Lecture PK-1: Formulation & Requirements of Parenteral Medicines 1 Flashcards

1
Q

alimentary canal

A

a continuous passage starting from the mouth and ending at the anus, which carries food through different parts of the digestive system and allows waste to exit the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

parenteral

A

Located outside the alimentary canal.

Taken into the body or administered in a manner other than through the digestive tract, as by intravenous or intramuscular injection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

intravenous ( IV)

A

rapid/predictable response
can be large or small volumes
solutions or emulsions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Intramuscular (IM or i.m.)

A

into a muscle; small volume of injection; relatively rapid absorption; can be used for controlled release formulations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Intradermal (ID or i.d.)

A

between the epidermis and dermis; up to 200 µL; allergy tests, some vaccines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Subcutaneous (SC or s.c.)

A

slower onset of action and sometimes <absorption of drugs; injection around 1 mL; route of choice for administration of insulin; can be used for implants

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Intrathecal (IT or i.t.)

A

into the cerebrospinal fluid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Epidural

A

outside the dura

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Intra-articular (IA or i.a.)

A

into the synovial fluid of a joint cavity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Intracardiac (IC or i.c.)

A

into the muscles of the heart;
only performed in emergencies

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Intra-arterial

A

similar to IV, but riskier so seldom used

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Intraocular

A

into the eye

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Advantages of Parenteral Formulations

A

Immediate physiological response (IV route) for acute medical situations, e.g., cardiac arrest, anaphylactic shock, asthma

Unconscious/uncooperative patients, patients with nausea/vomiting
Control of dosage and frequency of administration by trained medical staff (an exception being self-administration of insulin)
Requirement for localized effect
Correction of electrolytes (using infusion solutions)
Range of drug release profiles
Total parenteral nutrition (TPN)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Disadvantages of Parenteral Formulations

A

More complicated manufacturing process (aseptic technique); cost
Skill of administration: dosage form administered by correct route
Pain on administration, possible side-effects from rapid Cp elevation
Allergy to the formulation (rapid, intense reaction)
Difficult to reverse the effects of drugs that have been administered parenterally

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Formulation Considerations- Physicochemical properties of drug

A

Good solubility = solution
Moderate solubility = solution (with co-solvents), or suspension - caution: potential recrystallization
Low solubility = suspension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Formulation Considerations - Excipients

A

Co-solvents
Similar as for pharmaceutical solutions
Potentially greater toxicity when administered parenterally (toxicity IV> IM = SC)
Glycerol, ethanol, propylene glycol

Surfactants
As in solutions, suspensions
Non-ionic surface-active agents - e.g., Tween series (esp. for biologicals), poloxamers

Buffers
Acetate, citrate or phosphate salts to maintain correct pH
Preservatives
Must be included in multiple dose parenterals - e.g., benzalkonium chloride, benzoic acid, benzyl alcohol, cresol

Anti-oxidants
E.g., ascorbic acid and α-tocopherol (vitamins C and E; aqueous and oil-based preparations, respectively); sodium metabisulphite, sodium bisulphite; citric acid, EDTA (chelators)

Tonicity agents
Sodium chloride or dextrose

17
Q

Colligative Properties

A

Properties of solutions that are dependent on the ratio of solute particles to solvent particles in the solution, not the identity of the solute:
Vapour pressure depression
Boiling point elevation
Freezing point depression
Osmotic pressure

18
Q

Extensive Properties

A

Depend on the size of the sample e.g. volume, mass.

19
Q

Intensive Properties

A

Characteristic of the substance, independent of sample size e.g. density and concentration.

20
Q

Addition of a non-volatile solute to a solvent (water)

A

reduces the vapour pressure above the liquid

21
Q
A