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Pharmaceutics 2 > Chemical Pentration Enhancer Lect 3 Part1 > Flashcards

Chemical Pentration Enhancer Lect 3 Part1 Flashcards

1
Q

What are the chemical pentration enhancer?

A 
1_ surfactant
2_bile salts and derivatives
3_ fatty acids and derivatives
4_chelating agents
5_Sulfoxide
6_Monohydricalcohol
7_Miscellaneous
8_Polyols
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2
Q

How the penetration enhancers act?

A

It acts by : 1_increasing the drug permeability through the skin by causing reversible damage to the stratum corneum.
2_increasing the pation coefficient of the drug to promot its release from vehicle to the skin.

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3
Q

The water content of stratum corneum is ……%

A

15-20%

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4
Q

What are the mode of action of water in chemical pentration enhancing ?

A

1_Free water acts as solvent and alter solubility of permeants and so its partioning
2_The cells take up water and swell, shuch swelling of cell would impact upon the lipid structure between the cells causing some disruptionto the bilayer packing.

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5
Q

First chemically design molcule as a pentration enhancer

A

Azones

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6
Q

Promote flux both hydrophilic and lipophilic permeant

A

Azones

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7
Q

Highly lipophilic with log o/w =6.2

A

Azones

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8
Q

Azones are effective at concentration ……% to ….%

A

0.1%-5%

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9
Q

Azones are effective in high concentration (T or F)

A

F at low concentration (0.1% -5%)

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10
Q

Azones are soluble and compatible most organic solvents (T or F)

A

T

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11
Q

Enhances permiation of steroids, antiviral, antibiotics.

A

Azones

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12
Q

What is the mode of action of azones?

A

1_(fluidization) interact with thr lipid domains of the stratum corneum.
2_partition into the lipid bilayer to distrupt their packing arrangement.

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13
Q

Is used most commonly in patches

A

Ethanol

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14
Q

What happened if we use alcohol at high concentration?

A

At high concentration causes dehydration of biological membrane and decrease the permeation.

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15
Q

Alcohol used in concentration…..%

A

1-10%

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16
Q

The most effective one in alcohols is the ethanol(T or F)

A

F the butanol

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17
Q

The most used in alcohol is butanol(T or F)

A

F the ethanol

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18
Q

If the alcohol is branshed therefore its activity will increase (T or F)

A

F will have lower activity.

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19
Q

What is the mode of action of alcohols?

A

1(membran thining) because it is act as a solvent
2 volatile nature of ethanol help in modifying thermodynamic activity of drug .due to evaporation of ethanol drug concentration increases providing supersarurated state with greater driving force.
3_ solvent drug may carry permeant into the tissue. (بيشيل الدواء خلال الاغشية)

20
Q

Give reason. Volatile nature of ethanol helps in modifying thermodynamic activity od drug.

A

Due to evaporation of ethanol; drug concentration increases providing supersaturated state with greater driving force.

21
Q

Have potential to damage human skin

A

Surfactant

22
Q

Non ionic surfactants have minor (lower) effect but it is more safe
Anionic surfactant have pronounced effect(more effective) but it less safe
(T or F)

A

T

23
Q

What is the mode of action of surfactants?

A

Solubalise the lipophilic active ingredient and also have potential to solubalise lipids within the stratum corneum.

24
Q

Give reason the surfactant can not be able to do repultion(disrupt) the lipid bilayer packing arrangement as the fatty acids do.

A

Bacause the stracture of the surfactent are smaller than the stracture of the fatty acids

25
Q

Using in scaling condition such as psoriasis

A

Urea

26
Q

Usually urea used in combination with ……. for keratolysis

A

Salicylic acid

27
Q

What are the mode of action of urea?

A

1_Natural moisturizing factor binds with water to the skin, the increasing skin hydration increaseing drug permeation.
2_Has kyratolytic properties.
3_It produce significant stratume corneum hydration, produces hydrophilic diffusion channels.

28
Q

It is maily used (acts) as a vehicles to carry the drug

A

Phospholipids

29
Q

What is the MOA of phspholipids?

A

1_ Occlude the skin surface and increase tissue hydration.

2_ phospholipids fuse with the stratum corneum lipids.

30
Q

Small amphiphilic molecules

A

DMSO

31
Q

Used in chemistry as aprotic solvent

A

DMSO

32
Q

What is the MOA of DMSO at low conc.?

A

1_induces membrane thining

2_ increases the fluidity of the membran’s hydrophopic core

33
Q

What is the MOA od DMSO at high conc.(60%)

A

1DMSO induces transient water pores into the membrane.
2 DMSO binds to water, promoting water defect in the membrane, which lead to reorientation in the membrane structure resulting in bore formation

34
Q

What is the conc. Of the optimum action of DMSO?

A

More than 60%

35
Q

What are the MOA of DMSO?

A

1_ change the keratin conformation from a(alpha) helical to B(beta) sheet.
2_ interacts with the head groups of some bilayer lipids to distrot to the packing geometry.

36
Q

Fatty acids are effective at high concentration (t or f)

A

F at low conc. (<10%)

37
Q

It is colourless liquid

A

Linoleic acid

38
Q

It is un saturated omega 6 fatty acid

A

Lenoleic acid

39
Q

Lenoleic acid presence in …….

A

Safflower oil and poppy oil in conc. 70 -78%

40
Q

What are the uses of lenoleic acid ?

A

Is used in making soap as emulsifier and quick drying oils

41
Q

Is used in making soap as emulsifier and quick drying oils

A

Lenoleic acid

42
Q

A monosaturated fatty acid

A

Oleic acid

43
Q

What are the MOA of Oleic acid?

A

Acts as a pentration enhancer by lipid fluidization and lipid phase separation

44
Q

Is a saturated fatty acid with an 18 carbon chain.

A

Stearic acid

45
Q

Write a ahort note about the lipid phase separation.

A

The pentration enhancer insert its self between the phospholipid molcules of the bilayer of cell surface membrane, forming a change in the orientation of the molcules, resulting in formation of spease between the phospholipids allowing the drug to pentrate easier and faster.

Pharmaceutics 2 (10 decks)

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