取物在製備用於改善和/或促進皮膚微循環，或者消除和/或緩解與皮膚微循環不良有關的病症或狀態的產品中的用途。例如在用於改善和/或促進哺乳動物(特別是人的)皮膚微循環，或者消除和/或緩解與哺乳動物(特別是人的)皮膚微循環不良有關的病症或狀態的產品中的用途。To this end, the first aspect of the present invention provides a novel hesperidin or a plant extract comprising neohesperidin in the preparation for improving and/or promoting skin microcirculation, or eliminating and/or alleviating skin microcirculation. Use in products of illness or condition. Use, for example, in products for improving and/or promoting microcirculation of the skin of a mammal, particularly a human, or for eliminating and/or alleviating a condition or condition associated with poor microcirculation of the skin of a mammal, particularly a human. .
根據本發明第一方面的用途，其中所述皮膚微循環是眼部皮膚微循環。The use according to the first aspect of the invention, wherein the skin microcirculation is an ocular skin microcirculation.
根據本發明第一方面的用途，其中所述與皮膚微循環不良有關的病症或狀態是指與眼部皮膚微循環不良有關的病症或狀態。The use according to the first aspect of the invention, wherein the condition or condition associated with poor skin microcirculation refers to a condition or condition associated with poor microcirculation of the ocular surface of the eye.
根據本發明第一方面的用途，其中所述與眼部皮膚微循環不良有關的病症或狀態是指黑眼圈。The use according to the first aspect of the invention, wherein the condition or condition associated with poor microcirculation of the ocular skin refers to dark circles.
根據本發明第一方面的用途，其中所述包含新橙皮苷的植物提取物是指由芸香料枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物。The use according to the first aspect of the invention, wherein the plant extract comprising neohesperidin refers to an extract obtained from fruit extraction of Poncirus trifoliate (L.) Raf.
根據本發明第一方面的用途，其中所述包含新橙皮苷的植物提取物是指由芸香料枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物，並且該提取物中新橙皮苷含量不低於50重量%。在一個優選實施方案中，該提取物中新橙皮苷含量達到60重量%以上、70重量%以上、80重量%以上、85重量%以上、90重量%以上、或95重量%以上。The use according to the first aspect of the invention, wherein the plant extract containing neohesperidin refers to an extract obtained from fruit extraction of Poncirus trifoliate (L.) Raf. The content of neohesperidin in the extract is not less than 50% by weight. In a preferred embodiment, the content of neohesperidin in the extract is 60% by weight or more, 70% by weight or more, 80% by weight or more, 85% by weight or more, 90% by weight or more, or 95% by weight or more.
根據本發明第一方面的用途，其中所述產品是局部施用的產品。Use according to the first aspect of the invention, wherein the product is a topically applied product.
根據本發明第一方面的用途，其中所述產品是皮膚外用的局部施用的產品。Use according to the first aspect of the invention, wherein the product is a topically applied product for external use on the skin.
根據本發明第一方面的用途，其中所述產品是用於眼部皮膚的局部施用的產品。Use according to the first aspect of the invention, wherein the product is a product for topical application to the skin of the eye.
根據本發明第一方面的用途，其中所述產品是化妝品。Use according to the first aspect of the invention, wherein the product is a cosmetic.
根據本發明第一方面的用途，其中所述產品是呈溶液、乳狀、膏狀、乳膏、或凝膠的形式。Use according to the first aspect of the invention, wherein the product is in the form of a solution, a milk, a paste, a cream, or a gel.
根據本發明第一方面的用途，其中所述產品中包含：(1)新橙皮苷或包含新橙皮苷的植物提取物，和(2)生理學可接受的賦形劑。Use according to the first aspect of the invention, wherein the product comprises: (1) neohesperidin or a plant extract comprising neohesperidin, and (2) a physiologically acceptable excipient.
根據本發明第一方面的用途，其中所述產品中包含：(1)新橙皮苷或包含新橙皮苷的植物提取物，和(2)生理學可接受的賦形劑；並且其中所述新橙皮苷或包含新橙皮苷的植物提取物占該產品總重量的百分數以新橙皮苷計為0.01-20重量%。在一個實施方案中，所述新橙皮苷或包含新橙皮苷的植物提取物占該產品總重量的百分數以新橙皮苷計為0.01-15重量%、0.05-15重量%、0.1-10重量%、0.2-10重量%、或0.2-5重量%。Use according to the first aspect of the invention, wherein the product comprises: (1) neohesperidin or a plant extract comprising neohesperidin, and (2) a physiologically acceptable excipient; The percentage of total hesperidin or plant extract containing neohesperidin to the total weight of the product is from 0.01 to 20% by weight based on neohesperidin. In one embodiment, the neohesperidin or plant extract comprising neohesperidin comprises from 0.01% to 15% by weight, from 0.05% to 15% by weight, based on the total weight of the product, of neohesperidin. 10% by weight, 0.2-10% by weight, or 0.2-5% by weight.
