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1

Shubrook, Jay, Randall Colucci, Aili Guo, and Frank Schwartz. "Saxagliptin: A Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes Mellitus." Clinical Medicine Insights: Endocrinology and Diabetes 4 (January 2011): CMED.S5114. http://dx.doi.org/10.4137/cmed.s5114.

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The prevalence of type 2 diabetes mellitus is high and growing rapidly. Suboptimal glycemic control provides opportunities for new treatment options to improve the morbidity and mortality of this progressive disease. Saxagliptin, a selective DPP-4 inhibitor, increases endogenous incretin levels and incretin acitivty. In controlled clinical trials saxagliptin reduces both fasting and postprandial glucose and works in monotherapy and in combination with metformin, TZDs and sulfonylureas. Saxagliptin has a very favourable side effect profile and may have other beneficial non-glycemic effects. The
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2

Ayoub, Bassam M., Ramzia I. El-Bagary, and Ehab F. Elkady. "Spectrophotometric Methods Based on Charge Transfer ComplexationReactions for the Determination of Saxagliptin in Bulk and Pharmaceutical Preparation." International Journal of Biomedical Science 8, no. 3 (2012): 204–8. http://dx.doi.org/10.59566/ijbs.2012.8204.

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Simple, accurate and precise spectrophotometric methods have been developed for the determination of saxagliptin in bulk and dosage forms.The proposed methods are based on the charge transfer complexes of saxagliptin with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and7,7,8,8-tetracyanoquinodimethane (TCNQ). All the variables were studied to optimize the reactions' conditions. Beer's law was obeyed in the concentration ranges of 50-300 μg/ml and 10- 110 μg/ml with DDQ and TCNQ, respectively.The developed methods werevalidated and proved to be precise and accurate for the quality control of
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3

Kim, Ki-Young, Yeo-Jin Jeong, So-Young Park, et al. "Evaluation of the Drug-Induced Liver Injury Potential of Saxagliptin through Reactive Metabolite Identification in Rats." Pharmaceutics 16, no. 1 (2024): 106. http://dx.doi.org/10.3390/pharmaceutics16010106.

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A liver injury was recently reported for saxagliptin, which is a dipeptidyl peptidase-4 (DPP-4) inhibitor. However, the underlying mechanisms of saxagliptin-induced liver injury remain unknown. This study aimed to evaluate whether saxagliptin, a potent and selective DPP-4 inhibitor that is globally used for treating type 2 diabetes mellitus, binds to the nucleophiles in vitro. Four DPP-4 inhibitors, including vildagliptin, were evaluated for comparison. Only saxagliptin and vildagliptin, which both contain a cyanopyrrolidine group, quickly reacted with L-cysteine to enzyme-independently produc
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Wu, Suyan, Haifei Pan, and Yingying Huang. "Pharmacokinetic interaction of saxagliptin with andrographolide and their hypoglycemic effect in type 2 diabetes rats." Acta Poloniae Pharmaceutica - Drug Research 80, no. 4 (2023): 667–73. http://dx.doi.org/10.32383/appdr/170911.

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Controlling blood glucose is the primary therapeutic strategy for T2DM. Both saxagliptin and andrographolide possess hypoglycemic effects, which makes the combination easy. This study aimed to evaluate the co-administration of saxagliptin and andrographolide in rats and revealed their combined impact on type 2 diabetes (T2DM). T2DM rat models were established by high-fat diet and the injection of nicotinamide and streptozotocin. The blood glucose and insulin resistance index were monitored after modeling. The pharmacokinetics of saxagliptin was assessed by orally administrating 10 mg/kg saxagl
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5

Dhillon, Sohita, and Juliane Weber. "Saxagliptin." Drugs 69, no. 15 (2009): 2103–14. http://dx.doi.org/10.2165/11201170-000000000-00000.

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6

Yang, Lily P. H. "Saxagliptin." Drugs 72, no. 2 (2012): 229–48. http://dx.doi.org/10.2165/11208160-000000000-00000.

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7

Lam, Sum, and Maha Saad. "Saxagliptin." Cardiology in Review 18, no. 4 (2010): 213–17. http://dx.doi.org/10.1097/crd.0b013e3181daad5f.

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8

Cole, P., N. Serradell, J. Bolos, and R. Castañer. "Saxagliptin." Drugs of the Future 33, no. 7 (2008): 577. http://dx.doi.org/10.1358/dof.2008.033.07.1229229.

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9

Gurav, Sachin B., and Neela M. Bhatia. "Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC." Current Pharmaceutical Analysis 16, no. 8 (2020): 1074–82. http://dx.doi.org/10.2174/1573412915666190617153004.

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Introduction: Saxagliptin hydrochloride is an oral hypoglycemic agent used for the treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it is important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it is essential to identify the formation of cyclicamidine and other related substances. Materials and Methods: In the curren
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10

Dayyih, Wael Abu, Lina Tamimi, Eyad Mallah, Kenza Mansour, Tawfiq Arafat, and Mona Bustami. "SAXAGLIPTIN LEVELS AND ITS PHARMACOKINETIC APPLICATION IN PRESENCE OF SUCRALOSE IN ANIMALS SERUM BY HPLC METHOD: A RESEARCH ARTICLE." International Journal of Pharmacy and Pharmaceutical Sciences 10, no. 2 (2018): 178. http://dx.doi.org/10.22159/ijpps.2015v7i9.6109.

