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1. (WO2019026949) PREPARATION METHOD FOR SOLUTION CONTAINING BOTH WATER-SOLUBLE ACTIVE INGREDIENT AND PERCUTANEOUS-ABSORPTION CONTROL AGENT
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Pub. No.: WO/2019/026949 International Application No.: PCT/JP2018/028818
Publication Date: 07.02.2019 International Filing Date: 01.08.2018
IPC:
A61K 45/00 (2006.01) ,A61K 8/34 (2006.01) ,A61K 9/08 (2006.01) ,A61K 31/195 (2006.01) ,A61K 31/375 (2006.01) ,A61K 31/506 (2006.01) ,A61K 47/06 (2006.01) ,A61K 47/08 (2006.01) ,A61K 47/10 (2006.01) ,A61K 47/14 (2006.01) ,A61K 47/34 (2017.01) ,A61K 47/44 (2017.01) ,A61P 3/02 (2006.01) ,A61P 17/14 (2006.01) ,A61P 29/00 (2006.01) ,A61Q 19/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
8
Cosmetics or similar toilet preparations
18
characterised by the composition
30
containing organic compounds
33
containing oxygen
34
Alcohols
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
08
Solutions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
365
Lactones
375
Ascorbic acid, i.e. vitamin C; Salts thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
10
Alcohols; Phenols; Salts thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
14
Esters of carboxylic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
44
Oils, fats or waxes according to more than one of groups A61K47/02-A61K47/42109
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
02
Nutrients, e.g. vitamins, minerals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
14
for baldness or alopecia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
Q
SPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
19
Preparations for care of the skin
Applicants:
国立大学法人九州大学 KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION [JP/JP]; 福岡県福岡市東区箱崎六丁目10番1号 6-10-1, Hakozaki, Higashi-ku, Fukuoka-shi, Fukuoka 8128581, JP
日産化学株式会社 NISSAN CHEMICAL CORPORATION [JP/JP]; 東京都中央区日本橋二丁目5番1号 5-1, Nihonbashi 2-chome, Chuo-ku, Tokyo 1036119, JP
Inventors:
小野 文靖 ONO Fumiyasu; JP
後藤 雅宏 GOTO Masahiro; JP
Agent:
特許業務法人 津国 TSUKUNI & ASSOCIATES; 東京都千代田区麹町5-3-1 麹町ビジネスセンター Kojimachi Business Center, 5-3-1, Kojimachi, Chiyoda-ku, Tokyo 1020083, JP
山村 大介 YAMAMURA Daisuke; JP
Priority Data:
2017-14972202.08.2017JP
Title (EN) PREPARATION METHOD FOR SOLUTION CONTAINING BOTH WATER-SOLUBLE ACTIVE INGREDIENT AND PERCUTANEOUS-ABSORPTION CONTROL AGENT
(FR) PROCÉDÉ DE PRÉPARATION D’UNE SOLUTION CONTENANT À LA FOIS UNE SUBSTANCE ACTIVE HYDROSOLUBLE ET UN AGENT DE CONTRÔLE D’ABSORPTION PERCUTANÉE
(JA) 水溶性有効成分及び経皮吸収制御剤を含む溶液の調製方法
Abstract:
(EN) The purpose of the present invention is to satisfactorily dissolve a water-soluble active ingredient in a percutaneous-absorption control agent under mild conditions in a short time. The present invention relates to: a preparation method for a solution containing a water-soluble active ingredient and a percutaneous-absorption control agent, the method comprising a step in which the water-soluble active ingredient is dissolved in a short-chain alcohol to obtain a short-chain-alcohol solution (step 1), a step in which the percutaneous-absorption control agent is added to the short-chain-alcohol solution obtained in step 1 to obtain a liquid mixture (step 2), and a step in which the short-chain alcohol is removed from the liquid mixture obtained in step 2 (step 3); a percutaneous absorption composition which comprises a lipid-soluble medium and the solution obtained by said preparation method, which comprises a water-soluble active ingredient and a percutaneous-absorption control agent; and a method for controlling the release of the water-soluble active ingredient in the skin, the method including the aforementioned steps.
(FR) L’objectif de la présente invention est de dissoudre de façon satisfaisante une substance active hydrosoluble dans un agent de contrôle d’absorption percutanée dans des conditions douces en un temps court. La présente invention concerne : un procédé de préparation d’une solution contenant une une substance active hydrosoluble et un agent de contrôle d’absorption percutanée, le procédé comprenant une étape dans laquelle la substance active hydrosoluble est dissoute dans un alcool à chaîne courte pour obtenir une solution d’alcool à chaîne courte (étape1), une étape dans laquelle l’agent de contrôle d’absorption percutanée est ajouté à la solution d’alcool à chaîne courte obtenue dans l’étape 1 pour obtenir un mélange liquide (étape 2), et une étape dans laquelle l’alcool à chaîne courte est éliminé du mélange liquide obtenu dans l’étape 2 (étape 3) ; une composition d’absorption percutanée qui comprend un milieu liposoluble et la solution obtenue par ledit procédé de préparation, qui comprend une substance active hydrosoluble et un agent de contrôle d’absorption percutanée ; et un procédé de contrôle de la libération de la substance active hydrosoluble dans la peau, le procédé comprenant les étapes mentionnées ci-dessus.
(JA) 本発明は、水溶性有効成分が緩和な条件でかつ短時間で経皮吸収制御剤への良好な溶解性を達成することを目的とする。 本発明は、水溶性有効成分及び経皮吸収制御剤を含む溶液の調製方法であって、(工程1)前記水溶性有効成分を短鎖アルコールに溶解させて短鎖アルコール溶液を得る工程;(工程2)工程1で得られた短鎖アルコール溶液に前記経皮吸収制御剤を加えて、混合液を得る工程;(工程3)工程2で得られた混合液から、前記短鎖アルコールを除去する工程を含む調製方法;前記調製方法で得られる水溶性有効成分及び経皮吸収制御剤を含む溶液、ならびに脂溶性媒体を含む、経皮吸収組成物;ならびに前記工程を含む水溶性有効成分の皮膚中での放出を制御する方法に関する。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)