Adv Pharm Bull. 2015;5(4):569-581.
doi: 10.15171/apb.2015.077
PMID: 26819931
PMCID: PMC4729349
Scopus id: 84949658319
  Abstract View: 448
  PDF Download: 237

Original Research

Enhancement of the Oral Bioavailability of Fexofenadine Hydrochloride via Cremophor® El-Based Liquisolid Tablets

Soad Ali Yehia 1, Mohamed Shafik El-Ridi 2, Mina Ibrahim Tadros 1 * , Nolwa Gamal El-Sherif 3

1 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
2 Department of Pharmaceutical Technology, National Research Center, Dokki, Giza, Egypt.
3 Faculty of Pharmacy and Pharmaceutical Industries, Sinai University, Sinai, Egypt.

Abstract

Purpose: The current work aimed to develop promising Fexofenadine hydrochloride (FXD) liquisolid tablets able to increase its oral bioavailability and shorten time to reach maximum plasma concentrations (Tmax). Methods: Eighteen liquisolid powders were developed based on 3 variables; (i) vehicle type [Propylene glycol (PG) or Cremophor® EL (CR)], (ii) carrier [Avicel® PH102] to coat [Aerosil® 200] ratio (15, 20, 25) and (iii) FXD concentration in vehicle (30, 35, 40 %, w/w). Pre-compression studies involved identification of physicochemical interactions and FXD crystallinity (FT-IR, DSC, XRD), topographic visualization (SEM) and estimation of flow properties (angle of repose, Carr’s index, Hausner’s ratio). CR-based liquisolid powders were compressed as liquisolid tablets (LST 9 – 18) and evaluated for weight-variation, drug-content, friability-percentage, disintegration-time and drug-release. The pharmacokinetics of LST-18 was evaluated in healthy volunteers relative to Allegra® tablets. Results: Pre-compression studies confirmed FXD dispersion in vehicles, conversion to amorphous form and formation of liquisolid powders. CR-based liquisolid powders showed acceptable-to-good flow properties suitable for compaction. CR-based LSTs had appropriate physicochemical properties and short disintegration times. Release profile of LST-18 showed a complete drug release within 5 min. Conclusion: LST-18 succeeded in increasing oral FXD bioavailability by 62% and reducing Tmax to 2.16 h.
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Submitted: 29 Aug 2014
Revised: 30 Oct 2015
Accepted: 14 Nov 2015
First published online: 30 Nov 2015
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