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Objective: It is to develop a simple, valid and rapid chromatographic method for quantification of saxagliptin in rats serum in order to study saxagliptin pharmacokinetic parameters in sucralose fed rats simultaneously to detect any interaction possibility between saxagliptin and sucralose in rats. Methods: In our developed method of analysis, mobile phase consisted of phosphate buffer (pH =4) and methanol (70:30) v/v at flow rate of 1 ml/min with UV detection at 230 nm., C8 column of separation was used with temperature of 40 C ° using injection volume of 50 µl, samples run time was 10 min, a
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11

Santhosh, Illendula* Mallepally Sandeep Kumar Dr. K.N.V.Rao Dr. Rajeswar Dutt. "STABILITY INDICATING METHOD DEVELOPMENT AND VALIDATION AND SIMULTANIOUS ESTIMATION OF DAPAGLIFLOZIN AND SAXAGLIPTIN IN PHARMACEUTICAL DOSAGE FORM." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES o6, no. 07 (2019): 13791–808. https://doi.org/10.5281/zenodo.3270622.

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<em>A straightforward, precise, exact technique was developed for the evaluation of the Dapagliflozin&amp;Saxagliptinin tablet dosage form. Chromatogram was run through Altima 150 x 4.6 mm, 5</em><em>m</em><em>. Mobile phasecarryingBuffer0.1%OPA:ACN in use in the %50:50was injecting into column at a flow rate of 1ml/min and 220nm. Runtime of Dapagliflozin&amp;Saxagliptin was initiate to 2.691min and 2.143min. %RSD of the drugs were and get to be 0.8and 0.5 in the same way. %Recovery was get as 100.42% and 100.15%. LOD, LOQ values get from regression sum of Dapagliflozin&amp;Saxagliptin were 0.
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12

Dr., Vivek Panchabhai* Komal Chavan Moein Attar Dr. R. S. Sakhare. "Simultaneous Estimation of Dapagliflozin and Saxagliptin: Analytical Method Development and Validation." International Journal of Pharmaceutical Sciences 2, no. 7 (2024): 2435–45. https://doi.org/10.5281/zenodo.13171545.

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We present a robust and sensitive RP-HPLC method for the simultaneous quantification of Dapagliflozin and Saxagliptin in pharmaceutical dosage forms. The method adheres to ICH guidelines, ensuring accuracy, precision, and reliability. Luna C18 (150 mm &times; 4.6 mm, 5 &micro;m) serves as the stationary phase, with a mobile phase composed of Phosphate Buffer pH 3.0: Acetonitrile (45:55 v/v) delivered isocratically at a flow rate of 1.0 mL/min and detected at 228 nm UV wavelength. Results include LOD (Dapagliflozin: 0.171 &micro;g/mL, Saxagliptin: 0.267 &micro;g/mL) and LOQ (Dapagliflozin: 0.51
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13

Coppenrath, Valerie Azzopardi, and Tasmina Hydery. "Dapagliflozin/Saxagliptin Fixed-Dose Tablets: A New Sodium-Glucose Cotransporter 2 and Dipeptidyl Peptidase 4 Combination for the Treatment of Type 2 Diabetes." Annals of Pharmacotherapy 52, no. 1 (2017): 78–85. http://dx.doi.org/10.1177/1060028017731111.

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Objective: To review the pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of the fixed-dose combination (FDC) product, QTERN (dapagliflozin/saxagliptin) tablets. Data Sources: Searches of MEDLINE (1946 to July 1, 2017) were conducted using the keywords QTERN, saxagliptin, and dapagliflozin. Additional data were obtained from the prescribing information, the product dossier, and Clinicaltrials.gov . Study Selection and Data Extraction: All English language articles related to pharmacology, pharmacokinetics, efficacy, or safety of the combination therapy in human subjects w
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14

Li, Fang, Jiachao Chen, Fei Leng, Zhiqiang Lu, and Yan Ling. "Effect of Saxagliptin on Circulating Endothelial Progenitor Cells and Endothelial Function in Newly Diagnosed Type 2 Diabetic Patients." Experimental and Clinical Endocrinology & Diabetes 125, no. 06 (2017): 400–407. http://dx.doi.org/10.1055/s-0042-124421.

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Abstract Endothelial dysfunction is associated with the risk of cardiovascular complications in diabetic patients. Endothelial progenitor cells (EPCs) and flow-mediated dilation (FMD) are common markers of endothelial function. In this study, we aim to investigate whether the DPP-4 inhibitor saxagliptin modulate EPCs number and FMD in newly diagnosed, treatment-naive type 2 diabetic patients. This was a controlled, randomized, open-label clinical trial. Saxagliptin group and metformin group consumed either saxagliptin 5 mg per day or metformin 1 500 mg per day respectively for 12 weeks. Change
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15

Valiquette, G. "Saxagliptin efficacy." Diabetes, Obesity and Metabolism 12, no. 8 (2010): 734. http://dx.doi.org/10.1111/j.1463-1326.2010.01205.x.

