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.