摘要
目的研究劳拉西泮片(镇静药)在中国健康人体的药代动力学和生物等效性。方法健康志愿者20名,随机双交叉单剂量口服试验和参比制剂劳拉西泮片3mg;于服药后48h内,抽取静脉血;用高效液相色谱法测定血浆中劳拉西泮浓度;用3P97药代动力学程序计算相对生物利用度并评价2种制剂生物等效性。结果劳拉西泮的药代动力学参数Cmax分别为(35.77±6.84),(36.95±4.60)μg·L-1;tmax分别为(2.38±0.56),(2.23±0.48)h;t1/2(Ke)分别为(13.72±2.07),(13.83±2.49)h;AUC(0-48)分别为(542.19±84.33),(527.53±63.52)ng·h·mL-1;AUC(0-inf)分别为(605.22±93.52),(599.37±71.56)ng·h·mL-1。试验制剂与参比制剂的相对生物利用度F=(103.5±15.9)%。结论2种制剂具有生物等效性。
Objective To study the pharmacokinetics and bioequivalence of lorazepam tablets in Chinese healthy volunteers. Methods Twenty Chinese healthy male volunteers were involved in the study. Each subject received a single dose of 3 mg lorazepam test or reference formulation with a randomised crossover study. Blood sampling was conducted consequently within 48 hours. The plasma lorazepam concentration were deternlined by HPLC. The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by 3P97 program. Results After a single dose of 3 mg tested or reference formulation, the pharmacokinetic parameters of lorazepam were as follows： Cmax were （35.77 ±6.84） and （36.95 ± 4.60） μg · L^-1; tmax were （2.38 ± 0.56） and（ 2.23 ± 0.47） h; t1/2 were （13.72 ±2.07） and （13.83 ±2.49） h; AUC（0-48） were （542.19 ± 84.33） and （527.53 ± 63.52） ng·h·mL^-1; AUC（0-inf） were （605.22 ±93.52） and（ 599.37 ±71.56） ng·h·mL^-1 for test and reference formulation respectively. The relative bioavailability of tested formulation to reference formulation was F = （ 103.5 ± 15.9 ） %. Conclusion The two formulations were bioequivalence.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2006年第2期134-137,共4页
The Chinese Journal of Clinical Pharmacology
