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The Medicine (Y2) > Biopharmaceutics > Flashcards

Biopharmaceutics Flashcards

1
Q

Bioavailability is concerned with ADME. True or false?

A

False - absorption only

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2
Q

What is absolute bioavailability?

A

The fraction of drug in the dosage form that arrives in the systemic circulation

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3
Q

IV administration is extra-vascular. True or false?

A

False - intravascular

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4
Q

There are transport proteins present in the epidermal cells of the skin to help with absorption of drugs. True or false

A

False - no transport proteins

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5
Q

the stratum corneum is made of living cells. True or false?

A

False - dead cells

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6
Q

There is no blood supply within the epidermis. True or false?

A

True

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7
Q

In which part of the skin are blood vessels found?

A

papillary dermis

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8
Q

Only high molecular weight drugs can be used in transdermal drug delivery systems. True or false?

A

False - low molecular weight

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9
Q

Typically, how long does passage through the GIT take?

A

1 day - can vary based on eating, health etc.

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10
Q

Permeability in the mouth is less than in the skin. True or false?

A

False - greater than skin

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11
Q

Buccal and sublingual administration of drugs is good for hydrophilic drugs. True or false?

A

False - lipophilic drugs

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12
Q

First pass metabolism is avoided via buccal and sublingual administration. True or false?

A

True

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13
Q

The oesophagus is a significant site of absorption. True or false?

A

False - but is relevant to the mechanics of absorption

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14
Q

There are no transporters for nutrient absorption in the stomach. True or false?

A

True

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15
Q

When gastric emptying is slow, alcohol absorption is high. True or false?

A

False - alcohol absorption is slow

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16
Q

What are the two mechanisms of transport across the GI epithelium?

A

Transcellular

Paracellular

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17
Q

The transcellular route is preferred for small lipophilic molecules. True or false?

A

True

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18
Q

Drugs with a log P <0 cross via the transcellular route. True or false?

A

False - paracellular

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19
Q

Starting with disintegration, what are the steps that follow before a drug is absorbed?

A

Disintegration -> dissolution, permeation, pre-systemic metabolism

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20
Q

What are the two key competing processes to dissolution and permeation?

A

Transit and stability

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21
Q

In the BCS, a drug is considered to be highly soluble under what circumstances?

A

the highest dose strength is soluble in 250ml or less of aqueous media over the pH range 1-8

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22
Q

In the BCS, a drug is considered to be highly permeable under what circumstance?

A

When the extent of absorption in humans is expected to be more than 90% of the administered dose (predicted by lab methods)

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23
Q

Drugs in BCS class 3 have a high permeability but low solubility. True or false?

A

False - high solubility, low permeability

24
Q

What are the limitations of the BCS system?

A

Doesn’t take into account stability of drug e.g. at different pH values or the binding interactions with the gut or its contents

25
Q

Name a drug that is under Class I of BCS

A

Propranolol

26
Q

Name a drug that is in Class II of BCS

A

Ketoprofen

27
Q

Name a drug that is in class III of BCS

A

Atenolol

Gabapentin

28
Q

Name a drug that is in class IV of BCS

A

Furosemide

29
Q

Time to peak plasma concentration is related to the extent of absorption. True or false?

A

False - rate of absorption

30
Q

What indicates the extent of absorption?

A

Area under curve

31
Q

What is the equation for absolute bioavailability?

A

F = AUC(oral) / AUC (IV)

32
Q

When F = 100, it shows 100% bioavailability. True or false?

A

False, F = 1

33
Q

What is the difference between a drug and a medicine?

A

The drug is the API, pharmacological agent and therapeutic molecule whereas the medicine is the delivery system, drug + excipients and the formulation

34
Q

Why does “available at the site of action” translate to “arrives to the systemic circulation”?

A

For practical reasons - blood can be sampled easily
PK reasons - drug is central compartment from which drug is distributed
Pharmaceutics - once drug is in the blood, formulation is irrelevant - drug is dissolved in blood plasma

35
Q

What are the routes of administration across epithelial layers?

A

Skin
Small intestine
Buccal, gastric, rectal
Nasal

36
Q

How can the epithelial layer be bypassed?

A

Parenteral administration - intravascular or extravascular

37
Q

What are the exceptions to absorption of drugs in the stomach?

A

No absorption takes place in the stomach normally as there are no transporters of absorption proteins to exploit however highly permeable drugs e.g. ethanol and weakly acidic drugs e.g. aspirin are able to be absorbed in the stomach

38
Q

What is meant by bioequivalence?

A

No significant difference in AUC, Cmax and Tmax

39
Q

What are biopharmaceutics?

A

They can be biologics - examples include monoclonal antibodies, ADC, interleukins, peptides and virus-like particles

40
Q

What are the two ways in which biologics can be formulated as?

A

Liquids of lyophilised solids ready for reconstitution

41
Q

What are the advantages of solid form biologics?

A

Dose and injection volume are adjustable

Can be developed as multi-use formulations

42
Q

What are the advantages of luquid form biolog

A

More convenient to end user
Better patient compliance
Better accuracy

43
Q

What are the disadvantages associated with liquid form mabs?

A

Chemical degradation - hydrolysis

Physical stability more difficult to control - aggregation

44
Q

Name some buffers that can be used in the formulation of proteins and mabs

A

Acetate, citrate, succinate, histinde

45
Q

What are salt and tonicity modifiers used for in formulation of mabs and name a common one

A

Colloidal stability

NaCl

46
Q

Which type of mab injection requires an isotonic preparation?

A

IV

47
Q

Which type of mab injections are able to handle hypertonic or hypotonic conditions?

A

IM or SC

48
Q

What is the role of surfactants in the formulation of mabs and proteins?

A

mAbs are flexible molecules with hydrophobic and hydrophilic regions - unfolding leads to aggregation - surfactants cover interfaces therefore limit unfolding

49
Q

Why may antioxidants be needed in the formulation of proteins and mabs?

A 
Because polysorbates (surfactants)
can oxidise over time which can affect shelf-life so antioxidants e.g. EDTA needed
50
Q

Why are protein stabilisers needed in the formulation of proteins and mabs? Give an example of one

A

For preferential hydration of proteins. Stabilisers are preferentially excluded from the protein’s surface - allowing hydration. E.g.s include sugars e.g. sucrose and amino acids e.g. arginine

51
Q

What are the limitations of using sugars as protein stabilisers?

A

Disaccharides are susceptible to hydrolysis at low pH and sucrose hydrolyses to glucose and fructose at pH 5

52
Q

Which amino acids are most susceptible to oxidation?

A 
Methionine 
Tyrosine
Tryptophan 
Cystiene 
Histidine
53
Q

What is the limit for presence of aggregates set out by WHO?

A

less than 5%

54
Q

Which IgG is more prone to aggregation than others?

A

IgG2

55
Q

What are leachables?

A

Compounds released form container closure system when in contact with solvent

56
Q

What are extractables?

A

Subset of compounds eluting during normal storage or use conditions e.g. infusion bag

57
Q

What are the challenges for SC formulations?

A

Small vol, high concs so increased risk of aggregation

Increasing the amount of protein increases viscosity so it is harder to push out of syringe

The Medicine (Y2) (34 decks)

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