Intravenous Ilaprazole Is More Potent than Oral Ilaprazole Against Gastric Lesions in Rats

• Published in: Digestive diseases and sciences Vol. 59; no. 10; pp. 2417 - 2422
• Main Authors: Yu, Gang, Lu, Xin-Qiang, Su, Rui-Bin, Gong, Ze-Hui, Xie, He-Zhi, Hu, Hai-Tang, Hou, Xue-Mei
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01.10.2014; Springer; Springer Nature B.V
• Subjects: 2-Pyridinylmethylsulfinylbenzimidazoles - administration & dosage; 2-Pyridinylmethylsulfinylbenzimidazoles - therapeutic use; Animals; Anti-Inflammatory Agents, Non-Steroidal - toxicity; Biochemistry; Gastric Acid - metabolism; Gastroenterology; Gastrointestinal Agents - administration & dosage; Gastrointestinal Agents - therapeutic use; Hepatology; Histamine; Histamine - pharmacology; Indomethacin; Indomethacin - toxicity; Male; Medicine; Medicine & Public Health; Oncology; Original Article; Rats; Rats, Sprague-Dawley; Stomach - drug effects; Stomach - metabolism; Stomach - pathology; Stomach Ulcer - drug therapy; Stress, Physiological; Transplant Surgery; Gastroprotection; Intravenous administration; Ilaprazole; Acid secretion; Onset and duration of action
• ISSN: 0163-2116; 1573-2568
• DOI: 10.1007/s10620-014-3187-2

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.