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16

Lee, Chen-Hung, Shu-Chun Huang, Kuo-Chun Hung, Chia-Jung Cho, and Shih-Jung Liu. "Enhanced Diabetic Wound Healing Using Electrospun Biocompatible PLGA-Based Saxagliptin Fibrous Membranes." Nanomaterials 12, no. 21 (2022): 3740. http://dx.doi.org/10.3390/nano12213740.

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Delayed diabetic wound healing is an adverse event that frequently leads to limb disability or loss. A novel and promising vehicle for the treatment of diabetic wounds is required for clinical purposes. The biocompatible and resorbable poly (lactic-co-glycolic acid) (PLGA)-based fibrous membranes prepared by electrospinning that provide a sustained discharge of saxagliptin for diabetic wound healing were fabricated. The concentration of released saxagliptin in Dulbecco's phosphate-buffered saline was analyzed for 30 days using high-performance liquid chromatography. The effectiveness of the el
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17

THAKUR, PURSHOTTAM KUMAR, C. K. TYAGI, and NEELESH CHOUBEY. "FORMULATION AND EVALUATION OF GASTRO-RETENTIVE MICROSPHERE OF SAXAGLIPTIN ANTIDIABETIC AGENT." Current Research in Pharmaceutical Sciences 13, no. 3 (2023): 126–32. http://dx.doi.org/10.24092/crps.2023.130302.

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The objective of this study was to develop a gastro-retentive microsphere of Saxagliptin. Saxagliptin is an orally active hypoglycemic drug of the newdipeptidylpeptidase-4(DPP4) inhibitor class of drug. Nine formulations of Saxagliptin microsphere are prepared by Emulsion solvent diffusion method using polymers like Eudragit RS 100 and Ethyl cellulose at different drug to polymer ratios and Polyvinyl Alcohol as Stabilizing agent by Emulsion Solvent Diffusion Method. The formulations were optimized on the basis of percent buoyancy and in vitro drug release. The prepared microspheres were evalua
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18

Cristiani, Marco, Anna Citarella, Andrea Belisari, Guido Didoni, Lorenzo Giovanni Mantovani, and Sabato Montella. "Economic evaluation of the use of saxagliptin in the treatment of type 2 diabetes in Italy." Farmeconomia. Health economics and therapeutic pathways 11, no. 2 (2010): 103–15. http://dx.doi.org/10.7175/fe.v11i2.182.

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In this study we compare the cost-effectiveness of saxagliptin (Onglyza®) in combination with metformin to that of either sulphonylurea (SU) plus metformin or a thiazolidinedione (TZD) plus metformin, in type 2 diabetes mellitus patients who are not well-controlled on metformin alone. By using decision-analytic modeling, long-term costs and health outcomes associated with the investigated treatment strategies are estimated. This is achieved by modeling the risk of experiencing diabetes-related events (e.g. myocardial infarction) or side-effects such as hypoglycemia and weight gain. The risk of
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19

Suma A.H., Binoy Varghese Cheriyan, Vijey Aanandhi M., and Ramachandran S. "Method Development and Validation of RP-HPLC method for Saxagliptin and Sitagliptin in Pharmaceutical Dosage Form - A Review." International Journal of Research in Pharmaceutical Sciences 12, no. 2 (2021): 1338–44. http://dx.doi.org/10.26452/ijrps.v12i2.4687.

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The study's goal was to develop a plain, quick, and responsive RP-HPLC method for determining the concentrations of Saxagliptin and Sitagliptin in pharmaceutical bulk dosage form (bulk powders). Isocratic elution with Cosmosil C18 (250nm 4.6nm, 5m particle size) and UV detection at 212nm for Saxagliptin and Develosil ODS HG-5 RP-C18 (15cm 4.6mm, 5m particle size) and UV detection at 255nm for Sitagliptin were used in this chromatographic process. Methanol and water (70:30) in a mobile solution with a flow rate of 0.8ml/min for Saxagliptin and (0.05m) phosphate buffer: methanol and water (70:30
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20

Kurian, Aksa, Rekha T. N, Bhagyalakshmi C, et al. "SIMPLE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR SIMULTANEOUS QUANTIFICATION OF SAXAGLIPTIN AND DAPAGLIFLOZIN IN RAT PLASMA." Indian Drugs 59, no. 07 (2022): 52–59. http://dx.doi.org/10.53879/id.59.07.12537.

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A simple HPLC method was developed for the simultaneous estimation of saxagliptin and dapagliflozin in rat plasma. The separation has been achieved by C8 Eclipse plus column (25cm x 5cm x 4.6µ) at 1 mL min-1 flow rate. The mobile phase comprises of 0.01 % trimethylamine in water and methanol (40:60 V/V). The effluents were monitored at 228 nm. The retention times were found to be 4.243 min and 11.304 min for saxagliptin and dapagliflozin, respectively. The quantification ranges were found to be linear over 25-175 ng mL-1 and 100-700 ng mL-1 for saxagliptin and dapagliflozin, respectively. Regr
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21

Forst, Thomas, Mohammed Alghdban, Annelie Fischer, et al. "Sequential Treatment Escalation with Dapagliflozin and Saxagliptin Improves Beta Cell Function in Type 2 Diabetic Patients on Previous Metformin Treatment: An Exploratory Mechanistic Study." Hormone and Metabolic Research 50, no. 05 (2018): 403–7. http://dx.doi.org/10.1055/a-0591-9442.

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AbstractWe investigated the effect of sequential treatment escalation with dapagliflozin and saxagliptin on beta cell function in patients with T2DM insufficiently controlled on metformin monotherapy during a hyperglycaemic clamp investigation. Twenty-six patients (19 males, age 63.5±7.0 years; duration of diabetes 8.8±4.7 years; HbA1c 63.9±15.8 mmol/mol; mean±SD) were enrolled in the study. During a first treatment period (TP1) all patients received 10 mg dapagliflozin for one month, followed by the addition of 5 mg saxagliptin or placebo for another month (TP2). At baseline and at the end of
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Oche, Jephtah, Olufunke Olorundare, Saheed Afolabi, Mary Ologe, Anoka Njan, and Olatunde Akanbi. "Comparative Therapeutic Effect of Single/Combined Administration of Saxagliptin, Metformin and Intranasal Insulin on Dexamethasone Induced Insulin Resistance in Albino Wistar Rat Model." Nigerian Journal of Physiological Sciences 38, no. 1 (2023): 37–46. http://dx.doi.org/10.54548/njps.v38i1.7.

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Glucocorticoids have therapeutic benefits in the management of several inflammatory and immunological disorders. Despite these medicinal effects, they have the drawback of causing metabolic disorders such as hyperglycemia, insulin resistance etc., which is known to be a key indicator of metabolic syndrome. Metabolic syndrome is a major predisposing factor to type 2 diabetes mellitus and cardiomyopathy. This study was designed to compare and evaluate the effects of saxagliptin, metformin and intranasal insulin (when used singly or in combination) on dexamethasone induced insulin resistance. Fif
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Kaushal, Amit, Sandeep Arora, Neelam Sharma, and Sukhbir Singh. "Development of Bilayer Tablet Containing Saxagliptin Immediate Release and Metformin Sustained Release Using Quality by Design Approach." Current Drug Therapy 16, no. 2 (2021): 184–203. http://dx.doi.org/10.2174/1574885516666210315100848.

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Objective: Adequate glycemic control in diabetes patients requires oral combination therapy. Saxagliptin is a dipeptidyl peptidase-4 inhibitor having fewer adverse effects, and metformin is the first-line medicine for diabetes treatment. The aim of this research work is to develop a bilayer tablet of saxagliptin and metformin in fixed-dose combination (FDC) using quality by design (QbD) to acquire the immediate release of saxagliptin and sustained release of metformin from bilayer tablet to ultimately achieve superior patient compliance. Methods: The development of the bilayer tablet was done
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Pech, Vladimir, Khalid Abusaada, and Carlos Alemany. "Dipeptidyl Peptidase-4 Inhibition May Stimulate Progression of Carcinoid Tumor." Case Reports in Endocrinology 2015 (2015): 1–3. http://dx.doi.org/10.1155/2015/952019.

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Dipeptidyl peptidase-4 (DPP-4) inhibitors, such as saxagliptin, have gained a rapid growth in use in the treatment of type 2 diabetes mellitus in the past decade. Although they are considered to have a good safety profile, controversy exists regarding their potential to stimulate neoplasm growth. We report here a patient with metastatic carcinoid tumor. His disease was stable for several years with plasma serotonin level (which was used to monitor disease progression) in 700–800 ng/mL range. After initiation of treatment with saxagliptin, however, his serotonin level almost doubled (1358 ng/mL
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25

Shestakova, M. V., and O. Iu Sukhareva. "Extension of the group of incretin-targeted preparations: Saxagliptin – a new dipeptidyl peptidase-4 inhibitor." Problems of Endocrinology 56, no. 5 (2010): 52–60. http://dx.doi.org/10.14341/probl201056552-60.

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A new selective incretin-targeted dipeptidyl peptidase-4 inhibitor was registered in the Russian Federation in August 2010. The enzyme dipeptidyl peptidase-4 inactivates glucagon-like peptide-1 (GLP-1). A rise of GLP-1 concentration in blood plasma is known to result in the glucose-dependent stimulation of insulin secretion by pancreatic beta-cells and suppression of glucagon release. Saxagliptin is readily absorbed in the gastrointestinal tract and remains active within 24 hours after oral intake. It allows the drug to be taken once during 24 hours. Clinical studies have demonstrated that sax
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26

Thadanki*, Madhuri Latha. "Formulation and evaluation of sustained release saxagliptin microspheres by ionotropic gelation method." International Journal of Bioassays 6, no. 03 (2017): 5328. http://dx.doi.org/10.21746/ijbio.2017.03.0010.

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The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of an antidiabetic agent, saxagliptin. Saxagliptin microspheres were formulated using sodium alginate as the controlled release polymer by ionotropic gelation technique. The polymer sodium alginate alone and along with different coating polymers like pectin, ethyl cellulose was used in different ratios (1:1,1:1.5, 1:2 ) to formulate batches F1 to F9. The resulting microspheres were evaluated for particle size, densitie
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Njerve, Ida Unhammer, Sissel Åkra, Thomas W. Weiss, et al. "A Double-Blinded Randomized Study Investigating a Possible Anti-Inflammatory Effect of Saxagliptin versus Placebo as Add-On Therapy in Patients with Both Type 2 Diabetes And Stable Coronary Artery Disease." Mediators of Inflammation 2017 (2017): 1–9. http://dx.doi.org/10.1155/2017/5380638.

