Delving into the Latest Updates on Gliclazide/Metformin Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

二甲双胍格列齐特

Target

PRKAB1 x SUR

Mechanism

PRKAB1 activators(Protein kinase AMP-activated non-catalytic subunit beta 1 activators), SUR agonists(Sulfonylurea receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Les Laboratoires Servier SAS

Active Organization

Jiangsu Lianhuan Pharmaceutical Co., Ltd.

Inactive Organization

Les Laboratoires Servier SAS

Drug Highest PhaseApproved

First Approval Date

CN (22 Sep 2005),

Diabetes Mellitus, Type 2

Regulation-

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Structure

Molecular FormulaC15H21N3O3S

InChIKeyBOVGTQGAOIONJV-UHFFFAOYSA-N

CAS Registry21187-98-4

View All Structures (2)

本试验旨在研究单次空腹和餐后口服北京四环科宝制药有限公司研制、生产的二甲双胍格列吡嗪片（500 mg/2.5 mg）的药代动力学特征；以Teva Pharmaceuticals IND. LTD.生产的二甲双胍格列吡嗪片（500 mg/2.5 mg）为参比制剂，比较两制剂中药动学参数Cmax、AUC0-t、AUC0-∞，评价两制剂的人体生物等效性。

[Translation]

This study aims to study the pharmacokinetic characteristics of single fasting and postprandial oral administration of metformin glipizide tablets (500 mg/2.5 mg) developed and produced by Beijing Sihuan Kebao Pharmaceutical Co., Ltd.; using metformin glipizide tablets (500 mg/2.5 mg) produced by Teva Pharmaceuticals IND. LTD. as the reference preparation, compare the pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ of the two preparations, and evaluate the bioequivalence of the two preparations in humans.

Start Date06 Jan 2021

Sponsor / Collaborator

Beijing Sihuan Kebao Pharmaceutical Co., Ltd.

NCT03467971 / CompletedPhase 1

A Randomized, Open-label, Single Dose, 2x2 Crossover Trial to Evaluate the Food Effect on the Bioavailability of a Metformin/Gliclazide Fixed Combination Tablet (1000 mg /30 mg MR) Given in Fasting and Fed Conditions to Healthy Volunteers

This study will assess the food effect on bioavailability of Metformin/Gliclazide fixed dose combination tablet in fed and fasted state.

Start Date06 Mar 2018

Sponsor / Collaborator

Merck KGaA

NCT03467945 / CompletedPhase 1

Randomized, Open Label, Single Dose, 4 Treatment, 4 Period, Crossover Design (4 x 4) Trial to Evaluate the Bioequivalence and Secondarily Drug - Drug Interaction of Fixed Combination of Metformin Tablets 1000 mg/Gliclazide 30 mg MR, Compared With the Co-administration of Individual Tablets and Individual Administration of Each Single Tablet (Metformin 1000 mg XR and Gliclazide 30 mg MR) in Healthy Volunteers

This study investigated the bioequivalence and drug-drug interaction of Metformin/Gliclazide fixed combination tablet compared to co-administration of individual tablets of Metformin and Gliclazide.

Start Date16 Feb 2018

Sponsor / Collaborator

Merck KGaA

100 Clinical Results associated with Gliclazide/Metformin Hydrochloride

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100 Translational Medicine associated with Gliclazide/Metformin Hydrochloride

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100 Patents (Medical) associated with Gliclazide/Metformin Hydrochloride

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3

Literatures (Medical) associated with Gliclazide/Metformin Hydrochloride

01 Oct 2022·Pharmaceutical Research

Transdermal Delivery of Metformin Utilizing Ionic Liquid Technology: Insight Into the Relationship Between Counterion Structures and Properties

Article

Author: Qi, Ming-Hui ; Ren, Guo-Bin ; Wang, Qinglin ; Hong, Minghuang ; Li, Jinghui ; Wang, Kai

PURPOSEThe purpose of the present study was to explore the feasibility of transdermal delivery of metformin, a commonly used oral antidiabetic drug, by ionic liquid (IL) technology.METHODSMetformin hydrochloride (MetHCl) was first transformed into three kinds of ILs with different counterions. The physicochemical properties of the obtained ILs were characterized in depth. The simulation of stable configuration and calculation of interaction energies were conducted based on density functional theory (DFT). Skin-PAMPA was used to evaluate the intrinsic transdermal permeation properties. The cytotoxicity assay of these ILs was conducted using HaCaT cells to evaluate the toxicity to skin. These metformin ILs were then formulated into transdermal patch, and the transdermal potential was further evaluated using in vitro dissolution test and skin permeation assay. Finally, the pharmacokinetic profiles of these metformin IL-containing patches were determined.RESULTSAmong all the three Met ILs, metformin dihexyl sulfosuccinate (MetDH) with proper overall physiochemical and biological properties demonstrated the highest relative bioavailability. Metformin docusate (MetD) with the highest lipophilicity and intrinsic transdermal permeability exhibited the most significant sustained release profile in vivo. Both MetDH and MetD were the promising candidates for further clinical investigations.CONCLUSIONSOverall, the properties of ILs were closely related to the structures of counterion. IL technology provided the opportunities to finely tune the solid-state and biological properties of Metformin and facilitated the successful delivery by transdermal route.

