keyword
MENU ▼
Read by QxMD icon Read
search

Repaglinide

keyword
https://www.readbyqxmd.com/read/28276787/granulated-colloidal-silicon-dioxide-based-self-microemulsifying-tablets-as-a-versatile-approach-in-enhancement-of-solubility-and-therapeutic-potential-of-anti-diabetic-agent-formulation-design-and-in-vitro-in-vivo-evaluation
#1
Vikas Pandey, Ritu M Gilhotra, Seema Kohli
The current research work was executed with an aim to explore and promote the potential of self-microemusifying drug delivery systems (SMEDDS) in the form of tablets, in order to enhance solubility and oral bioavailability of poorly aqueous soluble drug Repaglinide (RPG). RPG-loaded liquid SMEDDS were developed consisting Labrafil M 1944CS, Kolliphor EL and Propylene glycol, which were then characterized on various parameters. After characterization and optimization, liquid SMEDDS were converted into solid form by adsorbing on Aeroperl® 300 pharma and polyplasdone(TM) XL...
February 23, 2017: Drug Development and Industrial Pharmacy
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
#2
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...
February 7, 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/28238899/estimation-of-the-contribution-of-cyp2c8-and-cyp3a4-in-repaglinide-metabolism-by-human-liver-microsomes-under-various-buffer-conditions
#3
Toshiyuki Kudo, Hitomi Goda, Yuki Yokosuka, Ryo Tanaka, Seina Komatsu, Kiyomi Ito
We have previously reported that the microsomal activities of CYP2C8 and CYP3A4 largely depend on the buffer condition used in in vitro metabolic studies, with different patterns observed between the two isozymes. In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. Montelukast and ketoconazole showed a potent and concentration-dependent inhibition of CYP2C8-mediated paclitaxel 6α-hydroxylation and CYP3A4-mediated triazolam α-hydroxylation, respectively, without dependence on the buffer condition...
February 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28169935/biomedical-informatics-approaches-to-identifying-drug-drug-interactions-application-to-insulin-secretagogues
#4
Xu Han, ChienWei Chiang, Charles E Leonard, Warren B Bilker, Colleen M Brensinger, Lang Li, Sean Hennessy
BACKGROUND: Drug-drug interactions with insulin secretagogues are associated with increased risk of serious hypoglycemia in patients with type 2 diabetes. We aimed to systematically screen for drugs that interact with the five most commonly used secretagogues-glipizide, glyburide, glimepiride, repaglinide, and nateglinide-to cause serious hypoglycemia. METHODS: We screened 400 drugs frequently co-prescribed with the secretagogues as candidate interacting precipitants...
February 1, 2017: Epidemiology
https://www.readbyqxmd.com/read/28115226/dual-crosslinked-pectin-alginate-network-as-sustained-release-hydrophilic-matrix-for-repaglinide
#5
Rajendra Awasthi, Giriraj T Kulkarni, Malipeddi Venkata Ramana, Terezinha de Jesus Andreoli Pinto, Irene Satiko Kikuchi, Daniela Dal Molim Ghisleni, Marina de Souza Braga, Paul De Bank, Kamal Dua
Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half-life of approximately 1h. Developing a controlled and prolonged release delivery system is required to maintain its therapeutic plasma concentration and to eliminate its adverse effects particularly hypoglycemia. The present study aimed to develop controlled release repaglinide loaded beads using sodium alginate and pectin with dual cross-linking for effective control of drug release. The prepared beads were characterized for size, percentage drug entrapment efficiency, in vitro drug release and the morphological examination using scanning electron microscope...
April 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28092161/estimation-of-ellagic-acid-and-or-repaglinide-effects-on-insulin-signaling-oxidative-stress-and-inflammatory-mediators-of-liver-pancreas-adipose-tissue-and-brain-in-insulin-resistant-type-2-diabetic-rats
#6
COMPARATIVE STUDY
Mohamed M Amin, Mahmoud S Arbid
Even though ellagic acid has previously been valued in many models of cancer, so far its full mechanistic effect as a natural antiapoptotic agent in the prevention of type 2 diabetes complications has not been completely elucidated, which was the goal of this study. We fed albino rats a high-fat fructose diet (HFFD) for 2 months to induce insulin resistance/type 2 diabetes and then treated the rats with ellagic acid (10 mg/kg body weight, orally) and/or repaglinide (0.5 mg/kg body weight, orally) for 2 weeks...
