Sustained release gastroretentive tablet of metformin hydrochloride based on poly (acrylic acid)-grafted-gellan

Int J Biol Macromol. 2017 Mar:96:137-148. doi: 10.1016/j.ijbiomac.2016.12.022. Epub 2016 Dec 9.

Abstract

Development of a gastroretentive sustained release tablet of metformin based on poly (acrylic acid)-grafted-gellan (PAAc-g-GG) is the main purpose of this study. At first, PAAc-g-GG was synthesized by microwave-promoted free radical initiation method using cerric (IV) ammonium nitrate (CAN) as redox initiator and characterized by elemental analysis, FTIR, DSC-TGA, 13C NMR, biodegradation and viscosity study. The synthetic parameters were optimized by 23 full factorial design using Design Expert software. Acute oral toxicity and histological studies were also performed as per OECD guideline. Tablets were then prepared employing wet granulation method using PAAc-g-GG and evaluated for various physical characters, in vitro drug release, ex-vivo mucoadhesion and swelling. Compatibility between drug and excipients was checked by DSC and FTIR analysis. The F3 batch showed excellent mucoadhesion and sustained drug release over a period of 10h with dissolution similarity factor, f2=77.43. Kinetic modeling unveiled Case-1 Fickian diffusion based drug release mechanism.

Keywords: Mucoadhesive; Poly (acrylic acid)-grafted-gellan; Sustained release.

MeSH terms

  • Acrylic Resins / chemistry*
  • Adhesiveness
  • Animals
  • Delayed-Action Preparations
  • Drug Carriers / chemistry*
  • Drug Liberation*
  • Female
  • Gastric Mucosa / chemistry
  • Gastric Mucosa / metabolism*
  • Metformin / chemistry*
  • Metformin / metabolism*
  • Mice
  • Microwaves
  • Polysaccharides, Bacterial / chemistry*
  • Tablets
  • Viscosity

Substances

  • Acrylic Resins
  • Delayed-Action Preparations
  • Drug Carriers
  • Polysaccharides, Bacterial
  • Tablets
  • carbopol 940
  • gellan gum
  • Metformin