Enhanced Oral Bioavailability and Stability Studies of Loratadine Tablets Based on Solid Dispersion of Modified Ziziphus spina-christi Gum

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 & Pharmaceutical Chemistry, College of Dentistry & Pharmacy, Buraydah Private Colleges, Buraydah 51418, Saudi Arabia
• Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt

• Preparatory Year Program, Department of Chemistry, Batterjee Medical College, Jeddah 21442, Saudi Arabia
• Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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.

Cite this article as:

Alwossabi M. Ameen*, Elamin Eltayeb S., Ahmed M.M. Elhadi, Ismail A. Eman, Ashour Ahmed, Osman Wadah, Sherif E. Asmaa, Mira Amira*, Bafail Rawan, Andijani Saleh Yusra, Ibrahim R.M. Sabrin*, Mohamed A. Gamal and Abdelrahman Mohammed, Enhanced Oral Bioavailability and Stability Studies of Loratadine Tablets Based on Solid Dispersion of Modified Ziziphus spina-christi Gum, Recent Advances in Drug Delivery and Formulation 2024; 18 (3) . https://dx.doi.org/10.2174/0126673878288535240530113418