| Faropenem is an orally-active beta-lactam antibiotic belongs to Carbapenems Antibiotics, usually exists as the state of sodium salt. It can be taken by injection or oral administration. Faropenem has a wide-spectrum antibacterial activity, especially for the drug-resistance gram-positive bacteria, such as Staphylococcus and Enterococcus, and Anaerobic Bacteria, such as bacteria. It is obviously better than the oral antibacterial drugs which are already in the markets. This article presents us some primary research in drug concentration, stability in test and the pharmacokinetics and bioequivalence in health Chinese volunteers.In the concentration test, we used perchloric acid as precipitant, and the drug in human plasma was detected by HPLC-UV. The results show that this method guarantees the stability and the accuracy. We improve the low detective limit to the level of 0.02mg/L. This assay established the method which can detect the drug concentration in human plasma. This method was simple, high-efficiency, noninterference and high sensitivity, which is suitable for the research in pharmacokinetics.In the pharmacokinetics test of tablet, 30 health volunteers were taken 150mg, 300mg, 600mg and multiple-does (300 mg/time, 3 times/day) of Faropenem tablets by oral. We treat the data by DAS2.0. Three groups of single-does volunteers do not have obviously difference in half-life, and the Cmax is proportional to the AUC0～∞ . The pharmacokinetic parameters of these three groups present linear features, and there is no obvious difference between male and female. T1/2 are (1.106±0.282)h, (0.969±0.213)h,(1.14±0.356)h,(1.007±0.205)respectively, and this indicate that faropenem is eliminated fast in human body. Cmin is typically less than Cmax(Cmin is less than 1/40 of Cmax), and this shows that faropenem is not accumulated in tissue. The drug in urine excretion shows that when volunteers oral administrate 300mg/person, the urinary excretory rate was (2.873±3.637)%, which indicates few drug is excreted from kidney as parent drug.In the bioequivalence test of granules, we detected the concentration of drug in human plasma by HPLC-UV after 20 health Chinese volunteers oral administrate 3 bags and 2 tablets of faropenem in the same drug dose. The relative bioavailability is estimated by the area method. Cmax, AUC0-8, AUC0-∞ of test preparation and reference preparation were variance analyzed after a logarithmic transformation. They were bioequivalence evaluated by the method of two one-side t-test and [1-2α] % confidence interval, and Tmax was analyzed by non-parametric method. The results indicate that test preparation and reference preparation are bioequivalence. |
