Routes of Administration - Oral Flashcards

1
Q

Absorbition of oral drugs

A
  • Movement of drug from the site of administration to bloodstream
  • It’s bioavailability
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2
Q

Protiens in phospholipid membrane

A
  • Embedded in the phospholipid membrane
  • Srranged related to solubility
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3
Q

Transcellular

A
  • Passive diffusion that is mediated by carrier protiens and active transport
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4
Q

Paracellular

A

Through the tight junction the cell membrane

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5
Q

Gastic emptying

A
  • Faster onset if gastric emptying is higher
  • Stomach pressure remains constant until 1L of food is ingested
  • Smooth muscle exibits plasticity due to unchanged pressure
  • Most vigorous peristalsis and mixing occurs near the pylorus valve while it is closed
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6
Q

Gastric emptying

Chyme

A
  • Delivered in small amounts (about 3 mL) to the duodenum
  • Forced backward into the stomach for further mixing
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7
Q

Factors that effect Gastric emptying

Meal volume

A

Gastric emptying is a simple exponential function of the volume of a meal - larger the meal the faster the gatric emptying

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8
Q

Factors that effect Gastric emptying

Meal composition

A
  • Stomach empties liquids faster than solids
  • Carbohydrate-rich chyme quickly moves through duodenum
  • Fat-laden chyme is digested more slowly causing food to remain in the stomach longer
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9
Q

Factors that effect Gastric emptying

pH of contents

A
  • Acids delays gastric emptying
  • pH of chyme in the small intestine of (< 3.5 – 4) will activate reflexes to inhibit stomach emptying until duodenal chyme can be neutralised by pancreatic and other secretions
  • Careful of antacids (e.g. aluminium hydroxide gel) that raise the pH of stomach contents (gaviscon)
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10
Q

Gastric emptying rate

A

Speed with which substances leave the stomach after ingestion

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11
Q

Absorbtion in deuodeum

A
  • The duodenum has the greatest capacity for the absorption of drugs from the GI tract
  • Rapidly reaches the stomach
  • Eventually, the stomach empties its contents into the small intestine
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12
Q

What will a delay in gastic emptying cause?

A
  • Delay in the gastric emptying time will slow the rate and possibly the extent of drug absorption
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13
Q

What times should Asprin be taken?

A
  • Take with food
  • May irritate the gastric mucosa during prolonged
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14
Q

What time should Amoxicillin be taken

A
  • Take before food
  • Improve absorption as food can affect absorption
  • Unstable in acid and will decompose if stomach emptying is delayed
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15
Q

Rate-limiting step

A

Slowest step in the series, which controls the overall rate and extent of appearance of the intact drug in the systemic circulation

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16
Q

Types of rate limiting factors

A
  • Drug release from dosage form – disintegrate
  • Gastric emptying
  • Dissolution – high log P hardly dissolves
  • Permeability – low log P is hardly absorbed
  • Metabolism – including metabolism in the liver
17
Q

Tablet formulation

A
  • Disintergrating tablets
  • Chewable tablets
  • Effervescent tablets
  • Lozenges
  • Sublingual tablets
  • Buccal tablet
18
Q

Advantages of tablets

A
  • Ease of administration and patient acceptance
    Swallowing
  • Chewable formulations
  • Elegance
  • Convenient handling/compactness
  • Accurate dosage
  • Chemical and physical stability
  • Different to tamper with
  • Low cost of manufacturing, packaging, shipping
19
Q

Steps of disintegration

A
  • Disintegration into granules
  • Deaggregation of granules forming primary drug particles
  • Drug in solution
20
Q

Types of capsule coating

A
  • Gelatin
  • Alternative polymers
  • Soft capsules
    Gelatin
  • Vegetarian option
21
Q

Advsantages of capsules

Patient complience

A
  • Easier to swallow as itis smooth & slippery
  • Tasteless and odourless which eliminate all contact between drug and mouth)
  • Can be opened up
  • Contents sprinkled on food
  • Clear, high-gloss coloured film that can be printed on
22
Q

Advantages of capsule

Drug delivery

A
  • Fast acting
  • Breakdown of capsule shell occurs readily ≈ disintegration of tablet
  • Beads/pellets/granules in addition to dry powder fills
  • A mixture of beads with different release rates
  • Other dosage forms in a capsule
  • Mini tablets and liquids
23
Q

Capsule dissolution

A
  • Hard gelatin capsules containing only hydrophobic drug particles
  • Hard gelatin capsules containing hydrophobic drug particles and hydrophilic diluent particles
  • In GI fluids, hard gelatin capsule shell dissolves, thereby exposing contents of fluids
  • Contents remain as capsule-shaped plug. Hydrophobic nature of contents impedes penetration of GI fluids
  • Particles of hydrophilic diluent dissolve in GI fluids leaving a porous mass of drug
    Dissolution of drug occurs only from surface of plug-shaped mass. Relatively low rate of dissolution
    GI fluids can penetrate porous mass
    Effective surface area of drug and hence dissolution rate is increased
24
Q

Liquid oral dosage form

A
  • Rapid and complete, greater bioavailability compared to other oral dosage forms
25
Q

liquid oral dosage suspension

A
  • Absorption may well be dissolution-limited
    Suspension of a finely divided powder will maximize the potential for rapid dissolution
  • Secondary dissolution to solution
26
Q

Sublingual

A

Application to the membranes of either the floor of the mouth or the underside of the tongue and entry into systemic circulation following absorption

27
Q

Buccal

A

Application to the lining of the cheek – entry into the systemic circulation following absorption

28
Q

Keratinised mucosa

A

Hard palate, gingiva and tongue

29
Q

Non-keratinised mucosa

A

Floor of the mouth, the soft palate, the lips and the cheek

30
Q

Advantages of Sublingual dosage form

A
  • Relatively permeable
  • Rapid absorption
  • Unsuitable for retentive system
  • Ideal for rapid onset of action
  • Sprays or fast-dissolving tablets
31
Q

Advantages of Buccal dosage form

A
  • Relatively less permeable
  • Not rapid absorption
  • Suitable for retentive system
  • Ideal for sustained release
  • Adhesive tablets or patches