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Background. Promising results regarding potential anti-inflammatory and antiatherosclerotic effects of gliptins have been reported. Our aim was to investigate whether saxagliptin treatment modifies expression of inflammatory markers, primarily in peripheral blood mononuclear cells (PBMCs) and in circulating leukocytes in patients with stable coronary artery disease (CAD) and T2DM. Methods. Patients (n=12) were randomized to saxagliptin 5 mg daily or placebo for 3 months. Samples were taken at baseline and end of study in fasting state prior to intake of medications. PBMCs were isolated and cry
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Bekele, Mengistu, Ole Frithjof Norheim, and Alemayehu Hailu. "Cost-Effectiveness of Saxagliptin Compared With Glibenclamide as a Second-Line Therapy Added to Metformin for Type 2 Diabetes Mellitus in Ethiopia." MDM Policy & Practice 6, no. 1 (2021): 238146832110057. http://dx.doi.org/10.1177/23814683211005771.

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Background. Metformin is a widely accepted first-line pharmacotherapy for patients with type 2 diabetes mellitus (T2DM). Treatment of T2DM with glibenclamide, saxagliptin, or one of the other second-line treatment agents is recommended when the first-line treatment (metformin) cannot control the disease. However, there is little evidence on the additional cost and cost-effectiveness of adding second-line drugs. Therefore, this study aimed to estimate the cost-effectiveness of saxagliptin and glibenclamide as second-line therapies added to metformin compared with metformin only in T2DM in Ethio
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Asti, Antonio, Alessandra D'Alessandro, Francesco Paolo Zito, et al. "Sitagliptin versus saxagliptin in decompensated type 2 diabetes mellitus patients." Italian Journal of Medicine 10, no. 1 (2016): 36. http://dx.doi.org/10.4081/itjm.2016.558.

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Sitagliptin and saxagliptin are oral hypoglycemic agents inhibitors of DPP-4, indicated in the treatment of type 2 diabetes mellitus in combination with metformin, in patients who have not achieved adequate glycemic control. In our study we enrolled 128 decompensated type 2 diabetes patients while on metformin maximum dosage. At time 0’ we have detected, body mass index (BMI), total cholesterol, high- and low-density lipoproteins (HDL and LDL), triglycerides, transaminases and pancreatic amylase; patients were randomized to receive sitagliptin or saxagliptin; follow-up was performed after 4 mo
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Bogdanov, Patricia, Hugo Ramos, Marta Valeri, et al. "Minimum Effective Dose of DPP-4 Inhibitors for Treating Early Stages of Diabetic Retinopathy in an Experimental Model." Biomedicines 10, no. 2 (2022): 465. http://dx.doi.org/10.3390/biomedicines10020465.

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The neurovascular unit (NVU) plays an essential role in the development of diabetic retinopathy (DR). We previously reported that the topical administration (eye drops) of sitagliptin and saxagliptin, two dipeptidyl peptidase-4 inhibitors (DPP-4i), prevents retinal neurodegeneration and vascular leakage in db/db mice. The aim of the present study is to evaluate the minimum effective dose of the topical administration of these DPP-4i. For this purpose, sitagliptin and saxagliptin were tested at different concentrations (sitagliptin: 1 mg/mL, 5 and 10 mg/mL, twice per day; saxagliptin: 1 and 10
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Minze, Molly G., Mary S. Klein, and Brian T. Terrell. "Saxagliptin and Metformin in Fixed Combination for the Treatment of Type 2 Diabetes in Adults." Clinical Medicine Insights: Endocrinology and Diabetes 6 (January 2013): CMED.S8510. http://dx.doi.org/10.4137/cmed.s8510.

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Type 2 diabetes affects millions of people worldwide and significantly contributes to morbidity and mortality of those affected by it. Current guidelines recommend individualized treatment regimens following first line metformin therapy. Saxagliptin, a dipeptidyl-peptidase 4 inhibitor, provides a secondary mechanism of action to decrease hyperglycemia when used in combination with metformin. The combination of metformin and saxagliptin has shown improvements in hemoglobin A1c and fasting plasma glucose in greater efficacy than when either agent is used alone. Adverse effects of combination the
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Singh, Dharmvir, Neetesh Kumar Jain, Apoorva Tiwari, and Neelam Khan. "Development and Validation of Simultaneous Equation Method for Estimation of Sitagliptin and Saxagliptin in Combined Pharmaceutical Dosage Form by Using UV Spectrophotometric Method." International Journal of Medical Sciences and Pharma Research 8, no. 2 (2022): 83–90. https://doi.org/10.22270/ijmspr.v8i2.43.

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Day by day the number of drug groups also the numbers of drugs within these groups for treatment of diabetes are increasing rapidly. The numbers of newer anti-diabetic formulations either in single or in combined dosage forms are marketed and investigated, sitagliptin with saxagliptin are not official in any pharmacopoeia. the aim of the present work was to develop and validate newer analytical methods like UV spectrophotometric methods, which should be applied for the further analysis of anti-diabetic drugs in bulk drugs and its pharmaceutical formulations. To develop and validate simultaneou
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33

Gallwitz, Baptist. "Drug Profile—Saxagliptin, a Novel Dipeptidyl Peptidase-4 Inhibitor for the Treatment of Type 2 Diabetes." US Endocrinology 05, no. 01 (2009): 70. http://dx.doi.org/10.17925/use.2009.05.1.70.

