Enhanced bioavailability of paclitaxel by bamboo concentrate administration

被引:3
作者
Kang, KW [1 ]
Choi, JS [1 ]
机构
[1] Chosun Univ, Coll Pharm, Kwangju 501759, South Korea
关键词
bamboo concentrates; paclitaxel; pharmacokinetic; bioavailability; CYP3A4;
D O I
10.1007/BF02977678
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The purpose of this study was to investigate the effect of a cotreatment of bamboo concentrates (Jukcho solution; 0.75, 1.5, and 3.0 mL/kg) with the chemotherapeutic agent paclitaxel on the bioavailability of orally administered paclitaxel (50 mg/kg) in rats. The effect of a pretreatment of bamboo concentrates (1.5 and 3.0 mL/kg for 1.0 h or a consecutive 3 day) was also examined. The paclitaxel plasma concentrations of rats orally administered paclitaxel plus bamboo concentrates (coadministration, 3.0 mL/kg and pretreatment, 1.5 and 3.0 mL/kg) were significantly higher than those of rats treated with paclitaxel alone. Plasma concentrations of paclitaxel in groups pretreated with bamboo concentrates for 3 day were markedly higher than those of a paclitaxel control group at the measured time points. The areas under plasma concentration-time curves (AUCs) of paclitaxel in groups pretreated with bamboo concentrates were elevated and the absolute bioavailability (AB%) and relative bioavailability (RB%) of paclitaxel were also significantly higher than those in the control group. The peak concentration (C-max), half-life (t(1/2)), and the elimination rate constant (K-el) of paclitaxel after 3 day of pretreatment with bamboo concentrates were also significantly higher than those in the control, but the time required to reacn the maximum plasma concentration (T-max) of paclitaxel was unaffected by the bamboo concentrates. Western blot analyses demonstrated that the level of CYP3A4 was increased in the livers of rats treated orally with paclitaxel, but this was reversed by pretreating with bamboo concentrates. These results show that bamboo concentrates enhance the bioavailability of orally administered paclitaxel and this effect may be associated with a diminished expression of CYP3A4 in the liver.
引用
收藏
页码:469 / 475
页数:7
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