Title:
ポリマー溶融物内の超安定型インスリン類似体のカプセル化
Document Type and Number:
Japanese Patent JP7203415
Kind Code:
B2
Abstract:
An insulin composition comprises an insulin analogue and polymer blend. The insulin analogue contains cysteine substitutions at positions B4 and A10 (to form cystine B4-A10), and one or more additional substitutions selected from the group consisting of: a connecting domain of 5-11 amino acids between insulin A- and B domains; a non-beta-branched amino-acid substitution at position A8; a non-beta-branched acidic or polar side chain at position A14; a halogenic modification of PheB24 at the ortho position; and substitution of lysine at position B29 by Glu, Ala, Val, Ile, Leu, amino-propionic acid, amino-butryic acid, or Norleucine. The insulin analogue is compatible with a process of manufacture that includes one or more steps within the temperature range 90-120° C. The encapsulated insulin analogue may optionally contain free PEG or be PEGylated. The insulin analogue-encapsulated polymer blend may be cast as a microneedle patch for topical administration or as micropellets for subcutaneous injection.
Inventors:
Weiss, Michael
Pokolski, John
Pokolski, John
Application Number:
JP2018524288A
Publication Date:
January 13, 2023
Filing Date:
December 23, 2016
Export Citation:
Assignee:
CASE WESTERN RESERVE UNIVERSITY
International Classes:
A61K38/28; A61K9/00; A61K9/10; A61K9/70; A61K47/34; A61P3/10
Domestic Patent References:
| JP2011529692A | ||||
| JP2011521621A | ||||
| JP2013530702A |
Foreign References:
| WO2007081824A1 | ||||
| WO2013010048A1 |
Other References:
Protein Sci. (2013), 22 (3), p.296-305
J. BIOL. CHEM. (2008), 283 (21), p.14703-14716
AAPS PharmSciTech (2012), 13 (1), p.313-322
J. BIOL. CHEM. (2008), 283 (21), p.14703-14716
AAPS PharmSciTech (2012), 13 (1), p.313-322
Attorney, Agent or Firm:
Taro Yaguchi
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