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Dosage Forms ~
Final Exam - Exam 3
250
Medical
Professional
12/12/2008

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Cards

Term
Suppositories are designed for insertion in which orifices?
Definition
rectum, vagina, or the urethra
Term
What is the usual weight for rectal suppositories for adults? for children?
Definition
2 g for adults
1 g for children
Term
What are some of the reasons for administering a suppository?
Definition
Infants and small children may have trouble taking medications orally. Severely debilitated patients might also have the same problem.

ex. epileptic or people with migranes w/vomiting
Term
What are some of the advantages of suppositories over oral therapy?
Definition
-better bioavailability to the small intestine

- no irritation in the stomach

- no acidic pH or enzymes to destroy drug
Term
What are some of the disadvantages of suppositories?
Definition
- uncomfort

- variation in absorption

- irritation for mucous caused by some drugs or bases
Term
What feature of the large intestine is crucial for systemic effect of suppositories?
Definition
The many veins and arteries.
Term
True or False

- Anorectal physiology contains no villi/microvilli

- the pH range here is 5-6
Definition
- True

- False (ph is 7 to 8)
Term
How does a local action suppository work on hemorrhoids?
Definition
shrinks body tissue, astringent, local anesthetic, vasoconstrictor, anti pruritic, antiseptic
Term
What percentage of a drug will be absorbed in blood circulation after rectal insertion?
Definition
50-70%
Term
What are the 3 main physicochemical factors affecting rectal absorption?
Definition
1) lipid solubility

2) particle size

3) suppository vehicle
Term
The ideal suppository base should dissolve or disintegrate in the presence of mucous secretions...How much mucous fluid is in the rectum?
Definition
2-3ml
Term
What are the two classifications of suppository bases?
Definition
oleaginous bases (hydrophobic)

and

water soluble or miscible bases (hydrophillic)
Term
Suppositories are composed of the following:

1) active ingredients
2) _________
3) suppository base
Definition
2) additives (such as emulsifiers and preservatives)
Term
True or false

One of the active ingredients for systemic action includes bismuth subgallate
Definition
False

bismuth subgallate is an active ingredient for local action
Term
How is surfactant used in suppositories?
Definition
used as a pharmaceutical additive to improve quality.
Term
What is the most common oil-soluble base?
Definition
cocoa butter
Term
Of the acids bonded to glycerin in cocoa butter, what % is disaturated triglycerides?
Definition
80%
Term
True or False

Cocoa butter melts at room temperature
Definition
False

- solid at room temp, melts at body temp (but in Florida, should keep in fridge)
Term
Because cocoa butter is polymorphic compound, overheating it will convert it to what structure?
Definition
a metastable structure that melts in the 25 to 30 degree celsius range
Term
What are the 4 forms of cocoa butter crystal?
Definition
1) beta (mp 34-36)
2) beta' (mp 27)
3) alpha (mp 22)
4) gamma (mp 18)
Term
True or False

synthetic triglycerides consist of hydrogenated vegetable oils and also exhibit polymorphism.
Definition
False

they are hydrogenated vegetable oils, but DO NOT exhibit polymorphism.
Term
What is the usual color of a fattybase synthetic tryglyceride?
Definition
white
Term
What percentage of glycerinated gelatin suppositories are gelatin?
Definition
20%

70% = glycerin, 10% = water
Term
True or False

Glycerinated gelatins are recommended as a rectal suppository base
Definition
False

- they may exert an osmotic effect and a defecation reflex, thus useful for vaginal suppositories but not rectal
Term
What are some of the disadvantanges for polyethylene glycol polymers?
Definition
Incompatible with solver salts, tannic acid, aminopyrine, quinine, aspiring, benzocaine, and sulfonamides.
Term
What is the rate limiting step in the selection for an appropriate base?
Definition
how fast the drug gets into/diffuse/partition from the base into the rectal mucosa
Term
What are the 3 common methods of preparing suppositories?
Definition
rolled (hand-shaped)

compression-molded (fused)

fusion or melt molding
Term
How are suppositories generally measured?
Definition
by weight because they are often made from solid ingredients - thus density calculations and mold calibrations are required
Term
How do you calculate the density factor?
Definition
density factor = weight of drug/weight of base displaced
Term
What are some of the reasons for using the topical route?
Definition
hydration, protection, systemic effect, and local effect = drug action
Term
What are the different types of liquid preparations for dermatological formulations?
Definition
liniments

