307,385 results match your criteria oral administration


Therapeutic review of cabotegravir/rilpivirine long-acting antiretroviral injectable and implementation considerations at an HIV specialty clinic.

Pharmacotherapy 2021 Jun 15. Epub 2021 Jun 15.

Indiana University Health, Indianapolis, Indiana, USA.

Cabotegravir/rilpivirine (CAB/RPV) was recently approved by the US Food and Drug Administration (FDA) as the first complete parenteral antiretroviral (ART) regimen for treatment of people living with HIV (PLWH). As a monthly intramuscular (IM) injection, this therapy constitutes a major departure from the traditional paradigm of oral therapy requiring (at least) daily administration that has defined HIV treatment for decades. Composed of a second-generation integrase inhibitor (INSTI) and nonnucleoside reverse transcriptase inhibitor (NNRTI), CAB/RPV has achieved high rates of sustained virologic suppression with a favorable safety profile for treatment-experienced PLWH following oral lead-in (OLI) during several clinical trials. Read More

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Characterization of chemical constituents and metabolites in rat plasma after oral administration of San Miao Wan by ultra-high performance liquid chromatography tandem Q-Exactive Orbitrap mass spectrometry.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 May 28;1178:122793. Epub 2021 May 28.

State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, Jiangsu Province, PR China; Department of Pharmacognosy, School of Traditional Chinese Pharmacy, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, Jiangsu Province, PR China. Electronic address:

San Miao Wan (SMW), composed of Phellodendri Chinensis Cortex, Atractylodis Lanceae Rhizoma and Achyranthis Bidentatae Radix, is widely used for the treatment of gout, hyperuricemia and other diseases. In the present study, an overall identification strategy based on ultra-high performance liquid chromatography tandem Q-Exactive Orbitrap mass spectrometry (UPLC-Q-Exactive Orbitrap/MS) method was established to characterize the multiple chemical constituents of SMW and its metabolites in rat plasma after oral administration of SMW. A total of 76 constituents including alkaloids, organic acids, lactones, terpenes, saponins, sterones and others types of components were identified in the extract of SMW. Read More

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Pharmacokinetic study of Ninjin'yoeito: Absorption and brain distribution of Ninjin'yoeito ingredients in mice.

J Ethnopharmacol 2021 Jun 12:114332. Epub 2021 Jun 12.

Department of Cellular and Molecular Anatomy, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka, 431-3192, Japan; Preppers Co. Ltd., 1-23-17 Kitashinagawa, Shinagawa Ward, Tokyo, 140-0001, Japan; International Mass Imaging Center, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka, 431-3192, Japan; Department of Systems Molecular Anatomy, Institute for Medical Photonics Research, Preeminent Medical Photonics Education & Research Center, 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka, 431-3192, Japan. Electronic address:

Ethnopharmacological Relevance: Ninjin'yoeito (NYT), a Japanese traditional Kampo medicine, has been reported to exert various clinical benefits such as relief from fatigue, malaise, anorexia, frailty, sarcopenia, and cognitive dysfunction. Recently, some review articles described the pharmacological effects of NYT and additionally indicated the possibility that multiple ingredients in NYT contribute to these effects. However, pharmacokinetic data on the ingredients are essential in addition to data on their pharmacological activities to accurately determine the active ingredients in NYT. Read More

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Impact of protocatechuic acid on high fat diet-induced metabolic syndrome sequelae in rats.

Eur J Pharmacol 2021 Jun 12:174257. Epub 2021 Jun 12.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.

The study aimed to assess the possible protective impact of protocatechuic acid (PCA) on high fat diet (HFD)-induced metabolic syndrome (Mets) sequelae in rats. Forty-two male Sprague-Dawley (SD) rats were randomly grouped as follows: CTR group; PCA group; HFD group; HFD-PCA group and HFD-MET group. Rats were fed on standard diet or HFD for 14 weeks. Read More

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Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and Characterization.

Assay Drug Dev Technol 2021 Jun 14. Epub 2021 Jun 14.

Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo, New South Wales, Australia.

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Systemic administration of cytotoxic T lymphocyte-associated antigen 4 (CTLA-4)-Ig abrogates alveolar bone resorption in induced periodontitis through inhibition of osteoclast differentiation and activation: An experimental investigation.

