Regional Intestinal Drug Absorption Biopharmaceutics and Drug Formulation

• Other Authors: Gonzalez-Alvarez, Maria Isabel (Editor), Dahan, Arik (Editor)
• Format: Electronic Book Chapter
• Language: English
• Published: Basel MDPI - Multidisciplinary Digital Publishing Institute 2022
• Subjects: Medicine; Pharmaceutical industries; bioequivalence; Biopharmaceutics Classification System; in vitro; dissolution test; pravastatin; oral absorption; in silico modeling; GastroPlus; Phoenix WinNonlin; pharmacokinetics; clinical studies; ibuprofen; manometry; gastrointestinal; mechanistic modeling; PBPK; PBBM; disintegration; dissolution; enteric-coated; ICH; quality control; regional intestinal permeability; permeation enhancers; absorption-modifying excipients; oral peptide delivery; intestinal perfusion; pharmaceutical development; controlled release drug product; biopharmaceutics classification system; drug solubility; drug permeability; location-dependent absorption; segregated flow intestinal model (SFM); traditional model (TM); route-dependent intestinal metabolism; first-pass effect; drug-drug interactions; DDI; in vitro in vivo extrapolations; IVIVE; zero-order absorption; first-order absorption; combined zero- and first-order absorption; transit compartment absorption model; in situ perfusion; microdevices; shape; mucoadhesion; colon absorption; nutrient digestion; nutrient absorption; gastrointestinal hormone; postprandial glycaemia; energy intake; region of the gut; obesity; type 2 diabetes; Franz-PAMPA; BCS drugs; biomimetic membrane; Franz cell; passive drug transport; BCS class IV drugs; segmental-dependent intestinal permeability; intestinal absorption; oral drug delivery; biopharmaceutics; physiologically-based pharmacokinetic (PBPK) modeling; furosemide; intestinal permeability; human colon carcinoma cell layer (Caco-2); hierarchical support vector regression (HSVR); drug absorption; drug solubility/dissolution; regional/segmental-dependent permeability and absorption
• Online Access: DOAB: download the publication; DOAB: description of the publication

The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In the book "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation" we aim to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.