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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
Take aspirin befor, after or with food?
Take with food May irritate the gastric mucosa during prolonged
26
Amoxicillin - take before or after food?
Take before food Improve absorption as food can affect absorption Unstable in acid and will decompose if stomach emptying is delayed
27
What is the Rate-limiting step?
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
Rate-limiting step differs from drug to drug because....
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
Small intestine epithelium - surface area
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
What are the advantages of tablets?
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
Disintegration and dissolution of tablets
1. Dinintegration > granules / primary drug particles (deaggration from granules to particles) 2. Dissolution 3. Drug in solution [in bottom of stomach]
32
Hard vs Soft capsules:
Hard; Gelatin (bovine, porcine, fish) Alternative polymers (HPMC hydroxypropylmethylcellulose, pullulan) Soft; Gelatin Vegetarian option (Vegecaps)
33
Advantages of capsules - 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
34
Advantages of capsules - 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
35
DISSOLUTION from capsule;
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
In GI fluids, hard gelatin capsule shell dissolves, thereby exposing contents of fluids, and then...
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
Liquid oral dosage forms (solution);
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
Injection advantages, consider bioavailability:
great precision and high repeatability, combined with speed, a low cost per part and a huge choice of available plastics 100% bioavailability
39
What is bioavailability?
the extent a substance or drug becomes completely available to its intended biological destination(s).
40
Liquid oral dosage forms (suspension)
> 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
Bioavailability (oral dosage forms)
Aqueous solution > precipitation > Suspension of fine particles of drug in Gi fluids > dissolution > solution of drug in GI fluid > absorption > blood
42
tablet steps - to be absorbed to the blood;
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
Which form is quicker liquid of solids + suspensions?
Liquid
44
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
45
Buccal
application to the lining of the cheek – entry into the systemic circulation following absorption
46
Non-keratinised
Keratinised mucosa Non-keratinised mucosa - Floor of the mouth, the soft palate, the lips and the cheek Hard palate, gingiva and tongue
47
Epithelium thickness
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
Sublingual and buccal properties;
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
Sublingual – tablet, chewing gum & spray
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
Examples of Buccal – adhesive tablets
- 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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