Determination of sitagliptinin human plasma using protein precipitation and tandem mass spectrometry

Zeng, Wei; Xu, Yang; Constanzer, M.L.; Woolf, Eric

doi:10.1016/j.jchromb.2010.05.013

Cited by 69 publications

(44 citation statements)

References 16 publications

(24 reference statements)

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“…Several LC-MS/MS method have been reported for the estimation of sitagliptin in biological matrices, such as plasma, urine and hemodialysate. The majority of the reported methods are used in clinical applications (Zeng et al, , 2010Nirogi et al, 2008;Hess et al, 2011;Bonde et al, 2013;Burugula et al, 2013;Reddy et al, 2015;Scherf-Clavel and Högger, 2015) compared with preclinical applications (Yao et al, 2011;Gananadhamu et al, 2012;Patel et al, 2014). Shantikumar et al (2015) reported an LC-QTOF/MS method for the determination of five gliptins (vildagliptin, saxagliptins, sitagliptins, linagliptins and teneligliptin) in clinical application.…”

Section: Hplc Coupled With Ms/ms Detectionmentioning

confidence: 99%

A concise review of the bioanalytical methods for the quantitation of sitagliptin, an important dipeptidyl peptidase‐4 (DPP4) inhibitor, utilized for the characterization of the drug

Suresh

Srinivas²,

Mullangi

2016

Biomedical Chromatography

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Inhibition of dipeptidyl peptidase-4 (DPP4) is an emerging therapeutic approach for treating type 2 diabetes and has revolutionized the concept of diabetes management. Sitagliptin is the first approved orally active, potent, selective and nonpeptidomimetic DPP4 inhibitor. Incidence of hypoglycemia and weight gain is negligible with sitagliptin treatment. It is used as monotherapy or in combination with other anti-diabetic drugs to treat type 2 diabetes. There are numerous bioanalytical methods published for the analysis of sitagliptin in preclinical and clinical samples. This review focuses on the various HPLC and LC-MS/MS methods that have been used to analyze sitagliptin in various biological matrices. A small section is devoted to the bioanalysis of other DPP4 inhibitors such as vildagliptin, saxagliptin and linagliptin. This review provides key information in a concise manner regarding sample processing options, chromatographic/detection conditions and validation parameters of the chosen methods for sitagliptin and other DPP4 inhibitors.

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Section: Hplc Coupled With Ms/ms Detectionmentioning

confidence: 99%

A concise review of the bioanalytical methods for the quantitation of sitagliptin, an important dipeptidyl peptidase‐4 (DPP4) inhibitor, utilized for the characterization of the drug

Suresh

Srinivas²,

Mullangi

2016

Biomedical Chromatography

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“…Serial plasma concentrations of sitagliptin were measured using protein precipitation and tandem mass spectrometry as reported elsewhere [2]. The levels of sitagliptin in the plasma the day before, 16 h after, and 7 days after the overdose were 197, 3,793, and 686 nM, respectively.…”

Section: Sulfonylureasmentioning

confidence: 99%

“…However, we did not observe evident hypoglycemia in this patient despite monitoring her blood glucose concentration carefully every few hours. This may be because: (1) blood glucose prior to the overdose of sitagliptin was poorly controlled; (2) it was a single oral overdose of sitagliptin; or (3) she did not take any other medications except sitagliptin. Nevertheless, we were able to find markedly elevated plasma sitagliptin levels even 16 h after drug ingestion.…”

Section: Glinidesmentioning

confidence: 99%

Suicide attempt by an overdose of sitagliptin, an oral hypoglycemic agent: A case report and a review of the literature