J Periodontal Res 2021 Jun 15. Epub 2021 Jun 15.

Department of Periodontology, Tokyo Dental College, Tokyo, Japan.

Background/objectives: Cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) is a critical immunoregulatory molecule expressed on T cells. CTLA-4 also binds to the surfaces of monocytes and macrophages, precursors of osteoclasts. Research on rheumatoid arthritis demonstrated that CTLA-4 suppresses inflammation and bone resorption. Read More

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Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir.

AAPS PharmSciTech 2021 Jun 15;22(5):181. Epub 2021 Jun 15.

Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, Pakistan.

In this study, two hydrophilic polymers hydroxypropyl methyl cellulose and beta-cyclodextrin (β-CD) are used to synthesize highly responsive and spongy polymeric matrices. Porous and stimulus-responsive polymeric network was developed to improve the solubility of acyclovir (ACV) at significant level. Grafting was successfully carried out by free radical polymerization technique. Read More

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Fabrication and Evaluation of Celecoxib Oral Oleogel to Reduce the Inflammation of Ulcerative Colitis.

AAPS PharmSciTech 2021 Jun 15;22(5):180. Epub 2021 Jun 15.

Biochemistry Department, Faculty of Pharmacy, October 6 University, 6th of October City, Central Axis, Part 1/1, Behind Sixth October City Authority, Giza, 12585, Egypt.

Oleogel consists of hydrophobic solvent and an oleogelator. In this study, attempts were made to study the influence of Celecoxib solubility, concentration and dispersability on its release, absorption, and biological performance. Oleogels were prepared to study the formulation variables on its stability and release. Read More

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Cissus quadrangularis extract attenuates diabetic nephropathy by altering SIRT1/DNMT1 axis.

J Pharm Pharmacol 2021 Jun 15. Epub 2021 Jun 15.

Pharmaceutics & Pharmacokinetics Division, CSIR-Central Drug Research Institute, Lucknow, India.

Objectives: Hyperglycemia-induced SIRT1, DNMT1, SODs, as well as oxidative stress, play a pivotal role in the progression of diabetic nephropathy. Cissus quadrangularis, holds antioxidant and hypoglycemic activity; however, a direct link between its activity and prevention of diabetic nephropathy has not been ascertained yet. Accordingly, we aimed to delineate the protective effect of ethanolic extract of Cissus quadrangularis (EECQ) against high-fat diet/streptozotocin (HFD/STZ) induced diabetic nephropathy rats. Read More

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Nanocrystals for Improving Oral Bioavailability of Drugs: Intestinal Transport Mechanisms and Influencing Factors.

AAPS PharmSciTech 2021 Jun 14;22(5):179. Epub 2021 Jun 14.

Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, Yinchuan, China.

With the limitation of solubility and dissolution rate of insoluble drugs, following oral administration, they would rifely prove poor and volatile bioavailability, which may fail to realize its therapeutic value. The drug nanocrystals are perceived as effective tactic for oral administration of insoluble drugs attributes to possess many prominent properties such as elevating dissolution rate and saturation solubility, high drug loading capacity, and improving oral bioavailability. Based on these advantages, the application of nanocrystals in oral drug delivery has acquired significant achievement, and so far more than 20 products of drug nanocrystals have been confirmed in the market. Read More

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Efficacy of green jackfruit flour as a medical nutrition therapy replacing rice or wheat in patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled study.

Nutr Diabetes 2021 Jun 14;11(1):18. Epub 2021 Jun 14.

God's Own Food Solutions Pvt Ltd, Kochi, Kerala, India.

Background/objectives: Medical nutrition therapy along with pharmacological interventions as a multidisciplinary approach is required to treat type 2 diabetes mellitus (T2DM). This study evaluated the efficacy of Jackfruit365™ green jackfruit flour as an integral part of daily meal in patients with T2DM.

Subjects/methods: This was a randomized, double-blind, placebo-controlled study conducted between May 2019 and February 2020. Read More

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Cytoplasmic expression of a model antigen with M Cell-Targeting moiety in lactic acid bacteria and implication of the mechanism as a mucosal vaccine via oral route.

