Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmaceutics 2 - Winter > 2 - Oral Dosage Form > Flashcards

2 - Oral Dosage Form Flashcards

1
Q

What are some advantages to the oral dosage form?

A
  • Effectiveness (systemic effects, onset/duration of action)
  • Accuracy
  • Convenience (noninvasive, product choice, compliance)
  • Cost
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are some flaws of the oral dosage form?

A
  • GI environment
  • Bioavailability
  • Drug targeting (drug will go anywhere once in solution)
  • Emergency usage (onset too long)
  • Pediatric/geriatric population
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is significant about the absorption in the stomach?

A
  • First passing site
  • Extreme pH
  • Food/drink effect
  • Short pass-over
  • Limited absorption (about 20%)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is significant about absorption in the small intestine?

A
  • Primary site
  • Milder environment
  • Larger area
  • Longer pass-over
  • Major absorption
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Does absorption occur in the large intestine?

A

Minimal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Does absorption occur in the esophagus?

A

No

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Does absorption occur in the mouth?

A

Buccal and sublingual absorption

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Does absorption occur in the rectum?

A

Yes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are some components required to make an oral capsule/tablet work?

A
  • Absorption (solubility, permeability, safety)
  • Stability (physical, chemical, biological, pharmacological)
  • Processing (compatibility, compressibility, stability, feasibility)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What should be done if a drug doesn’t have good stability in the GI tract?

A

Use a different dosage form

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is required for a drug to be considered stable?

A

Overall adequate stability to environmental factors like temp, light, moisture (in vitro); various pH values, enzymes, and possible first-pass metabolism (In vivo)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Why is entrophen enteric-coated?

A

So it will not be absorbed in the stomach, b/c it is known to cause ulcers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are ways to increase solubility?

A
  • Different salt forms
  • Particle micronization
  • Processing modification
  • Faster disintegration/dissolution
  • Formulating solutions
  • Surfactant application
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is a disadvantage to particle size micronization?

A

Increased solubility, but particles that are too small will stick together and cause processing problems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What can be done in vitro to increase stability?

A
  • Coating
  • Additive application (ex: antioxidants, preservatives)
  • Protective packaging (ex: amber glass, inert gas replacement)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What can be done in vivo to increase stability?

A
  • Coating
  • Controlled/sustained release
  • Site-specific release
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What can be done to bypass absorption limitation?

A
  • Improve solubility and stability
  • Select appropriate excipients
  • Increase disintegration and dissolution
  • Modify drug release profiles
  • Use administration strategies
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What can be done to prevent drug metabolism before absorption?

A
  • Structural modifications
  • Preparation coating
  • Controlled release
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What can be done to prevent drug metabolism after absorption?

A

Prodrug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What should be considered when metabolism is a problem?

A
  • Appropriate formulation
  • Dose increase (pay attention to toxicity)
  • Prodrugs
  • Enzyme inhibitors
  • Other administration routes (ex: rectal, sublingual, parenteral)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What can be used to retain formulations in the stomach or portions of small intestine?

A

Adhesive polymers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Is it possible to target oral drugs outside of the GI tract?

A

No

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What can be used for drug targeting?

A
  • Mucoadhesive polymers

- Hydrophilic gels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What should be considered when planning to target a drug?

A
  • Prolonged residence time
  • Increased contact w/ membrane
  • Localization in specific regions
  • Improved bioavailability
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What is very important w/ respect to oral solutions?

A

Taste and color

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Which dosage forms can have quick-dissolving properties?

A
  • Oral
  • Buccal
  • Sublingual
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Is there any PK/PD changes in quick-dissolving drugs?

A

No

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Which types of drugs are suitable to be quick-dissolving?

A
  • Analgesics
  • Antihistamines
  • Cough/cold
  • Migraine
  • Antidepressants
  • Anti-psychotics
  • Parkinson’s
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What are the different types of quick-dissolving dosage forms?

