Tablets Part 3 Flashcards
name 2 methods for All-In-One Granulation
fluid bed process
microwave vacuum processing
the fluid bed process uses what equipment to perform all in one granulation?
the fluid bed granulator
explain the 3 steps of the fluid bed granulator in performing all in one granulation
- the formulation powder (drug+fillers+disintegrants) is preblended in a bed with fluidized air
- the mixture is granulated by spraying (onto the fluidized powder bed) a liquid binder. (ie: aqueous solution of acacia, HPC, or povidone
- The granulated product is dried to the desired moitsure content
name 2 advantages of the dry granulation method
useful for water and heat sensitive drugs (both used in wet granulation)
fewer steps than wet granulation
name a disadvantage of dry granulation
requires drugs or excipients that have cohesive properties (bc no liquid binder)
name 2 methods of dry granulation
slugging
roller compaction
in order to do the direct compression method of preparing compressed tablets, what must the properties of the drug be?
the drug must be free flowing and sufficiently cohesive
what is the LEAST EXPENSIVE method of preparing compressed tablets?
the direct compression method
name 2 binders that can be used in the direct compression method
starch
CMC
name 3 disadvantages of the direct compression method
-requires materials that can be directly compressed
-the drug /excipients must have good flow properties
-you can get non uniform tablets
true or false
an advantage of the direct compression method is that it is possible to prepare a tablets from a powdered mixture WITHOUT granulation
true
true or false
a disadvantage of the direct compression method is that it is slower than the other 2 methods
FALSE - it is faster
direct compression method is useful for drugs with what properties?
name 4
drugs that are moisture sensitive
drugs that are heat sensitive
large dose drugs
crystalline drugs
which normally has better bioavailability - tablets prepared by wet granulation, dry granulation, or the direct compression method?
direct compression method has optimal bioavailability bc there is a limited # of excipients (remember - useful for large dose drugs = less excipients used)
what is commonly used as a filler/diluent in the direct compression method?
in which other method is it commonly used?
ditab
also used in dry granulation
what is tablet dedusting?
removes traces of loose powder that adhere to the tablets following compression
what step immediately precedes dedusting?
what happens after dedusting?
tableting machine and then right to dedusting
after dedusting is when the compressed tablets may be coated if desired
true or false
dedusting happens immediately after tablet coating
false – happens right before coating
what are the types of tableting machines?
single punch
rotary punch
where in the tableting machines is the granulation fed into?
the die cavity
where in the tableting machine is the formed tablet ejected from?
the die
what is capping?
a tablet defect.
the partial or complete separation of the top or bottom from the main body of the tablet
what is lamination?
a tablet defect
the horizontal separation of the tablet into 2 or more distinct layers
capping and ______ have the same causes and remedies
lamination
true or false
friability is related to capping and lamination
false - not related
what is the optimum moisture for granules?
what happens if the granules are too dry?
optimum moisture is 4-6%
if too dry, capping/lamination can occur
true or false
lack of fines can result in capping/lamination of tablets
false - excess fines
entrapped air can be a cause of tablet capping and lamination
what is a solution to this?
