Formulation of zein based compression coated floating tablets for enhanced gastric retention and tunable drug release

Eur J Pharm Sci. 2019 Apr 30:132:163-173. doi: 10.1016/j.ejps.2019.01.025. Epub 2019 Jan 26.

Abstract

The present study aimed to investigate the potential of zein (a protein obtained from corn) for development of gastroretentive floating tablets for the first time. A compression coated tablet design with outer floating layer and inner drug containing layer was followed to achieve floating over gastric fluid with sustained release of drug. Captopril was used as a model drug for this purpose. Eight formulations were developed and the influence of different components on drug release and floating behavior was evaluated. The drug in coating layer was found to be released at faster rate while sustained release behavior was observed from core layer. In vivo pharmacokinetic studies on rabbits showed significant increase in bioavailability and mean residence time (MRT). Moreover, radiographic study exhibited gastric retention of prepared tablets >12 h. In conclusion, zein can be used for development of gastroretentive floating tablets and by adjusting amount of different formulation factors, desired drug release rate can be achieved.

Keywords: Captopril; Floating tablets; Gastroretentive drug delivery systems; Oral controlled release; Zein.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Captopril / administration & dosage
  • Captopril / chemistry*
  • Captopril / pharmacokinetics*
  • Drug Design*
  • Drug Liberation
  • Female
  • Gastric Absorption
  • Gastric Mucosa / metabolism*
  • Rabbits
  • Solubility
  • Surface Properties
  • Tablets
  • Zein / chemistry*

Substances

  • Tablets
  • Zein
  • Captopril