Taste masking microspheres for orally disintegrating tablets

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Taste masking is crucial for patient compliance, especially for bitter active pharmaceutical ingredients.
• Orally disintegrating tablets (ODTs) offer convenient administration but can present taste-related challenges.
• Microsphere technology provides a potential solution for taste masking in oral dosage forms.

Purpose of the Study:

• To evaluate the efficacy of spray-dried microspheres for taste masking famotidine in ODTs.
• To optimize the spray-drying process for producing effective taste-masking microspheres.
• To assess the impact of microspheres on drug bioavailability and release.

Main Methods:

• Famotidine-loaded microspheres were prepared using spray drying.
• The spray-drying process was optimized using a central composite design.
• Microspheres were incorporated into ODTs, and their taste, encapsulation efficiency, particle size, and moisture content were evaluated.
• In vitro and in vivo studies were conducted to assess drug release and bioavailability.

Main Results:

• Optimal spray-drying parameters (34mg/ml solid concentration, 7ml/min feed rate) yielded microspheres with <10µm mean diameter and <4% moisture.
• Encapsulation efficiency ranged from 37.59% to 61.56%.
• Human volunteer studies showed significant taste improvement, and rat studies confirmed no significant decrease in bioavailability or release.

Conclusions:

• Spray-dried microspheres are an effective strategy for taste masking bitter drugs in ODTs.
• The optimized formulation enhances palatability without compromising pharmacokinetic properties.
• This approach holds promise for improving the acceptability of oral medications.