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目的3×3拉丁方研究国产麦考酚吗乙酯片剂、胶囊剂与进口麦考酚吗乙酯胶囊(商品名:骁悉)的生物等效性。方法24名健康男性志愿者随机交叉单剂量口服国产麦考酚吗乙酯片剂、胶囊剂和进口麦考酚吗乙酯胶囊500 mg,以HPLC法测定血药浓度,计算各药动学参数和相对生物利用度,并以WinNonlin程序计算药动学参数,评价生物等效性。结果国产麦考酚吗乙酯片剂、胶囊和进口麦考酚吗乙酯胶囊药-时曲线符合线性动力学一室开放模型,AUC0→48分别是(39.74±8.61)、(38.06±9.01)和(36.21±9.17)mg.h.L-1;AUC0→∞:(44.02±10.62)(、40.91±9.54)和(39.82±9.21)mg.h.L-1;ρmax:(20.19±9.63)、(17.42±6.03)和(18.48±7.06)mg.L-1;tmax:(0.74±0.64)(、0.72±0.35)和(0.56±0.20)h;t12:(13.43±4.58)、(12.20±3.08)和(13.59±5.40)h;MRT:(14.95±5.85)(、13.42±2.83)和(14.40±5.47)h。结论国产麦考酚吗乙酯片剂、胶囊与进口麦考酚吗乙酯胶囊具有生物等效性。
Objective 3 × 3 Latin square to study the bioequivalence of domestic mycophenolate mofetil ethyl capsules, capsules and imported mycophenolate mofetil ethyl ester (trade name: Xiaoxitai). Methods Twenty-four healthy male volunteers were randomized to receive a single oral dose of 500 mg of mycophenolate mofetil ethyl mycophenolate mofetil, ethyl gallate (500 mg), and their pharmacokinetic parameters were calculated by HPLC And relative bioavailability, and pharmacokinetic parameters were calculated using the WinNonlin program to evaluate bioequivalence. Results The IC50 of mycophenolate mofetil, capsules and imported mycophenolate mofetil ethyl capsules were in accordance with the linear kinetic open-chamber model. The AUC0 → 48 were (39.74 ± 8.61), (38.06 ± 9.01) And (36.21 ± 9.17) mg.hL-1; AUC0 → ∞: (44.02 ± 10.62) (40.91 ± 9.54) and (39.82 ± 9.21) mg.hL-1, respectively; pmax: (20.19 ± 9.63) and (17.42 ± 6.03) and (18.48 ± 7.06) mg.L-1; tmax: (0.74 ± 0.64) (, 0.72 ± 0.35) and (0.56 ± 0.20) h; t12: (13.43 ± 4.58), (12.20 ± 3.08) 13.59 ± 5.40) h; MRT: (14.95 ± 5.85) (, 13.42 ± 2.83) and (14.40 ± 5.47) h. Conclusions Domestic mycophenolate mofetil ethyl capsules and capsules are bioequivalent.