ENHANCEMENT OF LORATADINE DISSOLUTION BY SURFACE SOLID DISPERSION: THE POTENTIAL USE OF CO-PROCESSED EXCIPIENTS AS ON-SURFACE CARRIERS

Abstract

Objective: The aim of the work in this study is to enhance the dissolution rate of the poorly water-soluble drug; loratadine employing co-precipitated surface solid dispersions (SSDs) prepared using various hydrophilic on-surface carriers namely; Pearlitol® flash, Parteck® ODT, Prosolv® ODT G2 and Pharmaburst® C1. Methods: Loratadine solid dispersions (SDs) were prepared by co-precipitation method using copovidone, poloxamer 188 and gluconolactone at different ratios. The best formulae were selected, based on dissolution results obtained, to prepare 16 different SSDs. The prepared SSDs were subjected to drug content and in-vitro dissolution studies and the best formulae were further subjected to solid-state characterization, using X-ray powder diffraction (XRPD) and differential scanning calorimeter (DSC). The effect of aging on the best formulae was studied by evaluating the drug content, drug dissolution and the change in the crystalline state using (XRPD). Results: S1 formula, containing drug: poloxamer 188: pearlitol flash at 1:4:1 ratio, and S9 formula, containing drug: poloxamer 188: prosolv ODT at 1:4:1 ratio showed the highest dissolution efficiency. XRPD and DSC studies of S1 and S9 proved a decrease in drug crystallinity and confirmed solid dispersion formation. The stability study of S1 and S9 showed a slight reduction in the dissolution efficiency (DE) of S1 (from 84.6±0.8 to 81.4±0.7 and 81.4±1.3 at ambient and accelerated conditions, respectively) and a higher reduction in DE of S9 (from 83.5±2.4 to 69.6±1.0 and 57.3±2.9 at ambient and accelerated conditions respectively). Conclusion: Results obtained obviously confirmed the potential effect of the surface solid dispersion technique, using poloxamer 188 as a hydrophilic carrier and Pearlitol flash as an on-surface carrier, on improving the dissolution of loratadine.