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NOVEL CELL MEMBRANE-PERMEATING PEPTIDE 新技術説明会

外国特許コード F170008944
整理番号 (S2015-1544-N0)
掲載日 2017年2月1日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP064767
国際公開番号 WO 2016186140
国際出願日 平成28年5月18日(2016.5.18)
国際公開日 平成28年11月24日(2016.11.24)
優先権データ
  • 特願2015-101497 (2015.5.19) JP
発明の名称 (英語) NOVEL CELL MEMBRANE-PERMEATING PEPTIDE 新技術説明会
発明の概要(英語) The present invention addresses the problem of providing a novel membrane permeability-improving agent which can be applied to polymeric drugs. More specifically, the present invention addresses the problem of providing: a drug carrier which can improve the absorption efficiency of a polymeric drug in the small intestine; and a membrane permeation-improving agent containing the carrier. According to the present invention, a cell membrane-permeating peptide can be provided, which comprises an amino acid sequence selected from the group consisting of the following amino acid sequences: an amino acid sequence DNPGN (SEQ ID NO: 1); an amino acid sequence SRPAF (SEQ ID NO: 2); an amino acid sequence NDPRN (SEQ ID NO: 3); and an amino acid sequence MSVAN (SEQ ID NO: 4). According to the present invention, a cell membrane-permeating composition can also be provided, which comprises the peptide and a physiologically active substance.
従来技術、競合技術の概要(英語) BACKGROUND ART
Oral administration can be by a simple naturally in everyday life can be taken from the relatively safe non-invasive drug delivery method can be taken. In addition, that the gut structure and suitable for drug absorption, absorption from the surface area thereof is large, the development of pharmaceutical dosage forms as oral preparations has been desired. However, in order to enable the oral administration of drugs that must be overcome is the problem of some non-.
One, before shifting to the systemic circulation of the drug in the alimentary canal and may be decomposed by an enzyme at the same time. As a solution for this purpose, in the stomach by the enteric formulation technology or the like to prevent deactivation of the drug, drug is delivered to the intestinal tract is possible. Another problem is that the, drug intestinal mucosa, can be employed with sufficient transmission of the epithelium. Absorption in the gastrointestinal tract and pharmacokinetic of pharmaceuticals in oral administration of pharmacological activity is one of the critical determinant of. However, expected as a next generation pharmaceutical nucleic acid-soluble polymers such as pharmaceutical agents for extremely poor gastrointestinal absorption, in clinical, but oral administration by intravenous injection is limited to the method of administration.
So far, for an improved gastrointestinal absorption of a medicament in order to achieve, temporarily increase the permeability of biological membrane material and additives such as absorption promoters have been used for studies. Is an absorption enhancer, surfactant, fatty acid, alcohol or the like can be cited. However, absorption promoters and additives is, by opening and closing of tight junctions nonspecifically increase gastrointestinal absorption, diluted with water or the like in the living body to receive an adequate effect may not be exhibited, then, the safety of the local mucosa failure or the like in question. Therefore, the practical use are limited by the seat. In addition, these methods, the efficiency of absorption of a medicament for the improvement of the low molecular weight can be applied, absorption of a medicament to improve the efficiency of the polymer is insufficient.
In addition, the human immunodeficiency virus (HIV) peptide -1 Tat, peptide HIV-1 Lev, penetratin, transportan, arginine oligomers such as a membrane-bound peptides can be used to increase the gastrointestinal absorption of studies have been made. However, in basic research and promote absorption of insulin from the gastrointestinal tract and are available, and its efficiency is still about 20%, but is made with the clinical application, the sequence may be even more efficient has been sought. Further, a stem cell membrane-penetrating peptide-based co-polymer bonded to the transepithelial and improve absorption of a drug absorption enhancer also has been proposed (patent document 1).
In addition, liposomes modified with chitosan has been developed (non-patent document 1). The transport mechanism is used mainly for the transmission of spaces, acting on the actin F -, to attenuate the tight junctions. However, with respect to transcellular transport, through the interaction of mucin adsorption endocytosis is said to be in the barrier layer. This also has not reached the clinical application.
Small intestine absorption of a medicament as a method of improving polymer, proteolytic enzyme inhibitors is a combined method of the drag carrier has been proposed (non-patent document 2). Wherein, the peptide by an inhibitor of proteolytic enzymes, insulin protein formulation can suppress the decomposition of 100%. Then, smart hydrogel drag carrier is filled with insulin, the bioavailability of rats on oral administration and has been improved up to 10% have been reported (non-patent document 3). However, reaching the small intestine is drug absorption includes is still not sufficient. Therefore, oral administration is possible, for the purpose of improving the absorption in the small intestine and a more excellent drug carrier has been desired.
  • 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
  • NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY
  • 発明者(英語)
  • ITO, Shingo
  • OHTSUKI, Sumio
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 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
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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