Gastric Pre-Processing Is an Important Determinant of the Ability of Medium-Chain Lipid Solution Formulations to Enhance Oral Bioavailability in Rats

The dynamic gastric environment and its impact on drug and formulation behaviour

“…Bypassing the gastric compartment resulted in a decrease in cinnarizine bioavailability (Lee et al, 2013).…”

Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach

“…The report concluded that rapid transfer of medium chain formulation to intestinal mixed micelles possibly was achieved by efficient dispersion and partial digestion in stomach. Also absorption in the upper intestine prior to drug precipitation was preferred [ 48 ].…”

The Effect of Composition and Gastric Conditions on the Self-Emulsification Process of Ibuprofen-Loaded Self-Emulsifying Drug Delivery Systems: A Microscopic and Dynamic Gastric Model Study

“…15) to suggest that the digestion of the SEDDSs plays a leading role in bioavailability enhancement, as is now well established for conventional lipid delivery systems (17,18). A recent study focused on the evaluation of the impact of gastric digestion on the bioavailability of the model drug cinnarizine from lipid-based formulations composed of medium-and long-chain lipids (19). The results showed that the bioavailability of the poorly water-soluble drug administered orally to rats was higher than that of the same formulation administered intraduodenally, suggesting a pivotal role played by gastric processing.…”

“…There is compelling evidence that the behaviour of SEDDSs is highly species-dependent, this being ascribed to the amount of fluid within the gastrointestinal tract having an effect on the extent of self-emulsification (19,20). In humans, gastric digestion of either coarse (>20 μm) or fine (1 μm) emulsions has been shown to result in droplets between 15 and 20 μm, irrespective of the initial size, as a product of the enzymatic digestion and shear forces in the stomach (21,22).…”