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Exam 3
pharmaceutics
179
Other
Professional
11/10/2008

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Term
what are suppositories
Definition
suppositories are solid dosage forms intended for insretion into body orifices
Term
what are the different sites of insertion for suppositories
Definition
vagina, rectum, and urethra (vagina and rectum are the most common)
Term
Why use suppositories?
Definition
- has similar advantages as TDDS (skips hepatic first pass metabolism)
- good dosage forms for treating pts. with vomiting
- more drugs can be made into suppositories than can be made into TDDS
- suppositories have a faster rate of onset than TDDS
- local effects
Term
shapes of rectal suppositories
Definition
- usually tapered at one or both ends
- inserted with fingers
Term
adult rectal suppositories
Definition
- about 2 grams
- cocoa butter or theobroma oil (bases - synonyms of eachother)
Term
child rectal suppositories
Definition
- cocoa butter or theobroma oil (bases - synonyms of eachother)
- half the weight of adult suppositories
Term
shapes, weight, and content of vaginal suppositories
Definition
- globular or oviform
- 5 grams
- cocoa butter is the base
- "pessaries"
Term
most common urethral suppository
Definition
- medicated urethral system for erection (MUSE)
Term
another term used to describe urethral suppositories
Definition
- "bougies"
Term
physiologic factors affecting drug absorption from rectal suppositories
Definition
- colonic content
- pH and lack of buffering capacity of the rectal fluids
Term
physicochemical factors of the drug and suppository base
Definition
- lipid-water solubility
- particle size
- nature of the base
Term
when systemic effects are desired, can greater absorption be aquired when the rectum is empty or distended with fecal matter?
Definition
- empty rectum because drug has greater opportunity to make contact with absorbing surfaces
Term
evacuant enema
Definition
- empties rectum so that suppository can be administered
Term
buffer capacity
Definition
- ability of drug buffer to resist change in pH
Term
relationship between rectal fluids and buffer capacity
Definition
- rectal fluids have no buffer capacity therefore rectal fluids do not react with weak acid or weak base of drug
- without using another form for the suppository (i.e. ionic) the suppository is immiscible with body gluid and fails to release fat soluble drug readily into the rectum
Term
how do you incorporate fat soluble drugs in cocoa butter
Definition
- use ionic form therefore it is more soluble in aqueous solution and increases bioavailability
Term
between hydrophilic and lipophilic forms of the drug, which two has more tendency to escape out of the fatty suppository base?
Definition
- hydrophilic
Term
between hydrophilic and lipophilic forms of a drug, which of the two has more tendency to escape out of the fatty suppository base?
Definition
- both
- lipophilic escapes out readily because it has no affinity for water
- hydrophilic escapes out because the base dissolves in aqueous fluids
Term
relationship bt particle size and suppositories
Definition
- the smaller the particle size, the more readily the dissolution of the particle and the greater the chance for rapid absorption
Term
essential features of the base for suppositories
Definition
- must be capable of melting, softening, or dissolving in order to release drug for absorption
- should not interact with the drug to inhibit its release
- should not irritate the mucous membrane
Term
3 categories of suppositories
Definition
- fatty or oleaginous bases
- water-soluble or water-miscible bases
- miscellaneous bases
Term
fatty or oleaginous bases
Definition
- most frequently employed suppository base (cocoa butter)
Term
under what conditions should cocoa butter be prepared for suppository bases
Definition
- melts bt 30-36 degrees (just below body temp)
- should not be hastily or carelessly melted
Term
What happens if you overheat cocoa butter for a suppository base?
Definition
- the suppository formed will melt below 30 degrees
- cocoa butter exists in two forms (alpha and beta)
- want the beta form which has a melting point bt 30-35 degrees (ideal)
- melting point for alpha form is below 30 degrees therefore it will not solidify at room temperature
- alpha can convert back to beta form but it takes several days
Term
2 main members of water-soluble and water-miscible bases
Definition
- glycerinated gelatin
- PEG's
Term
glycerinated gelatin as a water-soluble base
Definition
- slower to soften and mix with the fluids and therefore provides a slower release
- tendency to absorb moisture as a result of hygroscopic nature of glycerin
Term
what must you do to the suppository when it has a glycerinated gelatin base before insertion?
