TDDS

Question 1

Designed to facilitate the passage of APIs through the skin and into the general circulation

Answer 1

TRANSDERMAL DOSAGE SYSTEMS

Question 2

B. History
* _____________ - 1965
* _____________ (_________) - 1979

Answer 2

B. History
* Stoughton - 1965
* Transderm Scop (Baxter) - 1979

Question 3

C. Comparison to other topical preparations

• Primarily intended for systemic effects
• Is designed with specific systems intended to be attached in the skin

Answer 3

TDDS

Question 4

D. Advantages
* ________________
* ________________
* ________________
* ________________
* ________________

Answer 4

D. Advantages
* Constant dosage can be maintained
* Avoids first pass effect
* Reduced need for active administration
* Noninvasive compared to parenteral therapy
* Can be promptly interrupted by removal

Question 5

E. Disadvantages
* ________________
* ________________
* ________________
* ________________
* ________________
* ________________

Answer 5

E. Disadvantages
* Skin structure poses a barrier on the MW of the drug
* For extremely potent drugs
* Drug should be both lipophilic and hydrophilic
* Can develop contact dermatitis

Question 6

Characteristics and Design Features

• Passes primarily through the ______________
• Penetrates this layer via ______________

Answer 6

• stratum corneum
• passive diffusion

Question 7

A. Parts of TDDS
1. _________________
2. _________________
3. _________________
4. _________________
5. _________________

Answer 7

A. Parts of TDDS
1. Occlusive backing layer
2. Drug Reservoir/Matrix System
3. Rate Controlling Membrane
4. Release Liner
5. Adhesive Layer

Question 8

B. Categories of TDDS
1. __________________
* With polymeric matrix layer

2. __________________
   * Drug reservoir and rate-controlling membrane

Answer 8

B. Categories of TDDS
1. Monolithic Systems
*With polymeric matrix layer

2. Membrane-Controlled Systems
   * Drug reservoir and rate-controlling membrane

Question 9

C. Suitable Drugs for TDDS

1. ________________
   * 100-800 (>400 is the IDEAL)
2. ________________
   * Must be soluble in BOTH lipid and water

Answer 9

1. Molecular Weight
   * 100-800(>400 is the ideal)
2. Solubility and Partition Coefficient

Question 10

C. Suitable Drugs for TDDS

3. _________________
   * Physicochemical attraction should be GREATER to the SKIN than the vehicle
4. _________________
   * Should be in UNIONIZED form before penetrating

Answer 10

3. Attraction to Skin
   * Physicochemical attraction should be greater to the skin than the vehicle
4. lonization
   * Should be in unionized form before penetrating

Question 11

Notable Ingredients/Delivery Methods

A. ______________
* Increases permeability by reversibly damaging or altering
the physicochemical nature of the stratum corneum

1. ______________
2. ______________
3. ______________
4. ______________
5. ______________

Answer 11

A. Chemical Penetration Enhancers (Ingredient)
* Increases permeability by reversibly damaging or altering
the physicochemical nature of the stratum corneum

1. Dimethyl sulfoxide
2. Ethanol
3. Propylene Glycol
4. Glycerin
5. Oleic acid

Question 12

Notable Ingredients/Delivery Methods
B. Delivery Methods

1. lontophoresis
   - delivery of a charged chemical compound across the skin membrane using an electrical field

• include lidocaine, dexamethasone, amino acids, peptides, and insulin, verapamil,and propranolol
• delivered by injection because of their rapid metabolism and poor absorption after oral delivery
• also poorly absorbed by the transdermal route because of their large molecular size and ionic character and the general impenetrability of the skin
• However, this has shown some promise as a means of peptide and protein administration.

Answer 12

1. lontophoresis

Question 13

Notable Ingredients/Delivery Methods
B. Delivery Methods

2. _______________
   - aka high-frequency ultra sound
   - influence the integrity of the stratum corneum and thus affect its penetrability
   - Among the agents examined are hydrocor tisone, lidocaine, and salicylic acid in such formulations as gels, creams, and lotions

Answer 13

2. Sonophoresis

Question 14

Notable Ingredients/Delivery Methods
B. Delivery Methods

3. __________________
   - promising devices for the delivery of drugs and vaccines into or the skin
   - rapidly take up skin interstitial fluid upon skin insertion to form continuous, unblock able, conduits from attached patch-type drug reservoirs to the dermal microcirculation
   - provide the ability for pain-free, safe, and convenient materials delivery through disruption of the outer layers of the skin to access potent immunocompetent cell populations residing within the epidermal/dermal tissues

Answer 14

3. Microneedle Arrays

Question 15

1. _____________
   - Motion Sickness
2. _____________
   - Prophylactic Tx for Angina
3. _____________
   - Smoking Cessation
4. _____________
   - Hypertension

Answer 15

1. Scopolamine (Transderm Scop”)
   - Motion Sickness
2. Nitroglycerin (Deponit®)
   - Prophylactic Tx for Angina
3. Nicotine (Nicoderm”)
   - Smoking Cessation
4. Clonidine (Catapres - TTS®)
   - Hypertension

Question 16

5. _____________
   - Breakthrough Pain
6. _____________
   - ADHD
7. _____________
   - HRT
8. _____________
   - HRT

Answer 16

5. Fentanyl (Duragesic®)
   - Breakthrough Pain
6. Methylphenidate (Daytrana)
   - ADHD
7. Estradiol (Climara)
   - HRT
8. Testosterone (Testoderm®)
   - HRT