February 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/28067999/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-cyp-enzyme-substrates-sildenafil-amlodipine-tolbutamide-and-repaglinide
#7
Michael Gillen, Chun Yang, David Wilson, Shakti Valdez, Caroline Lee, Bradley Kerr, Zancong Shen
Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors. In vitro assays indicate that lesinurad is an inducer of CYPs in the order CYP3A > CYP2C8 > CYP2C9 > CYP2C19 > CYP2B6 and an inhibitor of CYP2C8 and CYP2C9. To investigate the drug interaction potential of lesinurad, clinical drug interaction studies were conducted. Open-label studies in volunteers investigated the effects of single-/multiple-dose lesinurad on the pharmacokinetics of sildenafil and amlodipine (CYP3A4 induction), tolbutamide (CYP2C9 inhibition/induction), and repaglinide (CYP2C8 inhibition/induction)...
January 9, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28000562/synchronized-fast-spe-and-uflc-methods-for-the-analyses-of-eight-antidiabetic-drugs-in-human-plasma
#8
Imran Ali, Kamlesh Dutta, A K Jain
The number of the diabetic patients is increasing rapidly globally. The treatment of these patients is a complex phenomenon due to the use of the different drugs. The present article reports a synchronized fast SPE-UFLC separation of eight antidiabetic drugs in human plasma. The separated drugs include metformin HCl, vildagliptin, gliclazide, linagliptin, sitagliptin, pioglitazone, glimepiride and repaglinide. The column used was Sunshell C18 (150 x 4.6 mm, 2.6 µm) with mobile phase of acetate buffer (0.05% TEA in 0...
December 20, 2016: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/27998799/phospholipid-complex-enriched-micelles-a-novel-drug-delivery-approach-for-promoting-the-antidiabetic-effect-of-repaglinide
#9
Ahmed Alaa Kassem, Sameh Hosam Abd El-Alim, Mona Basha, Abeer Salama
To enhance the oral antidiabetic effect of repaglinide (RG), a newly emerging approach, based on the combination of phospholipid complexation and micelle techniques, was employed. Repaglinide-phospholipid complex (RG-PLC) was prepared by the solvent-evaporation method then characterized using Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffraction (XPRD). The results revealed obvious disappearance of the characteristic peaks of the prepared RG-PLCs confirming the formation of drug-phospholipid complex...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27967230/pathophysiology-and-management-of-hypoglycemiain-end-stage-renal-disease-patients-a-review
#10
Roma Y Gianchandani, Shristi Neupane, Jennifer J Iyengar, Michael Heung
OBJECTIVE: This review focuses on hypoglycemia in patients with end-stage renal disease (ESRD). It discusses the pathophysiology of glucose metabolism in the kidney, the impact of dialysis on glucose and insulin metabolism, and the challenges of glucose monitoring in ESRD. The clinical relevance of these changes is reviewed in relation to altered blood glucose targets and modification of antidiabetes therapy to prevent hypoglycemia. Based on current data and guidelines, recommendations for the outpatient and inpatient setting are provided for diabetes management in ESRD...
March 2017: Endocrine Practice
https://www.readbyqxmd.com/read/27904436/effects-of-metformin-on-blood-and-urine-pro-inflammatory-mediators-in-patients-with-type-2-diabetes
#11
Wei Chen, Xiaojie Liu, Shandong Ye
BACKGROUND: Metformin has been used for the treatment of type 2 diabetes by suppressing hepatic gluconeogenesis. It has been shown that the subclinical inflammatory responses play important roles in the pathogenesis of type 2 diabetes. In the present study, we determined the effects of metformin on the levels of pro-inflammatory cytokines (i.e., IL-6, TNF-α, and MCP-1) and anti-inflammatory mediator IL-10 in blood and urine of patients with type 2 diabetes. There were 210 patients with type 2 diabetes, which were randomized into metformin (n = 112) and non-metformin (gliclazide, acarbose, and repaglinide, n = 98) groups...
