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| 卡托普利生物黏附型缓释胶囊大鼠体内药动学研究 | |
| 引用本文： | 宋益民,于海鹏,周莉,宋世英,张学成.卡托普利生物黏附型缓释胶囊大鼠体内药动学研究[J].中国海洋大学学报(自然科学版),2010,40(4). |
| 作者姓名： | 宋益民 于海鹏 周莉 宋世英 张学成 |
| 作者单位： | 1. 青岛科技大学制药工程系,山东,青岛,266042;中国海洋大学生命学院,山东,青岛,266003 2. 青岛科技大学制药工程系,山东,青岛,266042 3. 中国海洋大学生命学院,山东,青岛,266003 |
| 基金项目： | 国家自然科学基金项目 |
| 摘 要： | 研究卡托普利生物黏附型缓释胶囊(Captopril/bioadhesive sustained-release capsules,CBSRCs)在大鼠体内的药动学,通过建立高效液相色谱(HPLC)-紫外检测法测定卡托普利(Captopril,Cap)的血药浓度,研究了大鼠灌胃CBSRCs和卡托普利普通片(Captopril ordinary tablet,COT)各5 mg/kg后16 h内的药动学,DAS 2.0软件计算出相应的药动学参数,t检验比较两种制剂的药动学参数。结果表明,Cap浓度在12.5～800μg/L范围内线性关系良好(r=0.998 7),最低检测限为12.5μg/L,平均回收率为99.40%,平均日内RSD为3.97%,平均日间RSD为4.84%;单剂量口服CBSRCs和COT,Tmax分别为(3.12±0.67),(1.53±0.27)h;Cmax为(722.97±133.68),(1 114.47±208.36)μg/L;T1/2α为(1.88±0.38),(1.15±0.21)h;T1/2β为(3.76±0.75),(2.87±0.59)h;CL为(2.87±0.51),(3.43±0.67)L/h,Vd为(10.98±1.90),(13.21±2.57)L;AUC0-t为(4 856.03±835.46),(4 616.29±915.49)μg.h/L;AUC0-∞为(5 218.39±1 037.58),(4 705.83±894.56)μg.h/L。CBSRCs和COT相比,T1/2α,T1/2β,AUC0-t,AUC0-∞,CL,Vd,Tmax,Cmax差异显著(P0.05或0.01)。说明CBSRCs与市售COT在大鼠体内的药动学特征差异具有显著性,说明高效液相色谱-紫外检测器测定Cap含量的方法稳定,结果准确可靠。CBSRCs与市售COT相比,CBSRCs显著改善了卡托普利原药的药动学性质,具有缓释和长效的作用。 |
| 关 键 词： | 卡托普利 生物黏附型缓释胶囊 药代动力学 高效液相色谱 |
Pharmacokinetic Study of Captopril/Bioadhesive Sustained-Release Capsules in Rats |
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| SONG Yi-Min,YU Hai-Peng,ZHOU Li,SONG Shi-Ying,ZHANG Xue-Cheng.Pharmacokinetic Study of Captopril/Bioadhesive Sustained-Release Capsules in Rats[J].Periodical of Ocean University of China,2010,40(4). | |
| Authors: | SONG Yi-Min YU Hai-Peng ZHOU Li SONG Shi-Ying ZHANG Xue-Cheng |
| Institution: | SONG+Yi-Min1,2,YU+Hai-Peng1,ZHOU+Li1,SONG+Shi-Ying1,ZHANG+Xue-Cheng2(1.Department+of+Pharmaceutical+Engineering,Qingdao+University+of+Science+%26+Technology,Qingdao+266042,China,2.College+of+Life+Science,Ocean+University+of+China,Qingdao+266003,China) |
| Abstract: | For the purpose of investigating the pharmacokinetics of captopril/bioadhesive sustained-re-lease capsules(CBSRCs),An HPLC process with UV detection was established for the determination of plasma concentration of captopril in rats.After CBSRCs and Captopril ordinary tablet(COT) were orally administrated to rats at a single dosage of 5 mg/kg respectively,their pharmacokinetic behaviors in 16 h were examined.The pharmacokinetics parameters were calculated and analyzed by DAS 2.0 software.Linear calibration c... |
| Keywords: | captorpril bioadhesive sustained-release capsules pharmacokinetics HPLC |
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