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Aim: To study effects of CYP3A4*1G (G>A), CYP3AP1*3 (G>A) and gender on pharmacokinetics of simvastatin and simvastatin acid.Methods: The polymorphisms of CYP3A4*1G and CYP3AP1*3 were determined by polymerase chain reaction-restriction fragment length polymorphism.Serial blood samples were obtained up to 24 h after a single dose of 40 mg simvastatin intake in healthy Chinese volunteers.