Prolonged-release ciprofloxacin
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Am J Drug Deliv 2006; 4 (2): 113-120 1175-9038/06/0002-0113/$39.95/0 © 2006 Adis Data Information BV. All rights reserved.
Prolonged-Release Ciprofloxacin Rachel H. Foster and Susan J. Keam Adis International Inc., Yardley, Pennsylvania, USA
Contents Abstract . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 113 1. Drug Delivery System Characteristics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 114 2. Pharmacodynamic Profile . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 115 3. Pharmacokinetic Profile . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 116 4. Therapeutic Efficacy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 117 5. Tolerability . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 118 6. Dosage and Administration . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 119 7. Prolonged-Release Ciprofloxacin: Current Status . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 119
Abstract ▲ 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 ma
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