Linezolid is the first synthetic antibiotic of oxazolidinone group that can inhibit bacterial
protein synthesis. Previous studies have found that linezolid was an effective treatment for
multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB). In
addition, the current dosage recommendation (1,200 mg/day) occasionally resulted in serious
adverse events including bone marrow suppression and peripheral neuropathy.
The objective study were determine the pharmacokinetics of oral linezolid 300 mg /day in
healthy volunteers. This study conducted in six healthy volunteers. All subject received an
oral linezolid 300 mg/day by directly observed treatment (DOT) at the same time each day for
5 days. Blood samples were collected on day 5 at 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and
24 h post dosing. The separated plasma samples were evaluated by ultra-performance liquid
chromatography (UPLC). All pharmacokinetic parameters were calculated.