TW201842917A - Topical compositions designed to maintain and restore the water homeostasis of the skin - Google Patents
Topical compositions designed to maintain and restore the water homeostasis of the skin Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7024—Esters of saccharides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/716—Glucans
- A61K31/722—Chitin, chitosan
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
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- Cosmetics (AREA)
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Abstract
Description
本發明係關於包含N,O-羧甲基聚葡萄胺糖及蔗糖八硫酸酯鈉或鉀鹽作為活性成分之局部組成物。本發明之組成物適用於保持及恢復皮膚之水份恆定,且可用於皮膚醫學及美容學。 The present invention relates to a topical composition comprising N, O-carboxymethyl polyglucosamine and sodium or potassium sucrose octasulfate as active ingredients. The composition of the present invention is suitable for keeping and restoring the skin's moisture constant, and can be used in dermatology and aesthetics.
經皮水份散失(TEWL;transepidermal water loss)係一種由水份自皮膚之最深層連續擴散至最外層所組成的生理現象,其中水份蒸發;該生理過程確保水份恆定,其對保持皮膚的完整、健康及良好狀況係為關鍵。 Transepidermal water loss (TEWL) is a physiological phenomenon consisting of the continuous diffusion of water from the deepest layer of the skin to the outermost layer, in which the water evaporates; this physiological process ensures that the water is constant and its effect on maintaining the skin Integrity, health and well-being are key.
然而,各種化學、物理、環境及病理因素會改變皮膚的水份恆定且有時會嚴重影響其完整、健康及外觀。 However, various chemical, physical, environmental, and pathological factors can change the skin's moisture content and sometimes seriously affect its integrity, health, and appearance.
正確的水份恆定容許表現皮膚的生理功能,諸如障壁功能,其能抵抗源自皮膚最深層的水份過度蒸發。反之,當水份恆定不正確時,皮膚缺乏塑性及彈性,且無法有效地防止侵略性、致敏性、刺激性及毒性外來物質的穿透。經改變的皮膚水份恆定使個體容易感染許多病症,諸如由尿布或衣物摩擦、由體液沉滯或由發熱所引起的局部刺激性症狀、發紅、褥瘡、血管病症及皮膚過早老化。 Correct moisture constant allows the skin to perform physiological functions, such as the barrier function, which resists excessive evaporation of water from the deepest layers of the skin. Conversely, when the moisture is constant and incorrect, the skin lacks plasticity and elasticity, and cannot effectively prevent the penetration of aggressive, allergenic, irritating and toxic foreign substances. Constant skin moisture changes make an individual susceptible to a number of conditions, such as local irritating symptoms caused by friction in diapers or clothing, stagnation of body fluids, or fever, redness, bedsores, vascular disorders, and premature skin aging.
為恢復及保持皮膚的正確水份恆定,使用根據其功能 來分類的化合物,例如封阻性物質諸如油或聚矽氧;水合性及吸濕性物質;恢復障壁功能的脂質物質;及刺激深度水合的物質。 To restore and maintain the correct moisture of the skin, use compounds classified according to their function, such as blocking substances such as oil or polysiloxane; hydrating and hygroscopic substances; lipid substances that restore the function of the barrier wall; and depth of irritation Hydrated substance.
然而,該等物質可能具有副作用;例如,封阻性物質會阻止皮膚最外層中的水份生理蒸發(TEWL),導致表面細胞改變及皮膚微生物相失衡,從而具有細菌、真菌或病毒感染的風險。吸濕性物質會隨時間經過刺激皮膚;基本上具有脂質特性的障壁功能調節劑容易分解,從而導致形成刺激性及毒性物質,及深度水合刺激劑會干擾皮膚的生理組成。 However, these substances can have side effects; for example, blocking substances can prevent the physiological evaporation of water (TEWL) in the outermost layer of the skin, causing changes in the surface cells and imbalance of the microbial phase of the skin, thereby posing a risk of bacterial, fungal, or viral infections . Hygroscopic substances can irritate the skin over time; basically, the barrier function modifiers with lipid characteristics are easily broken down, which leads to the formation of irritating and toxic substances, and the deeply hydrated stimulants can interfere with the physiological composition of the skin.
