OBJECTIVE:To establish the LC-MS/MS method for the determination of lamivudine in plasma and to evaluate the pharmacokinetics and bioequivalence of Lamivudine capsules and tablets in healthy volunteers . METHODS:A single oral dose (100 mg of Lamivudine capsules and tablets ) was given to 24 healthy volunteers in a randomized crossover study .The plasma concentration of lamivudine was determined by LC-MS/MS method .The pharmacokinetic parameters were calculated and the bioequivalence of the two formulations were evaluated by DAS 3.0 program.RESULTS:After a single dose , the pharmacokinetic parameters of Lamivudine capsules and tablets were as follows:Tmax:(1.05 ±0.43) h and (1.01 ±0.38) h; Cmax:(979.05 ±267.25) ng/ml and (1 023.59 ±340.14) ng/ml;t1/2:(9.55 ±4.64) h and (8.95 ±4.68) h; AUC0-t:(3 799.15 ±1 103.26) ng· h/ml and (3 727.14 ± 1 083.10) ng· h/ml;AUC0-∞:(3 881.94 ±1 135.72) ng· h/ml and (3 811.56 ±1 103.61) ng· h/ml respectively. The 90% confidential interval of AUC0-t , AUC0-∞ and Cmax was 95.4%-109.8 %, 95.3%-109.5% and 86.1%-109.1%, respectively.The relative bioavailability of Lamivudine capsules and tablets was ( 104.8 ±25.8 )%. CONCLUSIONS: The method can be used in the pharmacokinetics and bioequivalence of Lamivudine capsules and tablets, and the two preparations were bioequivalent .%目的：建立测定人血浆中拉米夫定含量的液相色谱串联质谱法（liquid chromatography tandem mass spectrometry，LC-MS／MS），并评价拉米夫定胶囊和片剂在健康人体内的药动学过程和生物等效性。方法：24名健康志愿者随机双交叉单剂量口服100 mg拉米夫定胶囊和片剂，采用LC-MS／MS法测定血浆中药物浓度，利用DAS 3.0软件计算药动学参数和生物利用度，并进行生物等效性评价。结果：单剂量口服拉米夫定胶囊和片剂后，达峰时间（Tmax）分别为（1.05±0.43）和（1.01±0.38） h，药峰浓度（Cmax）分别为（979.05±267.25）和（1023.59±340.14） ng／ml，半衰期（t1／2）分别为（9.55±4.64）和（8.95±4.68） h，药-时曲线下面积（AUC0～t）分别为（3799.15±1103.26）和（3727.14±1083.10） ng· h／ml；AUC0～∞分别为（3881.94±1135.72）和（3811.56±1103.61） ng· h／ml。拉米夫定胶囊AUC0～t、AUC0～∞和Cmax的90％置信区间分别为拉米夫定片的95.4％～109.8％、95.3％～109.5％和86.1％～109.1％，拉米夫定胶囊的相对生物利用度为（104.8±25.8）％。结论：该方法可用于拉米夫定药动学和生物等效性研究，本研究中国产拉米夫定胶囊与片剂生物等效。
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