国产盐酸托烷司琼片、胶囊与进口片剂人体生物等效性比较

Bioequivalence of Domestic Tropisetron Hydrocloride Tablets,Capsules and Imported Tablets

目的评价国产盐酸托烷司琼片、胶囊与进口参比制剂是否生物等效。方法男性健康受试者24名,随机分成6组,三交叉po受试制剂和参比制剂各20 mg,在一定时间点取静脉血分离血清,用高效液相色谱紫外检测法测定人血清中托烷司琼浓度,所得数据经BECS软件处理得到主要药动学参数。结果国产盐酸托烷司琼片、胶囊与进口参比制剂托烷司琼的tmax均为(1.7±0.4)h,ρmax分别为:(36.9±8.9),(36.3±8.9)和(36.1±9.3)μg.L-1,用梯形法计算所得的AUC0-t分别为(443±176),(448±196)和(443±191)μg.h.L-1。对经对数转换后的ρmax,AUC0-t进行方差分析和双单侧t检验及90%可信限判断,盐酸托烷司琼片、胶囊的ρmax落在参比制剂的90.7%-116.2%和89.1%-114.2%内,AUC0-t落在参比制剂的82.8%-124.0%和82.7%-123.8%内,tmax经非参数检验法检验无显著差异,盐酸托烷司琼片、胶囊AUC0-t的相对生物利用度分别为(102±9)%和(102±10)%。结论3种制剂具有生物等效性。

OBJECTIVE To evaluate the bioequivalence of domestic tropisetron preparations and imported tablets. METHODS A total of 24 healthy male volunteers, divided randomly into six groups, were administered with three preparations of tropisetron respectively in an open randomized three cross-over design. A single oral dose of the test and reference preparations was 20 mg. Tropisetron （Trop） concentrations in the serum were determined by high performance liquid chromatography. The pharmacokinetic parameters of tropisetron were obtained using BECS software. RESULTS Tropisetron parameters of the tablets, capsules and the reference preparations were as follows：tmax（1. 7 ±0.4） h;pmax（36. 9 ±8.9） ,（36. 3 ±8.9） and （36. 1 ±9. 3） μg · L^-1 ;AUC0-tn（443 ±176）, （448 ±196） and （443 ± 191 ） μg · h · L^-1. The result of statistical analysis showed that there was no significant differences on Pmax, muc0-tn and tmax among the three preparations. The relative bioavailability of tablets was （ 102 ± 9） % and the relative bioavailability of capsules was （ 102 ± 10） %. CONCLUSION The three preparations are bioequivalent.