兰索拉唑片相对生物利用度与生物等效性研究

Study on the relative bioavailability and bioequivalence of lansoprazole tablets

目的研究兰索拉唑片与兰索拉唑肠溶胶囊的人体相对生物利用度和生物等效性。方法健康志愿者24例,随机交叉单剂量口服兰索拉唑片与兰索拉唑胶囊,剂量均为30 mg,洗脱期1周。分别于服药后12 h内多点抽取静脉血,高效液相色谱法测定血浆兰索拉唑浓度。计算主要药动学参数及相对生物利用度,并评价两种制剂生物等效性。结果单剂量口服兰索拉唑片与兰索拉唑肠溶胶囊后血浆中兰索拉唑Cmax分别为（949.8±329.0）和（973.2±322.2）ng/mL;tmax分别为（2.44±0.52）和（2.06±0.70）h;t1/2分别为（1.97±1.12）和（1.84±1.11）h;AUC0→12分别为（3 054±2 019）和（2 911±1 818）ng.h/mL;AUC0→∞分别为（3 398±2 825）和（3 106±2 138）ng.h/mL。Cmax、AUC0→12和AUC0→∞的90%可信区间分别为90.7%~104.0%,94.0%~110.8%和94.9%~112.2%。以AUC0→12计算,兰索拉唑片的相对生物利用度为（105.0±24.6）%。结论兰索拉唑片与兰索拉唑肠溶胶囊具有生物等效性。

Purpose To study the relative bioavailability and bioequivalence of lansoprazole tablets and lansoprazole enteric capsules in human plasma.Methods 24 healthy volunteers in randomized crossover study were given a single oral dose of 30 mg of the test or of the reference.12 h later,blood was taken out at several time points.The plasma level of lansoprazole was determined by HPLC.The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS2.1 program.Results Cmax of the test formulation and the reference one were(949.8±329.0) and(973.2±322.2) ng/mL,tmax were(2.44±0.52) and(2.06±0.70) h,t1/2 were(1.97±1.12) and(1.84±1.11)h,AUC0→12 were(3 054±2 019) and(2 911±1 818) ng·h/mL,AUC0→∞ were(3 398±2 825) and(3 106±2 138) ng·h/mL,respectively.The 90% confidential interval of Cmax,AUC0→12 and AUC0→∞ of the test were 90.7%-104.0%,94.0%-110.8% and 94.9%-112.2%,respectively.The relative bioavailability was(105.0±24.6)% for the test and reference preparation.Conclusion These two formulations are bioequivalent.