Biopharmaceutic evaluation of furosemide as a potential candidate for a modified release peroral dosage form.
An attempt was made to evaluate some of the criteria for developing a modified release peroral dosage form for furosemide which has a poor bioavailability when given in the conventional peroral dosage forms. The pathway of absorption for furosemide was studied ex vivo employing the Wilson-Wiseman test. Passive absorption was found to be the predominant mechanism of transport across the ileum of the guinea pig followed by active transport to the extent of about 17%. The in situ procedure to study the extent of absorption of furosemide from the various sites in the lumen of the gastrointestinal tract of the rat indicated the stomach to be the major site of absorption followed by the duodenum. It is hence postulated that due to the site-specificity and mechanism of absorption a peroral modified release dosage form having a longer gastric residence time could possibly increase the bioavailability of furosemide.
Ritschel
W A
WA
University of Cincinnati Medical Center, Division of Pharmaceutics and Drug Delivery Systems, OH.
Menon
A
A
Sakr
A
A
D000284:Administration, Oral; D000818:Animals; D001665:Binding Sites; D001682:Biological Availability; D001693:Biological Transport, Active; D004064:Digestive System / Q000378:metabolism; D004304:Dosage Forms; D005665:Furosemide / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D004304:Dosage Forms; D005665:Furosemide