1,708 results match your criteria everted intestinal

Uncovering the pharmacological mechanisms of Xijiao Dihuang decoction combined with Yinqiao powder in treating influenza viral pneumonia by an integrative pharmacology strategy.

Biomed Pharmacother 2021 Jun 11;141:111676. Epub 2021 Jun 11.

School of Life Sciences, Beijing University of Chinese Medicine, Beijing, China. Electronic address:

Xijiao Dihuang decoction combined with Yinqiao powder (XDD-YQP) is a classical combination formula; however, its therapeutic effects in treating influenza viral pneumonia and the pharmacological mechanisms remain unclear. The therapeutic effect of XDD-YQP in influenza viral pneumonia was evaluated in mice. Subsequently, an everted gut sac model coupled with UPLC/Q-TOF MS were used to screen and identify the active compounds of XDD-YQP. Read More

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Promoting effect of the Maillard reaction products produced during the stir-frying process of on the intestinal absorption of active ingredients in .

Food Sci Biotechnol 2021 May 23;30(5):631-642. Epub 2021 Apr 23.

School of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, China.

This study was designed to evaluate the absorption promoting capacity of Maillard Reaction Products (MRPs) produced during the stir-frying process of on catechin, ferulic acid, quercetin and kaempferol by the ex vivo rat everted gut sac model, in situ single-pass intestinal perfusion model and the whole animal model. Moreover, verapamil, EDTA and mannitol were used for determining the transport mechanism of catechin, ferulic acid, quercetin and kaempferol. The tight junction (TJ) proteins including zonula occudens-1(ZO-1) and claudin-1 were chosen to investigate the promoting mechanism of MRPs by quantitative real-time PCR (qRT-PCR) and western blot analyses. Read More

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Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach.

Molecules 2021 May 19;26(10). Epub 2021 May 19.

School of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. Read More

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Measurement of Intestinal Permeability During Sepsis.

Methods Mol Biol 2021 ;2321:169-175

Department of Surgery and Emory Critical Care Center, Emory University School of Medicine, Atlanta, GA, USA.

Gut barrier function has been hypothesized to play a critical role in the pathophysiology of sepsis. Measuring intestinal permeability allows for a determination of barrier dysfunction under conditions of health and disease. Fluorescence-conjugated dyes such as fluorescein isothiocyanate-4 kDa dextran (FD4) have been commonly used for evaluating hyperpermeability. Read More

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January 2021

Bioactive peptide release and the absorption tracking of casein in the gastrointestinal digestion of rats.

Food Funct 2021 Jun;12(11):5157-5170

School of Food and Biological Engineering, Shaanxi University of Science and Technology, Xi'an, 710021, P. R. China.

Bovine casein is considered as an important source of many bioactive peptides (BAPs), which can also be produced via in vitro simulated gastrointestinal hydrolysis. To perform their physiological functions, some active peptides need to pass through the intestinal epithelial barrier and keep their structural integrity after oral administration. Owing to the complexity of in vivo digestion and absorption, there have been few studies in this area. Read More

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Effect of Pharmaceutical Excipients on Intestinal Absorption of Metformin via Organic Cation-Selective Transporters.

Mol Pharm 2021 Jun 6;18(6):2198-2207. Epub 2021 May 6.

Department of Pharmaceutical Analysis, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.

Growing evidence has shown that some pharmaceutical excipients can act on drug transporters. The present study was aimed at investigating the effects of 13 commonly used excipients on the intestinal absorption of metformin (MTF) and the underlying mechanisms using Caco-2 cells and an mouse non-everted gut sac model. First, the uptake of MTF in Caco-2 cells was markedly inhibited by nonionic excipients including Solutol HS 15, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and crospovidone. Read More

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Evaluation of Thymol-β-d-Glucopyranoside as a Potential Prebiotic Intervention to Reduce Carriage of Zoonotic Pathogens in Weaned and Feeder Pigs.

Microorganisms 2021 Apr 16;9(4). Epub 2021 Apr 16.

United States Department of Agriculture, Agricultural Research Service, Food and Feed Safety Research Unit, College Station, TX 77845, USA.

The gut of food-producing animals is a reservoir for foodborne pathogens. Thymol is bactericidal against foodborne pathogens but rapid absorption of thymol from the proximal gut precludes the delivery of effective concentrations to the lower gut where pathogens mainly colonize. Thymol-β-d-glucopyranoside is reported to be more resistant to absorption than thymol in everted jejunal segments and could potentially function as a prebiotic by resisting degradation and absorption in the proximal gut but being hydrolysable by microbial β-glycosidase in the distal gut. Read More

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Discovery of potential pharmacodynamic ingredients of Dang-Gui-Si-Ni decoction based on absorbed ingredients and molecular docking.

