title: Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration.
abstract: Pharmacokinetics and bioavailability of brotizolam after i.v. and oral administration were studied in healthy young volunteers. Kinetic parameters after i.v. administration were: volume of distribution 0.66 +/- 0.19 1/kg, total plasma clearance 113 +/- 28 ml/min, distribution half-life 11 +/- 6 min, and elimination half-life 4.8 +/- 1.4 h (mean values +/- s.d.). Kinetic parameters after oral administration were: absorption lag-time 8 +/- 12 min, absorption half-life 10 +/- 11 min, and elimination half-life 5.1 +/- 1.2 h (mean values +/- s.d.). Bioavailability of brotizolam was 70 +/- 22% when calculated by comparing oral and intravenous area-under-curve values, corrected for intra-individual half-life differences. An alternative calculation method, which is relatively independent of large clearance variations, provided a bioavailability of 70 +/- 24% (range: 47-117%).
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001381:Azepines / Q000008:administration & dosage / Q000378:metabolism*; D001682:Biological Availability; D005260:Female; D006207:Half-Life; D006801:Humans; D006993:Hypnotics and Sedatives / Q000008:administration & dosage / Q000378:metabolism*; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D014018:Tissue Distribution
chemical_list: D001381:Azepines; D006993:Hypnotics and Sedatives; C020960:brotizolam