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

Table 1.

Physicochemical, pharmacokinetic and safety data for currently marketed transdermal drugs

Drug	MW^a (Da)	MP (°C)^a Unionized	log P^b	S_aq (mg·mL⁻¹)^a Unionized (25°C)	Cl (L·h⁻¹) (70 kg)	t_1/2 (h)	Oral F (%)	Target plasma level (ng·mL⁻¹)	Estimated J_skin required (μg·h⁻¹)	In vivo J_skin (μg·cm⁻²·h⁻¹)^a″	Equivalent maximum hourly dose (μg·h⁻¹)^a‴	Safety margin = max dose per h/in vivo J_skin
Buprenorphine	468	209	3.8	0.047, 0.008^h (32°C)	77 i.v.^a′, 55 i.m.^b′	3 i.v.^a′, 28 s.l.^a′, 19 bc^a′, 26 t.d.^b′	51 s.l.^a′, 28 bc^a′	>0.1^c′	7.7	0.8	70.8	∼100
Clonidine	230	130	2.7	0.17, 13.58ⁱ	15^d′	8–13 i.v.^d′, 12–16 i.v.^e′, 20 t.d.^e′	95^d′	0.2–2^d′	3–30	1.2	12.5	∼10
Oestradiol	272	173–179	4.2	0.003, 0.003^j (30°C), 0.0015 1^k (25°C)	600–800^f′	∼1 p.o.^g′	5^h′	0.04–0.06^i′	24–48	0.2^b″, 0.17^c″, 0.14^d″, 0.12^e″, 0.42^f″, 0.18^g″, 0.63^h″, 0.23^i″, 0.09^j″	4.2	∼20
Ethinyl oestradiol	296	141–146	4.3	0.039, 0.0092^k (25°C)	70 p.o.^j′	7.7 p.o.^j′, 17 t.d.^k′	55^h′	0.025–0.075^l′	1.75–5.25	0.07	0.8	∼10
Fentanyl	337	83–84	3.9	0.15, 0.2^j (30°C), 0.2^l (25°C)	27–75^m′	3–12 i.v.^m′, 20–27 t.d.^m′	50 o.t.^n′	1–3^o′	27–225	2.4	100	∼40
Granisetron	312	152–154^c	2.6	0.017	33–76^p′	4–6 i.v.^p′, 36 t.d.^p′	60^q′	3.9 (t.d. mean C_max)^p′	129–296	2.5	129	∼50
Levonorgestrel	312	235–237	3.8	0.017	5.7 p.o.^j′	19.3 p.o.^j′, 28 t.d.^r′	94^h′	0.17 (t.d. C_ss)^r′	1	0.03	–	–
Methylphenidate	233	74–75, liquid	2.1	1.8	12(d); 21(l) (children 30 kg)^s′	1.5–5 p.o. (children)^s′	22(d); 5(l)^s′	5–15^t′	60–315	88	1250	∼15
Nicotine	162	−79, liquid	1.1	62, 1085ⁱ (30°C)	77^u′	2 i.v.^u′	20–45^v′	5–30^w′	385–2310	40^k″, 31^l″, 69^m″, 29^n″	875	∼20
Nitroglycerin (glyceryl trinitrate)	227	13, liquid	1	0.66, 1.3^j (30°C)	216–3270^x′	0.03–0.05 p.o.^x′	<1^y′	0.02–0.4^z′	4.32–1308	20^o″, 30^p″	833	∼30
Norelgestromin	327	110–130	3.67 (pred)	0.0043	–	28 t.d.^k′	–	0.6–1.2^l′	–	0.31	6.25	∼20
Norethindrone acetate (norethisterone acetate)	341	161–162	3.2	0.0065	20.6^aa′	34.8 p.o.^aa′, 6–8 t.d.^ab′	60^h′	0.5–0.8^ab′	10.3–16.5	0.65	10.4	∼20
Oxybutynin	358	56–58^d	4.3	0.0093	10–64^ac′	2 i.v.^ad′, 7–8 t.d.^ad′	6^ad′	0.5–3^ae′	5–192	4.2	162.5	∼40
Rivastigmine	250	Oil at 25°C^e	2.3	25	108^af′	1.3–2 p.o.^ag′, 3.4 t.d.^ag′	36^af′	2.5–20 (t.d. mean C_max)^ah′	270–2160	39	396	∼10
Rotigotine	316	75–77^f	4.7	0.017	600^ai′	7 t.d.^ai′	–	0.4–2^aj′	240–1200	8.3	250	∼30
Scopolamine (hyoscine)	303	55, liquid	0.8	1.8, 75^j (30°C)	65–121^ak′	1–5 p.o.^ak′	4–27^ak′	>0.05^al′	3.25–6.05	5.6	210^b‴	∼40
Selegiline (deprenyl)	187	Liquid at 25°C^g	2.7	0.73	84^am′	9–15 p.o.^an′, 15–25 t.d.^am′	4^an′	2^ao′	168	12.5	500	∼40
Testosterone	288	155	3.6	0.02, 0.02ⁱ (25°C)	41^ap′	0.17–1.7^aq′	7^ar′	3–10.5^aq′	123–430.5	13.9	417	∼30

