Pharmaceutics - Tableting and Roller Compacting Flashcards

1
Q

what are advantages of tablets?

A
  • Portable and convenient.
  • Accurate dosing.
  • Large GI surface area for drug absorption.
  • Solid dosage form stable.
  • Scalable for mass production.
  • MR formulations.
  • Excellent patient acceptability
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2
Q

what are the disadvantages of tablets?

A
  • Degradation by pH or enzyme in GI tract.
  • Not suitable if patient unconscious or dysphagic.
  • Difficult to withdraw therapy.
  • Food effects on drug absorption
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3
Q

what are the types of tablets based on their mode of administration?

A

oral
effervescent
sublingual
buccal

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4
Q

what are the types of tablets based on their release profile?

A
IR (Immediate Release)
ME (Modified Release)
DR (Delayed Release)
ER (Extended Release)
SR (Sustained Release)
CR (Controlled Release)
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5
Q

what do all medicines typically contain?

A
  1. Drug
  2. Filler
  3. Binder
  4. GLidant
  5. Lubricant
  6. Anti-adherent
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6
Q

What other excipients do IR tablets have besides the norm in other drugs?

A

disintegrants and coating

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7
Q

What other excipients do MR tablets have besides the norm in other drugs?

A

coating and matrix former

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8
Q

what is wet granulation?

A

Aggregation of primary particles using binder solution.

two types: (Shear granulation, fluidised bed granulation)

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9
Q

what is dry granulation?

A

Aggregation of primary particles using solid binders.

two types: (Slugging or roller compaction followed by milling)

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10
Q

what is direct compression?

A

Compaction of primary particles on tablet press without the need of granulation. Uses dry binders and cohesive powder

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11
Q

Explain the dry granulation technique and give an example of one?

A
  • dry granulation is the compaction of powders into a ribbon which is then milled into granules.
  • an example is roller compaction
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12
Q

what are the different compartments of a roller compaction and describe their roles?

A
  • Feeder unit: feeds powder to compaction rollers.
  • Compaction unit: Pair of rollers rotating in opposite directions compact powder into ribbon.
  • Size reduction unit: Mills compacted ribbon into granules.
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13
Q

what is a single-station tablet press?

A
  • a device driven by an eccentric motor with a low throughput (i.e. doesn’t make many tablets).
  • it compresses the powders then ejects them as tablets
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14
Q

what is a multi-station (rotary) tablet press?

A
  • a tablet press driven by rolls and cams
  • presses the powder on a rotating turret to form a tablet on ejection
  • has a high throughput
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15
Q

explain the compaction cycle?

A
  1. Filling
  2. Compression
  3. Ejection
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16
Q

what are the types of tablet defects?

A
  1. Capping: Top of tablet separates from main body.
  2. Lamination: Tablet body separates into layers.
  3. Cracking: Capping and/or lamination.
  4. Mottling: Uneven surface colour distribution.
  5. Chipping: Material removed from edges of friable tablets.
  6. Sticking: Powder adheres to punches.
  7. Picking: Embossed detail removed from tablet surface.
17
Q

what causes cracking in tablets?

A

-Air entrapment;
-inadequate dwell time;
-excessive die wall
friction.

18
Q

what causes mottling in tablets?

A
  • Inadequate mixing;

- solute migration.

19
Q

what causes sticking of tablets?

A

Adhesive powder.

20
Q

what is the solution to cracking?

A

-Pre-compression;
-tapered die;
-increase
dwell time;
-lubrication

21
Q

what is the solution to mottling?

A
  • Adequate mixing;
  • avoid static bed drying;
  • coating.
22
Q

what is the solution to sticking?

A

-Anti-adherent;
-non-stick coating of punches;
-increase dwell time;
-particle size and
humidity control.

23
Q

what is an osmotic system?

A

when the drug is forced through the orifice in the tablet coating by hydrostatic pressure

24
Q

what is a gastroretentive dosage form?

A

one which is retained in the stomach for drug release

25
Q

what is therapeutic threshold?

A

Minimum plasma concentration that produces a therapeutic effect.

26
Q

what is Toxicity threshold?

A

Minimum plasma concentration that

produces a toxic effect.

27
Q

what is therapeutic window?

A

Range of plasma concentration between therapeutic threshold and toxicity threshold.

28
Q

what is plasma half-life?

A

Time taken for drug concentration in plasma to halve (t1/2).

29
Q

what is clearance?

A

Removal of drug from plasma, responsible for

decline in plasma drug concentration and thus t1/2.

30
Q

what is duration of action?

A

Time plasma concentration remains in therapeutic window.

31
Q

what are some advantages of using extended release formulations?

A
  1. Extend t1=2.
  2. Keep plasma concentration within therapeutic window.
  3. Increase duration of action.
  4. Reduce dosing frequency.
  5. Improve medication adherence.
  6. Enhance therapeutic outcome.
32
Q

what types of drugs are extended release formulations more suited for?

A
  1. drugs with short half life in the immediate release form

2. drugs with a narrow therapeutic window

33
Q

what is a disadvantage of using extended release drugs?

A

causes dose dumping

34
Q

what is dose dumping?

A

when a significantly larger dose fraction than

intended is released over a short duration, leading to initial overdosing and subsequent under dosing.

35
Q

when does a drug become toxic?

A

when the plasma concentration of the drug exceeds the toxicity
threshold.

36
Q

what can cause dose dumping?

A
  1. Alcohol consumption (as it can dissolve the excipient controlling the drug release rate hence causing a large amount of drug to be released at once)
  2. incorrect use of the ER tablets (splitting, chewing, crushing), which destroys the mechanism for controlling the drug release rate