lotions

paints

ear drops
Term
What are some of the gels often used in preparation?
Definition
indocid

voltaren emugel
Term
What are some of the powder preparations in dermatological formulations?
Definition
cicatren

mycota powder
Term
What are some of the ointments used in dermatological formulations?
Definition
betnovate ointment

betadine ointment
Term
What are some of the aerosols used in dermatological formulations?
Definition
solarcain spray

mycota spray
Term
The skin composes what percent of human body weight?
Definition
16%
Term
The epidermis is composed of layers of _______
Definition
keratinocytes
Term
True or false

The epidermis prevents fluid loss
Definition
True
Term
What is the biggest layer of the epidermis?
Definition
the stratum corneum
Term
What divides the epidermis and the dermis?
Definition
the basal lamina
Term
The stratum lucidum (the clear layer) is only found on the _____ of the feet and the _____ of the hands.
Definition
soles

palms
Term
How are basophilic granules in the stratum granulosum often identified?
Definition
They are dyed with a base to cause a color change
Term
What kind of cells are found in the stratum spinosum?
Definition
cuboidal, polygonal, or squamus cells
Term
What is the typical amount of time for turnover for cells to go through all layers?
Definition
15-30 days
Term
Where are the mitotic, epidermal stem cells located?
Definition
in the stratum basale/germinativum (last layer of epidermis)
Term
The epidermal ridges are interlocked with dermal _______.
Definition
papillae
Term
What is skin color attributable to?
Definition
melanin amount, carotene content in subcutaneous fat and vascularization
Term
What is synthesized when epidermal cells are exposed to UV?
Definition
vitamin D3 (cholecalciferol)
Term
The dermis is a specialized thickened _____ _____ with a network of ______ fibers.
Definition
basal lamina
---
reticular
Term
What layer vessels supply epidermis?
Definition
the papillary layer
Term
What is the function of the sudomotor fibers in the dermis?
Definition
stimulates the sweat glands
Term
What percentage of body fact is in the hypodermis?
Definition
50%
Term
What are the 4 accessories (skin appendages)?
Definition
1) weat and sebaceous glands

2) hair follicles and hairs

3) nails

4) nerves & nervous receptors
Term
As a protective function - the skin is a barrier for which 6 things?
Definition
1) microbial barrier
2) chemical barrier
3) radiation barrier
4) electrical barrier
5) mechanical barrier
6) heat barrier
Term
What are the 3 rational approaches to topical treatment?
Definition
1) manipulate the barrier
2) direct drugs to viable skin tissues
3) skin treatment for systemic conditions
Term
In the penetration route of topical treatment - how is the drug eventually removed?
Definition
removed via circulation
Term
What are some of the treatments in the dermis corneum?
Definition
antipruritic and antihistamine
Term
What route of penetration goes through the appendages?
Definition
pilosebaseous unit and ecrine gland
Term
How do demulcents function?
Definition
can alleviate irritation of mucous membranes
Term
How do emollients function?
Definition
fat or oily substances used to increase moisture content of skin membranes
Term
What is the typical use of keratolytics?
Definition
causes peeling of skin - useful in treatment of eczema, acne, etc
Term
True or False
--

All topical agents must permeate the skin to act.
Definition
False
--
Not all topical agents must permeate the skin, however, the most common routes are transepidermal and transappendageal
Term
What are some biological factors that effect percutaneous absorption?
Definition
1) skin age
2) skin condition
3) regional skin sites, thickness
4) skin metabolism
5) circulatory effects
Term
What are some physicochemical factors that effect percutaneous absorption?
Definition
1) skin hydration
2) drug/skin binding
3) temperature
4) penetration enhancers
5) drug/vehicle interaction, dosage form properties
Term
Topical dosage forms generally contain what ingredients?
Definition
base or body of dosage form, medicinal agent, and preservative
Term
Ointments and creams are used topically for what purposes?
Definition
-protectants
-antiseptics
-emollients
-antipruritics
-kerotolytics
-astringents
Term
What is of prime importance when considering ointments?
Definition
The base or vehicle is the most important consideration.
Term
How are ointment bases generally classified
Definition
They are generally classified according to their interaction with water.
Term
Hydrocarbon bases are synonymous with _____ bases.
Definition
oleaginous
Term
True or false
--
Oleaginous bases are soluble in water.
Definition
False
--
insoluble in water, will not absorb water, and not water washable (need soap)
Term
What is the commercial product example of pertrolatum?
Definition
Vaseline
Term
What is an important therapeutic property of hydrocarbon bases?
Definition
Good occlusiveness (can have emollient effect) and prolonged contact with skin).
Term
What are the two types of absorption bases possible?
Definition
1) permit the incorporation of aqueous solutions - single phase

