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Ep001153602b1* (19) *EP001153602B1* (11) EP 1 153 602 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61Q 1/02 (2006.01) A61K 8/37 (2006.01) 05.11.2008 Bulletin 2008/45 A61Q 19/00 (2006.01) A61Q 19/02 (2006.01) A61K 8/34 (2006.01) A61K 8/39 (2006.01) (21) Application number: 00981822.0 (86) International application number: (22) Date of filing: 19.12.2000 PCT/JP2000/008982 (87) International publication number: WO 2001/045665 (28.06.2001 Gazette 2001/26) (54) SKIN PREPARATIONS FOR EXTERNAL USE COMPRISING DIETHOXYETHYL SUCCINATE ZUBEREITUNGEN ZUR ÄUSSEREN ANWENDUNG AUF DER HAUT ENTHALTEND DIETHOXYETHYLSUCCINAT PREPARATIONS CUTANEES A USAGE EXTERNE COMPRENANT DU DIETHOXYETHYL SUCCINATE (84) Designated Contracting States: (74) Representative: Merkle, Gebhard DE FR GB IT TER MEER STEINMEISTER & PARTNER GbR, Patentanwälte, (30) Priority: 20.12.1999 JP 36081899 Mauerkircherstrasse 45 26.01.2000 JP 2000017423 81679 München (DE) 07.08.2000 JP 2000238126 (56) References cited: (43) Date of publication of application: EP-A- 0 561 305 EP-A- 0 591 546 14.11.2001 Bulletin 2001/46 EP-A- 0 904 772 EP-A- 1 129 686 WO-A-95/00107 JP-A- 2 045 408 (73) Proprietor: SHISEIDO COMPANY LIMITED JP-A- 55 017 310 JP-A- 61 207 316 Tokyo 104-8010 (JP) JP-A- 61 289 023 US-A- 5 238 678 US-A- 5 993 793 (72) Inventors: • OHMORI, Takashi, • DATABASECA[Online]CHEMICALABSTRACTS Shiseido Res Cent (Shin-Yokohama) SERVICE, COLUMBUS, OHIO, US; KUNISHIGE, Yokohama-shi, TSUTOMU ET AL: "Pharmaceuticals for external Kanagawa 224-8558 (JP) use" retrieved from STN Database accession no. • MIYAHARA, Reiji, 93:101481 XP002218837 & JP 55 017310 A Shiseido Res Cent (Shin-Yokohama) (SHIONO KORYO KAISHA, LTD., JAPAN) 6 Yokohama-shi, February 1980 (1980-02-06) Kanagawa 224-8558 (JP) • DATABASECA[Online]CHEMICALABSTRACTS • KAKOKI, Hiroyuki, SERVICE, COLUMBUS, OHIO, US; FUJITA, Shiseido Res Cnt (Shin-Yokohama) YOSHIHIKO ET AL: "Forensic chemical study on Yokohama-shi, human hair. II. Identification of brand of women’s Kanagawa 224-8558 (JP) hair care products by remaining components on • NAMBA, Tomiyuki, human hair" retrieved from STN Database Shiseido Res Cent (Shin-Yokohama) accession no. 110:226718 XP002218838 & EISEI Yokohama-shi, KAGAKU (1989), 35(1), 37-48 , Kanagawa 224-8558 (JP) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 1 153 602 B1 Printed by Jouve, 75001 PARIS (FR) (Cont. next page) EP 1 153 602 B1 • GOTTSCHALCK, MCEWEN: "International Remarks: Cosmetic Ingredient Dictionary and Handbook, Thefilecontainstechnicalinformationsubmittedafter 10th ed." 2004, THE COSMETIC, TOILETRY AND the application was filed and not included in this FRAGRANCE ASSOCIATION, WASHINGTON, specification D.C. ISBN 1-882621-34-4, Vol. 3 * page 2229 * * page 2244 - page 2246 * 2 EP 1 153 602 B1 Description TECHNICAL FIELD 5 [0001] The present invention relates to an endermic liniment comprising diethoxy ethyl succinate and a humectant. BACKGROUND ART Invention defined in claim 1 10 [0002] Retention of moisture is essential for maintaining healthy skin, and many endermic liniments designed for moisture retention have been developed. As far as the sensation at the time of application of an endermic liniment is concerned, smoothness without a sticky sensation is desired. [0003] Research with regard to humectants is carried out intensively; humectants such as organic salts, polyhydric 15 alcohols, and water-soluble polymers are blended in an endermic liniment today. [0004] However, the blend ratio of these humectants must be increased in order to increase the moisture retaining effect, and as a result there are the following problems to be solved: the system becomes unstable, usability becomes poor, and, when applied to skin, it is repelled by sebum, or fitness for skin becomes poor. [0005] The inventors conducted earnest research in view of the aforementioned problems and discovered that an 20 endermic liniment that is superior in terms of the tactile sensation during use, smoothness in particular, without a sticky sensation, and having a lasting moisture retaining effect, can be obtained when diethoxy ethyl succinate and a humectant are blended in an endermic liniment, thus completing the present invention. [0006] The object of the present invention is to provide an endermic liniment comprising a polyoxyethylene dicarbo- xylate which promotes the effect of the ingredients, and in particular to provide an endermic liniment comprising a 25 humectant in combination with the polyoxyethylene dicarboxylate. DISCLOSURE OF INVENTION Invention defined in claim 1 30 [0007] That is, the present invention provides an endermic liniment as defined in claim 1. [0008] Also, the present invention provides said endermic liniment wherein said endermic liniment is a whitening endermic liniment. 