Pharmacotechnical Evaluation by SeDeM Expert System to Develop Orodispersible Tablets.

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Nevirapine, a BCS Class II drug, exhibits poor solubility, limiting its therapeutic efficacy.
• Solid dispersions offer a promising strategy to enhance the solubility and bioavailability of poorly soluble drugs.
• The Sediment Delivery Model (SeDeM) system provides a quantitative assessment of powder properties relevant to direct compression.

Purpose of the Study:

• To enhance the solubility of nevirapine using solid dispersions.
• To evaluate the direct compressibility of excipients and solid dispersions using the SeDeM system.
• To formulate and characterize orodispersible tablets (ODTs) for improved drug delivery.

Main Methods:

• Solid dispersions of nevirapine were prepared by solvent evaporation.
• Micromeritic properties of excipients and solid dispersions were analyzed using the SeDeM system.
• Orodispersible tablets (ODTs) were formulated by direct compression and evaluated for critical quality attributes.

Main Results:

• Solid dispersions with Eudragit S100 significantly increased nevirapine solubility (6-10 fold) in a pH-dependent manner.
• SeDeM analysis identified excipients with favorable micromeritic properties for direct compression and highlighted deficiencies in others.
• Formulated ODTs exhibited rapid drug release, with 40% released within the first minute in simulated salivary fluid.

Conclusions:

• The SeDeM system is a valuable tool for predicting and optimizing powder compressibility for direct compression.
• Solid dispersions effectively enhance the solubility of nevirapine, facilitating the development of ODTs.
• The study demonstrates a successful approach to formulating ODTs with enhanced solubility and rapid drug release using direct compression.