本發明第二方面提供一種組合物，其包含：(1)有效量的新橙皮苷或包含新橙皮苷的植物提取物，和任選的(2)生理學可接受的賦形劑。A second aspect of the invention provides a composition comprising: (1) an effective amount of neohesperidin or a plant extract comprising neohesperidin, and optionally (2) a physiologically acceptable excipient.
根據本發明第二方面的組合物，其包含：(1)有效量的新橙皮苷或包含新橙皮苷的植物提取物，和任選的(2)生理學可接受的賦形劑；並且其中所述新橙皮苷或包含新橙皮苷的植物提取物占該組合物總重量的百分數以新橙皮苷計為0.01-20重量%。在一個實施方案中。所述新橙皮苷或包含新橙皮苷的植物提取物占該組合物總重量的百分數以新橙皮苷計為0.01-15重量%、0.05-15重量%、0.1-10重量%、0.2-10重量%、或0.2-5重量%。A composition according to the second aspect of the invention, comprising: (1) an effective amount of neohesperidin or a plant extract comprising neohesperidin, and optionally (2) a physiologically acceptable excipient; And wherein the novel hesperidin or the plant extract comprising neohesperidin is 0.01% by weight based on the total weight of the composition, based on neohesperidin. In one embodiment. The percentage of the total hesperidin or the plant extract containing the new hesperidin to the total weight of the composition is 0.01-15% by weight, 0.05-15% by weight, 0.1-10% by weight, 0.2 based on the neohesperidin. -10% by weight, or 0.2% to 5% by weight.
根據本發明第二方面的組合物，其中所述包含新橙皮苷的植物提取物是指由芸香科枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物。The composition according to the second aspect of the invention, wherein the plant extract containing neohesperidin refers to an extract obtained from fruit extraction of Poncirus trifoliate (L.) Raf.
根據本發明第二方面的組合物，其中所述包含新橙皮苷的植物提取物是指由芸香科枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物，並且該提取物中新橙皮苷含量不低於50重量%。在一個優選實施方案中，該提取物中新橙皮苷含量達到60重量%以上、70重量%以上、80重量%以上、85重量%以上、90重量%以上、或95重量%以上。The composition according to the second aspect of the invention, wherein the plant extract containing neohesperidin refers to an extract obtained from fruit extraction of Poncirus trifoliate (L.) Raf. The content of neohesperidin in the extract is not less than 50% by weight. In a preferred embodiment, the content of neohesperidin in the extract is 60% by weight or more, 70% by weight or more, 80% by weight or more, 85% by weight or more, 90% by weight or more, or 95% by weight or more.
根據本發明第二方面的組合物，其是用作改善和/或促進皮膚微循環，或者消除和/或緩解與皮膚微循環不良有關的病症或狀態的產品。在一個實施方案中，所述皮膚微循環是眼部皮膚微循環。在一個實施方案中，所述與皮膚微循環不良有關的病症或狀態是指與眼部皮膚微循環不良有關的病症或狀態。在一個實施方案中，其中所述與眼部皮膚微循環不良有關的病症或狀態是指黑眼圈。A composition according to the second aspect of the invention for use as a product for improving and/or promoting microcirculation of the skin, or for eliminating and/or alleviating a condition or condition associated with poor microcirculation of the skin. In one embodiment, the skin microcirculation is an ocular skin microcirculation. In one embodiment, the condition or condition associated with poor skin microcirculation refers to a condition or condition associated with poor microcirculation of the ocular surface of the eye. In one embodiment, the condition or condition associated with poor microcirculation of the ocular skin refers to dark circles.
根據本發明第二方面的組合物，其是用作局部施用的產品。A composition according to the second aspect of the invention, which is a product for topical application.
根據本發明第二方面的組合物，其是用作皮膚外用的局部施用的產品。A composition according to the second aspect of the invention, which is a product for topical application for external application to the skin.
根據本發明第二方面的組合物，其是用作眼部皮膚的局部施用的產品。A composition according to the second aspect of the invention, which is a product for topical application to the skin of the eye.
