Gastric and Duodenal Ethanol Concentrations after Intake of Alcoholic Beverages in Postprandial Conditions.

Abstract:

:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crossover study. The fed state was simulated by ingestion of 250 mL of Nutridrink Compact Neutral. Volunteers subsequently consumed two standard units of beer (Stella Artois, 500 mL, 5.2% ethanol), wine (Blanc du Blanc, 200 mL, 11% ethanol), or whisky (Gallantry Whisky, 80 mL, 40% ethanol). Gastric and duodenal fluids were aspirated through two catheters over time and analyzed for ethanol content by head space gas chromatography. The capability of ethanol to permeate gastric and duodenal rat mucosa was examined in an Ussing chambers setup. A similar average gastric Cmax was observed in the beer and the wine conditions: 3.3% and 3.7% ethanol, respectively. The gastric Cmax in the whisky condition amounted to 8.5% ethanol. Lower ethanol concentrations were observed in the duodenum compared to the stomach. The duodenal Cmax was similar in all three conditions: 1.3%, 1.2%, and 1.6% ethanol for beer, wine, and whisky, respectively. Compared to the fasted state (reported in a previous study), higher gastric ethanol concentrations were observed during a longer time period. In the beer and wine conditions, similar concentrations were observed in the intestine regardless of the prandial state. After intake of whisky, however, the ethanol concentration was lower in the fed intestine. Alcohol was observed to permeate both gastric and duodenal rat mucosa. Higher intragastric ethanol concentrations were maintained for a longer period of time in fed compared to fasted state conditions. However, the observed concentration profiles were not in line with current FDA guidelines for alcohol resistance testing of formulations, stating that in vitro tests should investigate the impact of up to 40% ethanol for 2 h. The presented intraluminal ethanol concentrations may serve as reference data for the further development of relevant in vitro models to assess ethanol effects on formulation performance.

journal_name

Mol Pharm

journal_title

Molecular pharmaceutics

authors

Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

doi

10.1021/acs.molpharmaceut.7b00252

subject

Has Abstract

pub_date

2017-12-04 00:00:00

pages

4202-4208

issue

12

eissn

1543-8384

issn

1543-8392

journal_volume

14

pub_type

杂志文章
  • NMR and Thermal Studies for the Characterization of Mass Transport and Phase Separation in Paracetamol/Copovidone Hot-Melt Extrusion Formulations.

    abstract::The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.0c00188

    authors: Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

    更新日期:2020-06-01 00:00:00

  • Quantitative Imaging of the Hypoxia-Related Marker CAIX in Head and Neck Squamous Cell Carcinoma Xenograft Models.

    abstract::Tumor hypoxia plays a major role in radio- and chemotherapy resistance in solid tumors. Carbonic Anhydrase IX (CAIX) is an endogenous hypoxia-related protein, which is associated with poor patient outcome. The quantitative assessment of CAIX expression of tumors may steer cancer treatment by predicting therapy respons...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.8b00950

    authors: Huizing FJ,Hoeben BAW,Franssen GM,Boerman OC,Heskamp S,Bussink J

    更新日期:2019-02-04 00:00:00

  • Establishing the pharmaceutical quality of Chinese herbal medicine: a provisional BCS classification.

    abstract::The Biopharmaceutical Classification System (BCS), which is a scientific approach to categorize active drug ingredient based on its solubility and intestinal permeability into one of the four classes, has been used to set the pharmaceutical quality standards for drug products in western society. However, it has receiv...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp300502m

    authors: Fong SY,Liu M,Wei H,Löbenberg R,Kanfer I,Lee VH,Amidon GL,Zuo Z

    更新日期:2013-05-06 00:00:00

  • Renal Clearable Peptide Functionalized NaGdF4 Nanodots for High-Efficiency Tracking Orthotopic Colorectal Tumor in Mouse.

    abstract::The effective delivery of bioimaging probes to a selected cancerous tissue has extensive significance for biological studies and clinical investigations. Herein, the peptide functionalized NaGdF4 nanodots (termed as, pPeptide-NaGdF4 nanodots) have been prepared for highly efficient magnetic resonance imaging (MRI) of ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.7b00361

    authors: Chen H,Li X,Liu F,Zhang H,Wang Z

    更新日期:2017-09-05 00:00:00

  • Retro-inverso isomer of Angiopep-2: a stable d-peptide ligand inspires brain-targeted drug delivery.

