Table 3.
Drug (Trade name, year of FDA approval) | Patch design | Dose and size of patch – Delivery rate | Drug utilization rate (%)a | Residual amount of drug in the patch (mg)b | Patch area activity (%·cm−2)c |
---|---|---|---|---|---|
Methylphenidate (Daytrana®, 2006) | DIA | 27.5 mg in 12.5 cm2 – 1.1 mg·h−1 | 36 | 17.6 | 2.9 |
41.3 mg in 18.75 cm2 – 1.6 mg·h−1 | 34.9 | 26.9 | 1.9 | ||
55 mg in 25 cm2 – 2.2 mg·h−1 | 36 | 35.2 | 1.4 | ||
82.5 mg in 37.5 cm2 – 3.3 mg·h−1 | 36 | 52.8 | 1 | ||
Selegiline (Emsam®, 2006) | DIA | 20 mg in 20 cm2 – 6 mg per 24 h | 30 | 14 | 1.5 |
30 mg in 30 cm2 – 9 mg per 24 h | 30 | 21 | 1 | ||
40 mg in 40 cm2 – 12 mg per 24 h | 30 | 28 | 0.75 | ||
Rivastigmine (Exelon®, 2007) | Matrix | 9 mg in 5 cm2 – 4.6 mg per 24 h | 51.1 | 4.4 | 10.2 |
18 mg in 10 cm2 – 9.5 mg per 24 h | 52.8 | 8.5 | 5.3 | ||
27 mg in 15 cm2 – 13.3 mg per 24 h | 49.3 | 13.7 | 3.3 | ||
Rotigotine (Neupro®, 2007) | DIA | 2.25 mg in 5 cm2 – 1 mg per 24 h | 44.4 | 1.25 | 8.9 |
4.5 mg in 10 cm2 – 2 mg per 24 h | 44.4 | 2.5 | 4.4 | ||
6.75 mg in 15 cm2 – 3 mg per 24 h | 44.4 | 3.75 | 3 | ||
9 mg in 20 cm2 – 4 mg per 24 h | 44.4 | 5 | 2.2 | ||
13.5 mg in 30 cm2 – 6 mg per 24 h | 44.4 | 7.5 | 1.5 | ||
18 mg in 40 cm2 – 8 mg per 24 h | 44.4 | 10 | 1.1 | ||
Granisetron (Sancuso®, 2008) | DIA | 34.3 mg in 52 cm2 – 3.1 mg per 24 h | 63.3 | 12.6 | 1.2 |
Buprenorphine (Butrans®, 2010) | DIA | 5 mg in 6.25 cm2 – 5 μg·h−1 | 16.8 | 4.26 | 2.7 |
7.5 mg in 7.5 cm2 – 7.5 μg·h−1 | 16.8 | 6.24 | 2.2 | ||
10 mg in 12.5 cm2 – 10 μg·h−1 | 16.8 | 8.32 | 1.3 | ||
15 mg in 18.75 cm2 – 15 μg·h−1 | 16.8 | 12.48 | 0.9 | ||
20 mg in 25 cm2 – 20 μg·h−1 | 16.8 | 16.64 | 0.7 | ||
Oestradiol (Minivelle®, 2012) | DIA | 0.62 mg in 2.48 cm2 – 0.0375 mg·day−1 | 21.17 | 0.49 | 8.5 |
0.83 mg in 3.30 cm2 – 0.05 mg·day−1 | 21.1 | 0.66 | 6.4 | ||
1.24 mg in 4.95 cm2 – 0.075 mg·day−1 | 21.17 | 0.98 | 4.3 | ||
1.65 mg in 6.6 cm2 – 0.1 mg·day−1 | 21.21 | 1.3 | 3.2 | ||
Fentanyl (Duragesic®, 1990) discontinued | Reservoir/Membrane | 1.25 mg in 5 cm2 – 12.5 μg·h−1 | 72 | 0.35 | 14.4 |
2.5 mg in 10 cm2 – 25 μg·h−1 | 72 | 0.7 | 7.2 | ||
5 mg in 20 cm2 – 50 μg·h−1 | 72 | 1.4 | 3.6 | ||
7.5 mg in 30 cm2 – 75 μg·h−1 | 72 | 2.1 | 2.4 | ||
10 mg in 40 cm2 – 100 μg·h−1 | 72 | 2.8 | 1.8 | ||
Fentanyl (Mylan FTS, 2005) | DIA | 1.28 mg in 3.13 cm2 – 12.5 μg·h−1 | 70.3 | 0.38 | 22.5 |
2.55 mg in 6.25 cm2 – 25 μg·h−1 | 70.6 | 0.75 | 11.3 | ||
5.10 mg in 12.5 cm2 – 50 μg·h−1 | 70.6 | 1.5 | 5.6 | ||
7.65 mg in 18.75 cm2 – 75 μg·h−1 | 70.6 | 2.25 | 3.8 | ||
10.20 mg in 25 cm2 – 100 μg·h−1 | 70.6 | 3 | 2.8 | ||
Fentanyl (Lavipharm Labs FTS, 2006) | DIA | 1.375 mg in 5 cm2 – 12 μg·h−1 | 62.8 | 0.51 | 12.6 |
2.75 mg in 10 cm2 – 25 μg·h−1 | 65.4 | 0.95 | 6.5 | ||
5.5 mg in 20 cm2 – 50 μg·h−1 | 65.4 | 1.9 | 3.3 | ||
8.25 mg in 30 cm2 – 75 μg·h−1 | 65.4 | 2.85 | 2.2 | ||
11.0 mg in 40 cm2 – 100 μg·h−1 | 65.4 | 3.8 | 1.6 | ||
Fentanyl (Par Pharm FTS, 2007) | Reservoir/Membrane | 2.5 mg in 10 cm2 – 25 μg·h−1 | 72 | 0.7 | 7.2 |
5 mg in 20 cm2 – 50 μg·h−1 | 72 | 1.4 | 3.6 | ||
