EFFECT OF EUDRAGIT® E PO QUANTITY ON BITTER TASTE-MASKING OF DICLOFENAC SODIUM IN ORALLY DISINTEGRATING TABLETS

Abstract

Bitter taste-masking of diclofenac sodium (DS) was prepared by forming solid dispersion of drug and polymer using solvent method.  Polymeric materials used were ethyl cellulose (EC) or polymethacrylates E PO (Eudragit^® E PO).  Drug and polymer ratios were varied in the range of 1:1, 1:2, 1:3, and 1:4. Drug dissolution of solid dispersion powders were tested in simulated saliva fluid (SSF). Comparing to the drug (DS), increasing amount of polymer in the preparations decreased drug dissolution and reduced the bitter taste of drug. Drug released was retarded due to drug entrapment in the polymer. Because of stickiness and difficulty for size reduction of EC preparations at the ratio of 1:2 and higher, Eudragit^® E PO preparation was selected for tablet preparation. Orally disintegrating tablets (ODTs) of drug (DS ODTs) were prepared by direct compression. Effect of superdisintegrant type and quantity on disintegration time was studied.  ODTs of 5% by weight of crosslinked polyvinylpyrrolidone (P5) showed the fastest disintegration time.  ODTs with taste-masked DS (solid dispersion of drug to Eudragit^® E PO, 1:3) were prepared in the same manner of P5 and gave faster disintegration time than DS ODTs (13.15 second and 22.57 second, respectively). The percentage of drug released from taste-masked DS ODTs was lower than that from DS ODTs in SSF. (39.13% and 91.26% at 5 minutes, respectively)  In vitro taste-masking in 10 mL SSF was tested at 1, 3 and 5 minutes. Drug released of DS from taste-masked ODTs at various times were significant lower than those from DS ODTs (6.92, 9.48, 7.31 mcg/mL and 45.68, 67.40, 49.03 mcg/mL at 1, 3 and 5 minutes, respectively). Eudragit^® E PO could be used for taste-masking of bitter drug powder and drug bitterness was reduced with the increasing in the amount of polymer in the preparation.