Powders, tablets and capsules Flashcards

1
Q

What are advantages of powder formulation

A

Chemically more stable than liquid formulations
Preferred form of administration
May provide faster drug dissolution than tablets or capsules
Easier to swallow for very young and elderly populations

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2
Q

What are disadvantages of powder formulation

A

Accurate dosing is difficult to achieve
Less convenient to administer and transport
Difficult to mask taste and grittiness
Difficult to minimise drug irritation and drug degradation
Barrier packaging required for drugs that are volatile, deliquescent hygroscopic or readily oxidised

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3
Q

What are reasons for reducing particle size

A

Usually to micron size
For homogenous mixing
To minimise segregation of powders in a powder mix
* Narrow size distribution
* Prevent demixing
To improve drug dissolution rate and bioavailability
To minimise powder grittiness and enhance product acceptance
To optimise drug delivery to deep lungs

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4
Q

What are reasons for increasing particle size

A

Granulation
Maintain homogeneity of powder mix and reduce demixing
Improve handling
* Powder flow
* Reduce occupational hazards
* Reduce caking and hardening on storage
Improve compaction into tablets
Improve wettability
* Granules are larger to attract wetting agent, becomes close in proximity of wetting agent
Increase bulk density to reduce packing volume and costs of transport
* Powders stick to everything, granules reduce sticking

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5
Q

What is wet granulation

A

Mix powder with granulating fluid to form wet mass

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6
Q

Mechanisms of particle bonding

A

Formation of solid bridges between particles
Attractive van der Waals forces between solid particles
Mechanical interlocking of solid particles

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7
Q

Advantages of spheronisation

A

Same as other granules but smooth surface
* Spherical shapes allows for better flow
Smooth surface facilitates uniform thin layer coating
* Allows for mixing of incompatible ingredients and manufacture of modified release dosage forms

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8
Q

How are dry granulations made

A

Roller compaction
Milling of sheets/ flakes/ slugs

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9
Q

What is mixing

A
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10
Q

What is convective mixing

A

One part of powder bed moves relative to another part
Creates segregated mixture
Small particles with large particles

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11
Q

What is shear mixing

A

A layer of powder particles moves relative to another layer
This creates an ideal mixture

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12
Q

What is diffusive mixing

A

Individual powder particles move relative to each other
This creates a random mixture
* Requires velocity to obtain this mixture
* Introduce void space

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13
Q

How do you minimise demixing

A

Use narrow particle size range or ensure all particles are below 30microns
Control particle shape
Use particles of similar density
Use granulation or ordered mixing
Reduce vibration when processing post-mixed powders
Use one-stop operational equipment

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14
Q

What are the advantages of different drying processes

A
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15
Q

What are the disadvantages of
Fluidized bed dryin
Microwave
Spray
Freeze

A
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16
Q

What are the advantages for tablet formulation

A

Convenient and accurate dosing
Provision for identification
* Different colours
* Indentation
* Score lines
More stable compared to liquids
Controlled drug release possible
Cost effective industrial manufacture
Versatile design

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17
Q

What are the disadvantages for tablet formulation

A

Peroral BA may not be as good as liquids
Inappropriate for patients who have difficulty swallowing
Does not provide for flexible dosing compared to liquids for paedriatrics

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18
Q
A

Wet granulation

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19
Q
A

Dry granulation

20
Q
A

Direct compression

21
Q

Advantages of direct compression

A

Simplicity of manufacture
No water and drying processes
Faster disintegration and dissolution

22
Q

Disadvantages of direct compression

A

Requires a powder with adequate flow and good compressibility
Relatively large particles required
Challenging for
* Drugs with low dose to achieve content uniformity
o <10mg
* Drugs of high dose to achieve good flow and compressibility
o >50mg
Require diluents of specialised grades

23
Q

Reasons for coating tablets

A

Protection
Masking of taste
Improve aesthetics
Aid in identification
Confers added strength
Impart functional properties

24
Q

What are film coating

A

Uses polymers as coating agents
* Thin layer of polymer film deposited over tablet cores by atomisation of coating liquid

Controlled release function
Enteric coating
* Protect drug from being released in stomach

25
Q

Film vs sugar coating

A
26
Q

Disintegrating tablets

A

Designed to be swallowed, disintegrate and release entire drug load over a short period in the GIT
Also known as plain or conventional tablets

27
Q

Chewable tablets

A

Tablet disintegration in oral cavity

Fast tablet disintegration
o For rapid local or systemic action

28
Q

Effervescent tablets

A

Disintegrate and dissolve in water prior to oral administration
Benefit from faster stomach emptying

29
Q

Lozenges

A

Designed to dissolve slowly in the mouth
For local action

30
Q

Sublingual tablets

A

For fast disintegration, drug release and absorption in the sublingual cavity to avoid first pass metabolism

31
Q

Buccal tablets

A

Drug released and absorption in the buccal cavity to avoid first pass metabolism

32
Q

Quality standard and compendial requirements

A

Physical properties - defects
Defects in film coating - picking, twinning, mottling, erosion, bridging
Uniformity of dosage units
Dissolution test
Disintegration test
Friability test
Hardness test

33
Q

Examples of diluent

A

Lactose
Mannitol
Microcrystalline cellulose (MCC)
Calcium phosphate
Calcium carbonate

34
Q

Examples of binders

A

Solution binder
Gelatin
Glucose
Starch

Dry binder
MCC
Crosslinked polyvinyl pyrrolidine
Methylcellulose (MC)

35
Q

Examples of disintegrant

A

Starch
MCC
Crospovidone
Croscarmellose sodium
Sodium starch glycolate
Sodium bicarbonate plus citric and tartaric acids

36
Q

Examples of glidant

A

Colloidal silica
Magnesium stearate
Talc

37
Q

Examples of lubricant

A

Magnesium stearate
Polyethylene glycol
Sodium lauryl sulfate
Liquid paraffin

38
Q

Examples of antiadherent

A

Magnesium stearate
Talc
Starch

39
Q

Advantages of capsules

A

Similar to tablets
Gelatin shell provides taste masking and drug protection
More versatile and aesthetically pleasing

40
Q

Disadvantages of capsules

A

Little flexibility of dosing
Potential for gastric irritation for highly soluble drugs
Two step manufacture
Filling equipment is less efficient
More readily tampered

41
Q

Ideal features of capsules

A

Must not react with gelatine
Must not contain high level of free moisture
Unit dose must fit into capsule
Capable of being filled uniformly
Stable over storage period
Drug release kinetics comply with specifications

42
Q

Excipients of powder formulated capsules

A

Diluent
Glidant
Lubricant
Disintegrant
Wetting agent

43
Q

Excipients of liquid formulated capsules

A

Lipophilic Solvents
Solubilisers
Surfactants
Emulsifiers

44
Q

Quality standards and compendial requirements for capsules

A

Physical defects
Uniformity of dosage units
Drug content
Disintegration test
Dissolution test

45
Q

What are hard shells made out of

A

Gelatin
Colourants/ opacifying agents
Plasticisers
Wetting agents

46
Q

What are soft shells made out of

A

Gelatin
Plasticiser
Water
Colourant/ opacifying agents
Preservatives