Lovastatin is a standard
therapy for
dyslipidemia. Alternatively, some ethnomedicines, such as Coptidis preparation, have been used for the treatment of
dyslipidemia.
Statins and complementary and alternative medicines may possess individual mechanisms of action against
dyslipidemia. We hypothesize that the combination of Coptidis preparation and
lovastatin may have synergistic effects for the treatment of
dyslipidemia. To investigate this hypothesis, we developed a validated ultra-high-performance liquid chromatography-tandem mass spectrometry method to monitor
lovastatin and its metabolites for pharmacokinetic studies in rats. This study was divided into four groups:
lovastatin (10 mg/kg, p.o.) alone and
lovastatin (10 mg/kg, p.o.) + Coptidis preparation (0.3, 1, or 3 g/kg, p.o.) for five consecutive days. In pharmacodynamic studies, a high-fat diet (HFD) was used to induce
dyslipidemia in experimental rat models. The HFD rats were divided into four groups: treatment with HFD, HFD +
lovastatin (100 mg/kg, p.o.), HFD + Coptidis preparation (1 g/kg, p.o.), and HFD +
lovastatin (50 mg/kg, p.o.) + Coptidis preparation (1 g/kg, p.o.) for 28 consecutive days. The pharmacokinetic results demonstrated that Coptidis preparation significantly augmented the conversion of
lovastatin into its main metabolite
lovastatin acid in vivo. The pharmacodynamic results revealed that the Coptidis preparation and half-dose
lovastatin group reduced the
body weight, liver weight, and visceral fat in HFD rats. These findings provide constructive preclinical pharmacokinetic and pharmacodynamic applications of Coptidis preparation on the benefit of
hyperlipidemia.