Abstract
BACKGROUND: To assess the food effects and pharmacokinetic profile of oral prednisone (test preparation,5 mg) and prednisolone tablets (reference preparation,5 mg) using a randomized, two-period, two crossover, single-dose, fast and fed trial in 48 (24 in fast, 24 in fed) healthy Chinese adult subjects. MATERIALS AND METHODS: In the trial, the plasma concentrations were determined at different time points up to 24 h and the pharmacokinetic parameters were analyzed according to the concentration data by non-compartmental analysis using WinNonlin software. All laboratory parameters, vital signs and adverse events (AEs) were monitored and recorded under the supervision of the clinicians throughout the whole process of the study. RESULTS: Prednisone and prednisolone undergo interconversion in liver. On average, the bioavailability of prednisolone after oral prednisone is approximately 80% of that after prednisolone. And about 20% of prednisolone is converted to prednisone after administration of equivalent oral of prednisolone tablet. Food taken with prednisone or prednisolone tablets delays the time reach the peak prednisone or prednisolone concentration (T(max)) by approximately 0.5 h but does not affect systemic exposure. Prednisone and prednisolone tablets were well tolerated, and there were no serious adverse events reported in the study. CONCLUSIONS: For there was no information about the pharmacokinetic profile and food effects of oral prednisone and prednisolone tablets, the result of this research would be a clinical medication for doctors especially dealing patients with varying degrees of liver diseases. CLINICAL TRIAL REGISTRATION: CTR20200093; registered in http://www.chinadrugtrials.org.cn/ at 11 March 2020.