The Absolute Bioavailability and Food Effects on Pharmacokinetics of L-3-n-Butylphthalide Tablet in Healthy Chinese Subjects

L-3-n-butylphthalide (L-NBP) is a potential drug for treatment of Alzheimer's disease. This study evaluated the absolute bioavailability and food effects on pharmacokinetics of L-NBP tablet in healthy Chinese subjects. This was a single-center, randomized, single-dose, open-label, three-period, and cross-over study. Twelve healthy subjects were randomly assigned to receive single oral dose of 240 mg L-NBP tablet in fasted state or fed state or intravenous infusion of 70 mg L-NBP sodium chloride injection in fed state on 3 separate visits. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters were calculated with WinNonlin software. In fasted and fed state, the main pharmacokinetic parameters of L-NBP tablet were as follows: C-max were 303.92 +/- 126.39 and 273.23 +/- 144.51 ng/mL, t(1/2) were 7.54 +/- 1.31 and 8.94 +/- 3.47 h, t(max) were 1.31 +/- 0.56 and 2.96 +/- 1.09 h, AUC(0-48) h were 647.59 +/- 225.20 and 743.05 +/- 305.10 ng/mL.h, and AUC(0-8) were 659.82 +/- 229.07 and 758.77 +/- 311.86 ng/mL.h, respectively. The absorption rate of L-NBP tablet was delayed by food intake but the absorption degree was not affected. The absolute bioavailability of L-NBP tablet was 19.02 +/- 6.45%.