Determination of Biapenem Concentration in Human Plasma by HPLC and Pharmacokinetic Study

OBJECTIVE: To establish a simple and rapid method for the determination of biapenem in human plasma and investigate pharmacokinetics of it. METHODS: Plasma samples were added 5-hydroxyindoleacetic acid 20 μL and then precipitated by 7% zinc sulfate. Agilent Zorbax Bonus-RP column was used with mobile phase consisted of methanol-0.3% acetic acid solution (gradient elution) at the flow rate of 1.0 mL·min~(-1). UV detection wavelength was set at 300 nm. RESULTS: 30 healthy volunteers were randomly divided into low-dose group, medium-dose group and high-dose group with single intravenous infusion. Pharmacokinetic parameters of biapenem were as follows: t_(1/2) were (1.13±0.16) h, (1.06±0.10)h and (1.11±0.12)h; t_(max) were (1.02±0.21)h, (1.10±0.31)h and (1.05±0.27)h; c_(max) were (9.04±4.24) μg·mL~(-1), (17.64±4.55)μg·mL~(-1) and (35.10±4.23)μg·mL~(-1);AUC_(0～12 h) were (18.17±3.86)mg·h·L~(-1), (36.44±7.68)mg·h·L~(-1) and (70.24±8.91)mg·h·L~(-1);AUC_(0～∞) were (20.42±4.69)mg·h·L~(-1), (37.21±7.63)mg·h·L~(-1) and (72.40±9.03) mg·h·L~(-1). t_(1/2), t_(max), c_(max), AUC_(0～12 h) and AUC_(0～∞) of multiple dose were (1.07±1.35) h, (1.04±0.60) h, (19.61±3.68)μg·h~(-1), (32.47±3.90) mg·h·L~(-1) and (33.36±3.80)mg·h·L~(-1). CONCLUSION: Pharmacokinetic parameters of 3 groups are in linear correlation. There is no difference in interior-group and intra-group among different dosages, as well as different age, gender, height and body weight.