Routes Of Administration Oral (Tablets) Flashcards

1
Q

What is the pH in the stomach and transit time?

A
  • pH (fasted) 1/2, pH (fed) 4/5
  • 0/3 hr
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2
Q

What is the pH and transit time in the small intestine

A
  • pH 5/7
  • 3/4 hr
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3
Q

What is the pH and transit time in the large intestine?

A
  • pH 6/7.5
  • transit time highly variable
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4
Q

What are the advantages of the oral route?

A
  • Most common route
  • Simplest / convenient
  • Modified release formulations available
  • High Surface area with good absorptive capacity
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5
Q

What are the Oral route advantages?

A
  • Most common route
  • Simplest, convenient, safe
  • Modified release formulations available
  • High surface area with good absorptive capacity
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6
Q

What are the Oral route disadvantages?

A
  • Slower onset of action (dissolution is the rate limiting step)
  • Variable absorption (changes with age, gender)
  • Hostile environment (GI secretions, enzymes)
  • First pass metabolism
  • Difficult to reverse therapy
  • GI irritation
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7
Q

What is the British pharmacopeia’s definition of a tablet?

A
  • Are solid preparations each containing a single dose of 1 or more active substances
  • Obtained by compressing uniform volumes of particles
  • Tablets are intended for Oral Administration (some are swallowed whole, chewed, dissolved, dispersed or retained
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8
Q

What are the advantages of Tablets?

A
  • Convenient to take and handle
  • Better chemical, physical and microbiological stability compared to liquids (better shelf life)
  • Precise dosing of drug
  • Relatively cheap to mass produce with consistent quality
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9
Q

What do all tablets need to be?

A
  • Include the correct dose of drug
  • Be consistent in weight, size
  • Release drug in controlled and reproducible manner
  • Be biocompatible and not harm patients
  • Be of sufficient mechanical strength
  • Be chemically, physically, and microbiological stable
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10
Q

What are the different types of tablets?

A
  • Disintegrating
  • Gastro resistant
  • Modified release
  • Dispersible
  • Effervescent
  • Sublingual and Buccal
  • Lozenges and Pastilles
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11
Q

What is the disintegrating tablet?

A
  • Most common type
  • Swallowed and released in a short time
  • Excipients used are not intended to modify the drug release profile. Can be coated or uncoated
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12
Q

What are gastro resistant tablets?

A
  • They are delayed release tablets
  • Intended to resist the gastric fluid and to release the drug in the intestinal fluid
  • Prepared by covering the tablets with gastro resistant coating
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13
Q

What are modified release tablets?

A
  • Coated or uncoated tablets that contain special excipients and prepared by special procedures to modify rate or place
  • Normally swallowed whole
    —Prolonged release : drug released slowly at a constant rate
    —Delayed release : drug is released some time after Administration
    —Pulsatile release : drug is released from the formulation in 2 or more pulses
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14
Q

What are dispersible tablets?

A
  • Can be coated or uncoated intended to be dispersed in water before Oral Administration
  • Orodispersible tablets are uncoated tablets intended to be placed in the mouth where they disperse before swallowed
  • Soluble tablets can be uncoated or film coated intended to be dissolved in water before Administration
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15
Q

What are effervescent tablets?

A
  • They are uncoated tablets intended to be dissolved or dispersed in water before Administration
  • Containing a weak acid and a carbonate/ bicarbonate which react rapidly in the presence of water to release CO2
  • High carbonate results in a buffer solution temporarily increases stomach pH
  • Leads to fast emptying of stomach content
  • Allows drugs to enter the intestine faster for absorption
  • Provides a faster drug absorption and minimise stomach irritation
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16
Q

What are sublingual tablets?

A
  • Are placed under the tongue
  • Small and porous - rapid drug release for systemic effect without first pass liver metabolism
17
Q

What are buccal tablets

A
  • Placed in the buccal cavity (the side of the cheek)
  • High up between the inside of the upper lip and gum
  • Provide rapid drug release for systemic effect without first pass liver metabolism
18
Q

What are lozenges and pastilles?

A
  • Solid, single dose preparations
  • Lozenges are hard whereas pastilles are soft, flexible
  • Intended to dissolve or disintegrate slowly in the mouth when sucked (usually for local effect)
19
Q

What are the stages of tablet formation?

A
  1. Die filling (powder flows down from hopper into a die)
  2. Tablet formation - upper punch compresses powder into tablet (compression) upper punch moves upward (decompression)
  3. Tablet ejection - lower punch rises to eject the tablet and a pushing device removes tablet from the die
20
Q

What is the single punch press?

A
  • Consists of 1 die and 1 pair of punches
  • Lower punch is stationary, pressure applied
  • Produces 200 tablets per minute
21
Q

What is the rotators press?

A
  • Multi station presses
  • Upto 10,000 per minute
  • Multiple sets of punches and dies
  • Dies and punches both rotate together
22
Q

What are the different designs of tablets

A
  • Shapes: circular, oval, oblong, triangular
  • Side view: flat or convex (bevelled edges)
  • Break marks: Breaking for reproducible doses
  • Markings: embossed, debossed
23
Q

What are the important properties of a powder mix?

A
  • Homogeneity and segregation tendency (Under/ over mixing)
  • Flowability (controlled by gravity)
  • Compression and compaction
  • Friction and adhesive properties
24
Q

What are the commonly used excipients?

A
  • Filler
  • Disintegrant
  • Binder
  • Anti-adherent
  • Lubricant
  • Glidant
25
Q

Why is a filler added to tablets?

A
  • Increase the bulk volume of powder and tablet size for ease of handling
  • Lactose is a common tablet filler
26
Q

Why is disintegrant added to the tablets?

A
  • Allows tablet to break up into small fragments when in contact with liquid
  • Promotes rapid drug dissolution thus bioavailability
  • Starch is commonly used
27
Q

Why is the binder added to the tablet?

A
  • Ensures granules and tablets can be formed with the required mechanical strength
  • starch, cellulose
28
Q

Why is glidant added to the tablet?

A
  • To improve powder flowability by reducing cohesion between particles
  • Talc, colloidal silica
29
Q

Why is lubricant added to the tablet?

A
  • It lowers friction between the solid ingredients and the machine wall
  • It improves tablet formation and ejection
  • Magnesium stéarate is most widely used
30
Q

Why is anti-adherent added to tablets?

A
  • Reduces adhesion between powder and punch faces
  • Prevents particles sticking to the punches
  • Particularly important if tablet punches have markings
  • Starch, cellulose