LACK OF INFLUENCE OF GLYCINE ON THE SINGLE-DOSE PHARMACOKINETICS OF ACETYLSALICYLIC-ACID IN MAN

Galenic formulations consisting of acetylsalicylic acid and glycine we re developed to improve solubility of the drug, even in case of ingest ion without intake of water. It was the aim of this study to investiga te the potential influence of glycine on pharmacokinetics after single oral administration of 1,000 mg of acetylsalicylic acid. Therefore, a bioequivalence study using a randomized crossover design (reference = without glycine, test = with glycine) in 12 healthy male volunteers ( age 22 - 38 (median 26) years, body weight 64 - 83 (median 75) kg) was performed. Pharmacokinetic characteristics (AUG, C-max, t(max), t(1/2 ), MRT) were taken or calculated on the basis of plasma concentration/ time profiles. For both acetylsalicylic acid and salicylic acid the 90 % confidence intervals of the ratios of the expected median values (mu (T) and mu(R)) for the primary characteristics AUC and C-max of the te st and reference formulation were included in the equivalence range of 80 - 125%, which in case of multiplicative model is accepted for conc luding bioequivalence, Therefore, lack of influence of glycine on the pharmacokinetics of acetylsalicylic acid including its major metabolit e salicylic acid was concluded.