現已驚人地發現N,O-羧甲基聚葡萄胺糖與呈水溶性鹽形式之蔗糖八硫酸酯的組合減緩但並未阻止TEWL,因此導致皮膚被源自TEWL之生理功能之水份(內生水)的顯著、持續水合提升。 It has now been surprisingly found that the combination of N, O-carboxymethyl polyglucosamine and sucrose octasulfate in the form of a water-soluble salt slows but does not prevent TEWL, thus causing the skin to be water-derived from the physiological functions of TEWL Endogenous water).
本發明之組合亦沒有迄今已知之皮膚水合化合物的副作用。 The combination of the invention is also free of the side effects of skin hydrating compounds known to date.
N,O-羧甲基聚葡萄胺糖(NOCMC)係一種已知化合物,其製備記述於US 4,619,995中。可容易地於市面獲得,例如以Chitoceuticals®之商標獲自Heppe Medical Chitosan GmbH。 N, O-carboxymethyl polyglucosamine (NOCMC) is a known compound and its preparation is described in US 4,619,995. It is readily available on the market, for example under the trademark Chitoceuticals® from Heppe Medical Chitosan GmbH.
NOCMC於牙齒口腔領域中因其水合及成膜性質、保護黏膜防止病原體、及緩衝口腔之生理pH而著稱。 NOCMC is well-known in the dental and oral field for its hydration and film-forming properties, protection of mucous membranes against pathogens, and buffering of the physiological pH of the oral cavity.
蔗糖八硫酸酯(SOS)鋁鹽/錯合物(稱為斯克拉非(sucralfate))長久以來在胃腸專科中被用來治療十二指腸及胃潰瘍及食道炎、用來維護性治療消化性潰瘍、及用來治療及預防化學療法引起的口炎。 Sucrose octasulfate (SOS) aluminum salt / complex (known as sucralfate) has long been used in the gastrointestinal specialty to treat duodenal and gastric ulcers and esophagitis, to maintain the treatment of peptic ulcer, and Used to treat and prevent stomatitis caused by chemotherapy.
當經由外部局部投與使用時,作為鋁鹽/錯合物的 SOS因其癒合傷口、抗發炎及保護性質而被用於皮膚及黏膜治療組成物中。 When used topically via external administration, SOS, which is an aluminum salt / complex, is used in skin and mucosal treatment compositions because of its wound healing, anti-inflammatory, and protective properties.
作為鋁鹽/錯合物的SOS不適用於本發明之用途,因其實際上不溶於水且不具有親水性質,此不同於其之呈現高度水溶性且無局部或全身毒性的鈉或鉀鹽。 SOS as an aluminum salt / complex is not suitable for use in the present invention because it is practically insoluble in water and has no hydrophilic properties, unlike sodium or potassium salts which exhibit high water solubility and no local or systemic toxicity .
鈉鹽可容易地以固體形式或水溶液於市面獲得。Euticals S.p.A.(Lodi,Italy)銷售20% w/w水溶液。 Sodium salts are readily available commercially in solid form or in aqueous solution. Euticals S.p.A. (Lodi, Italy) sells a 20% w / w aqueous solution.
現已發現N,O-羧甲基聚葡萄胺糖與蔗糖八硫酸酯鈉或鉀鹽之組合具有與對親水性之增效作用相關的有利性質,其容許有效地吸收並滯留水份,減緩但並不阻止經皮水份散失。 It has been found that the combination of N, O-carboxymethyl polyglucosamine and sodium or potassium sucrose octasulfate has advantageous properties related to a synergistic effect on hydrophilicity, which allows effective absorption and retention of water, slowing down It does not prevent transdermal water loss.
因此,本發明之目的係經設計來施用至皮膚及黏膜的局部組成物,其包含N,O-羧甲基聚葡萄胺糖及蔗糖八硫酸酯鈉或鉀鹽作為活性成分,與適用於美容及/或皮膚醫學使用的適當賦形劑及/或載劑混合。 Therefore, the object of the present invention is a topical composition designed to be applied to the skin and mucous membranes, which contains N, O-carboxymethyl polyglucosamine and sodium or potassium sucrose octasulfate as active ingredients, and is suitable for beauty And / or a mixture of appropriate excipients and / or carriers used in dermatology.
本發明之組成物尤其適用於兒科及老年病學領域。 The composition of the present invention is particularly suitable for the fields of pediatrics and geriatrics.
