WO2017104759A1 - Produit cosmétique lyophilisé du type comprimé - Google Patents

Produit cosmétique lyophilisé du type comprimé Download PDF

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Publication number
WO2017104759A1
WO2017104759A1 PCT/JP2016/087423 JP2016087423W WO2017104759A1 WO 2017104759 A1 WO2017104759 A1 WO 2017104759A1 JP 2016087423 W JP2016087423 W JP 2016087423W WO 2017104759 A1 WO2017104759 A1 WO 2017104759A1
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WO
WIPO (PCT)
Prior art keywords
tablet
mass
cosmetic
dried
type freeze
Prior art date
Application number
PCT/JP2016/087423
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English (en)
Japanese (ja)
Inventor
雅之 菊田
Original Assignee
株式会社 資生堂
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 株式会社 資生堂 filed Critical 株式会社 資生堂
Publication of WO2017104759A1 publication Critical patent/WO2017104759A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin

Definitions

  • the present invention relates to tablet-type freeze-dried cosmetics, and more particularly to the improvement of handling ease as a tablet.
  • Patent Document 1 discloses L-ascorbic acid-2-phosphate, which is unstable in the presence of water, sugar alcohol, oligosaccharide having low hygroscopicity, and a technique relating to dry formulation of a liquid composition. It is described that an aqueous solution mixed with a water-soluble polymer can be kept stable until use by lyophilization.
  • Patent Document 2 discloses that a freeze-dried cosmetic obtained by freeze-drying an aqueous solution containing sodium hyaluronate, collagen, and an ascorbic acid derivative shrinks or cracks due to moisture absorption, bacteria and oxidation even after long-term storage. It is described that it dissolves in a very short time when it is redissolved with water or lotion during use.
  • Patent Document 3 describes that a hyaluronic acid solid composition stable at room temperature was obtained by freeze-drying an aqueous solution containing sodium hyaluronate and a saccharide.
  • Patent Document 4 a powder or granular cosmetic using a freeze-dried product of an aqueous solution containing hyaluronic acid or sodium hyaluronate and phosphoric acid-L-ascorbyl magnesium exhibits the solubility of both components in water. It is described to improve.
  • the freeze-dried compositions taught in Patent Documents 1 to 4 are not sufficient in terms of peelability from a container or the like, re-solubility, and feeling of use of the re-dissolved liquid as a molded tablet-shaped freeze-dried product. It has been difficult to produce tablet-type cosmetics that are highly portable and can be used easily. In particular, a technique relating to a tablet that has a low hygroscopicity during storage but dissolves instantly when water is added is not yet known. This invention is made
  • the inventors of the present invention comprising a polyethylene glycol of specific molecular weight and trehalose, and a composition formed into a tablet shape by freeze-drying so as to have a specific bulk specific gravity
  • the present invention was completed by finding that it dissolves instantly by addition of water despite its low hygroscopicity, has high releasability, and is easy to handle.
  • the tablet-type freeze-dried cosmetic according to the present invention is (A) 10-20% by mass of trehalose, (B) 0.5 to 3.0% by mass of polyethylene glycol having a number average molecular weight of 2500 to 20000, And having a bulk specific gravity of 0.1 to 0.5 g / ml.
  • (B) preferably contains polyethylene glycol having a number average molecular weight of 15000 to 20000.
  • the cosmetic preferably comprises (C) hyaluronic acid and (D) a thickener. In the cosmetic, it is preferable that the blending amount of (C) hyaluronic acid is 0.01 to 1% by mass.
  • the blending amount of (D) thickener is 0.01 to 0.5% by mass.
  • the thickener is preferably selected from xanthan gum, tamarind gum, sodium alginate, gellan gum, agar, polyvinyl alcohol, carboxyvinyl polymer, and quince seed.
  • the tablet-type freeze-dried cosmetics applied to the skin etc. which can be melt
  • the tablet-type freeze-dried cosmetic according to the present invention contains trehalose and polyethylene glycol having a specific number average molecular weight, and is basically produced by volatilizing a medium from a uniform solution / dispersion solution of the components. It is. First, the components of the present invention will be described.
  • Ingredients blended as an excipient in the present invention are (A) trehalose and (B) polyethylene glycol.
  • Trehalose used in the present invention is a disaccharide in which two D-glucoses are linked, and the binding mode is ⁇ , ⁇ -, ⁇ , ⁇ -, ⁇ , ⁇ - There are three types, and ⁇ , ⁇ -binding modes that are found in large numbers in nature are common.
  • Trehalose a type of sugar, has strong water retention, and is superior in terms of stability, resolubility and releasability as a freeze-dried cosmetic compared to sugars such as erythritol, xylitol, and sorbitol. Yes.