35 BEST MODE FOR CARRYING OUT THE INVENTION [0009] The configuration of the present invention is described in detail below. Invention defined in claims 1-3 40 [0010] Polyoxyethylene dicarboxylates of the chemical formula (1) are known substances. [0011] Chemical formula (1): 45 50 (In this formula, R1 and R2 are hydrogen or alkyl or branched alkyl groups having 1-4 carbon atoms, and m, n, X, and Y are integers 0-5 which are not all zero at the same time. R3 is a branched or linear chain alkylene group having 0-10 carbon atoms.) 55 [0012] In chemical 1 formula (1), R1 and R2 denote alkyl or branched alkyl groups with a carbon number of 1-4; when the carbon number exceeds 5, hydrophilicity is reduced and the stability of the system becomes poor as they are blended in an endermic liniment (lotion in particular), m, n, X, and Y denote an integer of 0-5. Preferably they should be integers 1-2. If the total of m, n, X, and Y is zero, then hydrophilicity is reduced and the stability of the system becomes poor as 3 EP 1 153 602 B1 they are blended in an endermic liniment (lotion in particular). If it is more than 15, then the tactile sensation during use, smoothness in particular, becomes insufficient. R3 denote an alkyl or branched alkyl group with a carbon number of 0-10; when the carbon number exceeds 10, hydrophilicity is reduced and the stability of the system becomes poor as it is blended in an endermic liniment (lotion in particular). 5 [0013] Of polyoxyethylene dicarboxylates (1), diethoxyethyl succinate is used according to the invention due to its tactile sensation during use. An endermic liniment with particularly superior smoothness and without a sticky sensation which has a lasting moisture effect can be obtained. [0014] The blend ratio of the diethoxyethyl succinate is not limited in particular, but preferably 0.001-20.0 wt%, more preferably 0.1-10.0 wt% based upon the total amount of the endermic liniment. If it is less than 0.001 wt%, then the 10 effect of the blending is not manifested. If it is over 20. 0 wt%, then a sti.cky sensation will arise after use. [0015] The humectant used in the present invention is selected from polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, xylitol, sorbitol, maltitol, hyaluronic acid, or diglycerin (EO)PO adduct. [0016] The blend ratio of the humectant is not limited in particular; it is preferably 0.001-20.0 wt%, more preferably 0.1-10.0 wt%, based upon the total amount of the endermic liniment. 15 Common description [0017] The endermic liniment of the present invention is prepared by blending the aforementioned essential ingredients in an existing endermic liniment base. In addition to the aforementioned essential ingredients, other ingredients used in 20 endermic liniments such as cosmetics and drugs can be blended as necessary in the endermic liniment of the present invention; examples of such ingredients include powder ingredients, liquid fats and oils, solid fats and oils, waxes, hydrocarbons, higher fatty acids, higher alcohols, esters, silicones, anionic surfactants, cationic surfactants, ampholytic surfactants, nonionic surfactants, humectants, water-soluble polymers, thickeners, coating agents, ultraviolet light ab- sorbents, sequestering agents, lower alcohols, polyhydric alcohols, sugars, amino acids, organic amines, polymer emul- 25 sions, pH adjusting agents, skin nutrients, vitamins, antioxidants, antioxidation assistants, perfumes, and water; and the endermic liniment can be prepared for the target formulation with a conventional method. Specific ingredients which can be blended in are listed below. The endermic liniment of the present invention can be prepared by blending the afore- mentioned essential ingredients and any one, two or more of the following ingredients. [0018] Examples of the powder ingredients include inorganic powders (for example, talc, kaolin, mica, sericite, mus- 30 covite, phlogopite, synthetic mica, lepidolite, biotite, vermiculite, magnesium carbonate, calcium carbonate, aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, tungstic acid metal salt, magnesium, silica, zeolite, barium sulfate, firing calcium sulfate (calcined gypsum), calcium phosphate, fluorine-apatite, hydroxy apatite, ceramic powder, metallic soaps (for example, myristic acid zinc, calcium palmitate, and
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