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目的研究盐酸阿比朵尔在大鼠体内的药代动力学。方法将健康♂Wistar系大鼠(200～220 g),随机分组,每组6只。单次灌胃给予药物,剂量分别为9、18、54 mg.kg-1,从眼眶静脉丛分时取血、处理。采用高效液相色谱-质谱联用方法测定药物在血浆中的浓度,应用DAS 2.0软件计算主要药代动力学参数。结果按9、18、54 mg.kg-13个剂量分别单次灌胃给予大鼠盐酸阿比朵尔后,药物在动物体内的Cmax分别为644.1、1002、4711μg.L-1;Tmax分别为0.35、0.28、0.18 h;AUC0-t分别为1127、1956、6790μg.h.L-1;AUC0-∞分别为1250、2224、7558μg.h.L-1;T12分别为3.2、3.6、3.3 h。结论以上数据经统计学分析,结果表明:在9～54 mg.kg-1剂量范围内,单剂量灌胃给予大鼠盐酸阿比朵尔后,药物在动物体内的动力学行为具有线性特征。
Objective To study the pharmacokinetics of abildom hydrochloride in rats. Methods Healthy ♂ Wistar rats (200 ~ 220 g) were randomly divided into 6 groups. A single oral administration of drugs, the dose was 9,18,54 mg.kg-1, respectively, from the orbital venous plexus bleeding, treatment. The concentration of drug in plasma was determined by HPLC-MS method. The main pharmacokinetic parameters were calculated by DAS 2.0 software. Results After intragastric administration of 9,18 and 54 mg.kg-13 doses of abiraterone hydrochloride, the Cmax values of the drugs in vivo were 644.1, 1002 and 4711 μg.L-1, respectively, and the Tmax were 0.35 , 0.28 and 0.18 h respectively; AUC0-t were 1127, 1956 and 6790 μg.hL-1; AUC0-∞ were 1250, 2224 and 7558 μg.hL-1, respectively; Conclusion The above data were statistically analyzed. The results showed that the pharmacokinetic behavior of the drug in rats was linear with the dose of 9-54 mg · kg-1.