[DOSAGE FORMS] Transdermal Drug Delivery System

a. Transdermal patches

[Transdermal Delivery Systems]
Controlled release drug delivery system or patches that allow the passage of drugs from the skin to the systemic circulation.

a. Transdermal patches
b. Implants
c. Suppositories
d. Ointments

• Constant dosage can be maintained

• Avoid first pass effect

• Reduced need for active administration

• Non-invasive compared to parenteral therapy

• Can be promptly interrupted by removal

[Transdermal Delivery Systems]

Advantages of Transdermal Patches [5]

• Skin structure poses a barrier on the MW of the drug (<500 Da)

• Usually reserved for extremely potent (<10mg) drugs except Nicotine (21mg)

• Drug should have adequate solubility in both lipophilic and aqueous environments

• Development of contact dermatitis

  • Remedy: alternate site of application

[Transdermal Delivery Systems]

Disadvantages of Transdermal Patches [4]

• Monolithic Systems

• Membrane-Controlled Systems

Types of Transdermal Delivery Systems [2]

a. Monolithic Systems

[Types of Transdermal Delivery Systems]

Incorporate a drug matrix layer (polymer with dispersed drug) beneath the backing layer

a. Monolithic Systems

b. Membrane-Controlled Systems

a. Monolithic Systems

[Types of Transdermal Delivery Systems]

Can be cut

a. Monolithic Systems

b. Membrane-Controlled Systems

b. Membrane-Controlled Systems

[Types of Transdermal Delivery Systems]

Contain a drug reservoir or pouch (liquid or gel) and a rate-controlling membrane

a. Monolithic Systems

b. Membrane-Controlled Systems

b. Membrane-Controlled Systems

[Types of Transdermal Delivery Systems]

Advantage: The drug is saturated, therefore release rate is constant

a. Monolithic Systems

b. Membrane-Controlled Systems

• Occlusive backing film

• Drug reservoir / Matrix system

• Rate-controlling membrane

• Adhesive layer

• Release liner / layer

Components of Transdermal Delivery System [5]

Occlusive backing film

[Components of Transdermal Delivery System]

Protects the patch from the outer environment

a. Occlusive backing film

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

a. Occlusive backing film

[Components of Transdermal Delivery System]

Prevents drug loss and water loss

a. Occlusive backing film

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

b. Drug reservoir / Matrix system

[Components of Transdermal Delivery System]

Stores and releases the drug at the skin site

a. Occlusive backing film

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

c. Rate-controlling membrane

[Components of Transdermal Delivery System]

Controls drug release from the reservoir in membrane-controlled systems

a. Occlusive backing film

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

d. Adhesive layer

[Components of Transdermal Delivery System]

Ensures contact of the patch to the skina. Occlusive backing film

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

e. Release liner / layer

[Components of Transdermal Delivery System]

Protects the drug during storage and is removed prior to use

b. Drug reservoir / Matrix system

c. Rate-controlling membrane

d. Adhesive layer

e. Release liner / layer

Scopolamine (Transderm Scop)

[Example of Transdermal Delivery System]

1st TDDS developed

a. Scopolamine (Transderm Scop®)
b. Clonidine (Catapres-TTS®)
c. Nicotine (Nicoderm®)
d. Nitroglycerin (Deponit®)

a. Motion sickness

[Example of Transdermal Delivery System]

Scopolamine (Transderm Scop®) is used for _____

a. Motion sickness

b. Hypertension

c. Diabetes

d. Schizophrenia

a. Behind the ear every 3 days

[Example of Transdermal Delivery System]

Scopolamine (Transderm Scop®) is applied:

a. Behind the ear every 3 days
b. On the upper chest once daily
c. On the hip area every 7 days
d. On the lower back once weekly

Nitroglycerin (Deponit®)

[Example of Transdermal Delivery System]

Used for prophylactic tx of angina

a. Scopolamine (Transderm Scop®)
b. Clonidine (Catapres-TTS®)
c. Nicotine (Nicoderm®)
d. Nitroglycerin (Deponit®)

b. Upper part of the body once daily

[Example of Transdermal Delivery System]

Nitroglycerin (Deponit®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Hip area 2 hours before effect is needed
d. Upper part of the body every 7 days

b. Clonidine (Catapres-TTS®)

[Example of Transdermal Delivery System]

