HME-assisted formulation of taste-masked dispersible tablets of cefpodoxime proxetil and roxithromycin

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Pediatric Pharmacology

Background:

• Pediatric antibiotic administration is challenging due to the bitter taste of medications like cefpodoxime proxetil (CP) and roxithromycin (ROX).
• Current formulations (dry suspensions, tablets) and manufacturing methods like lyophilization present issues with taste masking, cost, and time.
• Accurate dosing and patient compliance in children are compromised by unpalatable antibiotic formulations.

Purpose of the Study:

• To mask the bitter taste of CP and ROX using a novel manufacturing technique.
• To ensure solubility and drug release profiles remain comparable to existing marketed formulations.
• To develop a more efficient and cost-effective alternative to lyophilization for pediatric antibiotic preparations.

Main Methods:

• Hot melt extrusion (HME) technology was employed to process CP and ROX with Eudragit E PO polymer.
• Characterization of extrudates included Fourier transform infrared spectroscopy, powder X-ray diffraction, and differential scanning calorimetry.
• The processed drugs were formulated into dispersible tablets and evaluated for in vitro and in vivo taste-masking efficiency.

Main Results:

• Dispersible tablets exhibited comparable dissolution profiles to marketed formulations.
• Taste-masking efficiency was significantly enhanced in the HME-processed tablets compared to marketed CP and ROX tablets.
• In vivo human taste-masking evaluations corroborated the in vitro findings, confirming effective taste suppression.

Conclusions:

• Solvent-free, scalable, and continuous HME technology successfully addresses the bitter taste of CP and ROX.
• HME technology overcomes the disadvantages associated with the conventional lyophilization technique.
• This approach offers a promising solution for improving palatability and adherence of pediatric antibiotics.