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Book
Regional Intestinal Drug Absorption : Biopharmaceutics and Drug Formulation
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

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.

Keywords

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 --- 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


Book
Transmucosal Absorption Enhancers in the Drug Delivery Field
Authors: --- ---
ISBN: 3039218492 3039218484 Year: 2020 Publisher: MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Development of strategies to assist the movement of poorly permeable molecules across biological barriers has long been the goal of drug delivery science. In the last three decades, there has been an exponential increase in advanced drug delivery systems that aim to address this issue. However, most proprietary delivery technologies that have progressed to clinical development are based on permeation enhancers (PEs) that have a history of safe use in man. This Special Issue entitled “Transmucosal Absorption Enhancers in the Drug Delivery Field” aims to present the current state-of-the-art in the application of PEs to improve drug absorption. Emphasis is placed on identification of novel permeation enhancers, mechanisms of barrier alteration, physicochemical properties of PEs that contribute to optimal enhancement action, new delivery models to assess PEs, studies assessing safety of PEs, approaches to assist translation of PEs into effective oral, nasal, ocular and vaginal dosage forms and combining PEs with other delivery strategies.

Keywords

chitosan --- intestinal epithelial cells --- ocular delivery --- amphiphilic polymers --- cornea --- tight junction modulator --- cyclodextrin --- permeability --- gemini surfactant --- transferrin --- compound 48/80 --- epithelial permeability --- cervicovaginal tumors --- nanoparticles --- confocal laser scanning microscopy --- safety --- formulation --- salcaprozate sodium --- intestinal absorption --- FITC-dextran --- curcumin --- block copolymers --- nasal vaccination --- whole leaf --- brush border --- ocular drug delivery --- vaccine adjuvant --- nanoparticle --- nasal delivery --- efflux --- permeation enhancers --- absorption enhancers --- nose to brain delivery --- small intestine --- epithelium --- CNS disorders --- absorption modifying excipients --- insulin --- absorption enhancer --- gel --- intestinal delivery --- thermogel system --- Caco-2 --- biocompatibility studies --- absorption enhancement --- man --- PN159 --- poorly absorbed drug --- tryptophan --- tight junction --- oral macromolecule delivery --- penetration enhancer --- intestinal permeation enhancers --- nanocrystals --- simvastatin --- nanomedicine --- enterocyte --- N-dodecyl-?-D-maltoside (DDM) --- cell-penetrating peptide --- quaternization --- KLAL --- nasal --- nasal permeability --- transmucosal drug delivery --- Caco-2 cells --- mast cell activator --- penetration enhancers --- drug delivery --- nose-to-brain --- bioenhancer --- polymeric micelles --- mucoadhesion --- cell-penetrating peptide (CPP) --- simulated intestinal fluid --- vaginal delivery --- nasal formulation --- pharmacokinetic interaction --- sodium caprate --- clinical trial --- transmucosal permeation --- drug absorption enhancer --- sugar-based surfactants --- nanocapsules --- imatinib --- teriparatide --- osteoporosis --- hydrophobization --- F-actin --- combined microsphere --- transepithelial electrical resistance --- oral delivery --- ocular conditions --- metabolism --- antimicrobial peptide --- permeation enhancer --- drug administration --- antiepileptic drug --- amino acid --- in vivo studies --- sodium cholate (NaC) --- epithelial transport --- preclinical --- nose to brain transport --- pharmacokinetics --- chitosan derivatives --- ophthalmology --- tight junctions --- sheep --- cationic functionalization --- GLP-1 --- pulmonary --- and liposome --- cytochrome P450 --- claudin --- P-glycoprotein --- in situ hydrogel --- mucoadhesiveness --- PTH 1-34 --- Aloe vera --- oral peptides


Book
Regional Intestinal Drug Absorption : Biopharmaceutics and Drug Formulation
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

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.

Keywords

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


Book
Regional Intestinal Drug Absorption : Biopharmaceutics and Drug Formulation
Authors: ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

Loading...
Export citation

Choose an application

Bookmark

Abstract

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.

Keywords

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

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