J Ethnopharmacol 2021 Jul 5;275:114045. Epub 2021 Apr 5.

National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines, Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, 100700, China. Electronic address:

Ethnopharmacological Relevance: The Dang-Gui-Si-Ni (DGSN) decoction as a classic prescription has been widely used for thousands of years in the clinical practice of traditional Chinese medicine (TCM). Especially in recent years, the potential efficacy of TCM for the treatment of Raynaud's syndrome has attracted great attention as there are still no specific remedies for this disease. However, the active constituents and underlying mechanisms responsible for the therapeutic benefits are not well understood, which makes it difficult to ensure quality control or to design research and drug development strategies. Read More

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Missing Jejunal Perforation During Small Bowel Measurement in Patient Operated by Laparoscopic One-Anastomosis Gastric Bypass.

Obes Surg 2021 Jun 6;31(6):2841-2842. Epub 2021 Apr 6.

Department of Bariatric Surgery (ObesidadAlmería), General Surgery, Hospital Mediterráneo, Almería, Spain.

Background: Obesity surgery is justified as it produces sustained weight loss, increases life expectancy, and reduces the complications of obesity. For this reason, increasing numbers of patients are undergoing this surgery [1]. Complications following surgical treatment of severe obesity vary based upon the procedure performed and, although it is currently below 7% in more experienced centers, it may increase in more complex surgeries (such as revision surgery) and can be as high as 40% [2, 3]. Read More

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Effects of licorice extracts on the pharmacokinetics of brucine in rats and its possible mechanism.

Pak J Pharm Sci 2020 Sep;33(5):1995-2002

Department of Pharmacy, the Second Xiangya Hospital, Central South University, Changsha, China/ Institute of Clinical Pharmacy, Central South University, Xiangya Hospital, Central South University, Changsha, China.

The detoxification effects of licorice are believed to be related to its pharmacokinetic (PK) interference. This paper aimed to evaluate the effects of licorice water extracts (LWE) on the pharmacokinetics of brucine. Rats were administered brucine and/or LWE. Read More

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September 2020

Chronotoxicity of Semen Strychni is associated with circadian metabolism and transport in mice.

J Pharm Pharmacol 2021 Mar;73(3):398-409

Research Center for Biopharmaceutics and Pharmacokinetics, College of Pharmacy, Jinan University, Guangzhou, China.

Objectives: We aimed to determine the circadian responses of mice to Semen Strychni and to investigate the role of pharmacokinetics in generating chronotoxicity.

Methods: Total extract of Semen Strychni was administered by oral gavage to wild-type (WT) and Bmal1-/- (a circadian clock-deficient model) mice at different circadian time points for toxicity (including survival) and pharmacokinetic characterization. Nephrotoxicity and neurotoxicity were evaluated by measuring plasma creatinine and creatine kinase BB (CK-BB), respectively. Read More

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[Study on rat intestinal absorption characteristics of total flavonoids from Coreopsis tinctoria].

Zhongguo Zhong Yao Za Zhi 2021 Mar;46(6):1490-1497

School of Pharmacy,Shihezi University Shihezi 832000,China Ministry of Education Key Laboratory of Xinjiang Plant Resources Utilization Shihezi 832000,China.

The rat everted intestinal sac model was adopted to investigate the absorption of total flavonoids from Coreopsis tinctoria in different intestinal segments. Cyaniding-3-O-β-D-glucoside, chlorogenic acid, flavanomarein, quercetagetin-7-O-β-D-glucoside, iso-okanin, marein and 3,5-dicaffeoylquinic acid which as the major chemical components of total flavonoids from C. tinctoria were selec-ted as the study objects to evaluate the absorption characteristics of each component in different intestinal segments. Read More

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Precisely Fabricated Sulpiride-Loaded Nanolipospheres with Ameliorated Oral Bioavailability and Antidepressant Activity.

Int J Nanomedicine 2021 9;16:2013-2044. Epub 2021 Mar 9.

Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

Background: Sulpiride (SUL), is a selective antidopaminergic drug that had extensive biological activities. However, its sparingly aqueous solubility and limited gastrointestinal permeability lead to scanty oral bioavailability which hinders its clinical efficacy.

