Q1:Ophthalmic preparations are used to treat...

allergies, bacterial & viral infections, glaucoma and other

eye conditions
Q2:Which application is most often used to deliver a drug
to the eye?
solution- have a short duration action but spread easily
over the globe of the eye
Q3:What base is primarily used for Ophthalmic ointment
preparations
white petrolatum
Powders incorporated in the preparation must be
micronized and sterilized to ensure that the final
preparation is not gritty and thus is nonirritating
The size of the particles in an Ophthalmic suspension
must be
small enough that they do not irritate or scratch the
cornea. The micronized form is required. Ophthalmic
suspensions must be free from agglomeration or caking.
When preparing Ophthalmic solutions you must consider
these physiochemical parameters:
Clarity
tonicity
pH/buffers
sterility
This is usually used to remove particles and achieve
clarity of the solution
Filtration
The ideal tonicity is
300 mOsm/L however a range of 200 to 600 mOsl/L is
acceptable
A sodium chloride equivalent is defined as
the amount of sodium chloride that is osmotically
equivalent to 1g of the drug
Agents used to adjust tonicity
Boric acid
Dextrose
Glycerin
Mannitol
Potassium Chloride
Sodium Chloride
Ophthalmic solutions must be...
sterile
Sterility of an Ophthalmic solution is best achieved by...
sterile filtration which involves a 0.45 or 0.2 micron and
filtering into a container
Other methods of sterilizing or components of
Ophthalmics include...
dry heat
steam under pressure (autoclaving)
gas sterilization with ethylene oxide
Because most Ophthalmic solutions and suspensions are
prepared in multidose containers, they must be...
preserved with a preservative
A preservative must be...
compatible with the active active drug and other excipients
Q4:DO unit dose preparations need to be preserved?
no they can be preservative free
Examples of antioxidants used for Ophthalmics
EDTA
sodium bisulfite
sodium metabisulfite
thiourea
Viscosity enhancers allow the preparation to remain longer
in the eye to allow for more time for the drug absorption
and effect. The most common viscosity enhancer used in
Ophthalmics is...
methylcellulose
With a viscosity enhancer (actually all enhancers) it is
important for this to be maintained
clarity
Storage of Ophthalmic solutions
should be stored at room temp or refrigerated
(refrigeration decreases microbial growth)
Ophthalmic preparations should be labeled with
For the eye
Do not touch the eye or eyelid
Store as directed
Dispose after (appropriate date)
BUD for Ophthalmics ...
follows USP 797 because it is a sterile preparation
Patient counseling...
-cautioned not to allow the tip of dropper to touch eye or
any part of the eye
-allow the drug to freely fall into the eye an not to allow the
drug to touch the eye
How many drops should be administered to the eye at
once..
1 drop
For more than one drop or more than one drug is to be
administered the patient should wait how long between
doses to allow the drug to be distributed and absorbed
wait about 5 minutes
an advantage of an Ophthalmic suspension is...
they dissolve slowly and remain in the cul-de-sac longer
Ophthalmic ointments provide
maximum contact between the drug and the eye because
they are cleared quite slowly (0.5% per minute) from the
eye
T/F: the size of the drop delivered can vary with the angle
of the dropper and the size of the dropper orifice
true
Otic suspensions can be used when a
long duration of drug effect is desired or when the drug is
not soluble in the vehicles commonly used in otic
preparations
Categories of medications commonly use in the ear are:
Local anesthetics
Cleaning agents- peroxides
Anti-infectives
Antifungals
Liquids for cleaning, warming, or drying the external ear
and for removing any fluids that can be entrapped by local
ear wax build up
Vehicles most often used in otic suspensions are
glycerin
propylene glycol
PEGs such as PEG 300
agents are primarily used for otic irrigation
water and alcohol
good oil vehicles
Vegetable and olive oil
-Mineral oil is the vehicle used for some antibiotics
Otic ointments primarily use this vehicle
petrolatum
physiochemical considerations when developing otic
preparations
Solubility
Viscosity
Tonicity
Surfactant properties
Preservatives
Although sterility is not generally a consideration the
preparations need to be ...
clean
Why is the viscosity of an otic preparation important
keeps the medication in the ear canal; if the medication is
too thin it will drain out of the ear
If the otic preparation is hypertonic some fluid can be
withdrawn from the ear and thereby releasing some
pressure
Many otic preparations are self preserving because of the
high concentration of
glycerin, propylene glycol
Packaging of otic preparations
Otic preparations should be packaged in dropper
containers, or tubes appropriate and method of
administration
Storage of otic preparations
-should be stored at room temp or in refrigerated temps
-they should not be frozen
Labeling for otics
labeled
"for the ear"
"discard after appropriate date"
"use only as directed"
Stability for otics
These preparations do not generally have to be sterile but
do need to be "clean" so the BUD is 30 days for topical;
and water-containing formulations.
patient counseling for otics
instructed how to apply drops to the ear from dropper
bottles and they should be told to place a cotton or gauze
pad in the ear to keep the liquid from escaping.
Nasal solution Preparations:
nasal solutions are prepared for administration either as
sprays or drops.
Nasal suspensions:
are liquid preparations containing insoluble materials
Nasal gels and ointments are...
semisolid preparations for nasal application that can be
used either local or systemic effects
Gels have what type of solubility
water soluble
what is collunaria
is the term for early nasal preparations that contained
various oils as the vehicles...this shifted to aqueous
vehicles because the oil could harmful to the nose
In addition to the active drugs nasal preparations contain a
number of excipients which include:
vehicles
buffers
preservatives
tonicity adjusting agents
gelling agents
antioxidants ( if required)
Ingredients used in nasal preparations must be
non irritating and compatible with the nose
Physiochemical considerations:
A vehicle for a nasal solution should have a pH in the
range of 5.5-7.5 and have a mild buffer capacity
Physiochemical considerations:
A nasal solution should be
isotonic, stable, preserved and compatible with normal
ciliary motion.
-and it should not modify the normal mucous viscosity
Physiochemical considerations pH & buffering:
Nasal preparations are ordinarily buffered at a pH of
maximum stability for the drugs they contain
The buffer system of nasal preparation should be
designed to maintain the pH...
throughout the expected shelf life of the preparation but
with a low buffer capacity
Generally pH range is considered to be optimum is
4-8
buffering systems are usually compatible with most nasal
medications...
phosphate buffer system
The preferred agents for adjusting of nasal solutions are:
sodium chloride and dextrose
tonicity
isotonic equivalent to 0.9% NaCl
If tonicity is BEYOND range what happens to the ciliary
movement
slows down or even stops
Tonicity values ranging ___ NaCl equivalency are
generally acceptable
0.6 to 1.8%
If a solution is hypotonic you can add this to the substance
to attain the proper tonicity
NaCl, boric acid, dextrose
What tonicity is ideal for nasal otics
300 mOsm/L or a range of 200-600
Are nasal preparations required to be sterile
no
preservations:
yes because they are prepared in multiuse containers
The preservative must be compatible with...
ACTIVE DRUG & EXCIPIENTS