Abstract
The influence of pharmaceutical properties on the gastric lesions induced by AD-1590 (AD), a non-steroidal anti-inflammatory drug, was investigated in rats.AD, indomethacin (IM) and aspirin (ASA) were orally administered in powder or suspension form to fasted rats. It was found that the gastric ulcerogenic activity of the powder was stronger than that of the suspension in all cases. Thus, the gastric ulcerogenic activity was influenced by the dosage form.Solid preparations of AD having various pharmaceutical properties were orally administered to fasted rats, and it was found that the gastric ulceration caused by AD was associated with the residence time of preparations in the stomach rather than the maximum plasma concentration (Cmax) or extent of bioavailiability (area under the plasma concentration-time curve). Preparations having a long residence time caused gastric ulcers. The gastric ulceration caused by AD might be eliminated by improvement of dissolution and disintegration properties of the drug preparation and by suitable control of gastric emptying. Thus, it appears to be possible to evaluate the influence of pharmaceutical properties on gastric lesions induced by non-steroidal anti-inflammatory drugs (NSAIDs) by using small laboratory animals such as rats.
