The Pharmacokinetics Study of Gossypol-acetate Enantiomers in Rat

Abstract

To establish a sensitive HPLC method for determination of gossypol-acetate (GA) enantiomers in rat plasma. The study involved administration of oral and intravenous to rats. Plasma samples were collected before and during the predetermined time intervals following administration of GA enantiomers, which were analyzed using HPLC method. The method showed a good linear relationship in the calibration range from 0.005 to 98.5 μg/mL. The calculations of pharmacokinetic parameters were performed by noncompartmental analysis using the software DAS 2.0. The pharmacokinetics of GA enantiomers after oral administration was both best fitted with two-compartment and the pharmacokinetic parameters (AUC 0 t ) of (-)-GA, (+)-GA and (±)-GA were 22.4 ± 7.3, 42.7 ± 7.0, 75.7 ± 14.4 mg/L per hour, respectively. The pharmacokinetics of GA enantiomers after intervals administration was both best fitted with threecompartment and the pharmacokinetic parameters (AUC 0 t ) of (-)-GA, (+)-GA and (±)-GA were 451.8 ± 15.8, 476.5 ± 37.5, 347.3 ± 33.4 mg/L per hour, respectively. These differences were statistically significant (P<0.05). The findings, therefore, showed that the biological availability of despinner was higher than enantiomers after oral administration, and which was just opposite after intervals administration.