scholarly journals Cross Referencing 2D-LC Determination of Intact Gliptins in Urine

2020 ◽  
Vol 58 (10) ◽  
pp. 907-914
Author(s):  
Amal M Mohamad ◽  
Cenk A Andac ◽  
Sena Caglar Andac

Abstract Dipeptidyl peptidase-4 inhibitors, so-called gliptins, constitute a fairly novel class of oral hypoglycemic agents. The development and validation of an automated online SPE-LC-UV method to determine intact sitagliptin, saxagliptin, vildagliptin and metformin simultaneously in human urine samples were performed. For the two-dimensional chromatographic separation, a Gemini C18 (250.0 × 4.6 mm i.d., 110 A0, 5.0 μ) analytical column and a gradient elution with 10.0 mM o-phosphoric acid and methanol and for the online SPE analysis of urine samples, a LiChrospher® ADS SPE-column (20.0 mm × 2.0 mm i.d., 25.0 μm) were used through the study. The fractionation, transfer, elution and separation of the spiked urine samples were achieved in just 9.57 min runtime with 12.0 mL of solvent consumption which was green and economical compared to other sample preparation methods. The calibration curves were determined to be linear in a wide range of 0.10–100.00 μg/mL with satisfactory regression coefficients. Method developed for two-dimensional determination of gliptins would be useful as a reference in therapeutic drug monitoring and screening for forensic medical cases which involve the abuse, unintentional or misuse of multiple gliptins in terms of its practical use, easy detection and reliable results.

2018 ◽  
Vol 11 ◽  
pp. 117954761876335 ◽  
Author(s):  
Takumi Minezumi ◽  
Shin-ichi Takeda ◽  
Yusuke Igarashi ◽  
Kentaro Sato ◽  
Yoshiaki Murakami ◽  
...  

Blood glucose management in patients undergoing dialysis is clinically challenging. In this population, most conventional oral hypoglycemic agents are contraindicated, especially from the perspective of pharmacokinetics. Dipeptidyl peptidase-4 inhibitors exert unique pharmacologic actions via glucose-dependent mechanism and have an excellent tolerability profile with a very low risk of hypoglycemia. Furthermore, the literature reports that some dipeptidyl peptidase-4 inhibitors such as teneligliptin can be administered at the usual dose, regardless of a patient’s level of renal impairment. In this article, we report a case of hypoglycemic coma with a blood glucose level of 23 mg/dL. The patient became fully conscious shortly after receiving a glucose injection; however, severe hypoglycemia recurred for approximately 1.5 days. It eventually disappeared on the discontinuation of teneligliptin, which was the only antidiabetic agent that he had received. The present case may provide deep insights into promoting the safe use of hypoglycemic agents in patients undergoing dialysis.


2020 ◽  
Vol 24 (4) ◽  
pp. 368-373
Author(s):  
Naghma Ms. ◽  
Sadia M Azam Khan ◽  
Atta Ullah Khan ◽  
Zahoor Ahmed ◽  
Muhammad Umar ◽  
...  

Objective: This trial was conducted to evaluate the effectiveness of oral hypoglycemic agents on diabetic control and biochemical parameters of known diabetic subjects. Introduction:  T2DM   occurs due to abnormal metabolism of carbohydrate, proteins and lipids leading to increased blood glucose characterized by polyuria and polydypsia due to relative 5deficiency or lack of insulin. Beside dietary control and insulin therapy, various oral hypoglycemic such as sulfonylurea biguanide, thiazolidinedione, DPP–4 inhibitors, glucagon–like peptide inhibitors and SGL2.   Material and Methods: This comparative trial was carried out on previously diagnosed type–2 diabetic subjects. This trial was conducted at health care centers of District Nowshehra viz. NMC Nowshehra, DHQ Hospital Nowshehra, and ICS, Peshawar in collaboration with KMC and PIMC Peshawar, Khyber Pakhtunkhwa, Pakistan. A total of 200 known diabetic subjects were randomly recruited on the basis of predetermined selection criteria and were splited into two groups. Group A having 100 diabetic subjects was given DPP–4 inhibitor; Sitagliptin 50 mg two times a day alone for six (06) months while Group B comprising of 100 patients were treated   with combination of DPP–4 inhibitor (Sitagliptin 50 mg 1BD) and Metformin in a dose of 500 mg two times a day. Venous blood samples were taken from each patient in both fasting (10–12 hour night long fast) and random (2 hour post prandial) state. FBS, RBS, HbA1C, S. creatinine and fasting S. lipid profile were determined by using spectrophotometric colorimetric methods using kits (procured from Elitech, Spain) at  03 and 06 months follow up. Inclusion criteria was subjects with T2DM of age 18 years and above. T2DM patients on insulin, diabetic nephropathy and retinopathy were excluded. The data was analyzed by using SPSS software version 20. Results: Significant results (p < 0.05) were seen for glycemic control (FBS, RBS, HbA1C) in Group B as compare to Group A patients.


