Buoyancy-generating agents for stomach-specific drug delivery: an overview with special emphasis on floating behavior

J Pharm Pharm Sci. 2015;18(1):77-100. doi: 10.18433/j3602k.

Abstract

Gastric retentive drug delivery provides a promising technology exhibiting an extended gastric residence and a drug release independent of patient related variables. It is usually useful in improving local gastric treatment as well as overcoming drug-related problems .i.e. drugs having narrow absorption window, short half-life or low intestinal solubility. Buoyancy is considered one of the most promising approaches for gastro-retention of dosage forms. Floating drug delivery systems have a bulk density lower than gastric fluids and thus remain buoyant in the stomach causing an increase in gastric residence time. The buoyancy of these systems is attained by the aid of substances responsible to generate the low density. Various agents with different mechanisms were adopted either gas-generating agents, air entrapping swellable polymers, inherent low density substances, porous excipients, hollow/porous particles inducing preparation techniques or sublimating agents. Therefore, this review gives an exclusive descriptive classification of the different categories of these buoyancy-generating agents while representing the related research works. An overview is also conducted to describe relevant techniques assessing the floating behavior of such dosage forms either in vitro or in vivo. Finally, a collection representing FDA-approved floating pharmaceutical products is adopted with emphasis on the buoyancy-generating agent type used in each product.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems*
  • Excipients / chemistry*
  • Gastric Mucosa / metabolism
  • Half-Life
  • Humans
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / chemistry
  • Polymers / chemistry
  • Solubility

Substances

  • Excipients
  • Pharmaceutical Preparations
  • Polymers