拉米夫定片人体生物等效性评价

目的评价拉米夫定片在健康人体的生物等效性。方法健康志愿者22例，随机2×2交叉，单剂量口服受试和参比制剂拉米夫定片100mg，洗脱期为1周。采用LC．MS／MS法测定血药浓度，并用DAS药动学软件进行参数计算及评价2种制剂的生物等效性。结果单剂量口服受试和参比制剂后，血浆中拉米夫定的主要药动学参数：pmax分别为（881．44-236．8）和（985．0±292．4）μg·L-1，tmax分别为（O．989±0．323）和（1．0344-0．651）h，t1／2分别为（2．889±0．622）和（2．820±0．368）h，AUc-t分别为（3435±627．7）和（3504±506．7）μg·h·L-1，AUC0→∞分别为（3529±630．9）和（3592±519．4）μg·h·L-1，受试制剂与参比制剂的人体相对生物利用度（F）是（98．45±13．50）％。结论拉米夫定片受试制剂与参比制剂具有生物等效性。

Evaluation on bioequivalence of lamivudine tablets in healthy volunteers

AIM To evaluate the bioequivalence of lamivudine tablets in healthy male volunteers. METHODS Twenty-two healthy volunteers in randomized 2 × 2 crossover study were given a single oral 100 mg dose of test or refer- ence lamivudine tablets. The plasma concentrations were determined by LC-MS/MS, and the pharmacokinetic parameters were calculated and the bioequivalence of two formulations were evaluated by DAS program. RESULTS The main phar- macokinetic parameters for test and reference formulations were as follows： pmax were（ 881.4 ± 236.8） and （985.0 ± 292.4）/.tg. L- l, t max were （0.989 ± 0.323） and （ 1. 034 ± 0.651 ） h, t 1/2 were （ 2. 889 ± 0. 622） and （ 2. 820 ± 0. 368 ） h, AUC0→∞ were（3 435 ± 627.7）and（3 504 ± 506.7）μg h L-1, AUC0→∞ were（3 529 ± 630.9）and（3 592± 519.4） μg h L-1,respectively.The relative bioavailability of lamivudine was（98.45± 13.50）%. CONCLUSION The results show that the two lamivudine tablets made by two different corporations are bioequivalent.