Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits.
Eur J Ophthalmol
; 16(2): 311-7, 2006.
Article
em En
| MEDLINE
| ID: mdl-16703552
ABSTRACT
PURPOSE:
To evaluate the aqueous humor pharmacokinetics of rufloxacin in rabbits after topical administration of different formulations, and to individuate the ones showing the best pharmacokinetic profile.METHODS:
Six formulations were instilled in rabbit eyes two pH 7.2 suspensions of non-salified rufloxacin base, or zwitterion (RUF), one of which was viscosized with tamarind seed polysaccharide (TSP); two pH 7.2 solutions of RUF obtained using hydroxypropyl-beta-cyclodextrin (CD), one of which was viscosized with TSP; and two pH 5.0 solutions of rufloxacin hydrochloride (RUF-HCl ), one of which was viscosized with TSP. At different times after administration, samples of aqueous humor were withdrawn and analyzed by high-pressure liquid chromatography. The main pharmacokinetic parameters of RUF in the aqueous humor produced by the different formulations were calculated and statistical differences were assessed.RESULTS:
The best results, in terms of aqueous humor bioavailability, were observed with two TSP-viscosized formulations a solution of the hydrochloride (TSP/RUF-HCl) and a suspension of the base (TSP/RUF), followed by the non-viscosized solution of RUF-HCl. The formulations containing CD-solubilized RUF were much less effective.CONCLUSIONS:
The present data confirm the significant availability-enhancing properties of tamarind seed polysaccharide, and indicate that solubilization of RUF with hydroxypropyl-beta-cyclodextrin (CD/RUF) results in decreased drug availability with respect to standard formulations. Two of the TSP-viscosized formulations (RUF suspension and RUF-HCl solution) produced aqueous humor RUF concentrations in the range of activity against Enterobacteriaceae and Pseudomonas aeruginosa, thus warranting further studies on applications of rufloxacin in ocular therapy.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Soluções Oftálmicas
/
Corpo Vítreo
/
Quinolonas
/
Fluoroquinolonas
/
Anti-Infecciosos
Limite:
Animals
Idioma:
En
Revista:
Eur J Ophthalmol
Assunto da revista:
OFTALMOLOGIA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Itália
País de publicação:
EEUU
/
ESTADOS UNIDOS
/
ESTADOS UNIDOS DA AMERICA
/
EUA
/
UNITED STATES
/
UNITED STATES OF AMERICA
/
US
/
USA