Biopharmaceutical profile of cerivastatin: a novel HMG-CoA reductase inhibitor

The biopharmaceutical properties of cerivastatin were evaluated in a series of worldwide clinico-pharmacological studies, Young healthy males aged 18 - 45 years were randomized to receive 0.05 - 0.8 mg cerivastatin orally, gi ven either as single or multiple once-daily doses under fed or fasting cond itions in the morning, with evening meal or at bedtime, Following administr ation, cerivastatin was rapidly and almost completely absorbed into the gas trointestinal tract (> 98%), with maximum plasma concentrations (C-max) rea ched at 2 - 3 h post dose, The plasma concentration/time profile of the tab let is similar to an aqueous oral solution (relative bioavailability is 100 %), The dose-proportionality of cerivastatin (0.05 - 0.8 mg) in area under the curve and C-max showed low intra- and interindividual variability, The max effect of food (single-dose studies testing administration of cerivasta tin with a high-fat meal and clinical investigations in patients) or time o f administration (single- and multiple-dose once-daily/twice-daily studies) had no clinically relevant effects on the pharmacokinetics of cerivastatin , Marketed tablet strengths and drug formulations from different sources we re found to be bioequivalent. Cerivastatin is a noncomplicated drug with re spect to its biopharmaceutical profile and bioavailability.