Objective: SUL-loaded lipospheres (SUL-LPS) were designed to serve as an oral biocompatible nanovector for improving SUL permeability as well as conquering its low oral absorption and then in turn enhancing its antidepressant action. Read More

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Effect of Short-Term Exposure to Titanium Dioxide Nanoparticles on Intestinal Absorption of Glucose by Everted Rat Gut Sac Model.

J Nanosci Nanotechnol 2021 09;21(9):4586-4595

Department of Occupational and Environmental Health Sciences, School of Public Health, Peking University, Beijing 100191, China.

Titanium dioxide nanoparticles (TiO₂ NPs) as food additives were widely found in various foodrelated products, especially in high-sugar foods. The daily intake of TiO₂ NPs in the diet may therefore expose the small intestine to TiO₂ NPs and affect its physiological functions, including the absorption of nutrients. It is speculated that TiO₂ may cause serious health hazards by increasing sugar uptake. Read More

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September 2021

[Intestinal absorption characteristics of Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats via everted intestinal sac models].

Zhongguo Zhong Yao Za Zhi 2021 Jan;46(1):196-205

Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University Guiyang 550004, China.

The present study is to investigate the absorption characteristics of the main components in Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats with everted intestinal sac models. Intestinal sac fluid samples were collected in different part of intestine(duodenum, jejunum, ileum, colon) at different time after administration of different concentration of P. orientale extract(5. Read More

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January 2021

Protective Effect of Lacticaseibacillus casei CRL 431 Postbiotics on Mitochondrial Function and Oxidative Status in Rats with Aflatoxin B-Induced Oxidative Stress.

Probiotics Antimicrob Proteins 2021 Jan 29. Epub 2021 Jan 29.

Laboratorio de Química y Biotecnología de Productos Lácteos, Centro de Investigación en Alimentación y Desarrollo A.C., Carretera Gustavo Enrique Astiazarán Rosas, No. 46 Col. La Victoria, 83304, Hermosillo, Sonora, Mexico.

Studies have shown that the intracellular content of probiotic (postbiotics) has antioxidant properties, which can improve the antioxidant status in vivo. However, its absorption and mechanisms underlying the protective effects are still unknown. The antioxidant capacity of Lacticaseibacillus casei CRL431 (IC-431) postbiotics was determined after an in vitro simulated digestive process. Read More

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January 2021

Bioaccessibility and Intestinal Permeability of a Recombinant Lectin from Tepary Bean () Using the Everted Intestine Assay.

Int J Mol Sci 2021 Jan 21;22(3). Epub 2021 Jan 21.

Laboratorio de Biología Celular y Molecular, Facultad de Ciencias Naturales, Universidad Autónoma de Querétaro, Av. de las Ciencias s/n, Juriquilla, Querétaro 76230, Querétaro, Mexico.

Tepary bean () lectins exhibit differential and biological effects, but their gastrointestinal interactions and digestion have not yet been assessed. This work aimed to evaluate the changes of a recombinant Tepary bean lectin (rTBL-1) through an and gastrointestinal process. A polyclonal antibody was developed to selectively detect rTBL-1 by Western blot (WB) and immunohistochemical analysis. Read More

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January 2021

Inhibitory effects of Coptidis Rhizoma on the intestinal absorption and metabolism of Scutellariae Radix.

J Ethnopharmacol 2021 Apr 7;270:113785. Epub 2021 Jan 7.

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 102488, China. Electronic address:

Ethnopharmacological Relevance: The Scutellariae Radix (SR) and Coptidis Rhizoma (CR) herb couple is widely used in traditional Chinese medicine prescriptions for the treatment of diabetes mellitus due to its interaction and synergistic effect compared to either herb alone, but the underlying mechanism of interaction between these herbs is unclear. This study aimed to investigate the effects of CR on the metabolism and absorption of SR.

Materials And Methods: After rats were treated with normal saline (NS group) or the CR extract (CR-treated group) for seven consecutive days, the intestinal flora was extracted from rat faeces for a co-incubation with the SR extract to investigate the metabolism of SR flavonoids, and a non-everted gut sac was prepared in vitro to evaluate the intestinal absorption of the SR extract. Read More

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Comparison of the effects of the intestinal permeation enhancers, SNAC and sodium caprate (C): Isolated rat intestinal mucosae and sacs.

Eur J Pharm Sci 2021 Mar 23;158:105685. Epub 2020 Dec 23.

