An Open-Label, Single-Period, Two-Stage, Single Oral Dose Pharmacokinetic Study of Remogliflozin Etabonate Tablet 100 and 250 mg in Healthy Asian Indian Male Subjects Under Fasting and Fed Conditions

Joshi, Shashank; Gudi, Girish; Menon, Vinu; Tandon, Monika; Joshi, Vikas; Suryawanshi, Sachin; Barkate, Hanmant; Sawant, Nikhil; Katare, Sagar; Siddique, Waseem

doi:10.1007/s40262-019-00819-4

Cited by 4 publications

(5 citation statements)

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“…The assessment of pharmacokinetic parameters for remogliflozin etabonate after administration of reference product is similar to a previous pharmacokinetic assessment of RE performed in healthy Indian male subjects in fasted and fed states [10]. The AUC 0-∞ for remogliflozin and GSK279782 is reported to be ranging from 1266.1 -1546.6 ng*h/mL and 323.6 -651.1 ng*h/mL after single dose of RE 100mg.…”

Section: Discussionsupporting

confidence: 73%

Bioequivalence Study of Fixed-Dose Combination of Remogliflozin Etabonate 100 mg/Vildagliptin 50 mg with Individual Components in Healthy Indian Male Subjects under Fed Conditions

2022

J Diabetes Treat

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Background and Objective. Combination of sodium glucose co-transporter-2 (SGLT2) and dipeptidyl peptidase-4 (DPP4) inhibitors has shown promising results in the treatment of type 2 diabetes mellitus. A Fixed Dose Combination (FDC) of remogliflozin and vildagliptin will reduce the pill burden and help improve treatment compliance. This study was conducted to establish the bioequivalence of an oral FDC of remogliflozin etabonate (100mg) and vildagliptin (50mg) with single tablets of Remo ® (remogliflozin etabonate; 100 mg) and Galvus ® (vildagliptin; 50 mg) Methods. Pharmacokinetic parameters i.e. maximum concentration (C max ) and area under concentration-time curve (AUC 0-t , and AUC 0-∞ ) were calculated to determine bioequivalence. Safety was assessed and adverse events were monitored throughout the trial. Results.For both remogliflozin and vildagliptin, 90% confidence interval (CI) of the geometric least-squares mean ratios of C max , AUC 0-t , and AUC 0-∞ values between FDC and reference products fell within the standard regulatory bioequivalence range of 85.0-125.0%. Remogliflozin etabonate and its metabolite, GSK279782, also demonstrated geometric least-squares mean ratio of ~ 100%. No clinical abnormalities or adverse events were reported during the study. Conclusion.The FDC of remogliflozin etabonate and vildagliptin was bioequivalent to the reference products (Remo ® and Galvus ® ) under fed state without any safety concerns.

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Section: Discussionsupporting

confidence: 73%

Bioequivalence Study of Fixed-Dose Combination of Remogliflozin Etabonate 100 mg/Vildagliptin 50 mg with Individual Components in Healthy Indian Male Subjects under Fed Conditions

2022

J Diabetes Treat

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“…The noteworthy difference is a short half-life of the new molecule that necessitates a twice-daily dosing regimen. 15,41 All other drugs in the same class have a longer half-life (around 12 hours). [46][47][48][49] Hence, other approved SGLT2 inhibitors (empagliflozin, dapagliflozin, canagliflozin, ertugliflozin) are administered as once daily dose.…”

Section: Discussionmentioning

confidence: 99%

“…Hence RE can be administered with or without food. 15 The plasma protein binding of remogliflozin was around 65%. Either RE or remogliflozin was not preferentially distributed to blood cells, and there was no selective association of RE or its metabolites with melanincontaining tissues.…”

Section: Scientific Summary Pharmacokinetic (Pk)/pharmacodynamic (Pd)mentioning

confidence: 99%

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<p>Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy</p>

