Table II.
Ingredient (% w/w) | Batch Code | |||||||||
---|---|---|---|---|---|---|---|---|---|---|
B7 | B8 | B9 | B10 | B11 | B12 | B13 | B14 | B15 | B16 | |
Fluconazole | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 |
Ethyl cellulose | 7.5 | 5 | 3 | 7.5 | 5 | 3 | 7.5 | 5 | 3 | 5.25 |
Eudragit® RS100 | 15 | 15 | 15 | 10 | 10 | 10 | 5 | 5 | 5 | 10.6 |
PEG 400 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
Eutectic blend | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 |
Alcohol and acetone blend (q.s.) | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
Tests | Average results (n = 3) | |||||||||
Viscosity (a ± 2.7 cPs) | 128.3 | 92.8 | 70.8 | 69.7 | 48.9 | 38.1 | 52.5 | 34.0 | 23.7 | 52.9 |
Volume of solution delivered upon each actuation (b ± 0.03 ml) | 0.14 | 0.18 | 0.2 | 0.21 | 0.26 | 0.31 | 0.26 | 0.3 | 0.33 | 0.24 |
Spray angle (c ± 0.4o) | 91.5 | 88.2 | 83.8 | 84.2 | 81.8 | 80.6 | 82.6 | 79.8 | 78.7 | 82.6 |
Ex–in vivo film formation timea (d ± 35 sec) | 532 | 435 | 390 | 372 | 328 | 287 | 340 | 282 | 249 | 335 |
Feeling of warmth and subsequent cooling sensationa (e ± 1 min) | 19 | 18 | 17 | 18 | 16 | 15 | 17 | 13 | 13 | 17 |
Appearance of the filma | +++ | ++ | ++ | ++ | ++ | + | ++ | + | + | ++ |
Dermal adhesion and flexibility of the filma | +++ | +++ | +++ | +++ | +++ | +++ | +++ | ++ | ++ | +++ |
Water washabilitya | + | + | ++ | ++ | ++ | ++ | ++ | ++ | ++ | ++ |
aMeasured for placebo batches replacing fluconazole with blend of alcohol and acetone