decrease the compression speed
define picking
the removal of material from the surface of the tablet and its adherence to the punch face
define sticking
the adherence of material to the die wall
true or false
sticking is the removal of material from the surface of the tablet and its adherence to the punch face
FALSE - THIS IS PICKING
sticking is the adherence of the material to the die wall
true or false
picking and sticking have the same causes and remedies
true
name 2 causes of picking and sticking
excessive moisture in the granules
not enough lubricant
true or false
picking and sticking can be caused from granules that are too dry
false – granules that are too moist
too dry granules can cause capping and lamination
name 5 remedies to picking and sticking
clean and polish the tools
add silica gel or talc
use chromium plated punches
decrease the relative humidity in the compression area
use large lettering on the tools
define mottling
a tablet defect
unequal or uneven distribution of COLOR on the surface of the tablet
true or false
adding sugar coating could be a solution to mottling
true
name 5 causes of mottling of tablets
uneven mixing
dye migration during drying
color variation
dye precipitation
dye degrades while it’s drying
name 4 remedies for hardness variation
change granule density and porosity
change particle size and size distribution of granules
change compression pressure
change the nature of drug and excipients
true or false
to fix poor compression and soft tablets, smaller granules should be used
FALSE - larger granules
true or false
to fix poor compression and soft tablets, use less lubricant
true
use 0.25-0.5%
true or false
to fix poor compression and soft tablets, use more fines
false - fewer fines
true or false
to fix poor compression, soft tablets, lower the bulk density
true
true or false
to fix poor compression, soft tablets, decrease the granule porosity
false - increase
can changing the compression press fix poor compression, soft tablets?
yes - use precompression
give 4 reasons for tablet coating (general)
enhance product acceptance and appearance
maintain physical or chemical drug integrity
control the site of drug release
provide controlled, continuous release, or reduce the frequency of dosing
name 6 steps of sugar coating tablets
waterproofing and sealing
subcoating
smoothing and final rounding
finishing and coloring
imprinting
polishding
in subcoating, the 2nd step of sugar coating tablets, what is added on?
syrup – this is where the weight comes on
what are sugar coated tablets polished with
wax
name 3 advantages of sugar coated tablets
high glossy appearance
elegant
attrative
name 7 disadvantages of sugar coated tablets
children – candy (sugar)
hard to do - requires skill
takes 3-5 days per batch
high cost for space and equipment
microbial growth and contamination
hygroscopic
increases the tablet weight up to 50%
which need to be sealed and why - sugar coating, film coating, or both?
sugar coating needs to be sealed bc it’s water soluble
film does not - advantage
true or false
film coating and sugar coating are susceptible to microbial contamination
false - film coating is not
what weight does film coating add to the tablet?
only 10-20 micrograms - this is a major advantage
explain how the coat used in film coating is an advantage over sugar coating
it is noncaloric (sugar isnt’s) and it’s flexible
true or false
applying film coating is not as complex as sugar coating
true
true or false
applying film coating is not easily automated
false - it is
name 2 disadvantages of film coated tablets
cannot hide the tablet appearance (like chipping) that sugar coating CAN hide
the use of solvents needed bc polymers may be water soluble, effect on worker safety and the environment
in a nonaqueous film coating solution, name the 4 ingredients that are generally REQUIRED
a film former
an alloying substance
a plasticizer
a surfactant
in a nonaqueous film coating solution, name 4 ingredients that are generally OPTIONAL
opaquants and colorants
sweetners/flavors/aromas
a glossant
a volatile solvent
define what a film former is
is it required in film coating solutions?
yes it’s required
a film former is capable of producing a smooth, thin film that is reproducible and applicable to a VARIETY of tablet shapes
give an example of a film former
cellulose acetate phthalate
(CAP)
true or false
CAP is pH sensitive
TRUE
it’s very popular for enteric coating - won’t dissolve in the stomach
what is an alloying substance?
it provides water solubility or permeability to the film coating to ensure that it will be penetrated by the body fluids and be therapeutically available
true or false
an alloying substance is not required for film coating solutions
false - it is
give a common example of an alloying substance used in film coating solutions
polyethylene glycol
what is a glossant?
is it required?
function is to provide luster ti the tablets without requiring a whole separate polishing operation
NOT required for film coating solutions - it depends on the need
give an example of a popular glossant
beeswax
what is the function of a plasticizer?
give an example.
is it requird for film coating solutions
yes, it’s required
a plasticizer provides durability by producing flexability and elasticity of the coating
ex: castor oil
what is the function of a surfactant in film coating solutions?
is it required?
