T/F: single-dose containers can be resealed and used again.
false
T/F: multi-dose containers can be resealed.
true
T/F: single dose containers can be large or small volumes.
true
T/F: multiple dose containers are usually no more than 30 mL.
true; to avoid too many penetrations/uses and too much antibacterial agent needed
What type of containers do drugs that are highly sensitive to hydrolysis go in?
Advantage bags/snap bags/nurse activated systems
T/F: it is common practice and permitted to have a slight excess in volume compared to what the label says.
true
What is the typical amount of fluid range that makes an LVP?
150-1000mL
single dose only!
T/F: SVPs can be used for direct injection into vein, subQ, IM, etc.
true
T/F: LVPs are used for IV infusion only.
true
T/F: LVPs contain antibacterial preservatives.
false; do not!
What are some types of LVPs?
Maintenance therapy
Replacement therapy
Fluid requirement
Electrolyte requirement
Caloric requirement
Parenteral nutrition
Blood replenishment
irrigation solutions
dialysis solutions
pellets or implants
What is a maintenance therapy?
for patients entering or recovering from surgery or unconscious
What is a replacement therapy?
for patients with heavy loss of fluid and/or electrolytes due to severe diarrhea or vomiting
What is a fluid requirement?
when water is administered in a solution with Dextrose or electrolytes (avoids hemolysis)
What is an electrolyte requirement?
Potassium: for hypokalemia after a severe burn, GI disease, acute alcoholism, poor nutrition
Sodium: for hyponatremia during excessive sweating, diarrhea, use of some diuretics
Chloride: maintains acid-base balance
Calcium, Magnesium, Bicarbonate, Acetate, Lactate, etc.
What is a caloric requirement?
D5W is used to maintain basal caloric requirements, reduce a calorie deficit, and minimize breakdown of proteins
T/F: you can give up to 10% D5W to a patient that needs more calories.
true
T/F: IVFEs or parenteral nutrition must be given into the central vein of a patient.
true
What is another term for parenteral nutrition?
hyperalimentation
What is parenteral nutrition?
an infusion of large amounts of basic nutrients like amino acids, dextrose, electrolytes, vitamins and fats
for patients unable to get oral or enteral nutrition
T/F: D5W can be given into a peripheral vein.
true
T/F: irrigation solutions are used for injection.
false; only for washing debris
T/F: Pellets/implants are a form of parenteral dosage form.
true
T/F: a pellet or implant does not need to be sterile before it is implanted in the body.
false
T/F: CFCs are not allowed in pharmacy anymore due to their harmful effects.
False; allowed, but manufacturer must prove why another gas can't be used
How are aerosols completely different from any other dosage form?
the dose is not dependent on the patient, it is dependent on the container, valve and propellant
What is the definition of an aerosol?
dispersion of pressurized liquid and/or solid drugs in a gaseous medium (propellant)
T/F: an aerosol can be made of a gas within a gas.
true; anesthetics
What forms can an aerosol be made of?
cream
ointment
liquid
gas
powder
gel
foam
T/F: aerosols can come in glass, plastic, or metal containers.
true
What is the main difference between an aeorosol for inhalation and one for dermatologic therapy?
an aerosol for inhalation has much smaller particles in the form of a fine liquid mist or fine solid
a dermatologic aerosol is made of coarse particles and is less critical for efficacy
What is the most common aerosol dosage form?
aerosols for inhalation (MDIs)
What size should a particle be if we want the aerosol to reach the trachea and bronchi only?
20-40 micrometer
What size should a particle be if we want the aerosol to reach the bronchioles?
5-10 micrometer
What size should a particle be if we want it to reach the alveolar ducts and the alveoli (deepest part of lungs)?
less than 2 micrometers
What determines the amount of drug received by a patient when they use an MDI?
the dual valve chamber
What happens when the actuator on an MDI is released?
the dose chamber is refilled for the next dose
T/F: there are vaginal and rectal aerosols.
true
What are two examples of foam or cream aerosols?
vaginal and rectal
What is an example of a translingual aerosol and where should it be administered?