2) are without emlsions - two phase system
Term
Anhyrdrous absorption bases contain agents that confer an ability to absorb water and alcohol...however it can only absorb _____ to a lesser degree.
Definition
alcohol
Term
W/O absorption bases are similar to anhydrous absorption bases except ______
Definition
already contain varying amounts of water
Term
What are some of the characteristics of emulsion bases, O/W type?
Definition
- insoluble in water
- water washable
- will absorb water
- contains water
- emollient
- non-greasy
- non-occlusive
Term
Hydrophilic ointment - sodium laurylsulfate is an ____ agent
Definition
emulsifying
Term
A widely used water soluble base, glyceryl monostearate is composed of ______ alcohol esters.
Definition
polyhydric
Term
In the preparation of ointments, incorporation involves what tools?
Definition
mortar & pestle, spatula & slab
Term
Where does the "lost" ointment in the compounding process go?
Definition
It adheres to beakers, ointment tiles, or ointment pads
Term
After levigation, how should the final product feel?
Definition
Should slip, no gritty feel
Term
True or False

Levigation is the 2nd most common method for Rx compounding.
Definition
False
--
It is the MOST common method
Term
What are some of the disadvantages of levigation?
Definition
Poor uniformity, gritty feel
Term
True or False
--

Not all surfacants are compatible as levigating agents
Definition
True
Term
What are some methods to correct errors in compounding after levigation?
Definition
add more high/low viscosity component, keep triturating, or start over.
Term
In order to avoid excess heat during fusion, how are ingredients heated?
Definition
heated with a water bath.
Term
Fusion is used when solids can't be easily triturated...name some examples of these solids.
Definition
-beeswax
-cetyl alcohol
-paraffin
-stearic acid
-any fusible solid
Term
What are some of the pitfalls of over heating during fusion?
Definition
change in viscosity and discoloration...
Term
What is the appropriate fix for poor dispersion during fusion process?
Definition
reheat and add more surfactant
Term
How can you minimize the quantity of water lost through evaporation when mixing oil and aqueous phase?
Definition
Heat aqueous phase a few degrees higher than oil phase prior to mixing as aqueous cools faster than oil.
Term
Stability of the final product can be enhanced by melting the ingredient with the ____ melting point first.
Definition
highest
Term
True or False
--
It helps to use ice or water to accelerate the cooling process.
Definition
False
--
this may result in a change in consistency of the final product
Term
When should volatile ingredients such as oils, flavors, or drugs be added?
Definition
when the product is "cool to the back of the hand"
Term
When are preservatives not necessary to preserve ointments?
Definition
when there is no water present
Term
What are some common chemical antimicrobial preservatives for preserving ointments?
Definition
-p-hydroxybenzoates, phenols, benzoic acid, sorbic acid, quaternary ammonium salts, organic mercury compounds, and formaldehyde (no longer used)
Term
What is the most commonly used absorption enhancer in ointments?
Definition
DMSO - dimethylsulphoxide
Term
"vanishing creams" contain what two ingredients
Definition
water and stearic acid
Term
What is the usual internal phase range of o/w creams?
Definition
15-40% w/w
Term
What is the most acceptable topical dosage form?
Definition
o/w creams
Term
What are some of the differences between ointments and pastes?
Definition
- larger proportion of solid material in paste

- stiffer (paste)
Term
What is a common name for topical powders?
Definition
dusting powders
Term
What is a common physical problem with powders?
Definition
hygroscopicity can be a problem
Term
What are some of the therapeutic benefits of powders?
Definition
1) can promote drying

2) can reduce friction
Term
What are some characteristics of a gel?
Definition
semisolid systems

movement of dispersing medium restricted by interlacing 3d network of particles
Term
What are some of the common applications of gels?
Definition
-oral

