The Adme Encyclopedia: A Comprehensive Guide on Biopharmacy and Pharmacokinetics

ISBN-13: 9783030848590 / Angielski / Twarda / 2022 / 1190 str.

Alan Talevi

Spis treści

• Drug dissolution and drug release
• Mathematical models of drug dissolution and drug release
• Diffusion layer model
• Danckwert’s model
Interfacial barrier model
• First order model
• Higuchi model
• Korsmeyer-Peppas model
• Hixson-Crowell model
Baker-Lonsdale model
• Weibull model
• In vitro dissolution testing
• Modalities of dissolution tests
• Biorelevant dissolution media

 

• Drug absorption
• Free diffusion
• Facilitated diffusion
Active transport
• Transcytosis
• pH partition theory
• pKa determination
• Factors impacting drug absorption

 

• Drug distribution
• Factors impacting drug distribution
• Real volume of distribution
Apparent volume of distribution
• Drug binding to plasma proteins
• Drug displacement
• Non-linear binding to plasma proteins
• Drug binding to tissue components
• One-compartment pharmacokinetic model
• Two-compartment pharmacokinetic model
• Central nervous system bioavailability
• Blood-brain barrier
log BB
• Kpuu

 

• Drug metabolism
• Functionalization reactions
• Synthetic reactions
• Cytochrome P450
• Phase III reactions
• Factors impacting on drug metabolism
• Genetic variants. Polymorphism
• Age
• Gender
• Environmental factors: enzyme induction
• Precision medicine
• Pharmacogenomic DNA chips
• Microsomes

 

•  Drug excretion
• Biliary excretion
Enterohepatic recycling
• Enterohepatic recycling and antibiotics
• Renal excretion
• Glomerular filtration
• Tubular reabsorption
• Tubular secretion
• Clearance
• Organ clearance

 

Routes of administration
• Oral route
• Migrating motor complex
• Enteric coating tablets
Food-drug interactions
• Gastric emptying
• Gastroretentive drug delivery systems
• Multiparticulate drug delivery systems
Gut microbiota
• Lipinski rule of five
• Permeation enhancers
• Intestinal perfusion models
• Bucal and sublingual route
Rectal route
• Intravenous route
• Intravenous bolus
• Intravenous infusion
• Technological considerations for intravenous administration
• Intramuscular administration
• Subcutaneous administration
• Specialized parenteral routes
• Pulmonary administration
• Nasal administration
• Transdermal administration
• Permeation enhancers

 

• Next generation drug delivery systems
Nanocarriers
• Surface-to-volume ratio
• Surface chemistry
• Nanotoxicology
• Drug release from nanocarriers
• Passive targeting
• Smart systems / stimuli-responsive systems
• Active targeting
• Mononuclear phagocyte system
• Absorption and distribution of nanocarriers
• Elimination of nanocarriers
• PEGylationADME
• Viral vectors

 

• Pharmacogenomics
• Enzyme polymorphism
• Transporter polymorphism
• Pharmacogenomics and pediatrics

 

Bioavailability and bioequivalence
• Bioavailability
• Systemic bioavailability
• Generic drugs
• Post-approval changes
• Bioequivalence
• Absolute bioavailability
• Mass balance studies
• Bioequivalence studies
• Reference and test products
Biopharmaceutical Classification System
• Biowaivers
• BCS subclasses
• Dissolution testing
• Pharmacodynamic studies

 

• Biopharmaceutical drug products
• Absorption of protein drugs
• Distribution of protein drugs
• Elimination of protein drugs
• ADME properties of insulins
• ADME properties of heparins
• ADME properties of gene-based biopharmaceuticals

 

Drug-drug and food-drug interactions
• Plasma protein binding DDI
• Membrane transport DDI
• Metabolism DDI
• FDI based on induction of gastrointestinal changes

 

• In vitro and in silico ADME predictions
• Polarized cell lines
• Caco-2
MDCK
• Solubility
• Dissolution testing
• QSPR/QSAR
• Expert rules
Central Nervous System Multiparameter Optimization
• Dynamic transit models
• Sandwich-cultured hepatocytes
• Single-cell expression systems
• Membrane vesicles
• Molecular dynamics simulations

 

