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COMPOSITION FOR ORAL DELIVERY OF SORAFENIB AND USE OF SAID COMPOSITION NEW

外国特許コード F200010185
整理番号 S2020-0020-N0
掲載日 2020年7月28日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2019JP017366
国際公開番号 WO 2019208617
国際出願日 平成31年4月24日(2019.4.24)
国際公開日 令和元年10月31日(2019.10.31)
優先権データ
  • 特願2018-086627 (2018.4.27) JP
発明の名称 (英語) COMPOSITION FOR ORAL DELIVERY OF SORAFENIB AND USE OF SAID COMPOSITION NEW
発明の概要(英語) [Problem] To provide a pharmaceutical composition effective in fibrosis.
[Solution] Provided is: a composition containing a copolymer that includes a sorafenib and poly(ethylene glycol) segment, as well as a segment based on polystyrene having a cyclic nitroxide radical and a tri(alkoxysilane) each randomly in a side chain, the copolymer optionally containing a tetra(alkoxy)silane; or nanoparticles formed from said composition.
従来技術、競合技術の概要(英語) BACKGROUND ART
Such as fibrosis of liver fibrosis, associated with the result of the long-term damage of the tissue or organ, liver cirrhosis, results in failure and liver cancer. Adjusting the liver fibrosis progression of the major effector cells (HSCs) hepatic stellate cell is in. Sorafenib is a possibility of anti-fibrotic agents as inhibitors of tyrosine kinases. Sorafenib is the gastrointestinal tract due to the low solubility of the absorbent is not sufficient, the treatment effect is low, the porous silica material and the pH-sensitive copolymer (for example, Eudragit (registered trademark) ) by using nano-matrix composed of the disadvantages due to the nature of correct sorafenib attempt to also have been proposed (see non-patent document 1). Yet however, is not sufficiently satisfactory.
On the other hand, the inventors of the present invention, also referred to as a redox agent however, annular anti-oxide compounds classified (in particular, (TEMP) 2, 2, 6, 6-tetramethylpiperidinyl roh oxyradical) nitroxide poly (ethylene glycol) poly (chloromethylstyrene) and the segment of the copolymer containing the segment via a chloromethyl groups can be conjugated to a side chain caused by the polymer, which are stable in vivo, and, safety compounds that can be used successfully to create a, the proposed (Patent Document 1 and Patent Document 2). Thus providing a polymer (PEG-b-PMNT) circular nitroxide radical derived from the nanoparticles (N-TEMPO-RNP,O-TEMPO-RNP), for example, by intravenous administration of the blood during a dwell are achieved over a long period of time, the active oxygen species (ROS) due to the prevention or treatment of an inflammatory disease of the constant can be described. In the above, as a side chain of the poly (methylstyrene) PMNT nitroxide radical is bonded to the annular means, N-TEMPO and O-TEMPO is, in the polymer main chain and - NH-O - each TEMPO via means that are covalently bonded (hereinafter, these abbreviations are used throughout this specification may be the same.). These nano-particles is included in the rate constant for the agent is not necessarily high, the inventors of the present invention, further a trialkoxysilyl group in its side chain bonded to the copolymer was made to design, such a copolymer formed from silica-containing nanoparticle (siRNP) is a hydrophobic drug can be effectively included in the BNS-22, moreover, to increase the bioavailability of the drug and, the drug can be reduced due to the toxicity was observed (Non-Patent Document 2).
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • UNIVERSITY OF TSUKUBA
  • ASAHIKAWA MEDICAL UNIVERSITY
  • 発明者(英語)
  • NAGASAKI, Yukio
  • TRAN, Hao Thi
  • VONG, Binh Long
  • NISHIKAWA, Yuji
  • SHASHNI, Babita
国際特許分類(IPC)
指定国 National 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
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
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
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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