D6 What holds tablets together and excipients Flashcards

(53 cards)

1
Q

where does the compression of powders into tablets occur?

A

occurs in tableting machine (press)

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2
Q

list the tableting compression stages

A
  • filling of die
  • particle rearrangement
  • elastic deformation at points of contact
  • fragmentation / plastic deformation
  • bonding
  • plastic deformation of the solid body
  • decompression and ejection
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3
Q

explain the stage of tableting compression: filling of die

A
  • powder flows uniformly down and die is filled to its volume
  • glints are important here for promoting good flow
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4
Q

explain the stage of tableting compression: particle rearrangement

A

pressure starts being applied and loosely packed powders rearrange to expel air between particles and arrange more closely packed together

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5
Q

explain the stage of tableting compression: elastic deformation at points of contact

A
  • as more pressure is applied, the particles start to elastically deform
  • particles are coming together like people do in a crowd
  • if pressure stopped being applied, particles would return to their original shape
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6
Q

explain the stage of tableting compression: fragmentation and / or plastic deformation

A
  • pressure is continued to apply and particles fragment into small pieces or just plastically deform depending on the particle’s properties
  • either of the above can happen or both. if there are different particles in the powder mixture
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7
Q

explain the stage of tableting compression: bonding

A
  • even more pressure leads to particles bonding together
  • binder is the important excipient for this stage and for promoting bonding of particles together
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8
Q

which excipients are important for decompression and ejection of tablets

A
  • lubricants
  • similar to butter in a cake tin
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9
Q

what excipient is important for bonding in tableting?

A
  • binder
  • promotes bonding of particles together
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10
Q

what is the difference between elastic deformation and plastic deformation?

A
  • elastic deformation is reversible and temporary
  • plastic deformation is not reversible or temporary
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11
Q

what is capping pressure?

A
  • when compressing powders, there will also be air inside that can’t be expelled
  • if you have too much hair or you compress the tablets too much to be very dense, the air expands after compression and breaks the tablets
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12
Q

what is the relationship between water and hard tablets?

A
  • harder for water to penetrate and disintegrate harder tablets because the particles are packed very densely and water can’t penetrate gaps
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13
Q

what differences between tablets of the same drug can affect bioavailability?

A

same drug made into two tablets at different pressures (different hardness)

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14
Q

state the 3 theories for how tablets are held together

A
  • mechanical theory
  • intermolecular theory
  • liquid surface film theory
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15
Q

describe and explain the mechanical theory of how tablets are held together

A
  • mechanical interlocking of particles
  • particularly relevant when powder particles undergo plastic deformation during compression
  • molecules assume such a shape that they interlock together and do not come apart when pressure is removed
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16
Q

describe and explain the intermolecular theory of how tablets are held together

A
  • contact between new surfaces close enough so that Van Der Waals forces can act
  • particularly relevant when powder particles fracture during compression
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17
Q

what causes the liquid surface film theory?

A

surfaces melt (or dissolve in residual moisture) under applied pressure and upon the release of the pressure the melted (dissolved) material crystalline forming connections between the particles

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18
Q

where is pressure felt more in the liquid surface film theory? what does this mean?

A
  • pressure is felt more at the points where particles touch each other
  • this means you do not feel pressure equally everywhere
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19
Q

what 2 things can high pressure at points of contact do in the liquid surface film theory?

A
  • surface can melt at touching points so when pressure is removed, molten bridge remains and particles stick together
  • residual moisture that is present in powder turns into water at points of contact and dissolve a bit of each particle so the solution of dissolved material makes bridges between the touching particles and they stick together
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20
Q

what are excipients?

A

pharmaceutical substances other than the active drug or prodrug which has been appropriately evaluated for safety and are included in a drug delivery system

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21
Q

state 4 things that excipients can do

A
  • aid processing of the system during manufacture
  • protect, support or enhance stability, bioavailability or patient acceptability
  • assist in product identification
  • enhance any other attribute of the overall safety and effectiveness of the drug product during storage and use
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22
Q

what 3 excipients could be used to provide essential manufacturing technology functions?