Vaccine 2021 Jun 11. Epub 2021 Jun 11.

Graduate School of International Agricultural Technology, Seoul National University, Pyeongchang-gun 25354, Republic of Korea; Institute of Green-Bio Science & Technology, Seoul National University, Pyeongchang-gun 25354, Republic of Korea; Research Institute of Agriculture and Life Science, Seoul National University, Seoul 08826, Republic of Korea. Electronic address:

Lactic acid bacteria (LAB) have been widely studied as mucosal vaccine delivery carriers against many infectious diseases for heterologous expression of protein antigens. There are three antigen expression strategies for LAB: cytoplasmic expression (CE), cell surface display (SD), and extracellular secretion (ES). Despite the generally higher protein expression level and many observations of antigen-specific immunogenicity in CE, its application as a mucosal vaccine has been overlooked relative to SD and ES because of the antigens enclosed by the LAB cell wall. Read More

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Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies.

Allergy Asthma Proc 2021 Jun 14. Epub 2021 Jun 14.

Background: Hereditary angioedema (HAE) is a rare genetic disorder characterized by unpredictable and potentially life-threatening episodes of swelling in various parts of the body. These attacks can be painful and debilitating, and affect apatient's quality of life. Every patient who experiences an attack should be treated with on-demand medication to mitigateattack severity and duration. Read More

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Prescription Stimulant Misuse and Abuse: Characterization of Exposures Managed by United States (US) Poison Centers.

CNS Spectr 2021 Apr;26(2):166

Syracuse University, Syracuse, NY, USA.

The National Poison Data System (NPDS), is the data warehouse for the 55 US regional poison centers. While the primary role of a poison center is to provide medical management to the public and healthcare providers, a standardized database is used to collect case data. These data are routinely used to evaluate drug safety, including characterization of prescription medication misuse and abuse. Read More

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Substance Use Trajectories: Nonmedical Use (NMU) of Prescription Stimulants via Non-Oral Routes of Administration Among Adults Recruited from Reddit.

CNS Spectr 2021 Apr;26(2):166-167

Syracuse University, Syracuse, NY, USA.

NMU of prescription stimulant medications (RxStim) intended for treatment of attention deficit/hyperactivity disorder (ADHD) is a growing public health concern, particularly when used via non-oral routes of administration. However, the role of non-oral routes of administration for RxStim NMU in the larger substance abuse pathway is less well studied. The purpose of this study was to characterize RxStim NMU and investigate substance use trajectories among adults who reported non-oral RxStim NMU recruited from Reddit. Read More

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Antiviral effects of ergosterol peroxide in a pig model of porcine deltacoronavirus (PDCoV) infection involves modulation of apoptosis and tight junction in the small intestine.

Vet Res 2021 Jun 14;52(1):86. Epub 2021 Jun 14.

College of Veterinary Medicine, China Agricultural University, Beijing, China.

Porcine deltacoronavirus (PDCoV) is a newly discovered swine enteropathogenic coronavirus with worldwide distribution. However, efficient strategies to prevent or treat the infection remain elusive. Our in vitro study revealed that ergosterol peroxide (EP) from the mushroom Cryptoporus volvatus has efficient anti-PDCoV properties. Read More

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Assessment of Exenatide loaded Biotinylated Trimethylated Chitosan/HP-55 Nanoparticles.

Curr Drug Deliv 2021 Jun 13. Epub 2021 Jun 13.

Department of Pharmacy, Affiliated Jinhua Hospital, Zhejiang University School of Medicine, 365 Renmin East Road, Jinhua321000, China.

Background: Exenatide (EXE) is an anti-hyperglycemic agent approved for treating type 2 diabetes by the Food and Drug Administration (FDA). However, twice-daily injection of exenatide inconveniences most patients.

Objective: In this study, biotinylated trimethylated chitosan (Bio-TMC) based nanoparticles were proposed to promote oral absorption of exenatide. Read More

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Optimization and SAR research at the piperazine and phenyl rings of JNJ4796 as new anti-influenza A virus agents, part 1.

Eur J Med Chem 2021 Jun 5;222:113591. Epub 2021 Jun 5.

CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China. Electronic address:

JNJ4796, a small molecule fuse inhibitor targeting the conserved stem region of hemagglutinin, effectively neutralized a broad spectrum of group 1 influenza A virus (IAV), and protected mice against lethal and sublethal influenza challenge after oral administration. In this study, we reported the modification and structure-activity relationship (SAR) of C (piperazine ring) and E (phenyl ring) rings of JNJ4796. Compound (R)-2c was identified to show excellent in vitro activity against IAV H1N1 and Oseltamivir-resistant IAV H1N1 stains (IC: 0. Read More

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Induced forms of α-macroglobulin neutralize heparin and direct oral anticoagulant effects.

Int J Biol Macromol 2021 Jun 11. Epub 2021 Jun 11.

Université de Paris, Innovative Therapies in Haemostasis, INSERM UMR_S1140, F-75006, Paris, France; AP-HP, Centre-Université de Paris, Hôpital Européen Georges Pompidou, F-75015 Paris, France. Electronic address:

Alpha-macroglobulin (αM) is a physiological macromolecule that facilitates the clearance of many proteinases, cytokines and growth factors in human. Here, we explored the effect of induced forms of αM on anticoagulant drugs. Gla-domainless factor Xa (GDFXa) and methylamine (MA)-induced αM were prepared and characterized by electrophoresis, immunonephelometry, chromogenic, clot waveform and rotational thromboelastometry assays. Read More

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Health-related quality of life in patients with acute promyelocytic leukemia: a systematic literature review.

Expert Rev Hematol 2021 Jun 14. Epub 2021 Jun 14.

Italian Group for Adult Hematologic Diseases (GIMEMA), Data Center and Health Outcomes Research Unit. Rome, Italy.

: Remarkable advances have been made in acute promyelocytic leukemia (APL) research over the past decades and many patients can now also be cured without traditional chemotherapy. Therefore, the assessment of health-related quality of life (HRQoL) and other types of patient-reported outcomes (PROs) is highly relevant in the current APL treatment landscape.: A systematic literature review was performed to identify APL studies assessing HRQoL that were published over the last fifteen years. Read More

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Breed differences in the pharmacokinetics of orally administered meloxicam in domestic chickens ().

J Am Vet Med Assoc 2021 Jul;259(1):84-87

Objective: To determine the pharmacokinetics of meloxicam in Wyandotte hens and duration and quantity of drug residues in their eggs following PO administration of a single dose (1 mg of meloxicam/kg [0.45 mg of meloxicam/lb]) and compare results with those previously published for White Leghorn hens.

Animals: 8 healthy adult Wyandotte hens. Read More

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Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach.

Clin Pharmacokinet 2021 Jun 14. Epub 2021 Jun 14.

Department of Clinical Pharmacy, Institute of Pharmaceutical and Medical Chemistry, University of Münster, Corrensstr. 48, 48149, Münster, Germany.

Background And Objectives: Aripiprazole is an atypical antipsychotic drug that is metabolized by cytochrome P450 (CYP) 2D6 and CYP3A4, which mainly form its active metabolite dehydro-aripiprazole. Because of the genetic polymorphism of CYP2D6, plasma concentrations are highly variable between different phenotypes. In this study, phenotype-related physiologically based pharmacokinetic models were developed and evaluated to suggest phenotype-guided dose adjustments. Read More

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Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.

Adv Ther 2021 Jun 12. Epub 2021 Jun 12.

Department of Research, Development, and Innovation, FAES FARMA, Av. Autonomía 10, 48940, Leioa, Spain.

Introduction: Bilastine is a second-generation H antihistamine indicated for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. On the basis of the demonstrated efficacy and safety of the oral formulation, a new ophthalmic formulation of bilastine was recently developed. Previous preclinical studies had indicated that bilastine is mainly absorbed by the conjunctiva and shows low plasma concentration. Read More

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A Rare Case of Hypophosphataemic Osteomalacia in von Recklinghausen Neurofibromatosis.

Eur J Case Rep Intern Med 2021 25;8(5):002618. Epub 2021 May 25.

Department of Rheumatology, Rabta Hospital, Tunisia.

Background: Neurofibromatosis type 1 (NF1), also known as von Recklinghausen disease, is a one of the more common hereditary autosomal disorders. However, osteomalacia in neurofibromatosis type 1 is very rare tumour-induced osteomalacia; fibroblast growth factor-23 is usually implicated.

