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gliclazide

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https://www.readbyqxmd.com/read/28547295/high-loading-dose-of-microencapsulated-gliclazide-formulation-exerted-a-hypoglycaemic-effect-on-type-1-diabetic-rats-and-incorporation-of-a-primary-deconjugated-bile-acid-diminished-the-hypoglycaemic-antidiabetic-effect
#1
Svetlana Golocorbin-Kon, Jelena Calasan, Boris Milijasevic, Sasa Vukmirovic, Mladena Lalic-Popovic, Momir Mikov, Hani Al-Salami
BACKGROUND AND OBJECTIVE: Gliclazide is a drug commonly used in type 2 diabetes mellitus. Recently, gliclazide has shown desirable pharmacological effects such as immunoregulatory and anti-clotting effects, which suggests potential applications in type 1 diabetes mellitus (T1DM). Gliclazide has variable absorption after oral administration, and thus using targeted-delivery techniques, such as microencapsulation, may optimise gliclazide absorption and potential applications in T1DM. Bile acids such as cholic acid have shown microcapsule-stabilising and controlled-release effects, and thus their incorporation into gliclazide microcapsules may further optimise gliclazide release, absorption and antidiabetic effects...
May 25, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28545434/effects-of-dangguibuxue-decoction-on-rat-glomerular-mesangial-cells-cultured-under-high-glucose-conditions
#2
Xiao-Dan Ren, Ying-Wen Zhang, Xiu-Ping Wang, Ya-Rong Li
BACKGROUND: Dysfunction of glomerular mesangial cells (GMCs) plays an important role in pathogenesis of diabetic nephropathy. Here, we investigated the effects of Dangguibuxue decoction (DBD), an herbal traditional Chinese medicinal (TCM) formula composed of Astragali Radix and Angelicae Sinensis Radix, on GMC proliferation and fibrogenesis under high-glucose (HG) conditions. METHODS: Sixty male Sprague Dawley rats were divided into 5 groups and administered intragastric 0...
May 25, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28530396/the-hydrotropic-action-of-cationic-hydrotrope-p-toluidinium-chloride-on-the-solubility-of-sparingly-soluble-gliclazide-drug-molecule-a-computational-study
#3
Shubhadip Das, Sandip Paul
We perform classical molecular dynamics simulations of sparingly soluble drug gliclazide (GLC) and hydrotrope p-toluidinium chloride (PTOL) in water with a regime of PTOL concentrations. Our results demonstrate that PTOL starts to self aggregate above its minimum hydrotrope concentration (MHC). Further these PTOL aggregates create a mixed micellar like framework in which the hydrophobic small tail part of most of the PTOL molecules direct towards the inside whereas in order to make favorable contact with water molecules its hydrophilic ammonium group points outward...
May 22, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28515791/vildagliptin-has-the-same-safety-profile-as-a-sulfonylurea-on-bone-metabolism-and-bone-mineral-density-in-post-menopausal-women-with-type-2-diabetes-a-randomized-controlled-trial
#4
Andre Gustavo Daher Vianna, Claudio Silva de Lacerda, Luciana Muniz Pechmann, Michelle Garcia Polesel, Emerson Cestari Marino, Victoria Zeghbi Cochenski Borba, Fellype de Carvalho Barreto
BACKGROUND: Several antidiabetic therapies affect bone metabolism. Sulfonylureas have the lowest impact on bone among oral antidiabetics. The objective of this study is to compare the effects of vildagliptin and gliclazide modified release (MR) on bone turnover markers (BTMs) and bone mineral density (BMD) in postmenopausal women with uncontrolled type 2 diabetes (T2D). METHODS: Forty-two postmenopausal women with uncontrolled T2D were randomly allocated into vildagliptin or gliclazide MR (control) groups...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28513098/nafld-and-t2d-the-importance-of-glycemic-control
#5
EDITORIAL
Zachary Bloomgarden
NAFLD is an important concern, as it can be identified in the majority of T2D persons and tracks with adverse outcome ((1,2) ). In the current issue of the Journal, Feng et al describe effects of liraglutide, gliclazide, and metformin in a well-characterized group of patients with poorly controlled type 2 diabetes (T2D) and nonalcoholic fatty liver disease (NAFLD), whose HbA1c levels decreased from 8.9 to 5.9%, from 9.0 to 6.5%, and from 9.4 to 6.0%, respectively ((3) ). Intrahepatic fat decreased from baseline levels around 35% in all groups, by approximately 60% with liraglutide, significantly more than the decrease of approximately 30% with gliclazide, and the reduction in transaminase levels was only significant with liraglutide and with metformin...
