1. The pharmacokinetics and pharmacodynamic of concomitant administration of atorvastatin with bergamottin were investigated perspectives to reveal the potential herb-drug interaction between these two drugs.2. The hyperlipidaemia-induced Wistar rats received atorvastatin with or without bergamottin (2.5 mg/kg). The concentration of atorvastatin in the rats' serum was determined using an established HPLC/MS/MS method. The pharmacokinetic parameters were calculated using DAS software. Lipid levels were determined.3. Bergamottin increases the Cmax (from 48 ± 5 ng/mL to 89 ± 7 ng/mL), AUC0-∞ (from 176 ± 27 to 552 ± 131 h∗μg/L), and the elimination half-life of atorvastatin (t1/2) of atorvastatin. Co-administration of atorvastatin with bergamottin decreased total cholesterol (by 14%), low-density lipoproteins-cholesterol (by 20%), and triglyceride (by 12%), but increased thigh-density lipoprotein-cholesterol, when compared with atorvastatin alone.4. Co-administration of bergamottin and atorvastatin alters both pharmacokinetics and pharmacodynamics of atorvastatin. This study provides pre-clinical information evidence that bergamottin could potentiate the therapeutic efficacy of atorvastatin or increase its accumulation and adverse effects.
Keywords: Pharmacokinetics; atorvastatin; bergamottin; herb–drug interaction; pharmacodynamic.