Effect of slow-release β-alanine tablets on absorption kinetics and paresthesia

Oral β-alanine (βA) doses larger than 800 mg commonly result in unpleasant sensory symptoms (paresthesia). However, the association of form (pure vs. slow-release) with side-effects has not been fully described. The aim of this single-blinded, randomized three-arm clinical trial was to compare plasma kinetics and symptoms following βA bolus administration in solution or in slow-release tablet form. Eleven healthy adults ingested 1.6 g of a pure βA reference solution (REF), 1.6 g in slow-release βA tablets (TAB) or a placebo (PLA) after an overnight fast. During the next 6 h, urinary and plasma βA concentrations were measured and questionnaires about intensity, nature (pins and needles, itching, flushing, irritation, numbness, soreness), and spatial distribution of unusual sensations were filled in. TAB resulted in a smaller peak plasma concentration than REF (82 vs. 248 μmol L(-1), p<0.001), delayed time to peak (1.0 vs. 0.5 h, p<0.01) no difference in area under the curve, reduced loss in urine (202 vs. 663 μmol, p<0.0001), and improved retention (98.9 vs. 96.3%, p<0.001). Symptoms described as "pins and needles" were perceived rapidly on the skin of the arms and trunk after REF (Tmax=15 min) and their time course nearly mimicked plasma concentrations. Maximum intensity scores were weaker with TAB ("very low") than with REF ("low", p<0.001), while TAB and PLA did not differ with respect to side-effects. In summary, ingesting 1.6 g βA in slow-release tablets rather than pure in solution results in slower absorption kinetics, improved whole body retention and sensory side-effects that cannot be differentiated from PLA.