Tablets Flashcards

1
Q

What are disadvantages of tablets

A
  • Poor bioavailability of poorly soluble drugs (class 4)
  • compression can change the physical properties, particle size & crystal form
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2
Q

Explain Class 1 drugs
strategies to improve?
Example

A

High solubility, High permeability
Immediate-release
Choloroquine diphosphate

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3
Q

Explain Class 2 drugs
strategies to improve?
Example

A

Low solubility, High permeability
Particle size reduction, salt formation, solid dispersions, complexation, lipid formulations
Ibuprofen

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4
Q

Explain Class 3 drugs
strategies to improve?
Example

A

High solubility, Low permeability
permeation, enhancers, prodrugs, bioadhesives
Captopril

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5
Q

Explain Class 4 drugs
strategies to improve?
Example

A

Low solubility, Low permeability
Combination of methods or not feasible for oral, use IV administration
Furosemide

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6
Q

What is considered a highly permeable drug?
Highly soluble?

A

Highly permeable: absorption over 90% of dose
Highly soluble: when highest dose strength is soluble in 250mL or less at 37 degrees pH 1-7

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7
Q

When are Multiple Compressed Tablets used MCT

A

when separation of API is needed for stability purposes
- mixing process is inadequate to guranatee uniform distribution of 2+ API

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8
Q

What type of tablets do not need to add a disintegrant

A

chewable tablets

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9
Q

Explain the sublingual tablets

A

Rapid systemic effect
bypass first-pass effect (pass by liver)

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10
Q

Differentiate between Group 1 and 2 excipients

A

Group 1: for processing and compression characteristics
- diluents/filler
- binders
- glidants
- lubricants

Group 2: give physical characteristics
- disintegrant
- surfactants
- colours
- flavours
- sweetening agents
- polymers

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11
Q

What are the roles of binders?

A

-give cohesive qualities to the powder material
- ensures the tablet remains intact after compression

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12
Q

What are 2 the types of binders?

A

Solution binders: added as the granulation fluid, more effective

Dry binders: added before wet ingredients or mixed with other ingredients before compaction

(see onenote for examples)

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13
Q

What are the role of lubricants in tablets?
Examples of insoluble & soluble

A
  • prevent adhesion of the tablet to the surface of the dies and punches
  • Facilitate the ejection of the tablets from the die cavity

Insoluble:
- magnesium/calcium stearate
- Stearic acid
- Light mineral oil

Soluble:
- Sodium benzoate
- PEG 4000 & 6000
- Sodium lauryl sulfate

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14
Q

Which types of lubricants are the most effective and when are they added?

A

Insoluble (hydrophobic stearates)
- added last after all components mixed

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15
Q

What does too much lubricant do to drug dissolution?

A

Lowers

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16
Q

What does the least % concentration of lubricant have effect on drug absorption?

A

High plasma drug level

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17
Q

What are the roles of glidants?
Examples?

A

improves flow characteristics by reducing interparticle friction

Ex.
- Colloidal silicon dioxide (Aerosil)
- talc
- Calcium silicate
- Magnesium carbonate

18
Q

What are the roles of disintegrants?

A

A substance added to a tablet to facilitate its breakup after administration

19
Q

What type of tablets don’t have disintegrants?

A

chewable tablets

20
Q

What are mechanisms of disintegrants? (3)
Give examples

A
  1. Facilitated water uptake (bring liquids into pores of tablets)
    ex. starch (5-10%), microcrystalline cellulose, crospovidine
  2. Swelling on contact with water (super-disintegrants)
    Ex. sodium starch glycolate, croscarmellose)
  3. Gas production in effervescent tablets
21
Q

Role of colouring agents?
When can it be added? best?

A

Role:
- product identification
- Acceptable appearance

Added
- during the coating step (BEST)
- by adding to the formulation

22
Q

Benefits of granulation

A
  • prevent powder segregation
  • improve flow properties
  • improve compression
  • Reduce dust
  • Reduce clumping of hygroscopic powders
23
Q

Explain wet granulation

A

Connective mixing using a high-shear mixer

24
Q

Explain dry granulation

A
  • “slugging” preparation of large tablet which is then milled
  • roller compaction - powder is pressed between rollers then ground
25
Q

Explain when to use rapid drying vs slow drying in fluidized-bed granulators

A

Rapid drying: smaller, friable granules
Slow drying: larger more controlled granules

26
Q

What do tablet machines consist of?

A
  • Hopper (storing material for compressing)
  • Feed frame (distributing materials into dies)
  • Dies (controlling size & shape of tablet)
  • Punches (compressing materials within dies)
27
Q

Differentiate between powder compression and powder compaction

A

Powder compression
- reduction of volume of powders when a force is applied

Powder compaction
- Formation of a solid specimen with defined geometry by powder compression

28
Q

What are the 4 compaction phases?

A
  1. Particle rearrangement
    a. loose packing (bulk density)
    b. dense packing
  2. Elastic deformation
  3. Plastic deformation
  4. Brittle fracture
29
Q

Differentiate between elastic deformation and plastic deformation

A

Elastic
- reversible
- particles return to former shape
- cohesion LOST

Plastic
- permanent
- particles remain deformed
- Cohesion retained

30
Q

What does Porosity = 0 mean
What are densities for organic powders vs inorganic powders

A

P= 0
- all pores removed (solid fraction = 1)
P= 1 - solid fraction

Organic: 1-1.7g/mL
Inorganic 2-3g/mL

31
Q

What does the manufacturability profile mean?

A

Change in BREAKING strength with applied force

32
Q

What does tabletability profile mean?

A

Change in TENSILE strength with applied pressure

33
Q

What does compressibility profile mean?

A

Change in solid fraction (or porosity) with applied pressure

34
Q

What describes the heckel equation?

A

densification of powders during compression

changes in powder bed density during compression

35
Q

What can reduce tablet strength?

A
  • condensation of water in tablet pores = reduced intermolecular forces
  • dissolution in condensed water
  • water absorption = softening of amorphous material
36
Q

What can increase tablet strength?

A
  • crystallization of material dissolved in condensed water
  • Crystallization of amorphous material
  • rearrangement of solid material in the amorphous state and polymorphic transformation
37
Q

Differentiate between sticking and picking in manufacturing problems

A

Sticking = whole tablet adheres
Picking = localized particles adhere

38
Q

Which tablet characteristic is dependent in dies/punches (3)

A
  • Diameter size
  • Shape
  • Thickness
39
Q

When is uniformity of weight (mass) vs uniformity of content (active ingredient) used?

A

Of weight
- for big tablets

Of content
- good for small doses
- way more steps

40
Q

Explain tablet friability

A

tendency for a tablet to chip or crumble after compression

41
Q

Does disintegration imply complete dissolution

A

no

42
Q

Explain dissolution test

A

rate of release of drug from solid dosage form into a bioavailable form