Definition
- moisten with water prior to instertion
- moistening prevents dehydrating effect and irritation of tissues
Term
PEG's as a water-soluble base for suppositories
Definition
- polymers of ethylene oxide and water (HO-(CH2-CH2-O-)n-H)
- 300, 400, 600, 1000, 1450, 3350, 4600, 6000, 8000
- do not melt at body temp. but dissolve slowly in the body fluids
Term
what base is the most convenient in terms of storage and handling of suppositories?
Definition
- PEG's because it does not melt at body temp. and you do not need to refridgerate
Term
3 methods of preparing suppositories
Definition
- molding from a melt ("fusion method")
- compression
- hand rolling and shaping
Term
steps taken when molding from a melt for preparation of a suppository
Definition
- melting the base
- incorporating any req. medicaments
- pouring the melt into molds
- allowing melt to cool an congeal into suppositories
- removing the formed suppositories from the mold
Term
types of molds used when molding from a melt for preparing suppositories
Definition
- stainless steel
- aluminum
- brass
- plastic
- rubber molds
Term
is lubrication of a mold required when molding from a melt in preparing a suppository?
Definition
- depends on the formulation of suppository used
- cocoa butter or PEG (seldom necessary because suppositories contract significantly when cooling and they separate from inert surfaces)
- glycerinated gelatin (necessary; ex. mineral oil which is also used as a levigating agent)
Term
role of the physician in compounding of suppositories
Definition
- prescribes the dose for the pt.
Term
role of the pharmacists in compounding of suppositories
Definition
- determines the amt. of the base
- preparation of the suppository
Term
2 things required when molding from a melt in preparing a suppository
Definition
- density calculations
- mold calibrations
Term
density calculations
Definition
- different bases will have different densities
- DO PRACTICE PROBLEMS
Term
calculation for density factor
Definition
- density factor = wt. of drug/wt. of base displaced
Term
steps taken when doing a mold calibration
Definition
- determine the vol. of each cell in the mold by pouring the base into each cell and let it solidify; remove the bases from each cell and determine the total wt.; transfer all the solidified bases into a beaker; melt to get the vol.; calculate the wt. and vol. of each cell
Term
what are solutions
Definition
- liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents
- mixture of one substance dissolved in another
Term
classifications of solutions - based on use
Definition
- oral
- otic
- opthalmic
- topical
Term
classification of solutions - based on composition
Definition
- syrups
- elixirs
- spirits/aromatic water
- tinctures/fluid extracts
- injections
Term
syrups
Definition
- aqueous solutions containing a sugar
- can be vehicles without drug or liquid dosage forms with the drug
Term
elixirs
Definition
- sweetened hydroalcoholic solutions
- no aromatic materials
Term
spirits/aromatic water
Definition
- solutions of aromatic materials
- spirits have a OH solvent
- aromatic water has a aqueous solvent
Term
tinctures/fluid extracts
Definition
- solutions prepared by extracting active constiuents from crude drugs
- tinctures are when w:v is either 1:4, 1:5, or 1:10
- fluid extracts are when the w:v is 1:1 only
Term
injections
Definition
- solutions prepared to be sterile and pyrogen free and intended for parenteral administration
Term
how can you define high solubility
Definition
- highest dose strength (of drug substance) is soluble in 250mL or less of aqueous media over the pH range of 1-7.5
Term
how can you define high permeability
Definition
- when the extent of absorption in humans is 90% or more
Term
what is solubility
Definition
- max equilibrium amt. of solute that can dissolve per amt. of solvent
Term
what is dissolution
Definition
- kinetic phenomenon
- amt. of solute dissolved per unit time
Term
6 techniques to improve the solubility or the dissolution rate
Definition
- slat form
- particle size
- amorphous form
- temperature (increased temp. = increased solubility in liquid dosage forms)
- rigorous agitation in liquid dosage forms
- pH
Term
5 types of solvents used for liquid preparations
Definition
- alcohol, USP
- diluted OH
- rubbing OH
- isopropyl rubbing OH
- purified water, USP
Term
OH, USP
Definition
- most useful solvent next to water
- forms hydroalcoholic mixture with water
- 94.9%-96% C2H5OH by vol.
