In situ gelling pectin formulations for oral sustained delivery of paracetamol.
The purpose of this study was to evaluate the potential of a pectin formulation with in situ gelling properties for the oral sustained delivery of paracetamol (acetaminophen). The formulations consisted of dilute aqueous solutions (1% to 2% w/v) of low methoxy pectin containing calcium ions in complexed form, which on release in the acidic environment of the stomach caused gelation of the pectin. In vitro studies demonstrated diffusion-controlled release of paracetamol from the gels over a period of 6 h. A bioavailability of approximately 96% of that of a paracetamol solution could be achieved from gels containing an identical dose of drug formed in situ in the stomachs of rats, with appreciably lower peak plasma levels and a sustained release of drug over a period of at least 6 h.
Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, Hokkaido, Japan
Wataru
W
Kubo
Yasuhiro
Y
Konno
Shozo
S
Miyazaki
David
D
Attwood
D000082:Acetaminophen / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D019355:Calcium Citrate / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005079:Excipients / Q000737:chemistry*; D005782:Gels; D066298:In Vitro Techniques; D008297:Male; D010368:Pectins / Q000737:chemistry*; D019999:Pharmaceutical Solutions; D051381:Rats; D017208:Rats, Wistar; D014867:Water
D003692:Delayed-Action Preparations; D005079:Excipients; D005782:Gels; D019999:Pharmaceutical Solutions; D014867:Water; D000082:Acetaminophen; D010368:Pectins; D019355:Calcium Citrate