【摘要】 目的 :研究国产西那普利片在人体的药动学和相对生物利用度。方法 :采用随机交叉试验设计 ,12名健康男性志愿者单剂量西那普利片试验品与参比品各 2 5mg,po ,以放射酶学分析法对血浆中活性代谢产物西那普利拉进行定量测定。结果 :试验品与参比品的tmax分别为 (2 1± 0 4 ) ,(2 0± 0 5 )h ;cmax分别为 (10 2 7± 6 8) ,(10 4 6± 9 1)ng·mL-1;AUC0→t分别为(95 5 6± 2 73 7) ,(10 2 2 0± 42 8 7)ng·mL-1·h ;MRT0→t分别为 (18 8± 6 5 ) ,(19 5± 7 3)h。经交叉试验方差分析 ,上述药动学参数均无统计学差异 (P >0 0 5 )。试验品与参比品的cmax与AUC0→t经双单侧t检验分析 ,P >0 0 5。试验品的相对生物利用度为 (98 92± 17 87) %。结论 :试验品与参比品具有生物等效性。更多还原

【Abstract】 AIM: To study the pharmacokinetics and relative bioavailability of domestic cilazapril tablets in Chinese healthy volunteers. METHODS: Twelve male Chinese healthy volunteers received 2.5 mg, po, cilazapril tablet in a random crossover design. The active metabolite cilazapril was determined by radioenzymatic assay. RESULTS: The pharmacokinetic parameters of tested and reference cilazapril tablets were as follows: t max: (2.1±0.4) h and (2.0±0.5) h, c max: (102.7±6.8) ng·mL -1 and (104.6±9.1) ng·mL -1, AUC 0→t: (955.6±273.7) ng·mL -1·h and (1 022.0±428.7) ng·mL -1·h, MRT 0→t: (18.8±6.5) h and (19.5±7.3) h, respectively. There were no significant differences in the pharmacokinetic parameters above between the 2 tablets (P>0.05). The relative bioavailability of cilazapril tablet is (98.92±17.87)%. CONCLUSION: The results suggest that the 2 preparations have bioequivalence.更多还原