Abstract

SELECTION-EVALUATION OF DIFFERENT EXCIPIENTS FOR PREPARATION OF LEFLUNOMIDE TABLETS

Siddhartha Choudhury*

Abstract

Disease Modifying Anti Rheumatic Drug( DMARDs) reduces the rate of damage to the bone and cartilage and prevent bone and joint damage from occurring secondary to the uncontrolled inflammation. DMARDs have been found to produce durable remission and delay or half disease progression. Chemically synthesize DMARDs are Azathioprine, Cyclosporine, Hydroxychoroquine, d-penicillamine, Leflunomide. Leflunomide is recently introduced immonumodulator inhabits proliferation of activated lymphocytes in patients with Rheumatoid arthritis. Arthritis symptoms are suppressed and radiological progression of disease is retarded. The study was under taken with an aim of Selection-Evaluation of Excipients (Binders) for preparation of Leflunomide tablets will be carried out. Preformulation study was done on pure drugs and granules and results directed for further course of formulation. Based on preformulation studies different batches of Lefiunomide were formulated using different excipients. Granules were evaluated for Loss of drying, Angle of repose, Bulk density, Tapped density, Carrs index and Hausner‖s Ratio. Tablets were tested for weight variation, thickness, hardness, disintegration time. In-vitro drug release studies as per specifications. The formulation that has been found to posses ideal characteristics required for Leflunomide 10mg, 20mg Tablets, so it was concluded as the final formula for Leflunomide 10mg and 20mg tablets are 150mg, 200mg respectively made by co-precipitation of drug with Hydroxypropylmethylcellulose K100M, Polyvinylpyrrolidine K30, Gelatin, Guar gum. The drug release profile of Leflunomide compared with the market sample. From the studied it was concluded that preparation of Leflunomide tablets containing Lactose monohydrate, Starch, Magnesium streate, Dry starch taken as ideal or optimized preparation of tablets.

Keywords: Azathioprine, Cyclosporine, Hydroxychoroquine, d-penicillamine.