In vitro and In vivo Evaluation of Tablets Containing Meloxicam- PEG 6000 Ball-Milled Co-Ground Mixture

Abstract

This study aimed at a) preparing meloxicam (MLX) tablets containing ball milled co-ground mixture with PEG 6000 (1:4); b) evaluating the relevant in vitro quality parameters and stability; and c) comparing the bioavailability of the developed tablets with that of a reference meloxicam tablets (Mbc) in 6 human subjects. The dissolution rate of the prepared tablets was higher than that containing ball-milled or un-milled drug alone, as well as higher than four marketed meloxicam tablets. Upon storage for 12 months at 25±1oC / 60% RH, no remarkable changes in physical appearance of the prepared tablets, % drug content, thickness, disintegration time and in dissolution rate were observed. The prepared meloxicam tablets showed higher bioavailability which was indicated by significant higher AUC and significant shorter Tmax. The bioavailability of the developed test tablets was 126.45%, relative to the marketed brand product (Mbc tablets). Grinding of MXL with PEG 6000 resulted in a fast MLX release, which may provide rapid onset of action and allow also a reduction of required dose necessary to obtain the therapeutic effect. This, in turn, may further reduce the most common side effects observed with non-steroidal anti-inflammatory drugs (NSAIDs).