| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10587965 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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.
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Authors
Mohammed I. El-Gamal, Hanan S. Anbar, Hye Jin Chung, Hyun-Il Kim, Young-Jin Cho, Bong Sang Lee, Sun Ahe Lee, Ji Yun Moon, Dong Jin Lee, Dow Kwon, Won-Jai Choi, Hong-Ryeol Jeon, Chang-Hyun Oh,