Tabletting Flashcards

1
Q

what are tablets

A

single dose of compressed powder

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2
Q

why are tablets good

A

small, stable (no water and coating blocks light) , easy to identify with its colour/shape, taste masked by coating, packaging can be made water resistant

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3
Q

common shapes of tablets

A

round, oval, capsule
flat, bevelled, convex

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4
Q

name the stages of tablet manufacturing process

A

powder mixture of drug and excipients, wet/dry granulation then granules or direct compression, basing, compression into tablets, de-dusting, tablet coating, packing

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5
Q

what is basing

A

dry mixing in lubricant and more disintegrant if needed

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6
Q

list the 3 batch sizes

A

lab scale- formulation design stage
pilot scale- clinical trials
full scale industrial batch

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7
Q

what are excipients

A

inactive ingredient in drugs

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8
Q

what is the aim of a powder mixture

A

uniformly mixed, flows well, doesnt separate

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9
Q

what processes can cause powder separation and how

A

-transport, mixing, tablet machine vibration
-causes smaller particles to fall through the spaces between the bigger ones
-caused by difference in particle shape size and density

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10
Q

consequences of separation

A

variability in dosage which can lead to under or overdosing, uneven distribution of drug/excipients eg. some parts of the drug will have more disintegrant so it will be released faster than others

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11
Q

what is the aim of granulation (powder binded together forms granules)

A

prevent powder separation

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12
Q

describe wet granulation and its variables (know the diagram)

A

bowl, detector probe, rotating impeller and chopper, solution of binding agent sprayed onto powder, wet granules are dried then sieved

variables- mixing time, rate of adding liquid, speed of impeller and chopper, internal environments

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13
Q

stages of granule formation

A
  1. wetting and nucleation- small aggregates form from particles
  2. consolidation and coalescence- granules grow as aggregates combine

limits to granule growth- amount of fluid, breakage, attrition

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14
Q

how to detect granulation end point

A

trials or detector probes

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15
Q

what happens if you stop before the granulation end point

A

aggregates are under-wet, too fragile for drying process

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16
Q

what happens if you stop after the granulation end point

A

aggregates are over-wet, dry lumps are hard to compress

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17
Q

what is granulation end point

A

maximum amount of good granules

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18
Q

describe dry granulation (ribbon type) and its variables

A

hopper, screw feeder to ensure constant supply, powder is compacted between roles producing ribbons of compressed powder, ribbons are broken up then sieved to make granules

variables- feed rate, roller speed, moisture content of powder

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19
Q

difference between granules formed from wet and dry granulation

A

wet- particles glued together with binding agent (water soluble polymer)

dry-particles held by compression at points of contact

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20
Q

advantages and disadvantages of direct compression

A

advantages- saves money (no granulation equipment), saves energy, saves time, faster development time and less processes

disadvantages- mixture must flow, powder mix cant segregate, needs special excipients, hard on industrial scales

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21
Q

how are tablets compressed

A

using a rotary press or die and lower/upper punches

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22
Q

granule requirements for a good tablet to be formed

A

good flow- large round particle, fills die accurately to make uniform weight and dose

compactable powder mix- lots of inter particulate bonding, produces strong tablets, prevents capping/breaking

no separation- ensure composition of tablet stays the same, prevents deficiency in one component

right amount of lube- tablets can be ejected with minimum force, prevents them breaking due to high ejection pressure, too much can lead to weak tablets, machines struggles to eject if too little

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22
Q
A
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23
Q

why do tablets need the right amount of lubrication

A

to ensure tablets are ejected with minimum force, too much can break the tablets due to high ejection pressure, too little can be hard to eject, too much will have too little interparticulate bonds and form weak tablets

