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93 Cards in this Set

  • Front
  • Back
What is an ophthalmic?
A topical preperation for application to the eye to treat surface or intraocular conditions.
Name 5 types of conditions that can be treated with ophthalmics?
1. Antimicrobial

2. Mydriatic and cycloplegics

3. Allergic or infectious conjunctivitis or inflammation

4. Elevated intraocular pressure and glaucoma

5. Dry eye syndrome
Where does the drug MAINLY diffuse into the eye?
Mainly through the cornea.
What may happen through the conjunctiva of the eye?
What is more capable of penetrating through the eye cornea?
Lipophilic compounds
The normal volume range for tears?
7-10 microliters
The volume of tears in a blinking eye?
10 microliters
The average volume of a drop?
50 microliters
The tear system could also be referred to by this name?
The lacrimal system
What removes drugs that are applied to the eye?
The naso-lacrimal apparatus
What causes tear volume to exceed 10 mL when a drug is applied to the eye?
Reflex tearing
The involvement of the GI tract in the fate of drugs applied to the eye indicates what?
That there could be possible l(although minimal) systemic effects.
Drugs applied to the eye have superficial adsorption through the ? and rapid removal by ? ? ?.
Superficial adsorption through the conjunctiva and rapid removal by peripheral blood vessels
The ocular absorption of a drug is ? of the administered dose.
It is less than 1% of the administered dose.
4 methods to deliver more drug to the eye?
1. Suspension

2. Ointment

3. Patient can apply pressure to lacrimal sac

4. Increase drug concentration
How do suspensions make it possible to deliver more drug to the eye?
Some drug will adhere to conjunctiva and will be able to be absorbed later.
Name 4 ophthalmic dosage forms?
1. Ophthalmic solutions

2. Ophthalmic suspensions

3. Ophthalmic ointments

4. Ophthalmic inserts
Generally what kind of compounds are more capable of penetrating through the eye cornea?
Lipophilic compounds
Generally ophthalmic ? have longer effects when compared to solutions?
What are commonly used in the formulation of ophthalmics?
1. White petrolatum

2. Mineral oil base
All ophthalmics products are required to be what?
They need to be sterilized in addition to any preservatives.
Ophthalmic solutions need to be sterile and free from ? ?.
Free from foreign particles.
How many drops should be applied when using an eye dropper bottle?
One drop only. (Not two or three)
What do you do if more that one drop is required from an eye dropper bottle?
You need to space them at least 5 minutes apart.
How can you reduce the rate of drug loss when using a dropper bottle?
Press on the lacrimal sac for about 1-2 minutes.
What are suspensions?
AQUEOUS formulations containing SOLID particles.
The particle size in a suspension must be kept to a ? to prevent ? of the eye.
The part. size must be kept to a MINIMUM to prevent IRRITATION of the eye.
It has been recommended that particles in suspension be less than ? ? in size to minimize irritation to the eye.
Less than 10 microns.
In suspensions you use the ? ? of the drug.
You use the micronized form of the drug.
How does a suspension increase the duration of action when compared to a solution?
The undissolved particles adhere to conjunctiva until they can be absorbed.
What do ointments help the drug do?
They keep the drug in contact with eye longer than suspensions.
Most opht. ointment bases are a mixture of ? and ? and have a melting point close to ?.
Most are a mix of white petrolatum and M.O. and have a melting point close to body temperature.
Why would Anhydrous Lanolin be used in the preparation of ointments?
Sometimes they are used to take up an ingredient that was dissolved in a small amount of water to affect dissolution. Anh. Lan. is an absorption base with a tendency to absorb H2O. So you would dissolve a drug in H2O then add to lanolin and then add to the ointment.
Are ointments irritating to the eye?
No, they are nonirritating.
Ointments are free from ?.
Free from grittiness.
Ointments utilize ? form of ingredients.
Use micronized form (like suspensions do).
When preparing ointments you must ? all of the individual ingredients and then combine them under ? conditions.
You must sterilize them and then combine them under aseptic conditions.
What are ointments packaged in?
A sterile container such as an ointment tube.
When are ointments generally used and why?
Generally used at night because they could effect your vision.
Ophthalmic ointment tubes generally hold how much ointment?
3.5 grams per tube.
Name the 2 categories of inserts.
1. Non-erodible

2. Erodible
Give an example of a brand name for a non-erodible insert?
Ocusert (This was the first CR topical dosage form marketed in the US by Alza in 1973)
What does Ocusert deliver and what does it treat?
It delivers pilocarpine over the period of several days to tx glaucoma.
Describe the structure of a non-erodible ocular insert?
Soft and flexible elliptical membrane designed to be placed in the cul-de-sac.
Name 2 advantages of Non-erodible ocular inserts.
1. Steady levels for 7 days intraocular pressure (IOP)

2. vs. qid dosing from drops : potential fluctuation in IOP
Name 3 disadvantages of non-erodible ocular inserts.
1. Cost

2. Comfort

3. Tendency to float
Give an example of a brand name of an erodible ocular insert.
Lacrisert (Alza company)
What make an erodible ocular insert erodible?
Controlled erosion of the polymer matrix of the insert.
Erodible ocular inserts are ? soluble because of ? ? compounds.
The are poorly soluble due to high M.W. compounds.
Erodible ocular inserts are taken how many times a day and are used to treat what?
Taken qd or bid for moderate to severe dry eye syndrome.
An erodible ocular insert may be composed of this?
5 mg of hydroxypropylcellulose (anhydrous) in a rod shape
Where are erodible inserts placed?
Placed in the cul de sac.
2 disadvantages of erodible inserts?
1. Comfort

