In vivo evaluation of a colon-specific drug delivery system: an absorption study of theophylline from capsules coated with azo polymers in rats.
Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from capsules coated with the azo polymers was examined in the proximal part of the small intestine and the cecum of male Wistar rats. The capsules were surgically inserted in the region of interest. The plasma concentration of the drug was higher when the capsules were inserted in the cecum as compared to the small intestine. The appearance of theophylline in the plasma when capsules were administered in the small intestine can be attributed to simple diffusion of the drug through the swollen polymer coating. Release and absorption from the cecum is the combined results of diffusion and degradation of the azo polymer coatings by bacterial azo reductase.
Van den Mooter
G
G
Lab. Galenische en Klinische farmacie, K. U. Leuven, Belgium.
Samyn
C
C
Kinget
R
R
D000818:Animals; D001391:Azo Compounds / Q000737:chemistry; D001682:Biological Availability; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D003106:Colon / Q000378:metabolism*; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013806:Theophylline / Q000008:administration & dosage* / Q000493:pharmacokinetics
D001391:Azo Compounds; D002214:Capsules; D013806:Theophylline