bc, buccal; Cl, total body clearance; d, dextro isomer; F, oral bioavailability; i.m., intramuscular; i.v., intravenous; J_skin, skin flux; l, levo isomer; log P, log octanol–water partition coefficient; MP, melting point of the unionized form; MW, molecular weight; o.t., transmuscosal; p.o., per oral; S_aq, aqueous solubility of the unionized form; s.l., sublingual; t_1/2, elimination half-life; t.d., transdermal.

^aSci Finder Scholar, 2014. ^bChambers Fox, 2014. ^cGafni et al., 2008. ^dTang et al., 2008. ^eChiang et al., 2009. ^fKrivonos and Weisman, 2013. ^gGovil and Weimann, 2006. ^hRoy et al., 1994. ⁱMagnusson et al., 2004. ^jMichaels et al., 1975. ^kShareef et al., 2006. ^lRoy and Flynn, 1988.

^a′Kuhlman et al., 1996. ^b′Butrans® PI. c′Sittl et al., 2003. ^d′Lowenthal et al., 1988. ^e′Catrapres-TTS® PI. ^f′Cleary, 1993. ^g′Estraderm® PI. ^h′Fotherby, 1996. ^i′Good et al., 1985. ^j′Kanarkowski et al., 1988. ^k′Ortho Evra® PI. ^l′Abrams et al., 2002. ^m′Duragesic® PI. ^n′Actiq® PI. ^o′Duthie et al., 1988. ^p′Sancuso® PI. ^q′Kytril® PI. ^r′Climara Pro® PI. ^s′Ritalin LA® PI. ^t′Greenhill et al., 2001. ^u′Benowitz et al., 1982. ^v′Hukkanen et al., 2005. ^w′Bannon et al., 1994. ^x′Bogaert, 1987. ^y′Bauer and Seifert, 2005. ^z′Noonan and Benet, 1986.

^aa′Singh et al., 1979. ^ab′Combipatch® PI. ^ac′Douchamps et al., 1988. ^ad′Oxytrol® PI. ^ae′Lee et al., 1995. ^af′Exelon® capsules PI. ^ag′Lefèvre et al., 2008. ^ah′Frank et al., 2014. ^ai′Neupro® PI. ^aj′Lauterbach et al., 2002. ^ak′Guay, 2003. ^al′Nachum et al., 2006. ^am′Emsam® PI. ^an′Azzaro et al., 2007. ^ao′Kolli et al., 2010. ^ap′Horton et al., 1965. ^aq′Axiron® PI. ^ar′Tauber et al., 1986.

^a″In vivo J_skin is calculated by dividing the labelled dose rate by the patch size (active area). ^b″Estraderm. ^c″Climara®. ^d″Vivelle®. ^e″Alora®. ^f″Vivelle-Dot®. ^g″Menostar®.

^h″Minivelle®. ^i″Combipatch®. ^j″Climara Pro® . ^k″Nicoderm CQ®. ^l″Nicorette®. ^m″Nicorette® Invisi patch®. ^n″Habitrol®. ^o″Nitro-Dur®. ^p″Minitran®.

^a‴Maximum systemic daily dose (Watkinson, 2012) divided by 24 and multiplied by 1000 to express as μg·h⁻¹. ^b‴Maximum systemic daily dose from Drugs.com (Drugs, 2014).