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Biopharmaceutics > Oral Drug and Controlled Release Delivery > Flashcards

Oral Drug and Controlled Release Delivery Flashcards

1
Q

What are the advantages of an oral drug delivery system?

A

It is effective, accurate, convenient and cost effective

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2
Q

List the shortcomings of oral drugs.

A

Variability in GI environment
Bioavailability
Limited drug targeting
Pediatric/ geriatric population difficulties

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3
Q

What are the absorption sites with oral dosages?

A 
Stomach (limited)
Small intestine(primary site)
Large intestine(v. limited)
Mouth (buccal and sublingual)
Rectum
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4
Q

What are the 3 key drug properties that need to be considered in oral formulations?

A

Absorption
Stability
Processing

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5
Q

What is the most critical issue for preparation and delivery?

A

Solubility

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6
Q

What is the benefit and downside of solutions?

A

Increases drug absorption but is less stable

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7
Q

What does effect does particle size have on solubility?

A

Increases surface area

Faster disintegration/dissolution

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8
Q

How do we ensure stability in vitro?

A

Coating (tablets and capsules if not stable to light, moisture, etc)
Excipients
Protective packaging

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9
Q

How do we ensure stability in vivo?

A

Enteric coating
Controlled/sustained release
Site- specific release

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10
Q

What are some ways to increase absorption?

A 
Improve solubility
Increase disintegration and dissolution
Administration strategies (w/out food: absorbed quickly and excreted quickly, better to take with food even though slower absorption)
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11
Q

What are some strategies to deal with metabolism?

A

Dose increase
Pro drugs
Enzyme inhibitors
Other administration routes

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12
Q

Where is drug targeting limited to in oral delivery?

A

The GI tract

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13
Q

How is drug targeting achieved?

A

Adhesive polymers to stomach

Sustained/controlled release to small intestine

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14
Q

What are 4 common mucoadhesive polymers (hydrophilic gels)?

A

Chitosans
Polyacrylates
Polyglucons
Hyaluronans

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15
Q

What do mucoadhesive polymers do?

A

Prolong residence
Increase contact time and bioavailability
Localization in specific residence

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16
Q

Who utilizes oral solutions?

A

Pediatrics and elderly

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17
Q

What are the two important considerations that must be accounted for in oral solutions?

A

Taste and colour

Additives(alcohol, sugar, preservatives)

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18
Q

Name the 3 absorptive sites of quick dissolving formulations.

A

Oral
Buccal
Sublingual

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19
Q

What are the benefits of quick dissolving formulations?

A

Fast drug release
Little liquid needed
Convenient administration

20
Q

Why do quick dissolving drugs need special packaging?

A

They can’t be exposed to moisture

21
Q

What are some drugs that can be found as quick dissolving and why?

A

Analgesics, antihistamines, migraine, antidepressants, Parkinsons
Want quick onset or there is a difficulty in taking medications

22
Q

Common excipients used in quick dissolving solutions.

A

Mannitol, sorbitol, effervescent ingredients

23
Q

What are the 4 methods of forming quick dissolving tablets?

A

Spray drying, molding, wet granulation, compression

24
Q

What are some ways to taste mask?

A

Additive-dilution
Film coating
Melting with lipid-based excipients

25
Q

These devices can be inserted and a slow release of drug occurs.

A

Controlled release

26
Q

What are the benefits of controlled release?

A

Fewer administrations
Steady blood concentrations
Better therapeutic outcome
Improved patient compliance

27
Q

What are the 3 types of controlled release drugs?

A

Delayed release
Controlled release
Targeted release

28
Q

Release of two successive doses, initial plus replenishment.

A

Delayed release

29
Q

Drug release over a long period of time, independent of external factors or envornment.

A

Controlled release

30
Q

Site specific or receptor specific.

Sophisticated dosage forms, normally in Parenteral formulations

A

Targeted release

31
Q

What are the benefits of targeted release?

A

Smaller drug dose, fewer dosing, less potential SE, better compliance

32
Q

What are the drawbacks of controlled release?

A

“Dose dumping” potential
Difficult dosing termination
Variable absorption due to varying GI interactions
Increased production cost

33
Q

What are three conditions that controlled release is appropriate for?

A

Cardiovascular
Respiratory
Mood control

34
Q

What is the optimal half life of a drug to be a controlled release candidates?

A

2-8hrs
Any shorter and we need to increase drug dose
Any longer and there’s no need for it
Longer than 8 hrs and drug will be in large intestine (no absorption)

35
Q

What is the optimal dosing range for controlled release drugs?

A

0.5g- 1.0g, preferably less than 0.5g

36
Q

pH range of stability with controlled drugs?

A

1-8

37
Q

What are the 4 drug release mechanisms?

A

Diffusion controlled
Dissolution/Diffusion controlled
Dissolution controlled
Osmotic Pressure controlled

38
Q

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

A

Dissolution

39
Q

Describe the Reservoir System.

A

There is a drug core and the release rate is controlled by film properties: polymers(how fast it dissolve/how permeable to water it is)
There is a potential for toxicity if coating is accident lay destroyed.

40
Q

Describe the Matrix System.

A

Drug and polymer is mixed, release rate is controlled by polymer. This is more of a diffusion method vs dissolution.

41
Q

This system is cheaper and allows for the delivery of larger molecules but zero order delivery livery is impossible

A

Matrix system

42
Q

This system is harder to control due to dissolution and diffusion release rates and the rates being dependant on shape of dosage form

A

Bioerodible System (matrix)

43
Q

The release rate is controlled by the drug or the polymer?

A

Can be controlled by either or both.

44
Q

Describe osmotic pumps.

A

Coated tablet with semipermeable membrane, containing unique chemical in the core that creates osmotic pressure. Drug release is independant of environment

45
Q

Pressure produced by separate chemical cause what kind of order release?

A

Zero

46
Q

What are the 4 things quality control is watching for in controlled release drugs.

A

Drug content
Drug uniformity
Disintegration
Dissolution

Biopharmaceutics (4 decks)

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