-topical

-intranasal

-vaginal

-rectal
Term
When a gel mass consists of a network of small inorganic discrete particles, it is a ________ system
Definition
two-phase
Term
A single phase system is a gel mass that consists of a network of ________ particles
Definition
large organic
Term
Name the 6 classes of gels
Definition
1) hydrogel
2) h20
3) diapers crystalline
4) organogel
5) oil
6) non crystalline
Term
What is a major disadvantage of a gel?
Definition
requires preservatives to prevent bacterial/mold growth
Term
What is imbibition?
Definition
soaking up liquid without a marked increase in volume
Term
What is swelling (in terms of gel)?
Definition
soaking up liquid with an increase in volume
Term
What is syneresis?
Definition
when h2o comes out of a gel, causing shrinkage
Term
What is thixotropy?
Definition
viscous during storage but loses consistency and becomes fluid upon shaking
Term
What is the definition of xerogel?
Definition
where liquid is removed from a gel, only framework remains.
Term
What is the most common alginate?
Definition
calcium alginate gel
Term
What is alginic acid derived from?
Definition
seaweed
Term
In carbomers, gel viscosity is dependent on what?
Definition
pH
Term
What is the maximum of electrolytes that can be added before carbomer becomes a rubbery mass form?
Definition
3%
Term
What is the difference (other than viscosity) between carbopol 934 and carbopol 934p?
Definition
934P is only for pharmaceutical prep only and it is highly purified.
Term
The two advantages of cellulose derivatives are:

1) compatible with water and alcohol
2) ____________
Definition
2) viscosity of all derivatives is maintained over a wide pH range (3-11) - except CMC
Term
What is a common use of carboxymethyl cellulose?
Definition
broad food usage - salad dressings, ice cream (ex. fat free)
Term
What are the advantages of gum arabic as a gelling agent?
Definition
can thicken syrups

edible
Term
What is the molecular weight of gum arabic?
Definition
250,000-750,000
Term
What is a major factor in not using gum tragacanth?
Definition
high cost $$
Term
How is gelatine produced?
Definition
it is a protein produced by partial hydrolysis of collagen extracted from the bone and connective tissues of animals such as domesticated cattle, pigs, and horses.
Term
What composes over 95% of plastibase?
Definition
mineral oil
Term
What is a major advantage of plastibase as a gelling agent
Definition
temperature stability - can be heated upto 60 degrees celsius without substantial loss in viscosity
Term
What is a poloxamer?
Definition
a gelling agent that is thermoreversible. can be liquid @ cool or room temp and can become gel @ room or body temp
Term
What is bentonite composed of?
Definition
hydrated aluminum silicate formed from weathering of volcanic ash
Term
What are the only gelling agents recommended for oral intake?
Definition
carbopol 934p, methylcellulose, hydroxypropylmethycellulose, and cmc
Term
How would you fix the gelling agent's tendency to clump when added to dispersing medium?
Definition
sieve the agent onto the surface of medium as medium is stirring
Term
What are some tight containers for gel storage?
Definition
tubes, jars, squeeze bottles.
Term
What is the difference between topical solutions and topical tinctures?
Definition
solutions = aqueous vehicle

tinctures = alcoholic vehicle
Term
How do plasters work?
Definition
solid or semisolid - plasters spread upon backing for prolonged contact with skin

ex. salicylic acid plaster
Term
How is pyroxylin for collodions obtained?
Definition
action of mixture of nitric and sulfuric acids on cotton and consists chiefly of cellulose tetranitrate
Term
What is a common use of collodions?
Definition
used as adhesive to close small wounds, hold surgical dressings and topical medications.
Term
What types of cells compose the mucous membranes of the vagina and external surface of the cervix?
Definition
epithelial cells
Term
What is the normal vaginal pH?
Definition
pH 4-5
Term
In the vagina, what is the naturally occurring bacteria that releases a number of anti-microbial compounds?
Definition
lactobacilli
Term
What are some of the advantages of vaginal route of administration?
Definition
- avoidance of hepatic first-pass metabolism

