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Aim: To elucidate the effect of baicalin on the pharmacokinetics of theophylline in rats, focusing on plasma protein binding displacement and inhibitory effect on CYP1A2 in vivo and in vitro.Methods: This study was a randomized, three-period crossover design.Theophylline (5 mg/kg, iv) was administered to rats immediately following the injection of baicalin (450 mg/kg, given 1 time or divided into 3 times).