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PHRM 828: Dosage Forms > DOSAGE I: Exam 2 > Flashcards

DOSAGE I: Exam 2 Flashcards

1
Q

Why do we use enteric coatings? (5)

A

1.To prevent acid sensitive APIs from gastric fluids
2. To prevent gastric distress from the API
3. To target API delivery to a site in the intestine
4. To provide a delayed/sustained release.
5. To deliver the API in a higher local concentration in
the intestines where it may be absorbed and have a
higher bioavailability

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2
Q

What is sustained release?

A

the onset of pharmacologic action is delayed, but its therapeutic effect has a sustained duration

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3
Q

What is controlled release?

A

-goes beyond sustained release and
implies a reproducibility and predictability in the drug
release kinetics
-Allows us to maintain a narrow drug plasma concentration

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4
Q

Examples of controlled release formulations (4)

A
  1. coated beads, granules, microspheres
  2. multitablets
  3. microencapsulated
  4. drug embedded in a slowly eroding or hydrophilic matrix
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5
Q

Define “steady state”

A

-the rate going into the body must equal the
disposition (the rate distributing early and being metabolized, and/or being excreted from the body)
-allows us to maintain a narrow drug plasma concentration

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6
Q

Characteristics of drugs suited for controlled release formulation (5)

A
  1. Exhibit neither slow or fast rates of absorption
    and excretion
  2. Uniformly absorbed from the gastrointestinal
    tract
  3. Administered in relatively small doses
  4. Have good safety/therapeutic window
  5. Chronic therapies better suited than acute
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7
Q

Physiological factors affecting absorption (7)

A
  1. Absorbing Surface Area
  2. Residence Time at Absorption Site
  3. pH changes in lumen
  4. Permeability/Perfusion (Functional and molecular characteristics of transporters and metabolism)
  5. Dietary Fluctuations/Effects
  6. Complexation/protein binding
  7. Biliary uptake and clearance
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8
Q

Describe epithelia (3)

A
  1. cells predominantly used for external surface + endothelial cells
  2. sit on a layer of extracellular matrix proteins (cell side = apical, protein side = basal)
  3. polarized with directional transport
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9
Q

Define endothelial cells

A

simple squamous cells that line the inside surfaces of body cavities, blood vessels, and lymph

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10
Q

Composition of biological membranes (2)

A
  1. The cell membrane is a semi-permeable
    membrane, permitting the rapid passage of some
    chemicals while preventing the
    passage of others
  2. Cellular lipid composition is POLARIZED, and
    intracellular membrane lipids are different then
    extracellular lipids.
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11
Q

What does cholesterol do in lower levels? In higher levels?

A

In lower levels, cholesterol provides fluidity. At higher levels, causes membrane to undergo phase transition to liquid crystalline state

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12
Q

Intestinal transport mechanisms

A
  1. PASSIVE (non-saturable)
    -paracellular: between cells (hydrophilicity)
    -transcellular: through cells (lipophilicity)
  2. CARRIER-MEDIATED (saturable)
    -active: energy dependent
    -facilitated diffusion: energy independent
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13
Q

What is PAMPA?

A

Parallel artificial membrane permeability assay
SEE PICTURES

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14
Q

Define “influx transporters”

A

transfer substrates into cells

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15
Q

Define “efflux transporters”

A

pump substrates out of cells

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16
Q

Define “absorptive transporters”

A

transfers substrates into the systemic blood circulation

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17
Q

Define “secretory transporters”

A

transfer substrates from the blood circulation into bile, urine, or GI lumen

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18
Q

Nutrient and xenobiotic transporters

A

solute carriers (SLC) + ATP-binding cassettes (ABC)

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19
Q

Solute carriers (SLC): types

A

PepT1, OATs, OATPs
*influx and efflux

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20
Q

ATP-binding cassette (ABC): types

A

P-glycoprotein, MRPs
*efflux2

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21
Q

GI tract epithelia: oral cavity (buccal + sublingual)

A

buccal: stratified squamous
sublingual: simple squamous

22
Q

GI tract epithelia: esophagus

A

stratified squamous

23
Q

GI tract epithelia: trachea

A

pseudo-stratified squamous

24
Q

GI tract epithelia: stomach

A

columnar, goblet cells (mucus), parietal cells (acid), enterochromaffin cells (histamine)

25
Q

GI tract epithelia: small and large intestines

A

columnar

26
Q

GI tract epithelia: rectum

A

upper: simple columnar
lower: stratified squamous non-keratinized to stratified squamous keratinized

27
Q

Fasting pH of stomach

A

< 3

28
Q

Fed pH of stomach

A

5-7

29
Q

Function of stomach: fundus

A

contains gastric acid and produces contractions to move contents

30
Q

Function of stomach: body

A

reservoir for ingested foods and fluids

31
Q

Function of stomach: antrum

A

lowest part of stomach, pyloric region funnels/controls flow into the small intestine

32
Q

Where does most absorption occur?

A

small intestine

33
Q

Small intestine pH

A

5.0-6.5

34
Q

Define “bioavailability”

A

rate and extent of drug absorption

35
Q

Define “Paracelsian theory”

A

a chemical might have no effect, a beneficial effect, or a toxic effect

36
Q

Define “dose”

A

-amount of chemical in which the whole organism is treated
-the local concentration of the chemical at the biological response site

37
Q

What does ADMET stand for?

A

A= absorption
D= distribution
M= metabolism
E= excretion
T= toxicity

D+M+E = disposition phase
M+E = elimination

38
Q

Define “therapeutic window”

A

Plasma level between minimum effective level and minimum toxic level

39
Q

Sites of first pass metabolism

A

GI epithelium, liver

40
Q

Systemic metabolism

A

can occur in organs and in the blood stream

41
Q

Phase 1 metabolism

A

metabolism of the main compound i.e. decarboxylases, oxygenases, deamidation

**cytochrome P450s, especially CYP3A4

42
Q

Phase 2 metabolism

A

metabolism through addition, conjugation i.e. glucuronidation, sulfation

43
Q

Phase 3 metabolism

A

transport-multidrug resistance

  • ABCs and SLCs
44
Q

Increased surface area leads to…

A

increased dissolution rate

45
Q

Rate of dissolution

A

dM/dT = change in amount of mass that appears in solution over time

46
Q

What percent of approved drugs have pediatric labeling?

A

20-30%

47
Q

Therapeutic equivalence=

A

pharmaceutical equivalence + bioequivalence

48
Q

PAMPA = Caco-2

A

Passive diffusion

49
Q

PAMPA > Caco-2

A

Pgp efflux, secretory efflux

50
Q

PAMPA < Caco-2

A

Active uptake or paracellular transport

PHRM 828: Dosage Forms (5 decks)

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