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Epalrestat is a reversible noncompetitive inhibitor of aldose reductase with selective inhibition of aldose reductase. It can inhibit the accumulation of sorbitol in red blood cells in patients with diabetic peripheral neuropathy and can improve patients' conscious symptoms and neurological dysfunction. This study was designed to evaluate the bioequivalence in healthy Chinese subjects of a new test formulation and reference formulation of oral epalrestat (50 mg) in the fasting state. The study was performed with 44 healthy Chinese subjects according to a randomized 2‐way crossover design. The main pharmacokinetic parameters of test formulation and reference formulation as follows: 4793 and 4781 ng/mL for maximum plasma concentration, 8556 and 8431 ng h/mL for area under the plasma concentration‐time curve extrapolated to infinity. The test formulation of epalrestat was bioequivalent to the reference formulation. The bioequivalence study of epalrestat in healthy Chinese subjects suggests that the test and reference formulations have similar pharmacokinetics and both formulations are well tolerated in the dose range studied in healthy Chinese subjects. All these findings provided valuable pharmacokinetic knowledge for further clinical development. [ABSTRACT FROM AUTHOR]

A randomized, open‐label, 2‐period crossover study was performed to evaluate the pharmacokinetic properties and bioequivalence of 2 erlotinib hydrochloride tablets (a test formulation and a reference formulation) in healthy Chinese subjects. Subjects were randomized to receive a single oral dose of the erlotinib hydrochloride test or reference formulation (150 mg) under fasting conditions. The washout period was 12 days. Blood samples were collected at scheduled time points, and plasma concentrations were determined using a high‐performance liquid chromatography–tandem mass spectrometry method. A noncompartmental method was used to calculate pharmacokinetic parameters and to evaluate the bioequivalence of the 2 formulations. Safety assessments were performed during the whole study period. The results suggest that the pharmacokinetic parameter values of the test formulation were similar to those of the reference formulation. The 90% confidence intervals of the geometric least‐squares mean ratios of the test to reference formulation were 94.06% to 105.43% for maximum concentration, 88.21% to 97.57% for area under the concentration‐time curve to last measurement, and 87.37% to 97.14% for area under the curve extrapolated to infinity, which are all within the accepted bioequivalence range of 80% to 125%. No serious adverse events occurred during the study. These findings suggest that the 2 erlotinib hydrochloride tablets were bioequivalent in accordance with predetermined regulatory criteria. [ABSTRACT FROM AUTHOR]

The effects of food and gender on the pharmacokinetics of rosuvastatin in healthy Chinese subjects were investigated from 4 bioequivalence studies. These studies were designed as randomized, open‐label, and 2‐period crossover in both fasting and fed states. A total of 204 subjects were enrolled, 134 men and 70 women. These subjects received a single oral 10‐mg dose of rosuvastatin with a 7‐day washout between 2 periods. The plasma concentrations were determined using a validated liquid chromatography tandem mass spectrometry method, and pharmacokinetic parameters were calculated by noncompartmental methods. Compared with the fasting condition, administration after a high‐fat and high‐calorie meal resulted in an approximately 40% reduction of rosuvastatin exposure and a near 50% decrease in absorption rate. Moreover, the apparent clearance was significantly greater in the fed state than that in the fasting state. It was noted that the adverse events incidence is increased by approximately 30% in the fasting state; however, no serious adverse events were observed. Additionally, small differences in pharmacokinetic characteristics were found between male and female subjects. Food effect might be considered for optimal effectiveness and safety of rosuvastatin therapy. [ABSTRACT FROM AUTHOR]