May 16, 2017: Journal of Diabetes
https://www.readbyqxmd.com/read/28513070/influence-of-quercetin-on-the-interaction-of-gliclazide-with-human-serum-albumin-spectroscopic-and-docking-approaches
#6
Miroslava Kameníková, Paul Georg Furtmüller, Mária Klacsová, Arturo Lopez-Guzman, José Luis Toca-Herrera, Anika Vitkovská, Ferdinand Devínsky, Pavel Mučaji, Milan Nagy
Protein-binding interactions are displacement reactions which have been implicated as the causative mechanisms in many drug-drug interactions. Thus, the aim of presented study was to analyse human serum albumin-binding displacement interaction between two ligands, hypoglycaemic drug gliclazide and widely distributed plant flavonoid quercetin. Fluorescence analysis was used in order to investigate the effect of substances on intrinsic fluorescence of human serum albumin (HSA) and to define binding and quenching properties of ligand-albumin complexes in binary and ternary systems, respectively...
May 16, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28480665/dend-syndrome-with-heterozygous-kcnj11-mutation-successfully-treated-with-sulfonylurea
#7
Ja Hyang Cho, Eungu Kang, Beom Hee Lee, Gu Hwan Kim, Jin Ho Choi, Han Wook Yoo
Permanent neonatal diabetes mellitus (PNDM) is caused by mutations in the ATP-sensitive potassium channel (KATP channel) subunits. Developmental delay, epilepsy, and neonatal diabetes (DEND) syndrome is the most severe form of PNDM and is characterized by various neurologic features. We report on a patient with DEND syndrome following initial misdiagnosis with type 1 DM, who was successfully switched from insulin to sulfonylurea therapy. A 50-day-old male presented with fever and seizure, complicated by persistent hyperglycemia...
June 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/28468231/adamantane-isothiourea-hybrid-derivatives-synthesis-characterization-in-vitro-antimicrobial-and-in-vivo-hypoglycemic-activities
#8
Lamya H Al-Wahaibi, Hanan M Hassan, Amal M Abo-Kamar, Hazem A Ghabbour, Ali A El-Emam
A new series of adamantane-isothiourea hybrid derivatives, namely 4-arylmethyl (Z)-N'-(adamantan-1-yl)-morpholine-4-carbothioimidates 7a-e and 4-arylmethyl (Z)-N'-(adamantan-1-yl)-4-phenylpiperazine-1-carbothioimidates 8a-e were prepared via the reaction of N-(adamantan-1-yl)morpholine-4-carbothioamide 5 and N-(adamantan-1-yl)-4-phenylpiperazine-1-carbothioamide 6 with benzyl or substituted benzyl bromides, in acetone, in the presence of anhydrous potassium carbonate. The structures of the synthesized compounds were confirmed by ¹H-NMR, (13)C-NMR, electrospray ionization mass spectral (ESI-MS) data, and X-ray crystallographic data...
April 29, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28460615/formulation-characterization-and-in-vitro-evaluation-of-fast-dissolving-tablets-containing-gliclazide-hydrotropic-solid-dispersions
#9
Jyotsana R Madan, Virendra J Kamate, Rajendra Awasthi, Kamal Dua
BACKGROUND: Low aqueous solubility is a major problem faced with new drug molecules. The purpose of this research was to provide a fast dissolving oral dosage form of gliclazide (GLZ) using the concept of mixed hydrotropy. METHODS: Solubility of GLZ was determined individually in sodium salicylate, nicotinamide, lactose, sodium acetate, urea, trisodium citrate and sodium benzoate. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope amount, mixed hydrotropic agents were used...
April 26, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28432754/intraclass-differences-in-the-risk-of-hospitalisazion-for-heart-failure-among-type-2-diabetic-patients-initiating-a-dipeptydil-peptidase-4-inhibitor-or-a-sulphonylurea-results-from-the-osmed-health-db-registry
#10
Gian Paolo Fadini, Stefania Saragoni, Pierluigi Russo, Luca Degli Esposti, Saula Vigili de Kreutzenberg, Mario Melazzini, Angelo Avogaro
AIMS: Heart failure (HF) is frequent in type 2 diabetes (T2D) and several glucose-lowering medications may increase HF risk. In the SAVOR-TIMI trial, patients on Saxagliptin experienced a 27% higher risk of hospitalisation for HF (HHF). In a retrospective study on 127,555 patients, we showed that DPP-4i therapy was associated with a lower HHF risk than sulphonylurea (SU) therapy. We herein re-analyzed such data to evaluate intraclass differences among DPP-4i and SU. MATERIALS AND METHODS: We included T2D patients initiating DPP-4i or SU alone or in combination with metformin...
