摘要
目的 :比较单硝酸异山梨酯 (ISMN)片剂和注射剂在健康受试者中的药动学特征。方法 :18名男性健康受试者采用自身对照交叉给药的方式 ,单剂量ISMN 2 0mg ,po或ISMN 2 0mg +NS 5 0 0mL ,恒速静滴 (持续 4h) ,采用气相色谱法测定血药浓度。结果 :18名受试者ISMN口服或静滴后的药动学参数分别为 :tmax(0 .71± 0 .5 6 ) ,(4 .11± 0 .6 8)h ;cmax(388.71± 86 .2 8) ,(2 82 .5 6± 5 9.2 6 ) μg·L-1;MRT(5 .87± 0 .2 7) ,(6 .87± 0 .17)h ;T1/ 2 (6 .30± 0 .85 ) ,(5 .93± 0 .6 2 )h ;AUC0→ 2 4h(2 978± 4 93) ,(2 838±5 70 ) μg·L-1·h ;AUC0→∞(32 75± 6 2 4 ) ,(3192± 75 4 ) μg·L-1·h。将 2种制剂的AUC和cmax进行对数转换 ,并作双单侧t检验和置信区间法的检验 ,ISMN片剂与注射剂的AUC相比 ,P >0 .0 5 ;但cmax的 90 %置信区间落在 119.0 %～ 15 1.8%的范围内。结论 :考虑到静滴持续 4h的特殊情况 ,认为 2种制剂仍属生物等效 ,片剂的绝对生物利用度为 (10 3± 18) %。
AIM:To compare the pharmacokinetic parameters of isosorbide mononitrate (ISMN) tablet and injection in Chinese healthy volunteers. METHODS: A single dose of 20 mg of ISMN tablet and injection was given to 18 healthy volunteers in a randomized crossover design. ISMN concentration in plasma was determined by gas chromatography with electron capture detection. RESULTS: The main pharmacokinetic parameters of the tablet and injection were: t max were (0.71±0.56)h and (4.11±0.68)h,c max were (388.71±86.28)μg·L -1 and (282.56±59.26)μg·L -1,mean residence time were (5.87±0.27)h and (6.87±0.17)h,T 1/2 were (6.30±0.85)h and (5.93±0.62)h, AUC 0→24h were(2 978±493)μg·L -1·h and (2 838±570)μg·L -1·h, AUC 0→∞ were (3 275±624)μg·L -1·h and ( 3 192±754)μg·L -1·h, respectively. CONCLUSION: The 2 formulations are bioequivalent with respect to AUC. But as for c max, the 90% CIs was 119.0%-151.8%, it is not within the acceptable range. The 2 formulations are still bioequivalent due to special condition of intravenous infusion.
出处
《中国临床药学杂志》
CAS
2004年第2期81-83,共3页
Chinese Journal of Clinical Pharmacy
