Canagliflozin and Metformin Hydrochloride Modified-Release Tablet

According to the World Health Organization, more than 800 million adults worldwide are living with diabetes. As patent exclusivities on innovative combination therapies expire, generic pharmaceutical manufacturers face increasing pressure to develop therapeutically equivalent formulations that maintain consistent pharmacokinetic profiles whilst managing complex formulation challenges. Bilayer tablet technology has emerged as a strategic platform for delivering combination therapies, particularly in metabolic disease management. This approach enables the co-administration of APIs with different release profiles or chemical incompatibilities within a single dosage form, improving patient compliance whilst reducing pill burden. 

Canagliflozin and metformin hydrochloride come in the form of a bilayer tablet that contains canagliflozin immediate-release (IR) and metformin hydrochloride extended-release (ER) and is indicated, in conjunction with diet and exercise, to improve glycemic control in adults with type 2 diabetes mellitus.  

The primary formulation challenge when developing a robust IR/ER bilayer dosage form is providing pH-independent release characteristics and ensuring consistent 24-hour drug exposure. 

The development team at our Pharmaceutical Technical Centre (PTC) in Shanghai was involved in various development activities, including reverse engineering of the reference product, analytical method development, and design of prototype formulations. Prototype performance was evaluated in three biorelevant dissolution media and challenged through alcohol-induced dose-dumping studies to assess formulation robustness. Concurrently, detailed formulation and process risk assessments were conducted to identify the critical material attributes (CMAs) and critical process parameters (CPPs) most likely to impact product performance, quality, and manufacturability. 

Ideal for generic drug developers looking to accelerate market entry, this solution combines formulation expertise, risk-based development strategies, and access to all key formulation components, enabling faster decision-making, reduced development effort, and a streamlined path to commercialisation.