  • the amount of trehalose is preferably 10 to 20% by mass. Further, the content of 15 to 20% by mass is more preferable from the viewpoint of excellent high temperature stability. If it is less than 10% by mass, it is not preferable in that the stability at high temperatures and the solubility in water during re-dissolution may be insufficient. On the other hand, if it exceeds 20% by mass, the high temperature resistance is excellent, it is difficult to freeze, there is a case where bumping may occur, and it is not preferable from the viewpoint of usability.
  • trehalose for cosmetics
  • Hayashibara Co., Ltd. examples of commercially available trehalose
  • trehalose In addition to trehalose, other saccharides can be added as long as the effects of the present invention are not lost.
  • maltose, maltotetraose, maltosyl trehalose and the like can be mentioned.
  • Polyethylene glycol used in the present invention includes those having a number average molecular weight of 2500 to 20000 from the viewpoint of tablet formability. More preferably, it is preferably 15000 to 20000 in terms of moldability and releasability. When the number average molecular weight is less than 2500, it is not preferable in that the releasability may be deteriorated. Moreover, when the number average molecular weight is larger than 20000, it is not preferable in that re-solubility is poor and feeling in use may be inferior.
  • the blending amount of (B) polyethylene glycol is preferably 0.5 to 5% by mass, more preferably 0.5 to 3%, and further preferably 1 to 2% by mass with respect to the pre-lyophilization solution of the present invention. is there. When it mixes exceeding 5 mass%, the mold release property and usability of a tablet may fall.
  • the said polyethylene glycol may use what was synthesize
  • commercially available polyethylene glycol include PEG-20000 (manufactured by Sanyo Chemical Industries, Ltd.).
  • Hyaluronic acid used in the present invention is a linear polymer in which N-acetyl-D-glucosamine residues and D-glucuronic acid residues are alternately bonded. What was processed into the powder form etc. can be used.
  • the hyaluronic acid can be obtained by, for example, isolation and extraction from a chicken crown or other animal tissues, or a fermentation method using a microorganism such as Streptococcus.
  • a hyaluronic acid metal salt such as hyaluronic acid sodium salt and hyaluronic acid potassium salt
  • a hydroxyl group and a carboxyl group of hyaluronic acid are etherified, esterified and amidated.
  • powders such as hyaluronic acid derivatives obtained by acetylation, acetalization, and ketalization may be used.
  • hyaluronic acid examples include hyaluronic acid HA-LQ (manufactured by Kewpie Fine Chemical), hyaluronic acid FCH (manufactured by Kikkoman Biochemifa Co., Ltd.), and the like.
  • the molecular weight of (C) hyaluronic acid is not particularly limited, but it is preferable that the molecular weight is 100,000 or more, and the molecular weight is about 500,000 to 3,000,000.
  • the molecular weight is 100,000 or more, and the molecular weight is about 500,000 to 3,000,000.
  • the molecular weight is larger than 3 million, it is not preferable in that the solubility and the feeling of use after re-dissolution may be insufficient.
  • (C) hyaluronic acid in particular, exhibits extremely high viscosity even in the state of a low concentration aqueous solution, so its blending amount is related to the properties of the lyophilized tablet and its redissolved solution. Is expensive.
  • the blending amount of (C) hyaluronic acid is preferably 0.01 to 1% by mass, more preferably 0.05 to 0.2% by mass with respect to the pre-lyophilized solution of the present invention. If it exceeds 1% by mass, the solubility and releasability of the tablet will decrease, which is not preferable.
  • the (D) thickener used for this invention is used in order to improve the moldability and mold release property of tablet cosmetics.
  • a thickener water-soluble polymers such as xanthan gum, tamarind gum, sodium alginate, gellan gum, agar, polyvinyl alcohol, carboxyvinyl polymer, and quince seed can be used. Among these, it is preferable to use xanthan gum, tamarind gum, and quince seed in terms of using a tablet cosmetic and having less stickiness when dry, and less stickiness.
  • the blending amount of the thickener is preferably 0.01 to 0.5% by mass, more preferably 0.05 to 0.1% by mass, based on the pre-lyophilized solution of the present invention. If it exceeds 0.5% by mass, the releasability and usability of the tablet may decrease, and if the amount is less than 0.01% by mass, the moldability and releasability may decrease. is there.
  • thickeners examples include xanthan gum (Celtrol, manufactured by Kelco), tamarind gum (Glyloid 6C, manufactured by Dainippon Pharmaceutical Co., Ltd.), sodium alginate (Duck Algin NSPH, Kikkoman Biochemifa Corporation). ), Gellan gum (Kelcogel, DSP Gokyo Food & Chemical Co., Ltd.), agar (Inagar CS-110, Ina Food Industry Co., Ltd.), and the like.
