Single-Dose SUBA-Itraconazole's Bioavailability in Comparison to Conventional Itraconazole in Fed and Fasted Conditions

Background: Conventional itraconazole (C-ITZ) has inconsistent absorption. SUBA-itraconazole (S-ITZ) demonstrates greater bioavailability than C-ITZ at steady state when taken with food, but no data are available comparing their performance in a fasted state. Objective: The aim of the study was to compare Single-Dose SUBAItraconazole's Bioavailability in Comparison to Conventional Itraconazole in Fed and Fasted Conditions. Methodology: This study was a comparative study which was conducted at Ashiyan Medical College Hospital during Jan’2023 to Jan’24. Sample size was 120. The study was for evaluating the relative bioavailability of a single oral dose of SUBA-itraconazole (S-ITZ) compared to Conventional itraconazole (C-ITZ) capsules when administered under fasted and fed conditions. Ethical clearance was given from the IRB board of the institution. Data were analyzed by SPSS 26.0 version. Results: Out of 120 people, 49 (41%) were male and 71 (59%) were female with male: female ratio of 4:6. The mean (+SD) age was 31.91 (+11.34) years. Service holder were the largest population 50 (41.67%) and 35 (29.17%) were day students. Under the fasted condition, the AUCinf and Cmax ITZ levels for S-ITZ were higher than those for C-ITZ (23 and 62%, respectively). Under fed conditions, SITZ exhibited a 5% lower AUCinf and a 20% lower Cmax compared to C-ITZ. Similar results were observed for OH-ITZ levels and are available in . There was no Tmax difference between formulations under fasted conditions; under fed conditions, the median Tmax for S-ITZ was 2.5 h longer compared to C-ITZ. The geometric mean SITZ/C-ITZ ratios for ITZ levels under fasted conditions were 122.76% (90% CI = 109.72 to 137.34%) and 161.75% (90% CI = 141.40 to 185.02%) for AUCinf and Cmax, respectively. Under fed conditions, the geometric mean S-ITZ/C-ITZ ratios for ITZ were 94.67% (90% CI = 85.35 to 105.01%) and 80.26% (90% CI = 67.61 to 95.27%) for the AUCinf and Cmax, respectively. The geometric mean S-ITZ/C-ITZ ratios for OH-ITZ under fasted conditions were 125.77% (90% CI = 111.40 to 141.99%) and 143.40% (90% CI = 128.19 to 160.42%) for the AUCinf and Cmax, respectively. Under fed conditions, the geometric mean S-ITZ/C-ITZ ratios were 91.86% (90% CI = 79.26 to 106.47%) and 84.25% (90% CI = 73.09 to 97.11%) for the AUCinf and Cmax, respectively. Decreased relative bioavailability in the presence of food was seen for S-ITZ and C-ITZ. The mean AUCinf and Cmax for both ITZ and OH-ITZ were lower (31 and 40% for AUCinf; 57 and 54% for Cmax) when S-ITZ was administered after the study meal; a similar decrease was seen in C-ITZ (10 and 18% for AUCinf; 14 and 22% for Cmax) for ITZ and OH-ITZ, respectively. Conclusion: Conventional itraconazole (C-ITZ) suffers from absorption variability. SUBA-itraconazole (S-ITZ) is more bioavailable than C-ITZ at steady state in a fed condition, but there are no data comparing the two under a fasted state. This study showed that S-ITZ exhibits reduced variability compared to C-ITZ capsules when administered under fasted conditions.