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Pharmacokinetics and Bioavailability of Dilevalol in Normotensive Volunteers
Author(s) -
Kramer William G.,
Nagabhushan Nagamani,
Affrime Melton B.,
Perentesis George P.,
Symchowicz Samson,
Patrick James E.
Publication year - 1988
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1988.tb03189.x
Subject(s) - pharmacokinetics , bioavailability , oral administration , volume of distribution , pharmacology , medicine , urine , high performance liquid chromatography , chemistry , chromatography
The bioavailability and pharmacokinetics of dilevalol following oral and intravenous administration were investigated in 12 healthy male volunteers. Dilevalol HCl was administered as a 200‐mg oral tablet and a 50‐mg intravenous infusion using a randomized cross‐over design. Blood and urine samples were collected over 60 hours and analyzed for unchanged and total (unchanged plus Glusulase‐released) dilevalol using an high performance liquid chromatography (HPLC) assay. After intravenous administration, total body clearance and volume of distribution of unchanged dilevalol were determined to be 23.2 mL/min/kg and 24.6 L/kg, respectively. After oral administration, a mean maximum concentration of 62 ng/mL was reached at an average peak time of 1.4 hours. Drug was eliminated with a half‐life of 8.3 hours after oral administration and 12 hours after intravenous administration. Based on plasma levels and urinary excretion of total dilevalol, the drug was completely absorbed; however, due to first‐pass metabolism, the absolute bioavailability of unchanged drug was 11 to 14%.