替米沙坦胶囊正常人体相对生物等效性研究  

Study on Relative Bioequiavailability of Telmisartan Capsules in Healthy Subjects

作　　者：刘江[1] 杨鸿[2] 邝翠仪[3] 刘志林[4] 

机构地区：[1]河北医科大学第四附属医院药剂科,石家庄市050011 [2]中山大学附属第二医院药剂科,广州市510120 [3]中山大学附属第一医院药剂科,广州市510080 [4]广东外语外贸大学门诊部,广州市510420

出　　处：《中国药房》2006年第10期761-763,共3页China Pharmacy

摘　　要：目的:研究替米沙坦胶囊正常人体相对生物等效性。方法:20名健康男性志愿受试者单剂量随机交叉口服替米沙坦胶囊(受试制剂)或替米沙坦片(参比制剂)80mg,采用高效液相色谱法测定血药浓度,以3p97程序计算药动学参数和相对生物等效性。结果:受试制剂与参比制剂在体内血药浓度均呈二室模型,tmax分别为(2.08±1.64)、(2.02±0.86)h,Cmax分别为(2.10±1.36)、(1.95±1.08)μg/ml,AUC0～t分别为(116.25±55.97)、(123.94±65.66)(μg·h)/ml,t1/2β分别为(74.23±25.11)、(79.18±23.27)h。经配对t检验,受试制剂与参比制剂药动学参数无显著性差异(P>0.05),受试制剂相对于参比制剂的生物利用度为(93.80±12.24)%。结论:2种制剂具有生物等效性。OBJECTIVE： To study the relative bioequiavailability of telmisartan in healthy subjects. METHODS： A single dose of 80rag of telmisartan capsule （experimental preparation） or tablet（ reference preparation） was administered orally to 20 healthy male volunteers in a randomized crossover way and the plasma concentrations of telmisartan were determined by HPLC. The pharmacokinetic parameters and relative bioequiavailability were calculated with 3p97 pharmacokinetic program. RESULTS： The concentration curves of both experimental and reference preparation fitted twocompartment model. The peak time （tmax） Of capsule and tablet were （2.08± 1.64） h and （2.02± 0.86） h, respectively; the peak plasma levels （Cmax） were（2.10± 1.36）μg/ml and （1.95±1.08）μg/ml, ;AUC0-t were （116.25± 55.97）（μg· h）/ml and （123.94± 65.66）（μg · h）/ ml; half - life time（ t 1/2β） were （74.23 ± 25.11） h and （79.18 ± 23.27） h, respectively. No significant difference was found in pharmacokinetic parameters between two preparations by paired t test（P 〉0.05）. The relative bioavailability of experimental preparation vs. reference preparation was （93.80 ± 12.24）%. CONCLUSION： Telmisartan capsule has the same bioequiavailability with telmisartan tablet.

关 键 词：替米沙坦 生物等效性 药动学参数 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]