Nitrolingual
goes under and on the tongue
What are all the different categories of aerosols?
dermatologic
inhalation
vaginal
rectal
translingual
space
surface
What are some advantages of aerosols?
contents do not become contaminated
drug is not affected by oxygen, moisture, or light
sterility is maintained
site of action can be controlled well
exact dose every time
drug delivered in a clean way
can provide cooling effect on skin
don't have to touch the affected area to get a uniform application of the drug
What are the 2 main components of an aerosol?
product concentrate
propellant
T/F: a propellant can be either a liquid gas or a non-liquefied compressed gas.
true
Why are CFCs bad?
they reduce ozone in the atmosphere and increase UV light reaching the earth
How do CFCs propel a drug product out of a canister?
they are nonpolar and organic, so they oppose the liquid and push it out
What happens if a CFC is combined with alcohol?
it forms HCl-- very bad for the patient
T/F: CFCs are generally liquids when compressed or cooled below boiling point, but are gases at room temp.
true
What dual role do CFCs serve?
propellant
solvent or vehicle
What part of CFCs makes them so bad?
the 'fluor' in fluorinated hydrocarbons such as chlorofluorocarbon (CFC)
T/F: CFCs have been prohibited for general use since 1978, but are still allowed for pharmaceutical use.
true
What are some examples of non-liquefied gases used in aerosols?
nitrogen
nitrous oxide
carbon dioxide
Which non-liquefied gas is completely insoluble in the concentrate?
nitrogen gas
What gas(es) are slightly soluble in the concentrate?
nitrous oxide and
carbon dioxide
Which non-liquefied gas is typically used to replace oxygen in a parenteral vial and is taseteless, odorless, inert and protects from oxidation?
nitrogen gas
Which two gases are expelled with the product concentrate to produce a spray or a foam?
nitrous oxide
carbon dioxide
What is the main principle of how an aerosol works?
the canister is under pressure at all times
when the valve (actuator) is pushed, the vapor pressure forces the liquid phase up through the valve and pressure is released
after some of contents is expelled, the equilibrium between the liquid and gas phases is reestablished
What are the 3 types of aerosol technology systems?
2 phase system
3 phase system
compressed gas system
What are the 2 phases in a 2 phase system for aerosols?
1. vapor phase (gas propellant)
2. liquid phase (mix of liquified gas + product concentrate)
What are the 3 phases in the 3 phase system for aerosols?
1. aqueous product concentrate
2. vapor phase (water-immiscible gas propellant)
3. water-immiscible liquefied propellant in bottom of container
T/F: only 2 phase and 3 phase systems require shaking before use, not compressed gas systems.
true
T/F: compressed gas systems are under much higher pressure than 2 or 3 phase systems.
true
T/F: there is only about 20-30% of product concentrate in a compressed gas aerosol system and the remainder is gas.
true
What is a compressed gas only system for aerosols?
the pressure of compressed gas (usually CFC) in the headspace of the container forces the drug up the dip tube and out of the valve
T/F: compressed gas systems for aerosol use do not have any harmful side effects.
false
What is the main side effect that you might see with use of a CFC compressed gas system for aerosols?
cardio effects because this gas also has an affinity for the heart and lungs
What are the 2 methods used to prepare aerosols?
cold filling
pressure filling
Which method should not be used to make aerosols that contain aqueous product concentrate?
cold filling
Explain cold filling for an aerosol.
cool container to -30 or -40 F
cool product concentrate to -30 or -40 F as well
liquefy propellant and also cool to same temp as above
add cold concentrate to cold container
add liquefied propellant
assemble valve parts
What aerosol method is most commonly used to prepare pharm. products?
pressure filling
Why is pressure filling the most common method used to prepare aerosols?
because there is less moisture contamination and less propellant is lost in the process
Explain pressure filling method for aerosols.
add product to container
assemble valve
evacuate air by using a vacuum
add liquefied gas under pressure
What are some aspects of an aerosol that need to be tested?
leaks
weak spots in container
valve accuracy
reproducibility of dosage
drug concentration
spray pattern
particle size
particle distribution in spray
T/F: it is acceptable for a patient to spray a facial topical aerosol directly onto their face.
false; spray into hand first!
also clean affected area first.
