Rutaecarpine, an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa, has been shown to be anti-inflammatory. In the present study, a possible interaction between rutaecarpine and caffeine was investigated in male Sprague Dawley rats. Twenty four hr after the oral pretreatment wi...
Rutaecarpine, an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa, has been shown to be anti-inflammatory. In the present study, a possible interaction between rutaecarpine and caffeine was investigated in male Sprague Dawley rats. Twenty four hr after the oral pretreatment with rutaecarpine at 80 mg/kg for three consecutive days, rats were treated intravenously with 10 mg/kg of caffeine. Compared with control rats, the pharmacokinetic parameters of caffeine in rutaecarpine-pretreated rats were significantly changed, possibly due to the rapid metabolism. The production of three metabolites of caffeine (i.e., paraxanthine, theobromine and theophylline) was also significantly changed in rats pretreated with rutaecarpine. The present results suggest that oral rutaecarpine would change the intravenous pharmacokinetic characteristics of caffeine.
Rutaecarpine, an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa, has been shown to be anti-inflammatory. In the present study, a possible interaction between rutaecarpine and caffeine was investigated in male Sprague Dawley rats. Twenty four hr after the oral pretreatment with rutaecarpine at 80 mg/kg for three consecutive days, rats were treated intravenously with 10 mg/kg of caffeine. Compared with control rats, the pharmacokinetic parameters of caffeine in rutaecarpine-pretreated rats were significantly changed, possibly due to the rapid metabolism. The production of three metabolites of caffeine (i.e., paraxanthine, theobromine and theophylline) was also significantly changed in rats pretreated with rutaecarpine. The present results suggest that oral rutaecarpine would change the intravenous pharmacokinetic characteristics of caffeine.
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대상 데이터
Specific pathogen-free male Sprague-Dawley rats (250-280 g) were obtained from the Orient Co. (Seoul, Korea). The animals were received at 6 weeks of age and were acclimated for at least one week.
이론/모형
The total area under the mean serum concentration-time curve from time zero to time infinity (AUClast) was calculated using the trapezoidal rule-extrapolation method for caffeine (Chiou, 1978). The area from the last datum point to time infinity was estimated by dividing the last measured plasma concentration by the terminal-phase rate constant.
성능/효과
, 2011). In the study, it was found that caffeine was rapidly converted to its three N-demethylated metabolites, which were also quickly transformed to further metabolites, when animals were pretreated with rutaecarpine, a CYP inducer. Further metabolism of three demethylated metabolites to others was supported by signifi cant induction of CYP1A2 and CYP2E1 by rutaecarpine (Lee et al.
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