7.5 mg in 30 cm2 – 75 μg·h−1 | 72 | 2.1 | 2.4 | ||
10 mg in 40 cm2 – 100 μg·h−1 | 72 | 2.8 | 1.8 | ||
Fentanyl (Watson FTS, 2007) | Reservoir/Membrane | 2.5 mg in 10 cm2 – 25 μg·h−1 | 72 | 0.7 | 7.2 |
5 mg in 20 cm2 – 50 μg·h−1 | 72 | 1.4 | 3.6 | ||
7.5 mg in 30 cm2 – 75 μg·h−1 | 72 | 2.1 | 2.4 | ||
10 mg in 40 cm2 – 100 μg·h−1 | 72 | 2.8 | 1.8 | ||
Fentanyl (Aveva FTS, 2008) | DIA | 2.76 mg in 10.7 cm2 – 25 μg·h−1 | 65.2 | 0.96 | 6.1 |
5.52 mg in 21.4 cm2 – 50 μg·h−1 | 65.2 | 1.92 | 3 | ||
8.28 mg in 32.1 cm2 – 75 μg·h−1 | 65.2 | 2.88 | 2 | ||
11.04 mg in 42.8 cm2 – 100 μg·h−1 | 65.2 | 3.84 | 1.5 | ||
Fentanyl (Duragesic®, 2009) | DIA | 2.1 mg in 5.25 cm2 – 12.5 μg·h−1 | 42.9 | 1.2 | 8.2 |
4.2 mg in 10.5 cm2 – 25 μg·h−1 | 42.9 | 2.4 | 4.1 | ||
8.4 mg in 21 cm2 – 50 μg·h−1 | 42.9 | 4.8 | 2 | ||
12.6 mg in 31.5 cm2 – 75 μg·h−1 | 42.9 | 7.2 | 1.4 | ||
16.8 mg in 42 cm2 – 100 μg·h | 42.9 | 9.6 | 1 | ||
Fentanyl (Noven TTS, 2009) discontinued | DIA | 2.55 mg in 19 cm2 – 25 μg·h−1 | 70.6 | 0.75 | 3.7 |
5.10 mg in 38 cm2 – 50 μg·h−1 | 70.6 | 1.5 | 1.9 | ||
7.65 mg in 57 cm2 – 75 μg·h−1 | 70.6 | 2.25 | 1.2 | ||
10.20 mg in 76 cm2 – 100 μg·h−1 | 70.6 | 3 | 0.9 | ||
Fentanyl (Mallinckrodt FTS, 2011) | Reservoir/Membrane | 2.75 mg in 7.8 cm2 – 25 μg·h−1 | 65.5 | 0.95 | 8.4 |
5.50 mg in 15.6 cm2 – 50 μg·h−1 | 65.5 | 1.9 | 4.2 | ||
8.25 mg in 23.4 cm2 – 75 μg·h−1 | 65.5 | 2.85 | 2.8 | ||
11.0 mg in 31.2 cm2 – 100 μg·h−1 | 65.5 | 3.8 | 2.1 | ||
Nicotine (Nicoderm CQ®, 1991) | Reservoir/Matrix | 36 mg in 7 cm2 – 7 mg per 24 h | 19.4 | 29 | 2.8 |
75 mg in 15 cm2 – 14 mg per 24 h | 18.7 | 61 | 1.2 | ||
114 mg in 22 cm2 – 21 mg per 24 h | 18.4 | 93 | 0.8 | ||
Nicotine (Habitrol®, 1991) | Matrix | 17.5 mg in 10 cm2 – 7 mg per 24 h | 40 | 10.5 | 4 |
35 mg in 20 cm2 – 14 mg per 24 h | 40 | 21 | 2 | ||
52.5 mg in 30 cm2 – 21 mg per 24 h | 40 | 31.5 | 1.3 | ||
Nicotine (Prostep®, 1992) discontinued | Matrix | 15 mg in 24 (3.5) cm2 – 11 mg per 24 h | 73.3 | 4 | 20.9 |
30 mg in 32 (7) cm2 – 22 mg per 24 h | 73.3 | 8 | 10.5 | ||
Nicotine (Nicotrol®, 1992) discontinued | DIA | 8.3 mg in 10 cm2 – 5 mg per 16 h | 60.2 | 3.3 | 6 |
16.6 mg in 20 cm2 – 10 mg per 16 h | 60.2 | 6.6 | 3 | ||
24.9 mg in 30 cm2 – 15 mg per 16 h | 60.2 | 9.9 | 2 |
For instance, the rivastigmine transdermal patch (Exelon) dosage strength 4.6 mg per 24 h, application time 24 h, patch size (active surface) 5 cm2, overall amount of drug substance incorporated into the patch 9 mg. Drug utilization = 4.6 mg; drug utilization rate = 4.6/9 ≈ 50%; residual amount = 9 − 4.6 = 4.4 mg; patch area activity = 50/5 ≈ 10%·cm−2. When the patch has to be applied twice weekly (every 3–4 days), t = 3.5 days is considered for calculation.
aDrug utilization rate (%) = (delivery rate × duration of application)/drug content. bResidual amount (mg) = drug content − drug utilization. cPatch area activity (%·cm−2) = drug utilization rate/patch size − ‘it is a measure of the formulation's intrinsic capability to release drug substance from the patch in vivo and as such a surrogate measurement of thermodynamic activity’ (EMEA, 2012).