塞克硝唑胶囊健康人体生物等效性研究

Bioequivalent study of secnidazole in healthy volunteers

目的研究塞克硝唑胶囊在健康志愿者中的生物等效性。方法21名男性健康志愿者随机交叉单次空腹服用试验制剂塞克硝唑胶囊和参比制剂塞克硝唑片剂。用高效液相色谱法测定血清中塞克硝唑的药物浓度。结果受试者单剂口服1000mg塞克硝唑试验药和对照药后,主要药动学参数Cmax分别为(22.69±3.60)和(23.29±3.62)mg/L;Tmax分别为(1.18±0.49)和(1.15±0.65)h;t1/2β分别为(26.43±5.77)和(27.08±5.46)h;AUC0-t分别为(701.12±123.89)和(709.93±89.06)mg·h/L;AUC0-∞分别为(761.14±147.96)和(773.71±108.23)mg·h/L。试验制剂对于参比制剂的平均相对生物利用度AUC0-∞为(98.38±12.83)%。结论受试者单剂空腹给药后塞克硝唑在体内的过程符合二室模型,AUC0-t、AUC0-∞及Cmax经统计学处理,表明试验制剂塞克硝唑胶囊和参比制剂塞克硝唑片具有生物等效性。

Objective To study the bioequivalence of secnidazole capsule in healthy volunteers. Methods Twenty-one normal male volunteers were enrolled in a randomized crossover study. Each volunteer was given a single oral dose of secnidazole cap sule （test preparation） and reference preparation （tablet） for comparison. The serum concentrations of secnidazole were deter mined by HPLC. Results The pharmacokinetic parameters of secnidazole capsule and reference tablet after oral dose of 1 000 mg of secnidazole were Cmax （22. 69 ± 3. 60） and （23.29 ± 3.62） mg/L respectively, Tmax （1. 18 ± 0.49） and （1.15 ± 0.65 ） h respectively, t1-2β（26.43 ± 5.77） and （27.08 ± 5.46） h respectively, AUC0-t（701.12 ± 123.89） and （709.93 ± 89.06） h · mg/L respectively, AUC0-∞ （761.14± 147.96） and （773.71 ± 108.23） h · mg/L respectively. The bioavailability of secnidazole were （98.73 ± 11.34） % based on AUC0-t ,and （98.38 ± 12.83） % based on AUC0-∞. Conclusions The serum concentration-time data of secnidazole fit into a two-compartmental model. Results show that test preparation and reference tablet are bioequivalent.