L53 - Tablet Coating And Drug Release Flashcards

1
Q

What is tablet coating?

A

application of coating material to exterior of a tablet to confer beneficial properties as compared to uncoated

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2
Q

What are the 3 main types of coatings are in use?

A
  • sugar
  • film
  • tablet
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3
Q

Why do you coat tablets? (5)

A
  • ingredients need protection from environment
  • mask taste
  • easier to swallow
  • identification
  • controlled release or enteric
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4
Q

What does sugar coating do? (6)

A
  • prevent entry of water
  • subcoating - rounding, + calcium carbonate, talc in sucrose solution
  • smoothing
  • colouring
  • polishing
  • printing identification
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5
Q

What is film coating like? (3)

A
  • newly-launched coated products film coated
  • involved deposition (spraying) of thin film of polymer
  • coating liquid contains polymer with other ingredients in liquid
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6
Q

What is tablet coating like?

A

solution sprayed onto rotating, mixed tablet bed or fluid bed

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7
Q

What is the tablet like sugar vs film coating? (3)

A
  • rounded with polish / retains contour, not shiny
  • weight inc 30-50% / 2-3%
  • breaklines not possible vs possible
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8
Q

What is the process like sugar vs film coating? (3)

A
  • multistage / single stage
  • 8-12 hrs / 1.5-2 hrs
  • simple enteric coating / adaptable for controlled release
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9
Q

What are coating problems? (4)

A
  • picking/chipping
  • roughness
  • sticking
  • film cracking/peeling
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10
Q

What is does enteric coating do?

A

Protect the tablet core from disintegration in acid environment of stomach

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11
Q

Why use enteric coating? (4)

A
  • prevention of acid attack of drug unstable at low pH
  • protect stomach from irritation
  • facilitate absorption
  • taste masking
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12
Q

What are ideal polymers like? (2)

A
  • insoluble in aq media at low pH
  • abrupt, well defined inc in solubility at specific pH when inc
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13
Q

What are enteric polymers for direct film-coating? (2)

A
  • cellulose acetate phthalate - CAP
  • polyvinyl acetate phthalate - PVAP
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14
Q

what is enteric coat like?

A
  • sealing coat modified to comprise an enteric polymer acrylic derivative
  • sufficient weight required for efficiency, 2-3x simple film coating
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15
Q

what is delayed-release tablet like? (4)

A
  • drug core coated with delayed release memb (dry)
  • exposure to pH of SI (6.8) dissolves it
  • exposed drug core disintegrates
  • drug dissolves and is released
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16
Q

what is cumulative amount of drug released like from oral dosage forms? (3)

A
  • immediate - faster plateau
  • delayed - delayed plateau
  • extended - more linear til plateau
17
Q

what are typical enteric coating compositions? (5)

A
  • cellulose acetate phtalate, CAP
  • glyceryl triacetate
  • isopropyl alcohol
  • dichloromethane
  • water
18
Q

what are functional multi-particulate coatings like? (4)

A
  • provides opport for design of new m/r oral formulation
  • dose divided into 1000s spherical particles 0.5-2.0 mm
  • filled, encapsulated or compressed to tablet
  • used for C/R medicines w/ GR or ER properties or site specific drug delivery
19
Q

what are advantages of multiparticulates? (2)

A
  • more consistent GI transit than single dose
  • less likely to suffer from dose dumping
20
Q

what are disadvantages of multiparticulates? (2)

A
  • control of memb characteristics with film coating is difficult
  • they are difficult to retain in upper GI tractw
21
Q

what are properties of multiparticulates? (5)

A
  • good stability
  • good flow properties
  • high bulk density
  • v low hygroscopicity
  • easy to dose
22
Q

what are extruded/spheronised granulates? (2)

A
  • produced in modified granulating equip
  • drug granulates extruded thru // mesh under pressure = particles for spheronisation
23
Q

what are the different drug release mechs from multiparticulates? (3)

A
  • diffusion
  • osmosis
  • eroison
24
Q

what is diffusion of multiparticulates like? (4)

A
  • on contact with GI fluids
  • water enter interior by diffusion
  • dissolution occurs
  • drug diffuses across C/R coat
25
what is osmosis of multiparticulates like? (3)
- water enters - osmotic pressure builds up - forcing drug out
26
what is erosion of multiparticulates like? (2)
- some coatings designed to degrade gradually - releasing drug contained
27
what is enteric coating like in practice? (2)
- dont chew or crush - will dissolve in gastric fluid - dont take with antacid - pH of gastric fluid inc, might dissolve
28
What are multiple-unit pellet systems (MUPS)?
enteric coated particles compressed to tablet
29
what are MUPS like? (3)
- polymer coat flexible as compression forces applied - methacrylic acid copolymers suited - work on same principle as enteric coated granules in caps
30