TY  - JOUR
T1  - Oral Formulation Design Should Optimize Temporal Exposure Rather Than Dissolution Alone
A1  - Pieter Botha
A1  - Anel Van Wyk
A1  - Johan Marais
JF  - International Journal of Pharmaceutical Research and Allied Sciences
JO  - Int J Pharm Res Allied Sci
SN  - 2277-3657
Y1  - 2025
VL  - 14
IS  - 3
DO  - 10.51847/LLFtAW7hvk
SP  - 113
EP  - 123
N2  - Dissolution remains indispensable to oral formulation development, but its interpretation becomes incomplete when the quantity dissolved is treated as a sufficient surrogate for the drug exposure that can actually be generated from a dosage form. Oral absorption occurs within a moving physiological system in which gastric emptying, intestinal transit, changing luminal composition, formulation-state transformations, supersaturation, precipitation, re-solubilization, permeability, food, and patient physiology alter both the amount and the timing of drug available for uptake. A formulation that dissolves rapidly under one experimental condition may therefore produce no exposure advantage if release occurs before an absorptive opportunity, if dissolved drug becomes nonabsorbable, if precipitation precedes uptake, or if physiological variability shifts the sequence of formulation and gastrointestinal states. This Perspective argues for a time-resolved formulation-design objective centered on the trajectory of exposure-relevant drug availability rather than dissolution magnitude alone. Evidence from biorelevant dissolution, dissolution–permeation systems, dynamic gastrointestinal models, formulation-state studies, food-effect research, and physiologically based modeling is integrated while preserving molecule-, product-, dose-, physiological-, and model-specific boundaries. The resulting synthesis treats dissolution as one necessary process within a temporally coupled formulation–gastrointestinal–absorption system.
UR  - https://ijpras.com/article/oral-formulation-design-should-optimize-temporal-exposure-rather-than-dissolution-alone-zv35c4rrpiayooy
ER  -