Table 1.
Initial suspension composition (before spray-drying), theoretical composition of the spray-dried formulation, and ITZ experimental content as determined by HPLC
Suspension | ITZ (% w/v) | TPGS (% w/v) | TPGS (% w/wITZ) | ||||
---|---|---|---|---|---|---|---|
Initial suspension compositions in water/isopropanol (2:1) | |||||||
S1 | 0.33 | 0.017 | 5 | ||||
S2 | 0.33 | 0.033 | 10 | ||||
S3 | 0.5 | 0.025 | 5 | ||||
S4 | 0.5 | 0.050 | 10 | ||||
S5 | 1 | 0.050 | 5 | ||||
S6 | 1 | 0.1 | 10 | ||||
DPI theoretical composition after spray-drying | Experimental ITZ content | ||||||
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Formulation | ITZ (% w/w) | Mannitol (% w/w) | TPGS (% w/w) | NaTau (% w/w) | Mean ITZ content (% wt) | CV (%) | Relative error (%) |
| |||||||
Ca | 32.258 | 64.516 | 3.226 | – | 30.6 | 2.8 | −5.2 |
N1b | 90.91 | – | 9.09 | – | 90.2 | 2.4 | −0.76 |
N2b | 32.258 | 64.516 | 3.226 | – | 34.1 | 3.8 | 5.71 |
N3b,c | 32.154 | 64.309 | 3.215 | 0.322 | 27.4 | 9.4 | −14.9 |
N4b,c | 31.949 | 63.898 | 3.195 | 0.958 | 24.1 | 2.02 | −24.5 |
Notes:
Produced from the initial suspension S6;
produced from the S6 nanosuspension;
NaTau added to the carrier solution before spray-drying.
Abbreviations: CV, coefficient of variation; DPI, dry powder for inhalation; HPLC, high-performance liquid chromatography; ITZ, itraconazole; NaTau, sodium taurocholate; TPGS, tocopherol polyethylene 1000 succinate.