摘要
本研究是通过８名中国健康受试者对国产克拉霉素胶囊和颗粒剂与进口片剂进行人体药代动力学和相对生物利用度试验。血药浓度测定采用生物检定法。结果片剂、胶囊和颗粒剂三种制剂的药时曲线符合一房室模型，主要药代动力学参数分别为：Ｃｍａｘ２．２４±０．５３，２．０９±０．５６，２．５８±０．５８ｍｇ·Ｌ－１；Ｔｍａｘ１．７２±０．７３，２．１４±０．９７，０．６８±０．２０ｈ；Ｔ１／２４．９６±０．５１，４．５９±０．８９，４．７８±０．６７ｈ；药时曲线下面积ＡＵＣ０－ｔ平均值：１９．３９±３．１４，１８．４５±４．１２，１８．８２±２．９１ｍｇ·ｈ·Ｌ－１；相对生物利用度为：胶囊９２．４８±１６．５０％，颗粒剂１０１．３４±１６．２６％。试验结果经统计学处理均证明：受试的克拉霉素胶囊和颗粒剂与对照制剂为生物等效制剂。
The pharmacokinetics and bioavaiolability of clarithromycin were assessed in 8 Chinese healthy young volunteers after a single oral dose (500 mg). Plasma clarithromycin concentrations were determined using microbiologic assay. The plasma concentration-time curves of clarithromycin tablet, capsule and graunle fitted to a one-compartment open model with a first order absorption. The peak plasma levels(Cmax) averaged 2.24± 0.53, 2.09±0.56 and 2.58±0.58 mg·L-1 at 1.72±0.73,2.14±0.97 and 0.68±0.20 h , and the mean terminal elimination half-lives (T1/2) were 4.96±0.51, 4.59±0.89 and 4.78±0.67 h , respectively . The areas under the plasma concentration-time curve (AUC) were 19.39±3.14 , 18.45±4.12 and 18.82±2.91 mg·h·L-1 , respectively. The relative bioavaiolabilities of clarithromycin capsules and graunles compared with tablets were 92.48±16.50% and 101.34±16.26% respectively . The results showed that the three preparations were bioequivalent .
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1998年第2期94-98,共5页
The Chinese Journal of Clinical Pharmacology
关键词
克拉霉素
胶囊
颗粒剂
药代动力学
生物利用度
clarithromycin
pharmacokinetic
bioavaiolability
microbiologic assay