根據本發明第二方面的組合物，其是化妝品。A composition according to the second aspect of the invention, which is a cosmetic.
根據本發明第二方面的組合物，其是呈溶液、乳狀、膏狀、乳膏、或凝膠的形式。A composition according to the second aspect of the invention, which is in the form of a solution, a milk, a paste, a cream, or a gel.
本發明第三方面提供在有需要的個體中改善和/或促進皮膚微循環，或者消除和/或緩解與皮膚微循環不良有關的病症或狀態的方法，該方法包括給該個體施用有效量的新橙皮苷或包含新橙皮苷的植物提取物。A third aspect of the invention provides a method of ameliorating and/or promoting skin microcirculation in an individual in need thereof, or eliminating and/or alleviating a condition or condition associated with poor microcirculation of the skin, the method comprising administering to the individual an effective amount of New hesperidin or a plant extract containing neohesperidin.
根據本發明第三方面的方法，其中所述皮膚微循環是眼部皮膚微循環。A method according to the third aspect of the invention, wherein said skin microcirculation is an ocular skin microcirculation.
根據本發明第三方面的方法，其中所述與皮膚微循環不良有關的病症或狀態是指與眼部皮膚微循環不良有關的病症或狀態。The method according to the third aspect of the present invention, wherein the condition or state associated with poor skin microcirculation refers to a condition or state associated with poor microcirculation of the ocular surface of the eye.
根據本發明第三方面的方法，其中所述與眼部皮膚微循環不良有關的病症或狀態是指黑眼圈。The method according to the third aspect of the invention, wherein the condition or state associated with poor microcirculation of the ocular skin refers to dark circles.
根據本發明第三方面的方法，其中所述包含新橙皮苷的植物提取物是指由芸香科枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物。The method according to the third aspect of the invention, wherein the plant extract containing neohesperidin refers to an extract obtained by fruit extraction of Poncirus trifoliate (L.) Raf.
根據本發明第三方面的方法，其中所述包含新橙皮苷的植物提取物是指由芸香科枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得的提取物，並且該提取物中新橙皮苷含量不低於50重量%。在一個優選實施方案中，該提取物中新橙皮苷含量達到60重量%以上、70重量%以上、80重量%以上、85重量%以上、90重量%以上、或95重量%以上。The method according to the third aspect of the invention, wherein the plant extract containing neohesperidin refers to an extract obtained from fruit extraction of Poncirus trifoliate (L.) Raf. The content of neohesperidin in the extract is not less than 50% by weight. In a preferred embodiment, the content of neohesperidin in the extract is 60% by weight or more, 70% by weight or more, 80% by weight or more, 85% by weight or more, 90% by weight or more, or 95% by weight or more.
根據本發明第三方面的方法，其中所述有效量的新橙皮苷或包含新橙皮苷的植物提取物是以局部施用的產品的形式施用的。The method according to the third aspect of the invention, wherein the effective amount of neohesperidin or a plant extract comprising neohesperidin is administered in the form of a topically applied product.
根據本發明第三方面的方法，其中所述有效量的新橙皮苷或包含新橙皮苷的植物提取物是以皮膚外用的局部施用的產品的形式施用的。The method according to the third aspect of the invention, wherein the effective amount of neohesperidin or a plant extract comprising neohesperidin is administered in the form of a topically applied product for external application to the skin.
根據本發明第三方面的方法，其中所述有效量的新橙皮苷或包含新橙皮苷的植物提取物是以用於眼部皮膚的局部施用的產品的形式施用的。The method according to the third aspect of the invention, wherein the effective amount of neohesperidin or a plant extract comprising neohesperidin is administered in the form of a product for topical application to the ocular skin.
根據本發明第三方面的方法，其中所述有效量的新橙皮苷或包含新橙皮苷的植物提取物是以化妝品的形式施用的。The method according to the third aspect of the invention, wherein the effective amount of neohesperidin or a plant extract comprising neohesperidin is administered in the form of a cosmetic.
根據本發明第三方面的方法，其中所述有效量的新橙皮苷或包含新橙皮苷的植物提取物是以呈溶液、乳狀、膏狀、乳膏、或凝膠的形式施用的。The method according to the third aspect of the invention, wherein the effective amount of neohesperidin or a plant extract comprising neohesperidin is administered in the form of a solution, a milk, a paste, a cream, or a gel. .
