Study On Bioequivalence Of Sparfloxacin Capsules In Healthy Subjects

Sparfloxacin is a synthetic broad-spectrum antimicrobial agent, which has activity against a wide range of gram-negtive and gram-positive microorganisms. The aim of this study was to evaluate the bioequivalence between two kinds of sparfloxacin capsules.An HPLC method with high precision, particularity and sensibility was developed and validated for sparfloxacin assay in plasma sample. A Kromasil C18(150mm×4.6mm,5um) column was selected and the mobile phase was consisited of 50mM KH2PO4 solution (pH2.5)- acetonitrile (77: 23) at a flow rate of 1.0 mL·min-1. The detective wavelenghth was 364nm.A single oral dose of 300mg test or reference capsule of sparfloxacin was administered by randomized, two-period crossover self-control way in 18 healthy male volunteers and the plasma concentrations of sparfloxacin in 96 hours after dose were determined by HPLC. The pharmacokinetic parameters were calculated by software BAPP2.0.Tmax of the test capsules and reference capsules were 4.3±1.1h and 4.4±1.0h,Cmax were 1205.36±390.85mg·L-1 and 1143.01±309.33mg·L-1, T1/2 were 23.59±4.54h and 22.90±3.56h,AUC(0→t) were 33365.80±9661.41 mg·h·L-1 and 31571.94±7733.55 mg·h·L-1.The main PK parameters were analized by varience analysis, two one-side t-test and 90% confidential internal (AUC). The result showed that the 90% confidential internal of test capsule to reference capsule is 100.54%~108.80% in AUC(0→t), and the un-bioequivalence hypothesis was refused. It was concluded that test and reference sparfloxacin capsules were bioequivalence, indicating the test capsule could be a substitution in clinic use.