ABSTRACT
AIM: To compare the bioavailability of the test and reference formulation of secnidazole (2 g) tablets under fasting conditions. METHODS: This bioequivalence study was carried out in 20 healthy male Chinese volunteers according to a single dose, two-sequence, crossover randomized design. Fifteen blood samples per period were collected over 96 h, and plasma secnidazole concentrations were determined by locally validated high performance liquid chromatography (HPLC) assay and pharmacokinetic parameters were analyzed by the non-compartmental and compartmental methods. RESULTS: Plasma concentration-time profiles were adequately described by a one-compartment open model with first-order absorption. The main pharmacokinetic parameters of secnidazole test and reference tablets were as follows: tmax were (2.30±1.06) and (2.28±1.10) h, Cmax were (49.63±6.35) and (46.17±4.24) mg/L, t1/2 were (28.84±3.41) and (29.05±4.01) h, AUC0-96 were (1832.06±180.15) and (1847.14±204.14) mg·h-1·L-1, respectively. The relative bioavailability of test tablets was (99.99±11.92)%. CONCLUSION: The results indicate that the two formulations of secnidazole tablets are bioequivalent in the rate and extent of absorption.
ABSTRACT
OBJECTIVE:To establish a HPLC method for the determination of mycophenolic acid (MPA) in human plasma and to study its pharmacokinetics in human body.METHODS:After sedimentation by methanol,plasma sample of MPA was determined directly on Symmetry Shield C18 column with column temperature at 30℃,detective wavelength at 218mn and sample size at 20?L.The mobile phase consisted of acetonitrile-water-triethylamine(40∶60∶0.3) with a flow rate of 1.0mL?min-1.RESULTS:The calibration curve was linear over the range of 0.2～50mg?L-1(r=0.999 6)and the limit of quantitation was 0.2mg?L-1.The mean methodological recovery was 101.94% and the mean extraction recovery was 87.06%.The RSD of both the intra-day and the inter-day were less than 6%.The pharmacokinetic study showed that MPA had enterohepatic circulation in human body,which resulted in the occurrence of double peaks,and the concentration-time curves of MPA were fitted to one-compartment open model.CONCLUSION:This method is sensitive,rapid,specific,accurate and precise,and can be used for the study of pharmacokinetics of MPA.
ABSTRACT
This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet, Tp; sustained-release capsule, TJ and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. Tmax, Cmax and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5 +/- 16.9% (Tp) and 110.4% +/- 9.6% (Tj). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, Tmax, Cmax MRT and DF had significant difference (P < 0.05); Cav, Cmin and AUC0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.