Gliclazide Modified-Release Tablet

Developing effective modified-release (MR) oral dosage forms for poorly soluble BCS Class II drugs requires careful control of both formulation composition and API properties. While hydrophilic matrix systems based on hypromellose (HPMC) are widely used to control drug release, the interaction between HPMC concentration and API particle size remains a critical formulation challenge. 

Gliclazide, a second-generation sulfonylurea used in the treatment of type 2 diabetes, was selected as a model BCS Class II drug to investigate these effects. For BCS Class II compounds, drug absorption is often limited by the rate of dissolution rather than permeability, making formulation design critical for achieving consistent therapeutic performance. API micronisation is commonly used to increase surface area and enhance dissolution, while HPMC concentration directly impacts gel layer formation and drug release kinetics. Developing a modified-release (MR) gliclazide tablet is particularly challenging because both API particle size and matrix composition can strongly influence the dissolution profile. To investigate these factors, IMCD evaluated the performance of micronised and non-micronised gliclazide in HPMC matrix tablets formulated with varying levels of hypromellose.

Pharmaceutical manufacturers and formulators developing modified (extended or controlled-release) oral solid dosage forms, particularly: 

The study aimed to determine how particle size and polymer concentration affect drug release, providing formulators with practical strategies to optimise modified-release performance for this low dose poorly soluble antidiabetic API. Therefore, formulators would benefit from: