青木香及冠心苏合丸中马兜铃酸-Ⅰ和-Ⅱ在大鼠血清的药代动力学研究

摘要

The pharmacokinetic parameters of aristolochic acid-Ⅰ (AA-Ⅰ) and-Ⅱ (AA-Ⅱ) in rat serum after intragastrical administration of the crude drug powders of Radix Aristolochiae (RA) and Muskone containing equal amounts of RA were compared. The phar-macokinetic profiles of AA-Ⅰ and AA-Ⅱ could be fitted with a two-compartment model. The elimination half time (T1/2β) of AA-Ⅰ in Muskone was 1573.2 min and that of AA-Ⅰ in RA was 475.8 min; T1/2β of AA-Ⅱ in Muskone was 2344.8 min and that of AA-Ⅱ in RA was 427.8 min. The area under the concentration-time curve (AUC) of AA-Ⅰ in Muskone was 13.07 μg/h/mL and that of AA-Ⅰ in RA was 3.86 μg/h/mL; AUC of AA-Ⅱ in Muskone was 67.67 μg/h/mL and that of AA-Ⅱ in RA was 23.93 μg/h/mL. The bioavailabilities of AA-Ⅰ and AA-Ⅱ in Muskone were markedly increased compared with that in RA based on the elimination half-time and AUC values.%比较了大鼠分别灌胃给予青木香生药混悬液和含有等量青木香的冠心苏合丸生药混悬液后马兜铃酸-Ⅰ(AA-Ⅰ)和-Ⅱ(AA-Ⅱ)在大鼠血清的药代动力学参数.AA-Ⅰ和AA-Ⅱ在大鼠血清中的浓度变化情况符合血管外给药二室模型.灌胃给药冠心苏合丸和青木香后AA-Ⅰ的消除半衰期分别为1573.2 min和475.8 min;AA-Ⅱ的消除半衰期分别为2344.8 min和427.8 min.AA-Ⅰ的曲线下面积分别为13.07μg/h/mL和3.86 μg/h/mL;AA-Ⅱ的曲线下面积分别为67.67μg/h/mL和23.93μg/h/mL.研究结果表明,与单独灌胃给药青木香相比,灌胃冠心苏合丸后大鼠血清中AA-Ⅰ和AA-Ⅱ的消除半衰期明显延长,药时曲线下面积明显增加.