尼群地平缓释胶囊在家犬体内的药动学与相对生物利用度  

Pharmacokinetics and relative bioavailability of sustained-release nitrendipine capsules in healthy dogs

作　　者：杨明世[1] 崔福德[1] 岳鹏[1] 任睽睽[1] 高鹏[1] 范玉玲[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2003年第2期84-87,共4页Journal of Shenyang Pharmaceutical University

基　　金："九五"国家重点科技攻关项目 (96-90 2 -0 2 -1 5 )

摘　　要：目的研究尼群地平缓释胶囊在家犬体内的药代动力学与相对生物利用度。方法用高效液相色谱法测定了 6条健康家犬口服尼群地平缓释胶囊 (受试制剂 )和尼群地平普通片 (参比制剂 )后不同时间点血浆中尼群地平的浓度 ,绘制血药浓度 -时间曲线 ,计算药代动力学参数及相对生物利用度。结果受试犬口服含尼群地平 4 0mg的受试制剂和参比制剂后 ,血浆中尼群地平的tmax分别为 (6 1 7± 1 60 )和 (1 4 6± 0 5 1 )h;cmax分别为 (3 4 3 8± 1 2 2 6)和 (45 6 5± 1 0 7 4 )nmol L ;用梯形法计算 ,AUC0～t分别为 (1 93 0 1± 1 0 0 5 1 0 6)和 (1 790 8± 94 2 8)nmol·h L。以AUC计算 ,与参比制剂相比 ,受试制剂中尼群地平的相对生物利用度平均为 (1 1 0 5 9± 2 3 60 ) %。将AUC0～t经对数转换后进行方差分析 ,结果表明 ,受试制剂与参比制剂相比 ,除个体间外 ,周期间与制剂间无显著性差异 (P >0 0 5 ) ,受试制剂AUC0～t的 90 %置信区间为参比制剂的 88 5 4 %～ 1 3 1 93 %。结论尼群地平缓释胶囊与国外普通片相比 ,在犬体内具有更长的作用时间 。Objective To study the pharmacokinetics and relative bioavailability of the sustained-release nitrendipine capsules in healthy dogs.Methods Following oral administration of a single dose of the sustained-release nitrendipine capsules (test formulation) and conventional tablets (reference formulation) to each of the 6 healthy dogs in a randomized crossover design,the plasma levels of the active drugs at different time points were determined by HPLC and the plasma concentration-time curves of these formulations were obtained.The pharmacokinetic parameters as well as the relative bioavailability were analyzed.Results The t max values of the test formulation and reference formulation are(6.17±1.60) and (1.46±0.51)h,the c max values are (343.8±122.6) and (456.5±107.4)nmol/L, and the AUC 0～t are ( 1 930.12± 1 005.106) and ( 1 790.8±942.8)nmol·h/L,respectively.The relative bioavailability of the test formulation was found to be (110.59±23.60)% compared with the reference formulation.The results of the variance analysis show that there is no significant difference between the test and reference formulation in periods and formulations (P>0.05),but in subjects.The 90% confidence interval of AUC 0～t of the test formulation is 88.54%～131.93% compared with the reference formulation.Conclusions Compared with the conventional tablets,the sustained-release nitrendipine capsules have longer action time in dogs and similar relative bioavailability.

关 键 词：尼群地平 缓释胶囊 药代动力学 相对生物利用度 

分 类 号：R945[医药卫生—微生物与生化药学]