Discovery of olmesartan hexetil: A new potential prodrug of olmesartan

Title
Discovery of olmesartan hexetil: A new potential prodrug of olmesartan
Authors
모하메드엘가말Hanan S. Anbar정혜진김현일조영진이봉상이선애문지윤이동진권도우최원재전홍렬오창현
Keywords
Antihypertensive; Ester; Olmesartan medoxomil; Pharmacokinetics; Olmesartan hexetil; Prodrug
Issue Date
2013-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 23, NO 5, 1347-1350
Abstract
Synthesis of a new ester prodrug of olmesartan, olmesartan hexetil (1), is described. It is in vitro stabilities and in vivo pharmacokinetics (PK) were evaluated. It showed high stability in simulated gastric juice, and was rapidly hydrolyzed to olmesartan in rat liver microsomes and rat plasma in vitro. Cmax and AUClast for olmesartan were significantly increased in case of hexetil prodrug, compared with olmesartan medoxomil. Olmesartan hexetil is proposed to be an efficient prodrug of olmesartan with markedly increased oral bioavailability
URI
http://pubs.kist.re.kr/handle/201004/46267
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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