- ethyl OH, ethanol
Term
dehydrated OH, USP
Definition
- contains not less that 99,5% C2H5OH by vol.
Term
Recommended OH content for OTC oral products
Definition
- <6yrs. = 0.5% or less
- 6-12yrs. = 5% or less
- >12 yrs. = 10% or less
Term
diluted OH
Definition
- equal volumes of OH, USP and purified water, USP
- final volume is less than initial because OH contracts upon mixing
Term
Rubbing OH
Definition
- 70% C2H5OH
- rubefacient
- disinfectant
- denaturant employed is formula 23-H
- separation of ethyl OH becomes virtually impossible when it is added
- by adding denaturant you are discouraging use of rubbing OH as beverage
Term
Isopropyl rubbing OH
Definition
- 70% IPA by vol.
- rubefacient
- disinfectant
Term
rubefacient
Definition
- any agent that increases the redness of skin
Term
purified water, USP
Definition
- obtained by distillation, ion exchange tx, reverse osmosis, etc
- should not yield more than 0.001% of residue
- for aqueous dosage forms
- not for parenteral administrations (including injections)
Term
dry mixtures for solution
Definition
- some medicinal agents will have insufficient stability in aq. sol'n to meet extended shelf life periods "antibiotics"
- commercial manufacturers provide these products to the manufacturer in dry form "drugs to be reconstituted"
Term
what are syrups
Definition
- concentrated aq. preparations of a sugar or sugar substitute with or without flavoring agents and medicinal substances
Term
two types of syrups
Definition
- medicated syrups
- non-medicated syrups (flavored vehicles)
Term
components of syrups
Definition
- purified water
- medicinal agents
- sugar (usually sucrose or sugar substitute)
- antimicrobial preservatives
- flavorants
- colorants
- may contain some other excipients
Term
glycogenetic substances
Definition
- sugars that are converted to glucose in the body
Term
sugar substitutes
Definition
- nonglycongenetic substances (ideal for diabetic pt.)
- ex: methyl cellulose or hydroxy ethylcellulose
Term
advantages of syrups
Definition
- physical concealment of the taste of the drug
- inherent stability
- make them viscous by adding 60-80% of sugar
Term
inherent stability
Definition
- resistant to microbial growth b/c of the unavailability of the water req.
Term
what are elixirs
Definition
- sweetened hydroalcoholic sol'n intended for oral use
Term
two types of elixirs
Definition
- nonmedicated elixirs (vehicles)
- medicated
Term
advantages of elixirs
Definition
- have less sugar than syrups
- less viscous than syrups but not more susceptible to microbial
- elixirs are less effective in masking the taste
- elixirs are capable of dissolving both water-soluble and water-insoluble
- elixirs cannot be used in kids and adults who choose to avoid OH
Term
2 principle methods of drug extraction
Definition
- maceration
- percolation
Term
what is maceration
Definition
- comminuted drug is allowed to soak in a solvent until the cellular structure is softene and penetrated by the solvent
- i.e. tea bag in a cup of water - immobile
Term
menstruum
Definition
- solvent
Term
percolation
Definition
- mobile (i.e. coffee maker)
- drug extraction by slow passage of a suitable solvent through a column of the drug
Term
extraction apparatus
Definition
- percolator
Term
percolate
Definition
- collected extractive
Term
what are dispersed systems
Definition
- drug is undissolved or immiscible
- "dispersion"
Term
dispersed phase
Definition
- drug dispersed
- solute in liquid dosage
Term
dispersing phase
Definition
- solvent
- dispersion medium
- continuous phase
Term
colloidal dispersion
Definition
size range is 1-500nm
Term
coarse dispersions
Definition
- size is greater than 500 nm
Term
4 types of dispersions
Definition
- suspensions
- emulsions
- gels and magmas
- aerosols
Term
suspensions (dispersions)
Definition
- coarse dispersions containing finely divided insoluble material suspended in a liquid medium (particle size usually > 0.5 micrometers)
Term
emulsions (dispersions)
Definition
- liquid drug dispersed in liquid
- system consisting of at least two immiscible liquid phases
- study slide
Term
gels and magmas (dispersions)
Definition
- very fine particles dispersed in liquid but liquids are made semisolid
Term
aerosols (dispersions)
Definition
- solid or liquid drug is dispersed in gaseous medium
Term
oral suspension
Definition
ready to use form
Term
for oral suspension
Definition
- powder form and drug must be reconstituted using a suitable solvent
Term
why do we need suspensions
Definition
