MAYER M, MULFORD D, WITT G; Interscience Conference on Antimicrobial Agents and Chemotherapy.
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2000 Sep 17-20; 40: 20.
TAP Holdings Inc., Deerfield, IL
BACKGROUND: Cefditoren (CDTR) is an advanced generation oral cephalosporin which exhibits potent antibacterial activity against both Gram-negative and Gram-positive bacteria. The assessment of antibiotic concentrations in skin blister fluid is a commonly used experimental model to predict concentrations in tissues, and the ability of an antibiotic to control bacterial infections in peripheral tissues. A clinical trial was designed to evaluate the transfer of CDTR into blister fluid.METHODS: In a Phase I study, 12 subjects received a single 400 mg oral dose of CDTR as cefditoren pivoxil approximately 12 hours after non-inflammatory (vacuum suction-induced on the back) and inflammatory (cantharidin-induced on the forearm) blisters were raised.RESULTS: CDTR concentrations in blister fluid did not parallel those in plasma and were temporally different. A comparison of blister fluid to plasma AUC values indicated that the penetration of CDTR into blister fluid was 40-56%. Since concentrations of CDTR remained relatively high at 8 and 12 hours in blister fluid, and since the terminal elimination rate constant for CDTR in blister fluid could not been determined, it is likely that the total exposure of CDTR in blister fluid, and thus penetration, were underestimated. Mean pharmacokinetic results for CDTR are presented below. [table: see text]. Conclusion: Based on a comparison of blister fluid to plasma AUC values, the penetration of CDTR into blister fluid was at least 40-56%.KEYWORDS: Blister fluid; Cefditoren; Pharmacokinetics
Publication Types:
Keywords:
- Anti-Bacterial Agents
- Area Under Curve
- Bacterial Infections
- Blister
- Cantharidin
- Cephalosporins
- cefditoren
- cefditoren pivoxil
- pharmacokinetics
Other ID:
UI: 102247044
From Meeting Abstracts