Conditions in which Transdermal Patches are not used

The use of transdermal patch is not suitable when:

(1)Cure for acute pain is required. (2) Where rapid dose titration is required. (3) Where
requirement of dose is equal to or less then 30 mg/24 hrs.

Marketed Products of Transdermal Patches:

Brand Name Drug Manufacturer Indications

NicotinellR Nicotine Novartis Pharmacological smoking
cessation
MatrifenR Fentanyl Nycomed Pain relief patch
Ortho EvraTM Norelgostromin/ ORTHO-McNEIL Postmenstrual syndrome
Ethinyl Estradiol
NuPatch 100 Diclofenac Zydus Cadila Anti Inflammatory
diethylamine
NeuproR Rigotine UCB and Schwarz Pharma early-stage idiopathic
Parkinson’s disease
Alora Estradiol TheraTech/Proctol and Gamble Postmenstrual syndrome

NicodermR Nicotine Alza/GlaxoSmithKline Smoking cessation

Estraderm Estradiol Alza/Norvatis Postmenstrual syndrome

Climara Estradiol 3M Pharmaceuticals/Berlex labs Postmenstrual syndrome

Androderm Testosterone TheraTech/GlaxoSmithKline Hypogonadism in males

Nitrodisc Nitroglycerin Roberts Pharmaceuticals Angina pectoris

Transderm- Scopolamine Alza/Norvatis Motion sickness

ScopR

Nuvelle TS Estrogen/Proge Ethical Holdings/Schering Hormone replacement

sterone therapy

Deponit Nitroglycerin Schwarz-Pharma Angina pectoris

Nitro-dur Nitroglycerin Key Pharmaceuticals

Angina pectoris

Catapres TTSR Clonidine Alza/Boehinger Ingelheim

Hypertension
FemPatch Estradiol Parke-Davis Postmenstrual syndrome

Minitran Nitroglycerin 3M Pharmaceuticals Angina pectoris

Climaderm Estradiol Ethical Holdings/Wyeth-Ayerest Postmenstrual
syndrome

DuragesicR Fentanyl Alza/Janssen Pharmaceutical Moderate/severe

pain

Estraderm Estradiol Alza/Norvatis Postmenstrual

syndrome

Fematrix Estrogen Ethical Holdings/Solvay Postmenstrual

Healthcare Ltd. syndrome

Transderm- Nitroglycerin Alza/Norvatis Angina pectoris

NitroR

Testoderm TTSR Testosterone Alza Hypogonadism in males

OxytrolR oxybutynin Watson Pharma Overactive bladder

Prostep Nicotine Elan Corp./Lederle Labs Smoking cessation

Factors affecting transdermal bioavaibility

Two major factors affect the bioavaibility of the drug via transdermal routes:
(1)Physiological factors (2) Formulation factors
Physiological factors include
(1)Stratum corneum layer of the skin (2) Anatomic site of application on the body (3) Skin
condition and disease (4) Age of the patient (5) Skin metabolism (6) Desquamation (peeling or
flaking of the surface of the skin) (7) Skin irritation and sensitization (7) Race
Formulation factors include
(1)Physical chemistry of transport (2) Vehicles and membrane used (3) Penetration enhancers
used (4) Method of application (5) Device used
Care taken while applying transdermal patch
(1)The part of the skin where the patch is to be applied should be properly cleaned. (2) Patch
should not be cut because cutting the patch destroys the drug delivery system. (3) Before applying
a new patch it should me made sure that the old patch is removed from the site. (4) Care should
be taken while applying or removing the patch because anyone handling the patch can absorb the
drug from the patch. (5) The patch should be applied accurately to the site of administration.

Types of Transdermal Patch

1. Single-layer Drug-in-Adhesive
The adhesive layer of this system also contains the drug. In this type of patch the adhesive layer
not only serves to adhere the various layers together, along with the entire system to the skin, but
is also responsible for the releasing of the drug. The adhesive layer is surrounded by a temporary
liner and a backing.

2. Multi-layer Drug-in-Adhesive
The multi-layer drug-in adhesive patch is similar to the single-layer system in that both adhesive
layers are also responsible for the releasing of the drug. The multi-layer system is different
however that it adds another layer of drug-in-adhesive, usually separated by a membrane (but not
in all cases). This patch also has a temporary liner-layer and a permanent backing.

3. Reservoir
Unlike the Single-layer and Multi-layer Drug-in-adhesive systems the reservoir transdermal system
has a separate drug layer. The drug layer is a liquid compartment containing a drug solution or
suspension separated by the adhesive layer. This patch is also backed by the backing layer. In this
type of system the rate of release is zero order.

4. Matrix
The Matrix system has a drug layer of a semisolid matrix containing a drug solution or suspension.
The adhesive layer in this patch surrounds the drug layer partially overlaying it.

5. Vapour Patch
In this type of patch the adhesive layer not only serves to adhere the various layers together but
also to release vapour. The vapour patches are new on the market and they release essential oils
for up to 6 hours. The vapours patches release essential oils and are used in cases of decongestion
mainly. Other vapour patches on the market are controller vapour patches that improve the quality
of sleep. Vapour patches that reduce the quantity of cigarettes that one smokes in a month are
also available on the market.

