摘要
为了观察西替利嗪胶囊和片剂的生物等效性，１０名健康志愿者随机交叉单次口服西替利嗪胶囊或片剂２０ｍｇ后，用反相高效液相色谱－紫外（ＨＰＬＣ－ＵＶ）检测法定时测定３６ｈ内血浆浓度。根据房室拟合，其体内过程符合二室模型。国产西替利嗪胶囊主要药代动力学参数分别为Ｔ１／２β：９．７３±０．６３ｈ；Ｃｍａｘ：５９１．７±７７．０μｇ·Ｌ－１；Ｔｍａｘ：１．０５±０．４９ｈ；ＭＲＴ：１２．１０±１．６５ｈ；ＡＵＣ０－３６：５１４１．７±６８８．４μｇ·ｈ·Ｌ－１；西替利嗪胶囊对西替利嗪片剂的相对生物利用度（Ｆ％）为１０１．９８±７．５４。两种制剂各参数经配对Ｔ检验Ｐ＞０．０５，均无显著差异。两者的ＡＵＣ（ｌｎＡＵＣ）、Ｃｍａｘ（ｌｎＣｍａｘ）及ＭＲＴ（ｌｎＭＲＴ）经方差分析法和双单侧ｔ检验法等分析，证明国产西替利嗪胶囊与进口西替利嗪片剂具有生物等效性。
The pharmacokinetics and bioavailability of cetirizine capsules(test) and tablets (reference) have been studied in 10 healthy male volunteers. A single dose of 20 mg cetirizine hydrochloride was given according to a randomized two_way cross_over design. A reverse phase HPLC-UV method was used to determine cetirizine concentrations in plasma over 36 h. The main pharmacokinetic parameters of test drug were as follows: T1/2β 9.73±0.63 h, Cmax 591.0±77.0 μg·L-1, Tmax 1.05±0.44 h, MRT 12.10±1.65 h, AUC0-36 5141.7±688.4 μg·h·L-1. There was no significant difference between pharmacokinetic parameters of two preparations (P>0.05). Relative bioavailability of test drug was 101.98±7.54 %, indicating a excellent bioequvalence of domestic cetirizine compared to imported one.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1999年第4期266-269,共4页
The Chinese Journal of Clinical Pharmacology
