Formulation and Evaluation of Various Dosage Forms of Etodolac as a Nonsteroidal Anti - inflammatory Drug

Abstract

Nine different tablet formulations were suggested in an attempt to formulate a fast release oral dosage form which on rapid release of the drug could possibly enhance its dissolution, absorption and consequently therapeutic effect. Each formulation consisted of 300 mg etodolac in addition to one of the following carriers; Ludipress (F1 ), Kollidon CL (F2), Explotab (F3), Avicel PH101 (F4), Ac-Di-Sol (F5), soluble starch (F6), PVP K25 (F7), PEG 4000 (F8) and PEG 6000 (F9) and 1 % lubricant mixture. These tablet

powder mixtures were directly compressed into tablets. Uniformity of dosage unit, tablet friability, tablet hardness, disintegration time and dissolution rate were determined. All the formulated tablets had met the USP 24 requirements for the uniformity of dosage unit. Tablet hardness values

ranged from 7 Kg for PEG 4000 containing formulation (F8) and 16 Kg for Kollidon CL based tablets (F2). Kollidon CL (F2) and Avicel PH101 (F4) formulations showed the shortest disintegration time of 30 seconds. While soluble starch (F6), PVP K25 (F7), PEG 4000 (F8) and PEG 6000 (F9) based formulations failed disintegration till 30 minutes. Other tablet formulations

showed intermediate disintegration time values. Dissolution profiles revealed that F2 containing Kollidon CL showed the fastest drug release ( 100% at 15 minutes) with the maximum dissolution efficiency value of 95.69% while soluble starch (F6) based tablets showed the least dissolution efficiency of 2.88%. The reference capsules had a dissolution efficiency of 84.72%. On ageing, tablet hardness had increased for Ludipress formulation (F1) only to give 13, 14.5 and 15.5 after 3, 6 and 12 months of storage; respectively. Ludipress (F1 ), Explotab (F3), Avicel PH101 (F4) and Ac-Di-Sol (F5) formulations as well as the reference capsules showed parallel reduction in the dissolution of the drug as a function of the storage period. On the other hand, Kollidon CL based tablets (F2) didn't show any remarkable change in dissolution during the 12 months of storage. Therefore, in addition to the direct compression and the simplicity of formulation with minimum number of tablet excepients, tablets prepared with Kollidon CL (F2) showed the best tablet characteristics and succeeded to maintain them upon storage for one year at room temperature. This promising formulation was the candidate for further bioavailability assessment. Formulation and Evaluation of Various