Metformin liquid formulation
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Liquid Formulation of Metformin: Overview and Key Ingredients
Liquid formulations of metformin are designed to provide a therapeutically effective dose of the drug in a form that is easier to swallow, especially for pediatric and geriatric patients or those with swallowing difficulties. These formulations often include sweetening agents, cellulose, polyhydroxy alcohols, and pH stabilizers to ensure palatability and stability without increasing blood glucose levels after ingestion. They are primarily used for treating hyperglycemia and diabetes, offering an alternative to traditional tablet forms .
Pediatric and Geriatric Applications: Extemporaneous and Commercial Liquid Metformin
Several studies have focused on the development and evaluation of extemporaneous liquid formulations of metformin for pediatric use. These formulations, often prepared by dissolving metformin tablets in water with sweeteners like sucralose or Stevia, have demonstrated good physicochemical stability for up to 30 days under various storage conditions and retained over 90% of the initial drug content . Both sucralose and Stevia were found to be non-cytotoxic, making them suitable for pediatric formulations .
In clinical trials, liquid metformin formulations showed pharmacokinetics similar to those of tablets, with comparable maximum concentration (Cmax), time to maximum concentration (Tmax), and half-life, allowing for precise dose adjustments and easier administration in children and adolescents 36. This similarity in pharmacokinetics was also observed in healthy adult volunteers, supporting the use of liquid formulations for more accurate dosing and improved patient compliance .
Sustained-Release and In Situ Gel Liquid Formulations
Innovative liquid oral sustained-release (SR) formulations, such as floating in situ gels, have been developed to increase gastric residence time and provide controlled drug release. These gels, made with sodium alginate and various grades of hydroxypropyl methylcellulose (HPMC), gel instantly in gastric fluid and float for over 24 hours, releasing metformin in a sustained manner for up to 12 hours 29. Such formulations have shown significant reductions in blood glucose levels in animal studies and demonstrated safety with no observed toxicity to pancreatic tissues . These SR liquid forms are particularly beneficial for patients who have difficulty swallowing tablets, such as the elderly 29.
Extended-release oral suspensions based on metformin pellets coated with ethylcellulose and suspended in sugar-free syrup vehicles have also been developed. These suspensions provide uniform drug distribution, are stable, and release up to 85% of the drug over 8 hours, following zero-order kinetics .
Stability, Safety, and Analytical Methods
Liquid metformin formulations, whether extemporaneous or commercially developed, have been shown to be stable under various storage conditions, maintaining their integrity and drug content for extended periods . Analytical methods using ultra-performance liquid chromatography (UPLC) have been validated for measuring metformin levels in small blood samples, supporting clinical monitoring and dose adjustments .
Alternative Delivery: Transdermal Liquid Formulations
Research has also explored transdermal delivery of metformin using liquid crystalline lipid particles and ionic liquid technology. These approaches aim to reduce gastrointestinal side effects and improve patient adherence. Transdermal formulations have demonstrated high encapsulation rates, sustained drug release, and significant reductions in blood glucose levels in animal models, with no observed skin toxicity 78. The use of ionic liquids allows for fine-tuning of the drug’s properties, enhancing its suitability for transdermal delivery .
Conclusion
Liquid formulations of metformin offer significant advantages in terms of dosing flexibility, ease of administration, and patient compliance, especially for pediatric and geriatric populations. Both immediate-release and sustained-release liquid forms have demonstrated stability, safety, and pharmacokinetic profiles comparable to traditional tablets. Advances in formulation technology, including in situ gels and transdermal systems, further expand the therapeutic options for metformin delivery, making these formulations a promising alternative for diabetes management 12345678+1 MORE.
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