- large surface area

- rich blood supply

- reduction in the incidence and severity of gastrointestinal side effects

- self insertion and removal of dosage form
Term
What are some disadvantages of vaginal administration?
Definition
limited to potent molecules (steroids)

adverse effects

hormone dependent changes
Term
What has replaced vaginal suppositories by virtue of their ease of preparation?
Definition
vaginal tablets
Term
What is the advantage of an intrauterine progesterone drug delivery sys?
Definition
no estrogens, hormonal action is local - only at the uterus
Term
Why are creams and gels preferred over ointments in vaginal administration?
Definition
Ointments are greasier than creams and gels
Term
What are hemorrhoids?
Definition
known as Piles, enlarged and engorged blood vessels in or around the anus
Term
What type of gel does a diastat rectal delivery system use?
Definition
non-sterile diazepam
Term
What is an alternative use for diastat?
Definition
used by nonmedical patient caregivers to stop seizures in patients who are known to have epilepsy
Term
What is an enema?
Definition
insertion of a solution into the rectum and lower intestine given to remove feces when an individual is constipated or impacted or in preparation for an examination or surgery, or to give drugs or anesthetic agents
Term
What is sodium phosphate solution used for enemas?
Definition
draws additional water from the bloodstream into the colon and increases the effectiveness of the enema
Term
What are the three main sections of the ear?
Definition
outer, middle, and inner ear
Term
The visible part of the outer ear is called _____
Definition
pinna or the auricle
Term
The middle ear's connection to the ________ tube is the reason for simultaneous ear & throat infection
Definition
eustachian tube
Term
What are the two sac like structures in the inner ear?
Definition
the vestibule
Term
What are some common disorders of the ear?
Definition
Ear infections

Meniere's disease

deafness
Term
What is otitis media?
Definition
an infection of the middle ear that is common in young children.
Term
If untreated, otitis media can cause scarring of the ______ membrane and a permanent loss of hearing
Definition
tympanic
Term
True or False
--

Ear drops are are typically mixed with h2o
Definition
False
--
typically mineral oil or organic solvent - never h2o
Term
What is another name for "swimmer's ear?"
Definition
otitis externa
Term
How are ear infections typically treated?
Definition
Antibiotic ear drops
Term
True or False
--

There is no cure for meniere's disease
Definition
True
Term
What some symptoms of Meniere's?
Definition
dizziness (vertigo)

ringing in the ear (tinnitus)

temporary hearing loss

a feeling of pressure or fullness in the ear
Term
What are the two main types of deafness?
Definition
conductive hearing loss

sensorineural hearing loss
Term
What is type of solvent are ear drops?
Definition
lipophillic solvent
Term
What is cerumen?
Definition
wax - normal secretion of cerumenous glands in the external auditory canal - can obscure or partially obscure the drum
Term
What occurs with an excessive accumulation of cerumen?
Definition
itching, pain, impaired hearing
Term
How are solutions used for wax removal warmed?
Definition
typically warmed by holding in hands
Term
OTC drops for wax removal are typically composed of _____
Definition
water, oil, peroxide solutions
Term
How long should you keep your head tilted upon administering ear drops, so it can spread in your ear?
Definition
5 minutes
Term
What are 4 practical considerations for oral tablet/capsule administration?
Definition
1) avoid esophageal adhesions
2) wetting capsules with water or saliva can help swallowing
3) do not crush or chew enteric coated tablets
4) maintain dissolution stability by storing tablets under proper conditions
Term
Name the 6 factors predisposing to adhesions
Definition
1) shape
2) size
3) surface properties
4) patient position
5) volume of water
6) disease
Term
Name 6 types of tablets
Definition
1) buccal/sublingual
2) lozenges
3) chewable
4) vaginal inserts
5) effervescent
6) fast-dissolving
Term
True or False
--

Lozenges are usually intended for a local effect
Definition
True
Term
Chewable tablets - often have a high _____ or xylitol content and flavorants
Definition
mannitol
Term
What type of tablets are prepared by compressing the drug with sodium bicarbonate and citric acid?
Definition
Effervescent
Term
Why are claims of fast dissolving tablets' faster onset of action often not true?
Definition
Drug dissolution can be rate limiting because of faster disintengration/dissolution
Term
Which method of tablet manufacture leaves a very porous product?
Definition
Lyophilization (freeze-drying)
Term
True or false
--