2016: Journal of Inflammation
https://www.readbyqxmd.com/read/27862160/in-vitro-and-physiologically-based-pharmacokinetic-based-assessment-of-drug-drug-interaction-potential-of-canagliflozin
#12
Rao N V S Mamidi, Shannon Dallas, Carlo Sensenhauser, Heng Keang Lim, Ellen Scheers, Peter Verboven, Filip Cuyckens, Laurent Leclercq, David C Evans, Michael F Kelley, Mark D Johnson, Jan Snoeys
AIMS: Canagliflozin is a recently approved drug for use in the treatment of type 2 diabetes. The potential for canagliflozin to cause clinical drug-drug interactions (DDIs) was assessed. METHODS: DDI potential of canagliflozin was investigated using in vitro test systems containing drug metabolizing enzymes or transporters. Basic predictive approaches were applied to determine potential interactions in vivo. A physiologically-based pharmacokinetic (PBPK) model was developed and clinical DDI simulations were performed to determine the likelihood of cytochrome P450 (CYP) inhibition by canagliflozin...
November 11, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27857189/a-variation-in-kcnq1-gene-is-associated-with-repaglinide-efficacy-on-insulin-resistance-in-chinese-type-2-diabetes-mellitus-patients
#13
Xueyan Zhou, Jing Zhu, Zejun Bao, Zhenhai Shang, Tao Wang, Jinfang Song, Juan Sun, Wei Li, Temitope Isaac Adelusi, Yan Wang, Dongmei Lv, Qian Lu, Xiaoxing Yin
Repaglinide is an insulin secretagogue that often exhibits considerable interindividual variability in therapeutic efficacy. The current study was designed to investigate the impact of KCNQ1 genetic polymorphism on the efficacy of repaglinide and furthermore to identify the potential mechanism of action in patients with type 2 diabetes. A total of 305 patients and 200 healthy subjects were genotyped for the KCNQ1 rs2237892 polymorphism, and 82 patients with T2DM were randomized for the oral administration of repaglinide for 8 weeks...
November 18, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27769931/development-of-repaglinide-microspheres-using-novel-acetylated-starches-of-bitter-and-chinese-yams-as-polymers
#14
Adenike Okunlola, Amusa Sarafadeen Adebayo, Moji Christianah Adeyeye
Tropical starches from Dioscorea dumetorum (bitter) and Dioscorea oppositifolia (Chinese) yams were acetylated with acetic anhydride in pyridine medium and utilized as polymers for the delivery of repaglinide in microsphere formulations in comparison to ethyl cellulose. Acetylated starches of bitter and Chinese yams with degrees of substitution of 2.56 and 2.70 respectively were obtained. Acetylation was confirmed by FTIR, (1)H NMR spectroscopy. A 3(2) factorial experimental design was performed using polymer type and drug-polymer ratio as independent variables...
January 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27734142/a-liquid%C3%A2-chromatography-tandem-mass-spectrometry-analysis-of-nine-cytochrome-p450-probe-drugs-and-their-corresponding-metabolites-in-human-serum-and-urine
#15
Elena Puris, Markku Pasanen, Mikko Gynther, Merja R Häkkinen, Jussi Pihlajamäki, Tapani Keränen, Paavo Honkakoski, Hannu Raunio, Aleksanteri Petsalo
Cocktail phenotyping using specific probe drugs for cytochrome P450 (CYP) enzymes provides information on the real-time activity of multiple CYPs. We investigated different sample preparation techniques and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method with simple protein precipitation for the analysis of nine CYP probe drugs and their metabolites in human serum and urine. Specific CYP probe drugs (melatonin, CYP1A2; nicotine, CYP2A6; bupropion, CYP2B6; repaglinide, CYP2C8; losartan, CYP2C9; omeprazole, CYP2C19 and CYP3A4; dextromethorphan, CYP2D6; chlorzoxazone, CYP2E; midazolam, CYP3A4) and their main metabolites, with the exception of 3'-hydroxyrepaglinide, were quantified in human serum and urine using the developed LC-MS/MS method...