    abstract::The blood-brain barrier (BBB) prevents most drugs from reaching the site of central nervous system (CNS) diseases, intensively confining the therapeutic efficiency. Angiopep-2 (here termed (L)Angiopep), which is a 19-mer peptide derived from human Kunitz domain, can trigger transcytosis and traverse the BBB by recogni...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp500086e

    authors: Wei X,Zhan C,Chen X,Hou J,Xie C,Lu W

    更新日期:2014-10-06 00:00:00

  • Bacillus-shape design of polymer based drug delivery systems with janus-faced function for synergistic targeted drug delivery and more effective cancer therapy.

    abstract::The particle shape of the drug delivery systems had a strong impact on their in vitro and in vivo performance, but there was limited availability of techniques to produce the specific shaped drug carriers. In this article, the novel methotrexate (MTX) decorated MPEG-PLA nanobacillus (MPEG-PLA-MTX NB) was prepared by t...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp500464b

    authors: Cui F,Lin J,Li Y,Li Y,Wu H,Yu F,Jia M,Yang X,Wu S,Xie L,Ye S,Luo F,Hou Z

    更新日期:2015-04-06 00:00:00

  • Formation of stable nanocarriers by in situ ion pairing during block-copolymer-directed rapid precipitation.

    abstract::We present an in situ hydrophobic salt forming technique for the encapsulation of weakly hydrophobic, ionizable active pharmaceutical ingredients (API) into stable nanocarriers (NCs) formed via a rapid precipitation process. Traditionally, NC formation via rapid precipitation has been difficult with APIs in this class...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp300452g

    authors: Pinkerton NM,Grandeury A,Fisch A,Brozio J,Riebesehl BU,Prud'homme RK

    更新日期:2013-01-07 00:00:00

  • Doxorubicin and lapatinib combination nanomedicine for treating resistant breast cancer.

    abstract::Our objective was to design a polymeric micelle-based doxorubicin and lapatinib combination therapy for treating multidrug resistant (MDR) breast cancers. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonylpropylene carbonate) (PEG-PBC) polymers were synthesized for preparing doxorubicin and lapatinib loaded m...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp400687w

    authors: Wang H,Li F,Du C,Wang H,Mahato RI,Huang Y

    更新日期:2014-08-04 00:00:00

  • Oral Delivery of β-Lactoglobulin-Nanosphere-Encapsulated Resveratrol Alleviates Inflammation in Winnie Mice with Spontaneous Ulcerative Colitis.

    abstract::Resveratrol (RES) is a nutraceutical with promising anti-inflammatory properties for the treatment of inflammatory bowel diseases (IBD). However, the clinical effectiveness of resveratrol as an oral anti-inflammatory agent is hindered by its extremely poor solubility and poor stability. In this study, we encapsulated ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.0c00048

    authors: Pujara N,Wong KY,Qu Z,Wang R,Moniruzzaman M,Rewatkar P,Kumeria T,Ross BP,McGuckin M,Popat A

    更新日期:2021-02-01 00:00:00

  • A Mechanistic Study on Nanoparticle-Mediated Glucagon-Like Peptide-1 (GLP-1) Secretion from Enteroendocrine L Cells.

    abstract::L cells have attracted particular interest because of the pleiotropic effects of their secreted peptides (i.e., glucagon-like peptide (GLP) 1 and 2, peptide YY (PYY)). L cells express different G-protein-coupled receptors (GPCRs) that can be activated by endogenous ligands found in the gut lumen. We herein hypothesize...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.6b00871

    authors: Beloqui A,Alhouayek M,Carradori D,Vanvarenberg K,Muccioli GG,Cani PD,Préat V

    更新日期:2016-12-05 00:00:00

  • Cyclic RGD-Functionalized closo-Dodecaborate Albumin Conjugates as Integrin Targeting Boron Carriers for Neutron Capture Therapy.

    abstract::Cyclic RGD (cRGD) peptide-conjugated boronated albumin was developed to direct toward integrin αvβ3, which overexpresses on many cancer cells. A stepwise conjugation of c[RGDfK(Mal)] and maleimide-conjugated closo-dodecaborate (MID) to bovine serum albumin (BSA) afforded cRGD-MID-BSA, which was noncytotoxic toward bot...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.0c00478

    authors: Kawai K,Nishimura K,Okada S,Sato S,Suzuki M,Takata T,Nakamura H

    更新日期:2020-10-05 00:00:00

  • Insight into Amorphous Solid Dispersion Performance by Coupled Dissolution and Membrane Mass Transfer Measurements.