• Drug tansporters
• ABC transporters
MDR1
• MRPs
• BCRP
• Solute carriers
• Organic anion transporters
Organic cation transporters
• Peptide transporters

 

• Non-linear pharmacokinetics
Linear pharmacokinetics
• Positive deviations from linear behavior
• Negative deviations from linear behavior

 

• Time-dependent pharmacokinetics

 

• Pharmacometrics and physiologic models

 

 

O autorze

Prof. Alan Talevi was born in Buenos Aires, 1980. He obtained his Pharmacy degree in 2004 and completed his PhD studies in 2007, both at the University of La Plata (UNLP, Argentina). Among other recognitions, he obtained the award for the best PhD thesis on Computational Chemistry from the Argentinean Chemical Society (2008), a Pacifichem Young Scholar Award (USA, 2010) and the Award to Scientific and Technological Production at UNLP (2016). Since 2010, he holds a permanent position at the Argentinean Council of Scientific and Technical Research (CONICET), where he currently occupies an Independent Researcher position, and since 2012 he is the professor in charge of the Biopharmacy/Pharmacokinetics course at the Faculty of Exact Sciences, UNLP. He has published over 80 articles in periodicals and more than 30 book chapters, mostly in the fields of machine learning, drug discovery and biopharmacy. He was elected Head of the Department of Biological Sciences of the Faculty of Exact Sciences, UNLP, between 2015 and 2017. In 2018 he became the Head of the Laboratory of Bioactive Research and Development (LIDeB, UNLP). External reviewer for several agencies and universities, including the Argentinean National Institute of Cancer, Argentinean National Agency of Scientific and Technical Promotion, Argentinean Ministry of Education, University of La República (Uruguay), University of Buenos Aires (Argentina), University of Córdoba (Argentina), University of Mar del Plata (Argentina), the National Agency of Scientific and Technical Promotion (Uruguay), the United Nations University, the National Science Center (Poland) and the “Victor Babes” University of Medicine an Pharmacy (Romania), CONCYTEC (Perú), and UK Research and Innovation (UK). Reviewer of more than 80 periodicals (https://publons.com/researcher/1667052/alan-talevi/), mostly in the fields of Cheminformatics, Drug Discovery, Drug Design and Pharmacology, including the Nature Communications, Scientific Reports, Journal of Medicinal Chemistry, Journal of Chemical Information and Modelling, Journal of Molecular Graphics and Modelling, Expert Opinion on Drug Delivery, Expert Opinion on Drug Discovery, Expert Opinion on Drug Metabolism and Toxicology, European Journal of Medicinal Chemistry, European Journal of Pharmacology, International Journal of Pharmaceutics, Journal of Pharmacy and Pharmacology. Member of the editorial board of the Latin American Journal of Pharmacy (from 2014 and continues). Guest editor of Mini-Reviews in Medicinal Chemistry, Frontiers in Chemistry and Current Drug Safety. Editor of the Antiepileptic Drug Discovery Novel Approaches volume of the Springer Protocols series (2016), and also of ADME Processes in Pharmaceutical Sciences Dosage, Design, and Pharmacotherapy Success (Springer, 2018). Editor of the imminent Springer Nature Computer-Aided Drug Discovery and Design series (ongoing). Editor of the book Biopharmaceutical processes (UNLP Publishing - EdULP, 2016). He has taught several courses in Argentina, Uruguay and Mexico. He has been recipient of several national and international research grants.

Blurb

The ADME Encyclopedia covers pharmacokinetic phenomena (Absorption, Distribution, Metabolism and Excretion processes) and their relationship with the design of pharmaceutical carriers and the success of drug therapies. It covers both basic and advance knowledge, serving as introductory material for students of biomedical careers and also as reference, updated material for graduates and professionals working in any field related to pharmaceutical sciences (medicine, pharmaceutical technology, materials science, medicinal chemistry).

Structured as alphabetically ordered entries and subentries, the Encyclopedia not only provides basic knowledge on ADME processes, but also detailed entries on some advanced subjects such as drug transporters, multi-drug resistance related to pharmacokinetic phenomena, last generation pharmaceutical carriers, pharmacogenomics, personalized medicine, bioequivalence studies, biowaivers, biopharmaceuticals, pharmacokinetic drug interactions or in silico and in vitro assessment of ADME properties.