关键词: 吲达帕胺, 药动学, 生物等效, 一致性评价

Abstract:

AIM: To evaluate the pharmacokinetics and bioequivalence of 2 indapamide tablets in Chinese healthy subjects. METHODS: A single dose, randomized, open label, two- formulation, two-period crossover design was used. A total of 28 healthy subjects were randomly divided into 2 groups and given 1 tablet of test formulation (indapamide tablet, 2.5 mg/ tablet) or reference formulation (Natrilix, 2.5 mg/tablet) on fasted state. A total of 17 blood samples were collected before and within 72 h after administration, and the whole blood was fully mixed and packaged and stored in the refrigerator at -80 ℃ for storage. The indapamide concentration in human whole blood was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The pharmacokinetic parameters were calculated and the bioequivalence was evaluated. During the study period, vital sign, physical examination and laboratory test were measured after administration for safety assessment. RESULTS:All 28 subjects completed the test. The 90% confidence intervals of the geometric mean ratios of the tested and reference preparations Cmax, AUC0-t and AUC0-∞ were 104.94%-119.90%, 98.90%-106.34% and 98.59%-104.40%, respectively, all of which were within the bioequivalence range of 80.00%-125.00%. During the study, a total of 4 subjects reported 4 mild adverse events and no serious adverse events. CONCLUSION: Two indapamide tablets were safe and bioequivalent in the empty stomach of healthy subjects.

Key words: indapamide, pharmacokinetic, bioequivalence, consistency evaluation