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Inosiplex is a compound formulation composed of inosine and p-acetaminobenzoic acid (PABA) salt of N,N-dimethylamino-2-propanol (DIP). This study was to investigate the clinical plasma pharmacokinetic properties of DIP and PABA after single and multiple oral doses of inosiplex tablets in healthy Chinese volunteers. The established LC/MS/MS method for plasma DIP determination had a linear range of 0.02â10 µg/mL, and the HPLC method for plasma PABA determination had a linear range of 0.05â40 µg/mL. Linear pharmacokinetic characteristics were found with single oral doses of 0.5, 1.0 and 2.0 g. No obvious accumulation effects were observed for DIP and PABA. Keywords: Inosiplex, N,N-dimethylamino-2-propanol, p-Acetaminobenzoic acid, LC/MS/MS, HPLC, Pharmacokinetics