2019 ◽  
Vol 1 (2) ◽  
pp. 273-289 ◽  
Author(s):  
Junichi Kato ◽  
Yohei Shirakami ◽  
Masahito Shimizu

The global deaths due to colorectal cancer and diabetes mellitus have increased by 57% and 90%, respectively. The relationship between various cancers and diabetes mellitus has been shown in multiple epidemiological studies. Hence, better management of diabetes mellitus is expected to reduce the risk of various cancers. This review focuses on colorectal cancer and aims to summarize recent findings on the antitumor effects of various oral hypoglycemic drugs on colorectal cancer and their estimated mechanisms. Of the seven classes of oral hypoglycemic agents, only metformin was found to have suppressive effects on colorectal cancer in both clinical and basic research. Clinical and basic researches on suppressing effects of glinides, dipeptidyl peptidase-4 inhibitors, thiazolidinedione, α-glucosidase inhibitors, and sodium glucose cotransporter-2 inhibitors against colon carcinogenesis have been insufficient and have not arrived at any conclusion. Therefore, further research regarding these agents is warranted. In addition, the suppressive effects of these agents in healthy subjects without diabetes should also be investigated.


2020 ◽  
Vol 23 (4) ◽  
pp. 357-367
Author(s):  
Nina A. Petunina ◽  
Irina A. Kuzina ◽  
Ludmila V. Nedosugova

With the growing prevalence of type 2 diabetes mellitus (T2DM) the possibility of treating it with available drugs is one of the main issues. Although glycemic control and reduction of micro- and macrovascular outcomes remain important aspects of treatment, the main limiting factors are the availability and cost of oral hypoglycemic agents. Although newer agents, such as sodium -glucose cotransporter 2 inhibitors, dipeptidyl peptidase-4 inhibitors and glucagon-like peptide 1 receptor agonists, potentially being valuable for patients with insulin resistance and cardiovascular complications, they are relatively expensive and have limited availability. Second-generation sulfonylureas effectively reduce glycated hemoglobin and contribute to the prevention of micro- and macrovascular complications of T2DM The review substantiates the role of Gliclazide MR as a more affordable drug for the treatment of T2DM, the safety of which has been confirmed by many studies; cardio-and nephroprotective effects are shown, as well as mechanisms for influencing в-cells of the pancreas and extrapancreatic effects through activation of phospholipase C and the G-protein-сoupled-receptors (GPCR) are analyzed. The latest data on the assessment of adverse events of Gliclazide MR are presented in comparison with both other sulfonylureas and glucose-lowering drugs of other classes.


Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 278
Author(s):  
Jennifer Lagoutte-Renosi ◽  
Bernard Royer ◽  
Vahideh Rabani ◽  
Siamak Davani

Ticagrelor is an antiplatelet agent which is extensively metabolized in an active metabolite: AR-C124910XX. Ticagrelor antagonizes P2Y12 receptors, but recently, this effect on the central nervous system has been linked to the development of dyspnea. Ticagrelor-related dyspnea has been linked to persistently high plasma concentrations of ticagrelor. Therefore, there is a need to develop a simple, rapid, and sensitive method for simultaneous determination of ticagrelor and its active metabolite in human plasma to further investigate the link between concentrations of ticagrelor, its active metabolite, and side effects in routine practice. We present here a new method of quantifying both molecules, suitable for routine practice, validated according to the latest Food and Drug Administration (FDA) guidelines, with a good accuracy and precision (<15% respectively), except for the lower limit of quantification (<20%). We further describe its successful application to plasma samples for a population pharmacokinetics study. The simplicity and rapidity, the wide range of the calibration curve (2–5000 µg/L for ticagrelor and its metabolite), and high throughput make a broad spectrum of applications possible for our method, which can easily be implemented for research, or in daily routine practice such as therapeutic drug monitoring to prevent overdosage and occurrence of adverse events in patients.


