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TRANSMUCOSAL ABSORPTION PROMOTER FOR LOW-MOLECULAR PHARMACEUTICAL COMPOUND

Foreign code F180009517
File No. (S2017-0303-N0)
Posted date Nov 2, 2018
Country WIPO
International application number 2018JP004702
International publication number WO 2018147437
Date of international filing Feb 9, 2018
Date of international publication Aug 16, 2018
Priority data
  • P2017-023567 (Feb 10, 2017) JP
Title TRANSMUCOSAL ABSORPTION PROMOTER FOR LOW-MOLECULAR PHARMACEUTICAL COMPOUND
Abstract The present invention addresses the problem of providing a transmucosal absorption promoter for low-molecular pharmaceutical compounds. The problem is solved by providing a transmucosal absorption promotor for low-molecular pharmaceutical compounds, the promotor containing a cell membrane-penetrating peptide.
Outline of related art and contending technology BACKGROUND ART
New drug candidate compound is found in recent years, reduced membrane permeability, pharmaceutical, pharmacokinetic properties such as having a problem is pointed out that in many cases. Biopharmaceutics Classification System (BCS) 3 are not classified into the class is 4, and the like express Breast Cancer Resistance Protein (BCRP) P-glycoprotein (P-gp) the gastrointestinal tract of a substrate transporter can be a medicament outlet, low membrane permeability and the main factors. May be a good candidate compound, transmucosal absorption is significantly reduced, if dynamic control is difficult, during development the dropout rate increases. Anti-cancer agent such as an excessive rise in the development cost can be suppressed, the cost of medical care costs or country agent in order to reduce the, candidate pharmaceutical compounds to improve the properties of transmucosal absorption, increase the probability of successful research and development of pharmaceuticals is possible to construct the base technology is essential.
A substrate transporter and the discharge agent insoluble drug transmucosal absorption of the absorbent for the purpose of improving, with respect to the transporter to this as the use of a specific inhibitor of the interaction between drugs using the competitive techniques have been attempted. However, these conventional approaches are supposed to be originally provided with a living body is in the foreign matter discharge function to fail, or, to increase or decrease the effect of the drug of the other possibility, from the viewpoint of safety and is not always a universal method. In addition, a drug carrier to encapsulate the nano-particles from the transporter to avoid the perception of a technique has been attempted, cannot necessarily be useful, a preparation method thereof is also complicated.
In recent years, peptide TAT, such as a cell membrane of the various peptide (cell-penetrating peptides (CPPs) ) penetratin used, can facilitate the introduction of the drug in the bio cell has been reported (Non-Patent Document 1). However, these peptides, crosslinking of the drug by the drug used to facilitate transmucosal absorption or in, a protein, a peptide of a relatively high molecular weight to facilitate transmucosal absorption of the drug is large in (Patent Document 1) has.
Scope of claims (In Japanese)請求の範囲
[請求項1]
細胞膜透過ペプチドを含有する、低分子医薬化合物の経粘膜吸収促進剤。
[請求項2]
前記細胞膜透過ペプチドが、ペネトラチン及びオリゴアルギニンペプチドからなる群より選択される少なくとも1種である、請求項1に記載の経粘膜吸収促進剤。
[請求項3]
前記細胞膜透過ペプチドがペネトラチンである、請求項1又は2に記載の経粘膜吸収促進剤。
[請求項4]
前記低分子医薬化合物の分子量が1000以下である、請求項1~3のいずれかに記載の経粘膜吸収促進剤。
[請求項5]
前記低分子医薬化合物の経口バイオアベイラビリティが40%以下である、請求項1~4のいずれかに記載の経粘膜吸収促進剤。
[請求項6]
請求項1~5のいずれかに記載の経粘膜吸収促進剤及び低分子医薬化合物を含有する、医薬組成物。
[請求項7]
経粘膜投与剤である、請求項6に記載の医薬組成物。
[請求項8]
経口剤である、請求項6又は7に記載の医薬組成物。
[請求項9]
低分子医薬化合物の経粘膜吸収促進剤としての使用のための、細胞膜透過ペプチド。
[請求項10]
低分子医薬化合物の経粘膜吸収促進剤を製造するための、細胞膜透過ペプチドの使用。
[請求項11]
低分子医薬化合物と細胞膜透過ペプチドを併用することを含む、低分子医薬化合物の経粘膜吸収促進方法。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • KOBE GAKUIN EDUCATIONAL FOUNDATION
  • Inventor
  • TAKEDA, Mariko
  • KAMEI, Noriyasu
IPC(International Patent Classification)
Specified countries 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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