01 Jul 2020·International Journal of Biological MacromoleculesQ1 · CHEMISTRY

Development of metformin hydrochloride loaded dissolving tablets with novel carboxymethylcellulose/poly-l-lysine/TPP complex

Q1 · CHEMISTRY

Article

Author: Wu, Qing-Xi ; Zheng, Meng-Fei ; Guan, Yi-Xin ; Su, Ting ; Chen, Yan ; Wang, Zi-Dan ; Wang, Xiao-Hui

Natural polymers like polysaccharides, polypeptides and their derivatives are broadly applied in drug delivery due to excellent biocompatibility and biodegradability. In this study, the dissolving tablets, formed with carboxymethylcellulose/poly-l-lysine/tripolyphosphate (CMC/PLL/TPP) complex, were prepared using metformin hydrochloride (MetHCl) as model drug. Confocal laser scanning microscopy observation manifested that FITC-labeled PLL interacted with CMC and formed a uniform interior microstructure. Scanning electron microscope images showed the drug-loaded tablets had well-formed shapes with smooth surfaces. MetHCl embedded interior the microstructures of the tablets and represented in a crystal form. Thermo-gravimetric analysis and differential scanning calorimetry indicated that the drug-loaded tablets had stable thermal properties with less moisture content (3.52%). Fourier transform infrared spectrometer confirmed that the CMC/PLL/TPP complex was fabricated via the electrostatic interactions between -NH₃⁺, -COO^- and -[P₂O₅⁴-]^- groups. The drug-loaded tablets had a high drug loading efficiency of 85.76% and drug encapsulation efficiency of 81.47%, and a shorter wetting time of 2.16 min in SSF (pH 6.8) and lower swelling ratio of 233.34%. The drug loaded in the samples could be released completely within 10 min in simulated saliva fluid (SSF pH 6.8), indicating a rapid drug release and dissolving profile in the environment, which could be developed for dissolving tablets.

28 May 2017·Journal of Drug TargetingQ3 · MEDICINE

Preparation and in vitro/in vivo evaluation of metformin hydrochloride rectal dosage forms for treatment of patients with type II diabetes

Q3 · MEDICINE

Article

Author: Zaghloul, Abdel-Azim ; Abd-Allah, Fathy ; Nada, Aly ; Lila, Ahmad

BACKGROUNDMetformin hydrochloride (MtHCL) is an oral antidiabetic drug and has many other therapeutic benefits. It has poor bioavailability, narrow absorption window and extensive liver metabolism. Moreover, children and elders face difficulty to swallow the commercial oral tablets.OBJECTIVESPreparation, in vitro/in vivo evaluation of MtHCL suppositories for rectal administration to solve some of these problems.METHODSSuppository fatty bases (Witepsol^®, Suppocire^® and Massa^®; different grades) and PEG bases 1000, 4000 and 6000 (different ratios), were used to prepare rectal suppository formulations each containing 500 mg drug. These were characterized for manufacturing defects, and pharmacotechnical performance and formulations showing superior results were subjected to bioavailability testing in human volunteers compared with the commercial oral tablet (Ref) applying LC-MS/MS developed analytical technique.RESULTSThe preparation method produced suppositories with satisfactory characteristics and free of manufacturing defects. The fatty bases were superior compared with PEG bases regarding the physical characteristics. Three formulations were chosen for bioavailability testing and the results showed comparable bioavailability compared to the Ref.CONCLUSIONSThe fatty bases showed superior characteristics compared with the PEG bases. MtHCL formulated in selected fatty bases could be a potential alternative to the commercial oral tablets particularly for pediatric and geriatric patients.

100 Deals associated with Gliclazide/Metformin Hydrochloride

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R&D Status

Approved

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	CN	Jiangsu Lianhuan Pharmaceutical Co., Ltd.	22 Sep 2005

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 1	-	Les Laboratoires Servier SAS	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ADA2023	Not Applicable	Diabetes Mellitus, Type 2	110	Gliclazide-Metformin combination therapy	eqhwqzlwiq(jnlydybjhz) = mvnrnisosm bxhlayknyb (sfuazbbdhs ) View more	-	20 Jun 2023
				Insulin	eqhwqzlwiq(jnlydybjhz) = cvhkrslruo bxhlayknyb (sfuazbbdhs ) View more