1301633-27-1Relevant articles and documents
Discovery of olmesartan hexetil: A new potential prodrug of olmesartan
El-Gamal, Mohammed I.,Anbar, Hanan S.,Chung, Hye Jin,Kim, Hyun-Il,Cho, Young-Jin,Lee, Bong Sang,Lee, Sun Ahe,Moon, Ji Yun,Lee, Dong Jin,Kwon, Dow,Choi, Won-Jai,Jeon, Hong-Ryeol,Oh, Chang-Hyun
, p. 1347 - 1350 (2013)
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 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.