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Winter P1 > Pharm 734 Final > Flashcards

Pharm 734 Final Flashcards

(47 cards)

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1
Q

Topical Drug Delivery: Action, Uses

A

Local Action Only

  1. Protect injured areas of skin
  2. Hydrate skin
  3. Local therapeutic effect
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2
Q

Layers of Skin Anatomy

A

Epidermis
Dermis
Hyperdermis

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3
Q

Epidermis Features

A 
0.006 to 0.008mm thick
Stratum Corneum (outermost layer, 10-20% moisture)
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4
Q

Dermis Features

A

3-5mm thick

matrix of connective tissues, woven fibrous proteins, nerves, blood vessels

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5
Q

Hyperdermis Features

A

Subcutaneous Tissue

Mechanical cushion, thermal barrier, energy storage

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6
Q

Skin Appendages

A

Hair Follicles
Sweat Glands
Sebaceous Glands
Nails

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7
Q

Drug Travel Path from Skin (Cream, Gel, Lotion, Patch etc)

A

Skin Surface –> Stratum corneum –> Viable Epidermis –> Dermis –> Blood Circulation

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8
Q

Epidermis Layers and maturation

A

Stratum Basale (bottom, Hydrophilic)
Stratum Spinosum
Stratum Granulosum
Stratum Corneum (Top, Hydrophobic)

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9
Q

Protective Function of Skin

A
  1. Microbiological Barrier
  2. Chemical Barrier
  3. Radiation Barrier
  4. Heat/Temperature Regulation
  5. Immune response
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10
Q

Targeted Region of Topical Drug Delivery

A 
Surface Treatment (e.g. insect repellant, sunscreen)
Stratum Corneum (Emolient, Keratosis)
Skin Appendage (Acne, Antibiotics, Antiperspirant)
Viable Epidermis/Dermis (antihistamine, anesthetics)
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11
Q

Skin Problems at Different Regions of skin

A 
Stratum Corneum (Psoriasis, Dry Skin)
Viable Epidermis (Eczema)
Dermal/Epidermal interface (warts)
Dermis (scarring)
Hair Follicle/Sebaceous/Sweat gland (Hirsutism, Acne, Heatrash)
Other (Fungal/Athlete's foot)
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12
Q

Topical Dosage forms

A

Semi-Solids
Solids
Liquids

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13
Q

Semi Solid topical forms

A 
Ointments
Creams
Pastes
Gels
Jelly
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14
Q

Solid topical forms

A

Powders
Aerosol
Plaster

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15
Q

Liquid topical forms

A 
Solutions
Emulsions
Suspensions
lotions
Liniments
Aerosols
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16
Q

Advantages of Topical Drug Delivery

A

High drug concentration at site of application
Low risk of systemic side effects
Non-Invasive
Easy to Use

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17
Q

Disadvantages of Topical Drug Delivery

A 
Contact time for drug is limited
Ointments and creams are messy to use
Potential for systemic absorption
formulations can cause skin irritation
Difficult to measure exact dose
Rubbing, Heat, Exercise inc systemic absorption
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18
Q

Semi Solid Dosage Forms (applications)

A 
Intended for topical application
Medicated or non-medicated
Emolient (softens skin, no absorption)
Protective (protects skin against environment)
Vehicles
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19
Q

Antipruritics

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A

Relieve Itching of Skin (menthol, Camphor, coal tar)

20
Q

Keratolytics

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A

Remove/soften the thickened or scaly stratum corneum

21
Q

Antieczematous agents

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A

Assist in removal and treatment of oozing and vesicular excretions.

22
Q

Antiparasitics

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A

Destroy or inhibit living infestations

23
Q

Antiseptics and Antibiotics

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A

Bacteriostatic, bactericidal, fungistatic, Fungicidal

24
Q

Antiseborrheics

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A

Reduce discharge from sebaceous glands and remove symptoms

25
Types of ointment bases
hydrocarbon (oleaginous) absorption bases emulsions (W/O and O/W) Water-miscible bases
26
Gels are:
3D network of inorganic molecules and large organic molecules in a liquid Water-washable Drug is dispersed/dissolved in water or a water/ethanol mixture in gel Rate of drug release is usually fast Sunscreen gels, gel for anti-fungal and anti-inflammatory
27
Pastes are:
A large proportion of solid material than ointment, not less than 20% solid Less greasy than ointment Pastes are stiffer than ointments Good for absorption of secretions Not good for application to hairy areas due to stiffness Not water washable
28
Creams and Lotions are:
Homogenous semi-solid preparations consisting of opaque emulsion systems. Consistency and rhelogical properties depend on the type of emulsion. Creams can contain one or more medicinal agents dissolved in W/O or O/W O/W cream and water = Lotion
29
What physiological factors affect drug penetration
Thickness of SC | Condition of SC
30
What drugs can cross skin? (how can drug diffusion be increased?)
Small hydrophilic polar molecules Small hydrophobic molecules (Decreasing MW, Occluding the skin, damage to skin)
31
What is required for Drugs to penetrate SC?
Drug dissolved in base Drug diffuse to surface of skin Drug must partition into SC Drug must diffuse to site of action in epidermis
32
How can Drug penetration be increased?
Higher Drug Concentration Thicker Layer of Ointment Larger Surface Area
33
What is Levigation?
The process of reducing the particle size of a solid by triturating it with small amount of liquid or melted base to wet the solid
34
What are Humectants?
Ingredients that attract water (Glycerin, PEG, urea, lactic acid) Pulls water into SC from deeper layers Prevents drying of o/w creams/lotions
35
What are Astringents?
Substances that control oozing, discharge or bleeding Coagulate Protein, acts as protective coat, allows new cells to regenerate underneath Used for "weeping" wounds (E.g. Gallic Acid, Aluminum Sulfate)
36
Topical Patches (NOT transdermal)
Intended for local action at skin | E.g. Diclofenac
37
Nails
100x thicker than SC very impermeable to topical drugs Difficulty in retaining formulation on nail Occlusive covering helps penetration
38
Transermal Drug Delivery Systems
Facilitate the passage of therapeutic quantities of drug substance through skin into general circulation for systemic effect
39
TDDS Advantages
``` Bypass Hepatic "First Pass" Bypass GI Incompatibility Reduced Side Effects Greater Compliance Minimize Inter/Intra patient variation Terminate therapy by removing patch Etc. ```
40
TDDS Disadvantages
permeation through skin limited Skin irritation patches uncomfortable May not be economical
41
TDDS Drug properties
- Drugs w/ Short Hal-life - Proper lipophilicity/hydrophilicity - low molecular weight (~100-500 Da) - Potent drug (narrow therapeutic window) - should not bind extensively to skin - should not be irritating to skin - clinical necessity for steady state delivery - drugs can be subject to high 1st pass
42
Layers of Epidermis
Stratum Corneum Stratum Granulosum Stratum Spinosum Stratum Basale
43
Epidermis Notable Facts
- Turnover ~28 days (14 days dehydrate, 14 days shed) - Avascular - Stratum Corneum most important barrier
44
Dermis notable features
- Rich blood supply, lymphatic vessels and nerve endings - Drugs quickly diffuse - Collagen fibers (structural strength) - Elastin FIbers (Elasticity)
45
Fick's Law of diffusion in TDDS
``` J = Pe x Co J = Flux, movement of mass/area/time ```
46
TDDS LogP target zone
1-4 (partition coeffecient)
47
Construction of TDDS
1. Impermeable Backing membrane (occlusive) 2. Drug Reservoir/ Matrix 3. Rate-controlling membrane 4. Adhesive Layer 5. Protective Liner

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