  • the tablet-type freeze-dried cosmetic composition according to the present invention may contain other components that can be added to normal cosmetics and quasi-drugs as long as the effects of the present invention are not impaired.
  • an aqueous component is particularly preferable as the other component, but an oily component can be blended by solubilization using a surfactant or the like.
  • the aqueous component include polyhydric alcohols, water-soluble polymers other than the component (D), chelating agents, pH adjusters, preservatives, and the like.
  • polyhydric alcohol examples include ethylene glycol, propylene glycol, 1,3-butylene glycol, glycerol, polyethylene glycol having a molecular weight other than those described above, polyglycerol, and the like.
  • water-soluble polymers include those other than those described above, for example, hydrophilic synthetic polymers such as polyacrylic acid, polyethylene glycol, polyacrylamide, polyalkylacrylamide / polyacrylamide copolymer, carboxymethylcellulose, cationized cellulose, pluronic, macrogol.
  • hydrophilic synthetic polymers such as polyacrylic acid, polyethylene glycol, polyacrylamide, polyalkylacrylamide / polyacrylamide copolymer, carboxymethylcellulose, cationized cellulose, pluronic, macrogol.
  • hydrophilic natural polymers such as succinoglycan, guar gum, locust bean gum, curdlan, alginic acid, carrageenan, mannan, pectin, gum arabic, karaya gum, casein, ⁇ -cyclodextrin, Dextrin, dextran, gelatin, collagen, pectin, starch, chitin and its derivatives, chitosan and its derivatives, elastin, heparin, heparan Acid, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose; as a hydrophilic clay mineral, laponite, bentonite, smectite, and the like.
  • Examples of the chelating agent include 1-hydroxyethane-1,1-diphosphonic acid, 1-hydroxyethane-1,1-diphosphonic acid tetrasodium salt, disodium edetate, trisodium edetate, tetrasodium edetate, Examples include sodium acid, sodium polyphosphate, sodium metaphosphate, gluconic acid, phosphoric acid, citric acid, ascorbic acid, succinic acid, edetic acid, and trisodium ethylenediaminehydroxyethyl triacetate.
  • pH adjuster examples include buffers such as lactic acid-sodium lactate, citric acid-sodium citrate, and succinic acid-sodium succinate.
  • preservative examples include paraoxybenzoic acid ester and phenoxyethanol.
  • oil component examples include fragrances and oil-based drugs (for example, vitamin A).
  • humectants eg, 2-methacryloyloxyethyl phosphorylcholine (MPC) copolymer, PEG / PPG dimethyl ether such as PEG / PPG-14 / 7 dimethyl ether
  • water-soluble collagen e.g, hydrogen peroxide treatment Yeast hydrolysate, sodium dl-prolidonecarboxylate, L-hydroxyproline, calcium chloride, magnesium chloride
  • various extracts eg, rose, apricot, auren, sicon, peonies, assembly, birch, sage, loquat, carrot , Aloe, mallow, iris, grape, yokuinin, loofah, lily, saffron, senkyo, ginger, hypericum, onionis, garlic, capsicum, chimpi, cypress, seaweed, etc.
  • other water-soluble drugs eg, tranexamic acid
  • the tablet-type cosmetics according to the present invention can be obtained as a dry product that remains after dissolving or dispersing the above-described blended components in a volatile liquid medium such as water or lower alcohol, and sublimating by freezing after freezing.
  • a volatile liquid medium such as water or lower alcohol
  • the excipient component dissolved in a medium forms a three-dimensional network structure in the medium. If only the medium is removed from such a state, the network structure shrinks due to drying, and is distorted or collapsed. Therefore, it is usually difficult to maintain the structure.
  • trehalose blended with the excipient supports the network structure instead of the medium even after volatilization of the medium, so that it is considered that the structure by the excipient is almost maintained.
  • the dried product in which the three-dimensional network structure of the excipient is maintained is in a porous state in which the medium portion has been removed from the structure.
  • water is added during re-dissolution, water is introduced into the network structure from each hole. Penetration and dissolution of the entire tablet formulation proceeds. At that time, the higher the density of the constituents including the structure, the more difficult the water penetrates into the interior, and the formulation becomes less soluble. On the other hand, if the density of the constituent components is too low, the preparation itself is fragile and easily collapses, and it is easy to absorb moisture during storage.
  • the bulk density of the constituents is further set within a certain range.
