Study of controlled-release floating tablets of dipyridamole using the dry-coated method

Drug Dev Ind Pharm. 2018 Jan;44(1):116-124. doi: 10.1080/03639045.2017.1386198. Epub 2017 Oct 17.

Abstract

Dipyridamole (DIP), having a short biological half-life, has a narrow absorption window and is primarily absorbed in the stomach. So, the purpose of this study was to prepare controlled-release floating (CRF) tablets of dipyridamole by the dry-coated method. The influence of agents with different viscosity, hydroxypropylmethylcellulose (HPMC) and polyvinylpyrollidon K30 (PVP K30) in the core tablet and low-viscosity HPMC and PVP K30 in the coating layer on drug release, were investigated. Then, a study with a three-factor, three-level orthogonal experimental design was used to optimize the formulation of the CRF tablets. After data processing, the optimized formulation was found to be: 80 mg HPMC K4M in the core tablet, 80 mg HPMC E15 in core tablet and 40 mg PVP K30 in the coating layer. Moreover, an in vitro buoyancy study showed that the optimized formulation had an excellent floating ability and could immediately float without a lag time and this lasted more than 12 h. Furthermore, an in vivo gamma scintigraphic study showed that the gastric residence time of the CRF tablet was about 8 h.

Keywords: Dipyridamole; buoyancy; controlled-release floating tablets; gamma scintigraphic; orthogonal experimental design.

MeSH terms

  • Chemistry, Pharmaceutical / methods*
  • Delayed-Action Preparations
  • Dipyridamole / chemistry*
  • Dipyridamole / pharmacokinetics
  • Excipients / chemistry*
  • Half-Life
  • Hypromellose Derivatives / chemistry*
  • Povidone / analogs & derivatives*
  • Povidone / chemistry*
  • Tablets / chemistry*
  • Tablets / pharmacokinetics
  • Viscosity

Substances

  • Delayed-Action Preparations
  • Excipients
  • Tablets
  • polyvinylpyrollidon K30
  • Hypromellose Derivatives
  • Dipyridamole
  • Povidone