OBJECTIVE To develop a HPLC-ESI-MS assay for the determination of
sertraline in human
plasma and to investigate the
pharmacokinetics and bioequivalence of two sertraline tablets in human.METHODS After being treated with 1 mol·L~(-1) sodium hydroxide,plasma was processed by cyclohexane and compounds were separated on a reversed-phase C_(18) column with a mobile phase of methanol-10(mmol·L~(-1)) ammonium acetate buffer solution (pH 3.5)-acetonitrile(62∶28∶10).HPLC-ESI-MS was performed with the selected-ion monitoring mode.Target ions were at m/z 306.2 for sertraline and at m/z 306.1 for the internal standard.A randomized cross-over design was performed in 20 healthy volunteers.In the two study periods,a single dose of 50 mg sertraline
tablet was administered to each volunteer.RESULTS The calibration curve was linear over the range of 0.5～30 μg·L~(-1).The main pharmacokinetic parameters of t_(max),ρ_(max),t_(1/2) and AUC_(0～96 h) were(5.1±1.3) h,(15.24±2.52) μg·L~(-1),(29.32±5.02) h and(347.96±41.0) μg·h·L~(-1) for the reference tablet;(4.8±0.8) h,(15.86±2.78) μg·L~(-1),(29.53±5.40) h and(338.0±29.34) μg·h·L~(-1) for the test tablet.The
RESULTS of variance analysis and two one-side t-test showed that there was no significant difference between the two
formulations in the
AUC and ρ_(max).CONCLUSION The assay is proved to be sensitive,accurate and convenient.The two formulations are bioequivalent.
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