  • the tablet cosmetic according to the present invention contains the above-described constituents and has a bulk specific gravity of 0.1 to 0.5 g / ml, preferably 0.15 to 0.3 g / ml. Cost. If the bulk specific gravity is less than 0.1 g / ml, the hygroscopicity during storage increases, and if it exceeds 0.5 g / ml, the solubility in water tends to decrease. On the other hand, if the bulk specific gravity is within the above range, the number of holes through which the medium has escaped is moderately large, and the network structure of the thickener is also fixed in a moderately widened state. In this case, the solubility is extremely good.
  • the tablet weight after freeze-drying (g) ⁇ freeze-drying type volume (ml) is calculated.
  • the tablet-type cosmetic according to the present invention is, for example, filled in a tablet mold with a solution in which constituent components are dissolved or dispersed in a volatile liquid medium such as water or lower alcohol, and then freeze-dried. It can manufacture by taking out from.
  • the present invention can be molded into any size and shape by setting the volume of the preparation, the components and the amount of the medium so as to satisfy the above-mentioned bulk specific gravity.
  • an extremely thin shape or an excessively complicated shape is not preferable because there is a problem in moldability.
  • the present invention has a low hygroscopic property of the preparation, and has a high releasability and is easily peeled from the container. Therefore, the present invention is not limited to a form (for example, blister pack) packaged for each used portion while being filled in the container. Only the preparation removed from the mold) can be packaged in any form.
  • the tablet-type cosmetics according to the present invention can usually be used by adding an appropriate amount of water to redissolve the preparation and applying the solution to the skin or the like.
  • the amount of water to be added should be adjusted so that the viscosity is easy to apply, with the lower limit of the complete dissolution of the preparation, but if it is too much, the component concentration is too low to obtain a sufficient effect. Yes, if it is too little, it may become sticky at the time of application. Therefore, although not particularly limited, it is preferable to adjust the addition amount to about 1 to 10 times the volume of the preparation.
  • the place where water is added to the preparation may be on the palm, on the application site, or in a suitable container.
  • the preparation for one-time use is placed on the palm. After adding water, it is preferable to apply the solution on the palm as it is to the application site by hand. Note that lotion or the like may be used instead of water as long as the formulation can be redissolved.
  • the tablet-type cosmetic according to the present invention may be in any product form, such as lotion, cosmetic liquid, pack, cleansing, facial cleansing foam, hand cream, shampoo, rinse, hair treatment, sunscreen, etc., depending on the ingredients to be blended.
  • it is suitable for use as a moisturizing lotion or cosmetic liquid.
  • ⁇ Moldability> The moldability after the drying step in the production method of each test example composition was evaluated according to the following criteria.
  • test example compositions of the formulations described in the following tables were prepared according to the following production methods.
  • a volatile liquid medium such as water or lower alcohol
  • poured into a mold sublimed by freezing after freezing, and a tablet-type freeze-dried cosmetic was obtained as a dry product remaining later.
  • the present inventor further examined the usability as a tablet cosmetic.
  • the polyethylene glycol (B) preferably has a number average molecular weight of 4,000 to 20,000 in terms of moldability and usability.
  • Test Examples 7-1 to 7-6 were tablet cosmetics excellent in re-dissolvability and usability, and excellent in high-temperature stability.
  • the formulation example of the tablet-type freeze-dried cosmetic (detergent) of the present invention is as follows.
  • the formulation example of the tablet-type freeze-dried cosmetic (hair treatment) of the present invention is as follows.
  • the formulation example of the tablet-type freeze-dried cosmetic (shampoo) of the present invention is as follows.
  • Formulation examples 4 to 7 of the tablet-type freeze-dried cosmetic (cosmetic for skin application) of the present invention are as follows.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention porte sur un produit cosmétique du type comprimé présentant une excellente caractéristique de maniabilité. Le produit cosmétique du type comprimé selon la présente invention contient (A) de 10 à 20 % en masse de tréhalose et (B) de 0,5 à 3,0 % en masse de polyéthylène glycol ayant une masse moléculaire comprise entre 2500 et 20 000, et a une densité apparente relative comprise entre 0,1 et 0,5 g/ml.
PCT/JP2016/087423 2015-12-16 2016-12-15 Produit cosmétique lyophilisé du type comprimé WO2017104759A1 (fr)

