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. 1983;16(Suppl 2):285S–290S. doi: 10.1111/j.1365-2125.1983.tb02302.x

Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration

Roeline Jochemsen, J G J Wesselman, J Hermans, C J van Boxtel, D D Breimer
PMCID: PMC1428208  PMID: 6661374

Abstract

1 Pharmacokinetics and bioavailability of brotizolam after i.v. and oral administration were studied in healthy young volunteers.

2 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.).

3 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.).

4 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%).

Keywords: brotizolam i.v. and oral administration, pharmacokinetics, elimination half-life, healthy volunteers

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Selected References

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