苯酰甲硝唑胶囊人体生物等效性研究

The clinical pharmacokinetics and bioequivalence of benzoylmetronidazole capsules

目的 研究苯酰甲硝唑胶囊人体生物等效性。方法 10名健康男性志愿受试者 ,随机分为 2组 ,分别于早晨空腹 1次口服对照品或供试品 96 0mg。 1wk后再交叉服药。受试者分别于服药前和服药后 0 5、1、2、3、4、6、8、12、2 4、30、36和 48h抽取静脉血 3ml,以高效液相法测定甲硝唑血药浓度。结果 两药均符合口服一级吸收一房室开放模型。主要参数 :Tmax为 (3 12± 0 90 )h和 (5 10± 1 6 0 )h ,Cmax为 (6 5 1± 1 2 5 )mg·L-1和 (5 32± 0 87)mg·L-1,AUC为(113 5 9± 19 84)mg·h-1·L-1和 (10 6 96± 19 6 2 )mg·h-1·L-1。各参数间除Tmax和Cmax差异有显著性外 (P <0 0 5 )其它差异均无显著性。供试品相对生物利用度为 (95 0 7±14 70 ) % ,RSD 15 46 %。结论 生物等效性检验后认为两药AUC体内生物等效性相同 ,Cmax和Tmax生物等效有差异。

AIM To compare the pharmacokinetics and bioequivalence of between capsule and solution of benzoylmetronidazole. METHODS Ten chinese healthy male volunteers in a randomized 2-way crossover study were given a single oral dose 960 mg capsule(test) and solution (control) respectively. The serum concentrations of metronidazole, one of the metabolites of benzoylmetronidazole, was measured by high performance liquid chromatography. RESULTS The serum concentration-time curves appeared one-compartment open model. The results of the capsule and the solution of benzoylmetronidazole showed that T max (5.10±1.60) h and (3.12±0.90) h; C max (5.32±0.87) mg·L -1 and (6.51±1.25) mg·L -1 ; T 12 (10.56±1.75) h and (10.16±1.65) h; AUC (106.96±19.62) mg·h -1 ·L -1 and (113.59±19.84) mg·h·L -1 . CONCLUTION No significant difference appears in the pharmacokinetic parameters between the two formulations except of T max and C max ( P <0.05). The relative bioavailability of benzoylmetronidazole capsule is (95.07±14.70)%. The AUC between the two formulations is bioequivalent, but the T max and C max are non-bioequivalent.