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gemigliptin + metformin hydrochloride (ZemiMet / ZemiMet SR)

✓ Approved

LG Chem Ltd. · DPP4 · 小分子

什么是 gemigliptin + metformin hydrochloride？

gemigliptin + metformin hydrochloride 是一种小分子，由LG Chem Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名ZemiMet, ZemiMet SR
公司LG Chem Ltd.
药物类别小分子
分子靶点DPP4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, LG Chem Ltd.

作用机制

分子靶点

gemigliptin + metformin hydrochloride 作用于 1 个分子靶点：

DPP4dipeptidyl peptidase 4 (CD26, DPPIV)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

gemigliptin + metformin hydrochloride 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersType 2 diabetes mellitus✓ Approved

相关研究文献

PubMedPharmaceutics2026-10-27

Impact of Process Parameters on the Quality Attributes of High-Dose Metformin Hydrochloride Film-Coated Tablets.

Duc Nguyen Tan NT, Nguyen Dang-Khoa DK, Liet Huynh Thanh HT, Thiet Nguyen Huynh NH et al.

Background/Objectives: Formulating high-dose metformin hydrochloride film-coated tablets is challenging due to the poor flowability and compressibility inherent to high drug loading. To ensure process robustness and consistent product quality, understanding the impact of manufacturing variables is crucial. This study evaluated the effects of key process parameters on the quality attributes of 1000 mg metformin hydrochloride tablets to establish optimal processing conditions for reliable production. Methods: The manufacturing process, comprising wet granulation, compression, and film coating, was investigated to evaluate the influence of key process parameters on tablet quality attributes. Granules were characterized for bulk density, tapped density, and compressibility index. Core tablets were evaluated for physical appearance, weight variation, hardness, and dissolution at a 45 min sampling point across various compression forces and tableting speeds. Film-coating efficiency was assessed based on coating quality, dissolution behavior, and stability. Favorable manufacturing conditions were empirically identified through single-variable optimization and statistical analysis. Results: Wet granulation conducted at a chopper speed of 1400 rpm for 7 min yielded granules with the lowest compressibility index (11.88%), demonstrating significantly improved flowability. Compression at a force of 10 kN and a speed of 40 rpm produced core tablets with acceptable appearance, robust hardness (7.06-7.37 kP), and complete drug release (100%). Tablet hardness was governed by a strong interaction between compression force and tableting speed (partial η2 = 0.929, p < 0.001) rather than by either factor alone: at 20 kN, hardness collapsed sharply once tableting speed reached 30 rpm, coincident with mild capping, identifying this force-speed combination as a process-failure condition. For the coating process, maintaining a tablet bed surface temperature of 40 °C ensured optimal coating uniformity without compromising product quality. Dissolution profile comparison against a coated reference product in the primary dissolution medium (pH 6.8) yielded f2 similarity values above 50 for all eight core tablet conditions, and stability testing under accelerated/thermal-stress conditions (up to 65 °C) confirmed maintained dissolution, assay, and related-substance (1-cyanoguanidine) compliance for both the test and reference products. The optimized manufacturing conditions successfully produced film-coated tablets that conformed to all predetermined quality specifications. Conclusions: Manufacturing process parameters significantly influenced the quality attributes of high-dose metformin hydrochloride film-coated tablets. Proper selection and control of these processing conditions ensured consistent granule properties, optimal tablet quality, and enhanced manufacturing robustness.

PMID 42942796
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Bioequivalence Assessment of Sitagliptin/Metformin Extended-Release Fixed-Dose Combinations in Healthy Mexican Subjects Under Fasting and Fed Conditions.

Hernández Piña Omar Emmanuel OE, de la Cruz Cruz Porfirio P, Guido Ávila Erika Gabriela EG, Martínez Muñoz Alberto A et al.

