Biorelevant in-vitro performance testing of orally administered dosage forms

J Pharm Pharmacol. 2012 Jul;64(7):919-30. doi: 10.1111/j.2042-7158.2012.01474.x. Epub 2012 Mar 27.

Abstract

Objectives: This review focuses on the evolution and current status of biorelevant media and hydrodynamics, and discusses the usefulness of biorelevant performance testing in the evaluation of specific dosage form related lumenal processes.

Key findings: During the last 15 years our knowledge of the gastrointestinal environment (including the lower gut) has improved dramatically and biorelevant media composition and, to a lesser extent, biorelevant hydrodynamics, have been refined. Biorelevant dissolution/release testing is useful for the evaluation of formulation and food effects on plasma levels after administration of immediate release dosage forms containing low solubility compounds and after administration of extended release products. Lumenal disintegration times of immediate release dosage forms and the bile acid sequestering activity of resins in the lumen can also be successfully forecasted with biorelevant in vitro testing.

Summary: Biorelevant in-vitro performance testing is an important tool for evaluating intralumenal dosage form performance. Since the formulation of new active pharmaceutical ingredients for oral delivery is more challenging than ever before, efforts to improve the predictability of biorelevant tests are expected to continue.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / standards
  • Dosage Forms / standards*
  • Gastrointestinal Tract / physiology*
  • Hydrodynamics
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / blood
  • Quality Control
  • Solubility

Substances

  • Delayed-Action Preparations
  • Dosage Forms
  • Pharmaceutical Preparations