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Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor for the treatment of type 2 diabetes. It is a novel DPP-4 inhibitor with a high selectivity for DPP-4 compared with other dipeptidyl peptidases and a duration profile designed for once-daily application. DPP-4 inhibitors enhance endogenous concentrations of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide. This action leads to a glucose-dependent stimulation of insulin and inhibition of glucagon secretion post-prandially. DPP-4 inhibitors have no intrinsic risk of hypoglycemia and are weightneutra
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Gallwitz, Baptist. "Drug Profile—Saxagliptin, a Novel Dipeptidyl Peptidase-4 Inhibitor for the Treatment of Type 2 Diabetes." European Endocrinology 06 (2010): 70. http://dx.doi.org/10.17925/ee.2010.06.00.70.

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Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor for the treatment of type 2 diabetes. It is a novel DPP-4 inhibitor with a high selectivity for DPP-4 compared with other dipeptidyl peptidases and a duration profile designed for once-daily application. DPP-4 inhibitors enhance endogenous concentrations of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide. This action leads to a glucose-dependent stimulation of insulin and inhibition of glucagon secretion post-prandially. DPP-4 inhibitors have no intrinsic risk of hypoglycemia and are weightneutra
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Dr., A. Madhukar Shradha Rajesh Mahajan Vaishnavi Rameshrao Siral Ravindranath Bhagwan Rathod Bhagwan Shesharao Ingole. "METHOD DEVELOPMENT AND VALIDATION OF SAXAGLIPTIN BY USING UV SPECTROPHOTOMETRIC AND RP-HPLC TECHNIQUES IN BULK AND TABLET DOSAGE FORM." Journal of Pharma Research 12, no. 02 (2023): 15–24. https://doi.org/10.5281/zenodo.8094571.

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<strong><em>ABSTRACT</em></strong> <strong>S</strong>imple, precise, economical, fast and reliable UV and RP- HPLC Techniques have been developed for the estimation of Saxagliptin in bulk and pharmaceutical dosage form. UV method is based on measurement of absorption at maximum wavelength of 281 nm for Saxagliptin. Linearity for detector response was observed in the concentration range of 1 - 18&mu;g/ml. The accuracy of the methods was assessed by recovery studies and was found to be 98.26 to 101.143 %. Separation was achieved with an Inertsil ‐ Extend ‐ C18 (250 &times; 4.6 mm, 5 &micro;m) HP
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Zhou, Xiao-jun, Lin Ding, Jia-xin Liu, Le-qun Su, Jian-jun Dong, and Lin Liao. "Efficacy and short-term side effects of sitagliptin, vildagliptin and saxagliptin in Chinese diabetes: a randomized clinical trial." Endocrine Connections 8, no. 4 (2019): 318–25. http://dx.doi.org/10.1530/ec-18-0523.

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Aims To investigate the difference in the efficacy among dipeptidyl peptidase-4 (DPP-4) inhibitors in Chinese adults with newly diagnosed diabetes. Materials and methods In a multicenter, randomized study, we enrolled adults who were either treatment naive or off prior anti-hyperglycemic therapy for at least 3 months. Eligible patients had hemoglobin A1c (HbA1c) concentrations of 6.5–9.5%. Three hundred patients had been randomly allocated to sitagliptin 100 mg, once daily; vildagliptin 50 mg, twice daily and saxagliptin 5 mg, once daily for 12 weeks. Patients and investigators were masked to
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Othman, Ahmed Mohamed, Ibrahim Ashour Ibrahim, Samy M. Saleh, Dina M. Abo-Elmatty, Noha M. Mesbah, and Asmaa R. Abdel-Hamed. "The Safety and Efficacy of Combining Saxagliptin and Pioglitazone Therapy in Streptozocin-Induced Diabetic Rats." Biomedicines 11, no. 12 (2023): 3300. http://dx.doi.org/10.3390/biomedicines11123300.

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Background: Type 2 diabetes mellitus (T2DM) is a chronic progressive disease due to insulin resistance. Oxidative stress complicates the etiology of T2DM. Saxagliptin is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor, while Pioglitazone is a thiazolidinedione insulin sensitizer. This study aimed to assess the effect of Saxagliptin and Pioglitazone monotherapy and combination therapy on the biochemical and biological parameters in streptozotocin (STZ)-induced diabetic rats. Methods: The study included thirty-five male albino rats. Diabetes mellitus was induced by intraperitoneal STZ injec
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S. Bansode, Amol, Shubhangee S. Gaikwad, and Vishal D. Shelke. "REVERSE PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY (RP-HPLC) METHOD DEVELOPMENT AND VALIDATION OF SAXAGLIPTIN FROM HUMAN URINE." Indian Drugs 59, no. 12 (2022): 50–54. http://dx.doi.org/10.53879/id.59.12.12828.

