A pharmaceutical study on lornoxicam fast disintegrating tablets: formulation and in vitro and in vivo evaluation.

Abstract

Lornoxicam is an anti-inflammatory drug used to relieve rheumatoid arthritis pain, but the low water solubility and bitter taste of the drug present challenges for formulation as fast disintegrating tablets (FDTs). Complexation of the drug with β-cyclodextrin was initially carried out to increase the drug solubility and to mask its bitter taste. Tablets were prepared by direct compression of drug complex (DC), F-Melt, mannitol, crospovidone, and sodium starch glycolate (SSG). FDTs were characterized in terms of disintegration time (DT) and dissolution. A bioequivalence study was carried out using (Zeficam® tablets (Eva Pharma) as reference with the help of human volunteers (n=4). The chosen formula (F2, DC 24mg, F-Melt 88.4mg, and crospovidone 5mg) exhibited the shortest in vitro (18s) and in vivo DT (13s), and the percent drug released after Q6min was 95.90%. Following administration of F2 and Zeficam®, the respective maximum drug plasma concentrations (Cmax) were 510 and 532.5ng/mL, at times (Tmax) of 1 and 2.5h, of mean residence times (MRTs) of 12.25 and 11.35h and of areas under the plasma curve [AUC(0-24)] of 5080.253 and 4815.775ng/h/mL. There were significant differences in Tmax and MRT of both treatments (p<0.05). Moreover, the volunteers found F2 to be palatable. FDTs could be considered as promising dosage forms for lornoxicam as they exhibited a short in vivo DT and an increased rate of drug release and attained a relative bioavailability of 105.49%. This could offer a fast relief of pain accompanying rheumatoid arthritis.