Formulation Development and Evaluation of a Bilayered Tablet Containing Dapagliflozin and Metformin

Abstract

The overall Bilayered tablets may offer an effective platform for combining the two drugs or formulations with distinct release characteristics within a single dosage form. The current study had been done to design and develop bilayered tablets based on the concept of loading dose to achieve quick attainment of peak plasma concentration and sustained therapeutic efficacy. Design and development of twenty bilayered tablet formulations, incorporating the concept of loading dose strategy for both dapagliflozin and metformin. The immediate-release layer containing dapagliflozin was formulated to provide a rapid pharmacological response, while the sustained-release layer containing metformin was designed to maintain prolonged drug release. Due to the interaction between dapagliflozin and magnesium stearate observed, excipients and superdisintegrants were tried in the developed formulations S1–S10 and include sodium starch glycolate, croscarmellose sodium, sodium citrate, sodium lauryl sulphate, and potassium citrate (inclusive of BP grades). Metformin lactose monohydrate, lactose anhydrous, mascrogenol, and magnesium stearate were tested for interaction in the case of the metformin sustained-release layer. Based on this, formulations S11–S19 were prepared using hydrophilic polymers like HPMC K-15, HPMC E-50, and HPMC K-100 for controlled drug release. No major drug–excipient incompatibility was noted in optimized formulation. Optimized formulation S20 successfully ensured the loading dose through immediate release of dapagliflozin and sustained release of metformin. Optimization of immediate release layer and sustained-release layer was done separately.