N,O-羧甲基聚葡萄胺糖係以範圍介於0.005重量%與8重量%之間、較佳介於0.009%與5% w/w之間、及更佳介於0.010%與3%之間的百分比存在於本發明之組成物中。 N, O-carboxymethyl polyglucosamine is in a range between 0.005 wt% and 8 wt%, preferably between 0.009% and 5% w / w, and more preferably between 0.010% and 3%. The percentage is present in the composition of the present invention.
蔗糖八硫酸酯鈉或鉀鹽係以範圍介於0.010重量%與5.0重量%之間、較佳介於0.050%與3.0%之間、及更佳介於0.100%與1.0%之間的百分比存在於本發明之組成物中。 Sucrose octasulfate sodium or potassium salts are present in the range of 0.010% and 5.0% by weight, preferably between 0.050% and 3.0%, and more preferably between 0.100% and 1.0%. In the composition of the invention.
本發明之組成物可包含其他常用於皮膚醫學及美容學中之活性成分,且可藉由諸如於Remington之The Science and Practice of Pharmacy,20th Edition中所述之習知方法,使用例如於Handbook of Pharmaceutical Excipients,6th Edition,Pharmaceutical Press中所述之適宜賦形劑或載劑來製備。 The composition of the present invention may contain other active ingredients commonly used in dermatology and aesthetics, and may be used in conventional methods such as described in The Science and Practice of Pharmacy, 20th Edition of Remington, for example, in the Handbook of Suitable excipients or carriers as described in Pharmaceutical Excipients, 6th Edition, Pharmaceutical Press.
較佳調配物之實例係洗劑、凝膠、水包油(o/w)或油包水(w/o)乳液、乳霜、軟膏、噴劑及泡沫體。含有水作為載劑之組成物為特佳。 Examples of preferred formulations are lotions, gels, oil-in-water (o / w) or water-in-oil (w / o) emulsions, creams, ointments, sprays and foams. Compositions containing water as a carrier are particularly preferred.
以下所給實施例進一步例示本發明。 The examples given below further illustrate the invention.
百分比係以組成物之總體積的重量份數表示。 Percentages are expressed as parts by weight of the total volume of the composition.
Claims (9)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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IT102017000047632A IT201700047632A1 (en) | 2017-05-03 | 2017-05-03 | TOPIC COMPOSITIONS TO MAINTAIN AND RESTORE THE HYDRO-MOISTIC SKIN HOMEOSTASIS |
??102017000047632 | 2017-05-03 |
Publications (1)
Publication Number | Publication Date |
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TW201842917A true TW201842917A (en) | 2018-12-16 |
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Application Number | Title | Priority Date | Filing Date |
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TW107114898A TW201842917A (en) | 2017-05-03 | 2018-05-02 | Topical compositions designed to maintain and restore the water homeostasis of the skin |
Country Status (4)
Country | Link |
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AR (1) | AR111666A1 (en) |
IT (1) | IT201700047632A1 (en) |
TW (1) | TW201842917A (en) |
WO (1) | WO2018202456A1 (en) |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4619995A (en) | 1984-12-24 | 1986-10-28 | Nova Chem Limited | N,O-carboxymethyl chitosan and preparative method therefor |
DK505488D0 (en) * | 1987-12-21 | 1988-09-09 | Bar Shalom Daniel | MEDIUM AND USE OF SAME |
AU4941297A (en) * | 1996-11-15 | 1998-06-10 | Dumex-Alpharma A/S | A method for promoting tissue repair |
EP2737902A1 (en) * | 2012-11-28 | 2014-06-04 | Zarzatech, Inc. | Compositions comprising cimetidine and n,o-carboxymethyl chitosan for the prevention and therapy of pathologies of the skin and the mucous membranes and in the odontostomatological field |
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2017
- 2017-05-03 IT IT102017000047632A patent/IT201700047632A1/en unknown
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2018
- 2018-04-23 WO PCT/EP2018/060310 patent/WO2018202456A1/en active Application Filing
- 2018-05-02 TW TW107114898A patent/TW201842917A/en unknown
- 2018-05-02 AR ARP180101141A patent/AR111666A1/en unknown
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Publication number | Publication date |
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WO2018202456A1 (en) | 2018-11-08 |
IT201700047632A1 (en) | 2018-11-03 |
AR111666A1 (en) | 2019-08-07 |
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