Enantioselective oral bioavailability of 0-isovaleryl propranolol as a potential prodrug of propranolol.
The enantioselective oral bioavailability of propranolol (PL) from 0-isovaleryl-PL was determined and compared with parent PL in beagle dogs. The bioavailability of the individual enantiomer from the prodrug increased about 2 fold. The AUC ratio between the S(-)- and R(+)-isomer posed at 0.89 which was statistically not different from that obtained after administration of PL alone. These features indicate that 0-isovaleryl-PL promises to be a potential prodrug of PL from the pharmacokinetic and pharmacodynamic point of view.
Shameem
M
M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Imai
T
T
Otagiri
M
M
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D011355:Prodrugs / Q000493:pharmacokinetics*; D011433:Propranolol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics*; D013237:Stereoisomerism
D011355:Prodrugs; C079647:O-isovaleryl propranolol; D011433:Propranolol