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Pharmacokinetics of acyclovir in rabbit skin after i.v.-bolus, ointment, and iontophoretic administrations.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2004 Apr 15; Vol. 274 (1-2), pp. 201-11. - Publication Year :
- 2004
-
Abstract
- The aim of this study was to characterize and compare the pharmacokinetics of acyclovir (ACV) in skin and plasma after iontophoresis, i.v.-bolus, and ointment administrations in rabbit. On five occasions, each separated by at least 1-week washout, rabbits received a 10 mg/kg dose of ACV as i.v.-bolus, ACV iontophoresis for 1 h at different current densities (100, 200, 300 microA/cm2) or a commercially available ointment for two hours. Blood samples were collected serially up to 6 h. Skin ACV concentrations were monitored via microdialysis using linear microdialysis probes (1 cm window). Cathodic iontophoresis was performed using commercially available patches (10 cm2 contact area). Following i.v.-bolus, C(max) in skin occurred with a delay of 38 +/- 4 min compared with plasma. No quantifiable concentration of ACV was detected in the skin on passive drug delivery. Following iontophoresis, skin exposure to ACV was 40, 22, and 11% of that following i.v.-bolus. Conversely, systemic exposure to ACV was negligible and plasma concentrations were below the limit of quantification at any time-point. In skin dialysate, C(max), AUC, and half-life increased with current density. During ointment application, ACV in dermis was detectable only for the first 30 min thereafter ACV skin concentrations were below the LOQ (30 ng/ml).
Details
- Language :
- English
- ISSN :
- 0378-5173
- Volume :
- 274
- Issue :
- 1-2
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 15072796
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2004.01.024