T/F: written instructions are all that needs to be given to a patient who is receiving an aerosol.
false; verbal too
T/F: some drugs for inhalation can be used for systemic effects after they are absorbed from the lungs.
true; Oxygen or halothane
T/F: some solutions for inhalation can come in the form of a capsule or ampule.
true
What are some miscellaneous preps for respiratory administration?
nebulizers
humidifiers
vaporizers
sprays
What is a nebulizer?
an apparatus that produces fine particles for inhalation (a rubber bulb + a glass chamber)
What is the difference between a vaporizer and a humidifier?
humidifier= cool mist
vaporizer= mist of hot steam
Which is louder, a humidifier or a vaporizer?
a humidifier
Which is more energy efficient, a humidifier or a vaporizer?
a humidifier
Which one would an elderly person most likely prefer, a humidifier or a vaporizer?
a vaporizer because heats a room and does not deposit minerals on furniture
Which one is free of bacteria and mold, a humidifier or a vaporizer?
a vaporizer
T/F: a spray contains a propellant.
false
What are sprays generally made of and used for?
made of aqueous or oleaginous solutions
for topical use on skin or in the nasal-pharyngeal tract
T/F: a spray may or may not have a metered valve.
true
What is the definition of an emulsion?
a dispersion of immiscible liquids (polar and non-polar together)
usually in the form of droplets within the vehicle
T/F: the dispersion medium is continuous.
true
T/F: the dispersion medium is the internal phase.
false
What is the emulsifier also known as?
surfactant or wetting agent
What are the different types of emulsions?
O/W
W/O
liquid
semisolid/liquid
What is an example of an oral emulsion?
simethicone, mylanta
What is an example of a topical emulsion?
estrasorb
What is an example of a parenteral emulsion?
IVFE (fat emulsion)
What is an example of a semisolid/liquid emulsion?
cream and lotion
T/F: oral emulsions are usually the w/o type.
false; usually o/w in order to hide the oil
T/F: emulsions allow for enhanced absorption because oil as small globules are more digestible and better absorbed.
true
T/F: emulsions allow us to mask the taste of drugs well.
true
T/F: the flavoring for an emulsion should go into the internal phase.
false; will do no good there, must be in external phase
T/F: most commercial emulsion bases are w/o.
false; most are o/w
What are 3 examples of w/o emulsion bases?
eucerin
nivea cream
polysorb hydrate
What are some common emulsifiers?
sodium lauryl sulfate (SDS)
triethanolamine stearate
wool wax alcohol
etc, etc
What are the 3 theories of emulsification?
1) reduction of interfacial tension theory
2) oriented-wedge or electrical double layer theory
3) plastic or interfaciall-film theory
Why do we want to reduce interfacial tension?
because it causes small drops to join or coalesce, forming a larger drop which will break an emulsion
Explain the Reduction of Interfacial Tension theory of emulsification.
2 immiscible liquids are shaken together in order to get the smallest spherical droplets possible
use a surfactant, which will lower the interfacial surface tension and break up large globules into smaller ones
Explain the Oriented-wedge/Electrical double layer theory of emulsification.
emulsifier forms layers surrounding either the oil or water globules
the emulsifier hydrophilic and hydrophobic portions will orient themselves into each phase, producing electrical forces that repel approaching droplets
the phase in which the emulsifier is more soluble will become the external phase
What has a hydrophobic (water hating portion) and a hydrophilic (water loving portion)?
soaps!
Explain the Plastic/Interfacial Film Theory of emulsification.
the emulsifier surrounds the droplets of the internal phase as a thin layer of film aDsorbed on the surface of the droplets
there must be enough film forming material to completely surround each drop of the internal phase
T/F: usually emulsifiers are only used by themselves and not with other emulsifiers.
false
What type of emulsifier should be used for the initial formation of an emulsion?
one that lowers interfacial tension
What type of emulsifier should be used to maintain the stability of an emulsion?
an oriented wedge emulsifier or an interfacial film emulsifier
What are some examples of carbohydrate emulsifiers?
acacia
tragacanth
agar
pectin
Which emulsifiers are plant derived and natural?
carbohydrates
What are some examples of protein derived emulsifiers?
egg yolk
gelatin
casein
What are some examples of colloidal clays used as emulsifiers?
bentonite
magnesium hydroxide
aluminum hydroxide
What are the 3 different categories of surfactants?
anionic agents
cationic agents
nonionic agents
What are some examples of anionic surfactants?
SDS
triethanolamine oleate
monovalent, polyvalent and organic soaps
What is an example of a cationic surfactant?
benzalkonium chloride
What are some examples of nonionic surfactants?
SPAN 40,60,80
Tween 20, 60,80
Myrj 45
Brij 30
For an anionic surfactant, the lipophilic portion is_____ charged?
negatively
For a cationic surfactant, the lipophilic portion is ____ charged?
positively
For nonionic surfactants, the lipophilic portion is ____ charged?
no inclination to ionize!
