Exploring solid dispersion approach to improve the dissolution of atorvastatin calcium trihydrate

Articles in Press

Document Type : Original Article

Authors

1 Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University, Egypt.

2 Drug & Poison Information Center, Faculty of Pharmacy, Tanta University, Egypt

3 School of Pharmacy, University of Nottingham, Boots Science Building, Nottingham NG7 2RD, United Kingdom

Abstract

The low oral bioavailability of atorvastatin calcium trihydrate (ACT) arises from its limited water solubility and extensive hepatic first-pass metabolism. Therefore, this work aimed to explore different solid dispersion approaches while analyzing the effect of the carrier to enhance the dissolution of ACT and to prepare fast-disintegrating tablets (FDT). Binary and ternary solid dispersions using either Poloxamer 407 (P407) or polyethylene glycol 6000 (PEG-6000), alone or in combination, were prepared at different weight ratios. Aerosil 200 was added to some formulations as a carrier. The impact of the preparation technique on drug dissolution was studied. The adopted methods were either melt fusion or solvent evaporation. All formulations improved ACT dissolution compared to unprocessed drugs. P407 (non-ionic surfactant) was superior to PEG-6000 (hydrophilic polymer) in enhancing the dissolution parameters of ACT. Meanwhile, formulations prepared using melt congealing showed better dissolution behavior than those prepared using solvent evaporation. The optimized formula (1:3:0.2 of ACT:P407:Aerosil 200, respectively) liberated up to 70% of the supplied dose after 5 min., displaying a dissolution efficiency of 90%. Solid-state characterization, involving differential scanning calorimetry and X-ray powder diffraction, indicated decreased drug crystallinity associated with reduced particle size. Scanning electron microscopy images verified the deposition of the drug as reduced particles on the surface of the carrier. We successively prepared fast-dissolving tablets using the optimized formulation. This study introduces a convenient dosage form of ACT for buccal administration with an expected improvement in its therapeutic performance.

Keywords

Bulletin of Pharmaceutical Sciences Assiut University

Articles in Press, Accepted Manuscript
Available Online from 22 September 2025

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