April 21, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28431776/gliclazide
#11
Fatmah A M Al-Omary
Gliclazide is a second-generation oral hypoglycemic drug used for the treatment of noninsulin-dependent diabetes mellitus. It belongs to the sulfonylurea class that stimulates insulin secretion from pancreatic β-cells by inhibiting ATP-dependent potassium channels. Gliclazide also possesses unique antioxidant properties and other beneficial hemobiological effects. This profile represents a comprehensive description of the physical properties, chemical synthesis, spectroscopic characterization (FTIR, (1)H NMR, (13)C NMR, UV, and single-crystal X-ray), methods of analysis, pharmacological actions, and pharmacokinetic and pharmacodynamic properties of the title drug...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28397050/waist-circumference-dependent-peripheral-monocytes-change-after-gliclazide-treatment-for-chinese-type-2-diabetic-patients
#12
Qing Li, Hao-Yong Yu, Miao Chen, Feng Jiang, Jian Zhou, Yu-Qian Bao, Cheng Hu, Wei-Ping Jia
Gliclazide used for the treatment of type 2 diabetes mellitus (T2DM) stimulates insulin secretion and influences peripheral blood monocytes. The roles of gliclazide in peripheral monocytes of newly diagnosed T2DM patients were investigated in this study. A total of 105 newly diagnosed T2DM patients with no history of antihyperglycemic medication were treated with gliclazide-modified release for 16 weeks. The total and differential leukocyte profiles of peripheral blood were measured at baseline and week 16...
April 2017: Journal of Huazhong University of Science and Technology. Medical Sciences
https://www.readbyqxmd.com/read/28379974/non-invasive-phenotyping-and-drug-testing-in-single-cardiomyocytes-or-beta-cells-by-calcium-imaging-and-optogenetics
#13
Yu-Fen Chang, Connor N Broyles, Frances A Brook, Mark J Davies, Cameron W Turtle, Takeharu Nagai, Matthew J Daniels
Identification of drug induced electrical instability of the heart curtails development, and introduction, of potentially proarrhythmic drugs. This problem usually requires complimentary contact based approaches such as patch-clamp electrophysiology combined with field stimulation electrodes to observe and control the cell. This produces data with high signal to noise but requires direct physical contact generally preventing high-throughput, or prolonged, phenotyping of single cells or tissues. Combining genetically encoded optogenetic control and spectrally compatible calcium indicator tools into a single adenoviral vector allows the analogous capability for cell control with simultaneous cellular phenotyping without the need for contact...
2017: PloS One
https://www.readbyqxmd.com/read/28356096/%C3%AE-cell-protection-and-antidiabetic-activities-of-crassocephalum-crepidioides-asteraceae-benth-s-moore-extract-against-alloxan-induced-oxidative-stress-via-regulation-of-apoptosis-and-reactive-oxygen-species-ros
#14
Entaz Bahar, Kazi-Marjahan Akter, Geum-Hwa Lee, Hwa-Young Lee, Harun-Or Rashid, Min-Kyung Choi, Kashi Raj Bhattarai, Mir Mohammad Monir Hossain, Joushan Ara, Kishor Mazumder, Obayed Raihan, Han-Jung Chae, Hyonok Yoon
BACKGROUND: Medicinal plants are becoming more popular in the treatment of various diseases because of the adverse effects of the current therapy, especially antioxidant plant components such as phenols and flavonoids have a protective role against oxidative stress-induced degenerative diseases like diabetes. Thus, the purpose of this study was to investigate β-cell protection and antidiabetic activities of Crassocephalum crepidioides (Asteraceae) Benth. S. Moore. METHOD: The in-vitro study was conducted by the pancreatic β-cell culture and α-amylase inhibition technique which includes two methods, namely starch-iodine method and 3,5-dinitrosalicylic acid (DNSA) method...
March 29, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28349868/ultimate-biodegradability-and-ecotoxicity-of-orally-administered-antidiabetic-drugs
#15
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Hypoglycaemic pharmaceuticals are recently more and more frequently detected in the environment. In our previous study, we have shown that even though many of them undergo significant primary degradation some are transformed to stable products or undergo such transformation that a large part of the structure is still preserved. One of the main routes of elimination from wastewaters or surface waters is biodegradation and a lack thereof leads to accumulation in the environment. Within this work we tested the ultimate biodegradability of six oral antidiabetics: metformin and its main metabolite guanylurea, acarbose, glibenclamide, gliclazide, glimepiride and repaglinide...