What type of emulsifiers should be used if you want to make an O/W?
carbohydrates
proteins
colloidal clays or high mol. weight alcohols, depending on what you're making
T/F: colloidal clay emulsifiers can produce o/w or w/o emulsions, depending on which phase has a greater volume.
true
What type of emulsifiers are used as thickening agents and stabilizers?
high molecular weight alcohols
What type of emulsifier should be used if you wanna make a w/o emulsion for external use?
cholesterol and its derivatives
What type of emulsifier should be used if you wanna make an o/w emulsion for external use?
stearyl alcohol (also a binding agent)
cetyl alcohol
glyceryl monostearate (also a suspending agent)
Which type of emulsifier should be added to a powder with low solubility or that is so small it will float?
surfactant/wetting agent
Which type of colloidal clay emulsifier is Wyoming a huge producer of?
bentonite
What are the 6 methods for preparing emulsifications?
1. beaker method
2. in situ method
3. bottle/forbes bottle/shaking method
4. auxiliary methods
5. wet gum/English method
6. dry gum/Continental method
T/F: alcohol should be added last to a dry gum emulsion.
true
What is the dry gum/continental method aka?
4:2:1 method
4 ml/g of oil
2 mL/g of water
1 g of emulsifier
What is the hydrocolloid?
the oil + the gum (dry gum method)
In the dry gum method, what is the order of mixing the 3 main ingredients?
oil+gum(emulsifier)
then add water all at once
In the wet gum method, what is the order of mixing the 3 main ingredients?
water+gum(emulsifier)
then add oil in small portions
Which method of emulsification favors the w/o final form?
wet gum method (because the oil is added last)
Which emulsification method favors the o/w final form?
dry gum method (because water is added last)
In which method of emulsification do you need to hear a cracking sound to know that you have made your primary emulsion?
dry gum method
What is a mucilage?
small quantity of water + gum that is made by trituration in the wet gum method
can also be used as a filler for baby food or food for elderly
Which method has a primary emulsion that is creamy and white?
dry gum method
Which emulsification method is a variation of the dry gum method and is used for volatile oils and low viscosity oils?
Bottle/Forbes bottle/Shaking method
Explain the Bottle/Shaking/Forbes bottle method of emulsification.
add emulsifer and volatile oil together and shake in short, rapid movements
add water all at once and shake
add other aqueous materials in small amounts, shaking after each addition
Which method should be used for synthetic emulsifying agents?
the Beaker method
Explain the Beaker emulsification method.
prepare oil and water phases separately with their dissolved ingredients
heat both phases to 60-70 C if needed
add internal phase to the external phase and stir
remove from heat
gentle and periodic stirring to congeal
(think of cold cream)
What are some auxiliary methods for emulsification?
hand homogenizer
mechanical stirrer (mixers)
What is the in situ soap method for emulsification?
you create a calcium soap (a w/o emulsion) by adding cacium hydroxide solution (lime water) + vegetable oil
When should you use the in situ soap method to make an emulsification?
to reduce surface tension
for topical preps
T/F: it is acceptable to add more to the external/continuous phase of an emulsion.
true
T/F: very small amounts of other things can be added to the internal phase of an emulsion, but extra emulsifier must also be added.
true
Which phase of an emulsion affects the ending consistency of the product?
the external phase
Which phase of an emulsion affects the emulsifiability of the product?
the internal phase
T/F: a mortar and pestle that are used to prepare an emulsification should have a rough surface.
true
T/F: when making an emulsification, the aqueous phase should be heated to a few degrees warmer than the oil phase (if heat is used).
true
What does an HLB value tell you about an emulsifying agent?
it is a number that is indicative of it's polarity
What does HLB stand for and what does it mean?
Hydophile-Lipophile Balance
it describes the characteristics of a surfactant based on its chemical structure
T/F: emulsifying agents usually have a hydrophilic and a lipophilic portion with one or the other being more predominant.
true
T/F: something that is polar will dissolve in water.
true
What is the typical range of values for an emulsifying agent that likes oil and will be good for making w/o emulsions?
1-10
What is the typical range of values for an emulsifying agent that likes water and will be good for making o/w emulsions?
