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AAPS PharmSciTech

, Volume 19, Issue 7, pp 3277–3286 | Cite as

Development and Evaluation of Compression Coating Gastro-Floating Tablet of Alfuzosin Hydrochloride for Zero-Order Controlled Release

  • Ling Gong
  • Yanyan Sun
  • Miao Yu
  • Ying Gao
  • Meijuan Zou
  • Gang Cheng
Research Article
  • 26 Downloads

ABSTRACT

Alfuzosin hydrochloride is an appropriate candidate drug to prepare a gastro-retention controlled release dosage form since it demonstrates a narrow absorption window in the proximal section of the gastrointestinal tract with a short half-life. The purpose of the present study was to develop and optimize a gastro-floating tablet of alfuzosin hydrochloride by using the compression coating method for controlling drug release in a controlled manner. The floating tablets were developed utilizing hydroxypropyl methylcellulose and carbomer as matrix materials. The impact of formulation factors on buoyancy property and in vitro drug release of the floating tablet was investigated. The “similarity factor” (f2) was used as the indicator for the optimization of the formulations. Furthermore, in vivo pharmacokinetic study in rabbits and correlation of in vitro/in vivo study were also performed. It was found that the optimized formulation F9 could float immediately less than 2 min and remain lastingly buoyant over 24 h and follow zero-order release kinetics well. In comparison with the commercially available prolonged release tablets XATRAL® XL, the prepared floating tablet exhibited similar pharmacokinetic parameters (Cmax, Tmax, t1/2, and AUC0 − t) and plasma concentration versus time profile. Moreover, it indicated from the correlation of in vitro/in vivo study that the floating tablets exhibited a good correlation of in vitro/in vivo. In summary, the compression coating gastro-floating tablets might be a promising drug delivery system for alfuzosin hydrochloride to control drug release.

KEY WORDS

alfuzosin hydrochloride compression coating technology gastro-floating tablet controlled release pharmacokinetics 

Notes

Compliance with Ethical Standards

Conflict of Interest

The authors report no conflict of interest.

Supplementary material

12249_2018_1168_Fig7_ESM.png (1.4 mb)
Fig. S1

Supplemental figure. In vivo evaluation of the gastric retention time of the optimized formulation by near-infrared fluorescence imaging, (A) before the administration, (B) at 1 h, (C) 2 h, (D) 3 h, (E) 4 h, (F) 5 h, (G) 6 h, (H) 7 h after oral administration, respectively (PNG 1452 kb)

12249_2018_1168_MOESM1_ESM.tif (21 mb)
High Resolution Image (TIF 21531 kb)

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Ling Gong
    • 1
  • Yanyan Sun
    • 1
  • Miao Yu
    • 1
  • Ying Gao
    • 1
  • Meijuan Zou
    • 1
  • Gang Cheng
    • 1
  1. 1.Department of Pharmaceutics, School of PharmacyShenyang Pharmaceutical UniversityShenyangChina

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