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2 results on '"GCDC, glycochenodeoxycholate"'

1. The influence of the gut microbiota on the bioavailability of oral drugs

Author

Ying Han, Xintong Zhang, Wei Huang, Zhonggao Gao, and Mingji Jin

Subjects
SLC, solute carrier, Bioavailability, AMI, amiodarone, MPA, mycophenolic acid, TLCA, taurolithocholate, ASP, amisulpride, RA, rheumatoid arthritis, Review, NRs, nitroreductases, MDR1, multidrug resistance gene 1, NaGC, sodium glycholate, MATEs, multidrug and toxin extrusion proteins, NMEs, new molecular entities, 0302 clinical medicine, HFD, high fat diet, P-gp, P-glycoprotein, ACS, amphipathic chitosan derivative, Medicine, General Pharmacology, Toxicology and Pharmaceutics, LCA, lithocholic acid, 0303 health sciences, Gastrointestinal tract, IBD, inflammatory bowel disease, pKa, dissociation constant, RBC, red blood cell, FA, folate, OATs, organic anion transporters, 030220 oncology & carcinogenesis, MKC, monoketocholic acid, the GI tract, the gastrointestinal tract, AQP4, aquaporin 4, OCTNs, organic zwitterion/cation, T2D, type 2 diabetes, Gut microbiota, RM1-950, WHO, World Health Organization, 03 medical and health sciences, EcN, Escherichia coli Nissle 1917, Drug Transport Process, BDEPT, the bacteria-directed enzyme prodrug therapy, BCS, biopharmaceutics classification system, NEC, necrotizing enterocolitis, DRPs, digoxin reduction products, NaDC, sodium deoxycholate, Probiotics, CPP, cell-penetrating peptide, OCTs, organic cation transporters, TDCA, taurodeoxycholate, cgr operon, cardiac glycoside reductase operon, RA - Rheumatoid arthritis, DCA, deoxycholic acid, AA, ascorbic acid, BBR, berberine, Personalized medicine, BDDCS, the biopharmaceutics drug disposition classification system, SSZ, sulfasalazine, UDC, ursodeoxycholic acid, PPIs, proton pump inhibitors, BCRP, breast cancer resistance protein, CS, chitosan, Gut flora, Bioinformatics, PD, Parkinson's disease, SLN, solid lipid nanoparticle, SGLT-1, sodium-coupled glucose transporter 1, Oral administration, MRP2, multidrug resistance-associated protein 2, FAO, Food and Agriculture Organization of the United Nations, SVCT-1/2, the sodium-dependent vitamin C transporter-1/2, an OTC drug, an over-the-counter drug, CA, cholic acid, biology, ABC, ATP-binding cassette, T1DM, type 1 diabetes mellitus, NSAIDs, non-steroidal anti-inflammatory drugs, AR, azoreductase, GCDC, glycochenodeoxycholate, Drug delivery, GL, glycyrrhizic acid, PT, pectin, LPS, lipopolysaccharide, TME, the tumor microenvironment, T1D, type 1 diabetes, TCDC, taurochenodeoxycholate, Oral drugs, MDR1a, multidrug resistance protein-1a, SCFAs, short-chain fatty acids, CDCA, chenodeoxycholic acid, 030304 developmental biology, business.industry, dhBBR, dihydroberberine, biology.organism_classification, HTC, hematocrit, PWSDs, poorly water-soluble drugs, Colon-specific drug delivery system, stomatognathic diseases, SP, sulfapyridine, 5-ASA, 5-aminosalicylic acid, BSH, bile salt hydrolase, TCA, taurocholate, Therapeutics. Pharmacology, business
Abstract

Due to its safety, convenience, low cost and good compliance, oral administration attracts lots of attention. However, the efficacy of many oral drugs is limited to their unsatisfactory bioavailability in the gastrointestinal tract. One of the critical and most overlooked factors is the symbiotic gut microbiota that can modulate the bioavailability of oral drugs by participating in the biotransformation of oral drugs, influencing the drug transport process and altering some gastrointestinal properties. In this review, we summarized the existing research investigating the possible relationship between the gut microbiota and the bioavailability of oral drugs, which may provide great ideas and useful instructions for the design of novel drug delivery systems or the achievement of personalized medicine., Graphical abstract The gut microbiota may influence the bioavailability of oral drugs by the microbial enzyme activity, affecting the drug transport or changing the gastrointestinal properties. This may provide us some advice on preventing the possible drug–drug interaction and offer us some useful strategies for the drug delivery system design.Image 1

Published
2021

2. Impact of gastrointestinal tract variability on oral drug absorption and pharmacokinetics: An UNGAP review

Author

Christine M. Madla, Marlies Braeckmans, Mirko Koziolek, Christophe Matthys, Michael Grimm, Daniel Keszthelyi, Jef Stappaerts, Tim Vanuytsel, Laura E. McCoubrey, Mohammad Abdallah, Patrick Augustijns, Christos Reppas, Natalie L. Trevaskis, Brendan T. Griffin, Amitava Mitra, Nele Steenackers, Clive G. Wilson, José A. G. Agúndez, Jens Ceulemans, Maura Corsetti, Karel Allegaert, Maria Vertzoni, Abdul Basit, Werner Weitschies, Zahari Vinarov, and Pharmacy

