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. 2015 Mar 18;172(9):2179–2209. doi: 10.1111/bph.13059

Table 3.

Drug utilization rate and residual amount of drug after use of recently approved, fentanyl and nicotine transdermal patches

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).