Localization of [14C]clarithromycin in rat gastric tissue when administered with lansoprazole and amoxicillin

Abstract

After oral and intravenous administration of [14C]clarithromycin to rats, c. 60-70% of the radioactivity in the gastric tissue was found to be distributed in the mucosal layer. Co-administration of lansoprazole and amoxicillin had no apparent effect on this distribution pattern of [14C]clarithromycin. The amount of unchanged [14C]clarithromycin in gastric contents increased with co-administration of lansoprazole and amoxicillin. Microautoradiograms of the gastric mucosa showed that [14C]clarithromycin was highly distributed in the mucous layer and in surface epithelial cells following oral administration. Homogeneous distribution of radioactivity was evident in the fundic gland. With iv administration, [14C]clarithromycin seemed to be secreted by both secreting cells in the gland base and surface epithelial cells.

Mucoadhesive and muco-penetrating delivery systems for eradication of helicobacter pylori

“…[17] Because of poor penetration power of antibiotics across the gastric mucus membrane, incomplete eradication results. [11,12] The stability of commonly used antibiotics of triple therapy is another reason for treatment failure, which is not more than 3-4 h in gastric environment. [38] The most important issue in management of H. pylori is increased instances of antibiotic's resistance.…”

“…But poor stability of antibiotics in acidic environment and poor permeation of antibiotics across the mucus layer cause incomplete eradication and systemic side effects leading to patient noncompliance. [11,12] To sort out these problems, several research investigations on the gastro-retentive drug delivery systems like floating formulations, mucoadhesive drug delivery system, pH-sensitive gel system had been carried out for increasing the gastric residence and local concentration of drug at H. pylori-infected site. These studies indicated the benefit of targeting drug to the gastric mucosal layer by reducing the dose of antibiotic therapy as well as increased patient's compliance.…”