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PMP-103 > Routes of Administration - Oral > Flashcards

Routes of Administration - Oral Flashcards

1
Q

List all of the routes of administration;

A

Sublingual (under tongue)
Buccal
Ocular (eye)
Nasal (nose)
ear
Intrathecal
Intrathymic
Intravcardiac
Inhalation
Intravenous & arterial
Intramuscular
Subcutaneous
Topical (on top of skin)
Vaginal
rectal (intestines)
Oral

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2
Q

Define Absorption

A

Movement of drug from site of administration to the bloodstream

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3
Q

Biological membranes - phospholipids
Lipid molecules;

A

Sphingomyelin
Phosphatidylcholine
Phosphatidylserine
Phosphatidylinositol
Phosphatidylethanolamine

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4
Q

What is cholesterol?

A

A type of lipid

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5
Q

What is Glycolipid?

A

lipid with a carbohydrate attached

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6
Q

How are molecules arranged in biological membranes?

A

Arrangement related to solubility of PROTEIN molecules

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7
Q

Phospholipid bilayer

A
  • 2 layers
  • mosaic fluid model /cholesterol to helping the bilayer stay fluid in different environmental conditions.
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8
Q

Polar head

A

Face outwards in contact with aqueous medium(hydrophilic phosphate groups)

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9
Q

Non-polar lipid tails

A

Face towards the bilayer interior (hydrophobic alkyl chains)

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10
Q

Transport across biological membranes;

A

1) Trancellular
2) Paracellular

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11
Q

1) Trancellular

A

Passive diffusion
Carrier mediated transport
Facilitated diffusion
Active transport
Vesicular transport (endocytosis)

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12
Q

2) Paracellular

A

Tight junctions

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13
Q

Will small charged ions be able to transport through phospholipid bilayer

A

Yes, small molecule - polar

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14
Q

Gastrointestinal tract

A

Small intestine
Villus
Epithelial cells with microvilli

Villi > Epithelial cells > Microvilli

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15
Q

Gastric emptying (food)

A

Most vigorous peristalsis and mixing occurs near the pylorus

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16
Q

Types of transport

A

1) Transcellular - passive
2) Paracellular - passive
3) Transcelluar - carrier-medicated
5) Endocytosis - specialised (energy required)

*6) Efflux - when membrane will push something back out - cannot be defused in

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17
Q

How long will pressure in stomach remain constant?

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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18
Q

How is Chyme delivered?

A

Delivered in small amounts (about 3 mL) to the duodenum

Forced backward into the stomach for further mixing

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19
Q

What is chyme in stomach?

A

Your digestive glands in your stomach lining produce stomach acid and enzymes, which mix with the food to form a murky semifluid mass or paste called chyme

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20
Q

Neural reflex - what mechanism?

A

Hormonal mechanisms

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21
Q

Gastric emptying is affected by;

A

Meal volume; exponential function of the volume of a meal

Meal consumption;
- 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

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

22
Q

Gastric emptying rate (GER) =

A

Speed with which substances leave the stomach after ingestion

23
Q

Why do we want drug to go into small intenstine;

A

more abundant - existing in large volume

24
Q

gastric emptying - process from stomach to small intestine:

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

25
Q

Take aspirin befor, after or with food?

A

Take with food
May irritate the gastric mucosa during prolonged

26
Q

Amoxicillin - take before or after food?

A

Take before food
Improve absorption as food can affect absorption

Unstable in acid and will decompose if stomach emptying is delayed

27
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

DELAY absorption

28
Q

Rate-limiting step differs from drug to drug
because….

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 (first pass effect)

29
Q

Small intestine epithelium - surface area

A

Epithelium brush border
3000 microvilli per cell
200,000,000 per mm2

With this surface area even ionised weak acids will be absorbed in sufficient quantities

30
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

31
Q

Disintegration and dissolution of tablets

A
  1. Dinintegration > granules / primary drug particles (deaggration from granules to particles)
  2. Dissolution
  3. Drug in solution [in bottom of stomach]
32
Q

Hard vs Soft capsules:

A

Hard;
Gelatin (bovine, porcine, fish)
Alternative polymers(HPMC hydroxypropylmethylcellulose, pullulan)

Soft;
Gelatin
Vegetarian option (Vegecaps)

33
Q

Advantages of capsules - Patient compliance

A

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

34
Q

Advantages of capsules - 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

35
Q

DISSOLUTION from capsule;

A

Hard gelatin capsules containing only hydrophobic drug particles

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.

36
Q

In GI fluids, hard gelatin capsule shell dissolves, thereby exposing contents of fluids, and then…

A

Hard gelatin capsules containing hydrophobic drug particles () and hydrophilic diluent particles ()

Particles of hydrophilic diluent dissolve in GI fluids leaving a porous mass of drug

  • GI fluids can penetrate porous mass
  • Effective surface area of drug and hence dissolution rate is increased
37
Q

Liquid oral dosage forms (solution);

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

38
Q

Injection advantages, consider bioavailability:

A

great precision and high repeatability, combined with speed, a low cost per part and a huge choice of available plastics

100% bioavailability

39
Q

What is bioavailability?

A

the extent a substance or drug becomes completely available to its intended biological destination(s).

40
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 maximize the potential for rapid dissolution

41
Q

Bioavailability (oral dosage forms)

A

Aqueous solution > precipitation > Suspension of fine particles of drug in Gi fluids > dissolution > solution of drug in GI fluid > absorption > blood

42
Q

tablet steps - to be absorbed to the blood;

A

Immediate release solid dosage forms > Disintegration > Aggregate or granules > Degradation > suspension of fine particles of drug in GI fluids > dissolution > solution of drug in GI fluids > absorption > Blood

43
Q

Which form is quicker liquid of solids + suspensions?

A

Liquid

44
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

45
Q

Buccal

A

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

46
Q

Non-keratinised

A

Keratinised mucosa

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

Hard palate, gingiva and tongue

47
Q

Epithelium thickness

A

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

Buccal = 500 – 800 um in the buccal cavity

48
Q

Sublingual and buccal properties;

A

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

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

49
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

50
Q

Examples of Buccal – adhesive tablets

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

PMP-103 (33 decks)

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