Oral sustained delivery of paracetamol from in situ-gelling gellan and sodium alginate formulations.
The purpose of this study was to evaluate the potential for the oral sustained delivery of paracetamol of two formulations with in situ gelling properties. Oral administration of aqueous solutions of either gellan gum (1.0%, w/v) or sodium alginate (1.5%, w/v) containing calcium ions in complexed form resulted in the formation of gel depots in rabbit and rat stomachs as a consequence of the release of the calcium ions in the acidic environment. In vitro studies demonstrated diffusion-controlled release of paracetamol from the gels over a period of 6h. The bioavailability of paracetamol from the gels formed in situ in the stomachs of rabbits following oral administration of the liquid formulations was similar to that of a commercially available suspension containing an identical dose of paracetamol.
Kubo
Wataru
W
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, 061-0293, Hokkaido, Japan.
Miyazaki
Shozo
S
Attwood
David
D
D000082:Acetaminophen / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D000284:Administration, Oral; D000464:Alginates / Q000008:administration & dosage* / Q000737:chemistry; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D004339:Drug Compounding; D005782:Gels; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D008297:Male; D008954:Models, Biological; D011135:Polysaccharides, Bacterial / Q000008:administration & dosage* / Q000737:chemistry; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012212:Rheology; D012995:Solubility; D012996:Solutions
D000464:Alginates; D018712:Analgesics, Non-Narcotic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D006603:Hexuronic Acids; D011135:Polysaccharides, Bacterial; D012996:Solutions; D000082:Acetaminophen; C048288:gellan gum; D020723:Glucuronic Acid