摘要
目的建立测定兔血清中比卡鲁胺浓度的方法,研究比卡鲁胺在兔体内的药动学特征。方法以乙腈沉淀法对血样进行预处理,采用YMC-Pack ODS-A色谱柱(250 mm×4. 6 mm,5μm);流动相为0. 1%磷酸二氢钾缓冲液-乙腈(50∶50),流速1. 0 mL·min-1,检测波长210 nm,柱温30℃。6只新西兰大白兔分别灌胃比卡鲁胺50 mg,于不同时间点采集血样,HPLC法检测比卡鲁胺血药浓度。采用DAS药动学软件计算药动学参数。结果比卡鲁胺浓度在0. 05～5mg·L-1内线性良好(r=0. 999 3);低、中、高3种浓度的回收率为99. 71%、97. 04%和99. 95%; 3种浓度的日内、日间精密度的RSD(n=5)分别为4. 58%、2. 81%、2. 64%和7. 53%、4. 07%、3. 61%。比卡鲁胺在兔体内的AUC0→∞、MRT0→∞、t1/2z、ρmax和CLz/F分别为(175. 39±16. 64) mg·h·L-1、(62. 82±3. 09) h、(48. 67±5. 51) h、(2. 85±0. 34) mg·L-1和(0. 287±0. 026) L·h-1。结论本方法灵敏度高、特异性好,可用于兔血清样品中比卡鲁胺的含量测定;比卡鲁胺在兔体内药动学特征符合非房室模型。
AIM To establish an HPLC method for the determination of bicalutamide concentration and tostudy its pharmacokinetic characteristics in rabbits. METHODS The serum samples were pretreated by acetoni-trile precipitation method. YMC-Pack ODS-A chromatographic column( 250 mm ×4. 6 mm,5 μm) was used and themobile phase consisted of 0. 1% potassium dihydrogen phosphate-acetonitrile( 50 ∶ 50) with a flow rate of 1. 0mL·min^-1 ,the detection wavelength was set at 210 nm and the temperature of the column was controlled at 30℃.A total of 6 New Zealand white rabbits were administered with bicalutamide 50 mg respectively,blood samples weretaken at different time points and HPLC was used to detect the concentration of bicalutamide. The pharmacokineticparameters were calculated by DAS pharmacokinetic software. RESULTS The calibration curve was linear with-in the range of 0. 05 to 5 mg·L^-1 ( r =0. 999 3) . The recovery rate for three concentration of bicalutamide was99. 71%,97. 04% and 99. 95% respectively. Intra-day RSD and inter-day RSD( n =5) were lower than 5%. TheAUC 0→∞ ,MRT 0→∞ ,t 1/2 z,ρ max and CLz/F of bicalutamide in rabbits were ( 175. 39 ± 16. 64) mg·h·L^-1 ,( 62. 82 ±3. 09) h,( 48. 67 ±5. 51) h,( 2. 85 ± 0. 34) mg·L^-1and ( 0. 287 ± 0. 026) L·h^-1respectively.CONCLUSION The method has high sensitivity and good specificity,and can be used for the determination of bi-calutamide in rabbit serum samples. The pharmacokinetic characteristics of bicalutamide in rabbits are consistentwith non-compartmental model.
作者
楼永海
管咪咪
梁小龙
李晔
杨徐一
LOU Yonghai;GUAN Mimi;LIANG Xiaolong;LI Ye;YANG Xuyi(Department of Pharmacy,Taizhou Hospital ofZhejiang Province,Taizhou 317000,China)
出处
《中国临床药学杂志》
CAS
2018年第6期387-390,共4页
Chinese Journal of Clinical Pharmacy
基金
台州市科技计划项目(编号1201ky08)
