Pharm Flashcards
majority of drug penetration through the stratum corneum occurs through the inter/transcellular route
intercellular
intercellular entrance of drugs through the stratum corneum normally allows __ _ molecules to diffuse. ___ in this layer are highly hydrophobic and can act as a ___
small hydrophobic
lipids
reservoir for lipid soluble drugs
rate of absorption/flux of a drug to the skin is governed by ___ which =
Fick’s law
J =KpCv - permeability coefficient x concn of drug in vehicle
Kp = (diffusion coefficient x partition coeff) / length of diffusion pathway
In relation to topical drug absorption Km =
equilibrium of the drug in the stratum corneum relative to its solubility in the vehicle
lipophilic drug in a lipophilic base = ___ absorption
modest - drug prefers to stay in vehicle
Lipophilic drug in a hydrophilic base = ___ absorption
large amount of absorption
lots in circulation
Hydrophilic drug in hydrophilic base = ___ absorption
negligible
hydrophilic drug in lipophilic base = ___ absorption
limited
___ in a drug’s vehicle can enhance solubility and increase absorption
excipient
_____ in transdermal patch increases duration of drug absorption and can provide steady state delivery because __
excess non-dissolved drug
dissolved drug that is used up is replaced by undissolved drug
Physical and chemical factors that increase partitioning of a topical drug
hydrate skin by occlusion ( cream/clingfilm etc)
excipients increase hydrophobic drugs solubility
topical steroids diffuse across the ___ and combine with __ in cytoplasm which cause ___ to disocciate to activate their receptor that enters the nucleus via ___. receptor molecules assemble into ___ and bind to __ which turn transcription on/off
plasma membrane GRalpha nuclear receptors inhibitory heat shock protein importins homodimers GRE (glucocorticoid response elements)
most suitable drug characteristics for transdermal delivery
low molecular weight
moderately lipophilic
potent
relatively brief t1/2
a semisolid emulsion of oil in water with emulsifier and preservative
cream
pros of using cream as a drug base
high H20 content
non-greasy
cool skin
semi-solid oil/grease with no preservative
ointment
properties of ointment as a drug base
occlusive and emollient, restrict transepidermal H2O loss
BUT are greasy
suspension/solution of drug in liquid
lotion