阿奇霉素分散片对比卡鲁胺片在兔体内药动学的影响

Effects of Azithromycin Dispersible Tablets on the Pharmacokinetics of Bicalutamide Tablets in Rabbits

目的:研究阿奇霉素分散片对比卡鲁胺片在兔体内药动学的影响。方法:12只新西兰大白兔随机分为试验组和对照组,每组6只。试验组予以比卡鲁胺片50 mg灌胃,对照组予比卡鲁胺片50 mg+阿奇霉素分散片250 mg灌胃,于不同时间点采集血样。HPLC检测比卡鲁胺血药浓度,计算药动学参数后进行统计分析。结果:试验组和对照组AUC_((0-∞))分别为(99.66±23.72)和(83.13±6.92)mg·h·L^(-1),MRT_((0-∞))分别为(56.94±5.55)和(44.91±4.97)h,t_(1/2)分别为(60.81±21.16)和(52.82±23.82)h,C_(max)分别为(2.40±0.56)和(2.15±0.35)mg·L^(-1),CLz/F分别为(0.51±0.12)和(0.61±0.05)L·h^(-1)。两组AUC_((0-∞))、t_(1/2)z、C_(max)和CLz/F比较,差异均无统计学意义(P>0.05);两组MRT_((0-∞))比较,差异有统计学意义(P<0.05)。结论:阿奇霉素会延长兔体内比卡鲁胺的平均驻留时间,在临床使用过程中应注意避免药物在体内蓄积而影响治疗质量。

Objective:To study the effects of azithromycin dispersible tablets on the pharmacokinetics of bicalutamide tablets in rabbits.Methods:Totally 12 New Zealand white rabbits were randomly divided into test group and control group with 6 rabbits in each group.The test group was given bicalutamide tablets 50 mg by gavage,and the control group was given bicalutamide tablets 50 mg+azithromycin dispersible tablets 250 mg by gavage.Blood samples were collected at different time points.The blood concentration of bicalutamide was detected by HPLC,and the pharmacokinetic parameters were calculated for statistical analysis.Results:The AUC_((0-∞))of the test and control groups were(99.66±23.72)and(83.13±6.92)mg·h·L^(-1),MRT_((0-∞))were(56.94±5.55)and(44.91±4.97)h,t_(1/2)were(60.81±21.16)and(52.82±23.82)h,C_(max)were(2.40±0.56)and(2.15±0.35)mg·L^(-1),CLz/F were(0.51±0.12)and(0.61±0.05)L·h^(-1),respectively,and the AUC_((0-∞)),t_(1/2),C_(max)and CLz/F showed no statistically significant differences(all P>0.05),while the MRT_((0-∞))was with statistically significant difference(P<0.05).Conclusion:Azithromycin can prolong the average residence time of bicalutamide in rabbits.In the process of clinical use,attention should be paid to avoiding drug accumulation in body and affecting the quality of treatment.