国产四环格列齐特片在健康人体内的药物动力学及相对生物利用度

PHARMACOKINETICS AND RELATIVE BIOAVAILABILITY OF GLICLAZIDE TABLET IN HEALTHY VOLUNTEERS

10名健康志愿者随机自身交叉单次po国产被试格列齐特片80mg和国产标准参比格列齐特片80mg后,应用高效液相色谱法测定血浆格列齐特浓度.格列齐特在健康人体内的血药浓度-时间过程符合二室模型.被试格列齐特片的药物动力学参数分别为:T_(1/2ka)=1.01±0.67h,T_(1/2β)=4.81±1.91h,T_(max)=3.32±0.92h,C_(max)=4.20±1.77μg/ml,AUC=45.89±22.98(μg·h)/ml.参比格列齐特的药物动力学参数分别为:T_(1/2Ka)=0.84±0.42h,T_(1/2β)=6.30±3.22h,T_(max)=3.28±0.79h,C_(max)=3.68±1.89μg/ml,AUC=41.42±19.35(μg·h)/ml.两种格列齐特片剂的各项药物动力学参数经3P87程序及统计学分析处理,被试格列齐特片对标准参比格列齐特片的相对生物利用度为107%.

Serum levels of gliclazide following a single oral dose of 80mg Beijing-made (SiHuan) gliclazide tables and standard reference gliclazide tablets in 10 Chinese healthy vol-unteers were measured by HPLC and the pharmacokinetics and the relative bioavailability of the tablets were studied. Two compartment model with first-order absorption and elimination was fitted to the concentration-time profiles of the two formulations. The Pharmacokinetic parameters of the Beijing-made and standard tablets were as following :T_(1/2k_a) = (1.01±0.67) h,T_(1/2β)=(4.81±1.91)h,T_(max)= (3.32±0. 92)h,C_(max)= (4.20±1.77)μg/ml,AUC=(45.89±22.98)(μg·h)/ml,and T_(1/2k_a)=(0.84±0.42)h,T_(1/2β)=(6.30+3.22)h,T_(max)= (3.28±0.79) h,C_(max)=(3.68±1.89)μg/ml, AUC=(41.42±19.35)μg·h)/ml respectively. The relative bioavailability of Beijing-made gliclazide tablet was 107%.