FOrmulation of Analgesics- 12

Question 1

What is nociceptive pain.

Answer 1

Pain from physical damage or potential damage to the body.

Question 2

What is psychogenic pain

Answer 2

A pain that is primarily caused by psychological factors such as depression and anxiety

Question 3

What is neuropathic pain

Answer 3

Pain is caused by damage or disease affecting the somatosensory nervous system.

Question 4

What should an “ideal” formulation be.

Answer 4

Be effective against a broad range of pain types.
have a rapid onset and controllable duration.
Be free of undesirable side effects.
Be easy to administer, with extended dosing interval convenient for the patient.

Question 5

How does a patients characteristics effect dosage choice.

Answer 5

Young children and the elderly for example have difficulty swallowing and ingesting tablets so liquid dosage forms may be preferred.
Patients with impaired motor or memory skills may have trouble adhering to dosing schedules.

Question 6

How would a patients culture affect choice of dosage forms

Answer 6

In some countries, suppositories are routinely prescribed for pain whereas this suggestion may be declined in other nations.

Question 7

How would a patients medical condition affect choice of dosage form.

Answer 7

The severity and localisation of the pain will affect the route of administration and the dosage form.

Question 8

Examples of tablet forms of painkillers

Answer 8

Paracetamol, Aspirin, Ibuprofen, Diclofenac

Question 9

Advantages of Tablets

Answer 9

Convienient and easy to take
Chemical, Physical and microbiological stability
Can be prepared in versatile ways (controlled release)
Accurate dosing.

Question 10

Disadvantages of Tablets

Answer 10

The problem of poor bioavailability of drugs due to the unfavourable drug properties (poor solubility, poor absorption)
Local irritant effects.
Harm caused to the GI mucosa.

Question 11

What are some types of tablets.

Answer 11

Uncoated/Coated Tablets
Effervescent tablets
Soluble Tablets
Sublingual Tablets

Question 12

Advantages of Capsules

Answer 12

Chemical, Physical and microbiological stability
Allows for the controlled release of the drug.
Filled with dry solids or non-aqueous liquids.
Good patient compliance (use of colour for identification, Easy to swallow, Shell to mask the taste.
Accurate Dosing.

Question 13

Disadvantages of Capsules

Answer 13

Bulky Materials can result in large capsule size
Can be succeptible to moisture
Ingredients can interact with capsules shell.
More difficult to fill accurately
Capsule or Lubricant allergies
Softgel contents restricted to a tigh pH range
Hard capsules have to swallowed whole.

Question 14

What are some types of capsules

Answer 14

Hard Capsule- Open within 4 minutes of reaching the stomach.
Modified release tablets- release the drug continuously over a few hours.

Question 15

Why are caplets good.

Answer 15

presents the advantages of the tablet while being easy to swallow like a capsule.

Question 16

Advantages of Granules

Answer 16

can be intermediary for drugs normally administered as a solution or a suspension in an aqueous vehicle.
Reconstituted just prior to avoid chemical degredation
Powders are granulated to prevent agglomeration of the constituents of the powder mix
Faster dissolution rate than capsules or tablets.

Question 17

Disadvantages of Granules

Answer 17

Granules are not suitable method for the administration of drugs which are inactivated in or cause damage to the stomach .
Non-Masking of unpleasant taste

Less convenient to carry and to self-administer.

Question 18

Advantages of Suspensions

Answer 18

Convenient when the drug is not soluble in water and when a non-aqueous solvent cannot be used.
The insoluble solids act as a reservoir and continuously supply drugs into the solution.

Exhibit a higher rate of bioavailability compared to drugs in tablets or capsules.
Masking of unpleasant taste of drug.

Question 19

Disadvantages of Suspensions

Answer 19

Sedimentation of solids which causes a risk of caking which is difficult to disperse.
Risk of microbial contamination
Dose precision cannot be achieved unless suspensions are packed in unit dosage forms.

Question 20

Advantages of Syrups

Answer 20

Masking of unpleasant taste
Thick character has soothing effect in sore throats
Contain little to no alcohol
Easy to adjust fo child weight.

Question 21

Disadvantages of syrups

Answer 21

RIsk of deterioration and loss of potency faster than solid dosage forms.
Risk of incompatibilities between dissolved substances
Risk of bacteria and mould growth
Many flavouring and sweetening problems
Inaccuracy in the doses taken by the patient measuring with a spoon.

Question 22

Advantages of Suppositories

Answer 22

Absorption not affected by food or gastric emptying
Avoids pH changes in GI tract
Avoids action of gastric juices on drug
Avoids first pass metabolism
Good route of admin when vomiting
Used in paeds
No problems with flavouring.

Question 23

Disadvantages of Suppositories

Answer 23

irritation of mucus membrane
small surface area
less fluid for absorption
Drug degradation by bacterial flora
Interrupted by bowel movements
Patient acceptability

Question 24

What is topical administration

Answer 24

Application of a formulation to the skin to treat a local disorder.

Question 25

What is transdermal administration

Answer 25

Application of a formulation to the skin to deliver a drug to the systemic circulation

Question 26

What are advantages of gels.

Answer 26

Avoidance of serious adverse effects associated with oral NSAID’s, particularly in older patients
Achieve therapeutic concentrations of the drug in localised tissue while maintaining low serum levels of the drug.
Avoidance of the first pass
Good for people unable to take oral drugs.
Administration to the desired site of action
Increased compliance.

Question 27

Disadvantages of Gels

Answer 27

Difficulty to formulate, drug molecules must be small to go across the stratum corneum.
Must be aqueous and lipid-soluble
Variation of skin permeability among individuals
Local skin irritation

Question 28

Advantages of Transdermal Administration

Answer 28

Avoidance of the pH variations seen in Gi transit
Avoidance of the first pass hepatic metabolism
Can be removed quickly in adverse reaction

High patient compliance
Long duration of action

Question 29

Disadvantages of transdermal patches

Answer 29

Few drug molecules have the appropriate physicochemical and therapeutic properties for sustained transdermal delivery.

Question 30

What is a matrix patch.

Answer 30

Backing Layer
Drug/Adhesive layer
Release Liner
Skin

Ex Mezolar and Osmanil

Question 31

What is a reservoir patch

Answer 31

Backing layer
Drug reservoir
Rate controlling membrane
Adhesive layer
Release Liner

Fentalis, Tilofyl