摘要
目的研究环孢素软胶囊试验制剂和参比制剂的人体药动学和生物等效性。方法20名健康受试者随机交叉口服环孢素软胶囊的试验制剂和参比制剂,剂量均为300mg/人。血样加入内标(环孢素D)经预处理后用HPLC-UV法测定。结果试验及参比制剂的主要药动学参数Cmax分别为(1111.98±176.64)ng.mL-1,(1262.69±226.36)ng.mL-1;Tmax分别为(1.65±0.49)h,(1.45±0.65)h;t1/2分别为(6.55±1.08)h,(6.09±1.35)h;AUCo→t分别为(6032.68±1282.44)h.ng.mL-1,(6394.53±1563.64)h.ng.mL-1。以AUCo→t计算的试验制剂的相对生物利用度为(100.21±36.79)%。结论经方差分析及双单侧t检验结果显示,试验制剂和参比制剂具有生物等效性。
Objective To study the pharmacokinetics and bioequivalence of ciclosporin test and reference soft capsules in healthy volunteem. Methods A single oral dose of 300mg the test or the reference preparation was given to 20 healthy volunteers in a randomized two-period eressover study. HPLC-UV was performed to detect ciclosporin A and using ciclosporin D as the internal standard （IS） . Results The main pharmacokinetic parameters of test and reference soft capsules were as follow： Cmax were （937.12±327.74 ）ng·mL^-1 and （900.49±319.45 ）ng·mL^-1 ;Tmax were （3.97±0.53 ） h and （ 3.67±0.64 ） h ; t1/2： were （ 1.83±0. 95 ） h and （ 1.69±0. 64 ） h ; AUC0→t were （ 3 183.20±1 650.61） h·ng·mL^-1 and （2 922.22±1 413.72） h·ng·mL^-1, respectively. The relative bioavalability of the test soft capsules was （ 109.68±23.30） %. Conclusion The results showed that the test soft capsules of ciclosporin A was bioequivalent with the reference soft capsules.
出处
《内科》
2007年第2期162-165,共4页
Internal Medicine
