摘要 :
Two simple and sensitive visible spectrophotometric methods have been developed for the estimation of Sitagliptine in pure and pharmaceutical dosage forms. These methods are based on the nucleophillic substitution reaction between...
展开
Two simple and sensitive visible spectrophotometric methods have been developed for the estimation of Sitagliptine in pure and pharmaceutical dosage forms. These methods are based on the nucleophillic substitution reaction between NQS and Sitagliptine resulting in the formation of colored chromogen (λ_(max)450 nm) and the reaction between Picric acid (PA) and Sitagliptine resulting in the formation of molecular salt (λ_(max) 420 nm). The absorbance is measured against the corresponding reagent blanks. These methods have been statistically evaluated and found to be precise and accurate.
收起
摘要 :
This paper describes the development and validation of an isocratic LC-UV method for the assay of sitagliptin phosphate in tablets, a drug recently approved for the treatment of type 2 diabetes mellitus (DM). The method employs a ...
展开
This paper describes the development and validation of an isocratic LC-UV method for the assay of sitagliptin phosphate in tablets, a drug recently approved for the treatment of type 2 diabetes mellitus (DM). The method employs a Phenomenex~(~R) C18 column (150mm X 4.6mm I.D., 5 (mu)m with 0.025 M phosphate buffer pH 6.8: acetonitrile (60:40, v/v) as mobile phase, at a 0.8 mL min~(-1) flow rate and UV detection at 267 nm. The chromatographic separation was obtained within a retention time of 3.7 min. The method was linear (r velence 0.9999) in the range of 25-75 (mu)g.mL~(-1). The method's specificity and stability-indicating capability were proved through force degradation studies, being the peak purity evaluated by PDA detector. Sitagliptin phosphate was exposed to oxidative, hydrolytic and photolytic stress conditions, and no interference from degradation products was observed. The method has shown good and consistent recoveries (mean value 100.0percent) with low intra and inter-day relative standard deviation (RSD). In robustness study, it was observed that peak area was unaffected by small changes in critical factors. The validated method can be successfully applied to determine sitagliptin in tablets and in stability studies.
收起
摘要 :
<abstract_text><p>In this work, different chemometric calibration models were developed and validated for the purpose of determining of ternary mixture of oral antidiabetic drugs; vildagliptin (VDG), saxagliptin (SAX) and sitaglip...
展开
<abstract_text><p>In this work, different chemometric calibration models were developed and validated for the purpose of determining of ternary mixture of oral antidiabetic drugs; vildagliptin (VDG), saxagliptin (SAX) and sitagliptin phosphate (STG). The used models were Partial least squares (PLS) and Artificial Neural Networks (ANN). However, on these various models the impact of genetic algorithm (GA) as a form of variable selection was also investigated. The UV spectral data was used as basis in the quantitative study of the drugs analyzed in bulk and product formulations. The concentration range of the calibration curves of VDG, SAX and STG were 10-22 mu g mL(-1), 24-40 mu g mL(-1) and 82-130 mu g mL(-1), respectively. The calibration set included nineteen mixtures and the others six were used as a validation set to test the predictability of the developed multivariate models. The validation parameters of the evaluated methods were statistically determined. For the analysis of drugs studied in laboratory-prepared mixtures and their dosage forms, PLS-1, GA-PLS-1, ANN, and GA-ENN were successfully employed. The results obtained by the developed methods were compared to those given by a reported method and there were no statistically significant differences regarding accuracy and precision. (C) 2020 Elsevier B.V. All rights reserved.</p></abstract_text>
收起
摘要 :
AimsTo compare the once-weekly glucagon-like peptide-1 (GLP-1) receptor dulaglutide with the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin after 104weeks of treatment.
摘要 :
Aims/Introduction: Type 2 diabetes mellitus is a progressive disease that frequently requires patients to use more than one oral antihyperglycemic agent to achieve adequate glycemic control. The present multicenter, randomized stu...