本發明任一方面或該任一方面的任一具體實施方案所具有的特徵同樣適用於該方面的其它任一具體實施方案，也同樣適用於其它任一方面或其它任一方面的任一具體實施方案。Any aspect of any aspect of the invention or any one of the aspects of the invention is equally applicable to any other specific embodiment of the aspect, and is equally applicable to any of any other aspect or any other aspect. implementation plan.
面對本發明的各個方面和特點作進一步的描述。Various aspects and features of the present invention are further described.
本發明所引述的所有文獻，它們的全部內容通過引用併入本文，並且如果這些文獻所表達的含義與本發明不一致時，以本發明的表述為準。此外，本發明使用的各種術語和短語具有本領域技術人員公知的一般含義，即便如此，本發明仍然希望在此對這些術語和短語作更詳盡的說明和解釋，提及的術語和短語如有與公知含義不一致的，以本發明所表述的含義為準。All documents cited in the present invention are hereby incorporated by reference in their entirety, and if the meanings expressed by these documents are inconsistent with the present invention, the expression of the present invention shall prevail. Moreover, the various terms and phrases used in the present invention have the ordinary meanings that are known to those skilled in the art, and even though the present invention is intended to provide a more detailed description and explanation of the terms and phrases herein, the terminology and short If the language is inconsistent with the well-known meaning, the meaning expressed in the present invention shall prevail.
如本文所述的，術語“皮膚微循環”，是指皮膚真皮層下的微血管網，是迴圈的終末部分，屬於毛細血管，是動靜脈交接點，是血液與組織細胞進行物質交換的場所。皮膚微循環是一個複雜的動力系統，對皮膚顏色、溫度調節、皮膚代謝和透皮轉運起著非常重要的作用，直接影響皮膚的健康。As used herein, the term "skin microcirculation" refers to the microvascular network under the dermis of the skin, which is the terminal part of the loop, which belongs to the capillaries, is the arteriovenous junction, and is the place where the blood and tissue cells exchange material. . Skin microcirculation is a complex dynamic system that plays a very important role in skin color, temperature regulation, skin metabolism and transdermal transport, directly affecting skin health.
如本文所述的，術語“與皮膚微循環不良有關的病症或狀態”，是指由於皮膚局部微循環不良或障礙而出現的病理性或非病理性的身體狀態或者異常情況，例如皮炎、色素沉著、皮膚老化、皮膚蒼白、紅血絲、局部皮膚瘀腫、局部水分固積、黑眼圈等。As used herein, the term "disease or condition associated with poor microcirculation of the skin" refers to a pathological or non-pathological physical condition or abnormal condition that occurs due to local microcirculation or disorder of the skin, such as dermatitis, pigmentation. Calming, skin aging, pale skin, red blood, local skin bloated, local water accumulation, dark circles and so on.
如本文所述的，術語“改善”、“促進”、“消除”、“緩解”，例如本文所述“改善和/或促進皮膚微循環”和“消除和/或緩解與皮膚微循環不良有關的病症或狀態”，是指使由於皮膚局部微循環不良或障礙而出現病理性或非病理性的身體狀態或者異常情況產生有益的作用，例如改善皮膚局部微循環、促進皮膚局部微循環、消除由於皮膚局部微循環不良或障礙而出現病理性或非病理性的身體狀態或者異常情況、緩解由於皮膚局部微循環不良或障礙而出現病理性或非病理性的身體狀態或者異常情況。例如改善紅血絲、消除色素沉著、消除水腫、緩解瘀腫、消除黑眼圈等。As used herein, the terms "improving," "promoting," "eliminating," "alleviating," such as "improving and/or promoting skin microcirculation" and "eliminating and/or alleviating skin microcirculation are described herein. "The condition or state" refers to a beneficial effect of a pathological or non-pathological physical state or abnormal condition due to local microcirculation or disorder of the skin, such as improving local microcirculation of the skin, promoting local microcirculation of the skin, and eliminating A pathological or non-pathological physical state or abnormal condition occurs in the skin with microcirculation or disorder, and a pathological or non-pathological physical state or abnormality occurs due to local microcirculation or disorder of the skin. For example, improve red blood, eliminate pigmentation, eliminate edema, relieve swelling, eliminate dark circles and so on.
如本文所述的，術語“生理學可接受的”是指生理學相容的，特別是皮膚外用產品中使用的與皮膚接觸時可以使用的，例如不產生對皮膚的刺激性等副作用。特別是例如化妝品中可以使用的稀釋劑、表面活性劑、增稠劑、潤膚劑等。As used herein, the term "physiologically acceptable" means physiologically compatible, particularly when used in contact with the skin for use in external skin products, for example, without causing side effects such as irritation to the skin. In particular, for example, a diluent, a surfactant, a thickener, an emollient, or the like which can be used in cosmetics.