Background/Objectives: Management of Type 2 Diabetes (T2D) frequently requires combination therapy. Fixed-dose combinations (FDCs) of sitagliptin and extended-release (ER) metformin improve therapeutic adherence but pose biopharmaceutical challenges related to matrix robustness and food-drug interactions. This study evaluated the pharmacokinetics and bioequivalence of two generic sitagliptin/metformin ER FDCs (50/1000 mg and 100/1000 mg) versus reference products under fasting and fed conditions in healthy Mexican subjects. Methods: Four independent, randomized, open-label, two-period, single-dose crossover studies were conducted. We enrolled 184 healthy subjects (46 per study) with a 7-day washout period. Plasma concentrations of sitagliptin and metformin were quantified using a validated LC-MS/MS method. Results: The 90% confidence intervals for the geometric mean ratios (Test/Reference) of Cmax, AUC0-t, and AUC0-∞ for both analytes fell entirely within the 80.00-125.00% bioequivalence acceptance range across all studies. Under fed conditions, prolonged tmax and the absence of concentration spikes confirmed ER matrix preservation, with no evidence of food-induced dose dumping. The safety profile was highly favorable; all adverse events were mild or moderate and completely resolved without sequelae. Conclusions: The evaluated generic sitagliptin/metformin ER FDCs demonstrated pharmacokinetic bioequivalence to the reference products under fasting and fed conditions. These findings meet stringent regulatory requirements (NOM-177-SSA1-2013), support pharmacokinetic bioequivalence as the regulatory basis for safe therapeutic interchangeability, and provide robust, region-specific clinical data for the Latin American population. ClinicalTrials.gov identifiers: NCT07763899, NCT07763912, NCT07763951, and NCT07763964.

PMID 42943229
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Multi-Omics Analysis Identifies Gut-Associated Metabolic Signatures Associated with Metformin-Mediated Protection Against LPS-Induced Lung Injury.

Cheng Meihui M, Zhang Mi M, Wang Wei W, Jia Xianxian X et al.

Background/Objectives: Lipopolysaccharide (LPS)-induced lung injury involves pulmonary inflammation, metabolic disturbance, and intestinal dysregulation. This study investigated whether metformin attenuates LPS-induced lung and colonic injury and characterized associated gut microbiota-metabolite changes. Methods: Male C57BL/6J mice were assigned to control (CON), LPS, metformin 200 mg/kg (MET 200 mg/kg), and metformin 400 mg/kg (MET 400 mg/kg) groups. Metformin was administered by gavage for 7 days before intranasal LPS challenge. Lung and colon injury were assessed by histology, immunostaining, ELISA, and RT-qPCR. Untargeted serum metabolomics, colonic-content metabolomics, and colonic-content shotgun metagenomics were performed in the CON, LPS, and MET 400 mg/kg groups. Differential-feature, pathway-enrichment, and exploratory Spearman correlation analyses were conducted. Results: Metformin reduced LPS-induced lung injury, inflammatory cytokine production, F4/80- and MPO-positive immune-cell infiltration, and colonic inflammatory and barrier-related abnormalities. Serum metabolomics identified 468 differential features in LPS versus CON and 286 in MET versus LPS, with 218 overlapping features. Colonic-content metabolomics identified 1000 and 554 differential features, respectively, with 328 overlapping features. Eight metabolites showed metformin-associated directional shifts toward control levels in both serum and colonic contents. Metagenomics showed metformin-associated remodeling of gut microbial composition and predicted gene-content functional potential. Exploratory integrated analyses linked metformin-responsive genera and shared metabolites with pulmonary inflammatory indicators. Conclusions: Metformin was associated with attenuated LPS-induced lung and colonic injury and coordinated gut-associated microbiota-metabolite remodeling. Because the study did not include a metformin-only group or causal perturbation experiments, these findings identify candidate associations rather than demonstrating a causal gut microbiota-metabolite-lung mechanism.

PMID 42943340
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PubMedAdvances in drug and alcohol research2026-10-27

Acute metformin treatment increased social sniffing in male but not female BTBR mice.

Greene Susan M SM, Alcala Gloria-Andrea GA, Bordas Blanka B, Vu Vy V et al.

Autism spectrum disorders (ASDs) are characterized by social deficits and restrictive-repetitive behaviors. Metformin has recently been investigated for its potential behavioral effects in ASD models. This study examined the acute effects of metformin on social interaction preferences and marble burying in male and female BTBR T + Itpr3tf/J (BTBR) mice, with C57BL/6J and 129S1/SvImJ mice included as strain controls. The mice received a single intraperitoneal injection of metformin (0 mg, 75 mg, or 150 mg/kg), and the effects were compared using three-chamber social preference and marble burying tests. Acute metformin increased not only social interaction preferences, as determined by differences in time spent in chambers, but also by differences in social sniffing time in male BTBR mice at 150 mg/kg. Surprisingly, it did not alter sociability preferences in BTBR females or in C57BL/6J or 129S1/SvImJ mice. In C57BL/6J females, metformin reduced chamber entries and marble burying, whereas males were unaffected. Progesterone and corticosterone levels were measured in BTBR and C57BL/6J serum collected after behavioral testing, and their levels were unaffected by metformin treatment. These findings indicate that metformin acutely produces modest, beneficial behavioral effects in male BTBR mice, which otherwise exhibit social interaction deficits that are translationally relevant to ASD.

