Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2017038612) PHARMACEUTICAL COMPOSITION CONTAINING RAPAMYCIN OR DERIVATIVE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2017/038612 International Application No.: PCT/JP2016/074781
Publication Date: 09.03.2017 International Filing Date: 25.08.2016
IPC:
A61K 31/436 (2006.01) ,A61P 29/00 (2006.01) ,A61P 35/00 (2006.01) ,A61P 37/02 (2006.01) ,A61P 37/06 (2006.01)
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
436
the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
Applicants:
日本化薬株式会社 NIPPON KAYAKU KABUSHIKI KAISHA [JP/JP]; 東京都千代田区丸の内二丁目1番1号 1-1, Marunouchi 2-chome, Chiyoda-ku, Tokyo 1000005, JP
Inventors:
川村 大 KAWAMURA Dai; JP
Agent:
特許業務法人特許事務所サイクス SIKS & CO.; 東京都中央区京橋一丁目8番7号 京橋日殖ビル8階 8th Floor, Kyobashi-Nisshoku Bldg., 8-7, Kyobashi 1-chome, Chuo-ku, Tokyo 1040031, JP
Priority Data:
2015-16907528.08.2015JP
Title (EN) PHARMACEUTICAL COMPOSITION CONTAINING RAPAMYCIN OR DERIVATIVE THEREOF
(FR) COMPOSITION PHARMACEUTIQUE CONTENANT DE LA RAPAMYCINE OU UN DÉRIVÉ DE CELLE-CI
(JA) ラパマイシン又はその誘導体を含有する医薬組成物
Abstract:
(EN) The present invention addresses the problem of providing a pharmaceutical composition that has a high safety and with which the long-term stability can be ensured and the reduction in the amount of an active ingredient accompanying the oxidation or decomposition of rapamycin or a derivative thereof is inhibited. The invention of this pharmaceutical preparation containing rapamycin or a derivative thereof was achieved after discovering that the oxidation or decomposition of rapamycin or a derivative thereof can be inhibited by jointly using a tocopherol derivative and an ascorbic acid fatty acid ester. Preferably, the rapamycin or the derivative thereof, the tocopherol derivative, and the ascorbic acid fatty acid ester are a solid mixture prepared by preparing a solution that contains said components and then removing the solvent from the solution.
(FR) La présente invention aborde le problème de la fourniture d'une composition pharmaceutique dont la sûreté est élevée, dont la stabilité à long terme peut être assurée et dans laquelle la réduction de la quantité d'un ingrédient actif accompagnant l'oxydation ou la décomposition de la rapamycine ou d'un dérivé de celle-ci est inhibée. Ladite préparation pharmaceutique contenant de la rapamycine ou un dérivé de celle-ci a pu faire l'objet d'une invention après la découverte selon laquelle l'oxydation ou la décomposition de la rapamycine ou d'un dérivé de celle-ci peut être inhibée par utilisation conjointe d'un dérivé de tocophérol et d'un ester d'acide gras d'acide ascorbique. De préférence, la rapamycine ou le dérivé de celle-ci, le dérivé de tocophérol, et l'ester d'acide gras d'acide ascorbique forment un mélange solide préparé par préparation d'une solution qui contient lesdits composants puis par élimination du solvant de la solution.
(JA) 本発明は、ラパマイシン又はその誘導体の酸化や分解に伴う有効成分含量の低減を抑制し、長期安定性が確保でき、且つ安全性が高い医薬組成物を提供することを課題とする。本発明においては、ラパマイシン又はその誘導体を含有する医薬製剤において、トコフェロール誘導体及びアスコルビン酸脂肪酸エステルを組み合せて用いることでラパマイシン又はその誘導体の酸化又は分解が抑制できることを見出し、発明を完成させるに至った。該ラパマイシン又はその誘導体と、トコフェロール誘導体及びアスコルビン酸脂肪酸エステルは、これらを含有する溶液を調製した後、溶媒を除去することにより調製される固体混合物であることがより好ましい。
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 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)