尼索地平缓释胶囊的人体药动学及生物等效性研究  

Pharmacokinetics and Bioequivalence of Nisoldipine Sustained-release Capsules in Healthy Volunteers

作　　者：张华峰[1] 宋青[1] 戴博 王健康[1] 

机构地区：[1]解放军空军总医院药学部,北京100142

出　　处：《中国药房》2013年第38期3607-3609,共3页China Pharmacy

摘　　要：目的:建立测定人血浆中尼索地平浓度的方法,研究国产尼索地平的药动学特征及生物等效性。方法:18名男性健康受试者分别单剂量和多剂量口服尼索地平30 mg的受试制剂(缓释胶囊)和参比制剂(片剂),血样处理后采用高效液相色谱法进样测定。计算药动学参数并评价其生物等效性。结果:尼索地平缓释胶囊单剂量和多剂量口服后体内过程均符合二房室模型,主要药动学参数分别为:cmax(12.07±3.96)、(10.68±3.61)ng/ml,t1/2β(12.72±3.13)、(15.61±2.88)h,AUC0-24 h(52.54±16.71)、(70.81±15.81)ng·h/ml,平均相对生物利用度分别为(101.88±18.63)%、(93.37±19.17)%。结论:尼索地平缓释胶囊与普通片剂经单剂量、多剂量给药后,其AUC0-∞、AUC0-24 h为生物等效,而cmax、tmax不具生物等效性。OBJECTIVE： To establish a method for the determination of nisoldipine in human plasma, and to study the pharma- cokinetics and bioequivalence of domestic nisoldipine in healthy volunteers. METHODS： Single dose and multi-doses of test and reference preparation of 30 mg of nisoldipine were given to 18 male healthy volunteers orally. The content of nisoldipine in blood samples was determined by HPLC after treated. Pharmacokinetic parameters were calculated and bioequiavailability was evaluated. RESULTS： The pharmacokinetics of Nisoldipine sustained-release capsule was fitted with two-compartment open model after single dose or multiple dose administration. Main pharmacokinetic parameters were as follows： Cmax were （12.07 ± 3.96） ng/ml and （10.68± 3.61） ng/ml; t1/2β were （12.72 ± 3.13）h and （15.61 ± 2.88）h; AUC0-24h were （52.54 ± 16.71） ng.h/ml and （70.81 ± 15.81） ng. h/ml; relative bioavailability were （101.88 ±18.63） % and （93.37 ± 19.17） %, respectively. CONCLUSIONS： The AUC0-∞ and AUC0-t of the two kinds of dosage forms are proved to be bioequivalent, but the cmax and Cmax are not bioequivalent.

关 键 词：尼索地平 药动学 生物等效性 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学] R972.4[医药卫生—药学]