3.10 Flashcards
Tremendous variability of the skin as much as a _____ ____ patient permeability difference at a given skin site
ten-fold inter(patient)
Features of the skin can vary in different regions of the body especially the ___ can significantly vary from one site to another
SC (Stratum Corneum)
The viable epidermis contains many drug-metabolizing _____
Enzymes such as CYP and esterases
cutaneous first pass effect much less than hepatic
Example of Cutaneous first pass effect include
Nitroglycerin (up to 15-20% can be metabolized in skin)
Example of Cutaneous first pass effect include ____ which undergoes hydrolysis (esterase) to its active metabolite.
Tazarotene (prodrug for psoriasis)
Drug binding can occur where drug can bind to components of the stratum corneum such as the …
proteins and lipids
Drug binding (combine with slow drug passage) can have important implications:
- delay onset of drug action
2. create drug reservoir ( hold onto medication and can prolong drug effects)
SC in premature babies is not fully developed and SC in aged can _____ and become less hydrated
thickens
effects not easily predictable and complicated by changes in dermal microcirculation
The water uptake in the SC can take up to ____% of water (still dead cells)
75
Both the cells and the _____ spaces can take up water leads to swelling and softening of the SC.
interlamellar
_____ of the skin can enhance drug permeation through the skin because of its effect on SC.
Hydration
____ of the skin can be an important consideration in topical drug therapy, as it can increase drug permeation at the site.
Occlusion
blocks transepidermal water loss (TWL), leading to skin hydration at the site of occlusion
____ and ____ drugs are more lipophilic
Nonpolar and nonionized
Properties of the final ______ can have considerable effects on drug permeation: Ability to release the drug and occlude the skin
dosage form
_____ increases hydration and penetration.
Occlusion
_______ are semisolid preparations intended for external application to skin or mucous membranes and classified according to their interaction with water.
Ointment
Four classifications of ointment bases are …
1. Hydrocarbon/ Oleaginous Base (least) 2. Absorption base 3. Emulsion Base -w/o and o/w 4. Water-soluble Base (most)
____ ointment base are insoluble in water they are anhydrous, and incompatible with water.
Hydrocarbon (Oleaginous)
White petrolatum USP…
a highly refined mixture of saturated hydrocarbons (decolorized, e.g. Vaseline)
White Ointment USP…
White petrolatum+ white wax (beeswax)
Less greasy
Most occlusive topical agent because application to the skin, a hydrocarbon base will…
form an adherent, continuous, greasy, water-repellant film