Parenteral Products Flashcards
(27 cards)
1
Q
How are Drug Delivery Routes classified?
A
- Location e.g. oral, IV
- Can also be classified based on the target of action
- Topical (local)
- Enteral (system-wide effect, delivered via the GIT)
- Parenteral (systemic action, delivered by routes other than the GIT)
2
Q
What is a major advantage of Parenterals?
A
Have a more rapid onset of action than other delivery routes
3
Q
What are Parenteral Formulations?
A
- Sterile preparations (disadvantage) intended for administration by injection, infusion or implantation into the human or animal body
4
Q
Parenteral products can be divided into two general classes according to the volume of the product, what are these classes?
A
- Small-volume parenterals (SVP) or injections are < 100 mL
- Large-volume parenterals (LVP) or injections are > 100 mL
5
Q
What are the Types of Formulations that can be delivered via Small Volume Parenterals?
What are the types of containers?
A
- Solutions, emulsions, suspensions, dry solids
- Single dose ampoules (glass or plastic), Multiple dose vials, prefilled syringes
6
Q
What are the Types of Formulations that can be delivered via Large Volume Parenterals?
A
- Aqueous solutions or emulsions
- +/- additional drugs
- Infusion fluids
- Total parenteral nutrition
- IV abx
- Patient controlled analgesia
- Dialysis fluids
- Irrigation solutions
7
Q
List 2 complications associated with Large Volume Administration Apparatus
A
- Adsorption to surfaces
- Leaching of components from apparatus
8
Q
List the Categories of Parenteral Formulations
A
- Injections
- Infusions
- Concentrates for injections or infusions
- Powders for injections or infusions
- Gels for injections
- Implants
9
Q
Injections
- What formulations can be used?
- How are they prepared?
- Solutions are?
- Emulsions?
- Suspensions?
- Multidose injections contain an antimicrobial preservative, but not when?
A
- Sterile solutions, suspensions or emulsions
- Prepared by dissolving, emulsifying or suspending the active (and excipients) in water, a suitable non-aqueous liquid
- Solutions are clear and practically free of particulate matter
- Chunks don’t get stuck when moving through body
- Emulsions show no evidence of separation of phases
- Preparing a stable system
- Suspensions may show a sediment that is readily redispersed
- Multidose injections contain an antimicrobial preservative, but not when:
- The volume of injection > 15 mL
- It is to be given by an intracisternal, epidural, intrathecal or other route into the CSF
10
Q
Infusions
- What are they?
- Preparation?
- Solutions are?
- Emulsions are?
- Tonicity?
- Particle size is what?
- Volumes?
A
- Sterile solutions or polyphasic (o/w emulsions, colloidal suspensions, nanoparticulate dispersions)
- May be a readily prepared solution or an admixture
- Solutions are clear and practically free of particulate matter
- Emulsions show no evidence of separation of phases
- Iso-osmotic with respect to blood
- Particle size of polyphasic systems is controlled
- Larger volumes administered for an extended period
11
Q
Routes of Administration: What are the Characteristics of IV?
A
- Most rapid onset
- Complete bioavailability
- Bolus or infusion
- Aqueous solutions, emulsions, suspensions
- Less irritation
12
Q
What are the 2 Types of IV?
A
- Peripheral intravenous administration
- Central intravenous administration
13
Q
Routes of Administration: What are the Characteristics of IM?
A
- Easier administration than IV
- Slower onset but more prolonged action than IV
- Limited volumes; 2-5 mL
- Iso-osmolarity essential, no dilution occurs
- Solutions, suspensions & emulsions
- Delayed-release products
14
Q
What Muscles are used to give IM?
A
- Vastus lateralis
- Deltoid
- Gluteus maximus
15
Q
Routes of Administration: What are the Characteristics of SC?
A
- Slower onset than IM
- Technically simpler
- Less discomfort
- Lower risk of complications than IM
- < 2 mL bolus; slow infusion
- Narrow control of pH and tonicity
- Solutions, suspensions & emulsions
- Drugs ineffective orally - insulin, vaccines, some anticoagulants
16
Q
Routes of Administration: What are the Characteristics of ID?
