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

MOHAMED EL-NABARAWI; DOAA AHMED ELSETOUHY; REHAB ABDELMONEM; AMR EL-HOSSEINI

doi:10.22159/ijap.2022v14i6.46059

Authors

MOHAMED EL-NABARAWI Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt https://orcid.org/0000-0003-0070-1969
DOAA AHMED ELSETOUHY Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
REHAB ABDELMONEM Department of Industrial Pharmacy, Faculty of Pharmacy, Misr University for Science and Technology, 6th of October City, Egypt https://orcid.org/0000-0002-2522-8082
AMR EL-HOSSEINI Department of Research and Development, Sedico Pharmaceutical Co., 6th of October City, Egypt

DOI:

https://doi.org/10.22159/ijap.2022v14i6.46059

Keywords:

Loratadine, Solid dispersion, Surface solid dispersion, Hydrophilic carriers, On-surface carriers, Dissolution improvement, Co-processed excipient

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.

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