Plasma clearance of lovastatin versus Chinese red yeast rice in healthy volunteers

Objectives: It is now accepted that inhibition of cholesterol biosynthesis is effective in the primary and secondary prevention of heart disease. However, the perceived side-effects on muscle and liver reduce the general acceptance of statin drug therapy as well as compliance over the long term, which is necessary for prevention efforts to be successful. Chinese red yeast rice (CRYR) is a supplement containing lovastatin (monacolin K), eight other monacolins, pigments, tannins, and other phytochemicals. The authors previously reported on a double-blind placebo-controlled trial of CRYR supplement in 80 individuals demonstrating a significant decrease in cholesterol levels from 250 mg/dL to 210 mg/dL over 8 weeks independent of diet. The current study compared the pharmacokinetics of CRYR with lovastatin at the same bioeffective dose for lowering cholesterol. Methods: Eleven (11) healthy volunteers were randomized to a crossover study taking 2400 mg CRYR or 20 mg, of lovastatin. Results: The C-max and area under the curve (AUC) of lovastatin were 22.42 ng/mL, and 80.47 higher than CRYR (p = 0.001 and 0.002, respectively). The C-max for lovastatin hydroxy-acid was 36.63 ng/mL higher than the C-max of CRYR hydroxy-acid (p = 0.001). The AUC of lovastatin hydroxy-acid was 258.5 greater than that of CRYR (p = 0.001). Conclusions: The results suggested that the effect of CRYR on the cholesterol concentration might be caused by the additive and/or synergistic effects of monacolin K with other monacolins and substances in CRYR. It may lead to the ultimate development of a botanical supplement based on CRYR.