PMID 42935953
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PubMedDiabetes, obesity & metabolism2026-10-27

Metformin Use During Pregnancy and Early-Life Nutritional Status: A Systematic Review of Randomized Clinical Trials.

Perichart-Perera Otilia O, Hernández-Hernández Larissa L, Rodríguez-Cano Ameyalli M AM

Metformin is increasingly used to treat gestational diabetes mellitus and other insulin-resistant conditions during pregnancy. Because it crosses the placenta, concerns remain regarding its potential effects on offspring growth and metabolic programming. This systematic review evaluated the effects of prenatal metformin exposure on infant nutritional status and adiposity during the first year of life. PubMed and Scopus were searched from inception through May 2026 for randomized controlled trials comparing metformin with placebo or standard care during pregnancy. Eligible studies reported infant nutritional status or adiposity-related outcomes from birth to 12 months. Risk of bias was assessed, and results were synthesized narratively. Eight publications from six randomized controlled trials were included. Birthweight and birth size classifications were the most frequently reported outcomes. Metformin was not consistently associated with differences in birthweight or other anthropometric measures. One trial reported lower birthweight, while two reported fewer large-for-gestational-age or macrosomic infants. No study assessed direct measures of infant adiposity. Current evidence does not consistently support an effect of prenatal metformin exposure on early infant anthropometry. Limited postnatal data and absent adiposity measures limit conclusions regarding postnatal growth and early metabolic programming and support standardized longitudinal body composition assessment.

PMID 42935209
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PubMedPharmaceutics2026-10-27

3D-Printed Gastroretentive Floating Modified-Release Device for Dual Cardiovascular Drug Delivery: Isosorbide Dinitrate and Hydralazine.

Jaiseri Dareena D, Pengnam Supusson S, Opanasopit Praneet P, Suriyaamporn Phuvamin P et al.

Background: Isosorbide dinitrate (ISDN) and hydralazine hydrochloride (HDZ) are dual cardiovascular drugs used to treat heart failure. However, the drugs have limitations such as short plasma half-life, low bioavailability, and potential for tolerance of the nitrate component. To address the need for prolonged drug release, a floating dual-compartment drug delivery system was developed to provide controlled drug release under simulated gastric dissolution conditions. Objectives: This study aimed to develop floating dual-compartment devices (FDCDs) to contain ISDN and HDZ gel and modify drug release under simulated gastric conditions. Methods: The FDCD was designed in a cylindrical shape consisting of an air chamber on the upper part for floating ability, and two compartments for loaded drug gel and controlling the drug release rate. Fused deposition modeling (FDM) was selected to fabricate FDCDs using polylactic acid (PLA) filament. The ISDN formulation varied the ratio of polyvinylpyrrolidone (PVP) to achieve drug release for 12 h. The HDZ formulation was optimized by varying the ratio of PVP and hydroxypropyl methylcellulose (HPMC) to extend drug release at 24 h. Results: The shape dimension and weight variation in the FDCDs showed low standard deviation (SD). FDCDs exhibited immediate floating, resisted overturning, and demonstrated in vitro floating ability for more than 24 h. The formulation ISDN3 at a PVP: drug: water ratio of 5:2:3 exhibited complete release at 12 h, while the formulation of HDZ1 at an HPMC: PVP: drug: water ratio of 0.3:2.5:2:5.2 showed complete release within 24 h. The ISDN3- and HDZ1-loaded FDCDs demonstrated prolonged release behavior, with ISDN and HDZ release profiles showing the best fit to the zero-order and Higuchi models, respectively, based primarily on the coefficient of determination (R2), while root mean square error (RMSE) was used as a complementary measure of fitting error. Conclusions: These findings suggest that the developed dual-drug-loaded FDCD has potential as a dual-drug oral delivery platform for simultaneous delivery of ISDN and HDZ with prolonged drug release characteristics and further development of oral combination drug delivery systems.

PMID 42942809
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