A

binders
glidants
lubricants

23
Q

what 2 excipients can be used to enhance patient acceptance?

A

flavours
colourants

24
Q

what excipients could be added to provide aid in product identification?

25
what 4 excipients can be added to tablets to optimise or modify drug release?
disintegrants coating polymers hydrophilic-swelling polymers wetting agents
26
what do disintegrants do?
help with water absorption in the patient's stomach to aid disintegration
27
what types of tablets are flavours particularly important for?
'melts'
28
describe the function of fillers as excipients
- compromise bulk of tablet - make a tablet size practical for patient - at low dose, drug adsorption to filler can be an issue for drug bioavailability - fillers should not be used that can absorb drug
29
describe the quantities of very potent drugs in tablets
small quantities due to drug adsorption to filler
30
state 5 soluble filler excipients
lactose sucrose dextrose mannitol sorbitol
31
state insoluble filler excipients
calcium sulphate, dihydrate calcium phosphate, dibasic calcium carbonate starch modified starches microcrystalline cellulose
32
what is the function of binders as excipients?
provide cohesiveness required from granule, provide cohesiveness to a final tablet
33
state 3 things that binders can affect
granule uniformity ease of compression hardness of tablet
34
what is the most common binder excipient?
polyvinylalcohol
35
what is the function of glidants as excipients?
improve powder flow
36
how do glidants act as excipients?
- act by keeping particles apart as they form a thin film on the particle surface (smooths surface of granules to keep distance between particles) - increase the particle distance and consequently lower cohesion forces
37
typically, what kind of materials are glidants?
- low dielectric constant materials - reduce electrostatic cohesive forces between powder particles
38
describe the flow of different types of granules
rough, non-spherical granules flow less well than organised, smooth spherical granules
39
what property of powder is particularly important in the tableting process?
- flow rate of powder - adequate flow from the hopper into the die cavity
40
state 5 things that powder flow is a function of
- particle size - particle shape - the roughness of the particle surface - the chemical nature of the powder - the moisture content
41
describe and explain the flow of a powder with particles sized 200-250 micrometers
- good flow - mass of individual particle is relatively large
42
describe and explain the flow of a powder with particles sized 75-250 micrometers
- flow may be a problem - mass of individual particle is relatively small and increased surface area amplifies effects of surface forces
43
describe and explain the flow of a powder with particles sized 75-100 micrometers
- flow becomes a problem in most cases - cohesive forces, free surface energy and / or static electrical forces are large relative to particle size
44
flow problems may occur due to too fine particles. how can these problems be solved?
- particle enlargement - achieved by granulation
45
state 3 common glidants
colloidal silica dioxide magnesium stearate talc
46
describe the function of lubricants as excipients
- reduce friction between powder particles and die during compression and ejection of tablet - ease ejection of tablet from die - prevent sticking of tablet to punches - prevent excessive wear of punches / dies
47
how do lubricants act?
- by forming an adsorbed lubricant layer around the particles during mixing - (most of the lubricant will end up round the sides of the tablet, not inside)
48
explain why some lubricants are tricky to control
- they need to coat the sides of the tablet but if there is loads of lubricant between particles when compressing, particles won't be able to come close enough together to interlock, bond or stick together - too much lubricants can lead to tablets crumbling apart because you can't apply sufficient pressure to get particles to stick together - water also does not penetrate tablets as well if there is lots of lubricant round the sides
49
state 6 lubricant excipients
- magnesium stearate (most common) - sodium stearate - stearic acid - aluminium stearate - calcium stearate - polyethylene glycol 6000
50
what can too much lubricant in tablets cause?
can reduce bonding properties of powder particles, disintegration of tablet and decreased tablet strength
51
describe the function of colouring agents in tablets as excipients
- assist in product visual identification and provide acceptable appearance
52
what must all colourants be approved by?
all colourants used in pharmaceuticals must be approved and certified by the FDA
53
when are colourants often added in tablet production?
- during coating but can also be included in the formulation prior to compaction - in the latter case, the colourant can be added as a soluble dye (wet granulation process) or insoluble (direct compression)