コンプライアンスの向上を目的としたアムホテリシンＢ（ＡＭＰＨ）製剤の剤形の改善 ＡＭＰＨ含有アメ製剤の開発

Abstract

In hematopoietic cell transplantation, amphotericin B (AMPH) syrup is widely used for the prevention of local fungal infections in the intraoral and gastrointestinal tracts. However, the dosage compliance tends to be poor due to its unpleasant taste. We therefore developed a candy preparation for AMPH in order to improve compliance. In this study, we examined the thermostability, stability under storage and the dissolution pattern of AMPH in this preparation. The oral contents of AMPH after administration in the candy preparation were also measured in healthy volunteers. A low calorie sweetener was heated to melt and cooled down to several temperatures (150-190°C). After cooling, AMPH syrup or powder grinding tablets were added (9 mg/ 3 g/piece : the final contents). The results of a thermostability examination show that AMPH was not affected at 150°C, however, it tended to be damaged at higher temperatures. When one piece of AMPH candy preparation was administered for 30 sec to healthy volunteers, the oral concentration of AMPH is higher than 100μg/mL for 10 min, which is more than the minimal inhibitory concentration (MIC) for Candida albicans. Furthermore, the results of a texture test using healthy volunteers indicate that the taste, i.e., flavor, feel on the tongue, etc of the candy preparation made from syrup was superior to that made from powder. These results suggest that a sufficient oral concentration of AMPH to prevent fungal infection was obtained in this candy preparation. As a result, this candy preparation may improve not only the dosage compliance but also the QOL of the patients.