tabletting part 3 Flashcards

(85 cards)

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
example of superdisintegrant?
sodium croscarmellose
26
what is the function of a lubricant?
makes sure tablet is ejected out of the die with limited friction
27
common examples of lubricants?
magnesium stearate SDS stearic acid
28
disadvantages with magnesium stearate?
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
29
structure of lubricants?
long hydrocarbon chains stacks of flat waxy crystals so easy to slide over each other
30
function of flow aids?
increases flowability
31
examples of flow aids?
colloidal silicon dioxide
32
structure and function of flow aids?
smaller than other excipients in size coats surfaces of particles and absorbs moisture so they don't stick
33
disadvantages of flow aids?
dust hazard
34
types of tablets?
dispersible immediate release delayed release extended release tablets for special use
35
diagram of how dispersible tablets work?
slide 17
36
where is the absorption of most drugs?
upper small intestine by duodenum and jejunum
37
how are duodenum and jejunum adapted for absorption?
have vili on their surface increasing surface area
38
requirements for tablets hat rapidly dissolve in saliva?
'palatable rapid disintegration in mouth flat thin porous to maximise surface area for dissolving'
39
what is included in the formulation design?
soluble bulking agents wetting agents flavours disintegrants solubility enhancers
40
what considerations required for the packing of tablets that rapidly dissolve in saliva?
water proof pack so double aluminium foil because its hygroscopic
41
requirements for effervescent tablets?
should disintegrate rapidly palatable big tablet so it isn't directly swallowed
42
what is the formulation design for effervescent tablets?
soluble bulking agents wetting agents solubility enhancers flavours
43
pack considerations for effervescent tablets?
hygroscopic so pack has to be waterproof
44
requirements for chewable tablets?
bigger than usual flat- chewable palatable
45
formulation design for chewable tablets?
flavours sweeteners immediate release tablets
46
what are the requirements for packaging of chewable tablets?
hygroscopic so water proof package with double aluminium foil
47
what are chewable tablets use for?
drugs that need large doses and don't taste too bad small dose drugs formulated into chewable tablets
48
what are the requirements for lozenges?
dissolve slowly in the mouth palatable
49
formulation design for lozenges?
compressed powder tablets sweeteners no disintegrant no wetting agents as for immediate release tablets
50
requirements for lozenges packaging?
as for immediate release tablets
51
what are lozenges used for?
sore throat
52
how are immediate release tablets dissolved into the bloodstream?
'swallowed coating dissolves disintegrant absorbs stomach juices and the tablet swells disintegration happens dissolution occurs drug is in solution now and is absorbed'
53
what are the requirements for IR tablets?
should disintegrate in stomach size that can be swallowed palatable (taste masking)
54
what is the formulation design for IR tablet?
bulking agents compression aid disintegrant flow aid binder lubricant
55
what is the pack requirement for IR tablets?
hygroscopic
56
what is the point of packaging?
designed to protect tablet
57
what are the three blister packages?
transparent plastic semi-transparent double aluminum foil
58
requirements for delayed release tablets?
remains in tact and no drug released in the stomach disintegrates rapidly in neutral ph of upper intestine
59
what is the formulation design for delayed release tablets?
polymer coating that is gastro-resistant as for immediate release
60
what is the packaging for delayed release tablets?
hygroscopic
61
what are DR tablets used for?
to protect stomach form irritation causes by drug to protect tablet against stomach acid
62
how are DR tablets absorbed?
'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
requirements for extended release tablets?
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
what is the formulation design of the extended release drug?
coated or matrix coated no disintegrant
65
packaging for extended release tablets?
hygroscopic
66
what are extended release tablets used for?
for daily dosing a few time with short half-life for prolonged therapy
67
how are extended release coated tablets absorbed in the body?
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
what are the different coatings for an extended release tablet?
diffusion barrier coating phase separate diffusion barrier coat phase separated porous coat
69
how does diffusion barrier coating work?
release of drug controlled by diffusion through permeable coat
70
how does phase separated diffusion barrier coat work?
drug diffuses through one component of the coat
71
how does phase separated porous coat work?
drug released through holes in the coating when component is dissolved
72
what is the rate controlling factor when drug is diffusing?
water
73
how are extended release matrix tablets absorbed in the body?
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
difference types of matrix?
inert matrix at low drug loading inert matrix at high drug loading hydrophilic matrix wax matrix
75
what is inert matrix low drug loading?
when drug is released by diffusion through matrix
76
what is inert matrix at high drug loading?
drug released through percolation channels
77
what is hydrophilic matrix?
polymer in tablet hydrates forming gel layer (a surface diffusion barrier) drug released via diffusion through this layer
78
what is wax matrix?
surface erodes as it goes through GI tract and particles dissolve when they've reached the surface
79
requirements vaginal tablets?
release drug in vagina shaped for easy insertion
80
formulation of vaginal tablets?
hygroscopic
81
what are vaginal tablets?
local effects only
82
requirements buccal and Sublingual Tablets and Lozenges?
drug release in mouth if immediate release-should dissolve quickly if extended release- retained for a long time
83
what is the formulation design?
for immediate release: dispersible tablets-very fast release immediate release lozenges for extended release: as hydrophilic matrix mucoadhesive
84
what is the packaging for lozenges?
hygroscopic
85
what are Buccal and Sublingual Tablets and Lozenges used for?
local effect- mouth ulcer systematic effect- angina relief