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PHRM 100 – PDD > PDD 08: Solid Oral Dosage Forms – Excipients > Flashcards

PDD 08: Solid Oral Dosage Forms – Excipients Flashcards

1
Q

What are dosage forms?

A
  • different manners of drug substances present in market
  • unique in their physical and pharmaceutical characteristics
  • determines the physical form of the final pharmaceutical preparation
  • drug delivery system formed by technological processing
  • reflect therapeutic intentions, route of administrations, dosing etc.
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2
Q

What are some oral dosage forms?

A
  • tablets
  • capsules
  • powders
  • solutions
  • syrups
  • suspensions
  • magmas
  • gels
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3
Q

What are some parenteral dosage forms?

A
  • solutions
  • suspensions
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4
Q

What are some intraocular dosage forms?

A
  • solutions
  • suspensions
  • ointment
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5
Q

What are some sublingual dosage forms?

A
  • tablets
  • troches
  • lozenges
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6
Q

What are some intravaginal dosage forms?

A
  • suppositories
  • cream
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7
Q

What are some intranasal dosage forms?

A
  • solutions
  • sprays
  • inhalations
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8
Q

What are some intrarectal dosage forms?

A
  • suppositories
  • cream
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9
Q

What are some conjunctival dosage forms?

A
  • contact lens inserts
  • ointments
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10
Q

What are some solid dosage forms?

A
  • tablets
  • capsules
  • powders
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11
Q

What are some liquid dosage forms?

A
  • solution
  • syrup
  • emulsion
  • suspension
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11
Q

What are some semi-solid dosage forms?

A
  • cream
  • paste
  • gel
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12
Q

What are some gas dosage forms?

A
  • inhaler
  • aerosole
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13
Q

What are the advantages of oral solid dosage forms?

A

easier to patients:

  • non-invasive
  • easy administration
  • portable
  • palatable

easier to manufacturers:

  • established manufacturing process
  • accurate dosing
  • drug stability
  • easy to package, ship, and store
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14
Q

What are the disadvantages of oral solid dosage forms?

A

patients:

  • GI tract irritation
  • swallowing (large tablets/capsules)

manufacturers:

  • poor oral bioavailability/poor water solubility
  • formulations difficulties
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15
Q

What are the types of tablets?

A
  • compressed
  • film coated
  • enteric coated
  • rapid dissolving
  • layered
  • sugar coated
  • effervescent
  • controlled release
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16
Q

What do active pharmaceutical ingredients (APIs) do?

A

alter biological conditions

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17
Q

What do excipients do?

A

various actions during manufacturing, storage, and use

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18
Q

What is a pharmaceutical excipient?

A

pharmacologically inactive substances (no therapeutic effect) added to the API during product formulation to improve or modify:

  • bioavailability
  • stability
  • manufacturing
  • drug release
  • flavour
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19
Q

What are the ideal properties of pharmaceutical excipients? (4)

A

(all components must work together to create the desired product)

  • no interaction with drug
  • cost effective
  • pharmacologically inert
  • stable for handling
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20
Q

What are the types of excipients? (8)

A
  • diluents
  • binders
  • disintegrants
  • lubricants
  • glidants
  • colourants
  • sweeteners
  • flavouring
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21
Q

What are diluents?

A

make up largest proportion of tablet weight and volume

  • typical tablet weighs > 50 mg
  • imagine the difficulty of accurately dosing and handling potent APIs without a diluent
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22
Q

What do diluents do? (2)

A
  • dilute the drug
  • increase bulk volume of tablets for ease of handling
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23
Q

What are the characteristics of a good diluent? (7)

A
  • chemically inert
  • hydrophilic/water soluble
  • non-hygroscopic
  • palatable
  • compactable
  • cheap
  • biocompatible
24
Q

What are some common diluents?

A
  • lactose
  • cellulose
  • inorganic diluents
25
Q

What is lactose?

A
  • most common diluent
  • readily soluble in water
  • palatable
  • non-hygroscopic
  • good compactibility
  • inert
26
Q

What is cellulose?

A
  • second most common diluent
  • compactable
  • inert
  • hygroscopic
  • can also act as a binder/disintegrant
27
Q

What are inorganic diluents?

A
  • calcium phosphate
  • calcium carbonate
  • excellent compactibility
  • might interact with acids or base sensitive APIs
28
Q

What does selection of excipients require?

A

empirical testing and experience

  • hundreds of products are available for each type of excipient
29
Q

What do binders do?

A
  • important for tablet manufacturing
  • acts as adhesive to hold granules together
  • varying proportion of tablet formulation (1-20% w/w)
30
Q

What are some common binders?