Patients And Methods: We report the case of a patient with a history of von Recklinghausen neurofibromatosis who presented with hypophosphataemic osteomalacia. Read More

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Stumbling block for inferior alveolar nerve block in predoctoral students: An analytical observational study and review of literature of mandibular nerve block techniques.

J Family Med Prim Care 2021 Apr 29;10(4):1633-1638. Epub 2021 Apr 29.

General Dentist, Ministry of Health, Kingdom of Saudi Arabia.

Introduction: Dentists earnestly try to practice painless treatment. Conventional inferior alveolar nerve block technique is preferred by most of the dentists despite its various modifications.However its failure rate as per literature is quite high. Read More

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Assessment of Oral Vancomycin-Induced Alterations in Gut Bacterial Microbiota and Metabolome of Healthy Men.

Front Cell Infect Microbiol 2021 27;11:629438. Epub 2021 May 27.

Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, South Korea.

Several classes of antibiotics have reduced the mortality caused by infectious diseases; however, orally administered antibiotics alter the composition of gut microbiota, leading to dysbiosis-related disease. Therefore, in this study, we used 16S rRNA gene sequencing- and metabolomics-based approaches to investigate the effects of oral vancomycin on gut bacterial microbiota and the metabolome in biospecimens collected from healthy men. Samples collected from 11 healthy men were analyzed using 16S rRNA gene sequencing and metabolomics. Read More

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Oral Baclofen Withdrawal Resulting in Hyperactive Delirium: A Case Report.

Cureus 2021 May 12;13(5):e14979. Epub 2021 May 12.

Psychiatry, University of Kentucky, Bowling Green, USA.

Baclofen is used in the treatment of muscle spasms by acting as an agonist GABA receptors. Limited case reports describing baclofen withdrawal-induced delirium have largely been demonstrated to occur upon cessation of intrathecal baclofen administration. Fewer reports have characterized the presentation from oral baclofen withdrawal. Read More

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Apremilast in the Management of Disseminated Granuloma Annulare.

Cureus 2021 May 9;13(5):e14918. Epub 2021 May 9.

Dermatology, St. Joseph Dermatopathology, Houston, USA.

Granuloma annulare (GA) is a common inflammatory skin condition that manifests as annular skin colored to erythematous papules and plaques. Disseminated GA is a subtype of GA that presents with diffuse cutaneous involvement. While topical and intralesional corticosteroids and phototherapy have been used as therapies for GA, there is no consensus on the best course of treatment for GA. Read More

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The effect of morning versus evening administration of empagliflozin on its pharmacokinetics and pharmacodynamics characteristics in healthy adults: a two-way crossover, non-randomised trial.

F1000Res 2021 26;10:321. Epub 2021 Apr 26.

Clinical Pharmacy Department, Faculty of Pharmacy, AinShms University, Cairo, 11566, Egypt.

: Empagliflozin is an SGLT2 inhibitor approved for use in patients with diabetes mellitus type 2 (DMT2) with or without other cardiovascular disease. Empagliflozin is taken once daily without rationale on the optimal timing for administration. This study aimed to determine the chronopharmacological effects of morning vs evening administration of empagliflozin (10 mg) in healthy Egyptian adults, by investigating the pharmacokinetics and pharmacodynamics parameters of empagliflozin depending on the intake time. Read More

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The Insulin Response to Oral Glucose in GIP and GLP-1 Receptor Knockout Mice: Review of the Literature and Stepwise Glucose Dose Response Studies in Female Mice.

Front Endocrinol (Lausanne) 2021 27;12:665537. Epub 2021 May 27.

Kansai Electric Power Hospital, Osaka, Japan.

A key factor for the insulin response to oral glucose is the pro-glucagon derived incretin hormone glucagon-like peptide-1 (GLP-1), together with the companion incretin hormone, glucose-dependent insulinotropic polypeptide (GIP). Studies in GIP and GLP-1 receptor knockout (KO) mice have been undertaken in several studies to examine this role of the incretin hormones. In the present study, we reviewed the literature on glucose and insulin responses to oral glucose in these mice. Read More

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