如本文所述的，術語“有效量”是指可在受試者中實現治療、預防、減輕和/或緩解本發明所述疾病或病症的劑量。As used herein, the term "effective amount" refers to a dose that can achieve treatment, prevention, alleviation, and/or alleviation of a disease or condition described herein in a subject.
如本文所述的，術語“組合物”，其還可以是指“化妝品”、“化妝品組合物”、“藥物組合物”，其可用於在個體中實現治療、預防、減輕和/或緩解本發明所述疾病、病症、或身體狀態。As used herein, the term "composition," which may also refer to "cosmetic," "cosmetic composition," "pharmaceutical composition," which can be used to achieve treatment, prevention, alleviation, and/or alleviation in an individual. The invention is a disease, disorder, or physical condition.
如本文所述的，術語“個體”，其還可以是指“受試者”、“患者”或者其它接受本發明組合物以改善和/或促進其出現的皮膚微循環，或者消除和/或緩解其出現的與皮膚微循環不良有關的病症或狀態的動物，特別是哺乳動物，例如人、狗、猴、牛、馬等，特別是人。As used herein, the term "individual" may also mean "subject", "patient" or other skin microcirculation that accepts the compositions of the invention to ameliorate and/or promote its appearance, or eliminate and/or An animal, particularly a mammal, such as a human, a dog, a monkey, a cow, a horse, etc., particularly a human, which alleviates the condition or condition in which it is associated with poor microcirculation of the skin.
如本文所述的，術語“眼部皮膚微循環”是指眼睛周圍的皮膚中的微循環。As used herein, the term "ocular skin microcirculation" refers to microcirculation in the skin surrounding the eye.
根據本發明，所述新橙皮苷可由芸香科枳屬植物枳(Poncirus trifoliate(L.) Raf.)的果實提取獲得，也可以根據本領域已知的化學方法合成或經生物轉化而得。該新橙皮苷可以是單體化合物，也可以是新橙皮苷含量不低於50%(w/w)的提取物。在本發明中，以新橙皮苷單體化合物使用量計，新橙皮苷以0.01%-20%(w/w)、優選0.05%-15%(w/w)、最優選0.1%-10%(w/w)的濃度用於本發明的組合物中。According to the present invention, the novel hesperidin can be obtained from the fruit extraction of Poncirus trifoliate (L.) Raf., or can be synthesized according to chemical methods known in the art or biotransformed. The neohesperidin may be a monomeric compound or an extract having a neohesperidin content of not less than 50% (w/w). In the present invention, neohesperidin is 0.01%-20% (w/w), preferably 0.05%-15% (w/w), most preferably 0.1%, based on the amount of neohesperidin monomer compound used. A concentration of 10% (w/w) is used in the composition of the present invention.
本發明也包括含新橙皮苷的化妝品護膚組合物。The present invention also encompasses cosmetic skin care compositions containing neohesperidin.
本發明涉及一種化妝品護膚組合物，該組合物包括：(1)以0.1%-10%重量的量存在的新橙皮苷；和(2)化妝品中可接受的媒介物。The present invention relates to a cosmetic skin care composition comprising: (1) neohesperidin present in an amount of from 0.1% to 10% by weight; and (2) a cosmetically acceptable vehicle.
在本發明的組合物中使用新橙皮苷是為了達到祛除眼部黑眼圈的效果。The use of neohesperidin in the compositions of the present invention is to achieve the effect of eliminating dark circles in the eye.
本發明的組合物和方法還包括化妝品中可接受的媒介物來作為組合物中活性成分的稀釋劑、分散劑或載體，從而當組合物用於皮膚時促進其分佈。The compositions and methods of the present invention also include a cosmetically acceptable vehicle as a diluent, dispersant or carrier for the active ingredient in the compositions to facilitate the distribution of the composition when it is applied to the skin.
水以外的媒介物包括液體或固體潤膚劑、表面活性劑、溶劑、增稠劑。Vehicles other than water include liquid or solid emollients, surfactants, solvents, thickeners.
各種類型的活性成分都可存在於本發明的化妝品組合物中。活性物質被定義為不同於潤膚劑和僅改善組合物的物理性能的成分的物質。Various types of active ingredients may be present in the cosmetic compositions of the present invention. An active substance is defined as a substance that is different from an emollient and an ingredient that only improves the physical properties of the composition.
