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Evaluation of the in-vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products
Abstract
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 ea…
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MC blends of mono-/di-glycerides were rapidly digested, forming an aqueous dispersed phase or a precipitated fraction.
“Alternatively, the relatively poor performance of MCM systems may have reflected a higher precipitation risk from MC systems as observed in a study by Sek et al. whereby MC blends of mono-/di-glycerides were rapidly digested, forming an aqueous dispersed phase or a precipitated fraction (Sek et al., 2002).”
From Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption (2020) · cites this paper as Sek et al., 2002
LC blends of glycerides were more slowly digested, with the undigested oily phase still present throughout the 30-minute digestion.
“In contrast, LC blends of glycerides were more slowly digested, the undigested oily phase still being present throughout the 30-minutes digestion (Sek et al., 2002).”
From Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption (2020) · cites this paper as Sek et al., 2002
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Griffin, B. T., Kuentz, M., Vertzoni, M., Kostewicz, E. S., Fei, Y., Faisal, W., Stillhart, C., O’Driscoll, C. M., Reppas, C., & Dressman, J. B. (2014) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2013.10.016 · Cited by 126
Ilie, A.-R., Griffin, B. T., Brandl, M., Bauer-Brandl, A., Jacobsen, A.-C., Vertzoni, M., Kuentz, M., Kolakovic, R., & Holm, R. (2020) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2020.105452 · Cited by 33
“…the relatively poor performance of MCM systems may have reflected a higher precipitation risk from MC systems as observed in a study by Sek et al. whereby MC blends of mono-/di-glycerides were rapidly digested, forming an aqueous dispersed phase or a precipitated fraction (Sek et al., 2002).”
BackgroundInfluential
Metadata
- Authors
- Sek, L., Porter, C. J. H., Kaukonen, A. M., & Charman, W. N.
- Affiliations
- Monash University (AU)
- Venue
- Journal of Pharmacy and Pharmacology
- Publisher
- Oxford University Press (OUP)
- Published
- 2002-01-01
- Volume
- 54
- Issue
- 1
- Pages
- 29-41
- ISSN
- 0022-3573 (ISSN-L)
- 2042-7158
- OpenAlex
- W1979049827
- Cited by
- 304
- References
- 1
- Citations by year
- 2026: 4 · 2025: 13 · 2024: 11 · 2023: 12 · 2022: 12 · 2021: 15 · 2020: 14 · 2019: 17 · 2018: 22 · 2017: 14 · 2016: 19 · 2015: 21 · 2014: 15 · 2013: 16 · 2012: 19
- FWCI
- 9.13
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model (vor)
- Locations
- Journal of Pharmacy and Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Agricultural and Biological Sciences › Food Science › Proteins in Food Systems
- Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- in vitro digestion, medium-chain triglycerides, long-chain triglycerides, lipolysis, phase behavior, bile salts, monoglycerides, diacylglycerol, fatty acids, lipid-based formulations, Miglyol 812, Capmul MCM, soybean oil, digestion kinetics
- MeSH terms
- Caprylates, Chromatography, Thin Layer, Digestion, Glycerides, Lipolysis, Models, Biological, Soybean Oil, Structure-Activity Relationship, Triglycerides
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