Effect of formulation factors on in vitro permeation of moxifloxacin from aqueous drops through excised goat, sheep, and buffalo corneas |
| |
Authors: | Pravin Kondiba Pawar Dipak K Majumdar |
| |
Institution: | (1) Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, New Delhi, India |
| |
Abstract: | The purpose of this investigation was to evaluate the effect of formulation factors on in vitro permeation of moxifloxacin
from aqueous drop through freshly excised goat, sheep, and buffalo corneas. Aqueous isotonic ophthalmic solutions of moxifloxacin
hydrochloride of different concentrations (pH 7.2) or 0.5% (wt/vol) solutions of different pH or 0.5% solutions (pH 7.2) containing
different preservatives were made. Permeation characteristics of drug were evaluated by putting 1 mL formulation on freshly
excised cornea (0.50 cm2) fixed between donor and receptor compartments of an all-glass modified Franz diffusion cell and measuring the drug permeated
in the receptor (containing 10 mL bicarbonate ringer at 37°C under stirring) by spectrophotometry at 291 nm, after 120 minutes.
Statistical analysis was done by one-way analysis of variance (ANOVA) followed by Dunnett’s test. Increase in drug concentration
in the formulation resulted in an increase in the quantity permeated but a decrease in percentage permeation. Increase in
pH of the solution from 5.5 to 7.2 increased drug permeation, indicating pH-dependent transport. Compared with control formulation,
moxifloxacin 0.5% (wt/vol) solution (pH 7.2) containing disodium edetate (EDTA) (0.01% wt/vol) produced significantly (P<.05) higher permeation with all the corneas. Formulation with benzyl alcohol significantly (P<.05) increased permeation with buffalo cornea compared with its control. Presence of benzalkonium chloride (BAK) (0.01% wt/vol)
and EDTA (0.01% wt/vol) in the formulation increased permeation to the maximum with all the corneas. The results suggest that
moxifloxacin 0.5% ophthalmic solution (pH 7.2) containing BAK (0.01%) and EDTA (0.01%) provides increased in vitro ocular
availability through goat, sheep, and buffalo corneas.
Published: February 10, 2006
Formerly College of Pharmacy, University of Delhi, Pushp Vihar, Sector III, New Delhi-110017, India |
| |
Keywords: | moxifloxacin concentration pH preservative cornea permeation |
本文献已被 PubMed SpringerLink 等数据库收录! |
|