在本發明的一個實施方案中，提供了一種具有如下配方的組合物：In one embodiment of the invention, a composition is provided having the following formulation:
按照本發明，通過局部應用新橙皮苷，可達到減少或消除眼部黑眼圈的作用。According to the present invention, the effect of reducing or eliminating dark circles of the eye can be achieved by topical application of neohesperidin.
本發明涉及新橙皮苷在化妝品方面的新用途，特別是新橙皮苷作為改善皮膚微循環的化學成分在祛除眼部黑眼圈方面的新用途。優選在該用途中，所述新橙皮苷以占組合物0.01%-10%重量的量存在。The invention relates to a new use of new hesperidin in cosmetics, in particular, the new use of neohesperidin as a chemical component for improving skin microcirculation in eliminating eye dark circles. Preferably, in this use, the neohesperidin is present in an amount from 0.01% to 10% by weight of the composition.
為了更好地利用新橙皮苷，本發明對新橙皮苷局部施用於皮膚表面的促微循環效果進行了研究，結果表明新橙皮苷局部外用後可明顯改善皮膚微循環，本發明人將其應用於眼部護理產品中，發現新橙皮苷具有明顯地祛除黑眼圈的作用。In order to make better use of the new hesperidin, the present invention has studied the effect of the local application of neohesperidin on the surface of the skin, and the results show that the topical application of the new hesperidin can significantly improve the skin microcirculation. Applying it to eye care products, it was found that neohesperidin has a significant effect of eliminating dark circles.
通過下面的實例可以對本發明進行進一步的描述，然而，本發明的範圍並不限於下述實例。本領域的專業人員能夠理解，在不背離本發明的精神和範圍的前提下，可以對本發明進行各種變化和修飾。The invention is further described by the following examples, however, the scope of the invention is not limited to the examples described below. A person skilled in the art will appreciate that various changes and modifications can be made to the invention without departing from the spirit and scope of the invention.
本發明對試驗中所使用到的材料以及試驗方法進行一般性和/或具體的描述。雖然為實現本發明目的所使用的許多材料和操作方法是本領域公知的，但是本發明仍然在此作盡可能詳細的描述。在本發明的上下文中，如果無其它特別的說明，%表示wt%，即重量百分數。The present invention provides a general and/or specific description of the materials and test methods used in the tests. While many of the materials and methods of operation used to accomplish the objectives of the present invention are well known in the art, the present invention is still described in detail herein. In the context of the present invention, % means wt%, ie weight percent, unless otherwise specified.
促微循環試驗方法：取體重為3.0-3.5 kg雄性日本大耳白兔，背部剃毛後，用記號筆在兔子無毛區劃定測試血流的10個點，左右側各5個點，畫點避開大血管；塗樣品前，用雷射多普勒血流儀測定各組實驗兔子10個點的血流基礎值，各組兔子背部左側塗抹空白溶液，右側塗抹含新橙皮苷(新橙皮苷購自西安小草植物科技有限責任公司，純度98% HPLC，批號：xc091215；除非特別說明，下同)的溶液[三組動物，藥液濃度分別為0.5%(w/v)、1%(w/v)、2%(w/v)，每隻動物用量0.1毫升]，每個濃度樣品平行3隻兔子。以類似方法口服2%(w/v)的藥液，用藥量為2%(w/v)藥液塗抹組的100倍。用藥後每經1小時用雷射多普勒血流儀測定相同部位的血流值，直至血流值不再發生變化為止，並計算血流變化指數[血流變化指數=(每個時間點測得的血流值/基礎血流值)×100%]，評價新橙皮苷對兔子背部血流的影響，血流變化指數越高表示促進微循環作用效果越好。表1是新橙皮苷溶液濃度為2%(w/v)的藥液作用於兔子背部皮膚的血流變化指數。Microcirculation test method: Take a male Japanese white rabbit with a body weight of 3.0-3.5 kg. After shaving the back, use a marker to delineate 10 points of blood flow in the rabbit hairless area, 5 points on each side and left. Points were avoided from the large blood vessels; before the samples were applied, the baseline values of blood flow at 10 points in each group of rabbits were measured by laser Doppler flowmetry. The left side of each group was coated with a blank solution on the left side and the right side was coated with new hesperidin (new Hesperidin was purchased from Xi'an Xiaocao Plant Technology Co., Ltd., purity 98% HPLC, batch number: xc091215; unless otherwise stated, the same solution) [three groups of animals, the concentration of the drug solution is 0.5% (w / v), 1% (w / v), 2% (w / v) , 0.1 ml per animal], 3 rabbits in parallel for each concentration sample. A 2% (w/v) solution was orally administered in a similar manner, and the dose was 100 times that of the 2% (w/v) solution. The blood flow value of the same site was measured by laser Doppler flowmeter every hour after administration until the blood flow value no longer changed, and the blood flow change index was calculated [blood flow change index = (each time point measurement) The obtained blood flow value / basal blood flow value) × 100%], evaluation of the effect of neohesperidin on the blood flow of the back of the rabbit, the higher the blood flow change index indicates that the effect of promoting microcirculation is better. Table 1 shows the blood flow change index of the drug solution having a concentration of 2% (w/v) of the new hesperidin solution on the back skin of the rabbit.