Subjects
Male, TAG, Triacylglycerides, SITT, Small intestinal transit time, Physiology, Diseases, 02 engineering and technology, L-DOPA, Levodopa, GIT, Gastrointestinal tract, Food-Drug Interactions, 0302 clinical medicine, PBPK, Physiologically based pharmacokinetic modelling, TC, Taurocholate, Child, Pediatrics and geriatrics, media_common, TCDC, Taurochenodeoxycholate, ADME , Absorption, distribution, metabolism and excretion, CD, Cyclodextrin, CRA, Cannabinoid receptor agonist, CTT, Colon transit times, SBWC, Small bowel water content, HPMCP, Hydroxypropyl methylcellulose phtalate, HIV, Human immunodeficiency virus, HPMC, Hydroxypropyl methylcellulose, IBD, Inflammatory bowel disease, 0210 nano-technology, Drug, Physiologically based pharmacokinetic modelling, GCDC, Glycochenodeoxycholate, media_common.quotation_subject, COLONIC BACTERIAL METABOLISM, PPI, Proton pump inhibitors, Variation, BMI, Body mass index, Lyso-PC, Lyso-phosphatidylcholine, Anorexia, CV, Coefficient of variance, RS, 03 medical and health sciences, CIPO, Chronic intestinal pseudoobstruction, Pharmacokinetics, PROTON PUMP INHIBITORS, Drug formulation, GDC, Glycodeoxycholate, Humans, BCS, Biopharmaceutics classification system, OROCECAL TRANSIT-TIME, Aged, CI, Confidence interval, RYGB, Roux-en-Y gastric bypass, VEGF-C, Vascular endothelial growth factor C, DDI, Drug-drug interactions, t(max), Time to reach maximum plasma concentration, UDC, Ursodeoxycholate, IN-VITRO, IR, Immediate release, AUC, Area under the curve, TKI, Tyrosine kinase inhibitors, DAG, Diacylglycerides, Intestinal Absorption, ENTEROHEPATIC RECIRCULATION, IMMC, Inter-digestive migrating motor complex, NAPQI, N-acetyl-p-benzoquinone imine, variation, fasted and fed state, physiology, pediatrics and geriatrics, diseases, drug formulation Abbreviations list 5-FU, 5-fluorouracil, FaSSIF, Fasted state simulated intestinal fluids, MRI, Magnetic resonance imaging, AIDS, Acquired immunodeficiency syndrome, PD, Pharmacodynamic(s), Administration, Oral, Pharmaceutical Science, LYMPHATIC TRANSPORT, 030226 pharmacology & pharmacy, HPMC-AS, Hydroxypropyl methylcellulose acetate succinate, FaHIF, Fasted state human intestinal fluids, TDC, Taurodeoxycholate, SIBO, Small intestinal bacterial overgrowth, ADME, CYP, Cytochrome P450, Fasted and fed state, Area under the curve, Ursodeoxycholate, 021001 nanoscience & nanotechnology, GET, Gastric emptying time, NSAID, Nonsteroidal anti-inflammatory drug, Pharmaceutical Preparations, PEG, Polyethylene glycol, Drug development, Female, medicine.symptom, HUMAN INTESTINAL FLUID, CETP, Cholesterylester transfer protein, PC, Phosphatidylcholine, C(max), Maximum plasma concentration, OHM, 1-hydroxy-midazolam, DOSAGE FORMS, PK, Pharmacokinetic(s), TYROSINE KINASE INHIBITORS, medicine, FDA, U.S. Food and drug administration agency, D(v50), Median particle size by volume, SHORT-BOWEL SYNDROME, MAG, Monoacylglycerides, UNGAP, European network on understanding gastrointestinal absorption-related processes, business.industry, Gastrointestinal Tract, FFA, Free fatty acids, business, EHC, Enterohepatic circulation, GC, Glycocholate
Abstract

The absorption of oral drugs is frequently plagued by significant variability with potentially serious therapeutic consequences. The source of variability can be traced back to interindividual variability in physiology, differences in special populations (age- and disease-dependent), drug and formulation properties, or food-drug interactions. Clinical evidence for the impact of some of these factors on drug pharmacokinetic variability is mounting: e.g. gastric pH and emptying time, small intestinal fluid properties, differences in pediatrics and the elderly, and surgical changes in gastrointestinal anatomy. However, the link of colonic factors variability (transit time, fluid composition, microbiome), sex differences (male vs. female) and gut-related diseases (chronic constipation, anorexia and cachexia) to drug absorption variability has not been firmly established yet. At the same time, a way to decrease oral drug pharmacokinetic variability is provided by the pharmaceutical industry: clinical evidence suggests that formulation approaches employed during drug development can decrease the variability in oral exposure. This review outlines the main drivers of oral drug exposure variability and potential approaches to overcome them, while highlighting existing knowledge gaps and guiding future studies in this area. ispartof: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES vol:162 ispartof: location:Netherlands status: published

Published
2021

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