Evaluation of the in-vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products

• Published in: Journal of pharmacy and pharmacology 2002-01, Vol.54 (1), p.29-41
• Main Authors: Sek, Leab, Porter, Christopher J. H., Kaukonen, Ann Marie, Charman, William N.
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Caprylates - metabolism; Chromatography, Thin Layer; Digestion - physiology; General pharmacology; Glycerides - metabolism; Lipolysis - physiology; Medical sciences; Models, Biological; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Soybean Oil - metabolism; Structure-Activity Relationship; Triglycerides - metabolism
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1211/0022357021771896

An evaluation of the in‐vitro digestion profile and phase behaviour of the common formulation lipids Miglyol 812 (medium chain triglyceride, MCT), Capmul MCM (C8/C10 monoglyceride/diglyceride mixture), soybean oil (long chain triglyceride, LCT) and Maisine 35‐1 (C18 monoglyceride/diglyceride mixture), is described. Experiments were conducted using titrimetric, high‐performance thin‐layer chromatographic (HPTLC) and ultracentrifugational techniques under model fasted and post‐prandial intestinal conditions. The rate and extent of digestion of the medium chain lipids was greater than the corresponding long chain lipids, and independent of bile salt concentration, with complete conversion to monoglyceride and fatty acid occurring after 30 min digestion. The long chain lipid digests separated into an oily phase (containing undigested triglyceride and diglyceride), an aqueous phase (containing bile salt, fatty acid and monoglyceride) and a pellet phase (containing approximately 5 mM of fatty acid, presumably as an insoluble soap) after ultracentrifugation. Higher proportions of long chain fatty acid and monoglyceride were dispersed into the aqueous phase with increasing bile salt concentrations. In contrast, medium chain lipolytic products separated only into an aqueous phase and a pellet fraction in a bile‐salt‐independent manner. The digestion of both the C8/C10 and C18 monoglyceride/diglyceride lipid mixtures was more rapid than the corresponding triglyceride, especially at early time points. This investigation provides insight into the relative digestion kinetics of medium chain and long chain lipids and provides information regarding the phase behaviour of their lipolytic products under conditions modelled on those expected after oral administration. The data also provide a background for improved understanding of the potential utility of long chain and medium chain lipid‐based formulations.