註：其中*表示樣品側與空白側相比，P＜0.05，**表示樣品側與空白側相比，P＜0.01。Note: where * indicates that the sample side is P<0.05 compared to the blank side, and ** indicates that the sample side is P<0.01 compared to the blank side.
實驗結果用SPSS11.5軟體進行統計分析，計量資料應用t檢驗評價試驗結果，P＜0.05即可被認為具有統計顯著性。在表2的結果中列出了測試中出現P＜0.05的全部時間點。The experimental results were statistically analyzed with SPSS11.5 software. The measurement results were evaluated by t test. P<0.05 was considered to be statistically significant. All time points at which P < 0.05 occurred in the test are listed in the results of Table 2.
註：表中“─”表示以2%藥液口服時未出現P＜0.05的時間點。Note: “─” in the table indicates that the time point of P<0.05 did not occur when taken orally with 2% of the drug solution.
試驗結果表明，兔子背部塗抹含不同濃度新橙皮苷的樣品後，與空白側相比，能顯著提高兔子皮膚微血管血流。The results showed that the rabbits with different concentrations of neohesperidin on the back of the rabbit significantly increased the microvascular blood flow in the rabbit skin compared with the blank side.
方法：本研究採用8週兩種配方兩側眼部對比使用試驗。METHODS: This study used a two-week test of contrast between the two sides of the two formulations.
在本研究中招募了中重度黑眼圈志願者50名，將其分為三組，保證每個成對比較組有效人數至少為15人。在受試者間隨機分配並左/右眼平衡使用，成對比較。其方法為眼部一側塗抹含新橙皮苷的組合物(即基礎配方+不同濃度的橙皮苷)，另一側塗抹不含新橙皮苷的組合物(即基礎配方)，持續8週。在0週(處理前)、2週、4週、6週和8週對其祛除黑眼圈效果進行功效評價。In this study, 50 moderate-to-severe dark-skinned volunteers were recruited and divided into three groups to ensure that the effective number of each paired comparison group was at least 15. Randomly assigned between subjects and left/right eye balanced use, pairwise comparison. The method comprises applying a composition containing neohesperidin on one side of the eye (ie, a base formula + different concentrations of hesperidin), and coating the other side without a new hesperidin (ie, a base formula) for 8 week. Efficacy evaluation was performed on the effect of removing dark circles at 0 weeks (before treatment), 2 weeks, 4 weeks, 6 weeks, and 8 weeks.
功效評價方法：試驗0天拍攝受試者的眼部圖像作為基準資料，試驗2、4、6和8週進行圖像拍攝。採用photoshop軟體Lab系統進行色度分析計算，以L值表示眼部肌膚白度，L值越高說明皮膚越白，與基準資料對比分析，SPSS統計結果用以評定產品功效，P＜0.05即可被認為具有統計顯著性。Efficacy evaluation method: The eye image of the subject was photographed for 0 days as a reference material, and image photographing was performed at 2, 4, 6 and 8 weeks. The photoshop software Lab system was used for colorimetric analysis. The L value was used to indicate the whiteness of the eye skin. The higher the L value, the whiter the skin. Compared with the baseline data, the SPSS statistical results were used to evaluate the efficacy of the product, P<0.05. It is considered to be statistically significant.
測試者使用表3中的基礎配方和表4中的組合物進行測試。The testers were tested using the base formulation in Table 3 and the compositions in Table 4.
