替硝唑片在中国健康受试者中的生物等效性研究

Bioequivalence of tinidazole tablets in Chinese healthy volunteers

目的评价2种替硝唑片在中国成年健康受试者中的生物等效性。方法将24例成年健康受试者随机分为2组,试验用自身交叉对照设计,餐后口服单剂量替硝唑片500 mg。用高效液相色谱串联质谱(HPLC-MS/MS)法测定血浆中替硝唑的浓度,用DAS2.1.1软件按非房室模型计算药代动力学参数,并进行生物等效性评价。结果替硝唑受试制剂和参比制剂的主要药代动力学参数:t_(max)分别为(2.37±1.46),(2.28±1.09)h;C_(max)分别为(13.21±2.28),(13.38±1.96)μg·mL^(-1);AUC_(0-t)分别为(272.38±39.86),(266.70±42.78)μg·mL^(-1)·h;AUC_(0-∞)分别为(282.64±42.49),(280.10±38.40)μg·mL^(-1)·h;t_(1/2)分别为(14.88±1.71),(14.95±1.52)h,以AUC_(0-72h)计算2种制剂的相对生物利用度为(99.6±7.6)%。结论 2种替硝唑片在中国健康受试者体内具有生物等效性。

Objective To evaluate the bioequivalence of two tinidazole tablets in Chinese healthy volunteers. Methods A single oral dose 500 mg of test and reference tinidazole tablets were given to 24 subjects according to an open randomized crossover design. The concentration of tinidazole in plasma were determined by high performance liquid chromatography tandem mass spectrometry. The pharmacokineric parameters were calculated and the bioequivalence was compared by non-compartment model of DAS 2. 1. 1. Results The main pharmacokinetic parameters of tinidazole test preparation and reference preparation were calculated. tmax were（ 2. 37 ± 1. 46）,（ 2. 28 ± 1. 09） h; Cmax were（ 13. 21 ± 2. 28）,（ 13. 38 ± 1. 96） μg · mL-1; AUC0-t were（ 272. 38 ± 39. 86）,（ 266. 70 ± 42. 78） μg·mL-1·h; AUC（0-∞） were（ 282. 64 ± 42. 49）,（ 280. 10 ± 38. 40） μg · mL-1· h; t（1/2） were（ 14. 88 ± 1. 71）,（ 14. 95 ± 1. 52） h,respectively. The relative bioavailability of tinidazole test preparation to reference formulation was（ 99. 6 ± 7. 6） % with AUC0-72 h. Conclusion The two tinidazole tablets were bioequivalent in Chinese healthy volunteers.