A
- Absorption very slow
- < 0.1 mL
- Diagnostics and vaccines
17
Q
What are other routes of Parenteral Administration?
A
- Intra-arterial
- Usually requires surgery to expose the artery
- Localize larger fraction of dose to a tissue (chemotherapy)
- Intra-articular
- Directly into joint
- Intrasynovial
- Joint fluid area
- Intracardiac
- Directly into the heart
- Intraspinal
- Anaesthesia
- Analgesia
- Antispasmodic agents
- Antibiotics
18
Q
What are Disadvantages of Parenteral Products?
A
- Expensive to manufacture (more complex manufacturing)
- Require trained personnel to administer
- Difficult to remove if adverse or toxic reaction
- Patient acceptability – varying levels of pain
- Introduction of micro-organisms/toxins - potentially fatal (especially as patient often already very sick)
- Thrombosis, phlebitis, air emboli, haemolysis, precipitation in the vein, extravasation, tissue/nerve damage
19
Q
What are the Requirements of Manufacturing Parenteral Products?
A
- All parenteral products are sterilized and must meet all the requirements for sterility and particulate matter and must be pyrogenfree
- They must be prepared using strict sanitation standards in environmentally controlled areas by individuals trained to meet these standards
- The injections are overfilled with a small excess over the labelled volume to ensure that the required volume can be obtained from the product
20
Q
What is Lyophilisation (Freeze Drying)?
A
- A process that removes water from a liquid drug creating a solid powder, or cake
- The lyophilized product is typically stable for extended periods of time and MAY allow storage at higher temperatures.
- In protein formulations, stabilizers are added (e.g. sugars) to replace the water and preserve the structure of the molecule
- Lyophilized drugs are stored in vials, cartridges, dual chamber syringes, and prefilled mixing systems
21
Q
What are Advantages and Disadvantages of Formulating Parenteral Products?
A
- Advantages
- Easy to formulate
- Uniform doses
- Suitable for all routes of administration (aqueous)
- Prolonged clinical effect (oil-base, IM SC routes)
- Disadvantages
- Not suitable for
- Insoluble actives
- Depot effect
- Not suitable for
22
Q
Parenteral Formulations: Preparing Solutions
What Characteristics can be used to prepare solutions?
A
- Improve solubility, improve/maintain dispersibility
- Solvent/co-solvent
- Surfactants
- Polymers
- Make formulation iso-osmotic with blood
- Adjust pH
- Buffers
- Prevent degradation of active ingredients
- Antioxidants
- Chelating agents
- Provide adequate antimicrobial properties
- Preservatives
- Modify rate of release of active ingredient
23
Q
What are Important Factors during Formulation of Polyphasic Systems?
A
- Particle size - emulsions and suspensions
- Homogeneity of disperison
- Viscoity
- Sterile and free of pyrogens
24
Q
Why would we administer parenteral emulsions?
A
- Lipids as a source of nutrition (parenteral nutrition)
- Emulsion of an insoluble liquid active ingredient (e.g. propofol)
- Solution of a poorly aqueous soluble drug in oil (e.g. diazepam)
- Avoids use of more toxic co-solvents for dissolution
- Avoids risk of precipitation from co-solvent mixtures
- Potential for delayed-release from i.m., s.c. administration
25
What oils are used for Parenteral Emulsions?
* General oils: soybean, safflower, arachis, sesame, corn (all 10 to 20%); castor (20%); coconut (≈ 30%)
* Medium-chain triglycerides: synthesized by re-esterifying fatty acids (octanoic, decanoic) from coconut oil with glycerol (glycerin)
26
What are the Reasons for Using Parenteral Nutrition in Australia?
* Inaccessible gastrointestinal tract
* Complete rest for tract e.g. upper tract fistula • Loss of tract function (e.g. ileus1 )
* Severe vomiting and diarrhoea
* Severe mucositis
* Nutritional requirements unable to be met adequately via the gastrointestinal tract
27
How can Parenteral Emulsions be Stabilised?
* Tightly packed layer
* Surface charge
* Steric stabilisation
