吗替麦考酚酯胶囊人体生物等效性研究

目的:研究2种吗替麦考酚酯胶囊的人体生物等效性。方法:18名受试者随机、交叉、单剂量分别口服吗替麦考酚酯胶囊受试制剂(国产)和参比制剂(进口)1000mg。血药浓度采用反相高效液相色谱法测定;计算药动学参数并评价生物等效性。结果:受试制剂与参比制剂的主要药动学参数Cmax分别为(26.38±9.55)、(25.84±12.08)μg·mL-1,tmax分别为(0.79±0.40)、(0.94±0.59)h,t1/2分别为(18.01±7.65)、(15.62±8.50)h,AUC0～48分别为(54.69±15.58)、(51.68±12.36)μg.h.mL-1,AUC0～∞分别为(61.10±17.06)、(57.99±17.21)μg.h.mL-1。受试制剂的相对生物利用度为(107.22±25.39)%。结论:国产与进口吗替麦考酚酯胶囊生物等效。

Bioequivalence of Mycophenolate Mofetil Capsules in Human Body

OBJECTIVE： To study the bioequivalence of the domestic and the imported mycophenolate mofetil capsules in human body. METHODS： A single dose of 1 000mg domestic mycophenolate mofetil capsules （trial） or its reference capsule （imported ones） were given to each volunteer in a randomized double cross over design. The plasma concentration was determined by RP - HPLC, The pharmacokinetic parameters of two preparations were calculated and the bioequivalence of which was evaluated. RESULTS： The main pharmacokinetic parameter of the trial vs. the reference preparations of mycophenolate mofetil capsules were as follows： Cmax： （26.38±9.55） versus （25.84＋ 12.08） μg·mL^1; tmax（0.79±0.40）h versus （0.94±0.59） h;t 1/2： （18.01±7.65）h versus （15.62± 8.50）h;AUC0-48： （54.69±15.58） versus （51.68±12.36）μg·h·mL^1 ; AUC0-∞ （61.10±17.06） versus （57.99±17.21） μg·h·mL^1. The relative bioavailability of the trial preparation was （107.22± 25.39） %. CONCLUSION： The results suggest that the two formulations are bioequivalent.