Table I.
Ingredient (% w/w) | Batch code | |||||
---|---|---|---|---|---|---|
B1 | B2 | B3 | B4 | B5 | B6 | |
Fluconazole | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 |
Ethyl cellulose | 3 | 5 | 7.5 | – | – | – |
Eudragit® RS100 | – | – | – | 5 | 10 | 15 |
PEG 400 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
Eutectic blend | 10 | 10 | 10 | 10 | 10 | 10 |
Alcohol and acetone blend (q.s.) | 100 | 100 | 100 | 100 | 100 | 100 |
Tests | Average results (n = 3) | |||||
Viscosity (a ± 2.7 cPs) | 15.0 | 26.4 | 43.5 | 7.6 | 20.2 | 51.6 |
Volume of solution delivered upon each actuation (b ± 0.03 ml) | 0.32 | 0.30 | 0.26 | 0.39 | 0.31 | 0.24 |
Spray angle (c ± 0.4°) | 78.0 | 79.1 | 81.0 | 76.1 | 78.3 | 82.2 |
Y a1 | 21.07 | 17.07 | 12.55 | 23.44 | 14.12 | 11.73 |
Y b2 | 94 | 115 | 196 | 120 | 160 | 210 |
Ex–in vivo film formation timec (d ± 35 sec) | 130 | 160 | 210 | 110 | 152 | 230 |
Feeling of warmth and subsequent cooling sensationc (e ± 1 min) | 12 | 14 | 15 | 12 | 14 | 16 |
Appearance of the filmc | + | + | ++ | + | + | ++ |
Dermal adhesion and flexibility of the filmc | ++ | ++ | ++ | ++ | +++ | +++ |
Water washabilityc | ++ | ++ | ++ | +++ | +++ | ++ |
a Y 1 is the amount of drug transported (μg) per ml at the end of first hour
b Y 2 is the time (min) required to transport 50% of the drug (t 50%)
cMeasured for placebo batches replacing fluconazole with blend of alcohol and acetone