Influence of Dispersion Method on Dissolution Rate and Bioavailability of Digoxin from Triturations and Compressed Tablets II

Abstract

Ball milling or muller milling digoxin with a 20-fold excess of lactose, sucrose, calcium phosphate dibasic, or microcrystalline cellulose significantly enhanced its dissolution rate. Tablets prepared with such triturations also exhibited superior rates of dissolution. Those prepared with the digoxin-lactose trituration gave plasma levels in rats that were 89.6% of the values from an oral solution of digoxin. A simple blend of unmilled digoxin with lactose yielded tablets producing plasma levels only 80% as high. Excellent content uniformity was characteristic for all triturations and tablets prepared by ball or muller milling.