Pharmacokinetics and Bioequivalence Study of Levodopa and Benserazide Tablets in Healthy Chinese Subjects Under Fasting and High-Fat Meal Conditions.

Levodopa and benserazide tablets (LBTs) are a combined preparation of levodopa (L-DP), a dopamine precursor, and benserazide (BZ), a peripheral dopa decarboxylase inhibitor, used for the treatment of Parkinson's disease, which predominantly affects middle-aged and elderly individuals. This study employed a single-center, randomized, open-label, two-formulation, three-period, three-sequence, partially replicated (reference formulation only) clinical study design to evaluate the pharmacokinetics and bioequivalence of the test and reference formulations of LBT administered orally to 96 healthy Chinese subjects under fasting or fed conditions. After fasting for at least 10 h and abstaining from water for 1 h, subjects received one tablet of either the test or reference formulation with 240 mL of warm water on Days 1, 8, and 15 of the study, either in the fasting state or 30 min after starting a high-fat meal. Plasma drug concentrations were determined using an ultra-high performance liquid chromatography-tandem mass spectrometry method. The 90% confidence intervals of the geometric mean ratios for the pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ met the bioequivalence criteria, indicating that the test formulation is bioequivalent to the reference formulation in healthy Chinese adult subjects. No serious adverse events were reported.