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PHRM828 > Exam 2 Knipp > Flashcards

Exam 2 Knipp Flashcards

1
Q

Why are excipients the key ingredients for controlling drug delivery?

A

Coatings and other dosage forms can help control when the drug gets released based off of their physiochemical properties

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2
Q

What do coatings help with?

A

Protection from air and humidity, can help mask the taste, can provide special drug release, aesthetics and can help prevent inadvertent contact with other drugs.

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3
Q

What is enteric coatings?

A

A coating added to a drug to help prevent early breakdown of the drug where it will undergo a chemical or metabolic breakdown.

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4
Q

What are the 5 primary reasons for enteric coatings

A
  1. To prevent acid sensitive API from gastric fluids
  2. To prevent gastric distress from API (getting sick)
  3. To prevent API delivery to a site in the intestine
  4. To provide delayed / sustained release (help it release in a certain area
  5. To deliver the API to a more bioavailiable region of the intestine
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5
Q

What is sustained release drug?

A

The onset of the drug is delayed, but the TE has sustained duration

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6
Q

What is controlled release?

A

A dosage form which allows us to maintain a narrow drug plasma concentration steady state

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7
Q

Traditional controlled release formulations

A

Coated beads, granules, microspheres, multitablet system, microencapsulated, drug embedding in a slowly eroding or hydrophillic matrix

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8
Q

What is steady state?

A

The rate of API going into the body must be equal to the amount being disposition

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9
Q

Characteristics of drugs best suited for oral controlled release formulation

A

Exhibit neither a slow or fast rates of absorption and excretion, uniformly absorbed in the GI tract, have a safe therapeutic window, administered in relatively small doses

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10
Q

What are some physiological factors affecting absorption?

A

Absorbing surface area, pH change in the lumen, API permeability, dietary fluctuation

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11
Q

Epithelial tissue, know the 4 different types

A

Simple squamous-thin layer (permeable, lines most blood vessels-placenta) Simple columnar (usually found in the GI tract) Translational- (composed of several layers with different shapes usually stretchy) Stratified squamous (subject to wear and tear, example is the skin)

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12
Q

What are endothelial cells

A

Cells that line the surfaces of body cavities, blood vessels and lymph (endo = in, therefore internal surfaces)

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13
Q

Whats the composition of biological membranes?

A

Semi permeable, Isolates the cellular inside components, Polarized, All living cells are composed of one or more membranes which defines it as a living unit.

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14
Q

Does cholesterol only have harmful effects of membranes?

A

No, at lower levels it provides fluidity, but at higher levels it forms a crystalline state which is called hardening atherosclerosis which can also cause the cell to lyse.

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15
Q

What type of cells are targeted by too much cholesterol?

A

Muscle cells are the main cells attacked by high cholesterol

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16
Q

Membrane and cell-based assays

A

Used to help find permeability

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17
Q

Transport systems in the intestines

A

Passive (non-saturable), Paracellular (between cells), Transcellular (through cells), Carrier mediated (saturable), Active (energy dependent), Facilitated diffusion (energy independent)

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18
Q

General Interpretation of Caco-2 vs PAMPA data

A

PAMPA is passive diffusion, Caco-2 is passive, active influx, efflux, and paracellular. Both make the line usually linear.

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19
Q

Drug transporters general knowledge

A

Membrane bound proteins, function is to move molecules across the membrane, Drug transporters are crucial for tissue and cellular distribution not only for drug clearance but also for sanctuary organs

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20
Q

Nutrient and xenobiotics transporters

A

Solute carrier (SLC), APT-binding cassette (ABC)

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21
Q

Effects of solute carriers

A

43 subfamilies, > 300 members identified, influx of secretory efflux transporters

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22
Q

Effects of ATP-binding cassete

A

7 subfamilies, 50 members presently identified, usually an efflux multidrug resistant transporters

23
Q

Routes of absorption

A
  1. influx transporter mediated
  2. passive transcellular
  3. passive transcellular and efflux
  4. passive paracellular
  5. metabolism
  6. efflux of the metaoblite(s)
24
Q

What is influx?

