Oral Tablets Flashcards by Holly Grey

Is oral route the most common route?

YES

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What is the European Pharmacopoeia?

A single reference work for quantity control of medicines

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What is the BP?

Provides collection of authoritative official standards for UK pharmaceutical substances + medicinal products

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What are the advantages of tablets?

Convenient to take + handle
Better stability compared to liquid
Longer shelf life
precise dosing of drug
Cheap to mass produce

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What are the disadvantages of tablets?

Slower onset of action
Poorer bioavailability = unfavourable drug properties
Instability in GI
Difficult to reverse therapy
GI irritation

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Describe disintegrating tablet

Most common
Swallowed
Release drug quickly
Excipients used are not intended to modify drug release

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Why is it good that disintegrating drugs release quickly?

Aids fast + complete drug release once in digestive fluids

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Why are there uncoated disintegrating tablets?

Conventional or plain tablets

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Why are there coated disintegrating tablets?

Smooth surface + coloured

BUT doesn’t alter release profile

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Describe gastro-resistant tablets

Delayed-release
Intended to resist gastric fluid
Release drug in intestinal fluid

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What are gastro-resistant tablets covered in?

Gastro-resistant coating
OR
Granules/particles already covered with gastro-resistant coating

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Describe modified-release tablets

Coated or uncoated
Contain special excipients
Should be swallowed whole

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What are modified-release tablets designed for?

Modify rate, place or time at which drugs are released

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What is prolonged-release?

Drug released slowly at constant rate

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What is delayed-release?

Drug released at some time after adminstration

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What is pulsatile-release?

Drug released from formulation in 2 or more pulses

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Describe effervescent tablets

Uncoated
Intended to be dissolved/dispersed in H2O
Contain WA + carbonate/bicarbonate

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Why does effervescent tablets have a high carbonate content?

Buffer solution temporarily increases stomach pH
= fast emptying of stomach
= drug enters intestine quicker
= faster absorption
= minimises stomach irritation

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Why does effervescent tablets contain WA + carbonate?

React rapidly in H2O

= releases CO2

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Describe sublingual tablets

Under the tongue

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Describe buccal tablets

Buccal cavity (side of cheek)

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What do both sublingual + buccal tablets do?

Provide rapid drug release for systemic effect without first-pass liver metabolism

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Describe lozenges + pastilles

Solid, single dose preparations
Dissolve/disintegrate slowly in mouth
Local effect = oral cavity + throat

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What is the difference between lozenges + pastilles?

Lozenges = hard
Pastilles = soft, flexible

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What are the product quality attributes

``` Correct dose Consistent weight, size, appearance + elegant Drug released in controlled manner Biocompatible Sufficient mechanical strength Stable throughout shelf-life Packaged safely Formulated suitable for patient ```

What is biocompatibility?

Not cause patient harm

Why must the product have sufficient mechanical strength?

Withstand fracture + erosion during handling

What is the most common manufacturing?

Powder compression

Describe powder compression

Requires 2 punches + die | When forced applied bonds formed

What is die filling? | 1

Powder flows down from hopper into die

What is tablet formation? | 2

Upper punch comes down into die Compresses powder into tablet When required amplified force reached Upper punch moves upwards

What is tablet ejection? | 3

Lower punch rises to eject tablet | Pushing device removes tablet form die

Describe single punch press

1 die + 1 pair of punches Lower punch = stationary Pressure applied by upper punch when descends

When is single punch press used?

Used in formulation development + production for clinical trials

Describe rotary press

Large scale production Multiple punches + dies Die table + punches rotate together

Describe tablet tooling

Come in different shapes + sizes | Dictated by different tools + design of die + punches

What are the different tablet shapes?

Circular, oval, oblong, triangular + quadratic

What are different side views?

Flat, convex | With/without bevelled edges

Why do tablets have break marks?

Facilitate tablets breaking for reproducible doses

What are different markings?

Embossed or debossed

Why do tablets have excipients?

Control quality attributes | Aid manufacturing

When would a tablet have no excipients?

If active ingredient has optimal properties

What are the excipients?

``` Filler (diluent) Disintegrate Binder (adhesive) Glidant Lubricant Anti-adherent ```

When is filler added?

When tablets more than 50mg

Why is filler added?

To increase bulk vol of powder | = increases tablet size

What is the most common filler and why is it used?

``` Lactose Readily dissolves in H2O Pleasant taste Good compatibility Non-hygroscopic ```

What is limitation of lactose?

Lactose intolerant

Why is disintegrate used?

Allows tablet to break up into small fragments when in contact with liquid = promotes rapid drug dissolution = bioavailability

What is the most common disintegrate + why is it used?

Starch Swells in contact with H2O Swelling disrupts tablet = larger SA during dissolution

How much starch is normally added?

Up to 10%

Why is binder added?

Ensures granules + tablets can be formed with required mechanical strength

How can binders be added?

Powders or solutions

What are examples of solution binders?

Starch, sucrose, gelatin + polymers (PVP)

What are examples of dry binders?

Microcrystalline cellulose

Why are glidant added?

Improve powder flowability by reducing cohesion between particles

What is the most common glidant + why is it used?

Colloidal silica Vey small particles Adhere to particles surface of other ingredients Reduce inter-particulate friction = improves flow

How much colloidal silica normally added?

1-2% w/w

Why is lubricant added?

Lower friction between solid + machine wall | Improve tablet formation + ejection

What is the most common lubricant?

Magnesium stearate

Why is anti-adherent added?

Reduces adhesion between powder + punch faces Prevents particles sticking to punches Important if tablet has markings

What are examples of anti-adherent?

Mg stearate, talc, starch + cellulose