Journal ArticleDOI
In vitro model for ciclosporin intestinal absorption in lipid vehicles.
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TLDR
The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vivo and olive oil was a significantly better vehicle than MCT, whereas the difference between both lipids was only a trend in the digested state.Abstract:
The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vitro. The effect of the intestinal lipid digestion was considered on the partition of the drug from olive oil or middle-chain triglyceride (MCT) into phases of simulated intestinal content. The phases obtained after ultracentrifugation were analyzed for their Ciclosporin content and characterized for their lipid classes. For both lipid vehicles the presence of lipolysis products did not promote the partition of the drug into the aqueous phase. The absorption in vivo was not related to the drug amount in the aqueous phase and in the oil phase. Therefore, phase quantification in vitro cannot simulate the dynamics of in vivo absorption events following application of a poorly water-soluble drug in a lipid vehicle.read more
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Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs
TL;DR: The mechanisms by which lipids and lipidic excipients affect the oral absorption of lipophilic drugs are detailed and a perspective on the possible future applications of lipid-based delivery systems is provided.
Journal ArticleDOI
In vitro human digestion models for food applications
TL;DR: A survey of in vitro digestion models found that the most predominant food samples tested were plants, meats, fish, dairy, and emulsion-based foods, and the most frequently used biological molecules included in the digestion models were digestive enzymes, bile salts, and mucin.
Journal ArticleDOI
Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies.
TL;DR: The properties of excipients are discussed, the formulation strategies that can be used for each type of lipid formulation are outlined, and a framework for the in vitro testing of each type is suggested.
Journal ArticleDOI
Enhancing intestinal drug solubilisation using lipid-based delivery systems.
TL;DR: The mechanistic rationale which underpins the use of lipid-based delivery systems to enhance drug solubilisation is described and the available literature describing increases in oral bioavailability after the administration of lipid solution, suspension and self-emulsifying formulations is reviewed.
Journal ArticleDOI
Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH
TL;DR: Case studies are presented in which postprandial changes in bioavailability are rationalized in terms of the sensitivity of the physicochemical properties of the administered drug to the altered GI environment.
References
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Clinical Pharmacokinetics of Cyclosporin
TL;DR: Therapeutic drug monitoring of cyclosporin is essential for several reasons, including minimising drug toxicity by maintaining trough concentrations below that which toxicity is most likely to occur, and monitoring for compliance since patient non-compliance with drug regimens is a significant reason for graft loss after 60 days.
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Micelle Formation by Bile Salts: Physical-Chemical and Thermodynamic Considerations
Martin C. Carey,Donald Small +1 more
TL;DR: While bile salts increase slightly the solubility of relatively nonpolar molecules (such as cholesterol or fatty acids), they have a striking capacity to render soluble certain important insoluble molecules of biological importance such as phospholipids and monoglycerides.
Journal ArticleDOI
Watching fat digestion
John S. Patton,Martin C. Carey +1 more
TL;DR: During fat digestion a number of physicochemical events can be seen directly by light microscopy, including hydrolysis of emulsified fat droplets by human pancreatic lipase and the sequential formation of two visible product phases.