A

Transporters transfer substrates into the cell

25
Q

What is efflux?

A

Transporters pump substrates out of the cell

26
Q

What is absorptive?

A

When transporters transfer substrates into the systemic blood circulation

27
Q

What does secretory mean?

A

Transporters that transfer their substrates from blood circulation into bile, urine, or GI lumen

28
Q

What is the esophagus composed of?

A

Stratified squamous epithelium

29
Q

What is the trachea composed of?

A

Psuedostratified squamous epithelial cells

30
Q

What is the stomach composed of?

A

Columnar epithelial cells

31
Q

What are the small and large intestine composed of?

A

Mostly columnar epithelial cells

32
Q

What is the role of the stomach?

A

To digest food, fasted pH is usually less than 3, fed pH is usually 5-7, gastric emptying half-time is usually 30 min, “housekeeper wave”

33
Q

What is the organization of the stomach

A

Fundus (top part which contains the gas pocket), Body, Greater curvature, Pyloric sphincter (where food gets pushed top the intestine)

34
Q

Does the stomach fluctuate pH during the day?

A

Yes

35
Q

Do different types of food you eat directly effect how fast food moves out of the stomach?

A

Yes, example is : carbonated drinks move it faster, while a big mac will slow gastic emptying down

36
Q

Mouth to anus time :

A

24-32 hours

37
Q

How long does it take to move through the small intestine?

A

3 Hours

38
Q

Where does most food and drug absorption occur?

A

The small intestine

39
Q

Whats the pH of the small intestine?

A

5.0-6.5 pH

40
Q

Characteristics of the intestinal absorption surface area.

A

Folds of kerckring x3 -> villi x30 -> microvilli x600 -> all folds increase the surface area greatly allowing for better absorption

41
Q

Know the relative size of micro vs nano particles

A

Example was picture of the rat jejenum

42
Q

Columnar epithelium characteristics

A

The anchor cells, contain the crypt region and villus region

43
Q

Characteristics of the colon

A

125cm from caecum to anus (transport is much slower than the small intestine), AC is 20cm long, TC is 45cm long, DC is 30cm long. Thickness of the colon is 2.5cm (sigmoidal region) - 8.5cm (caecum) Colon is responsable for water and electrolyte absorption

44
Q

Is colon transit longer in younger people or older people?

A

Colon transit is longer in older people

45
Q

Is there a relationship between the stomach emptying rates and colonic retention

A

Yes the stomach and colonic retention appear to correlate quite well over fairly extended time periods

46
Q

Characteristics of the rectum

A

Upper rectum (simple columnar) and lower regions (stratified squamous non-keratinized) the non-keratinized epithelium allows for high drug absorption, there are a number of high potency drugs which can be delivered rectally, there is a low residence time

47
Q

The considerations for oral consumption

A

How the drug gets absorbed and the entire path that it takes to get to where it needs to go

48
Q

What is the biorelavant dissolution times in men

A

Average is around 3.45 hours

49
Q

GI transit time variation

A

The effects of enough water consumption can aid in getting drugs absorbed more effectively

50
Q

GI transit time variation

A

Greater GI residence leads to higher absorption

51
Q

Characteristics of pH in the intestine & colon

A

Jejunum ~ 7pH, ileum ~ 7.8pH, Colon ~ 8.1pH

52
Q

Where is the bile salt content in the intestine

A

Only bile salt concentration is ~2.88mM

53
Q

What are the factors influencing drug solubility along the GI tract?

A

Buffer capacity, bile salts, regional fluids, other drugs, potential issues from endogenous substrates

54
Q

Segregated blood flow through the intestine and how does it effect drugs?

A

While moving through the different blood flows will effect manufacturing and dosage forms so they will need to plan accordingly to make sure it is effective

PHRM828 (3 decks)

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