Effervescent excipients are hygroscopic
Definition
True
Term
What is the definition of buccal?
Definition
lining of the cheek - usually between the cheek and the gums
Term
What is the definition of sublingual?
Definition
Ventral surface of the tongue and floor of the mouth
Term
True or False
--
Administration of drugs to the oral cavity only achieves a local effect
Definition
False
--
Both systemic and local
Term
The oral mucosae includes the structure and properties between _______ and _______
Definition
intestinal mucosa and epidermis
Term
Why is the epithelium in the oral mucosae good for systemic delivery?
Definition
highly vascularized
Term
True or False
--
Buccal and sublingual membrane are keratinized to form a tough barrier
Definition
False
--
buccal and sublingual membranes are not keratinized
Term
Which is thicker, buccal or sublingual?
Definition
Buccal epithelium is 2-8 times as thick
Term
Which is more permeable? Buccal or sublingual?
Definition
Sublingual - nitroglycerins - small lipophillic
Term
What are some positives and negatives about saliva?
Definition
it can dissolve drug, but can also wash it away
Term
What are the 3 advantages of sublingual/buccal delivery?
Definition
1) avoidance of GI acid degradation, GI enzymatic degradation, and the hepatic first pass effect

2) can achieve rapid onset of action and high blood levels for some drugs

3) can also be used for prolonged action
Term
What are the 3 disadvantages of sublingual/buccal delivery?
Definition
1) relatively low permeability for drugs

2) the drug can be washed away

3) sometimes unpredictable bioavailability
Term
What are some differences between sublingual and buccal products?
Definition
sublingual - designed for rapid drug release over a short period of time

buccal - generally designed for slower drug release over a sustained period of time (but some buccal products can give fast relief)
Term
Sublingual tablets include compressed and _____
Definition
molded
Term
What is an example of a compressed sublingual tablet?
Definition
isosorbide dinitrate

nitroglycerin

hyoscyamine sulfate

ergotamine tartrate

cyanocobalamin
Term
True of False
--
Compressed tablets tend to be softer than molded tablets
Definition
False
--
Molded tablets tend to be softer
Term
Name some excipents that are used with NTG in modling NTG tablets.
Definition
1) lactose
2) polyethylene glycol
Term
How do chewing gums such as nicorette deliver nicotine?
Definition
nicotine bound to a cation exchange resin
Term
Lollipops are essentially ______ on a stick
Definition
lozenges
Term
What is the very lipophillic, high hepatic and intestinal first pass lollipop used for pain?
Definition
fetanyl citrate lollipop - actiq
Term
What characteristic of mucoadhesive tablets helps keep it in place?
Definition
very sticky
Term
What are some examples of mucoadhesive excipients?
Definition
1) striant - testosterone buccal system

2) nitrogard - prolonged form of nitroglycerin
Term
True or False
--
All orally disintegrating tablets are meant for GI absorption
Definition
False
Term
How are orally disintegrating tablets prepared?
Definition
by lyophilization
Term
Ophthalmic drug delivery is meant for ____ use
Definition
local
Term
Two types of products for ophthalmic deliver are ___ and ___
Definition
topical and injections
Term
Some common conditions treated by ophthalmic topical drugs are ____
Definition
1) glaucoma
2) infections
3) inflammation
4) dry eyes
Term
The eye wall of the eyeball consists of which three concentric layers?
Definition
1) outermost - conjunctiva/sclera and cornea

2) middle - uveal tract (chorioid, ciliary body, and iris)

3) innermost - retina
Term
How are the insides of the eyeball divided?
Definition
by the lens - into the aqueous and vitreous humors
Term
What is the approximate volume in the anterior chamber of the aqueous humor?
Definition
250 microliters
Term
The exit of the aqueous humor into the systemic circulation is mainly through _____
Definition
schelemm's canal
Term
What is the conjunctiva?
Definition
a thin, transparent, vascularized mucous membrane that extends from the edge of the cornea, across a portion of the sclera, then extends to the internal surface of the eyelids to form the conjunctival sacs
Term
What glands are responsible for tear production?
Definition
the lacrimal gland
Term
What is the pumping mechanism to the lacrimal canaliculi?
Definition
blinking of the eye
Term
What are the 4 major drug target areas of ophthalmic drugs?
Definition
pre-ocular structures

cornea

tissues in the anterior segment

tissues in the posterior segment
Term
The tear film of the cornea has what three layers?
Definition
1) mucoid layer