展开
Aims/Introduction: Type 2 diabetes mellitus is a progressive disease that frequently requires patients to use more than one oral antihyperglycemic agent to achieve adequate glycemic control. The present multicenter, randomized study assessed the efficacy and safety of the addition of sitagliptin to ongoing voglibose monotherapy (0.2-0.3 mg three times daily) in Japanese patients with type 2 diabetes mellitus who had inadequate glycemic control (glycated hemoglobin ≥6.9% and <10.5%). Materials and Methods: The present study had an initial 12-week, double-blind treatment period in which patients were randomized (1:1) to sitagliptin 50 mg/day (n = 70) or placebo (n = 63), followed by a 40-week, open-label treatment period during which all patients received sitagliptin 50 mg/day, that could have been increased to 100 mg/day for patients meeting predefined glycemic criteria. Results: After 12 weeks, treatment with sitagliptin resulted in placebo-subtracted mean changes from baseline in glycated hemoglobin (the primary end-point), fasting plasma glucose and 2-h postmeal glucose of -0.9%, -22.5 mg/dL and -51.3 mg/dL, respectively (all, P < 0.001). During the double-blind period, adverse experiences were reported with similar frequency in both treatment groups, and the occurrences of hypoglycemia and gastrointestinal adverse experiences were low. In the open-label period, sustained improvements in glycemic parameters were observed with sitagliptin treatment, and sitagliptin was generally well tolerated. Conclusions: Sitagliptin added on to ongoing voglibose monotherapy provided significant improvements in glycemic parameters and was well tolerated in Japanese patients with type 2 diabetes mellitus who had inadequate glycemic control. This trial was registered with ClinicalTrails.gov (no. NCT00837577).
收起
摘要 :
Background: Coronavirus disease 2019 (COVID-19) is associated with a high risk of mortality especially among diabetes mellitus (DM) patients. Effective treatments against COVID-19 can complement the vaccination effort worldwide. M...
展开
Background: Coronavirus disease 2019 (COVID-19) is associated with a high risk of mortality especially among diabetes mellitus (DM) patients. Effective treatments against COVID-19 can complement the vaccination effort worldwide. Many review articles studied the effects of the dipeptidyl peptidase 4 (DPP-4) inhibitors among COVID-19 patients and found conflicting results. This heterogeneity may be due to different systemic pleiotropic effects of different DPP-4 inhibitors. Sitagliptin appears to be one of the good DPP-4 inhibitors that have antiinflammatory and antithrombotic effect. Therefore, this review assessed the benefits and safety of sitagliptin in the treatment of COVID-19. Methods: A detailed literature review using the electronic databases of Pubmed and Google Scholar was conducted during July and August 2021 to find out studies that published in English language and discussed the role of sitagliptin for COVID-19 patients. Results: 14 articles were eligible and thus included in this narrative review. Nine of these articles agreed to the benefit of sitagliptin in the treatment of COVID-19, while 3 studies considered sitagliptin as non useful or even risky, and one study was neutral in its conclusion towards the usage of sitagliptin in COVID-19. Only one study focused on the safety of sitagliptin and found that it is safe. Conclusion: Sitagliptin has anti-inflammatory, antiflbrotic and antiapoptotic properties; such effects may be beneficial in reducing risks of COVID-19. Sitagliptin has good safety and fair benefits to reduce mortality among DM patients with COVID-19. Further randomized clinical trials are needed to confirm these benefits especially among patients without DM.
收起
摘要 :
Background: Hypoglycemia is one of the most common side effect of insulin treatment, it affect liver and can potentiate ketoconazole toxicity. Objectives: To measure effect of ketoconazole on liver enzymes, hypoglycemic oxidative ...
