Comparative pharmacokinetic study between lenampicillin, bacampicillin and amoxycillin

Area of Science:

• Pharmacokinetics and Drug Metabolism
• Microbiology and Infectious Diseases

Background:

• Antibiotic efficacy is influenced by absorption, distribution, metabolism, and excretion (ADME) properties.
• Understanding the pharmacokinetic profiles of different ampicillin prodrugs is crucial for optimizing therapeutic outcomes.

Purpose of the Study:

• To compare the serum kinetics and urinary excretion of lenampicillin, bacampicillin, and amoxicillin.
• To evaluate the potential pharmacokinetic advantages of orally administered lenampicillin and bacampicillin over amoxicillin.

Main Methods:

• A crossover study involving six healthy, fasting volunteers.
• Administration of comparable oral doses of lenampicillin, bacampicillin, and amoxicillin.
• Serial blood and urine sampling for 6 and 12 hours, respectively, followed by assay for free ampicillin/amoxicillin concentration using Bacillus subtilis.

Main Results:

• Lenampicillin demonstrated the most rapid time to peak serum concentration (Tmax) and the highest peak serum concentration (Cmax).
• Bacampicillin also showed a more rapid Tmax and higher Cmax compared to amoxicillin.
• Area under the curve (AUC) and total percentage of urinary recovery were similar across all three antibiotics.

Conclusions:

• Lenampicillin and bacampicillin exhibit superior pharmacokinetic profiles, characterized by faster absorption and higher peak serum concentrations, compared to amoxicillin.
• These findings suggest a potential clinical advantage for lenampicillin and bacampicillin in achieving rapid therapeutic drug levels.