A
  • Oral disintegrating tablets
  • Fast-melt tablets
  • Quick-dissolving tablets
  • Mouth-dissolving tablets
  • Orodispersible tablets
  • Flashtab
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

What are some common excipients used in quick-dissolving compounds?

A
  • Mannitol and sorbitol
  • Crospovidone, sodium starch glycolate, croscarmellose
  • Combination w/ effervescent ingredients (calcium bicarbonate)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

What can be done to mask the taste of a drug?

A
  • Additive dilution
  • Film coating of particles/granules
  • Melting w/ lipid-based excipients
  • Cyclodextrin encapsulation
  • Wet granulation
32
Q

What should taste-masking NOT affect?

A

Drug properties and in vivo profiles

33
Q

Why would a drug need to have a controlled release?

A
  • Fewer administration frequency
  • Steady blood concentration
  • Better therapeutic outcome
  • Improved px compliance
34
Q

What is the definition of controlled release?

A
  • Modified drug release rate
  • Extended period of drug release
  • Controlled drug direction to site
35
Q

Controlled release drugs have better ____ therapeutic outcomes

A

In vivo

36
Q

What is the difference between sustained release and controlled release?

A
  • Sustained release = any dosage form that provides medication over an extended period of time
  • Controlled release = system is able to provide some actual therapeutic control
37
Q

What should be some characteristics of the ideal controlled release preparation?

A

Should be able to provide an exact amount of drug at the site of action for a precise period of time (zero-order drug release)

38
Q

Most controlled release or sustained release tablets release drug contents in ______ or _____ kinetics

A

First-order or pseudo zero-order kinetics

39
Q

Most delayed release dosage forms are for ___ drug delivery

A

Oral

40
Q

For controlled release, release of drug is independent of _____

A

External factors or environment

41
Q

Are controlled release dosage forms only for oral drug delivery?

A

No, various administration routes

42
Q

Targeted release is generally for _____ drug delivery

A

Parenteral

43
Q

Do controlled release drugs have improved therapeutic outcomes? Why or why not?

A

Yes b/c they reduce drug concentration fluctuations and optimize drug bioavailability

44
Q

Do controlled release drugs generally increase or decrease patient compliance?

A

Increase

45
Q

What are some disadvantages to controlled release dosage forms?

A
  • “Dose-dumping” dangers
  • Difficult dosing termination
  • Possible erratic or variable absorption due to GI interactions
  • Complex production and quality control procedures
  • Higher unit cost
46
Q

Which diseases are controlled release dosage forms appropriate for?

A
  • Chronic conditions and long-term administration regimens

- Ex: CV (hypertension, heart diseases); respiratory (asthma, allergy); others (depression, mood control)

47
Q

When should controlled release dosage forms NOT be used?

A

For short-term uses (less than 2 weeks, antibiotics, analgesics)

48
Q

What is a suitable half life range for a controlled release dosage form? What would a half life out of this range cause?

A
  • 2-8 hours
  • Too short = higher drug dose
  • Too long = no need for controlled release
49
Q

What is a suitable GI tract passage time for a controlled release dosage form and why?

A

8-12 hours b/c limited absorption after small intestine

50
Q

For a controlled release dosage form, should absorption rate or drug release rate be faster?

A

Absorption rate

51
Q

Can controlled release drugs be chewed or crushed?

A

No, never

52
Q

What is the preferred dosing range for a controlled release drug and why?

A
  • Preferred less than 0.5 g, but can be 0.5-1 g
  • Less than 500 mg is more suitable for controlled release b/c unit dose may be increased in order to accommodate administration frequency
53
Q

What are some stability requirements for a controlled release dosage form?

A
  • Wide pH range (1-8)
  • No acid-base hydrolysis
  • No enzymatic cleavage
  • No potential drug/drug or drug/food interactions
54
Q

What are the various types of drug release mechanisms?

A
  • Diffusion controlled (reservoir and matrix)
  • Dissolution/diffusion controlled
  • Dissolution controlled (reservoir and matrix)
  • Osmotic pressure controlled
55
Q

Does diffusion or dissolution play more of a significant role in drug release?