進行以下成對比較：Make the following pairwise comparisons:
成對比較1：組合物1(基礎配方)對組合物2(基礎配方+0.5%新橙皮苷)；Pairwise comparison 1: Composition 1 (basic formula) versus composition 2 (basic formula + 0.5% neohesperidin);
成對比較2：組合物1(基礎配方)對組合物3(基礎配方+2%新橙皮苷)；Pairwise comparison 2: composition 1 (basic formula) versus composition 3 (basic formula + 2% neohesperidin);
成對比較3：組合物1(基礎配方)對組合物4(基礎配方+10%新橙皮苷提取物)。Pairwise comparison 3: Composition 1 (basic formula) versus composition 4 (basic formula + 10% neohesperidin extract).
獲得的結果列於表5A至5C：The results obtained are listed in Tables 5A to 5C:
** ：基礎配方+0.5%新橙皮苷在使用6週開始提供了比基礎配方更顯著的改善(P＜0.05)。 ** : Base Formula + 0.5% Neohesperidin provided a significant improvement over the base formulation at 6 weeks of use (P < 0.05).
#：無活性成分的基礎配方亦出現變化，扣除此變化有助於提供試驗的準確性。出現此基礎配方出現變化的原因可能包括但不限於：基礎配方本身的刺激作用、受冷熱刺激、情緒、以及拍攝環境明暗度等非客觀因素。這些因素均可能會導致L值發生變化，從而降低測試結果的客觀性，因此在實驗過程中需嚴格控制實驗條件。在實驗方法中設置左右眼自身對照，可以最大程度地消除或平衡實驗過程中無關變數的影響，因此實驗組與對照組兩者之差異，可認定為是來自實驗變數的效果。如在本實施例中，測試結果表明塗抹基礎配方一側的L值在不同測試時間內均有不同程度的增加，說明在該實驗條件下非客觀因素對L值有一定的影響，而塗抹添加新橙皮苷一側的L值增加的程度更高，與前者相比具有顯著性，並且說明該顯著性是新橙皮苷的效果所致，以下兩組成對比較與此類似。#: The base formula without active ingredients also changed. Deducting this change helps to provide the accuracy of the test. Reasons for this change in the base formula may include, but are not limited to, non-objective factors such as the stimulating effect of the base formula itself, the heat and cold stimulation, mood, and the brightness of the shooting environment. These factors may cause the L value to change, thereby reducing the objectivity of the test results, so the experimental conditions need to be strictly controlled during the experiment. Setting the left and right eye self-controls in the experimental method can eliminate or balance the influence of irrelevant variables during the experiment to the greatest extent. Therefore, the difference between the experimental group and the control group can be considered as the effect from the experimental variables. As in the present example, the test results show that the L value on the side of the smear-based formulation has different degrees of increase in different test times, indicating that non-objective factors have a certain influence on the L value under the experimental conditions, and the smear is added. The L value on the side of the new hesperidin increased to a greater extent, was significant compared to the former, and indicated that the significance was due to the effect of neohesperidin. The following two composition pairs were similar.
以上成對比較結果表明，組合物中添加了新橙皮苷後，與不添加新橙皮苷的組合物相比，具有顯著地改善黑眼圈的作用。該實施例說明新橙皮苷可用於改善皮膚微循環特別是可用作祛除黑眼圈的化妝品護膚產品。The above pairwise comparison results showed that the addition of neohesperidin to the composition significantly improved the dark circles compared to the composition without the addition of neohesperidin. This example illustrates that neohesperidin can be used to improve skin microcirculation, particularly as a cosmetic skin care product for removing dark circles.
以上實施例說明了本發明的局部用組合物可以以常規方式加工得到，它們適合於化妝護膚用途，特別適合用於祛除黑眼圈以改善眼部皮膚外觀和感覺。The above examples illustrate that the topical compositions of the present invention can be processed in a conventional manner, which are suitable for cosmetic skin care applications, and are particularly suitable for use in removing dark circles to improve the appearance and feel of the eye skin.
Claims (11)
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EP1113726B1 (en) * | 1998-09-15 | 2004-03-24 | Korea Research Institute of Bioscience and Biotechnology | Use of neohesperidin dihydrochalcone for the manufacture of a medicament for preventing or treating elevated blood lipid level-related diseases |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EP1113726B1 (en) * | 1998-09-15 | 2004-03-24 | Korea Research Institute of Bioscience and Biotechnology | Use of neohesperidin dihydrochalcone for the manufacture of a medicament for preventing or treating elevated blood lipid level-related diseases |
Non-Patent Citations (1)
| Title |
|---|
| 岳學狀等;"橙皮苷、beta-七葉皂苷、丹參酮等局部外用對甲皱皮膚微循環的影響";臨床皮膚科雜誌，2005年，第34卷第7期，第427~429頁。 * |
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