The purpose of this study was to investigate the effect of ketoconazole (20 mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel (40 mg/kg) orally coadministered in rats. The plasma concentration of paclitaxel in combination with ketoconazole was significantly (p<0.05) increased from 8 hr to 24 hr compared to that of control. Area under the plasma concentration-time curve (AUC) of paclitaxel with ketoconazole was significantly (coadministration p<0.05, pretreatment p<0.0l) higher than that of control. Peak concentration $(C_{max})$ of paclitaxel pretreated with ketoconazole were significantly (p<0.05) increased compared to that of control. Time to peak concentation $(T_{max})$ of paclitaxel pretreated with ketoconazole were significantly (p<0.05) shorter than that of control. Half-life at elimination phase $(t_{1/2{eta}})$ of paclitaxel pretreated with ketoconazole was significantly (p<0.05) prolonged compared to that of control. Based on these results, it might be due to both inhibition of the enzyme cytochrome P450 and p-glycoprotein, which engaged in paclitaxel absorption and metabolism in liver and gastrointestinal mucosa.