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Phay 6 > Tableting > Flashcards

Tableting Flashcards

1
Q

Why make tablets

A
  1. mass production
  2. increased drug stability
  3. mask unpleasant taste of API
  4. simple and easy administration
  5. convenient and accurate doses
  6. can alter drug release rate
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2
Q
  1. Describe the properties of: bi-layer tablets; chewable tablets; minitabs; gastro-resistant tablets.
A

Bi-layer tablets have two layers – these may contain the same or different APIs. Can use to control the delivery rate of one/two APIs, etc.

Chewable tablets – formulated to effect slow release and local action of API, or for absorption of API in mouth for subsequent systemic action.

Minitabs (mini tablets) – small tablets with diameter ≤ 3 mm. Usually filled into a capsule or compressed into larger tablets. Can put many different types of minitab into a capsule, e.g. with different minitabs releasing drug at different times after administration.

Gastro-resistant tablets – outer layer of tablet does not dissolve at low pH, and so the API cannot be released in the stomach. Ensures API release lower down GI tract.

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3
Q

stages of powder compaction

A
  1. loose packing - air between particles
  2. dense packing = pre-compression eliminate air in between particles
    - brittle fracture of powder here is fine
  3. elastic deformation = reversible manner
    –> fragmentation - some particles may break
  4. plastic deformation = permanent shape change
    –> should stop tableting heree to get tablets
    –> held tgt by VDW
  5. brittle fracture of tablet
    –> brittle fracture of powder/granule is fine since it increases SA and increase bonding. Yet, brittle fracture of tablet not ok
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4
Q

what holds the tablet together

A
  1. Brittle fracture
    - Force - increase SA - more IMF - stronger tablet - but harder to remove from die - drug disintegration problem
  2. Deformation of tablet
    - just changing shape - no increase in SA - less IMF - weaker tablet- so easiler to remove from die = has less dissolution problems
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5
Q

successful tablet formulation must

A
  1. disintegrate
  2. release the drug
  3. fit for purpose
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6
Q

Successful powder formulation

A
  1. flows well
  2. not segregate
  3. be compressible
  4. be lubricated
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7
Q

excipients in direct compression

A
  1. Diluents
    - inert substance is added to increase bulk –> compressibility & API even distribution
    - insoluble drug = add hydrophilic diluents
    - good compati
  2. Disintegrants
    - to help breakup of tablets into individual granules/particles upon contact with water
  3. Lubricants & Glidants
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8
Q

Diluent requirements

A
  1. similar particle size to drug
  2. have good compressibility
  3. insoluble drug = hydrophilic diluent (if hydrophobic diluent used, hydrophobic diluents will stick to hydrophobic drug and not be released in body)
  4. good compatibility with drug
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9
Q

Disintegrant MoA

A
  1. Wicking - capilary forces promotes rapid water uptake into wtablet
  2. Swelling - water uptake causes tablet to swell
  3. Release of gases upon contact with water
  4. Melting at body temp
  5. Enzymatic destruction of binder
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10
Q

When is disintegrant added

A

2/3 before granulation
1/3 to dry granules

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11
Q

example of common excipients

A

MCC & Starch
- both dilluent & disintegrant
- saves money, and every product is checked

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12
Q

over lubrication
under lubrication

A

over = soft tablet that dissolves too quickly
under = sticking & picking (=ingredients stick to equipment)

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13
Q

how to select excipients for formulation

A
  1. chemical compatibility
  2. compressibility / fracture behaviour
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14
Q

direct compression mix composition

A
  1. drug
  2. disintegrant
  3. compression aid
  4. lubricant
  5. diluent
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15
Q

wet granulation composition

A
  1. drug
  2. disintegrant
  3. compression aid
  4. lubricant
  5. diluent
  6. binder
  7. colour/flavour
  8. granulation fluid
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16
Q

when to use super disintegrant

A

low drug solubility - super
large amt of binder has been used to form strong granule = super

17
Q

potential problems in tableting

A
  1. weight variation in tablets
  2. segmentation of granules/powders in hopper
  3. capping/lamination
  4. sticking
  5. picking
  6. chipping/cracking
  7. poor dissolution properties
18
Q

greater compaction leads to

A
  • greater hardness
  • reduced thickness
19
Q

compression pressure and temp

A

1-10MPa, up to 60˚c

20
Q
A

Phay 6 (8 decks)

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