2) tear fluid

3) lipid film
Term
What is the function of the lipid film in the tear film?
Definition
reduces evaporation of the tear fluid
Term
What are some of the components of tear fluid?
Definition
aqueous solution of inorganic electrolytes, proteins, and glucose
Term
What are the disparate layers of the cornea?
Definition
epithelium, bowman's membrane, stroma, decemets membrane
Term
What are the most important layers for drug absorption?
Definition
epithelium, stroma, and endothelium
Term
What are the squamous cells on the surface of the corenal epithelium surrounded by?
Definition
surrounded by tight junctions and have microvilli
Term
What is the main barrier for drug passage through the cornea?
Definition
the epithelium
Term
What is the stroma composed of?
Definition
about 60 thin lamella, each composed of collagen fibers - and mostly water
Term
What is the single cell layer that provides metabolic exchange between the cornea and the aqueous humor?
Definition
the endothelium
Term
True or False
--
In transcorneal drug absorption, about 15% of the does (instilled as drops) will cross the cornea.
Definition
False, less than 5%
Term
What are some of the possible fates of the drops applied to the eye?
Definition
1) spillage
2) removal by nasolacrimal drainage
3) enzymatic degradation
4) conjunctival permeation followed by systemic absorption
Term
After crossing the cornea, where are the greatest concentrations usually achieved?
Definition
Within the aqueous humor in the anterior region of the eye
Term
What types of drugs can bind to melanin in the iris?
Definition
lipophilic drugs
Term
Other than the aqueous humor turnover - where can drugs enter the systemic circulation in the eye?
Definition
through the uveal blood vessels
Term
What are the two routes of systemic absorption of topical ophthalmic?
Definition
1) absorption through tissues encountered following nasolacrimal drainage

2) absorption through blood vessels in the conjunctiva
Term
True or False
--
A significant fraction of topical ophthalmics can be systemically absorbed in the nasal cavity
Definition
true
Term
The _____ is more permeable than the cornea and covers a much greater surface area
Definition
conjunctiva
Term
Over ___% of the instilled dose can be systemically absorbed
Definition
50%
Term
What are some important organisms to be concerned about in terms of ophthalmic sterility?
Definition
1) pseudomonas aeruginosa

2) staphylococcus aureus, candida albicans, aspergilus niger, escherichia coli
Term
What is the most widely used antimicrobial preservative in ophthalmic applications?
Definition
benzalkonium chloride
Term
What are some other important excipients in ophthalmic applications?
Definition
1) polyquad
2) thimerosal
3) chlorobutanol
4) oxidants
Term
What is the normal pH of tears?
Definition
7 - 7.4
Term
True or False
--
Tear film has a very limited buffer capacity
Definition
True
Term
How are ophthalmic buffers chosen?
Definition
based on compatibility with the drug product and on desired pH
Term
What is the normal osmolarity of tears?
Definition
between 302 and 318 mOsm/kg
Term
What factor in ophthalmic drugs is very important for comfort - and drugs out of this characteristic range can irritate
Definition
isotonicity
Term
What are the effects of increased viscosity in ophthalmic drugs?
Definition
increase retention time/reduced drainage rate
Term
Name some ophthalmic viscosity modifiers
Definition
glycerin

cellulose derivatives

polyvinyl alcohol

PEGs
Term
Eyedrops are sterilized by either ____ or _____ filtrate
Definition
sterilize

membrane filtration
Term
In formulation of eyedrop suspensions, particle size should be less than ___
Definition
10 micrometers
Term
True or False
--
Ophthalmic suspensions do no provide a drug depot, but mix with tears less rapidly
Definition
True
Term
What are some antioxidents in eyedrops?
Definition
sodium metabisulfities
Term
How are surfactants such as polysorbate and tyloxapol used in eyedrop suspensions?
Definition
used as wetting agents for suspensions and can facilitate spreading of the drops
Term
What are the main advantages and disadvantages of semisolid ophthalmics?
Definition
advantage - prolonged contact time

disadvantage - can cause blurred vision and matting of eyelid
Term
How are semisolid ophthalmics sterilized?
Definition
first using heat, then filtered while molten - the sterilized drug is added and excipients aseptically
Term
When using eyedrops - while eyelid is closed, apply gentle pressure against inner corner of eye for at least ___ seconds
Definition
30 seconds
Term
When using two different medications - use at least __ minutes apart
Definition
5 minutes
Term
True or False
--
When compounding ophthalmics, it is performed with the same precautions as for parenterals.
Definition
True
Term
What is an example of a gel former used in ophthalmics?
Definition
Carbomer or gums
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