    abstract::The tendency of highly supersaturated solutions of poorly water-soluble drugs to undergo liquid-liquid phase separation (LLPS) into drug-rich and water-rich phases when the concentration exceeds the amorphous solubility, for example, during dissolution of some amorphous solid dispersions, is thought to be advantageous...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.8b01117

    authors: Hate SS,Reutzel-Edens SM,Taylor LS

    更新日期:2019-01-07 00:00:00

  • In Silico Docking of Alkylphosphocholine Analogs to Human Serum Albumin Predicts Partitioning and Pharmacokinetics.

    abstract::Alkylphosphocholine (APC) analogs are a novel class of broad-spectrum tumor-targeting agents that can be used for both diagnosis and treatment of cancer. The potential for clinical translation for APC analogs will strongly depend on their pharmacokinetic (PK) profiles. The aim of this work was to understand how the ch...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.8b01301

    authors: Zhang RR,Grudzinksi JJ,Mehta TI,Burnette RR,Hernandez R,Clark PA,Lubin JA,Pinchuk AN,Jeffrey J,Longino M,Kuo JS,Weichert JP

    更新日期:2019-08-05 00:00:00

  • Predictable Heating and Positive MRI Contrast from a Mesoporous Silica-Coated Iron Oxide Nanoparticle.

    abstract::Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.5b00866

    authors: Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

    更新日期:2016-07-05 00:00:00

  • Temperature/pH/Enzyme Triple-Responsive Cationic Protein/PAA-b-PNIPAAm Nanogels for Controlled Anticancer Drug and Photosensitizer Delivery against Multidrug Resistant Breast Cancer Cells.

    abstract::The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.7b00737

    authors: Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

    更新日期:2017-12-04 00:00:00

  • A bacteria deriving peptide modified dendrigraft poly-l-lysines (DGL) self-assembling nanoplatform for targeted gene delivery.

    abstract::Achieving effective gene therapy for glioma depends on gene delivery systems. The gene delivery system should be able to cross the blood-brain barrier (BBB) and further target glioma at its early stage. Active brain tumor targeted delivery can be achieved using the "Trojan horse" technology, which involves either endo...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp500084s

    authors: Liu Y,He X,Kuang Y,An S,Wang C,Guo Y,Ma H,Lou J,Jiang C

    更新日期:2014-10-06 00:00:00

  • Disposition of nanoparticles and an associated lipophilic permeant following topical application to the skin.

    abstract::The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp9001188

    authors: Wu X,Price GJ,Guy RH

    更新日期:2009-09-01 00:00:00

  • Genetically modified mesenchymal stem cells for improved islet transplantation.

    abstract::The use of adult stem cells for therapeutic purposes has met with great success in recent years. Among several types of adult stem cells, mesenchymal stem cells (MSCs) derived from bone marrow (BM) and other sources have gained popularity for basic research and clinical applications because of their therapeutic potent...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1021/mp200135e

    authors: Wu H,Ye Z,Mahato RI

    更新日期:2011-10-03 00:00:00

  • Biomimetic urothelial tissue models for the in vitro evaluation of barrier physiology and bladder drug efficacy.

    abstract::The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1021/mp500065m

    authors: Baker SC,Shabir S,Southgate J

    更新日期:2014-07-07 00:00:00

  • Delivery of polysaccharides using polymer particles: implications on size-dependent immunogenicity, opsonophagocytosis, and protective immunity.

    abstract::Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp400589q

    authors: Anish C,Khan N,Upadhyay AK,Sehgal D,Panda AK

    更新日期:2014-03-03 00:00:00

  • Role of prostaglandin pathway and alendronate-based carriers to enhance statin-induced bone.

    abstract::This study investigated the role of the prostaglandin (PG) pathway in locally applied, simvastatin-induced oral bone growth. The possibility of enhancing long-term bone augmentation with an alendronate-based carrier was initiated. Mandibles of 44 mature female rats were treated bilaterally with the following combinati...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp200045p

    authors: Lee Y,Liu X,Nawshad A,Marx DB,Wang D,Reinhardt RA

    更新日期:2011-08-01 00:00:00

  • Targeted and Synergic Glioblastoma Treatment: Multifunctional Nanoparticles Delivering Verteporfin as Adjuvant Therapy for Temozolomide Chemotherapy.

    abstract::Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.8b01001

    authors: Pellosi DS,Paula LB,de Melo MT,Tedesco AC

    更新日期:2019-03-04 00:00:00

  • High-Content Surface and Total Expression siRNA Kinase Library Screen with VX-809 Treatment Reveals Kinase Targets that Enhance F508del-CFTR Rescue.

