A bioequivalence study of gliclazide based on quantification by high-performance liquid chromatography coupled with electrospray tandem mass spectrometry

Mendes, Gustavo Duarte; Moreira, Leonard D; Pereira, Alberto dos Santos; Borges, André; Yui, F; Mendes, FD; Nucci, G De

doi:10.5414/cpp45175

Cited by 9 publications

(4 citation statements)

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“…Figure 1 depicts the workflow of this project: (1) literature search and subsequent development of a PK model for gliclazide IR and MR formulation, (2) re‐estimation of the PD model for post‐prandial glucose and insulin 15,16 with placebo arm data, 17 (3) developing a PK‐PD model for gliclazide, exploring the drug site of action and (4) simulations of dosing regimens and two formulations for predicting steady‐state glycated haemoglobin (HbA1c) and risk of hypoglycaemia. All studies used to generate the data for this analysis are already published 18–38 …”

Section: Methodsmentioning

confidence: 99%

“…The literature search, with search terms gliclazide and pharmacokinetic*, identified 258 unique articles, of which 30 articles were reviewed in full (Figure B1). Of the 25 articles fulfilling the inclusion criteria, 21 articles were digitizable (i.e., sufficient resolution; Table B1); 11 studies of IR formulation in HV, [18][19][20][21][22][23][24][25][26][27][28] two studies of IR formulation in patients with T2D, 29,30 five studies of MR formulation in HV, [31][32][33][34][35] two studies of IR in both HV and patients 36,37 and one study in HV of both IR and MR formulation. 38 The total number of arms was 77 (58 IR in HV, 7 IR in patients with T2D and 12 MR in HV).…”

Section: Pk Datamentioning

confidence: 99%

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Optimal dosing of gliclazide—A model‐based approach

Mim

Hussein

Vidadi

et al. 2023

Basic Clin Pharma Tox

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Gliclazide was approved as a treatment for type 2 diabetes in an era before model-based drug development, and consequently, the recommended doses were not optimised with modern methods. To investigate various dosing regimens of gliclazide, we used publicly available data to characterise the doseresponse relationship using pharmacometric models. A literature search identified 21 published gliclazide pharmacokinetic (PK) studies with full profiles. These were digitised, and a PK model was developed for immediate-(IR) and modified-release (MR) formulations. Data from a gliclazide dose-ranging study of postprandial glucose were used to characterise the concentration-response relationship using the integrated glucose-insulin model. Simulations from the full model showed that the maximum effect was 44% of the patients achieving HbA1c <7%, with 11% experiencing glucose <3 mmol/L and the most sensitive patients (i.e., 5% most extreme) experiencing 35 min of hypoglycaemia. Simulations revealed that the recommended IR dose (320 mg) was appropriate with no efficacy gain with increased dose. However, the recommended dose for the MR formulation may be increased to 270 mg, with more patients achieving HbA1c goals (i.e., HbA1c <7%) without a hypoglycaemic risk higher than the resulting risk from the recommended IR dose.

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Section: Methodsmentioning

confidence: 99%

Section: Pk Datamentioning

confidence: 99%

Optimal dosing of gliclazide—A model‐based approach

Mim

Hussein

Vidadi

et al. 2023

Basic Clin Pharma Tox

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“…Plasma concentrations of gliclazide were determined by a high-performance liquid chromatography-mass spectrometric (HPLC LC/MS) assay. 13 The method was referenced to the Bioanalytical Method Guidance as stated in the United States Food and Drug Administration. The calibration standards and quality control samples were prepared by spiking known amounts of gliclazide in drugfree plasma.…”

Section: Determination Of Gliclazide Concentration In Plasmamentioning

confidence: 99%

CYP2C19*2 Polymorphism Is Associated with Impaired Oral Clearance of Gliclazide in Healthy Chinese

Chow¹,

Poon²,

Fok³

et al. 2020

PGPM

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Background: Previous studies suggest gliclazide is metabolised primarily by CYP2C19 rather than CYP2C9, unlike other sulphonylureas. CYP2C19 *2 and *3 polymorphisms are more common in Asians. Methods: We investigated the effect of CYP2C19 polymorphisms on gliclazide pharmacokinetics in 15 healthy male Chinese subjects after a single 80mg oral dose. Results: In CYP2C19 poor metabolisers (*2/*2, n=4), plasma area-under-the-curve was higher by nearly two-fold compared with intermediate metabolisers (*2 and *3 heterozygotes, n=7) and extensive metabolisers (*1/*1, n=4) (p<0.001). Apparent oral clearance was mean (SD) 0.70 (0.12), 1.22 (0.22) and 1.52 (0.47) mL/min/kg in poor, intermediate and extensive metabolisers, respectively (p = 0.005). Conclusion: CYP2C19*2 polymorphism is associated with increased total gliclazide concentration and reduced oral clearance. Pharmacogenetic studies are warranted on the impact of CYP2C19 polymorphisms on treatment response and hypoglycaemia.

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“…From the literature survey, quantification of GLZ has been reported employing high performance liquid chromatography (HPLC)/UV (Al Mahmud et al, 2015;Damanjeet and Lakshmi, 2009;Khan et al, 2014;Ravi kumar et al, 2013;Rouini et al, 2003), electrochemical (Kuoa and Wua, 2005), calorimetric (Awasthi and Kulkarni, 2014), or mass detection (Hu et al, 2009;Mendes et al, 2007;Wang et al, 2008;Zhong et al, 2005). HPLC continues to be the most widespread, cost-effective method for the analysis of drugs in biological samples.…”

Section: Introductionmentioning

confidence: 99%

Impact of sample storage conditions on gliclazide quantification in rat plasma by UHPLC/UV method: storage recommendation and pharmacokinetic application

Taha¹,

Elsayed²,

El-Ashmawy³

et al. 2021

J Appl Pharm Sci

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The effect of different storage durations/temperatures on the stability of gliclazide (GLZ) in plasma was not studied before in the literature. A simple, reproducible ultra-high performance liquid chromatography coupled with ultraviolet detection (UHPLC/UV) was established for monitoring GLZ in rat plasma was established, with all stability parameters fully evaluated. The developed method provided simple solvent extraction for both GLZ and Glibenclamide as an internal standard (I.S.) with a short run time (≤ 7 minutes). A linear calibration curve (0.1-40 µg/ml), with good intra-and inter-day precision and accuracy, was established based on 40-ul plasma volume. Lower and upper limits of quantification allowed effective monitoring of the expected variations in GLZ absorption. The stock solution, freeze-thaw, short-term and bench stability results safeguard the rationale of the UHPLC/UV method. However, GLZ plasma samples were only stable for 1 week storage at −20°C or −80°C. The present study emphasized the importance of proper storage conditions, with recommendations for direct analysis of GLZ in plasma after sample collection or maximum storage for 1 week at −20°C or −80°C until analysis, to ensure accurate measurement of the drug in plasma. This method was effectively applied in a pharmacokinetic study of GLZ single oral dose from the market product Diamicron ® MR 30 mg administered in six rats.

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A bioequivalence study of gliclazide based on quantification by high-performance liquid chromatography coupled with electrospray tandem mass spectrometry

Cited by 9 publications

References 0 publications

Optimal dosing of gliclazide—A model‐based approach

Optimal dosing of gliclazide—A model‐based approach

<p><em>CYP2C19</em>*<em>2</em> Polymorphism Is Associated with Impaired Oral Clearance of Gliclazide in Healthy Chinese</p>

Impact of sample storage conditions on gliclazide quantification in rat plasma by UHPLC/UV method: storage recommendation and pharmacokinetic application

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