Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method

Nayyer Islam¹, Muhammad Irfan¹ , Nasir Abbas², Haroon Khalid Syed¹, Muhammad Shahid Iqbal³, Ikram Ullah Khan¹, Akhtar Rasul¹, Sana Inam¹, Amjad Hussain², Noor ul Amin Mohsin⁴, Mohammad Sohail Arshad⁵, Mohsin Ali⁶

¹Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, GC University, Faisalabad; ²University College of Pharmacy, University of the Punjab, Lahore, Pakistan; ³Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam bin Abdulaziz University, Alkharj, Kingdom of Saudi Arabia; ⁴Department of Chemistry, Faculty of Pharmaceutical Sciences, GC University Faisalabad; ⁵Department of Pharmacy, Bahauddin Zakriya University, Multan; ⁶Department of Pharmacology, Faculty of Pharmaceutical Sciences, GC University, Faisalabad, Pakistan.

For correspondence:- Muhammad Irfan Email: manipharma@yahoo.co.uk Tel:+923349392369

Accepted: 20 August 2020 Published: 30 September 2020

Citation: Islam N, Irfan M, Abbas N, Syed HK, Iqbal MS, Khan IU, et al. Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method. Trop J Pharm Res 2020; 19(9):1797-1805 doi: 10.4314/tjpr.v19i9.1

© 2020 The authors.
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Abstract

Purpose: To investigate the efficiency of different solubilizing agents in improving solubility as well as dissolution rate of ebastine (a BCS class II drug) by incorporating prepared solid dispersion into fast disintegrating tablets.

Methods: The solubility of ebastine was determined in distilled water, lipids and solubilizing agents. Subsequently, the binary solid dispersions were prepared by kneading method using varying weight ratios of ebastine and solubilizing agents. The solid dispersions were then incorporated into fast disintegrating tablets (SD-FDT). Central composite rotatable design (CCD) was used to determine the impact of super disintegrating agents on disintegration time and friability of tablets. The solubility and dissolution rate of developed SD-FDT were compared with a marketed brand. The solid dispersion particles were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder x-ray diffraction (P-XRD) and scanning electron microscopy (SEM).

Results: The saturated solubility of pure ebastine in water was 0.002 ± 0.041 mg/ml while the aqueous solubility of EBT/poloxamer solid dispersion SET3 (P) was 0.018 ± 2.510 mg/ml; on the other hand, EBT/soluplus solid dispersion SET1(S) has an aqueous solubility of 0.242 ± 1.390 mg/ml. Within 30 min, drug release was 14.00 ± 1.77, 78.00 ± 2.31 and 98.70 ± 2.54 % from pure EBT, SET3 (P) and SET1(S), respectively.

Conclusion: The solubility and dissolution rate of ebastine has been successfully enhanced by incorporating its solid dispersion in fast-disintegrating tablets (SD-FDT).

Keywords: Ebastine, Solid dispersion, Poloxamer 188, Soluplus, Solubility, Dissolution