Prolonged-release ciprofloxacin

▲ Prolonged-release ciprofloxacin (ciprofloxacin PR) is a novel oral formulation of the fluoroquinolone antibacterial that allows once-daily administration. The polymeric matrix of the tablet particles swells so that the particles are retained in the fed stomach. The particles erode on contact with gastric acid, releasing approximately 90% of a 500mg ciprofloxacin PR dose at a near constant rate to the upper gastrointestinal tract over a 6-hour period. ▲ The bactericidal activity of ciprofloxacin PR is similar to that of immediate-release ciprofloxacin (ciprofloxacin IR). Both formulations showed similar in vitro activity against common uropathogens, including Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis. In patients with ciprofloxacin-susceptible uncomplicated urinary tract infections, bacterial eradication rates for each of these uropathogens were similar with ciprofloxacin PR or ciprofloxacin IR. ▲ Oral ciprofloxacin PR 500mg once daily produces similar systemic exposure to that of ciprofloxacin IR 250mg twice daily, but the time to maximum plasma concentration is prolonged and the initial peak in drug concentration is higher than with ciprofloxacin IR. A similar pattern is seen in terms of urinary excretion. Other pharmacokinetic parameters are similar to those of ciprofloxacin IR. ▲ In 523 evaluable women with ciprofloxacin-susceptible uncomplicated urinary tract infection, 3 days’ treatment with ciprofloxacin PR 500mg once daily had similar efficacy to ciprofloxacin IR 250mg twice daily. Initial bacterial eradication rates were ≥90% and initial clinical cure rates were ≥86% for either formulation. ▲ Ciprofloxacin PR was well tolerated in clinical trials in women with acute cystitis. Fungal infection (mostly vaginal yeast infection) was the most common adverse event possibly related to ciprofloxacin PR treatment. A tolerability advantage for ciprofloxacin PR over ciprofloxacin IR was seen in terms of nausea and diarrhea, which occurred significantly less often with ciprofloxacin PR.