A
  • starch
  • polyvinylpyrrolidone (povidone)
  • carboxymethyl cellulose
  • microcrystalline cellulose
  • acacia (Gum Arabic) forms very hard granules
  • sucrose and other sugars
  • gelatin
  • polyethylene glycol
31
Q

What do disintegrants do?

A

allow the tablet to break apart in the GI tract

32
Q

What is the disintegration time of tablets?

A

regulated by Pharmacopeia, ranging from 3 minutes for soluble tablets up to several hours for extended release formulations

33
Q

What is the mechanism of action of disintegrants?

A
  • facilitate water uptake to wet drug particles and excipients
  • swelling of disintegrant leads to rupture of tablet structure
34
Q

What is the main mechanism of disintegration?

A

capillary action (wicking), swelling and strain
recovery

  • disintegrants do not necessarily need to be soluble
  • in order to work properly disintegrants must be uniformly distributed through powder/granule mixture
  • added in varying proportion of tablet formulation (1-20% w/w)
35
Q

What are some common disintegrants?

A
  • starch
  • crosslinked polyvinylpyrrolidone (crospovidone)
  • sodium starch glycolate
  • sodium croscarmellose
  • microcrystalline cellulose
36
Q

What is starch?

A
  • partially water soluble, especially at higher temperatures
  • large surface area for water adsorption
37
Q

What is crosslinked polyvinylpyrrolidone (crospovidone)?

A
  • not soluble in water
  • readily absorbs water to promote swelling
38
Q

What is sodium starch glycolate?

A
  • carboxymethylated starch (higher solubility than starch)
  • can be internally crosslinked to form
39
Q

What is microcrystalline cellulose?

A
  • derived from partially depolymerized cellulose
  • degree of polymerization typically <400
  • can also act as a binder/diluent
40
Q

What do lubricants do?

A

reduce friction between particles

41
Q

What are lubricants added for?

A

ensure tablet formation and ejection occurs without friction

42
Q

What are lubricants?

A
  • often hydrophobic and may reduce dissolution times
  • small fraction of tablet composition (0.5-3%)
43
Q

What are some common lubricants?

A
  • magnesium stearate
  • stearic acid
  • polyethylene glycol (PEG) 4000-8000
  • sodium lauryl sulphate
  • liquid paraffin
44
Q

What are glidants used for?

A
  • added to the powders prior to compression to improve the flowability of powder or granules
  • forms a film over particles to create a smooth surface
45
Q

Why is flowability of tablet mass important?

A

critical for high production speeds

46
Q

What are some common glidants?

A
  • colloidal silicon dioxide (Aerosil)
  • talc (Mg6(SiO2)4(OH)4)
  • titanium dioxide
  • magnesium stearate
47
Q

What are the functions of colorants?

A
  • added for pharmaceutical elegance
  • increase compliance by creating optically attractive formulations
  • identification/branding
  • batch-to-batch uniformity
  • increase stability of photosensitive APIs
48
Q

What are the various classes of colourants used?

A
  • organic dyes (ie. Erythrosine, Sunset Yellow, Patent Blue V)
  • lakes (FD&C colours on a surface of alumina or other carriers, creates fast drying opaque layer)
  • inorganic colours – ie. ferric oxide (high light stability)
  • natural colours such as vegetable or animal colours
49
Q

What are the functions of sweeteners?

A

taste masking

50
Q

What are sweeteners important for?

A

lozenges, pediatric formulations, sublingual tablets, etc.

51
Q

What are sweeteners generally less of a consideration for?

A

tablets that are swallowed whole

52
Q

What are the two types of sweeteners?

A
  • bulk sweeteners
  • intense sweeteners
53
Q

What do bulk sweeteners do?

A

add texture and bulk to the formulation and usually make up large proportion of tablet

54
Q

What do intense sweeteners do?

A

provide sweetness at low concentrations

55
Q

What does the choice of sweetener depend on?

A

technical, regulatory, pharmacological considerations

  • patient population: caloric content, comorbidities (ie. aspartame cannot be metabolized by patients with Phenylketonuria)
  • flavour profile: many artificial sweeteners have unpleasant aftertaste
  • chemical compatibility – ie. phenylalanin plus aspartame results in poor heat and acid stability
  • processability
56
Q

What is the function of flavouring agents?

A

added to give tablets addition taste or flavour, particularly for taste masking

  • especially important for pediatric formulations
57
Q

What does flavouring usually match?

A

matches the colour to improve acceptability

58
Q

Where do flavouring agents come from?

A
  • derived from natural or synthetic sources such as menthol, vanillin, fruit flavours, etc.
  • sweeteners such as sucrose and sorbitol sometimes added as flavouring agent

PHRM 100 – PDD (14 decks)

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