Development of a stable fixed-dose combination of Montelukast Sodium and Levocetirizine Dihydrochloride using multi-layering API coating technology.

Abstract

Purpose: This study aimed to develop a combination drug containing Montelukast Sodium and Levocetirizine Dihydrochloride using Multi-Layering API Coating Technology (M-LAC Tech) to prevent chemical interactions, enhance stability, and enable sequential drug release.

Methods: A core tablet containing Montelukast Sodium was prepared, followed by a barrier coating layer. Levocetirizine Dihydrochloride was then applied as a drug coating over the barrier layer, ensuring complete separation of the two drugs. M-LAC Tech effectively prevents chemical interactions, overcoming the limitations of conventional single-layer and bilayer tablets. An outer coating was added to protect against environmental factors, resulting in a multi-layered film-coated tablet with improved stability and drug release characteristics.

Results: The developed tablet reduced size by 50% compared to bilayer tablets, improving patient compliance. The barrier coating effectively prevented drug interactions, ensuring stability, while sequential drug release reduced AUC variability and shortened T_max, enhancing absorption and efficacy. Compared to the reference "tablet-in-capsule" formulation, which releases both drugs simultaneously, the M-LAC Tech tablet demonstrated superior pharmacokinetic properties through controlled sequential release.

Conclusion: M-LAC Tech enabled the stable incorporation of two drugs in a single dosage form, achieving the smallest tablet size among similar formulations. The technology's ability to block drug interactions and optimize release profiles provides significant clinical advantages. These findings highlight the potential of M-LAC Tech in advancing combination drug development.