Title:Enhanced Oral Bioavailability and Stability Studies of Loratadine Tablets Based on Solid Dispersion of Modified Ziziphus spina-christi Gum
Volume: 18
Issue: 3
Author(s): Ameen M. Alwossabi*, Eltayeb S. Elamin, Elhadi M.M. Ahmed, Eman A. Ismail, Ahmed Ashour, Wadah Osman, Asmaa E. Sherif, Amira Mira*, Rawan Bafail, Yusra Saleh Andijani, Sabrin R.M. Ibrahim*, Gamal A. Mohamed and Mohammed Abdelrahman
Affiliation:
- Department of Pharmacy, Faculty of Medical Sciences, Al-Razi University, Sana’a, Yemen
- Department of Pharmaceutics,
Faculty of Pharmacy, University of Gezira, Wad Medani, Sudan
- Department of Pharmaceutics, Faculty of
Pharmacy, Hodiedah University, Hodiedah, Yemen
- Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University,
Mansoura, 35516, Egypt
- Department of Pharmacognosy & Pharmaceutical Chemistry, College of Dentistry &
Pharmacy, Buraydah Private Colleges, Buraydah, 51418, Saudi Arabia
- Preparatory Year Program, Department of Chemistry, Batterjee Medical College, Jeddah, 21442, Saudi Arabia
Keywords:
Ziziphus spina-christi, loratadine, solid dispersion, solubility enhancement, bioavailability, drug discovery, health and wellbeing.
Abstract:
Background: Solid dispersion is a common technique used for solubility enhancement of
poorly soluble drugs.
Objective: In this study, loratadine (LOR), a class II biopharmaceutical classification system (BCS),
was formulated as solid dispersion tablets using modified Ziziphus spina-christi gum (MZG) as a
carrier.
Methods: The solvent evaporation method was used for LOR-MZG solid dispersion (SD) preparation.
A variety of tests were conducted to characterize and optimize the formulation. Solubility,
Fourier transform infrared (FTIR) analysis, Differential Scanning Calorimetry (DSC), X-Ray Diffraction
(X-RD), and Scanning Electron Micrograph (SEM) of solid dispersions were carried out.
Accelerated stability testing and pharmacokinetic studies of formulated tablets were also performed
using albino Wistar rats.
Results: Solid dispersion improved the solubility of LOR by 51 folds. FTIR spectra excluded drugpolymer
interactions, and results obtained by DSC, X-RD, and SEM proved the transition from the
crystalline to the amorphous state. The stability of LOR-MZG solid dispersion tablets was found to
be better when the Alu-Alu package was used. The pharmacokinetics of LOR-MZG compared to
MZG-free loratadine tablets (LOR pure) and commercial loratadine tablets (LOR-TM) following
oral administration revealed that about 6 folds and 10 folds bioavailability were achieved with
LOR-MZG compared to LOR pure and LOR-TM, respectively.
Conclusion: Such promising results encourage more studies on MZG to be used for improving the
aqueous solubility and bioavailability of a wide range of poorly soluble drugs.
