LAUSR

Abstract Context: Ginkgo leaf tablets (GLT), an effective traditional Chinese multi-herbal formula, are often combined with atorvastatin calcium (AC) for treating coronary heart disease in clinic. Objective: This study investigated the effects of GLT on the pharmacokinetics of AC and the potential mechanism. Materials and methods: The pharmacokinetics of AC (oral administered at a dose of 1 mg/kg) with or without pre-treatment of GLT (oral administered at a dose of 80 mg/kg/day for 10 days) were investigated in male Sprague–Dawley rats. The effects of GLT on the metabolic stability of AC were also investigated using rat liver microsome incubation systems. Results: The results indicated that the Cmax increased from 36.84 ± 4.21 to 48.68 ± 6.35 ng/mL, and the AUC(0-t) increased from 135.82 ± 21.05 to 77.28 ± 12.92 ng h/mL, and t1/2 also increased from 2.62 ± 0.31 to 3.32 ± 0.57 h when GLT and AC were co-administered. The metabolic stability of AC was also increased (48.2 ± 6.7 vs. 36.7 ± 5.3 min) with the pre-treatment of GLT. Discussion: This study indicated that the main components in GLT could accelerate the metabolism of AC in rat liver microsomes and change the pharmacokinetic behaviours of AC. So these results showed that the herb-drug interaction between GLT and AC might occur, and the clinical efficacy could increase when they were co-administered. Therefore, the clinical dose of AC should be decreased when GLT and AC are co-administered.