FINAL Flashcards
refers to the injectable routes of administration. It derives from the Greek words para (outside) and enteron (intestine) and denotes routes of administration other than the oral routes.
parenterals
Are sterile preparations intended to be administered by injection under or through one or more layers of the skin or mucous membranes. They are usually packed in ampules or vials.
parenteral
parenteral solutions which are administered by intravenous route.
transfusion fluid
commonly used as injections and available in single dose containers or multiple dose containers
solutions/emulsions of medicaments for injection
these drugs are supplied as dry sterile solids which are dissolved in a suitable solvent for administration into the body.
sterile solids
Available in dry solids because drugs are not stable in solution form.
sterile solids
sterile suspensions of drugs in a suitable solvent and are administered by intramuscular route.
sterile suspensions
Liquid preparations that are drug substances or solutions thereof
[drug] injection
Dry solids that, upon the addition of suitable vehicles, yield solutions conforming in all respects to the requirements for Injections.
[drug] for injection
Liquid preparations of drug substances dissolved or dispersed in a suitable emulsion medium.
[drug] injectable emulsion
Liquid preparations of solid suspended in a suitable liquid medium.
[drug] injectable suspension
Dry solids that, upon the addition of suitable vehicles, yield preparations conforming in all respects to the requirements for Injectable
Suspensions.
[drug] for injectable suspension
sterile preparations should be free from all types of microorganisms.
sterility
Ophthalmic formulations must be especially free from Pseudomonas aeruginosa, gram-negative bacteria which is commonly found in ophthalmic formulations and can cause serious infections to cornea.
sterility
Parenteral preparations should be isotonic with blood plasma and body fluids.
isotonocity
Ophthalmic formulations must be isotonic with lachrymal secretions.
isotonocity
sterile formulations must be free from pyrogens and toxins.
• These products must pass pyrogen test as pyrogens are responsible for rise in body temperature.
free from pyrogens
these products must be free from foreign particles, dust, fibers and must pass clarity test.
free from foreign particles
pH of tears is about 7.4. pH plays crucial role in therapeutic activity, solubility, stability, and comfort to the patient.
pH of ophthalmic preparations
physical and chemical stability of sterile formulations should be maintained during storage.
stability
Commonly used non-aqueous vehicles
alcohols and oils
properties of sterile dosage forms
sterility
isotonicity
free from pyrogens
free from foreign particles
pH of ophthalmic preparations
stability
general process of sterile dosage forms
accumulation and selection of components
production facilities and procedure
control
packaging and labeling
vehicles, solutes, containers, and closures
accumulation and selection of components
the sequential steps of preparing the product, filtering the solutions, filling containers, and sterilizing the product
production facilities and procedures
evaluation and determination of components
control
all steps necessary to properly identify the finished product.
packaging and labeling
the component present in largest quantity. Normally, a it has no therapeutic value and is non-toxic. Nevertheless, it is of great importance in the formulation since it presents to the body tissues in the form of active ingredients or constituents’ absorption.
Vehicle
packaged in single-dose containers not larger than 1 L.
it must be pyrogen- free but does not have an allowable endotoxin level, not more than 0.25 USP EU/mL.
water for injection, usp
sterile water for injection containing one or more suitable antimicrobial agents. It is packaged in prefilled syringes or in vials containing not more than 30 mL of the water.
bacteriostatic water for injection, usp
may not contain any added substances.
water for injection
may not contain any antimicrobial agent or other added substances.
sterile water for injection
these are used primarily to effect solubility of certain drugs and to reduce hydrolysis.
water-miscible vehicles
these are often used as isotonic vehicles. The additional osmotic effect of the drug may not be enough to produce any discomfort when administered.
aqueous vehicles
Fixed oils are the most important group of this and used particularly for certain hormones.
non aqueous vehicles
factors that determine the quality of solutes for parenteral preparations
solutes
Preparation in
containers are required to contain bacteriostatic or fungistatic agent in adequate amount at the time of use to prevent the multiplication of microorganisms inadvertently introduced into the preparation when withdrawing a portion of it.
antimicrobial agents
Must be evaluated for their activity in the total formula to assure their activity when needed at the time of use.
antimicrobial agents
Common Antimicrobial agents with their concentration limits:
Phenylmercuric Nitrate and Thimerosal - 0.1%
Benzethonium Chloride and Benzalkonium Chloride - 0.1%
Phenol and Cresol - 0.5%
Chlorobutanol - 0.5%
Preserves the balance of acidity and alkalinity of a solution.
Used to stabilize a solution against a chemical degradation that would occur if there is a mark change in pH.
Buffers
Commonly employed buffers
acid salts: acetates, citrates, phosphates
most commonly used antioxidant
sodium bisulfate 0.1%
has been found to enhance the activity of antioxidant in some cases apparently by chelating metallic ions that would otherwise catalyze the oxidation reaction.
Sodium salt of Ehtylenediamine Tetra Acetic acid
known as bacterial endotoxins, are organic metabolic products shed from gram-negative bacteria, which can cause fever and hypotension in patients when they are in excessive amounts in intravenous injections.
pyrogens
These are products of the growth of microorganisms, chemically lipids in nature, sometimes containing phosphorus, and is attached a polysaccharide or a protein or both.
pyrogens
They are unwanted contaminants which are difficult to remove without affecting the product. This cause a febrile reaction in human being; these are rarely fatal but produces discomfort.
pyrogens
the greatest potential source of pyrogens
water
it will absorb pyrogens from water
ion-exchange resins
the most reliable method for eliminating pyrogens from water as they do not distill over.
distillation
this will remove pyrogens by absorption, but once the fibers are saturated, the rest of the pyrogens are no longer absorbed
Filtration with Asbestos filters
It also introduces pyrogens especially reused containers
Equipment
it may also contain pyrogens, hence must be purified by recrystallization, precipitate, washing or other means.
solutes
at present the use of these
containers is limited to components of disposable injection units where in contact with the solution is brief.
plastic
the container of choice for most injections. The basic structural network of glass is formed by Silicon oxide tetrahedron and boric acid enters the structure.
glass
glass container in general, will be suitable for all products, although sulfur oxide treatment is done to increase its resistance.
Type I Borsilicate glass
may be suitable for a buffered solution or one that has an acid reaction or is not reactive with glass.
Type II Soda-Lime treated glass
suitable for anhydrous liquids or dry substances.
Type III soda-lime glass
glass container not suitable for parenterals.
NP - Non-Parenteral Soda-lime glass
Commercially available
vary in size from
0.5 ml to 1,000 mL
sizes obtained as ampoules and vials
up to 1000 mL
size of single-dose container
1,000 mL
size of multiple dose containers
30 mL
are made up primarily of natural rubber (latex), a synthetic polymer or both.
closures
in pharmaceutical preparations, means destruction of all living organisms and their spores or their complete removal from the preparation.
Sterilization