UCD School of Veterinary Medicine, Belfield, Dublin 4, Ireland; UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland. Electronic address:

SNAC and C are intestinal permeation enhancers (PEs) used in formulations of peptides for oral delivery in clinical trials. Our aims were to compare their: (i) mechanism of action in isolated rat intestinal mucosae mounted in Ussing chambers and in non-everted gut sacs, (ii) effects on mucosa integrity in those models and also in in situ intra-jejunal instillations and (iii) interactions with intestinal mucus. SNAC increased the apparent permeability coefficient (P) of the paracellular marker, FITC-dextran 4000 (FD4), across isolated rat gastric mucosae in concentration-dependent fashion, whereas C did not, while both reduced the transepithelial electrical resistance (TEER). Read More

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The Intestinal Efflux Transporter Inhibition Activity of Xanthones from Mangosteen Pericarp: An In Silico, In Vitro and Ex Vivo Approach.

Molecules 2020 Dec 11;25(24). Epub 2020 Dec 11.

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Rajathevi, Bangkok 10400, Thailand.

The capacity of α-mangostin (α-MG) and β-mangostin (β-MG) from mangosteen pericarp on P-glycoprotein (Pgp) in silico, in vitro, and ex vivo was investigated in this study. Screening with the ADMET Predictor™ program predicted the two compounds to be both a Pgp inhibitor and Pgp substrate. The compounds tended to interact with Pgp and inhibit Pgp ATPase activity. Read More

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December 2020

The enhanced intestinal permeability of infant mice enables oral protein and macromolecular absorption without delivery technology.

Int J Pharm 2021 Jan 26;593:120120. Epub 2020 Nov 26.

Department of Chemical Engineering, Carnegie Mellon University, Pittsburgh, PA 15213, United States; Department of Biomedical Engineering, Carnegie Mellon University, Pittsburgh, PA 15213, United States. Electronic address:

Oral delivery of macromolecular drugs is the most patient-preferred route of administration because it is painless and convenient. Over the past 30 years, significant attention has been paid to oral protein delivery in adults. Unfortunately, there is an outstanding need for similar efforts in infants, a patient population with distinct intestinal physiology and treatment needs. Read More

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January 2021

Synthesis and Evaluation of PEG-PR for Water Flux Correction in an In Situ Rat Perfusion Model.

Molecules 2020 Nov 4;25(21). Epub 2020 Nov 4.

Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

Phenol red (PR) is a widely used marker for water flux correction in studies of in situ perfusion, in which intestinal absorption usually leads to the underestimation of results. In this paper, we propose a novel marker polyethylene glycol (PEG)-PR (i.e. Read More

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November 2020

Exploring efficacy of natural-derived acetylphenol scaffold inhibitors for α-glucosidase: Synthesis, in vitro and in vivo biochemical studies.

Bioorg Med Chem Lett 2020 12 10;30(23):127528. Epub 2020 Sep 10.

Shaanxi Key Laboratory of Natural Products & Chemical Biology, Shaanxi Engineering Center of Bioresource Chemistry & Sustainable Utilization, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, China. Electronic address:

The discovery of novel α-glucosidase inhibitors and anti-diabetic candidates from natural or natural-derived products represents an attractive therapeutic option. Here, a collection of acetylphenol analogues derived from paeonol and acetophenone were synthesized and evaluated for their α-glucosidase inhibitory activity. Most of derivatives, such as 9a-9e, 9i, 9m-9n and 11d-1e, (IC = 0. Read More

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December 2020

Structural changes of ethanolamine plasmalogen during intestinal absorption.

Food Funct 2020 Sep;11(9):8068-8076

Food and Biodynamic Chemistry Laboratory, Graduate School of Agricultural Science, Tohoku University, Sendai, Miyagi 980-8572, Japan.

Considerable attention has been paid to the absorption mechanisms of plasmalogen (Pls) because its intake has been expected to have preventive effects on brain-related diseases. Possible structural changes of Pls during absorption (i.e. Read More

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September 2020

Solid-in-oil nanodispersions as a novel delivery system to improve the oral bioavailability of bisphosphate, risedronate sodium.

Eur J Pharm Sci 2020 Dec 19;155:105521. Epub 2020 Aug 19.

Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, Fukuoka819-0395, Japan; Advanced Transdermal Drug Delivery System Center, Kyushu University, Fukuoka819-0395, Japan; Center for Future Chemistry, Kyushu University, Fukuoka819-0395, Japan. Electronic address:

The aim of the current study was to modify the oral absorption of risedronate sodium (RS) using solid-in-oil nanodispersions (SONDs) technology. The oral therapeutic effect of RS is limited in vivo because of its low membrane permeability and the formation of insoluble precipitates with bivalent cations (such as Ca) in the gastrointestinal (GI) tract.We used SONDs to prepare medium-chain triglyceride (MCT)-based nanodispersions of the hydrophilic drug, which used the oral absorption mechanism of MCT digestion to improve bioavailability of RS in vivo. Read More

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December 2020

Formulation development of linagliptin solid lipid nanoparticles for oral bioavailability enhancement: role of P-gp inhibition.

Drug Deliv Transl Res 2021 Jun;11(3):1166-1185

Maliba Pharmacy College, Uka Tarsadia University, Gopal Vidyanagar, Bardoli Mahuva Road, Dist. Surat, Tarsadi, Gujarat, 394350, India.

Linagliptin (LGP), a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type II diabetes. One of the major disadvantages of LGP is its low oral bioavailability (29.5%) due to first-pass metabolism and P-gp efflux. Read More

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Effects of paralytic shellfish toxins on the middle intestine of Oncorhynchus mykiss: Glutathione metabolism, oxidative status, lysosomal function and ATP-binding cassette class C (ABCC) proteins activity.

Ecotoxicol Environ Saf 2020 Nov 3;204:111069. Epub 2020 Aug 3.

Laboratorio de Ecotoxicología Acuática, Subsede INIBIOMA-CEAN (CONICET-UNCo), ruta provincial 61, km 3, CCP 7, Junín de los Andes, 8371, Neuquén, Argentina. Electronic address:

We studied the absorption, cytotoxicity and oxidative stress markers of Paralytic Shellfish Toxins (PST) from three extracts from Alexandrium catenella and A. ostenfeldii, in middle Oncorhynchus mykiss intestine in vitro and ex vivo preparations. We measured glutathione (GSH) content, glutathione-S transferase (GST), glutathione reductase (GR) and catalase (CAT) enzymatic activity, and lipid peroxidation in isolated epithelium exposed to 0. Read More

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November 2020

Effect of Baizhu (Rhizoma Atractylodis Macrocephalae) extract on intestinal absorption of brucine and strychnine in vitro and in situ.

J Tradit Chin Med 2020 08;40(4):562-570

Key Laboratory of Modern Preparation of Traditional Chinese Medicine of Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.

Objective: To investigate the antagonistic effect of the extract of Baizhu (Rhizoma Atractylodis Macrocephalae) (RAM) on the intestinal absorption of brucine and strychnine in Strychnos nux-vomica (NUX) and propose the mechanism of these effects.

Methods: The apparent permeability value (Papp) and absorption rate constant (Ka) were chosen as indices. The everted intestinal sac model and in situ single-pass intestinal perfusion model were used to study the effects of the RAM extract on the absorption of brucine and strychnine. Read More

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Enhanced Solubility and Permeability of Naringenin Across Non-Everted Sacs of Rat Small Intestine by Lipid Nanocapsules.

Recent Pat Nanotechnol 2021 ;15(1):55-69

Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

Background: Naringenin (NRG) has many health benefits, including; anti-atherogenic, antiinflammatory, antitumor, and anticancer activity, as well as improvement of lipid metabolism. However, its use is limited due to its low solubility and bioavailability.

Objectives: The aim of the present patent study was the preparation and optimization of NRG loaded Novel Lipid Nanocapsules (LNCs) for the improvement of NRG solubility and gut permeability. Read More

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January 2021

Hydrophobic ion pair loaded self-emulsifying drug delivery system (SEDDS): A novel oral drug delivery approach of cromolyn sodium for management of bronchial asthma.

Int J Pharm 2020 Jul 4;585:119494. Epub 2020 Jun 4.

Pharmaceutical Technology Department, National Research Centre, El-Buhouth St, Dokki, Cairo 12622, Egypt.

The aim of the present study is to develop a self-emulsifying drug delivery system (SEDDS) for the hydrophobic ion pair (HIP) complex of cromolyn sodium (CS), in order to enhance its intestinal absorption and biological activity. Two ion pairing agents (IPAs) were investigated: hexadecyl pyridininum chloride (HPC) and myristyl trimethyl ammonium bromide (MTAB). The optimum binding efficiency for complexation between investigated IPAs and CS was observed at a molar ratio of 1. Read More

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