10-20
What is the best way to make a stable emulsion?
use more than one emulsifier
an emulsifier with an HLB value between 1-10 is predominantly _____ and less _____.
lipophilic
less polar
an emulsifier with an HLB value between 10-20 is _____ and is more ______.
hydorphilic
highly polar
T/F: When blending emulsifiers, the HLB needed can be obtained even if that specific HLB value is not on hand by using alligation.
true
T/F: the preservative in an emulsion should be concentrated in the aqueous phase.
true
T/F: parabens are not good preservatives for emulsions.
false; the BEST
T/F: preservatives should be present in the un-ionized state in an emulsion.
true; will be most effective against bacteria
Why do we add antioxidants to emulsions?
to prevent rancidity of oils and fats
What are some common antioxidants used in emulsions?
ascorbic acid (citric acid)
butylated hydroxyl-anisole
gallic acid
sulfites
I-tocopherol
Which antioxidant are some patients allergic to and are also used in wines and foods?
sulfites
must be aware of patient allergy
"you don't want to be walking around w/ a big cloud of smell around you, unless you are wearing ______" -G
Chanel #5 :)
T/F: flavoring/odorants should be added to the internal phase of an emulsion.
false
When adding a flavoring oil to an emulsion, when and what should it be added to?
add to surfactants before addition to the aqueous phase
you can also add it to a cosolvent like glycerin or ethanol
T/F: oral emulsions need to have a wide mouth opening.
true
What two statements (labels) absolutely must be on an emulsion?
shake well before use
for oral use/for topical use
What do emulsions need to be protected from when they are packaged?
light
extreme temps of hot or cold
What feature does a container for an emulsion need that is different from other dosage forms?
extra head space so that it can be shaken well
what is the optimum ratio of oil to water or vice versa?
40% internal/60% external
By decreasing the size of globules in an emulsion, what are you doing?
enhancing stability
What can you do if you want to make an emulsion thicker?
add a substance that is soluble in or miscible with the external phase
o/w: add a hydrocolloid
w/o: add a wax, viscous oil, fatty alcohol or fatty acid
What is another term for coalescence?
cracking or braking
T/F: coalescence is an irreversible process.
true; very hard to get an emulsion back
What is it called when an o/w switches to a w/o or vice versa?
phase inversion
What is it called when the internal phase forms aggregates or globules upon standing. Aggregates may rise to the top or fall to the bottom of an emulsion.
creaming (aggregation)
T/F: in an emulsion, 'creaming' is an irreversible process.
false; can be reversed by shaking
What are 3 forms of instability in an emulsion?
coalescence
creaming
phase inversion
What is a microemulsion?
a biphasic o/w system
stabilized w/ surfactants w/ HLB values of 15-18
contains droplets of 100-5000 angstroms (very small)
T/F: a microemulsion is optically transparent.
true
T/F: vitamin oils like A, D and E are examples of microemulsions.
true
T/F: IVFEs are not microemulsions.
false; parenteral IVFEs are microemulsions
T/F: microemulsions can be used in patches.
true
What are some advantages of microemulsions?
more rapid and efficient oral absorption of drugs
increased diffusion of drug into the skin
can make artificial RBCs
can get cytotoxic drugs to cancer cells better
T/F: in transdermal drug delivery systems, the target is the skin.
false!
Where is the most delicate area of our skin?
behind the ear
and the testicles :)
What was the first TDDS system to be manufactured?
Transderm Scop (scopalomine)
What type of absorption are we achieving with a TDDS?
percutaneous absorption
What are some factors that influence percutaneous absorption?
physical/chemical properties of the drug
condition of the skin
vehicle used
surface area of the patch
time
T/F: patch systems are hard to test.
true; there are no animal models that have skin like we do
Where should you not apply a patch?
to compromised, irritated, or damaged skin
What is main barrier for a patch delivery system (specific)?
epidermis
What is another name for the stratum corneum?
horny layer
What is the outermost layer of the epidermis?
stratum corneum/horny layer
What are the 3 layers of the epidermis?
