Oral Drug Delivery Flashcards

1
Q

What are advantages to an oral delivery route?(7)

A
  1. Patient acceptability and compliance 2. Large surface area for absorption in GI tract 3. Rich blood supply
  2. Prolonged retention 5. Possible for zero-order controlled release 6. Inexpensive 7. For local or systemic delivery
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2
Q

What is something to be noted about patient compliance?

A

Many drugs taste bad and it is difficult for people to be perfectly compliant patients.

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3
Q

Why do we want drugs to be near a zero order controlled release?

A

Body releases substances at very consistent levels and we should try to emulate this with drugs

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4
Q

Why do some drugs cause adverse reactions to an organ that they have nothing to do with?

A

Body does not like when given a high dose of anything, and may make a person feel sick, headache, vomiting.

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5
Q

What are three factors effecting systemic absorption and bioavailability of a drug? (3)

A
  1. Physicochemical properties of the drug
  2. Formulation factors
  3. Anatomy and physiology of the drug absorption site
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6
Q

What are some examples of Physicochemical properties effecting systemic absorption and bioavailability of a drug? (3)
Which of these is the biggest problem for drug delivery?

A
  • Drug pKa
  • log P
  • solubility
  • solubility
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7
Q

What are some examples of formulation factors effecting systemic absorption and bioavailability of a drug? (4)

A
  1. Type of formulation
  2. particle size
  3. surface area
  4. excipients
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8
Q

What are some examples of anatomy and physiology of the drug absorption site factors effecting systemic absorption and bioavailability of a drug?
(7)

A
  1. Transport routes & mechanisms
  2. GI motility
  3. pH
  4. Metabolism
  5. P-gp efflux
  6. Presence of food
  7. Individual variations
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9
Q

-acid in a an acid is

A

Unionized (less of it in solution)

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10
Q

-acid in a a base is

A

Ionized (more of it in solution)

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11
Q

-base in a base is

A

Unionized (more of it in solution

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12
Q

-base in an acid is

A

Ionized (more of it in solution)

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13
Q

What are ideal log P ranges?

Do most drugs follow these?

A

1-3

No

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14
Q

What are some dosage forms used for drugs?

7

A
  1. Solutions
  2. Emulsions
  3. Suspensions
  4. Powders
  5. Tablets
  6. Capsules
  7. Modified release granules, tablets & capsules (aka controlled, sustained, extended release)
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15
Q

What are dis-advantages to an oral delivery route?(4)

A
  1. Variability in patient population
  2. Adverse reactions
  3. Proteins & peptides cannot be delivered
  4. Metabolism & efflux issues
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16
Q

Why does particle size matter?

A

-Smaller particles of the same amount have much greater surface area. Smaller particles allow for greater dissolution

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17
Q

What is formulation are drugs in to give greatest surface area?

A

Micronized or microcrystalline drug forms

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18
Q

What are 5 examples of excipients?

A
  1. Wetting agents/ surfactants
  2. Diluents
  3. Binders (adhesives)
  4. Disintegrants
  5. Lubricants
19
Q

What is an excipient?

A

An excipient is a natural or synthetic substance formulated alongside the active ingredient of a medication

20
Q

What are wetting agents/ surfactants?An example? (2)What do they do?

A

-Surfactants are compounds that lower the surface tension between two liquids or between a liquid and a solid. Also help with absorption of drugs.-Polysorbate 80 and Sodium dodecyl sulfate

21
Q

What is a diluent?What are they for?

A

-Something used to bulk up drugs for oral consumption-Allow for a person to pick up a drug.-

22
Q

What are some examples of diluents? (3)

A

Lactose, dextrose, sucrose, microcrystalline cellulose

23
Q

Hydrophilic diluents cause …

A

rapid tablet disintegration (want the tablet to go all at once)

24
Q

Hydrophobic diluents …

A

decrease dissolution rate of drug (extended release)

25
Q

What is a binder?

A

Something that you organize your papers with. lulz jkHelp bind powders during the granulation processes & help with compression

26
Q

What are examples of binders?(3)

What is a particularly good binder?

A
  • Starch mucilage
  • gelatin
  • polyvinylpyrrolidone
  • Starch mucilage
27
Q

How can binders control drug release rate?

A

-For a slower release coating drug particles with starch (which is a slowly dissolving binder)-For faster release coating drug particles with gelatin or PVP (which are soluble binders)

28
Q

What is something to note about particles that are used in binding?

A

When you look at them they have very jagged edges.

29
Q

What are Disintegrants?What are they for?

A

-Swell in presence of water to burst open tablet-They are for rapid dissolution and higher bioavailability

30
Q

What are lubricants?What are they used for?What are two key properties they should have?

A

-substance introduced to reduce friction between surfaces in mutual contact-help tablet ejection from machines and; improve flow-Tend to be hydrophobic and; retard dissolution

31
Q

What are some examples of lubricants used in pharmacy?

A

Stearic acid its Mg and Ca salts widely used

32
Q

What is the pH of saliva?

What is transit time approximately?

A

pH: 6.5-7.5

Transit time: less than 1 minutes

33
Q

What is the pH of the stomach?

What is transit time approximately?

A

pH: 1-3.5
Transit time for liquids: 8-12 minutes
Transit time for solids: 144-277 minutes

34
Q

What is the pH of the duodenum?

What is transit time approximately?

A

pH: 5-7
Transit time for liquids: 2-60 minutes
Transit time for solids: 2-60 minutes

35
Q

What is the pH of the jejunum and Ileum?

What is transit time approximately?

A

pH: 6-7.5
Transit time for liquids: 1-3 hours
Transit time for solids: 1-5 hours

36
Q

What is the pH of the Colon?

What is transit time approximately?

A

pH: 5.5-7

Transit time: 12-48 hours

37
Q

What is the pH of the Rectum?

A

pH: 7

38
Q

What is something that the FDA requires on all tablets?

A

That they are able to disenergrate

39
Q

What happens to stomach pH as more food is consumed?

A

The pH increases (Volume of liquid expands)

40
Q

Liquids vs. solids which one gets processed faster by the GI tract?

A

Liquids

41
Q

What is the colons main job?

A

to reabsorb water

42
Q

Where are really hot or really cold foods kept until they reach a normal temperature?

A

The stomach

43
Q

What is pH in the GI tract most affected by?

A

Diet