期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 5, 页码 1347-1350出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.12.090
关键词
Antihypertensive; Olmesartan medoxomil; Olmesartan hexetil; Prodrug; Ester; Pharmacokinetics
资金
- Seoul RBD program [PA100015]
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. C-max and AUC(last) 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. (C) 2013 Elsevier Ltd. All rights reserved.
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