Metformin hydrochloride

• CAS: 1115-70-4
• Catalog Number: ACM1115704
• Category: Main Products
• Molecular Weight: 165.62
• Molecular Formula: C4H12ClN5
• Synonyms: 1,1-Dimethyl-biguanidhydrochloride
• IUPAC Name: 3-(Diaminomethylidene)-1,1-dimethylguanidine;hydrochloride
• Canonical SMILES: CN(C)C(=N)N=C(N)N.Cl
• InChI: InChI=1S/C4H11N5.ClH/c1-9(2)4(7)8-3(5)6;/h1-2H3,(H5,5,6,7,8);1H
• InChI Key: OETHQSJEHLVLGH-UHFFFAOYSA-N
• Melting Point: 223-226 °C(lit.)
• Density: 1.36 g/cm³ at 20 °C
• Appearance: White powder
• Storage: 2-8 °C
• Complexity: 132
• Exact Mass: 165.0781231
• Monoisotopic Mass: 165.0781231
• pKa: 12.4 (at 20 °C)
• Topological Polar Surface Area: 91.5 Ų

Case Study

Microparticle and Nanoparticle Drug Delivery Systems for Metformin Hydrochloride

Cetin, Meltem, et al. Drug delivery, 2016, 23(8), 2796-2805.
Choudhury, Pratim K., et al. Journal of Microencapsulation, 2009, 26(1), 46-53.

Metformin hydrochloride is a biguanide derivative widely used to treat type 2 diabetes and also has potential antitumor effects. In order to improve the oral bioavailability and biological half-life of metformin, many studies have explored more advantageous particulate drug delivery systems, including microspheres and microcapsules.
· Metformin hydrochloride loaded microcapsules: The preparation methods of metformin hydrochloride loaded microcapsules include emulsified ion transfer gel, non-aqueous emulsion-solvent evaporation method and Wurster fluidized bed method. For example, sodium alginate and karaya gum (1:1 w/w) are used as coating materials in the preparation of microcapsules, and metformin hydrochloride is prepared by using ion transfer gel and emulsified ion transfer gel methods. Microcapsules have controlled release properties and good mucoadhesive properties.
· Metformin hydrochloride loaded microspheres: Common preparation methods for metformin hydrochloride loaded microspheres are emulsion-solvent evaporation (ESE), non-solvent addition method (NSA), emulsification-free solvent evaporation method, spray drying method and nanoprecipitation method, etc. For example, emulsion-solvent evaporation (ESE) and non-solvent (petroleum ether) addition method (NSA) were used to prepare ethylcellulose microspheres containing metformin hydrochloride with controlled release characteristics.

Transdermal Delivery Strategy of Metformin Hydrochloride

Migdadi, Eman M., et al. Journal of controlled release, 2018, 285, 142-151.

A strategy for transdermal delivery of high-dose drug metformin hydrochloride in a sustained manner via a hydrogel-forming microneedle (MN) patch is proposed. This drug delivery strategy provides an alternative mode of drug delivery and helps minimize the gastrointestinal side effects and changes in small intestinal absorption associated with traditional oral administration.
Fabrication of lyophilised metformin hydrochloride reservoirs
· Metformin HCl-based drug reservoirs were produced by combining varying amounts of metformin HCl, gelatin, mannitol, and deionized water. After hand-mixing the components, the mixture was sonicated for 60 minutes at 37°C.
· The resulting formulations were then poured into cylindrical moulds (300mg, 150mg, or 100mg) with a diameter of 8mm and a depth of 4mm. The moulds were frozen at -80°C for at least 60 minutes and then lyophilized in a freeze drier using the following process: Primary drying at -40°C for 90 minutes, followed by drying at -30°C for 90 minutes, -20°C for 90 minutes, -10°C for 530 minutes, and 0-10°C for 90 minutes.
· Secondary drying was carried out at a shelf temperature of 25°C and a vacuum pressure of 50mTorr for 660 minutes.