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Archives of Pharmacal Research

, Volume 38, Issue 4, pp 522–533 | Cite as

Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability

  • Roshan Pradhan
  • Tuan Hiep Tran
  • Ju Yeon Choi
  • Im Soon Choi
  • Han-Gon Choi
  • Chul Soon YongEmail author
  • Jong Oh KimEmail author
Research Article

Abstract

The purpose of this study was to improve the gastric solubility and bioavailability of rebamipide (RBM) by preparing the RBM solid dispersion tablet (RBM-SDT) from solid dispersion powder prepared by spray-drying technique. For preparation of rebamipide solid dispersions (RBM-SDs), solubility study was performed in various hydrophilic carriers and alkalizers, among which sodium alginate and sodium carbonate were selected as the hydrophilic polymer and alkalizer, respectively. Different combinations of drug–polymer–alkalizer were dissolved in aqueous solution and spray-dried in order to obtain solid dispersions. Noticeable improvement in aqueous solubility (approximately 200 times) and in vitro dissolution rate was observed by RBM-SDs, compared to RBM powder. The optimized formulation of RBM-SD powder consisted of RBM powder/sodium alginate/sodium carbonate at the weight ratio of 1/2/2. The transformation of crystalline RBM to amorphous RBM-SD powder was clearly demonstrated by powder X-ray diffraction, differential scanning calorimetry (DSC) and scanning electron microscopy. The optimized RBM-SD was formulated in tablet dosage form, containing approximately 2 % sodium lauryl sulphate and poloxamer F68 as wetting agents. The RBM-SDT exhibited enhanced dissolution in hydrochloric acid buffer (pH 1.2) and distilled water. Moreover, pharmacokinetic study in rats showed higher AUC and Cmax for RBM-SDT than those for RBM powder and commercial product. Thus, the developed RBM-SDT formulation can be more efficacious for improving oral bioavailability of RBM.

Keywords

Rebamipide Solubility Solid dispersion Spray-drying Bioavailability 

Notes

Acknowledgments

This study was supported by a grant from the Medical Cluster R&D Support Project of Daegu Gyeongbuk Medical Innovation Foundation, Republic of Korea (2013) (No. HT13C0011).

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Copyright information

© The Pharmaceutical Society of Korea 2014

Authors and Affiliations

  • Roshan Pradhan
    • 1
  • Tuan Hiep Tran
    • 1
  • Ju Yeon Choi
    • 1
  • Im Soon Choi
    • 1
  • Han-Gon Choi
    • 2
  • Chul Soon Yong
    • 1
    Email author
  • Jong Oh Kim
    • 1
    Email author
  1. 1.College of PharmacyYeungnam UniversityGyongsanSouth Korea
  2. 2.College of PharmacyHanyang UniversityAnsanSouth Korea

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