January 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/27665059/drug-drug-interactions-between-immunosuppressants-and-antidiabetic-drugs-in-the-treatment-of-post-transplant-diabetes-mellitus
#16
REVIEW
Thomas Vanhove, Quinten Remijsen, Dirk Kuypers, Pieter Gillard
Post-transplant diabetes mellitus is a frequent complication of solid organ transplantation that generally requires treatment with lifestyle interventions and antidiabetic medication. A number of demonstrated and potential pharmacokinetic drug-drug interactions (DDIs) exist between commonly used immunosuppressants and antidiabetic drugs, which are comprehensively summarized in this review. Cyclosporine (CsA) itself inhibits the cytochrome P450 (CYP) 3A4 enzyme and a variety of drug transporters. As a result, it increases exposure to repaglinide and sitagliptin, will likely increase the exposure to nateglinide, glyburide, saxagliptin, vildagliptin and alogliptin, and could theoretically increase the exposure to gliquidone and several sodium-glucose transporter (SGLT)-2 inhibitors...
September 14, 2016: Transplantation Reviews
https://www.readbyqxmd.com/read/27659712/clinical-and-molecular-characterization-of-a-novel-ins-mutation-identified-in-patients-with-mody-phenotype
#17
Barbara Piccini, Rosangela Artuso, Lorenzo Lenzi, Monica Guasti, Giulia Braccesi, Federica Barni, Emilio Casalini, Sabrina Giglio, Sonia Toni
Correct diagnosis of Maturity-Onset Diabetes of the Young (MODY) is based on genetic tests requiring an appropriate subject selection by clinicians. Mutations in the insulin (INS) gene rarely occur in patients with MODY. This study is aimed at determining the genetic background and clinical phenotype in patients with suspected MODY. 34 patients with suspected MODY, negative for mutations in the GCK, HNF1α, HNF4α, HNF1β and PDX1 genes, were screened by next generation sequencing (NGS). A heterozygous INS mutation was identified in 4 members of the same family...
November 2016: European Journal of Medical Genetics
https://www.readbyqxmd.com/read/27647480/efficacy-and-safety-of-repaglinide-added-to-sitagliptin-in-japanese-patients-with-type-2-diabetes-a-randomized-24-week-open-label-clinical-trial
#18
Akihiro Nishimura, Shuki Usui, Naoki Kumashiro, Hiroshi Uchino, Azusa Yamato, Daijiro Yasuda, Kaoru Nagasawa, Minoru Okubo, Yasumichi Mori, Takahisa Hirose
Although sitagliptin and repaglinide monotherapies improve postprandial hyperglycemia, the long-term effects and safety of their combination has not been examined. In this randomized 24-week trial of Japanese patients with poor control (HbA1c 7.0-8.5%) by sitagliptin, we divided 40 patients randomly into two equal groups of the repaglinide add-on to sitagliptin (ADD-ON, n=20), or sitagliptin switched to repaglinide (SWITCH, n=20). The meal tolerance test was carried out at weeks 0 and 24. The primary outcomes were changes in HbA1c and area under the curves (AUC) of glucose from the baseline to week 24...
December 30, 2016: Endocrine Journal
https://www.readbyqxmd.com/read/27635199/antioxidant-properties-of-repaglinide-and-its-protections-against-cyclosporine-a-induced-renal-tubular-injury
#19
Dao Li, Jin Li, Hui Li, Qiong Wu, Qi-Xiong Li
OBJECTIVES: Repaglinide (RG) is an antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus. It has a good safety and efficacy profile in diabetic patients with complications in renal impairment and is an appropriate treatment choice, even for individuals with more severe degrees of renal malfunctions. The aim of the present study was to examine the protective effect of RG on cyclosporine A (CsA)-induced rat renal impairment and to evaluate the antioxidant mechanisms by which RG exerts its protective actions...
July 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27631194/mapping-slco1b1-genetic-variation-for-global-precision-medicine-in-understudied-regions-in-africa-a-focus-on-zulu-and-cape-admixed-populations
#20
Nisreen Hoosain, Brendon Pearce, Clifford Jacobs, Mongi Benjeddou
The U.S. President Barack Obama has announced, in his State of the Union address on January 20, 2015, the Precision Medicine Initiative, a US$215-million program. For global precision medicine to become a reality, however, biological and environmental "variome" in previously understudied populations ought to be mapped and catalogued. Chief among the molecular targets that warrant global mapping is the organic anion-transporting polypeptide 1B1 (OATP1B1), encoded by solute carrier organic anion transporter family member 1B1 (SLCO1B1), a hepatic uptake transporter predominantly expressed in the basolateral side of hepatocytes...
September 2016: Omics: a Journal of Integrative Biology
keyword
keyword
42765
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"