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目的研究替加色罗胶囊与片剂在人体内的生物等效性。方法24名健康男性受试者随机交叉给药,分别单次口服受试制剂替加色罗胶囊和参比制剂替加色罗片剂12mg,采用液相色谱-串联质谱法测定替加色罗的血药浓度,用DAS1.0软件计算药动学参数和生物等效性评价。结果胶囊与片剂的主要药动学参数:AUC0～t分别为(28±s8)和(28±11)μg.h.L-1,AUC0～∞分别为(31±9)和(30±12)μg.h.L-1,ρmax分别为(9.0±2.7)和(9±3)μg·L-1,tmax分别为(1.2±0.4)和(1.1±0.3)h,t1/2分别为(8.5±2.8)和(7±4)h。经置信区间法及双单侧t检验表明,主要药动学参数间差别均无显著意义(P>0.05);受试制剂的相对生物利用度为(112±43)%。结论2种替加色罗制剂具有生物等效性。
Objective To study the bioequivalence of tegaserod capsules and tablets in human. Methods Twenty-four healthy male subjects were randomized to receive oral administration of tegaserod capsule and reference drug tegaserod tablet 12 mg once daily, respectively, and tegaserod was determined by liquid chromatography-tandem mass spectrometry Of plasma concentration, using the DAS1.0 software to calculate pharmacokinetic parameters and bioequivalence assessment. Results The main pharmacokinetic parameters of capsule and tablet were AUC0 ~ t (28 ± s8) and (28 ± 11) μg.hL-1, respectively. The AUC0 ~ ∞ were (31 ± 9) and ρmax were (9.0 ± 2.7) and (9 ± 3) μg · L-1, tmax was (1.2 ± 0.4) and (1.1 ± 0.3) h respectively, t1 / 2 was 2.8) and (7 ± 4) h. Confidence interval method and double unilateral t-test showed that there was no significant difference between the main pharmacokinetic parameters (P> 0.05). The relative bioavailability of the test preparation was (112 ± 43)%. Conclusions The two tegaserod formulations have bioequivalence.