- some drugs are unstable in sol'n but stable when formulated as suspension
- suspensions are better at masking taste
- ease of swallowing
- flexibility of administration of a range of doses
Term
stokes equation
Definition
- dx/dt=d2(pi-pe)g/18n
- study slides
Term
how do you prevent formation of cake
Definition
- intentional formation of a less rigid or loos aggregation of partiles
- "floc"
- "floccule"
Term
flocculation
Definition
- process of intentional formation of a less rigid or loose aggregation of the particles
- dispersed particles come together but do not fuse
Term
flocculating agents
Definition
- agents used to prepare flocculated suspensions
Term
examples of flocculating agents
Definition
- clays such as diluted betonite magma
Term
problems with highly flocculated suspensions
Definition
- rapid settling
- unsightly a supernatant layer
- both of the above occur if large amt. of flocculating agents added
Term
how cam problems that occur due to highly flocculated suspensions be overcome
Definition
- adding suspending agents to the disperions medium
- high viscosity of dispersion medium ("vehicle")
- ex: acacia, methyl cellulose, carboxymethylcellulose
Term
what is extemporaneous compounding
Definition
- used in kids/adult who cannot swallow solid dosage forms
Term
why should you not use preservatives, colorings flavorings, or OH in extemporaneous compounding
Definition
- because they may have acute or long-term side effects for neonates (newborn <4wks old)
Term
why should you use extreme caution with benzyl OH for neonates in extemporaneous compounding
Definition
- because liver does not metabolize benzyl OH and benzyl OH causes gasping syndrome (condition which leads to multiple organ failure)
Term
two common emulsions
Definition
- oil in water emulsions (o/w)
- water in oil emulsions (w/o)
Term
emulsifying agent
Definition
- added to prepare a stable emulsion
- ex: acacia, tragacanth, and gelatin
Term
3 most prevalent theories of emulsification
Definition
- surface tension theory (emulsifiying agents act to decrease interfacial tension)
- oriented-wedge theory
- plastic or interfacial film theory
Term
interfacial tension
Definition
- forces bt molecules of same liquid that prevent breaking down into small substances
Term
HLB
Definition
- hydrophilic-lipophilic balance
- emulsifying agents can be categorized by HLB
- ranges from 1-40
- high HLB # = o/w
- low HLB # = w/o
Term
tree methods used for small-scale extemporaneous preparation of emulsions
Definition
- continental or dry gum method
- english or wet gum method
- bottle or Forbes bottle method
Term
4:2:1 method
Definition
- oil:water:gum
- for every 4 parts oil added, 2 parts water are added and one part gym added
- used in the preparation of initial or primary emulsion
Term
steps for dry gum emulsion preparation
Definition
- gum is triturated with oil until thoroughly mixed
- two parts of water are added all at once
- end point - creamy white and crackling sound
- STUDY SLIDE
Term
wet gum (english) method for preparation
Definition
- smae proportions of oil, water, and gum except order of mixing is different (water added before oil)
- mucliage prepared by triturating gum with ater
- oil is added slowly in portions
Term
coalescence
Definition
- dispersed particles come together, fusion of particles take place and leads to the decrease in number of particles
Term
creaming
Definition
- upward movement of the dispersed droplets relative to the continuous phase
Term
sedimentation
Definition
- downward movement of the dispersed droplets relative to the continuous phase
Term
breaking
Definition
- complete separation of the internal phase from the continuous phase and formation of internal phase as a separate layer
Term
inversion
Definition
- an emulsion is said to be invert when it changes from an o/w to a w/o emulsion or vice versa
Term
gels
Definition
- semisolid systems consisting of either suspensions made up of small inorganic particles or large organic molecules interpenetrated by a liquid
Term
example of gelling agent
Definition
- carbomer
Term
two phase system
Definition
- "magma"
- the gel contains small discrete particles
Term
one phase system
Definition
- gel does not appear to have discrete particles
Term
thixotropy
Definition
- "reversible gel-sol phenonmenon"
- some gels become fluid on agitation, only to resume their solid or semisolid state after remaining undisturbed for a period of time
Term
inhibition
Definition
- taking up of certain amt. of liquid without a measurable increase in vol.