    abstract::The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.7b00928

    authors: Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

    更新日期:2018-03-05 00:00:00

  • Vitamin E Succinate-Grafted-Chitosan Oligosaccharide/RGD-Conjugated TPGS Mixed Micelles Loaded with Paclitaxel for U87MG Tumor Therapy.

    abstract::The poor therapeutic efficacy of hydrophobic chemotherapeutic drugs is an intrinsic limitation to successful chemotherapy. In the present study, a multitask delivery system based on arginine-glycine-aspartic acid peptide (RGD) decorated vitamin E succinate (VES)-grafted-chitosan oligosaccharide (CSO)/RGD-conjugated d-...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.6b01068

    authors: Chen Y,Feng S,Liu W,Yuan Z,Yin P,Gao F

    更新日期:2017-04-03 00:00:00

  • Enhanced tumor treatment using biofunctional indocyanine green-containing nanostructure by intratumoral or intravenous injection.

    abstract::Indocyanine green (ICG) is a conventional dye that can be used in clinical near-infrared (NIR) imaging, and it is also an effective light absorber for laser-mediated photothermal therapy. However, applications of ICG were limited due to its fast degradation in aqueous media and quick clearance from the body. Herein, a...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp200526m

    authors: Zheng X,Zhou F,Wu B,Chen WR,Xing D

    更新日期:2012-03-05 00:00:00

  • Increasing the Net Negative Charge by Replacement of DOTA Chelator with DOTAGA Improves the Biodistribution of Radiolabeled Second-Generation Synthetic Affibody Molecules.

    abstract::A promising strategy to enable patient stratification for targeted therapies is to monitor the target expression in a tumor by radionuclide molecular imaging. Affibody molecules (7 kDa) are nonimmunoglobulin scaffold proteins with a 25-fold smaller size than intact antibodies. They have shown an apparent potential as ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.6b00089

    authors: Westerlund K,Honarvar H,Norrström E,Strand J,Mitran B,Orlova A,Eriksson Karlström A,Tolmachev V

    更新日期:2016-05-02 00:00:00

  • Photothermal, Targeting, Theranostic Near-Infrared Nanoagent with SN38 against Colorectal Cancer for Chemothermal Therapy.

    abstract::Cancer research regarding near-infrared (NIR) agents for chemothermal therapy (CTT) has shown that agents with specific functions are able to inhibit tumor growth. The aim of current study was to optimize CTT efficacy for treatment of colorectal cancer (CRC) by exploring strategies which can localize high temperature ...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/acs.molpharmaceut.7b00315

    authors: Tsai MH,Peng CL,Yang SJ,Shieh MJ

    更新日期:2017-08-07 00:00:00

  • Segmental dependent transport of low permeability compounds along the small intestine due to P-glycoprotein: the role of efflux transport in the oral absorption of BCS class III drugs.

    abstract::The purpose of this study was to investigate the role of P-gp efflux in the in vivo intestinal absorption process of BCS class III P-gp substrates, i.e. high-solubility low-permeability drugs. The in vivo permeability of two H (2)-antagonists, cimetidine and famotidine, was determined by the single-pass intestinal per...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp800088f

    authors: Dahan A,Amidon GL

    更新日期:2009-01-01 00:00:00

  • Association of chemotherapeutic drugs with dendrimer nanocarriers: an assessment of the merits of covalent conjugation compared to noncovalent encapsulation.

    abstract::Cancer is a leading cause of death within developed nations, and part of this morbidity is due to difficulties associated with its treatment. Currently, anticancer therapy relies heavily upon the administration of small molecule cytotoxic drugs that attack both cancerous and noncancerous cells due to limited selectivi...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1021/mp2005966

    authors: Kaminskas LM,McLeod VM,Porter CJ,Boyd BJ

    更新日期:2012-03-05 00:00:00

  • Increased target specificity of anti-HER2 genospheres by modification of surface charge and degree of PEGylation.

    abstract::Genospheres are cationic lipid-nucleic acid nanoparticles prepared by the assembly of the lipids and nucleic acids from an aqueous/organic liquid monophase that independently dissolves the components, where the resultant particles are homogeneously sized (70-110 nm), with efficiently incorporated and protected DNA. In...

    journal_title:Molecular pharmaceutics

    pub_type: 杂志文章

    doi:10.1021/mp060040v

    authors: Hayes ME,Drummond DC,Hong K,Zheng WW,Khorosheva VA,Cohen JA,C O N 4th,Park JW,Marks JD,Benz CC,Kirpotin DB

    更新日期:2006-11-01 00:00:00