A Versatile Approach for Evaluation of Linagliptin and Metformin Extended-Release Tablet by Drug Layering Technique

Type ۲ diabetes, a chronic metabolic condition characterized by hyperglycemia, frequently requires combination medication to maintain optimal glycemic control. Metformin, a biguanide, and linagliptin, a dipeptidyl peptidase-۴ (DPP-۴) inhibitor, have shown synergistic effects in improving glycemic outcomes. A unique and effective strategy for improving patient compliance and ensuring prolonged medication administration is to formulate a fixed-dose combination (FDC) as an extended-release (ER) tablet utilizing the drug layering technique. Creating a single ER tablet containing both medications can improve patient compliance by minimizing pill burden and ensuring consistent drug levels. The drug layering technique provides a possible strategy to develop such a combination product. This study covers how to formulate, optimize, and evaluate Linagliptin and Metformin ER tablets using this technique. The current work focuses on the formulation and optimization of extended-release (ER) tablets comprising Linagliptin and Metformin Hydrochloride, which employ a drug stacking approach. To improve patient compliance and maintain optimal glycemic control, drug layering tablet was developed with an immediate-release (IR) drug coating of Linagliptin and an ER layer of Metformin. The formulation approach required stacking Linagliptin onto inert cores with an appropriate binder solution in a fluid bed processor to ensure consistency and quick release. The ER Metformin layer was formulated with hydrophilic matrix-forming agents such hydroxypropyl methylcellulose (HPMC) to achieve regulated drug release over ۱۲-۲۴ h. The developed tablets were evaluated for physicochemical properties, drug release profiles, and stability in accordance with ICH recommendations. In vitro dissolution experiments revealed a biphasic release profile rapid release of Linagliptin and sustained release of Metformin which met USP criteria. The improved formulation had adequate drug content, friability, hardness, and predictable release kinetics.

کلیدواژه ها:

Linagliptin ، Metformin ، extended-release ، drug layering ، comparative dissolution profile