Effect of lecithin coating on the pulmonary absorption of furosemide in rats.
The effect of lecithin coating on the pulmonary absorption of furosemide after application by metered dose inhalers (MDI) containing HFA 227 was evaluated in rats. The plasma concentration of furosemide after application of lecithin-coated furosemide was higher than that after application of the un-coated form. Since the disposition in the lung 2 min after application of un-coated furosemide was significantly lower than that after application of the coated form and the adsorption to a polyethylene tube used for the application of the un-coated form was significantly higher than that of the coated form, the higher plasma concentration after application of lecithin-coated furosemide could be partly related to the efficient delivery of the furosemide particles to the lung. The permeation-enhancing effect of the lecithin coating was investigated using Calu-3 cell monolayers. The cumulative amount of furosemide permeated over 2 h from a suspension containing lecithin-coated furosemide through the monolayers was significantly higher than that from a conventional furosemide suspension. This enhancing effect could also contribute to the high plasma concentration of furosemide in rats. The lecithin-coated furosemide will be useful for the formulation of MDI offering high bioavailability.
Saso
Yuko
Y
Hokkaido Pharmaceutical University School of Pharmacy, Japan.
Seki
Toshinobu
T
Fukuchi
Rie
R
Chono
Sumio
S
Morimoto
Kazuhiro
K
D000818:Animals; D018699:Coated Vesicles; D005665:Furosemide / Q000097:blood / Q000493:pharmacokinetics*; D008168:Lung / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D010713:Phosphatidylcholines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D010713:Phosphatidylcholines; D005665:Furosemide