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24
why do powders need to resist separation
ensure tablet composition stays the same during production, ingredients may separate due to machine vibrations, tablets can become enriched or deficient in one component
25
why do powders need to be compactable
so strong/hard tablets can be produced, prevents lamination/capping/breaking, wont survive coating if its weak
26
how do powders compact
inter-particulate bonding
27
why do powders need to have good flow
ensures die fills accurately to prevent variation in weight and dose
28
main stages of tablet compression cycle (learn diagram)
1. dye filled with powder/granules 2. upper punch applies force down to make tablet and withdraws 3. lower punch ejects tablet
29
why doesnt the tablet fit the die anymore after its been ejected
elastic expansion
30
types of internal bonds formed during tabletting
interlocking, melting at contact points, molecular bonding (H bonds, VDW)
31
types of defects in tablets
laminations- horizontal cracks due to over compression capping- top comes off due to lamination chipping- edges chipped picking/sticking- surface pitted because material stuck to punches stress cracks- cracks due to elastic expansion after compression friability- edges erode, turns to powder
32
examples of problems in formulation
lots of elastic ingredients- tablet defects poor compression low mp- sticks to punch drug reacts with excipients wrong amount of lubricant
33
types of tablet machines
single punch- 50 tablets per min rotary- multiple punches, 20,000 per min, pilot and full scale manufactures compaction simulator- single punch, one at a time
34
tablet coating process
uncoated tablet, none/sugar/film/compression coating, cleaning and polishing, packing
35
sugar coating process (diagram) and its variables
1. coating liquid poured onto tablet bed at intervals 2. pan rotates and coats tablets evenly 3. hot air blown to dry coat then more liquid is added, thin layers produce a thick sugar coat variables- rate of liquid added, pan rotation, air flow, air temperature
36
film coating process and variables (diagram)
1. coating liquid continuously sprayed onto tablet bed 2. drum rotates and spreads liquid over tablets 3. hot air goes in and liquid evaporates and leaves a solid polymer film variables- spray rate, drum rotation speed, temperature, air flow
37
what does film coating liquid contain
polymer latex- no organic solvents plasticiser- helps particles coalesce colour- fine suspension lake surfactant- helps spread liquid separating agent- tablets become sticky during drying
38
compression coating process (diagram)
1. weak tablet formed 2. coating formulation compressed onto it 3. double compression makes tablet stronger
39
why are bulking agents needed
make tablets big enough to swallow
40
examples of some bulking agents
sugars, minerals, polymers glucose, talc, starch, microcrystalline cellulose
41
desirable characteristics of bulking agents
good compactability, good flow, chemically compatible with drug, cheap
42
why are compression aids needed
make strong tablets when ingredients are poorly compactible
43
example of a compression aid
microcrystalline cellulose
44
desirable characteristics of compression aids
excellent compactability and plastically deforms so it flows so it maximises bonding in tablets
45
structure of cellulose
linear polymer of glucose bonded together by glycosidic bonds, forms layers connected by hydrogen bonding, chains slip under pressure and H bonds break and reform
46
issues with MCC as a compression aid
more expensive than bulking agents, hygroscopic so needs to be stored in a dry place, doesnt flow well when damp
47
what is MCC
microcrystalline cellulose
48
what is the function of disintegrants and common examples
accelerate the break up tablet when exposed to fluid, releases drug for dissolution examples- starch, MCC, sodium starch glycollate
49
mechanism of disintegrants
swelling- disintegrant sweels and tablet bursts apart eg. starch wicking- water drawn in through network of disintegrant fibres and soluble materials inside tablet dissolve eg. MCC effervescent material- make CO2 gas to break tablet
50
why is an insoluble disintegrant good
tabletting part 3 page 22 idk
51
problems with disintegrants
elastic so weakens tablets, less effective if wetted or high humidity, superdisintegrants interact with drugs to form salts
52
why are lubricants needed and common examples
lubricates ejection of tablet from die after compression eg. magnesium stearate, SDS, stearic acid
53
mechanism of lubricants
particles are stacks of flat, waxy crystals which can slide over each other
54
issues with magnesium stearate as a lubricant
hydrophobic, makes drug water repellent which reduces drug dissolution, slows drug release, weakens inter-particulate bonding during compression so weaker tablets are formed
55
what is the function of flow aids and common examples
increases flowability of power/granules, good flow is important examples- colodial silicon dioxide
56
mechanism of flow aids
coats surface of particles, adsorbs surface moisture so they dont stick together
57
issues of flow aids
dust hazard
58
types of tablets
chewable/dispersable, immediate release, delayed release, extended release, tablets for special routes
59
types of chewable tablets
effervescent tablets, tablets that dissolve rapidly in mouth
60
how do dispersible tablets release drugs
dissolve in water/saliva, solution/suspension of drug, drug solution in GI tract, diffuses through gut wall and bloodstream absorbs drug molecules
61
where are most drugs absorbed
upper small intestine
62