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M103 > W11 Routes Of Administration- Oral > Flashcards

W11 Routes Of Administration- Oral Flashcards

1
Q

What are the different routes of administration?

A

Oral, Ocular, Nasal, Ear, Inhalation, Intramuscular, Intravenous, Intra-arterial, Topical, Subcutaneous, Vaginal, Rectal, Intrathecal & epidural, Intrathymic, Intracardiac

Sublingual- Under the tongue
Buccal- Inside the cheek

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2
Q

Top 5 prescribed medicines in NHS England primary care in 2019 (in millions)
(for info)

A

Astorvatin- Cholesterol
Levothyroxine
Omeprazole- Stomach
Amlodipine- Blood pressure
Ramipril

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3
Q

Top 5 administration routes of globally approved
products between 2013–2018 (in %)

A

Oral, Injection, Opthalmic, Topical, Inhalation

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4
Q

Define Absorption:

A

Movement of drug from site of administration to the
bloodstream

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5
Q

Biological membranes- Lipid bilayer (for info)

A

There are different types of phospholipids:
Sphingomyelin
Phosphatidylcholine
Phosphatidylserine
Phosphatidylinositol
Phosphatidylethanolamine

Cholesterol regulates the fluidity
Glycolipid- lipid with carbohydrate chain attached

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6
Q

How thick is the lipid bilayer?

A

5-8nm thick

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7
Q

What molecules can pass through the cell membrane?

A

Hydrophobic, small, uncharged molecules (non-ionic)

Water-soluble components
(Na+, K+, and Cl−) of the cell
retain inside the cell

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8
Q

What are examples of transcellular transport?

A
  • Passive diffusion
  • Carrier mediated transport
  • Facilitated diffusion
  • Active transport
  • Vesicular transport (endocytosis)
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9
Q

What are examples of paracellular transport?

A

-Tight junctions
Some hydrophilic molecules pass through this way

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10
Q

Why do epithelial cells in the small intestine have microvilli?

A

To increase the surface area for absorption

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11
Q

What happens during Gastric emptying? (food)
- How is it regulated?
- Role of chyme?

A
  • Regulated by neural reflex and hormonal mechanisms
  • Most vigorous peristalsis and mixing occurs near the pylorus.
  • Stomach pressure remains constant until 1L of food ingested
  • Relative unchanging pressure results from intrinsic ability of smooth muscle to exhibit “plasticity”

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

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12
Q

What affects gastric emptying?

A
  1. Meal volume
    * Gastric emptying is a simple exponential
    function of the volume of a meal
  2. pH of content
    * 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
  3. Meal composition
    * 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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13
Q

Acidic/basic?
The stomach is….
The small intestine is….

A

Acidic
Basic

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14
Q

What is the Gastric emptying rate (GER)?

A

Speed with which substances leave the stomach after ingestion
e.g. rapid emptying with glucose and slow emptying of a viscous meal.

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15
Q

What has greatest capacity for the absorption of drugs from the GI tract?
Where does a swallowed drug go?
What will a delay in gastric emptying mean?

A

The duodenum.
The stomach then it is emptied into the small intestine.
It will slow the rate and possibly the extent of
drug absorption

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16
Q

Aspirin is taken with what caution (instructions)?

A

Take with food
* May irritate the gastric mucosa
during prolonged

17
Q

Amoxicillin/penicillin is taken when?

A
  • Take before food
  • Improve absorption as food can affect absorption
  • Unstable in acid and will decompose if stomach emptying is delayed
18
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

19
Q

Examples of rate-limiting steps in drug? absorption? (5)

A
  1. Drug release from dosage form – disintegrate
  2. Gastric emptying
  3. Dissolution – high log P hardly dissolves
  4. Permeability – low log P is hardly absorbed
  5. Metabolism – including metabolism in the liver (first pass effect)
20
Q

What is the Dissolution (P) equation:
What do the log P values mean?

A

P= [Organic solvent] / [Water]

High log P- hardly dissolves
Low log P is hardly absorbed

21
Q

Features of the Small intestine epithelium (for info)

A
  • Epithelium brush border
  • 3000 microvilli per cell
  • 200,000,000 per mm
  • With this surface area even ionised weak acids will be absorbed in sufficient quantities.
22
Q

What are the different types of tablets? (6)

A
  1. Disintegrating tablets
  2. Chewable tablets
  3. Effervescent tablets
  4. Lozenges
  5. Sublingual tablets
  6. Buccal tablets
23
Q

What are the advantages of tablets? (5)

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
24
Q

Disintegration and dissolution of tablets:
What are the 3 steps?

A
  1. Disintegration
  2. Deaggregation
  3. Dissolution=Drug in solution
25
Q

What are the types of capsules?

A

Hard capsules:
* Gelatin
(bovine, porcine, fish)
* Alternative polymers
(HPMC- hydroxypropylmethylcellulose,pullulan)

Soft capsules:
* Gelatin
* Vegetarian option (Vegecaps)

26
Q

What are the advantages of capsules over tablets?
(Explain the aspects Patient compliance and Drug delivery)

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

Drug delivery:
* 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

When are drugs commonly given in solution?
Is an oral solution a good dosage form?

A
  • 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
28
Q

Liquid oral dosage forms (suspension)

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

Definition of 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

30
Q

What is the Buccal route?

A

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

31
Q

Which part of the mouth contains
-Keratinised mucosa?
-Non-keratinised mucosa?

What are the benefits of keratin?

A

The floor of the mouth is non-keratinised

Keratinised mucosa- Hard palate, gingiva and tongue

Non-keratinised mucosa- Floor of the mouth, the soft palate, the lips and the cheek

Makes tissue stronger and better at forming barriers.

32
Q

Epithelium thickness of sublingual and buccal (for info)

A

Sublingual
100 – 200 micrometers on the underside
of the tongue and on the floor of the mouth

Buccal
500 – 800 micrometers in the buccal cavity

33
Q

What are the features of Sublingual Vs buccal?
Which is more permeable?
What is the onset of action like?
What medicinal forms do each route have?

A

Sublingual:
* Relatively permeable
* Rapid absorption
* Unsuitable for retentive system
* Ideal for rapid onset of action
* Sprays or fast-dissolving tablets

Buccal:
* Relatively less permeable
* Not rapid absorption
* Suitable for retentive system
* Ideal for sustained release
* Adhesive tablets or patches

34
Q

Sublingual – tablet, chewing gum & spray

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

35
Q

What has greatest capacity for the absorption of drugs from the GI tract? (Specific)

Where does a swallowed drug go?
What will a delay in gastric emptying mean?

A

The duodenum (first part of small intestine)
The stomach then it is emptied into the small intestine.

It will slow the rate and possibly the extent of
drug absorption

36
Q

Examples of buccal adhesive tablets:

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

Buccastem M
Hydrocortisone

M103 (46 decks)

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