(from outer to inner)
stratum corneum
stratum lucidum (granulosum)
stratum germinativum
What are the 3 main layers of the skin that a drug must pass through?
epidermis
dermis
subcutaneous
Which layer of the skin do we start to see small, thin blood vessels?
dermis
T/F: blood vessels are the largest in the subcutaneous layer of the skin.
true
What 3 things can we find on the outer layer of our skin all the time, and might effect drug absorption?
sweat
sebum/oil
dead cells
In which layer of our skin do we find keratin?
stratum corneum
T/F: the stratum corneum lacks continuity and is not a significant factor in drug penetration.
true
T/F: We have 15-25 layer of cells in the stratum corneum over most of our bodies.
true
T/F: Drugs do not pass through the stratum corneum by passive diffusion.
false; they do
T/F: the stratum corneum acts like a semipermeable artificial membrane for drug penetration.
true
Which layer of our skin is the main rate limiting barrier to transdermal drug transport?
the stratum corneum
Which layer of our skin can be considered the 'living epithelium'?
stratum lucidum (granulosum)
Which layer of our skin can be considered the 'living epidermis'?
stratum germinativum
Which layer of our skin do we want to get the drug to and why?
dermis because it is highly vascularized
Which layer of our skin is a barrier layer with living cells at several differentiated levels?
stratum lucidum (granulosum)
Lipid-rich, non-polar drugs pass through our skin in what way?
transcellular (across)
Polar drugs pass through the skin in what way?
intercellular (between)
What is the major route of drug penetration in our skin?
intercellular passage
What is it called when drugs pass through hair follicles, sweat glands, and sebaceous glands with minor drug absorption?
trans-appendageal absorption
What is the only patch that is placed behind the ear (according to Glaucia)?
Transderm Scop
T/F: patches mimic a parenteral delivery.
true
How do patches mimic a parenteral delivery system?
they have a similar concentration vs. time curve
T/F: almost all patches have penetration enhancers in them.
true
What is the molecular weight range that is best for a patch system?
100-800 (400 is the best)
Why are more drugs not in a patch form?
because they don't have a molecular weight between 100-800
What is inunction?
rubbing the skin
T/F: inunction (rubbing) and exercise both increase vasodilation in the skin and may increase the amount of drug released by a patch.
true
What main factors affect absorption of a drug in patch form into the skin?
physical factors
drug chemical factors
skin factors
vehicle factors
What are some factors that are related to the vehicle when talking about factors affecting skin absorption of a TDDS?
adherence to skin
miscibility with sebum
action as a moisture barrier
What are some factors that are related to the skin when talking about affecting skin absorption of a TDDS?
intact vs. broken skin
surface area applied
site of application (thin horny layer)
What are some factors that are related to the drug when talking about affecting skin absorption of a TDDS?
concentration
particle size
molecular weight
solubility in water and oil
attraction to the skin
What are some physical factors that affect skin absorption of a TDDS?
rubbing
exercise
vasodilation
time of contact with the skin
multiple application
site of application
What are some chemical methods used to enhance percutaneous absorption of a TDDS?
use a carrier mechanism
modification of lipids in intercellular channels
modification of stratum corneum's hydration
reduction of stratum corneum's resistance
What are the 3 types of percutaneous CHEMICAL enhancers?
solvents
miscellaneous
amphiphiles
What are some examples of solvents (penetration enhancers for TDDS)?
water
alcohol (methanol, ethanol)
alkyl methyl sulfoxides (DMSO)
pyrrolidones
Laurocapram (Azone)
acetone
dimethyl acetamide
dimethyl formamide
What are some examples of amphiphiles (penetration enhancers for TDDS)? Hint: amphi= on both sides
high-frequency ultrasound facilitates drug penetration through the stratum corneum
a microchip embedded in the patch
Ex: salycylic acid for warts, lidocaine also, hydrocortisone
T/F: a patch is a rate-controlled system.
true
T/F: patches deliver a drug at a controlled rate to intact skin without buildup in the dermal layers.
true
T/F: patches release the drug promptly from the system into the s. corneum for penetration into the general circulation for systemic effects.
true
What is a therapeutic advantage of a patch that other dosage forms lack?
no drug is lost
they cause occlusion of the skin so there is only a 1-way flux of drug
Patches should cause no irritation or sensitization to the skin due to the _______, ______, or _________?
drug, vehicle, or adhesive used
Which dosage form is 'paradise for compliance' according to G?
patches
What are some advantages of a patch?
patient compliance
avoid GI difficulties
substitute for oral administration
avoid first pass effect
substitute painful parenteral administration
provide multi-day therapy with a single application
drug's effect can be terminated by removing the patch
fast ID during an emergency (no medical record needed)
convenient
What are some disadvantages of a patch?
unsuitable for irritating or sensitizing drugs or highly sensitive people
can cause contact dermatitis
only relatively potent drugs can be made in a patch
technical difficulties during prep of a patch
can contaminate others if not disposed of properly
What are some examples of patches that are monolithic/matrix systems?
estradiol (Climara, Alora, VivelleDot)
OrthoEvra
Lidoderm
What are some examples of patches that are membrane-controlled/reservoir systems?
