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PMP103 - Practice Of Pharmacy > Routes of Administration: Oral > Flashcards

Routes of Administration: Oral Flashcards

1
Q

What is absorption?

A

Movement of drug from site of administration to the
bloodstream

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2
Q

What types of lipids are in biological membranes?

A

Sphingomyelin
Phosphatidylcholine
Phosphatidylserine
Phosphatidylinositol
Phosphatidylethanolamine

Glycolipid – lipid with a carbohydrate attached
Cholesterol – a type of lipid

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3
Q

What are the two types of cellular transport across membranes?

A

*transcellular
*paracellular

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4
Q

What are the types of transcellular transport?

A
  • Passive diffusion
  • Carrier mediated transport
  • Facilitated diffusion
  • Active transport
  • Vesicular transport (endocytosis)
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5
Q

What is the type of paracellular transport?

A
  • Tight junctions
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6
Q

What structures are involved in the GI tract?

A

*small intestine
*vilus
*epithelial cells with microvilli

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7
Q

Describe pressure changes during gastric emptying of food

A
  • Stomach pressure remains constant until ~1 L of food ingested
  • Relative unchanging pressure results from intrinsic ability of
    smooth muscle to exhibit “plasticity”
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8
Q

Describe what happens to chyme (stomach acid) during gastric emptying

A

Chyme is either:
* Delivered in small amounts (about
3 mL) to the duodenum
* Forced backward into the stomach
for further mixing

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9
Q

What is gastric emptying regulated by?

A

*neural reflex
* hormonal mechanisms

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10
Q

What is gastric emptying affected by?

A

*meal volume
*meal composition
*pH content

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11
Q

How does meal composition affect gastric emptying?

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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12
Q

How does pH content affect gastric emptying?

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
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13
Q

What is GER?

A
  • Gastric emptying rate (GER) = Speed with which substances leave the
    stomach after ingestion
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14
Q

How do the structures of the GI tract do drug gastric emptying?

A
  • The duodenum has the greatest capacity for the absorption of drugs from the GI tract
  • Anatomically, a swallowed drug rapidly reaches the stomach
  • Eventually, the stomach empties its contents into the small intestine
  • Delay in the gastric emptying time will slow the rate and possibly the extent of drug absorption
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15
Q

What type of advice can be given for oral drugs and the disadvantages?

A
  • Take with food
  • May irritate the gastric mucosa
    during prolonged
  • Take before food
  • Improve absorption as food can
    affect absorption
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16
Q

What is the 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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17
Q

What are the various rate limiting steps for different drugs?

A

Rate-limiting step differs from drug to drug:
* 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 (first pass effect)

18
Q

what is the SA of the small intestine epithelium?

A
  • Epithelium brush border
  • 3000 microvilli per cell
  • 200,000,000 per mm2
19
Q

How will the epithelium brush SA help?

A
  • With this surface area
    even ionised weak acids
    will be absorbed in
    sufficient quantities
20
Q

What are the different types of tablets?

A

*disintegrating tablet (Zantac)
*lozeneges (strepsils)
*chewable tablets (gaviscon)
*effervescent tablets (beroca)
*sublingual tablets (nicorette)
*buccal tablets (buccastem m)

21
Q

What are the 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
22
Q

What are the types of capsules?

A

*hard capsules
*soft capsules

23
Q

What are hard capsules composed of?

A
  • Gelatin
    (bovine, porcine, fish)
  • Alternative polymers
    (HPMC
    hydroxypropylmethylcellulose,
    pullulan)
24
Q

What are soft capsules composed of?

A
  • Gelatin
  • Vegetarian option (Vegecaps)
25
Q

What are the advantages to capsules? in terms of patient compliance

A

Patient compliance
* Easier to swallow
* Smooth & slippery
* Tasteless and odourless
* Eliminate all contact between drug
and mouth)
* Can be opened up
* Contents sprinkled on food
* Clear, high-gloss coloured film
* Can be printed on

26
Q

What are the advantages capsules? in terms of 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
27
Q

Describe dissolution of capsules containing both hydrophobic and hydrophilic drug particles

A

*Hard gelatin capsules containing
hydrophobic drug particles and
hydrophilic diluent particles
* the capsules will dissolve in GI liquid leaving a porous mass of drug
*GI fluids can penetrate porous mass
*Effective surface area of
drug and hence dissolution
rate is increased

27
Q

Describe dissolution of capsules containing only hydrophobic drug particles

A

*hard capsule containing only hydrophobic drug particles
*the capsule shell will dissolve in GI fluid exposing contents
*Contents remain as capsule-shaped plug.Hydrophobic nature of contents impedes penetration of GI fluids
*Dissolution of drug occurs only from surface of plug-shaped mass. Relatively low rate of dissolution

28
Q

Why are oral solutions give+ absorption?

A
  • Drugs are commonly given in solution
  • in cough/cold remedies
  • for the young and elderly
  • Absorption from an oral solution is often rapid and complete, greater
    bioavailability compared to other oral dosage forms
29
Q

What is the absorption of oral suspensions like?

A
  • Second to a solution in terms of superior bioavailability
  • Absorption may well be dissolution-limited
  • Suspension of a finely divided powder will maximize the potential for rapid
    dissolution
29
Q

What are sublingual tablets for?

A
  • Sublingual – application to the
    membranes of either the floor of
    the mouth or the underside of the
    tongue and entry into systemic
    circulation following absorption
30
Q

What are buccal tablets for?

A
  • Buccal – application to the lining
    of the cheek – entry into the
    systemic circulation following
    absorption
31
Q

What makes up the Floor of the mouth, the soft palate, the lips and the cheek?

A

Non-keratinised mucosa

32
Q

What makes up Hard palate, gingiva and tongue?

A

Keratinised mucosa

33
Q

What is the epithelium thickness of the sublingual route?

A

100 – 200 µm on the underside
of the tongue and on the floor of
the mouth

34
Q

What is the epithelium thickness of the buccal route?

A

500 – 800 µm in the buccal
cavity

35
Q

What are some properties of the sublingual route?

A
  • Relatively permeable
  • Rapid absorption
  • Unsuitable for retentive system
  • Ideal for rapid onset of action
  • Sprays or fast-dissolving tablets
36
Q

What are some properties of the buccal route?

A
  • Relatively less permeable
  • Not rapid absorption
  • Suitable for retentive system
  • Ideal for sustained release
  • Adhesive tablets or patches
37
Q

What are the three sublingual oral types?

A

*chewable tablets
*sprays
*tablet

38
Q

What are each sublingual oral route made of?

A
  • Sublingual tablets
  • Consist of lactose mannitol sucrose for fast dissolution
  • Solutions and sprays
  • Administration of nitroglycerin (angina prevention)
  • Chewing gum
  • A gum base of a cellulosic or acrylic polymer
39
Q

What are some examples of buccal adhesive tablets?

A
  • Buccastem M: prochlorperazine
    (antiemetic)
  • Suscard Buccal: Glyceryl trinitrate
    (relieves chest pain)
  • Buccal sustained release of
    flurbiprofen (NSAID)

PMP103 - Practice Of Pharmacy (16 decks)

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