Powders, tablets and capsules Flashcards

(46 cards)

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
Film vs sugar coating
26
Disintegrating tablets
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
Chewable tablets
Tablet disintegration in oral cavity Fast tablet disintegration o For rapid local or systemic action
28
Effervescent tablets
Disintegrate and dissolve in water prior to oral administration Benefit from faster stomach emptying
29
Lozenges
Designed to dissolve slowly in the mouth For local action
30
Sublingual tablets
For fast disintegration, drug release and absorption in the sublingual cavity to avoid first pass metabolism
31
Buccal tablets
Drug released and absorption in the buccal cavity to avoid first pass metabolism
32
Quality standard and compendial requirements
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
Examples of diluent
Lactose Mannitol Microcrystalline cellulose (MCC) Calcium phosphate Calcium carbonate
34
Examples of binders
Solution binder Gelatin Glucose Starch Dry binder MCC Crosslinked polyvinyl pyrrolidine Methylcellulose (MC)
35
Examples of disintegrant
Starch MCC Crospovidone Croscarmellose sodium Sodium starch glycolate Sodium bicarbonate plus citric and tartaric acids
36
Examples of glidant
Colloidal silica Magnesium stearate Talc
37
Examples of lubricant
Magnesium stearate Polyethylene glycol Sodium lauryl sulfate Liquid paraffin
38
Examples of antiadherent
Magnesium stearate Talc Starch
39
Advantages of capsules
Similar to tablets Gelatin shell provides taste masking and drug protection More versatile and aesthetically pleasing
40
Disadvantages of capsules
Little flexibility of dosing Potential for gastric irritation for highly soluble drugs Two step manufacture Filling equipment is less efficient More readily tampered
41
Ideal features of capsules
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
Excipients of powder formulated capsules
Diluent Glidant Lubricant Disintegrant Wetting agent
43
Excipients of liquid formulated capsules
Lipophilic Solvents Solubilisers Surfactants Emulsifiers
44
Quality standards and compendial requirements for capsules
Physical defects Uniformity of dosage units Drug content Disintegration test Dissolution test
45
What are hard shells made out of
Gelatin Colourants/ opacifying agents Plasticisers Wetting agents
46
What are soft shells made out of
Gelatin Plasticiser Water Colourant/ opacifying agents Preservatives