Test 1-Mass transfer Flashcards

(49 cards)

1
Q

What is mass transfer (definition)?

A

A net movement of mass from one location to another in response to applied driving forces

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2
Q

When and where in the human body does mass transfer happen?

A

Occurs across different types of cell membranes and under different physiological conditions

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3
Q

What studies is mass transfer important for?

A

Dosage form design
ADME

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4
Q

What does diffusion of a drug through biological membrane involve?

A

Diffusion
Partitioning
Permeation

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5
Q

What is the diffusion step?

A

The drug’s diffusion through the aqueous medium that bathes the membrane

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6
Q

What is the partitioning step?

A

Passage of the drug molecules form the aqueous medium of the GI fluids into the lipid bilayer of the membrane

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7
Q

What is the permeation step?

A

Diffusion of the drug through the membrane

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8
Q

What is drug permeation?

A

Drug transfer - molecular diffusion of the drug through relatively non porous media

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9
Q

What does drug permeation depend on?

A

Drug partitioning
The structural nature of biological membrane
The nature of diffusion layer (GI content)

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10
Q

What is drug partitioning?

A

The ability of the drug to distribute in a mixture of aqueous and lipid system

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11
Q

How is drug partitioning across biological membrane measured?

A

By using a mixture of octanol (nonpolar) and water (polar) to get Kd and then Lop P which represents the drugs lipophilicity

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12
Q

What does lipophilicity affect?

A

Aqueous solubility (decreases with an increasing Log P)
Permability (increases with increase in Log P)

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13
Q

How do most therapeutic agents exist?

A

As either weakly acidic or basic in nature

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14
Q

What does aqueous solubility of a drug depend on?

A

pKa or the dissociation constant
pH of the solution

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15
Q

TF: The ionized states of a drug exhibit greater aqueous solubility than un ionized states

A

True because the ionized states are polar

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16
Q

What does pH of the surrounding fluid affect for the drug?

A

Solubility
Dissolution
Permeation

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17
Q

What kind of drugs are predominantly present in their un-ionized forms in the GI fluid in the stomach and upper part of the duodenum?

A

Weakly acidic drugs because of the lower pH which aids in their permeation in these areas

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18
Q

What kind of drugs are poorly absorbed in the stomach?

A

Weakly basic drugs
They exist largely in the ionized states at the GI pH

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19
Q

Why is the lipophilic nature of drugs important?

A

Because the biological membranes are lipid barriers

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20
Q

What is the most common process for the passage of drugs through biological membranes?

A

Passive diffusion

21
Q

What is passive diffusion?

A

When drugs diffuse across a cell membrane from a region of high concentration (GI fluid) to a region of low concentration (blood)

22
Q

What is diffusion rate directly proportional to?

23
Q

TF: small particles pass the membranes much slower than large molecules

A

False
They diffuse faster

24
Q

What is passive diffusion of drugs governed by?

A

Fick’s law of diffusion

25
Drug molecules bound to other structural materials do/dont participate in diffusion process?
Do not
26
What happens in transcellular transport?
Drugs diffuse through the matrix or core of the membrane
27
Transcellular transport is ______ across different tissue membranes.
Constant
28
What does transcellular transport depend on?
Lipophilicity, polarity and molecular weight of drug molecule
29
What happens during paracellular transport?
Drugs diffuse through the water filled gaps between adjacent cells
30
Paracellular transport ____ from tissue to tissue.
Vary
31
What does paracellular transport depend on?
Size of the junction and size of the drug molecules
32
What polar compounds cross the biological membrane faster than non polar compounds?
Ones that have specialized carrier and transporters
33
What is the best studied system of active transport?
ATPase proteins that are particularly important in maintaining concentration gradients of small ions in cells
34
What are transporters?
Proteins that reside on biological membranes and serve to facilitate the passage of chemicals into or out of a cell
35
What do transporters located on the intestinal membrane influence?
Drug absorption
36
What do transporters on the hepatocyte influence?
Metabolism
37
What do transporters on the renal tubular membrane influence?
Excretion
38
What is MRP?
Multi-Drug Resistance Proteins
39
What is BSEP?
Bile Salt export pump
40
What are the two broad classes of transporters?
Influx (uptake) transporters Efflux transporters
41
What do influx transporters do?
Transport drugs into the tissue/cell
42
What type of transporter is MRP?
Efflux
43
What type of transporter is BSEP?
Efflux
44
What do efflux transporters do?
Transport drug out of the tissue/cell
45
What are OATPs and what type of transporters are they?
Organic anionic transport proteins Influx
46
What type of transporter is p-glycoprotein?
Efflux
47
What is MDR1 and what type of transporter is it?
Multi drug resistance 1 Efflux
48
What is BCRP and what type of transporter is it?
Breast cancer receptor proteins Efflux
49
What is pore transport?
The aqueous channels which exist in cell membranes to allow very small hydrophilic molecules such as urea, water and low molecular weight sugars to be transported into the cell