Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets

Polim Med. 2016 Jul-Dec;46(2):117-127. doi: 10.17219/pim/68170.

Abstract

Background: Norfloxacin is fluoroquinolone anti-infective used in the treatment of urinary tract infections, prostatitis, gonorrhea and genital tract infections. It has plasma half life of 3 to 4 h requiring multiple dosing in the treatment. Releaseretarding polymers can be used to modulate the drug release of norfloxacin.

Objectives: The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets.

Material and methods: Norfloxacin was procured as a gift sample from Concept Pharma Ltd. Aurangabad (India) and HPMC K100M was procured as a gift sample from Colorcon Asia Pvt. Ltd., Goa (India). The tablets were prepared by direct compression method and various pharmaceutical parameters were evaluated.

Results: It was observed that all tablet formulations F1-F9 retained the drug release up to 12 h with good floating property but only Batch-F4 complies with the USP dissolution limits with a minimum floating lag time. The drug release kinetics were evaluated by the model-dependent (curve fitting) method using PCP Disso v3 software shows Batch-F4 shows to best fit with Peppas model for which R2 value was 0.9921 and the release exponent value was 0.6892.

Conclusions: The drug release kinetics study indicates that the floating tablets release the drug by diffusion followed by erosion mechanism. Obtained in-vitro drug release data was analyzed by design expert software for drug release at first hour and at 12th h values and found that release the selected independent variables like HPMC K100M and sodium alginate concentration has a significant effect on drug release.

Keywords: drug dissolution; floating drug delivery systems; gastroretentive drug delivery systems; norfloxacin.

MeSH terms

  • Alginates / chemistry*
  • Delayed-Action Preparations*
  • Drug Liberation*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Hypromellose Derivatives / chemistry*
  • Kinetics
  • Norfloxacin / pharmacokinetics*
  • Tablets*

Substances

  • Alginates
  • Delayed-Action Preparations
  • Hexuronic Acids
  • Tablets
  • Hypromellose Derivatives
  • Glucuronic Acid
  • Norfloxacin