Formulation and evaluation of sustained release paracetamol peroral matrix tablets: in vivo bioavailability evaluation in man

Abstract

A comparative in vivo bioavailability evaluation of a newly formulated sustained release paracetamol peroral matrix tablets and a marketed conventional rapidly disintegrating paracetamol tablets was carried out according to a two-period, two-treatment, two-sequence, randomised crossover design with a 4-day washout period between the treatments using urinary drug excretion data. The in vivo study was conducted on 10 healthy human male volunteers aged between 24-30 years. The subjects swallowed either the sustained release or the conventional paracetamol tablets at equal dose levels and urine samples were collected at different times over a 24-hour period. Based on the urinary drug excretion data, the mean relative bioavailability of the sustained release tablets with respect to the conventional tablets was 0.949 ± 0.287, indicating that the bioavailability was not significantly different from that of the conventional tablets (P = 0.2701). Moreover, by using the sustained release tablets, it was possible to prolong the elimination half-life of the drug from 2.589 h to 3.840 h.

Keywords: sustained release, paracetamol matrix tablets, comparative bioavailability, urinary drug excretion, elimination half-life

Ethiopian Pharmaceutical Journal, vol. 22 (2004): 39-46