摘要
对酮洛芬速溶颗粒剂进行了人体药物动力学研究。在体内试验中，选１０名健康受试者，采用交叉设计方案，以酮洛芬肠溶片为对照对颗粒剂做单剂量给药试验，建立了ＨＰＬＣ－ＵＶ法测定血浆中酮洛芬的浓度。结果显示，建立的酮洛芬血浆浓度测定方法，线性范围为０．５０～５０．０μｇ／ｍｌ，检测限为０．０６μｇ／ｍｌ。人体药动学结果显示：颗粒剂Ｔｍａｘ、Ｃｍａｘ及ＡＵＣ等主要药动学参数分别为０．５２ｈ，１３．６２μｇ／ｍｌ，２６．２９ｈ·μｇ／ｍｌ，肠溶片的相应参数分别为：３．３ｈ，６．５１μｇ／ｍｌ，２４．３２ｈ·μｇ／ｍｌ。与肠溶片比较，颗粒剂具有吸收速度快的特点。颗粒剂相对于肠溶片的生物利用度为１０６．４３％。经双单侧检验，属生物等效。
An HPLCUV method is established for determination of ketoprofen(KP) concentration in human plasma. The assay is performed using reverse phase chromatography, and naproxen serves as internal standard. The linearity range is from 0.50 to 50.0 μg/ml, and the limit of detection is 0.06 μg/ml. The method can meet the requirement of chromatographic analysis.A singledose crossover design is used for pharmacokinetic study. KP fastdissolved granules (50 mg) and commercial KP entericcoated tablets(50 mg) serve as test and standard samples, respectively. It is suggested that the kinetics of KP in vivo fitted twocompartment model, and the halflife is about 2.6 h. The main pharmacokinetic parameters of KP fastdissolved granules are Tmax=0.52 h, Cmax=13.62 μg/ml, AUC=26.29 h· μg/ml, and that of KP entericcoated tablets are Tmax=3.3 h, Cmax=6.51 μg/ml ,AUC=24.32 h· μg/ml. The relative bioavailability of KP fastdissolved granules is 106.43%,compared with KP entericcoated tablets. The statistical analysis, two onesided test, is performed to the AUC ,and it is found that the two formulations are bioequivalent.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1998年第2期105-108,共4页
Journal of China Pharmaceutical University