Applications Claiming Priority (2)

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JP2015-245470 2015-12-16
JP2015245470 2015-12-16

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WO2017104759A1 true WO2017104759A1 (fr) 2017-06-22

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Publication number Priority date Publication date Assignee Title
KR102641043B1 (ko) * 2017-01-06 2024-02-26 가부시키가이샤 미르본 모발용 조성물, 및 모발 처리 방법
JP2022126833A (ja) * 2017-01-06 2022-08-30 株式会社ミルボン 毛髪用組成物、及び毛髪処理方法
JP6404405B1 (ja) * 2017-06-14 2018-10-10 株式会社 資生堂 タブレット型凍結乾燥化粧料
KR20200016878A (ko) * 2017-06-19 2020-02-17 가부시키가이샤 시세이도 타블렛형 동결 건조 화장료
EP4201392A1 (fr) 2021-12-21 2023-06-28 Universitat Internacional De Catalunya, Fundació Privada Produit de soins personnels solide et procédé pour obtenir un tel produit

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JPS61180800A (ja) * 1985-02-06 1986-08-13 Kanebo Ltd 粉末状絹フイブロインペプチド及びその製造法
JPH0368507A (ja) * 1989-08-07 1991-03-25 Shiseido Co Ltd 固型化粧料組成物
JPH08507064A (ja) * 1993-02-23 1996-07-30 ジェネンテク・インコーポレイテッド 有機溶媒を用いて処理したポリペプチドの賦形剤安定化
JPH08245418A (ja) * 1995-03-09 1996-09-24 Behringwerke Ag 安定なトランスグルタミナーゼ製剤およびそれらを製造する方法
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JP2006182750A (ja) * 2004-12-27 2006-07-13 Bio Meito:Kk 凍結乾燥化粧品およびその製造方法
JP2015061871A (ja) * 2009-09-03 2015-04-02 株式会社林原 ２−Ｏ−α−Ｄ−グルコシル−Ｌ−アスコルビン酸無水結晶含有粉末とその製造方法並びに用途
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