March 16, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28332301/a-randomized-trial-comparing-gliclazide-liraglutide-and-metformin-effects-on-diabetes-with-nonalcoholic-fatty-liver-disease
#16
Wenhuan Feng, Caixia Gao, Yan Bi, Min Wu, Ping Li, Shanmei Shen, Wei Chen, Tingting Yin, Dalong Zhu
OBJECTIVE: To compare the effects of gliclazide, liraglutide, and metformin in type 2 diabetes mellitus (T2DM) patients with non-alcoholic fatty liver disease (NAFLD). METHODS: Eighty-seven subjects were randomized to receive liraglutide, metformin, or gliclazide for 24 weeks. Primary outcomes included hemoglobin A1c (HbA1c) levels, intrahepatic fat (IHF) content, and liver function. RESULTS: HbA1c levels and IHF content reduced after treatment in the three groups...
March 23, 2017: Journal of Diabetes
https://www.readbyqxmd.com/read/28330524/rapid-simultaneous-separation-of-four-oral-antidiabetic-drugs-and-quantitative-determination-of-glibenclamide-using-conventional-and-fused-core-silica-columns
#17
Laura Maria Fontes Prado Moraes, Gerson Antônio Pianetti, Isabela da Costa César, Christian Fernandes
Diabetes mellitus is a chronic disease with high and growing prevalence worldwide. Therefore, the development of fast and efficient methods for the QC of antidiabetic drugs is of fundamental importance. Two ultra-fast methods, using a conventional (C18 100 × 2.1 mm, 5 μm fully porous particle) column or a fused-core (C18 100 × 2.1 mm, 2.7 μm fused-core particle) column, were developed for the simultaneous determination of four antidiabetic drugs (chlorpropamide, glibenclamide, gliclazide, and glimepiride)...
February 15, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28323955/rapid-onset-of-diabetic-ketoacidosis-after-sglt2-inhibition-in-a-patient-with-unrecognized-acromegaly
#18
Marino Quarella, Daniel Walser, Michael Brändle, Jean-Yves Fournier, Stefan Bilz
Context: Diabetic ketoacidosis has been described as a rare complication of acromegaly and may be observed in 1% of affected patients. The well-described direct lipolytic effect of growth hormone results in increased availability of free fatty acids (FFAs) for hepatic ketogenesis and is an important pathogenic event. More recently, ketoacidosis has been identified as an important complication of sodium-glucose-transport-protein 2 inhibitors (SGLT2i). Increased pancreatic glucagon secretion, impaired renal ketone body clearance, and an increase in FFA concentrations secondary to decreased insulin concentrations are likely precipitating factors...
May 1, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28284082/simultaneous-determination-of-glipizide-and-its-four-hydroxylated-metabolites-in-human-urine-using-lc-ms-ms-and-its-application-in-urinary-phenotype-study
#19
Bo Tan, Aidong Yang, Weian Yuan, Yue Li, Lei Jiang, Jian Jiang, Furong Qiu
Cytochrome P450 (CYP) 2C9 and CYP2C19 genetic mutant could influence the plasma concentration of glipizide in human subjects, which refers to glipizide safety and adverse effects in clinic practice. A further study to investigate the relationship of the concentrations between glipizide and its metabolites in human with different CYP mutants was valuable. We firstly develop a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for simultaneous quantification of glipizide and its hydroxylated metabolites in human urine...
May 30, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28271251/efficacy-and-safety-of-metformin-and-sitagliptin-based-triple-antihyperglycemic-therapy-strategy-a-multicenter-randomized-controlled-non-inferiority-clinical-trial
#20
RANDOMIZED CONTROLLED TRIAL
Wen Xu, Yiming Mu, Jiajun Zhao, Dalong Zhu, Qiuhe Ji, Zhiguang Zhou, Bin Yao, Anhua Mao, Samuel S Engel, Bin Zhao, Yan Bi, Longyi Zeng, Xingwu Ran, Juming Lu, Linong Ji, Wenying Yang, Weiping Jia, Jianping Weng
Despite the current guideline's recommendation of a timely stepwise intensification therapy, the "clinical inertia", termed as the delayed treatment intensification, commonly exists in the real world, which may be partly due to the relatively little substantial evidence and no clear consensus regarding the efficacy and safety of triple oral agents in patients inadequately controlled with dual therapy. In this clinical trial performed in 237 centers in China, 5,535 type 2 diabetic patients inadequately controlled by previous therapies were treated with a stable metformin/sitagliptin dual therapy for 20 weeks...
March 2017: Science China. Life Sciences
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