et al. 2012

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DipeptiDyl peptiDase-4 (Dpp-4) inhibitors have recently been approved worldwide for the management of diabetes. Although insulin is a wellknown anti-diabetic agent that is occasionally used for attempting suicide, the effect of an oral overdose of anti-diabetic agents, such as sitagliptin, a DPP-4 inhibitor, remains unclear. The incidence of hypoglycemia across a range of sitagliptin doses (50, 100, and 200 mg) in a 12-week double-blind randomized controlled study in Japanese patients with type 2 diabetes mellitus was as low as 1.3-4.4% [1]. We present a case report of sitagliptin overdose in a suicide attempt. We also review the literature on overdose with oral antidiabetic agents, and highlight the best use of oral anti- abstract. Dipeptidyl peptidase-4 (DPP-4) inhibitors are a newer class of oral hypoglycemic agents for the management of diabetes that elevate the plasma concentration of active glucagon-like peptide-1 via inhibition of DPP-4. They effectively lower not only glycosylated hemoglobin levels, but also fasting and postprandial plasma glucose levels. Patients with diabetes occasionally consume an overdose of oral hypoglycemic agents in suicide attempts: the prevalence of depression is high in patients with diabetes, and depression is a strong risk factor for suicide. We encountered an 86-year-old woman with type 2 diabetes and depression, who was transferred to the emergency room 4h after ingestion of 1,700 mg of the DPP-4 inhibitor sitagliptin (1,700 mg is 17 times greater than the approved maximum dose). Upon arrival, she was fully conscious, plasma glucose was 124 mg/dL, and serum immunoreactive insulin level was 5.81 μU/mL. Thereafter, the plasma concentration of sitagliptin rose to 3,793 nM, which is 4.5 times higher than the value found under regular treatment with the maximum dose. The patient did not suffer from hypoglycemia, suggesting that a single oral overdose of sitagliptin is unlikely to cause hypoglycemia. A literature review of oral anti-diabetic agents revealed that overdose of biguanides is occasionally fatal when immediate intensive care is not provided. In summary, sitagliptin is a good treatment option for diabetic elderly patients or patients with psychiatric disorders who are suicidal and do not require insulin.Key words: Dipeptidyl peptidase-4 inhibitors, Hypoglycemia, Overdose, Sitagliptin diabetic agents in elderly people and in patients with psychiatric disorders. Case ReportAn 86-year-old woman with a 10-year history of type 2 diabetes mellitus was admitted to our hospital after sitagliptin overdose (1,700 mg: 34 tablets, 50 mg each) in a suicide attempt. She had been suffering from depression, and was prescribed sitagliptin 50 mg/day for 10 months; her HbA1c levels were stable at about 7.9% (National Glycohemoglobin Standardization Program). On admission, she was conscious and alert. Her blood pressure was 124/80 mm Hg and body temperature was 36.5°C. Blood glucose and immunoreactive insulin levels were 124 mg/dL and 5.81 μU/mL, respectively. Other laboratory data were a...

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“…Sgli was quantified in human plasma using protein precipitation and tandem mass spectrometry (LC-MS/MS) by Zeng et al [6] and using liquid-liquid extraction and MS/MS (LC-MS/MS) by Nirogi et al [7].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the interaction between sitagliptin and cyclodextrin derivatives by capillary electrophoresis and nuclear magnetic resonance spectroscopy

Sohajda¹,

Hu²,

Zeng³

et al. 2011

Electrophoresis

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An aqueous capillary electrophoretic method was developed for chiral analysis of the novel anti-diabetic drug, sitagliptin. The acid-base profiling of the analyte was carried out using both capillary electrophoresis and nuclear magnetic resonance pH titrations. The apparent complex stability and chiral separation properties were investigated with 30 different cyclodextrins under acidic conditions. The effect of concentration and pH of the BGE, temperature of the capillary, and the type and concentration of the chiral selector on the enantiomer resolution were thoroughly investigated. The effects of dual cyclodextrin systems on separation were also extensively studied. Complete separation of racemic sitagliptin with good resolution (R(S)=2.24) was achieved within a short time (15 min) with optimized parameters (10°C, pH=4.4, 40 mM phosphate buffer) of a sulfobutylether-β-cyclodextrin (averaged degree of substitution ~4) and native β-cyclodextrin dual system. The averaged stoichiometry of the inclusion complex was determined using the Job plot method with both (1)H and (19)F NMR experiments and resulted in a 1:1 complex. The structure of the inclusion complex was elucidated using 2-D ROESY NMR experiments.

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Determination of sitagliptinin human plasma using protein precipitation and tandem mass spectrometry

Cited by 69 publications

References 16 publications

A concise review of the bioanalytical methods for the quantitation of sitagliptin, an important dipeptidyl peptidase‐4 (DPP4) inhibitor, utilized for the characterization of the drug

A concise review of the bioanalytical methods for the quantitation of sitagliptin, an important dipeptidyl peptidase‐4 (DPP4) inhibitor, utilized for the characterization of the drug

Suicide attempt by an overdose of sitagliptin, an oral hypoglycemic agent: A case report and a review of the literature

Evaluation of the interaction between sitagliptin and cyclodextrin derivatives by capillary electrophoresis and nuclear magnetic resonance spectroscopy

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