give an example of a popular one
a surfactant enhances the spreadability of the film when it is being applied to the tablet
YES required
ex: polyoxyethylene sorbitan derivatives (TWEEN)
what is the function of a volatile solvent in film coating solutions?
is it required?
give an example
function is to allow the spread of other components over the tablets while allowing rapid evaporation. this gives an effective yet speedy operation
not required - depends on the need
ex: alcohol mixed with acetone
what is the function of opaquants/colorants in film coating solutions?
is it required?
give examples
not required - optional
to make the appearance of the coated tablets handsome and distinctive
opaquant: titanium dioxide
colorant: FD&C or D&C dyes
what is the function of sweeteners/flavors/aromas in film coating solutions?
is it required?
give examples
to enhance acceptability of the tab by the pt
not required - optional
sweeteners: saccharin
flavors/aromas: vanillin
true or false
vanillin is an example of a sweetner in film coating solutions
FALSE – it is flavor/aroma
ex of sweetner would be saccharin
normally, how many reagants are used in NONAQUEOUS film coating solutions and how many are actually required?
4 are actually required but 7 are normally used out of 8 possible
give the ingredients in a typical aqueous film coating formulation
film forming polymer
plasticizer
colorant and opacifier
vehicle (water)
give 4 examples of film forming polymers commonly used in a typical aqueous film coating formulation
CAP
cellulose ether polymers like:
HPMC
HPC
MC
in an aqueous film coating formulation, what % of plasticizer is used?
give 5 examples of plasticizers that are commonly used
0.5-2% (very small amt)
glycerin
propylene glycol
polyethylene glycol
diethyl phthalate
dibutyl subacetate
what % of colorant and opacifier is typically used in an aqueous film coating solution?
give exampkes of what is typcially used
2.5%-8%
FD&C or D&C lakes
iron oxide pigments
TRUE OR FALSE
phthalates are not pH sensitive
FALSE - they are
that’s why CAP is used in enteric coating, and all phthalate groups in general
what is the function of enteric coating?
to pass through the stomach intact and disintegrate and release the drug content for absorption in the INTESTINES
some enteric coatings are designed to dissolve at what pH?
4.8 or greater
the design of the enteric coating may be based onw hat 2 things?
-the transit time required for passage to the intestines - change coating thickness based on this
-based on factors of pH - resist dissolution in highly acidic environment of the stomach
how can enteric coating be applied?
either to whole compressed tablets OR to drug particles or granules that are used in the making of tablets or capsules
applied in MULTIPLE PORTIONS to build either a thick coating or a thin film coat
true or false
the coating system of enteric coating can only be aqueous based
FALSE - can be aqueous or organic solvent based, as long as the coating material RESISTS BREAKDOWN IN GASTRIC FLUID
name 5 enteric coating agents
pharmaceutical shellac
HPMC phthalate
PVA phthalate
diethyl phthalate
CAP
true or false
high pH means high acidity
false - low pH means high acidity
besides tablets and capsules, name 5 other solid dosage forms for oral administration
lozenges (troches)
lollipops
pellets
bolus tablets
pills
explain what lozenges are.
what is another name for them
another name = troches
solid oral dosage forms that dissolve or disintegrate slowly in the mouth. contains 1 or more active drugs that are slowly releeased from the flavored and sweetened base
true or false
lozeneges give local action only
false - can give systemic too
give an example of a lollipop and what it’s used for
Fentanyl Actiq (cephalon) - raspberry lollipop
sugar-based lozenge on a stick containing fentanyl citrate
1st product designed to aid breakthrough cancer pain
explain what pellets are
sometimes called beads - small, solid particles of uniform shape that are nearly spherical
can be administered orally or parenteraly
true or false
it is a requirement for pellets to be spherical
FALSE - not a requirement, though they usually are nearly spherical
what are bolus tablets
large (usually elongated) tablets intended to be administered to large animals
what are pills
small, round solid oral dosage forms containing a medicianl agent to be administered orally
