Chapter 183- Principles of Topical Therapy Flashcards
Efficacy of topically applied drug depends on 3 things:
- Whether drug was applied
- Delivery of active molecule by its vehicle
- Inherent potency of active molecule
Factors that affect penetration of drug: (4)
- Soluble drug concentration
- Regional variations in skin barrier properties
- Frequency of application
- Effects of vehicle on barrier function
Primary barrier that limits percutaneous absorption of compounds is
Stratum corneum
Topical therapy involves 3 key steps:
- Topical application
- Percutaneous absorption
- Binding of active molecule to target site
Nonadherence to prescribed medicines in chronic conditions is between ___%
30 to 50%
Low absorption does not necessarily translate into low efficacy.
True or False
True
3 compartment model of skin
- Skin surface
- Stratum corneum
- Viable tissue
Most significant role in determining diffusion of compunds into body
Stratum corneum
When a patient applies a dermatologic preparation, the layer of formulation is ___ .
0.5 to 2 mg/cm2
Matching type
- Diffusion
- Reservoir
- Thermodynamic activity
- Binding
- Resorption
- Evaporation
A. Vehicle
B. Stratum corneum
C. Epidermis
D. Dermis
- B>A
- B
- A
- C> B
- C
- A
Amount of active ingredient that is still in contact with nonvolatile constituents of formulation after latter has been massaged into skin surface
Reservoir
Optimum size of particles for penetration into hair follicles is between ___ nm to a depth of 100 to 500 um
300-600 nm
Several paramaters to consider when selecting a formulation (5)
- Thermodynamic activity of the active ingredient
- Amount of compund that can be incorporated into the formulation
- Stability of formulation
- Partition coefficient of active ingredient between the vehicle and the stratum corneum
- Enhancer activity
Percutaneous absorption is proportional to ___
Thermodynamic activity of the compound
Stratum corneum measures __um
10 - 20 um
Arrange the ff reservoir from highest to lowest
Scalp
Forehead
Calf
Scalp» forehead»_space; calf
Three pentration oathways
Intracellular
Intercellular
Follicular
Nanoparticles are stored ___ times longer in hair follicles than in the stratum corneum
10
Accurate and reproducible measurement of skin barrier activity is
Transepidermal water loss
Transepidermal water loss varies __% by site; __% by day of measurement; and __% amongst individuals
8%
21%
35 to 48%