Term
swelling
Definition
- taking up of liquid by a gel with an increase in vol.
Term
syneresis
Definition
- when a gel stands for some time, it may shrink naturally and some of the liquid is pressed out
Term
xerogel
Definition
- formed when the liquid is removed from a gel and only frame work remains
Term
rheology
Definition
- study of flow
- addresses the viscosity and flow properties of powders, fluids, and semisolids
Term
2 categories of rheology
Definition
- newtonian flow
- non-newtonian flow
Term
newtonian flow
Definition
- characterized by constant viscosity, regardless of shear rates applied
- STUDY SLIDES
Term
non-newtonian flow
Definition
- fail to follow newton's eq.
- plastics
- pseudoplastic
- dilatant
Term
plastics
Definition
- higher viscosity than newtonian fluid
- substances that exhibit plastic flow are called bingham bodies
- plastic flow does not begin until a shearing stress corresponding to a certain yield value is exceeded
- STUDY SLIDES
Term
pseudoplastic flow
Definition
- begins when a shearing stress is applied
- STUDY SLIDE
Term
dilatant flow
Definition
- exhibit an increase in resistance to flow with increasing rates of shear
- STUDY SLIDE
Term
pharmaceutical aerosols
Definition
- pressurized dosage forms that upon actuation emit therapeutic ingredients as a fine dispersion of a liquid or solid material in a gaseous medium
Term
advantages of aerosols
Definition
- rapid onset of action
- avoid hepatic first pass metabolism
- most of contents used are hemetic (airtight) therefore are protected from degredation by oxygen or humidity
Term
steps in filling aerosols
Definition
- determine what aerosol container will be made of
- add product (drug and other excipients)
- fit valve
- add propellant
- fit actuator
Term
what are parentals
Definition
- dosage form that enters body other than GIT
- injections
- sterile (free from microorganisms)
Term
injections
Definition
- most common parental
- sterile
- pyrogen-free
- preaparations intended to be admin. parenterally
Term
pyrogens
Definition
- substances that induce fever
Term
advantages of parentals
Definition
- rapid onset of action bc drug injected directloy into the blood
- for pts. who are uncooperative or unconscious
- when drugs are ineffective by other routes
Term
disadvantages of parentals
Definition
- drugs cannot be retrieved
- req. trained personnel in most cases
Term
routes of parenteral administration
Definition
- intra-articular (joints)
- intrasynovial (joint-fluid area)
- intraspinal (spinal column)
- intrathecal (spinal fluid)
- intra-arterial (arteries)
- intracardiac (heart)
Term
hypodermic needles
Definition
- stainless-steel or AL devicesthat penetrate the skin for the purpose of admin. a parenteral product
Term
parts of hypodermic needles
Definition
- bevel (needle tips - slanting edge)
- shaft or barrel (long portion of needle)
- hub (connects to syringe)
- needle gauge (gauge number on hub)
Term
needle gauge
Definition
- outside diameter of the needle shaft
- larger the number = smaller diameter
Term
needle lengths
Definition
- range from 1/4 to 6 inches
- choice of needle length depends on the desired penetration
Term
two types of hypodermic needle physical hazards
Definition
- phlebitis
- thrombosis
Term
phlebitis
Definition
- minor complication resulting from a vein injury or irritation
Term
thrombosis
Definition
- formation of a blood clot in a vein or artery
Term
intravenous route of admin for parentals
Definition
- provides rapid action compared with other routes of admin b/c injected directly into blood and solubility, dissolution, and absorption are not factors
Term
intarmuscular route
Definition
- less rapid bc drug has to absorbed into the blood from the muscle
- longer lasting
Term
injection
Definition
- liquid preparations that are substances or sol'n directly injected into the human body
Term
for injection
Definition
- dry solids that depend on the add'n of suitable vehicles
Term
injectible emulsion
Definition
- must be dissovled in emulsion mediums
Term
injectible suspension
Definition
- liquid preparation of solid suspended in a suitable liquid medium
Term
for injectable suspension
Definition
- dry powders, solids, etc. that upon add'n of suitable vehicle yields preparatio conforming in all respects to injectible suspensions
