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Drew 924 > 4_3TopTransderm2 > Flashcards

4_3TopTransderm2 Flashcards

1
Q

At what Km is Pe best?

A

10^0.3

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2
Q

Describe how Pe is related to Kow.

A

high Pe directly correlates with Kow up to a point

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3
Q

What factors does the Potts and Guy Equation evaluate?

A

MW and Kow

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4
Q

What factors does the Abraham Equation take into account?

A

H-donating ability; H-accepting ability; hydrophobic area

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5
Q

Describe the relative importance of MW and Kow.

A

Kow more important than MW

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6
Q

Describe the relative importance of H-donating, hydrophobic region and H-accepting abilities.

A

accepting > V > donating

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7
Q

With what does the hydrophobic region of a drug correlate?

A

Pe

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8
Q

With what does the MW of a drug correlate?

A

diffusivity

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9
Q

What is the purpose of the Hadgraft and Pugh Equation?

A

compares functional groups’ relative contributions to Pe

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10
Q

Why is a ceramide headgroup so polar?

A

3 OH and 1 amide

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11
Q

What are the 3 general methods for enhancing transport rate?

A

1) prodrug; 2) permeation-enhanced vehicle modification; 3) solubility-enhanced vehicle modification

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12
Q

What functions are most commonly added with prodrugs?

A

esters

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13
Q

What factors beside MW affect diffusivity for a prodrug?

A

1) solubility, 2) enzyme affinity for prodrug

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14
Q

Why are prodrugs beneficial in transport?

A

decrease H-bonding and increase Kow

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15
Q

What are the 3 methods for permeation-enhanced vehicle modification?

A

1) occlusive dressings; 2) surfactants; 3) high concentration organic co-solvents

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16
Q

What are the disadvantages to permeation-enhanced vehicle modification?

A

1) irritation; 2) inter-subject variability; 3) animal models (source of data) more sensitive than humans

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17
Q

How do surfactants work?

A

disrupt H-bonding or lipid chain packing

18
Q

What are ADRs for surfactants?

A

irritation

19
Q

How does the special co-solvent DMSO work?

A

solvates lipid polar heads in aqueous region

20
Q

How does the special co-solvent azone work?

A

inserts between lipid chains in lipid region

21
Q

What are examples of surfactants?

A

1) DMSO, 2) sodium dodecyl sulfate, 3) oleic acid, 4) azone

22
Q

How do surfactants differ from co-solvents?

A

larger alkyl chain and amphiphilic

23
Q

How do co-solvents work?

A

1) extract lipid from SC to make porous; 2) swells lipid membranes to decrease viscosity

24
Q

What are examples of high-concentration organic co-solvents?

A

1) DMSO, 2) dimethyl formamide, 3) propylene glycol, 4) EtOH, 5) N,N-dimethyl acetamide, 6) N-methyl-2-pyrrolidone; 7) 2-pyrrolidone

25
Q

How do co-solvents differ from surfactants?

A

low MW, H-bonding group, few carbons

26
Q

What is the enhancement factor equation?

A

flux in presence of promotor / flux in absence

27
Q

How is solubility-enhanced vehicle modification achieved?

A

1) pH, 2) liposomes/SLNs, 3) supersaturation with co-solvents

28
Q

What are the methods for achieving supersaturation with cosolvents?

A

1) solvent evaporation, 2) co-solvents, 3) complexation

29
Q

When can changing pH to enhance solubility be done?

A

when compound is ionizable; can increase patch dose and drug stability

30
Q

What are ADRs for pH modification?

A

skin irritation

31
Q

Describe the structure of an SLN?

A

entire core is lipid

32
Q

What is the best use for liposomes/SLNs?

A

cosmetics (local delivery)

33
Q

What are future areas of development for liposomes/SLN?

A

interferon and gene delivery

34
Q

How is complexation achieved?

A

cyclodextrins

35
Q

a-CD

A

6

36
Q

b-CD

A

7

37
Q

g-CD

A

8

38
Q

How do cyclodextrins increase flux?

A

at low CD, they form an inclusion complex with the drug. At high CD, drug won’t dissociate

39
Q

With what drugs do CDs interact?

A

hydrophobic

40
Q

How does the degree of supersaturation change flux?

A

directly proportional!

41
Q

Nss =

A

Sss / St

Drew 924 (16 decks)

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