摘要
目的：研究二氟尼柳分散片的人体药动学及生物等效性。方法：采用随机交叉、自身对照试验设计，18名健康男性志愿者，随机等分成两组，每组9人，志愿者单剂量口服二氟尼柳分散片或普通片后，不同时间点取肘部静脉血4～5mL，血药质量浓度采用高效液相色谱（HPLC）法测定。由血药质量浓度计算药动学参数，主要药动学参数（AUC、Cmax）经对数转换后进行方差分析．以双单侧t检验及90％的可信区间进行生物等效性判定。结果：志愿者单次服用500mg二氟尼柳分散片或普通片后药动学参数AUC0-∞分别为（797．7±301．8）和（824．9±306．3）mg·h·L^-1，AUC0-∞分别为（1125．4±485．5）和（1160．7±501．8）mg·h·L^-1,Cmax分别为（55．5±16．4）和（57．2±17．4）mg·L^-1，tmax分别为（2．5±1．0和（2．6±1．2）h。相对生物利用度为（97．0±13．1）％。双单侧t检验证明分散片与普通片等效。结论：分散片的药动学与普通片的药动学统计学上无差异，且二者具有生物等效性。
OBJECTIVE To compare the pharmacokinetics and bioequivalence of diflunisal dispersible tablets with tablets in healthy volunteers. METHODS The plasma concentrations of diflunisal were assayed by high performance liquid chromatography （HPLC） after a single dose of 500 mg was given to 18 healthy volunteers in a two-period crossover study. RESULTS The characteristic of plasma concentration-time curve of diflunisal was fitted to one compartment model. The main pharmacokinetic parameters of diflunisal tablets and dispersible tablets were as follows： AUC0-∞（797. 7 ± 301.8） and （ 824. 9 ± 306. 3） μg·h·mL^-1 ,AUC0-∞（1 125.4±485.5） and （1160.7±501.8）mg·h·L^-1 ,Cmax（55.5±16.4 and 57.2±17.4）mg·L^-1 ,tmax（2.5±1.0） and （2. 6 ± 1.2）h. The relative bioavailability of diflunisal dispersible tablets was （97. 0 ± 13. 1 ） %. No statistical difference was found in AUC0-∞, AUC0-∞ and Cmax between two formulations. CONCLUSION The two formulations had similar pharmacokinetic characteristics and were bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2007年第2期196-198,共3页
Chinese Journal of Hospital Pharmacy