Drugs used in the Transdermal Patch25

(1) Nicotine: to quit tobacco smoking
(2) Fentanyl: analgesic for severe pain
(3) Estrogen: menopause and osteoporosis
(4) Nitroglycerin: angina
(5) Lidocaine: peripheral pain of shingles (herpes zoster). Recent developments expanded their
use to the delivery of hormonal contraceptives, antidepressants and even pain killers and
stimulants for Attention Deficit Hyperactivity Disorder/ADHD.

Recent research done in the field:

Many research works have been and are few are going on in this field. Few of the latest research
done in the field of transdermal patches are stated below:
Pain-free diabetic monitoring using transdermal patches
The first prototype patch measures about 1 cm2 and is made using polymers and thin metallic
films. The 5×5 sampling array can be clearly seen, as well as their metallic interconnections. When
the seal is compromised, the interstitial fluid, and the biomolecules contained therein, becomes
accessible on the skin surface. Utilizing micro-heating elements integrated into the structural layer
of the patch closest to the skin surface, a high-temperature heat pulse can be applied locally,
breaching the stratum corneum. During this ablation process, the skin surface experiences
temperatures of 130°C for 30ms duration. The temperature diminishes rapidly from the skin
surface and neither the living tissue nor the nerve endings are affected.
This painless and bloodless process results in disruption of a 40–50μm diameter region of the
dead skin layer, approximately the size of a hair follicle, allowing the interstitial fluid to interact
with the patch's electrode sites.

Testosterone Transdermal Patch System in Young Women with Spontaneous

Premature Ovarian Failure

In premenopausal women, the daily testosterone production is approximately 300 µg, of which
approximately half is derived from the ovaries and half from the adrenal glands. Young women
with spontaneous premature ovarian failure (sPOF) may have lower androgen levels, compared
with normal ovulatory women. Testosterone transdermal patch (TTP) was designed to deliver the
normal ovarian production rate of testosterone. The addition of TTP to cyclic E2/MPA therapy in
women with sPOF produced mean free testosterone levels that approximate the upper limit of
normal.

Transdermal Patch of Oxybutynin used in overactive Bladder

The product is a transdermal patch containing Oxybutynin HCl and is approved in US under the
brand name of Oxytrol and in Europe under the brand name of Kentera. OXYTROL is a thin,
flexible and clear patch that is applied to the abdomen, hip or buttock twice weekly and provides
continuous and consistent delivery of oxybutynin over a three to four day interval. OXYTROL offers
OAB patient’s continuous effective bladder control with some of the side effects, such as dry
mouth and constipation encountered with and oral formulation. In most patients these side effects
however are not a troublesome.

Transdermal Patch (Ortho Evra™)

The patch is 4.5 square centimeters in size and has three layers: the inner release liner which
should be removed before application, a layer containing hormones, and an outer polyester
protective layer. The patch contains 6 milligram of progestin, Norelgestromin 0.75 milligram of
Ethinyle Estradiol. The patch is applied on the skin through which the hormones are absorbed in
order to provide continuous flow of hormones during menstrual cycle. The patch is marketed by
Ortho McNeil Pharmaceutical with the brand name Ortho Evra.

Rotigotine transdermal patch

The rotigotine transdermal patch is used for symptom control in Parkinson’s disease. The patches
are effective in reducing the symptoms of early Parkinson’s disease, and in reducing “off” time in
advanced Parkinson’s disease. It is available in market under the brand name of NeuproR.
TRANSDERMAL LECTURE

Additional info for different transdermal patches

Transderm Nitro (Nitroglycerin) is a transdermal systems which allows the drug to come out all at
once

Estraderm Patch is an estrogen hormone. It works by replacing natural estrogens in a woman who
can no longer produce enough estrogen
 Estraderm transdermal patch changed for t wice a week

Deponit (Nitroglycerin) is use in the Prophylaxis of angina pectoris. Long-term treatment of CHD
 Deponit is a transdermal delivery system contains drug in the adhesive backing

Nitrodur system is Transdermal Infusion System (Nitroglycerin by Key Pharmaceutical)

 .It contains the active ingredient glyceryl trinitrate Nitro-Dur is used to prevent angina, but
is not for the relief of a sudden attack of angina

Nitro disc (Nitroglycerin) 5 & 10

 The Nitrodisc pad incorporates a patented Microseal Drug Delivery'" system consisting of a
solid, nitroglycerin-impregnated polymer bonded to a flexible, non-sensitizing adhesive
bandage, lt is designed to be applied topically.
 Nitrodisc provides constant and controlled drug delivery over a uniform skin surface area
for 24 hours.
 Nitrodisc is available in two strengths that release either 5 mg or 10 mg of nitroglycerin
during a 24-hour period. The 5 mg/24 hr system contains 16 mg nitroglycerin over an 8
cm2 releasing surface.
 The 10 mg/24 hr system contains 32 mg nitroglycerin over a 16 cm2 releasing surface

Catapress TTS
 CATAPRES-TTS is a transdermal system providing continuous systemic delivery of clonidine
for 7 days at an approximately constant rate. Clonidine is a centrally acting alpha-agonist
hypotensive agent.
 CATAPRES-TTS transdermal therapeutic system is a multi-layered film, 0.2 mm thick,
containing clonidine as the active agent.
 The system areas are 3.5 cm2 (CATAPRES-TTS-1), 7.0 cm2 (CATAPRES-TTS-2) and 10.5
cm2 (CATAPRES-TTS-3) and the amount of drug released is directly proportional to the
area