OBJECTIVE To investigate the relationship between the dissolution rate and bioavailability of paracetamol tablets. METHODS The dissolution rate of paracetamol tablet was determined according to methods described in the Pharmacopoeia of the People's Republic of China. Ultraviolet spectrophotometry was employed to measure urine concentration of paracetamol, and the relative bioavailability was determined in 25 male healthy volunteers, with the relationship between the dissolution rate and bioavailability of paracetamol assessed. RESULTS The 15-min dissolution rates of 5 kinds of paracetamol tablets were 100.43+/-2.61, 99.76+/-1.97, 96.47+/-3.52, 89.58+/-1.85, and 85.85+/-1.83 respectively, with their bioavailability of 86.34+/-10.06, 85.82+/-11.21, 87.10+/-10.86, 81.71+/-12.34, and 76.53+/-11.73 respectively, showing obvious linear relationship between them, which conformed to the equation y = 0.6122x + 25.175, r = 0.9642. CONCLUSIONS As there is a good linear relationship between the dissolution rate and bioavailability of paracetamol tablets, the latter parameter can be derived from the measurement of the former.