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Reversed phase high performance liquid chromatography (RP-HPLC) method for the quantitative determination of saxagliptin (SXG) in human urine was developed and validated to support clinical studies. Chromatographic separation was achieved on an Inertsil® column (250 mm x 4.6 mm, 5 µm). Isocratic elution using a mobile phase of potassium dihydrogen phosphate buffer pH (3) - acetonitrile (80:20, V/V) at a flow rate of 1 mL min-1 with UV detection at 212.1 nm was performed. The retention time of saxagliptin was 6.4 min. The method was validated according to United State Food and Drug Administrati
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Evans, Marc. "Review: Saxagliptin: a review." British Journal of Diabetes & Vascular Disease 10, no. 1 (2010): 14–20. http://dx.doi.org/10.1177/1474651409347118.

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ASFUROGLU KALKAN, Emra, Berna İmge AYDOĞAN, İrem DINÇER, and Sevim GÜLLÜ. "Effects of DPP-4 inhibitors on brain natriuretic peptide, neuropeptide Y, glucagon like peptide-1, substance P levels and global longitudinal strain measurements in type 2 diabetes mellitus patients." Journal of Health Sciences and Medicine 5, no. 5 (2022): 1424–30. http://dx.doi.org/10.32322/jhsm.1133314.

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Introduction: Previously, a significant relationship between saxagliptin treatment and increased rate of hospitalization for congestive heart failure was reported. We aimed to investigate effects of vildagliptin and saxagliptin on brain natriuretic peptide (BNP), neuropeptide Y (NPY), substance P (SP), glucagon like peptide-1 (GLP-1) levels and left ventricular global longitudinal strain (GLS), assessed by 3-dimensional speckle tracking echocardiography in uncontrolled type 2 Diabetes mellitus (T2DM).&#x0D; Material and method: Thirty seven uncontrolled T2DM (HbA1c&gt;7,5%) patients who were r
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Feryal Hashim Rada. "Clinical assessment of saxagliptin therapy in diabetic patients with corpulence." GSC Biological and Pharmaceutical Sciences 21, no. 1 (2022): 109–15. http://dx.doi.org/10.30574/gscbps.2022.21.1.0389.

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Saxagliptin is an oral hypoglycemic agent act by inhibiting dipeptidyl peptidase 4 and prescribed for the management of diabetes alone or with other anti-diabetic drug. The idea of the research is to clarify the impact of saxagliptin treatment on adipokines of corpulence in diabetic patients. Of seventy-three diabetic patients with corpulence (43 males and 30 females), aging (45± 7) years of either sex were appointed to take Saxagliptin (5 mg/day) for 5 months periods. Data were pooled on fasting state prior treatment and after five months treatment. The variables involved body mass index, HOM
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Scheeren, Laís Engroff, Ana Isa Pedroso Marcolino, Andréa Inês Horn Adams, and Clarice Madalena Bueno Rolim. "Stability indicating RP-LC-PDA method for the quantitative analysis of saxagliptin in pharmaceutical dosage form." Brazilian Journal of Pharmaceutical Sciences 51, no. 2 (2015): 461–66. http://dx.doi.org/10.1590/s1984-82502015000200023.

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&lt;p&gt;Saxagliptin is a potent and selective inhibitor of the enzyme dipeptidyl peptidase 4. It is effective in the treatment of type 2 diabetes mellitus because it stimulates the pancreas to produce insulin. In the present study, a liquid chromatography method was developed and validated to quantify the drug in tablets. This method was based on the isocratic elution of saxagliptin, using a mobile phase consisting of 0.1% phosphoric acid at pH 3.0 - methanol (70: 30, v/v) at a flow rate of 1 mL.min&lt;sup&gt;-1&lt;/sup&gt; with UV detection at 225 nm. The chromatographic separation was achie
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Alshamrani, Ali A., Mohammed A. Al-Hamamah, Norah A. Albekairi, et al. "Impacts of the DPP-4 Inhibitor Saxagliptin and SGLT-2 Inhibitor Dapagliflozin on the Gonads of Diabetic Mice." Biomedicines 11, no. 10 (2023): 2674. http://dx.doi.org/10.3390/biomedicines11102674.

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Diabetes mellitus is a metabolic disease that can cause systemic problems, including testicular dysfunction. Several diabetes medications have demonstrated potential adverse effects on the male reproductive system; however, the effects of saxagliptin and dapagliflozin have not been sufficiently examined. This investigation studied the impacts of saxagliptin and dapagliflozin treatments on the gonads in a male mouse model of diabetes. Testicular disturbances were assessed by sperm DNA damage, diakinesis-metaphase I chromosome examination, and spermiogram analysis. Our results showed more sperm
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Feryal, Hashim Rada. "Clinical assessment of saxagliptin therapy in diabetic patients with corpulence." GSC Biological and Pharmaceutical Sciences 21, no. 1 (2022): 109–15. https://doi.org/10.5281/zenodo.7648918.

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Saxagliptin is an oral hypoglycemic agent act by inhibiting dipeptidyl peptidase 4 and prescribed for the management of diabetes alone or with other anti-diabetic drug. The idea of the research is to clarify the impact of saxagliptin treatment on adipokines of corpulence in diabetic patients. Of seventy-three diabetic patients with corpulence (43 males and 30 females), aging (45&plusmn; 7) years of either sex were appointed to take Saxagliptin (5 mg/day) for 5 months periods. Data were pooled on fasting state prior treatment and after five months treatment. The variables involved body mass ind
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Fisher, Miles. "Series: Cardiovascular outcome trials for diabetes drugs Saxagliptin and SAVOR-TIMI 53." British Journal of Diabetes 19, no. 1 (2019): 34–36. http://dx.doi.org/10.15277/bjd.2019.213.