Transderm-Scop
Nicotine (Habitrol)
Estraderm
Catapres TTS
Duragesic
T/F: Monolithic/Matrix system patches can be cut.
true
T/F: Membrane-controlled/reservoir system patches can be cut.
false!
What patch is used once a day for the prophylaxis of angina pectoris?
NitroDur, Minitran, Transderm-Nitro
What patch is used to treat hypertension?
Catapres-TTS
Which patch is used to treat urinary incontinence?
Oxytrol
Which patch is used to treat Alzheimer's?
Exelon
Which patch is used to treat Major Depressive Disorder?
Emsam
Which patch system allows the skin to control the rate of absorption of the drug?
monolithic/matrix system
Which patch system usually has excess amounts of drug?
monolithic/matrix system
Which patch system delivers uniform quantities of drug to the skin over a period of time?
membrane-controlled/reservoir
Which patch system contains drug (liquid or gel) that remains saturated and the release of the drug is constant?
membrane-controlled/reservoir
Which patch system allows the patch itself to control the rate of delivery of drug with a rate-controlling membrane?
membrane-controlled/reservoir
T/F: the adhesive layer (glue) of a membrane-controlled patch contains an initial priming dose.
true
Which patch system maintains a wide range of plasma concentration over which the drug is effective, but never toxic?
monolithic/matrix
Which patch system has the drug blended or dissolved in a polymer matrix?
monolithic/matrix
Which patch system is made of a release/film layer, an active drug plus adhesive layer, and a third layer of backing film?
monolithic/matrix
Define a suspension.
a 2 phase system of finely divided drug particles (suspensoid) mixed into a vehicle (dispersion medium)
What is the study of flow?
rheology
What are some advantages of a suspension?
chemically stable
easy to swallow
flexible administration
range of doses can be given
good bioavailability
can mask the bad taste of a drug
How can suspensions be administered (what are all the different ways)?
oral
topical
ophthalmic
rectal
nasal
otic/aural
parenteral (IM)
What are the ready to use commercial suspensions called?
"oral suspension"
What are the commercial suspensions that are in powder form and need to be reconstituted called?
"for oral suspension"
What are some features of suspensions?
therapeutic efficacy
chemical stability
esthetic appeal
resuspendability
thixotropy
T/F: thixotropy is desirable in a suspension for increasing physical stability.
true
T/F: the order of mixing the ingredients of a suspension is not important to its stability.
false; it is important
T/F: additives like flavoring, coloring, and preservatives should be added to the dispersed phase of a suspension.
false; to the dispersion medium
A ______ particle size equals slower sedimentation rate?
smaller
An _______in vicosity equals slower sedimentation rate?
increase
Why do we not want too much of an increase in viscosity of a suspension?
will make it too hard to pour
A ____ density particle equals a faster sedimentation rate?
higher
What is the most important consideration when referring to the dispersed phase of a suspension?
particle size
What are some ways to reduce the size of particles for a suspension?
comminution
dry milling
micropulverization
fluid energy grinding (jet milling, micronizing)
spray drying
What is the best range of particle size for a suspension?
1-50 micrometers
Which method of reducing particle size makes particles which are 10-50 micrometer and are used for oral and topical suspensions?
micropulverization
Which method of reducing particle size makes particles that are less than 10 micrometers and are used for ophthalmics and parenterals?
fluid energy grinding (jet milling)
Particle ______ affects caking?
shape
What shape of particles are more stable in a suspension?
symmetrical barrel shaped = more stable than asymmetrical needle shaped
_______ cake upon standing and cannot be redistributed in a suspension?
needles (needle shaped particles)
How can we avoid caking in a suspension?
using a flocculating agent
What is a floc or floccule?
a loose aggregate of particles held together by weak particle-particle bonds
less prone to caking
settle faster than fine particles
break up easily and can be redistributed readily with agitation
What are some common flocculating agents?
clays (bentonite magma)
electrolytes like KCl and NaCl
surfactants
change the pH of the dispersed phase
T/F: viscosity is inversely related to sedimentation in a suspension.
