Effect of Filler Hydrophilicity on Superdisintegrant Performance and Release Kinetics From Solid Dispersion Tablets of A Model BCS Class II Drug

Abstract

Superdisintegrant absorbs water by wicking or capillary action, undergoes swelling, induces hydrodynamic pressure in the tablet core leading to disintegration. Moreover, they can be functional in accelerating drug release by producing finer particles of higher specific surface area available for interaction with dissolution medium. Disintegrant activity, however, may be influenced by the hydrophilicity of the filler excipient. In the present experimental work, soluble diluent, lactose and hygroscopic, insoluble diluent, di-calcium phosphate dihydrate, were combined with superdisintegrant, Ac-di-sol to produce tablets of Danazol solid dispersion and evaluated for their effects on the water absorption percentage, disintegration time and release kinetics. High hydrophilicity and fibrous nature of Ac-Di-Sol resulted in water absorption percentages of 60% and 52% into the tablet structure for the batches DZ-SDT(L)-2 and DZ-SDT(D)-2 respectively. Use of di-calcium phosphate dihydrate as filler in tablet containing 8% w/w of Ac-di-sol as suerdisintegrant imparted a matrix characteristic to tablet of Danazol solid dispersion which absorbed water sufficiently, followed by quite rapid disintegration, release of 60% of drug within 8 mins and 6-fold lowering in Mean Dissolution Time value. Therefore, proper combination of filler and superdisintegrant is crucial to achieve desired disintegration characteristics and release profile of drug from solid dispersion tablets of a BCS Class II drug.