DISSOLUTION ENHANCEMENT AND FORMULATION OF FILM COATED TABLETS OF LORNOXICAM BY PHASE TRANSITION METHOD: IN-VITRO AND IN-VIVO EVALUATION
Objective: This study aimed to enhance the oral solubility and dissolution of poorly soluble lornoxicam by antisolvent precipitation, and the manufacture of oral tablets by phase transition method.
Methods: The solvent used was polyethylene glycol 400 and absolute ethanol. Three stabilizers Inutec SP1, Pluronic F127, Sucrose ester S1670 at two concentrations and two matrix formers Mannitol, and Avicel PH102 were used to obtain 12 formulae. The formulae were characterized regarding their infrared spectroscopy (IR), differential scanning calorimetry (DSC), particle size (PS) measurement, drug content and dissolution. Further characterizations were done for the optimum formula by scanning electron microscopy (SEM) and X-ray diffraction (XRD). Four tablets formulae were manufactured by phase transition method. The optimum tablets (T3) were evaluated through hardness, drug content, disintegration, dissolution, IR, and stability studies. Finally, (T3) were compared to conventional tablets in male New Zealand rabbits using crossover design.
Results: The dissolution rate for the prepared formulae was enhanced, from 3.44 to 5.96 folds. Statistical significance was obtained using one and two way ANOVA among formulae. The optimum tablet formula (T3) had hardness 5.637 ±1.57 kg, drug content 90.424% ± 1.19, disintegration time 341.5 ± 9.62 second and amount of drug dissolved 72.107 ± 0.0025. Stability, after one month storage of the selected tablets at (25ºc/60% relative-humidity), were satisfactory. The extent of absorption of lornoxicam from (T3) compared to the conventional tablets was higher.
Conclusion: Taken together, the obtained results confirmed successfully the potential of the promising formula (T3), over the conventional tablets of lornoxicam.
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