2. Tendency to float
3 limitations of absorption for ophth.s?
1. Limited surface area

2. Resistance for permeation

3. Continous washing
List 10 uses for ophthalmic products.
1. Anti-inflammatory agents

2. Antibiotic/Antimicrobial

3. Antiviral agents

4. Astringents

5. Beta-adrenergic blocking agents

6. Local Anesthetics

7. Miotics

8. Mydriatics

9. Topical Protectants

10. Vasoconstrictors
The capacity of the eye to retain liquids and ointments is ?.
Topical applications are administered in ? ?.
Small amounts
6 formulation factors to consider with ophth.s.
1. Buffer

2. Iso-tonicity

3. Antioxidants

4. Preservative

5. Viscosity

6. Sterility
What is a buffer?
A compound that resist changes in pH upon the addition of limited amounts of acid or base.
What is the optimum physiologic pH of blood and tears?
It is approximately 7.4
Although the optimum pH for blood and tears is approx. 7.4 what can be said about the eye?
The eye can tolerate a wider range. The appropriate pH to prevent corneal damage is 6.5-8.5.
Give 5 reasons why a buffer would be used in the preparation of ophth.s.
1. To reduce discomfort to the patient

2. To ensure drug stability

3. To enhance aqueous solubility of drug

4. To control the therapeutic activity of drug substance

5. To maximize preservative efficacy
Isotonic solutions do not ? tissue or cause ?.
Do not damage tissue or cause pain.
Isotonicity is important for ?.
Name 4 tonicity adjusting agents.
1. NaCl

2. Mannitol

3. Glycerin (1%)

4. Propylene Glycol (1%)
Lacrimal fluid has the tonicity of ? ?. Which is ?%.
The tonicity of normal saline which is 0.9%.
Although lacrimal tonicity is 0.9% what is an acceptable range?
The eye can tolerate ? solutions more that ? solutions. Why?
Can tolerate hyertonic solutions (>0.9%) more than hypotonic solutions (<0.9%). This is because a ruptured cell can not be prepared and a hypotonic solution would cause cells to take on water, swell, and possible burst.
Why are antioxidants used in the preparation of ophth.s?
They are used to delay or prevent deterioration of the drug because otherwise it could oxidize.
Give 3 examples of antioxidants used in the preparation of antioxidants.
1. Sodium metabisulfite

2. Ascorbic acid

3. Edetic acid
When would a preservative be used in the preparation of ophthalmics?
Only used if the preparation is to be put in a multi-use container.
A single use container for an ophthalmic does not need to be ? but it still needs to be.
Does not need to be preserved but it still needs to be sterilized.
What do preservatives inhibit?
They inhibit the development of microorganisms
Preservatives are added in ? ?.
Low concentrations
Name 5 examples of preservatives used in the preparation of ophth.s.
1. Benzalkonium chloride

2. Thiomerosal

3. Chlorobutanol

4. Polyquat (polyquaternium-1)

5. Methyl- and propylparaben
How does increased viscosity affect retention time?
Viscosity increases retention time.
How does increased viscosity affect the drainage rate?
Viscosity decreases the drainage rate.
How does increased viscosity affect the ocular bioavailability of a drug?
Viscosity increases the ocular bioavailablity.
Viscosity causes products to have a ? effect.
To have a lubricant effect.
Some examples involved in giving products viscosity?
1. Cellulose derivatives (hydroxypropylmehtyl and methylcellulose)

2. Polyvinyl alcohol
A diadvantage of increased viscosity in a preparation?
Crust formation and transient blurring.
Every ophthalmic product must be ? in its final container to prevent ? of the eye.
Every product must be sterile to prevent contamination of the eye.
? are added to the formulation to maintain ? once the container has been opened.
Preservatives are added to maintain sterility once the container has been opened.
Why do we sterilize ophth. formulations?
Because contaminated formulations may result in eye infections that could ultimately cause blindness.
What is the most dangerous organism related to eye infections?
Pseudomonas aeroginosa
Where should product be prepared?
In a laminar flow hood.
For sterilization purposes ? should be filtered and ? should not be filtered. Obviously, ? cannot be filtered. Explain.
Solutions should be filtered and suspensions should not be and ointments obviously cannnot be. If a suspension is filtered it is possible to filter out the drug.
In sterilization ? ? are sterilized ?.
Individual ingredients are sterilized separately.
Ophthalmics are formulated using ? ?.
Aseptic techniques
Describe the packaging of eye drops.
1. Plastic dropper bottles

2. Low-density polyethylene (LDPE)

3. 5, 15, and 30 mL
Describe the packaging of eye ointments.
1. Small collapsible tubes

2. Usually tin

3. 3.5 g
Patient consultation for the use of ophthalmic drops? (4 steps)
1. Wash hands

2. Draw lower lid

3. Instill 1 drop, don't touch eye with dropper

4. Try not to blink for 30 seconds, press fingers on lower corner for about 1 minute. Tightly cap the bottle.

(Also make sure you warn about contamination : Try not to wear contacts, make-up, etc.)
Patient consultation for the use of ophthalmic ointments? (4 steps)
1. Wash your hands

2. Draw lid

3. Squeeze oint. in eye

4. Close eye and rotate