Disposition of polaprezinc (zinc L-carnosine complex) in rat gastrointestinal tract and effect of cimetidine on its adhesion to gastric tissues.
The disposition of polaprezinc in the rat gastrointestinal tract was studied by a double tracer method using [14C]- and [65Zn]polaprezinc. At 0.5 h after oral administration of [14C]-,[65Zn]polaprezinc to rats, the 14C-radioactivity in the gastric contents was comparable with the 65Zn-radioactivity. However, a significant difference was observed in the time course of changes in gastric contents between 14C- and 65Zn-radioactivity over 1 h after administration, indicating that polaprezinc existed in complex form at 0.5 h after administration and was dissociated to L-carnosine and zinc in the gastrointestinal tract as a function of time. The adhesion of zinc to stomach mucosa after oral administration of polaprezinc to rats was significantly increased by treatment with cimetidine. These results suggest that the adhesion of zinc to gastric tissues is increased by inhibiting the dissociation of polaprezinc, and that H2-receptor antagonists, such as cimetidine, may increase anti-ulcer effects of polaprezinc.
Furuta
S
S
Central Research Laboratories, Zeria Pharmaceutical Co. Ltd., Saitama, Japan.
Toyama
S
S
Miwa
M
M
Sano
H
H
D000284:Administration, Oral; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002250:Carbon Radioisotopes; D002336:Carnosine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002927:Cimetidine / Q000008:administration & dosage / Q000494:pharmacology*; D004064:Digestive System / Q000378:metabolism*; D005766:Gastrointestinal Contents / Q000187:drug effects; D007553:Isotope Labeling; D008297:Male; D009942:Organometallic Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013047:Specific Pathogen-Free Organisms; D013054:Spectrophotometry, Atomic; D013055:Spectrophotometry, Infrared; D014018:Tissue Distribution; D017967:Zinc Compounds
D000897:Anti-Ulcer Agents; D002250:Carbon Radioisotopes; D009942:Organometallic Compounds; D017967:Zinc Compounds; C061957:polaprezinc; D002927:Cimetidine; D002336:Carnosine