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SAVOR-TIMI 53 was the first FDA-mandated cardiovascular outcome trial to be presented and published. It compared saxagliptin and placebo in 16,492 patients with type 2 diabetes. SAVOR-TIMI 53 demonstrated non-inferiority for major cardiovascular events (cardiovascular death, myocardial infarction, stroke) but not superiority. An unexpected statistically significant increase in adjudicated hospitalisation for heart failure was seen in the saxagliptin group. Post hoc analysis demonstrated that subjects at greatest risk for hospitalisation for heart failure had previous heart failure, an estimate
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Atmakuri, Lakshmana Rao, Jhansi Nelapati, Bhaskar Vallamkonda, Ranadheer Reddy Challa, Subrahmanya Sai Malleswara Sharma Sonti, and Krishna Sudarsana Bhuvanagiri. "Design and Development of Saxagliptin Microparticles for Diabetes." Biomedical and Pharmacology Journal 17, no. 4 (2024): 2287–94. https://doi.org/10.13005/bpj/3024.

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This study investigates the design, development, and evaluation of sustained-release Saxagliptin microparticles, utilizing Eudragit L-100 and Eudragit S-100 as polymers to achieve prolonged drug release. A total of eight formulations were prepared, employing varying drug-to-polymer ratios (1:1, 1:2, 1:3, and 1:4) for both core and coat materials. This approach facilitated an assessment of the concentration of coating material influenced the drug release rate. The solvent evaporation method proved effective in producing discrete, spherical microparticles characterized by good flowability and mi
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Lee, Jeong-Min, Jin-Ha Yoon, Han-Joo Maeng, and Yu Chul Kim. "Physiologically Based Pharmacokinetic (PBPK) Modeling to Predict CYP3A-Mediated Drug Interaction between Saxagliptin and Nicardipine: Bridging Rat-to-Human Extrapolation." Pharmaceutics 16, no. 2 (2024): 280. http://dx.doi.org/10.3390/pharmaceutics16020280.

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The aim of this study was to predict the cytochrome P450 3A (CYP3A)-mediated drug–drug interactions (DDIs) between saxagliptin and nicardipine using a physiologically based pharmacokinetic (PBPK) model. Initially, in silico and in vitro parameters were gathered from experiments or the literature to construct PBPK models for each drug in rats. These models were integrated to predict the DDIs between saxagliptin, metabolized via CYP3A2, and nicardipine, exhibiting CYP3A inhibitory activity. The rat DDI PBPK model was completed by optimizing parameters using experimental rat plasma concentrations
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Zinjad, Sanchay S., S. G. Patel, D. D. Gaikwad, and S. L. Jadhav. "Analytical Method Development of Saxagliptin HCl by RP-HPLC." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 274–78. http://dx.doi.org/10.22270/jddt.v9i4.3040.

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Reversed-phase chromatography is the mainly used in chromatographic mode, it is used to separate neutral molecules in solution based on their hydrophobicity. This technique is the reverse of normal-phase chromatography in the intelligence that it involves the employ of a polar mobile phase and a non-polar stationary phase. A sensitive, accurate, rapid, cost effective and robust HPLC method was developed for the quantification of Saxagliptin Hydrochloride (SGH) with UV detector. In this method, a reversed-phase Grace C18 (250mm x 4.6ID, Particle size: 5 micron) column with a mobile phase of met
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Torre, Enrico, Giacomo Matteo Bruno, Sergio Di Matteo, et al. "Cost-Utility Analysis of Saxagliptin/Dapagliflozin Versus Gliclazide and Insulin Glargine: Economic Implications of the Outcomes of the CVD-Real Studies I and II." Health Services Insights 13 (January 2020): 117863292092998. http://dx.doi.org/10.1177/1178632920929982.

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Diabetes treatment cost represents an ever-growing problem. The adoption of new drugs in therapy, although they can guarantee an improvement in patient’s quality of life, can meet obstacles when it involves an increase in costs. We decided to compare the costs and benefits of the new saxagliptin and dapagliflozin combination versus traditional therapies. Bodyweight loss and the sharp reduction in hypoglycemic episodes were the 2 main clinical outcomes that emerged from registered studies of saxagliptin and dapagliflozin compared with the sulfonylureas. These results, combined with the good car
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Alhamhoom, Yahya, Gundawar Ravi, Riyaz Ali M. Osmani, Umme Hani, and Gowrav M. Prakash. "Formulation, Characterization, and Evaluation of Eudragit-Coated Saxagliptin Nanoparticles Using 3 Factorial Design Modules." Molecules 27, no. 21 (2022): 7510. http://dx.doi.org/10.3390/molecules27217510.

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Background and Introduction: Saxagliptin is a hypoglycemic drug that acts as a dipeptidyl peptidase-4 (DPP-4) inhibitor and is preferably used in the treatment of Type 2 Diabetes Mellitus (T2DM). It is safe and tolerable; however, the major disadvantage associated with it is its low bioavailability. Aim: The present research aimed to enhance the bioavailability of the drug by enteric coating with a polymer that controls the rate of drug delivery, and it was prepared as Solid Lipid Nanoparticles (SLNs). Methodology: In the current study, various SLN formulations were developed using a central c
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