展开
Background: Hypoglycemia is one of the most common side effect of insulin treatment, it affect liver and can potentiate ketoconazole toxicity. Objectives: To measure effect of ketoconazole on liver enzymes, hypoglycemic oxidative stress and to evaluate if N-acetylcysteine, can modulate this effect. Methods: Thirty five male rabbits were randomly divided into five groups: Group 1: (control group), Group 2:( ketoconazole), Group 3: (insulin), Group 4: ( ketoconazole+ insulin), Groups 5: (ketoconazole + insulin + N-Acetyl cysteine). Animals were sacrificed at day 3. Blood collected for measurement of liver enzymes, and total bilirubin. Malondialdehyde and glutathione were measured in serum and liver. Results: Ketoconazole increased serum and liver malondialdehyde, 0.594 ± 0.17 and 4614.49 ± 1288.00 nmol/gm. Increased aspartate aminotransferase 38.19 ± 17.29 and alkaline phosphatase 29.29 ± 10.2 U/L. Insulin increased serum malondialdehyde 0.522 ± 0.19, alkaline phosphatase 15.77 ± 6.12 U/L and bilirubin 0.56 ± 0.26 mg/dl. Ketoconazole + insulin, increased serum malondialdehyde 0.850 ± 0.16 μmol/l and bilirubin 0.77 ± 0.55 mg/dl. Ketoconazole + insulin increased serum malondialdehyde 0.850 ± 0.16 μmol/l, aspartate amino transferase 54.35 ± 18.34 U/L, alanine amino transferase, 34.74 ± 11.08 U/L, alkaline pohospahtase 30.81 ± 12.4 U/L and bilirubin 2.51 ± 1.55 mg/dl. N-acetylcysteine reduced aspartate aminotransferase 28.12 ± 22.21 U/L, alkaline phosphatase 11.81 ± 3.03 IU/L) and bilirubin 0.39 ± 0.18 mg/dl Conclusion: Hypoglycemia caused hepatotoxicity and oxidative stress and potentiates the toxicity of ketoconazole. N-acetylcysteine partly reverse this hepatotoxicity.
收起
摘要 :
The use of doxorubicin (DOX) as an antitumor therapeutic agent is limited due to its cardiotoxic effects. Metformin (Met) and sitagliptin (Sitg) are suggested to improve cardiac function. The present study aimed to determine the p...
展开
The use of doxorubicin (DOX) as an antitumor therapeutic agent is limited due to its cardiotoxic effects. Metformin (Met) and sitagliptin (Sitg) are suggested to improve cardiac function. The present study aimed to determine the potential protective effects of Met and Sitg on DOX-induced cardiotoxicity. Rats were divided into six groups: groups I, II, and III received normal saline, Met, and Sitg, respectively. Groups IV, V, and VI received DOX only, Met + DOX, and Sitg + DOX, respectively. Heart tissue was used for biochemical assays which measured cardiac reduced glutathione (GSH), thiobarbituric acid reactive substances (TBARS), and tumor necrosis factor (TNF-). Serum creatinine kinase (CK) and lactate dehydrogenase (LDH) were also measured. The heart apex was prepared for histological (hematoxylin and eosin) and immunohistochemical examination. Intoxication of DOX was associated with a significant elevation in serum CK-MB and LDH, reduction in cardiac GSH, and increased TBARS and TNF- compared to the controls. Administration of Met or Sitg to DOX-intoxicated rats suppressed serum CK-MB and LDH. Moreover, cardiac GSH was elevated with decreased TBARS and TNF-. These results were confirmed by histological study. Met and Sitg caused inhibition of caspase 3 and upregulation of B-cell lymphoma 2 (Bcl-2) expression in DOX-intoxicated animals. Sitg was found to exert a significantly better protective effect compared to that of Met. It was concluded that Sitg might be more effective than Met in reducing myocardial injury in DOX-induced cardiotoxicity in rats.
收起
摘要 :
Aims To assess the safety and efficacy of monotherapy with once‐weekly subcutaneous (s.c.) semaglutide vs sitagliptin in Japanese people with type 2 diabetes (T2D). Methods In this phase IIIa randomized, open‐label, parallel‐gr...