1 st TDDS for HTN

a. Scopolamine (Transderm Scop®)
b. Clonidine (Catapres-TTS®)
c. Nicotine (Nicoderm®)
d. Nitroglycerin (Deponit®)

c. Upper part of the body every 7 days

[Example of Transdermal Delivery System]

Clonidine (Catapres-TTS®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Upper part of the body every 7 days
d. Hip area 2 hours before effect is needed

c. Nicotine (Nicoderm®)

[Example of Transdermal Delivery System]

Contains 21mg and used for smoking cessation

a. Scopolamine (Transderm Scop®)
b. Clonidine (Catapres-TTS®)
c. Nicotine (Nicoderm®)
d. Nitroglycerin (Deponit®)

b. Upper part of the body once daily

[Example of Transdermal Delivery System]

Nicotine (Nicoderm®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Upper part of the body every 7 days
d. Hip area 2 hours before effect is needed

b. Fentanyl (Duragesic®)

[Example of Transdermal Delivery System]

Used for breakthrough pain.

a. Nicotine (Nicoderm®)
b. Fentanyl (Duragesic®)
c. Methylphenidate (Daytrana®)
d. Estradiol (Climara®)

c. Upper part of the body every 3 days

[Example of Transdermal Delivery System]

Fentanyl (Duragesic®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Upper part of the body every 3 days
d. Hip area 2 hours before effect is needed

c. Methylphenidate (Daytrana®)

[Example of Transdermal Delivery System]

Used for attention deficit hyperactivity disorder (ADHD) in children.

a. Nicotine (Nicoderm®)
b. Fentanyl (Duragesic®)
c. Methylphenidate (Daytrana®)
d. Estradiol (Climara®)

b. 9 hours

[Example of Transdermal Delivery System]

Methylphenidate (Daytrana®) lasts only for _____ hours.

a. 6 hours
b. 9 hours
c. 12 hours
d. 24 hours

d. Hip area 2 hours before an effect is needed

[Example of Transdermal Delivery System]

Methylphenidate (Daytrana®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Upper part of the body every 7 days
d. Hip area 2 hours before an effect is needed

a. Estradiol (Climara®)

[Example of Transdermal Delivery System]

Used for Hormone Replacement Therapy including:

• Primary ovarian failure

• Female hypogonadism

• Vasomotor symptoms associated with menopause

• Atrophic vaginitis

• Kraurosis Valvae (Briesky Disease)

a. Estradiol (Climara®)

b. Methylphenidate (Daytrana®)

c. Nicotine (Nicoderm®)

d. Nitroglycerin (Deponit®)

c. Lower abdomen or upper buttocks twice weekly

[Example of Transdermal Delivery System]

Estradiol (Climara®) is applied:

a. Behind the ear every 3 days
b. Upper part of the body once daily
c. Lower abdomen or upper buttocks twice weekly
d. Hip area 2 hours before effect is needed

c. Both a and b

• Androderm®

• Testoderm®

[Example of Transdermal Delivery System]

Testosterone transdermal patches used for hormone replacement therapy (HRT).

a. Androderm®
b. Testoderm®
c. Both a and b
d. Neither a nor b

c. Upper part of the body or thighs

[Example of Transdermal Delivery System]

Androderm® is applied to:

a. Scrotum

b. Behind the ear

c. Upper part of the body or thighs

d. Hip area

c. Scrotum

[Example of Transdermal Delivery System]

Testoderm® is applied to:

a. Upper part of the body

b. Thighs

c. Scrotum

d. Lower abdomen

a. Contraceptive System (OrthoEvra®)

[Example of Transdermal Delivery System]

Contains:

• Norelgestromin

• Ethinyl estradiol

a. Contraceptive System (OrthoEvra®)
b. Hormone replacement (Climara®)
c. Testosterone patch (Androderm®)
d. ADHD treatment (Daytrana®)

a. Contraceptive System (OrthoEvra®)

[Example of Transdermal Delivery System]

Combination contraceptive patch with a contact surface area of 20 cm²

a. Contraceptive System (OrthoEvra®)
b. Hormone replacement (Climara®)
c. Testosterone patch (Androderm®)
d. ADHD treatment (Daytrana®)

• Site of application should be rotated

• Cut or dry shave first the hair before placing the patch

• It may be left on when showering, bathing,or swimming

• Use of skin lotion should be avoided at the application site

[Transdermal Delivery System]

Applications for Transdermal Delivery System [4]