title: Enhancement of the Oral Bioavailability of Fexofenadine Hydrochloride via Cremophor(®) El-Based Liquisolid Tablets.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  LST-18 succeeded in increasing oral FXD bioavailability by 62% and reducing Tmax to 2.16 h.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: Soad Ali
authors.initials: SA
authors.lastname: Yehia
authors.affiliation: Department of Pharmaceutical Technology, National Research Center, Dokki, Giza, Egypt.
authors.forename: Mohamed Shafik
authors.initials: MS
authors.lastname: El-Ridi
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: Mina Ibrahim
authors.initials: MI
authors.lastname: Tadros
authors.affiliation: Faculty of Pharmacy and Pharmaceutical Industries, Sinai University, Sinai, Egypt.
authors.forename: Nolwa Gamal
authors.initials: NG
authors.lastname: El-Sherif
keywords: Cremophor® EL; Fexofenadine hydrochloride; Liquisolid tablets; Oral bioavailability; Pharmacokinetics
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