Intravenous ilaprazole is more potent than oral ilaprazole against gastric lesions in rats.

Abstract

BACKGROUND AND AIMS:

Ilaprazole is a novel proton pump inhibitor that has been marketed as an oral therapy for acid-related diseases in China and Korea. This study aimed to compare the gastroprotective effects of intravenous and enteral ilaprazole in rat models.

METHODS:

The rats were divided into 7-8 groups receiving vehicle, esomeprazole, and different doses of intravenous and enteral ilaprazole. The rats were then exposed to indomethacin (30 mg/kg, i.g.), or water-immersion stress and gastric lesions were examined. The effects of different treatments on histamine (10 μmol/kg/h)-induced acid secretion were also observed.

RESULTS:

Intravenous ilaprazole exhibited high antiulcer activity in a dose-dependent manner. Ilaprazole at a dose of 3 mg/kg decreased ulcer number and index to the same extent as 20 mg/kg esomeprazole. Moreover, the potency of intravenous ilaprazole is superior to that of intragastric ilaprazole. In anesthetized rats, the inhibitory effect of intravenous ilaprazole on histamine-induced acid secretion is faster and longer-lasting than that of intraduodenal ilaprazole.

CONCLUSION:

Intravenous ilaprazole is more potent than oral ilaprazole against indomethacin- or stress-induced gastric lesions, with faster and longer inhibition of acid secretion.

• Authors: Gang Yu, Xin-Qiang Lu, Rui-Bin Su, Ze-Hui Gong, He-Zhi Xie, Hai-Tang Hu, Xue-Mei Hou
• Journal: Digestive diseases and sciences (Dig Dis Sci) Vol. 59 Issue 10 Pg. 2417-22 (Oct 2014) ISSN: 1573-2568 [Electronic] United States
• PMID: 24801687 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 2-Pyridinylmethylsulfinylbenzimidazoles
• Anti-Inflammatory Agents, Non-Steroidal
• Gastrointestinal Agents
• ilaprazole
• Histamine
• Indomethacin

Topics

• 2-Pyridinylmethylsulfinylbenzimidazoles (administration & dosage, therapeutic use)
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (toxicity)
• Gastric Acid (metabolism)
• Gastric Mucosa (metabolism)
• Gastrointestinal Agents (administration & dosage, therapeutic use)
• Histamine (pharmacology)
• Indomethacin (toxicity)
• Male
• Rats
• Rats, Sprague-Dawley
• Stomach (drug effects, pathology)
• Stomach Ulcer (drug therapy)
• Stress, Physiological