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The Science Of Medicines (PHAR 1021) year 1 > tabletting part 3 > Flashcards

tabletting part 3 Flashcards

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1
Q

what is the function of bulking agents?

A

‘making tablets that are big enough to swallow and handle’

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2
Q

common examples of bulking agents?

A

sugars, sugar alcohols, minerals, polymers, Spray Dried Lactose, Lactose monohydrate - crystalline

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3
Q

what are desirable characteristics of bulking agents?

A

good compactability
good flow
chemically compactable with drug
inexpensive
available in different grades of size and shapes

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4
Q

what does good compactability mean?

A

strong tablets formed at low pressures

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5
Q

what is required for good flowing tabelts?

A

particles that are round

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6
Q

what is spray dried lactose good for?

A

compresses really well because it has anhydrous lactose
good for direct compression
large crystals give good flowability

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7
Q

properties of lactose monohydrate-crystalline?

A

poor compressibility
good for wet granulation because with large crystals it takes longer to dissolve so more control over the end point of the granulation

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8
Q

what is the function of compression aids?

A

to make tablet stronger when particles don’t compact well

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9
Q

common example of compression aid?

A

Microcrystalline cellulose (MCC)

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10
Q

desirable characteristics of compression aids?

A

‘compactable
plastically deforms so maximised bonding inside tablet’

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11
Q

what is cellulose?

A

linear polymer of glucose

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12
Q

what is the function of an disintegrant?

A

makes the break up of tablets faster when exposed to fluids and releases drug particles

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13
Q

what is starch?

A

swelling disintregrant

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14
Q

how is starch a disintegrant?

A

OH groups to attach to water

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15
Q

what is a polymorph?

A

crystalline forms of drugs

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16
Q

what are the disadvantages of lactose?

A

you need a compression aid present with other tablets that are poorly compressible
lubricants weaken bonding
causes browning of tablets with the aldehyde group

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17
Q

disadvantages of MCC

A

more expensive than bulking agents
hygroscopic so has to be stored in a dry place
if damp it doesn’t flow well

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18
Q

properties of of MCC?

A

‘chains that are stacked into orderly manner
under pressure the chain slips and it has a plastic behaviour’

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19
Q

examples of disintegrants?

A

MCC, starch

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20
Q

disadvantages of disintegrants?

A

elastic- tablets are made weaker

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21
Q

what are the mechanisms for disintegrants?

A

swelling-swells causing tablet to burst
wicking- water drawn in through fibres
effervescent- co2 produced

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22
Q

what is MCC?

A

wicking disintegrant

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23
Q

properties of MCC?

A

cellulose fibres

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24
Q

properties of super disintegrant?

A

they attract water
cellulose polysaccharide chain
crosslink limits swelling forming an insoluble sponge

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25
Q

example of superdisintegrant?

A

sodium croscarmellose

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26
Q

what is the function of a lubricant?

A

makes sure tablet is ejected out of the die with limited friction

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27
Q

common examples of lubricants?

A

magnesium stearate
SDS
stearic acid

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28
Q

disadvantages with magnesium stearate?

A

hydrophobic so when rubbed over other particles it makes them water repellent which decreases drug dissolution
weakens inter-particulate bonding so weaker tablets
so mixed for a short time
SDS can be an alternative but not as effective

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29
Q

structure of lubricants?

A

long hydrocarbon chains
stacks of flat waxy crystals so easy to slide over each other

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30
Q

function of flow aids?

A

increases flowability

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31
Q

examples of flow aids?

A

colloidal silicon dioxide

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32
Q

structure and function of flow aids?

A

smaller than other excipients in size
coats surfaces of particles and absorbs moisture so they don’t stick

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33
Q

disadvantages of flow aids?

A

dust hazard

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34
Q

types of tablets?

A

dispersible
immediate release
delayed release
extended release
tablets for special use

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35
Q

diagram of how dispersible tablets work?

A

slide 17

36
Q

where is the absorption of most drugs?

A

upper small intestine by duodenum and jejunum

37
Q

how are duodenum and jejunum adapted for absorption?

A

have vili on their surface increasing surface area

38
Q

requirements for tablets hat rapidly dissolve in saliva?

A

‘palatable
rapid disintegration in mouth
flat
thin
porous to maximise surface area for dissolving’

39
Q

what is included in the formulation design?

A

soluble bulking agents
wetting agents
flavours
disintegrants
solubility enhancers

40
Q

what considerations required for the packing of tablets that rapidly dissolve in saliva?

A

water proof pack so double aluminium foil because its hygroscopic

41
Q

requirements for effervescent tablets?

A

should disintegrate rapidly
palatable
big tablet so it isn’t directly swallowed

42
Q

what is the formulation design for effervescent tablets?

A

soluble bulking agents
wetting agents
solubility enhancers
flavours

43
Q

pack considerations for effervescent tablets?

A

hygroscopic so pack has to be waterproof

44
Q

requirements for chewable tablets?