A

Dissolution

56
Q

What is involved in a diffusion controlled reservoir system?

A
  • Drug core surrounded by insoluble polymeric film

- Nature of polymer film determines rate of drug release from system

57
Q

What are some characteristics of a diffusion controlled reservoir system?

A
  • Zero-order delivery possible
  • Difficult to deliver large molecules
  • Potential toxicity if failed in vivo
  • Physically removed from site
58
Q

What does Fick’s law describe?

A

Process of drug movement across the membrane

59
Q

What are the 2 types of matrix systems?

A

Soluble and insoluble

60
Q

What does a diffusion controlled matrix system include?

A
  • Drug-polymer mixture (drug dispersed homogeneously through polymer)
  • Insoluble matrix
  • Release rate controlled by polymer
61
Q

What are some characteristics of a diffusion controlled matrix system?

A
  • Easy to manufacture
  • Many polymer choices
  • Possible to deliver large molecules
  • Zero-order delivery impossible
  • Removal of matrix necessary if implanted
62
Q

What does a bioerodible system contain?

A
  • Drug-polymer mixture (drug dispersed homogeneously in chemical polymers)
  • Soluble matrix
  • Release rate controlled by polymer
  • Diffusion and dissolution type
63
Q

What are some characteristics of bioerodible systems?

A
  • Easy to manufacture
  • Many polymer choices
  • Possible to deliver large molecules
  • Difficult to control release rate due to both dissolution and diffusion
  • Potential problem w/ degraded polymers in vivo
  • Will change physical configuration over dissolution period
64
Q

What does a dissolution system include?

A
  • Reservoir or matrix

- Release rate controlled by drug, polymer, or combinations

65
Q

What does making a dissolution system involve?

A
  • Selecting appropriate salts or derivatives w/ lower aqueous solubility
  • Coating drug w/ slowly dissolving material
  • Incorporating substance into tablet made of slowly dissolving carrier
66
Q

What are some characteristics of a dissolution system?

A
  • Different choices for formulations
  • Possible to deliver large molecules
  • Release rate dependent on many parameters
  • Complex release mechanisms
67
Q

How does a dissolution system maintain drug concentrations?

A
  • Beads w/ thinnest coating will provide the initial dose

- Beads w/ thicker coatings can maintain necessary drug concentrations at later durations

68
Q

What does an osmotic pump involve?

A
  • Drug core w/ osmotic-producing agent
  • Semipermeable membrane
  • Release rate controlled by osmotic pressure
69
Q

What are some characteristics of an osmotic pump?

A
  • Zero-order release achievable
  • One model fits all drugs (theoretical); as long as no compatibility issues btwn drugs
  • Drug release independent of environment
  • Higher production cost due to special equipment and stringent quality controls
70
Q

What determines the drug release rate of an osmotic pump?

A

Water flowing rate into the device and drug concentration w/in the device

71
Q

Which drug release mechanisms are used for tableting?

A
  • Matrix (uncoated)

- Tablet cores (for further coating)

72
Q

Which drug release mechanisms are used for fluid-bed technology?

A
  • Pellets for capsules/tablets

- Reservoir

73
Q

Which drug release mechanisms are used for film coating?

A
  • Reservoir
  • Osmotic pumps
  • Enteric-dissolved
74
Q

What is tested during quality control?

A
  • Drug content
  • Drug content uniformity
  • Drug disintegration (required for enteric-coated formulations; not needed for most controlled release formulations)
  • Drug dissolution (in different mediums like gastric fluid, intestinal fluid, water)
75
Q

What is required for a drug to pass dissolution testing?

A

Over 85% drug release w/in 8 hours

76
Q

What is coming in the future w/ regards to oral dosage form?

A
  • More controlled release products
  • Protein and peptide formulation
  • Improvement in bioavailability and drug targeting
  • More biodegradable polymers

Pharmaceutics 2 - Winter (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions