健康成人および出血性潰よう患者におけるＯｍｅｐｒａｚｏｌｅ含有坐剤のバイオアベイラビリティについて 腸溶錠との比較

Abstract

In 1991, we prepared a suppository containing omeprazole as a non-oral dosage form. The therapeutic effect is well recognized by endoscopy after administration to hemorrhagic ulcer patients.We investigated the bioavailability of the suppository compared with the commercial enteric tablet in four healthy volunteers and five hemorrhagic ulcer patients who were extensive metabolizers (EM). In the healthy volunteers, the difference between the area under the serum omeprazole level versus time curve (AUC) after the administration of the suppository and the enteric tablet was not significant. In contrast, in the patients, the AUC of the suppository was lower than that of the enteric tablet, although the difference was not significant. The difference in AUC values observed between volunteers and patients might depend on repeated administration in patients under treatment which has caused saturation of the metabolic enzyme and, hence, increased AUC in EM.These results clearly indicated that the suppository has a therapeutic effect comparable to the commercial enteric tablet. Thus, the suppository is a useful dosage form of omeprazole for the acute hemorrhagic ulcer patient who cannot tolerate oral administration, in Japan as well as in many other countries where non-oral dosage forms are not available.