title: The gut in the beaker: Missing the surfactants?
abstract: Gastrointestinal drug administration is the preferred route for the majority of drugs however, the natural physiology and physicochemistry of the gastrointestinal tract is critical to absorption but complex and influenced by factors such as diet or disease. The pharmaceutical sciences drive for product consistency has led to the development of in vitro product performance tests whose utility and interpretation is hindered by the complexity, variability and a lack of understanding. This article explores some of these issues with respect to the drug, formulation and the presence of surfactant excipients and how these interact with the natural bile salt surfactants. Interactions start in the mouth and during swallowing but the stomach and small intestine present the major challenges related to drug dissolution, solubility, the impact of surfactants and supersaturation along with precipitation. The behaviour of lipid based formulations and the influence of surfactant excipients is explored along with the difficulties of translating in vitro results to in vivo performance. Possible future research areas are highlighted with the conclusion that, "a great deal of work using modern methods is still required to clarify the situation".
authors.affiliation: Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, Scotland, UK. Electronic address: c.g.wilson@strath.ac.uk.
authors.forename: Clive G
authors.initials: CG
authors.lastname: Wilson
authors.affiliation: Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, Scotland, UK.
authors.forename: Gavin W
authors.initials: GW
authors.lastname: Halbert
authors.affiliation: Capsugel, Encap Drug Delivery, Livingston, EH53 0TH, Scotland, UK.
authors.forename: Jenifer
authors.initials: J
authors.lastname: Mains
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005079:Excipients / Q000737:chemistry; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008055:Lipids / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D005079:Excipients; D008055:Lipids; D004364:Pharmaceutical Preparations; D013501:Surface-Active Agents
keywords: Bile salt; Formulation; Gastrointestinal tract; Lipid-based formulation; Physiology; Surfactant