格列齐特/盐酸二甲双胍(Gliclazide/Metformin Hydrochloride) - 药物靶点：PRKAB1 x SUR_在研适应症：2型糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

二甲双胍格列齐特

靶点

PRKAB1 x SUR

作用机制

PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂)、SUR激动剂(磺酰脲受体激动剂)

治疗领域

内分泌与代谢疾病

在研适应症

2型糖尿病

非在研适应症-

原研机构

Les Laboratoires Servier SAS

在研机构

江苏联环药业股份有限公司

非在研机构

Les Laboratoires Servier SAS

最高研发阶段批准上市

首次获批日期

中国 (2005-09-22),

2型糖尿病

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C15H21N3O3S

InChIKeyBOVGTQGAOIONJV-UHFFFAOYSA-N

CAS号21187-98-4

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关联

4

项与格列齐特/盐酸二甲双胍相关的临床试验

CTR20202686 / CompletedN/A

二甲双胍格列吡嗪片单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性研究

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。

开始日期2021-01-06

申办/合作机构

北京四环科宝制药股份有限公司

NCT03467971 / Completed临床1期

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.

开始日期2018-03-06

申办/合作机构

Merck KGaA

NCT03467945 / Completed临床1期

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.

开始日期2018-02-16

申办/合作机构

Merck KGaA

100 项与格列齐特/盐酸二甲双胍相关的临床结果

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100 项与格列齐特/盐酸二甲双胍相关的转化医学

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100 项与格列齐特/盐酸二甲双胍相关的专利（医药）

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3

项与格列齐特/盐酸二甲双胍相关的文献（医药）

2022-10-01·Pharmaceutical Research

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

Article

作者: 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.

2020-07-01·International Journal of Biological Macromolecules1区 · 化学

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

1区 · 化学

Article

作者: 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.

2017-05-28·Journal of Drug Targeting3区 · 医学

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

3区 · 医学

Article

作者: 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 项与格列齐特/盐酸二甲双胍相关的药物交易

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研发状态

批准上市

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适应症	国家/地区	公司	日期
2型糖尿病	中国	江苏联环药业股份有限公司	2005-09-22

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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	临床1期	-	Les Laboratoires Servier SAS	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ADA2023	N/A	2型糖尿病	110	Gliclazide-Metformin combination therapy	齋簾艱齋膚膚範構範遞(齋憲鹽醖築觸淵築顧積) = 構窪窪築醖積壓顧蓋鹽窪壓餘衊膚選淵淵膚襯 (鹽鹽窪築夢網構鹽窪艱 ) 更多	-	2023-06-20
				Insulin	齋簾艱齋膚膚範構範遞(齋憲鹽醖築觸淵築顧積) = 夢鏇願膚艱壓製選窪膚窪壓餘衊膚選淵淵膚襯 (鹽鹽窪築夢網構鹽窪艱 ) 更多