氯雷他定片人体药动学及生物等效性研究

Pharmacokinetics and Bioequiavailability of Loratadine Tabletes in Healthy Volunteers

目的:评价2种氯雷他定片在健康人体内的生物等效性。方法:采用双周期自身对照交叉试验设计,20名健康志愿者按体重配对随机分为A、B组,分别单剂量口服40mg受试制剂与参比制剂,采用固相萃取-高效液相色谱法测定血浆中氯雷他定浓度。结果:参比制剂与受试制剂的Cmax分别为(17.00±3.90)、(18.41±2.58)μg.L-1,tmax分别为(1.06±0.25)、(0.93±0.20)h,t1/2ke分别为(1.34±0.38)、(1.08±0.38)h,AUC0～∞分别为(37.41±17.38)、(36.38±16.73)μg.h.L-1,AUC0～8分别为(35.11±15.72)、(34.76±15.34)μg.h.L-1。受试制剂相对于参比制剂的生物利用度为(99.0±18.7)%,经方差分析、双单侧t检验均无显著性差异。结论:2种氯雷他定片生物等效。

OBJECTIVE： To evaluate the bioequiavailability of two kinds of loratadine tabletes in Chinese healthy volunteers. METHODS： A single oral dose 40 mg of two loratadine preparations （reference and test preparations） was given to 20 volunteers （whom were divided into two groups） in a randomized cross - over study. The concentration of loratadine in plasma was determined by solid phase extraction-HPLC. RESULTS： The main pharmacokinetie parameters of reference and test preparations were as follows： C were （17.00±3.90） and （18.41±2.58）μg·L^1;tmax were （1.06±0.25） and （0.93±0.20） h; t 1/2kc were （1.34±0.38） and （1.08±0.38） h; AUC0-∞ were （37.41± 17.38） and （36.38±16.73）μg·h ·L^-1; AUC0-8 were （35.11±15.72） and （34.76±15.34）μg·h ·L^-1 respectively. The relative bioavailability of the test preparation was （99.0±18.7） % as against .the reference preparation, and no significant differences was noted for the two formulations in ANOVA and two-one side t test. CONCLUSION： The two formulations were bioequivalent.