2015 ◽  
Vol 13 (2) ◽  
pp. 6-9
Author(s):  
Binaya Shrestha

Introduction: Diabetes Mellitus is one of the major causes of morbidity, mortality and needs lifelong treatment. There is a wide range of variation in the prices of antidiabetic drugs marketed in Nepal. Thus, a study was planned to find out price variations in the oral hypoglycemic drugs available singly and number of manufacturing companies for each, also to evaluate the difference in cost of different brands of same active drug by calculating percentage variation of cost.Methods: Cost of a particular drug being manufactured by different companies, in the same strength and dosage forms was obtained from the price list provided by the pharmaceutical companies in Nepal and Indian Drug Review September 2013. The difference in the maximum and minimum price of the same drug manufactured by different pharmaceutical companies and percentage variation in price was calculated.Results: Percentage price variation of the commonly used drugs found was metformin (500mg) 171.42%, metformin (850mg) 128.42%, metformin (1000mg) 80%, pioglitazone (15mg) 150% pioglitazone (30mg) 188.89%, sitagliptin (50mg) 33.33%, sitagliptin (100mg) 40% acarbose (25mg) 39.58%, acarbose (50mg) 32.60%, gliclazide (80mg) 108%, gliclazide (40mg) 83.33%, glibenclamide (2.5mg) 87%, glibenclamide (5mg), 80%, glimiperide (1mg) 91.67%, glimiperide (2mg) 300%, glimiperide (3mg) 100%, glimiperide (4mg) 36.84%.Conclusion: The average percentage price variation of different brands of the same oral hypoglycemic drugs manufactured in Nepal is very wide. The appraisal and management of marketing drugs should be directed toward maximizing the benefits of therapy and minimizing negative personal and economic consequences.


2017 ◽  
Vol 1528 ◽  
pp. 35-40 ◽  
Author(s):  
Junwei Liu ◽  
Zhifen Deng ◽  
Zuoyi Zhu ◽  
Yong Wang ◽  
Guoqing Wang ◽  
...  

2015 ◽  
Vol 1 (1) ◽  
pp. 36-42
Author(s):  
Rameshwar Mahaseth

The endogenous incretins, glucose-dependent insulinotropic polypeptide and Glucagon-like peptide, are peptide hormones secreted from endocrine cells in the small intestine. Glucagon-like peptide-1 stimulates insulin and suppresses glucagon secretion, delays gastric emptying, and reduces appetite and food intake, which explains the positive effect of incretin mimetics on weight. The incretins have also been shown to have a sustained improvement in glycemic control over three years. A wide range of cardiovascular benefits have also been claimed, such as lowering of blood pressure and postprandial lipids. Clinical trials with the incretin mimetic exenatide and liraglutide show reductions in fasting and postprandial glucose concentrations, and haemoglobin A1c (1–2%), associated with weight loss (2–5 kg). The most common adverse event associated with Glucagon-like peptide-1 receptor agonists is nausea, which lessens over time. Orally administered Dipeptidyl Peptidase-4 inhibitors reduce hemoglobin A1c by 0·5–1·0%, with few adverse effects and no weight gain. These new classes of anti-diabetic agents also expand β-cell mass in preclinical studies. However, long-term clinical studies are still needed to determine the benefits of incretin for the treatment of type 2 diabetes. DOI: http://dx.doi.org/10.3126/jpahs.v1i1.13015 Journal of Patan Academy of Health Sciences. 2014 Jun;1(1):36-42 


RSC Advances ◽  
2015 ◽  
Vol 5 (43) ◽  
pp. 34342-34352 ◽  
Author(s):  
Yiran Fan ◽  
Guanghu Shen ◽  
Ping Li ◽  
Xiaonan Xi ◽  
Haiting Wu ◽  
...  

An integration of sample pretreatment automation using online SPE technique could provide an easy to use, efficient, sensitive and high quality methods for TDM.


Sign in / Sign up

Export Citation Format

Share Document