Term
oleaginous and suspensions relationship to injections
Definition
- types of injections that are restricted to types other than intravenous bc interrupts normal blood flow
Term
formulation of parentals for a drug unstable in sol'n
Definition
- prepare dry product
- formulate as suspension
Term
formulation of parenterals if drug is unstable in water
Definition
- use non-aq. solvent (i.e. vegetable oils)
Term
formulation of parenterals if an aq. sol'n is desired
Definition
- use water-soluble solid form
Term
solvents and vehicles for injections
Definition
- water for injections, USP
- sterile water for injection, USP
- bacteriostatic water for injection, USP
- sodium chloride injection, USP
- bacteriostatic sodium chloride injection, USP
- nonaq. vehicles
Term
water for injection
Definition
- purified by distillation or by reverse osmosis
- presence of total solids - NMT 1mg/100mL
- not req. to be sterile , it must be pyrogen free bc used for a large scale manufacture of injections
Term
sterile water for injection, USP
Definition
- designated solely for parenteral use only after add'n of drugs that req dilution or must be dissolved in an aq vehicle prior to injection
- packaged in single-dose containers not larger than 1L
- no antimicrobial agent
Term
bacterostatic water for injection, USP
Definition
- sterile water for injection containing one or more antimicrobial agents
- flexibility for multiple dose vials
- packaged in prefilled syringes or in vials containing NMT 30mL
- used in parenterals that are admin in small vol. b/c do not want to admin. large amt. of antimicrobial agents into blood
- USP labeling req. = NOT FOR USE IN NEONATES
- limited detoxification capacity of the neonate liver for benzyl OH
- benzyl Oh poisoning - gasping syndrom (multiple organ failure)
Term
which solvents and/or vehicles for injections are isotonic with blood
Definition
- sodium chloride injections
- bacteriostatic sodium chloride injections
Term
nonaq vehicles
Definition
- used when drug has limited aq. solubility or when drugs are subject to hyrolysis
- fixed vegetable oils, glycerin, PEGs, propylene glycol
- oleaginous injections are mostly admin intramuscularly bc interrupt blood flow
Term
methods of sterilization
Definition
- destruction of all living organisms and their spores or their complete removal from the prepation
- dry heat
- steam
- filtration
- gas
- ionizing radiation
Term
dry heat sterilization
Definition
- usually carried out in oven
- b/t 150-170 degrees C
Term
if chemical X melts or decomposes at 170degrees C but is un affected at 140 degrees C, what steps should be taken?
Definition
- decrease temp, but increase exposure time
Term
what is one of the important factors responsible for dug degradation
Definition
- heat
Term
dont you tink 150 or 170 is too high for certain pharmaceutical prodcuts
Definition
- yes - therefore use steam because microorganisms are destroyed at much lower T
Term
what is the highest T steam can acieve
Definition
100 (bc water)
Term
what if you need a T of 110 to destroy microorganism
Definition
- use pressure
Term
methods of steam sterilization
Definition
- autoclave
- employs steam under pressure in order to increase T
- it sis the T, not the P, that destroys the microorganism
Term
sterilization by filtration
Definition
- physical removal of microorganism by adsorption on the filter medium
- used for heat sensitive sol'ns
- milipor filters (most commonly used for filtrations)
Term
gas sterilization
Definition
- exposure to ethylene oxide or propylene oxide gas
Term
sterilization by ionizing radiation
Definition
- sterilization by gamma rays and by cathode rays
Term
three types of properties of drug molecules
Definition
- additive
- constitutive
- colligative
Term
additive
Definition
- properties that depend on the total contribution of atoms in the molecule or on the sum of properties of the constituents in soln'
Term
constitutive
Definition
- properties that depend on the arrangement of atoms in a molecule
Term
colligative properties
Definition
- properties that depend primarily on the number of particles in sol'n
- lowering of v.p
- increase in bp
- decrease in freezing point
- osmotic pressure
- STUDY SLIDES
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