ABSTRACT
Dissolution of drugs from their oral dosage forms in the gas-
trointestinal (GI) tract is a prerequisite to the absorption process.
Examination of dissolution attributes of a drug from its formulation
is of critical importance in the development of oral drug products.
It is highly desirable that the in vitro dissolution test for drug
products closely mimics the in vivo situation in preclinical species
and human subjects in order to assess its bioperformance.1−3
Biorelevant media such as fasted simulated gastric fluids (FaSGF),
fasted simulated small intestine fluids (FaSSIF), fed simulated small
intestine fluids (FeSSIF), and bicarbonate buffers have been widely
used to simulate conditions in the GI tract for in vitro dissolution
and solubility assessments,4−5 especially for Biopharmaceutical Classification System (BCS) type II and IV drugs. Biorelevant
dissolution test methods with appropriate simulated media and
hydrodynamics are useful during early stages of drug development
for identifying the key issues associated with the biopharmaceutical
performance of the drug (i.e., solubility limited-or dissolution-
limited absorption, food effect, precipitation in the small intestine,
etc.) and assessing manufacturability of the drug product with its
impact on bioperformance. Application of biorelevant dissolution
tests can effectively facilitate formulation selection and optimization
during drug product development.