Mohan¹,

Mithal²,

Joshi³

et al. 2020

DDDT

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Type 2 diabetes mellitus (T2DM) is an emerging epidemic in Asian countries, especially in India. With the advent of the SGLT2 inhibitor class of drugs demonstrating benefits beyond glycemic control, viz. weight loss, blood pressure reduction, and cardiovascular and renal protection, the management of T2DM has taken a quantum leap. Remogliflozin etabonate (RE) is the latest addition to the SGLT2 inhibitor class of drugs that have been recently approved in India for the management of T2DM. RE is a potent and selective inhibitor of SGLT2 with the unique distinction of being administered as a prodrug, existence of active metabolites, and short half-life necessitating twice-daily dosing. The Phase III study of RE demonstrated it to be an efficacious and safe agent and non-inferior to the currently available SGLT2 inhibitors. This paper reviews not only the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of RE but also its molecular and clinical development program. This review has taken into consideration all available published as well as unpublished literature on RE and discusses the individual studies performed during its development for characterization of pharmacological profile.

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“…However, no quantitative analytical method has been described for the concurrent estimation of VGN and RGE from a formulation. Derivative UV spectrophotometric techniques are simple, accurate, fast, and may possibly be utilized for the quantification of multicomponent formulations showing overlapping spectra [28][29][30][31][32] . Hence, in the current work, three spectrophotometric methods were validated and applied to a concurrent determination of VGN and RGE from laboratory mixed solutions and formulations.…”

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confidence: 99%

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2023

IJPSR

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Remogliflozin Etabonate, Metformin, Vildagliptin are anti-diabetic drugs. It inhibits the sodium-glucose transport proteins (SGLT), which are responsible -for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Several attempts were made on simultaneous analysis of Metformin with either Vildagliptin or Remogliflozin but no work were carried out on simultaneous analysis of all three drugs combination. In the present work, efforts are made to develop a simple new accurate, precise and linear reverse phase high performance liquid Chromatographic (RP-HPLC) method for simultaneous estimation of Remogliflozin etabonate (RGE), Metformin (MET) and Vildagliptin (VGN) in bulk drug and marketed tablet formulation Different analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection (LOD) and limit of quantification (LOQ) were determined according to International Conference on Harmonization ICH Q2B guidelines. Chromatographic separation was achieved on Acclaimed Mix Mode HILIC-1 column (150 mm × 4.6 mm, 5µm) applying an isocratic elution based on 20 mM ammonium acetate: acetonitrile (75:25, v/v) as a mobile phase. The ultraviolet detector was operated at 230 and 254 nm. The retention time for RGE was 3.81+0.5min, VGN was 4.86+0.5min, MET was 5.81+0.5min. The standard curve was linear over the concentration range of 3.9-62.5µg/ml with r2 close to one (1 to 0.999). The proposed method was validated for system suitability, specificity, linearity, accuracy, precision, LOD, LOQ and robustness. All parameters were found to be within the acceptance limit. INTRODUCTION: Remogliflozin Etabonate is an anti-diabetic drug, chemically known as 5-Methyl4 -[4-(1-methyl ethoxy) benzyl]-1-(1 methylethyl)-1H-pyrazol -3yl -6 -O-(ethoxy carbonyl)-β-D glucopyranoside. It inhibits the sodium-glucose transport proteins (SGLT), which are responsiblefor glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine 1-2 .

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An Open-Label, Single-Period, Two-Stage, Single Oral Dose Pharmacokinetic Study of Remogliflozin Etabonate Tablet 100 and 250 mg in Healthy Asian Indian Male Subjects Under Fasting and Fed Conditions

Cited by 4 publications

References 14 publications

Bioequivalence Study of Fixed-Dose Combination of Remogliflozin Etabonate 100 mg/Vildagliptin 50 mg with Individual Components in Healthy Indian Male Subjects under Fed Conditions

Bioequivalence Study of Fixed-Dose Combination of Remogliflozin Etabonate 100 mg/Vildagliptin 50 mg with Individual Components in Healthy Indian Male Subjects under Fed Conditions

<p>Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy</p>

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