true
The ________ ______ supports the suspensoid in a suspension?
dispersion medium
_______/________ agents help to suspend the suspensoid and provide structure in a suspension?
thickening/suspending
What are some common suspending agents?
xantham gum
bentonite (also a flocculator)
polyvinyl pyrrolidone
microcrystalline cellulose
methylcellulose
carboxymethylcelllulose
How do you make a sustained release suspension?
the drug is complexed with ion exchange resins
this complex is then coated with ethyl cellulose
What is a Pennkinetic system?
when a drug is complexed with ion exchange resins
ex: Tussionex extended release suspension
T/F: you can make an extended release suspension by crushing an ER tablet and adding it to other ingredients.
true
When formulating a suspension for a newborn, what should not be included? (4 different things)
coloring
flavoring
preservatives (benzyl alcohol, propylene glycol)
alcohol (includes Aromatic Elixir, NF)
What can benzyl alcohol do to a neonate if it is used in a prep?
cause Gasping syndrome- multiple organ dysfunction and death
What can propylene glycol do to a neonate if it is used in a prep?
cause seizures or stupor
What can alcohol do to a neonate if it is used in a prep?
cause CNS depression
alter liver function
gastric irritation
What 3 things should be considered when packaging a suspension?
wide mouth container
air tight, light resistant container
adequate head space for thorough mixing
What 3 things should be considered when talking about storage of a suspension?
keep at room temp or refrigerated
protect from freezing
protect from excessive heat
When labeling a suspension, what should absolutely go on the labels?
shake well before use
how to store (room temp, fridge)
external or internal use
BUD
When telling your patient about the suspension, what 2 things do you need to make sure you mention?
give them the correct measuring tool, show them how to use it
tell them to watch for color/consistency changes in the suspension during use
_____ are semisolid systems consisting of dispersions of small inorganic particles or large organic molecules interpenetrated by a liquid?
Gels
______ are semirigid systems in which the movement of the dispersed medium is restricted by an interlacing 3-D network of particles or solvated macromolecules of the dispersed phase? (second definition by USP)
Gels
_____ are excellent drug delivery systems for oral, topical, nasal, vaginal, rectal use and are compatible with many different drugs?
Gels
T/F: gels are relatively easy to prepare and are very efficacious.
true
What are some examples of alcohol penetration enhancers?
methanol
ethanol
propanol
octanol
What are some examples of fatty acid penetration enhancers?
stearic acid
myristic acid
oleic acid
What are some examples of fatty alcohols for penetration enhancers?
cetyl alcohol
stearyl alcohol
myristyl alcohol
What are some examples of some fatty acid esters for penetration enhancers?
isopropyl myristate
isopropyl palmitate
What is an anionic surfactant that is used for a penetration enhancer?
SDS
What are some polyols that are used as penetration enhancers?
propylene glycol
glycerol
polyethylene glycol
What are some cationic surfactants used for penetration enhancers?
benzalkonium chloride
cetylpyridinium chloride
What is an amphoteric surfactant used as a penetration enhancer?
lecithins
What are some nonionic surfactants used as penetration enhancers?
Spans
Tweens
What is imbibition (gels)?
taking up of a liquid with no increase in volume
T/F: some gels may be clear as water, while others might be turbid.
true
T/F: most gels are water-washable, water-solublem, water-absorbing and greaseless, but some have continuous phase alcohol or oleaginous.
true
What are some common preservatives used in gels?
benzalkonium chloride (also a cationic sufactant/penetration enhancer)
sodium benzoate
methylparaben
propylparaben
What is the normal concentration of gelling agent in a prep?
0.5-2%
What is a single-phase gel system?
a gel that contains linear or branched polymer macromolecules that dissolve in water and have no apparent boundary with the dispersing medium
What is a two-phase gel system?
a gel that contains small, discrete particles
these gels are thixotropic
if the particles are larger, it is called a magma
What is a magma or milk?
a two-phase system with large particles or floccules of small, distinct particles
ex: Bentonite Magma, NF
what are some gelling agents?
acacia
pectin
starch
tragacanth
xantham gum
alginic acid (seaweed)
gelatin
animal/vegetable fat: lard, cocoa butter
bentonite
veegum
CMC
carbomer resins
PEG ointment
PVA
petrolatum, mineral oil, plastibase
What is a neutralizer (for gels)?
it thickens the gel after the gelling agent is dispersed