展开
Aims To assess the safety and efficacy of monotherapy with once‐weekly subcutaneous (s.c.) semaglutide vs sitagliptin in Japanese people with type 2 diabetes (T2D). Methods In this phase IIIa randomized, open‐label, parallel‐group, active‐controlled, multicentre trial, Japanese adults with T2D treated with diet and exercise only or oral antidiabetic drug monotherapy (washed out during the run‐in period) received once‐weekly s.c. semaglutide (0.5 or 1.0?mg) or once‐daily oral sitagliptin 100?mg. The primary endpoint was number of treatment‐emergent adverse events (TEAEs) after 30?weeks. Results Overall, 308 participants were randomized and exposed to treatment, with similar baseline characteristics across the groups. In total, 2.9% of participants in both the semaglutide 0.5?mg and the sitagliptin group prematurely discontinued treatment, compared with 14.7% in the semaglutide 1.0?mg group. The majority of discontinuations in the semaglutide 0.5 and 1.0?mg groups were attributable to adverse events (AEs). More TEAEs were reported in semaglutide‐ vs sitagliptin‐treated participants (74.8%, 71.6% and 66.0% in the semaglutide 0.5?mg, semaglutide 1.0?mg and sitagliptin groups, respectively). AEs were mainly mild to moderate. Gastrointestinal AEs, most frequently reported with semaglutide, diminished in frequency over time. The mean glycated haemoglobin (HbA1c [baseline 8.1%]) decreased by 1.9% and 2.2% with semaglutide 0.5 and 1.0?mg, respectively, vs 0.7% with sitagliptin (estimated treatment difference [ETD] vs sitagliptin ?1.13%, 95% confidence interval [CI] ?1.32; ?0.94, and ?1.44%, 95% CI ?1.63; ?1.24; both P ?<?.0001). Body weight (baseline 69.3?kg) was reduced by 2.2 and 3.9?kg with semaglutide 0.5 and 1.0?mg, respectively (ETD ?2.22?kg, 95% CI ?3.02; ?1.42 and ?3.88?kg, 95% CI ?4.70; ?3.07; both P ?<?.0001). Conclusions In Japanese people with T2D, more TEAEs were reported with semaglutide than with sitagliptin; however, the semaglutide safety profile was similar to that of other glucagon‐like peptide‐1 receptor agonists. Semaglutide significantly reduced HbA1c and body weight compared with sitagliptin.
收起
摘要 :
Previous randomized controlled trials (RCTs) have reported conflicting results for the efficacy of sitagliptin and sulfonylurea therapy in patients with type 2 diabetes mellitus showing inadequate glycemic control with metformin m...
展开
Previous randomized controlled trials (RCTs) have reported conflicting results for the efficacy of sitagliptin and sulfonylurea therapy in patients with type 2 diabetes mellitus showing inadequate glycemic control with metformin monotherapy. To clarify these findings, a meta-analysis was conducted of the outcomes of all published RCTs comparing sitagliptin with sulfonylureas in the treatment of type 2 diabetes mellitus. Standard medical databases were searched to identify relevant English- and Chinese-language RCTs. RCT results were compared regarding the mean change in glycated hemoglobin (HbA1c) level; the proportion achieving <7% HbAlc; and a change in body weight. No significant differences were found between the metformin plus sitagliptin and metformin plus sulfonylurea groups regarding HbAlc or the proportion achieving <7% HbAlc, while the metformin plus sitagliptin group experienced fewer hypoglycemic events (P<0.00001) and a greater reduction in body weight (P<0.00001). Metformin plus sitagliptin therapy may decrease HbAlc values in patients with type 2 diabetes mellitus who are not achieving their glycemic targets with metformin monotherapy in a manner similar to metformin plus sulfonylurea therapy, whilst posing a lower risk of hypoglycemia, and yielding a more beneficial effect on body weight.
收起
原文获取