发明名称 |
GLP-1 DERIVATIVES AND TRANSMICOSAL ABSORPTION PREPARATIONS THEREOF |
摘要 |
A GLP-1 derivative comprising a peptide having an amino acid sequence derived from the amino acid sequence of GLP-1 (7-35) by deletion, substitution and/or addition of one to several amino acids and having a GLP-1 activity to the C-terminus of which a sequence Waa-(Xaa)n-Yaa (wherein Waa represents Arg or Lys; Xaa represents Arg or Lys; n is an integer of from 0 to 14; and Yaa represents Arg, Arg-NH2, Lys, Lys-NH2 or Hse) is added. This derivative has a high transmucosal absorbability. Moreover, tolerance to dipeptidyl peptidase IV can be imparted to the derivative by substituting the 8-position of the GLP-1 amino acid sequence into Ser, while tolerance to trypsin can be imparted thereto by substituting the 26-position into Gln and the 34- position into Asn. The transmucosal absorbability of the above GLP-1 derivative can be further elevated by formulating into a preparation with the use of a charge-controller fat emulsifier having a surface charge controlled to the negative level.
|
申请公布号 |
KR20050049525(A) |
申请公布日期 |
2005.05.25 |
申请号 |
KR20057005890 |
申请日期 |
2005.04.06 |
申请人 |
SANWA KAGAKU KENKYUSHO CO., LTD. |
发明人 |
HAYASHI, YUJI;JOMORI, TAKAHITO;KOUZAKI, TOSHIYUKI;MAKINO, MITSUHIRO;TAKEDA, MOTOHIRO |
分类号 |
A61K38/00;A61K38/26;A61P3/04;A61P3/10;C07K14/605;(IPC1-7):C07K14/605;C07K14/575;A61K38/22 |
主分类号 |
A61K38/00 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|