A

bigger than usual
flat- chewable
palatable

45
Q

formulation design for chewable tablets?

A

flavours
sweeteners
immediate release tablets

46
Q

what are the requirements for packaging of chewable tablets?

A

hygroscopic so water proof package with double aluminium foil

47
Q

what are chewable tablets use for?

A

drugs that need large doses and don’t taste too bad
small dose drugs formulated into chewable tablets

48
Q

what are the requirements for lozenges?

A

dissolve slowly in the mouth
palatable

49
Q

formulation design for lozenges?

A

compressed powder tablets
sweeteners
no disintegrant
no wetting agents
as for immediate release tablets

50
Q

requirements for lozenges packaging?

A

as for immediate release tablets

51
Q

what are lozenges used for?

A

sore throat

52
Q

how are immediate release tablets dissolved into the bloodstream?

A

‘swallowed
coating dissolves
disintegrant absorbs stomach juices and the tablet swells
disintegration happens
dissolution occurs
drug is in solution now and is absorbed’

53
Q

what are the requirements for IR tablets?

A

should disintegrate in stomach
size that can be swallowed
palatable (taste masking)

54
Q

what is the formulation design for IR tablet?

A

bulking agents
compression aid
disintegrant
flow aid
binder
lubricant

55
Q

what is the pack requirement for IR tablets?

A

hygroscopic

56
Q

what is the point of packaging?

A

designed to protect tablet

57
Q

what are the three blister packages?

A

transparent plastic
semi-transparent
double aluminum foil

58
Q

requirements for delayed release tablets?

A

remains in tact and no drug released in the stomach
disintegrates rapidly in neutral ph of upper intestine

59
Q

what is the formulation design for delayed release tablets?

A

polymer coating that is gastro-resistant
as for immediate release

60
Q

what is the packaging for delayed release tablets?

A

hygroscopic

61
Q

what are DR tablets used for?

A

to protect stomach form irritation causes by drug
to protect tablet against stomach acid

62
Q

how are DR tablets absorbed?

A

‘tablet swallowed
coating is resistant to stomach acid so tablet passed through
polymer coat ionises and dissolves at intestinal ph
tablet disintegrant and releases the entire dose’

63
Q

requirements for extended release tablets?

A

gradual release of drug
drug release should continue in all conditions of GI tract
dose shouldn’t be release at once
should contain enough drug to be released gradually over a long time

64
Q

what is the formulation design of the extended release drug?

A

coated or matrix coated
no disintegrant

65
Q

packaging for extended release tablets?

A

hygroscopic

66
Q

what are extended release tablets used for?

A

for daily dosing a few time with short half-life
for prolonged therapy

67
Q

how are extended release coated tablets absorbed in the body?

A

tablet swallowed
the coating controls rate of release of drug
no disintegration
drug released slowly through transport in the GI tract
all drug is slowly released

68
Q

what are the different coatings for an extended release tablet?

A

diffusion barrier coating
phase separate diffusion barrier coat
phase separated porous coat

69
Q

how does diffusion barrier coating work?

A

release of drug controlled by diffusion through permeable coat

70
Q

how does phase separated diffusion barrier coat work?

A

drug diffuses through one component of the coat

71
Q

how does phase separated porous coat work?

A

drug released through holes in the coating when component is dissolved

72
Q

what is the rate controlling factor when drug is diffusing?

A

water

73
Q

how are extended release matrix tablets absorbed in the body?

A

tablet swallowed
matrix material controls the rate of release of drug and drug released slowly through GI tract
most matrix gradually erode through the GI tract

74
Q

difference types of matrix?

A

inert matrix at low drug loading
inert matrix at high drug loading
hydrophilic matrix
wax matrix

75
Q

what is inert matrix low drug loading?

A

when drug is released by diffusion through matrix

76
Q

what is inert matrix at high drug loading?

A

drug released through percolation channels

77
Q

what is hydrophilic matrix?

A

polymer in tablet hydrates forming gel layer
(a surface diffusion barrier)
drug released via diffusion through this layer

78
Q

what is wax matrix?

A

surface erodes as it goes through GI tract and particles dissolve when they’ve reached the surface

79
Q

requirements vaginal tablets?

A

release drug in vagina
shaped for easy insertion

80
Q

formulation of vaginal tablets?

A

hygroscopic

81
Q

what are vaginal tablets?

A

local effects only

82
Q

requirements buccal and Sublingual Tablets and Lozenges?

A

drug release in mouth
if immediate release-should dissolve quickly
if extended release- retained for a long time

83
Q

what is the formulation design?

A

for immediate release:
dispersible tablets-very fast release
immediate release
lozenges
for extended release:
as hydrophilic matrix
mucoadhesive

84
Q

what is the packaging for lozenges?

A

hygroscopic

85
Q

what are Buccal and Sublingual Tablets and Lozenges used for?

A

local effect- mouth ulcer
systematic effect- angina relief

The Science Of Medicines (PHAR 1021) year 1 (20 decks)

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