Evaluation of an oral prolonged-release antibiotic formulation

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Clinical Pharmacy

Background:

• Cephalexin is a widely used oral antibiotic.
• Optimizing oral antibiotic delivery can improve patient compliance and efficacy.
• Prolonged-release formulations aim to maintain therapeutic drug concentrations over extended periods.

Purpose of the Study:

• To formulate and evaluate an oral prolonged-release tablet of cephalexin.
• To compare the pharmacokinetic profile of the prolonged-release tablet with existing formulations (capsule, intravenous).
• To investigate the relationship between in vitro dissolution and in vivo absorption.

Main Methods:

• Development of an oral prolonged-release cephalexin tablet.
• In vitro dissolution testing of the prolonged-release formulation.
• In vivo pharmacokinetic study in 10 human subjects.
• Comparison of blood levels after oral prolonged-release tablet, oral capsule, and intravenous administration.

Main Results:

• The prolonged-release tablet demonstrated sustained absorption for at least 6 hours.
• Lower peak blood levels were observed with the prolonged-release tablet compared to other forms.
• In vitro dissolution data correlated with in vivo absorption, indicating dissolution rate-limited absorption.
• The prolonged-release formulation exhibited complete bioavailability, similar to the commercial oral capsule.

Conclusions:

• The developed prolonged-release cephalexin tablet is completely bioavailable.
• Drug absorption from the prolonged-release tablet is primarily limited by its dissolution rate.
• This formulation offers a viable alternative for sustained delivery of cephalexin.