Tablets Flashcards
Tablets are usually prepared by ______ of the drug with several excipients
compression
T/F Tablets may be scored for fairly accurate breaking
TRUE
Why does the powder in tablets need to be compacted?
because it is not filled in a gelatin shell and has a BINDER and DISINTEGRATE (helps facilitate compaction)
Types of compressed tablets? (7)
- immediate release
- sugar coated
- film coated
- enteric coated
- multiple compressed tablets
- chewable
- controlled release
immediate release tablets
breaks up in the body immediately
film coated tablets (2)
- used when the drug is bitter
- typically uses thin polyminic film
enteric coated tablets dissolve in the ______ and are resist to dissolution in the _______
intestine; stomach
What polymer is used for enteric coated tablets?
cellulose acetate phthalate
Variations of Tablets? (3)
- caplets
- geltabs
- gelcaps
An enteric coated tablet must disintegrate in simulated gastric (stomach) fluid within:
a. 2 minutes
b. 15 minutes
c. 30 minutes
d. None of the above
NONE OF THE ABOVE
multiple compressed tablets can be: (2) explain?
- layered tablets (used when 2 drugs are incompatible)
- press-coated tablets (tablet inside a tablet)
chewable tablets (2)
- contain a lot of mannitol
- meant to be chewed because they may not contain a disintegrate
controlled release tablets
slow release
Effervescent tablets involve the reaction of _____ with _______, liberating _______
sodium bicarbonate; tartaric or citric acid
liberating carbon dioxide
T/F Effervescent tablets ARE NOT temperature dependent.
FALSE: ARE
EFFERVESCENT TABLET:
What could be the solid material undissolved in water?
-magnesium stereate or talc
Rapid dissolving tablets disintegrate/dissolve in 15-30 ses in the mouth due to ______
super disintegrate
Advantages of Rapid dissolving tablets? (4)
- fast absorption
- good for travel
- increase patient compliance
- good for children and elderly
Disadvantages of Rapid dissolving tablets? (2)
- high friability (too soft)
- taste masking is difficult
What manufacturing techniques can be used to make rapid dissolving tablets? (3)
- Zydis delivery system
- soft direct compression
- fast dissolving excipients + effervescent material
________ lyophilize a foam of drug/gelatin/sugar in a mold that also serves as the unit dose dispensing package
Zeds delivery system
_______ or molded tablets are small masses of molded powders with rapidly soluble materials
tablet triturates
T/F The MORE dense the powder the LESS you can fit in a tablet
FALSE: the more dense the powder the more you can fit in a tablet
Lozenges or Troches dissolve….
slowly for localized effects
Tablet presses compress powdered/granulated tableting material through…..
the use of various shaped punches and dies
_____ punches + _____ die + 1 Station
2 punches; 1 one
To improve the flow of tablets we can use ______
granules
Example: one revolution with 27 stations will make _____ tablets
27
Granules or powder is compressed within a steel die cavity by the ________ exerted by the movement of two steel punches
pressure
concave punches = ___ tablets
convex
What is controlled by the amount of die fill and compression pressure?
-weight and thickness
In a rotary press, material flows from _____ to ______
hopper (where the powder is put in) to feed frame
What can be induced to produce a high production rate?
die feeder
Making a tablet?
-How can you make a size that can be handled?
diluent (provide bulk to make the tablet a practical size for compression)
-examples LACTOSE, MICROCRYSTALLINE CELLULOSE
Making a tablet?
-How can you make sure the powder is flowing freely?
Glidant (improve flow characteristics of powders)
-examples: COLLOIDAL SILICONE DIOXIDE, TALC
Making a tablet?
-How can you make sure the tablet is lubricated?
lubricant (prevents adhesion of powder to surfaces of die and punches and may improve flow)
-examples MAGNESIUM STEREATE, TALC
Making a tablet?
-How can you make sure the tablet is cohesive?
binder (imparts cohesiveness to the tablet formulation)
-examples STARCH, GELATIN, POVIDONE, NATURAL SYNTHETIC GUMS
Making a tablet?
-How can you make sure the drug is released in the body?
disintegrant (facilitate the breakup of tablets after administration)
What will happen if a lubricant is not added to a tablet?
it may stick to the die during production
T/F If a drug dose is HIGH you MAY NOT need a diluent.
TRUE. vs
If the drug is potent (low dose) may need a LOT of diluent
Talc is both a ____ and ______
lubricant and glidant
Excess lubricant may result in ….
poor disintegration or delayed dissolution (makes the tablet more resistant to water)
Colloidal silicone dioxide is a…
light, loose powder with a particle size of about 15 nm
HPMC is an example of a ____
binder
The same excipients can have different roles, an example is
starch paste in water–> binder
starch dry powder–> disintegrant
What are colors useful in tablets?
help distinguish one dose from another
CLASS ACTIVITY: A tablet batch failed the disintegration test. Upon investigation, the only thing found different was that the batch as left for mixing for an extended period of time over lunch break. What could be the possible reason for failure of disintegration test?
-the magnesium had more time to coat the batch–> resistant to dissolving
What are the methods of making tablets? (3)
- wet granulation
- dry granulation
- direct compression
What is the purpose of granulation?
so that powder can flow evenly and freely from the hopper into the dies
What are the steps of granulation? (2)
- Powders are first weighed and blended
2. Treated with either binder (wet granulation) or compacted (dry granulation)
What is a drawback of wet granulation?
when the drug is not stable to heat or moisture
wet granulation
-optimum amount of binding agent added and damp mass screened
What is the next step in wet granulation after added the appropriate amount of binder?
drying, dry screening, lubrication and compression
When is dry granulation used? (2)
- when drug is moisture or heat sensitive
- and/or powder has cohesive properties
Dry granulation has ____ slugs and broken and dry screened
compressed
Fluid Bed Granulation (2)
- granulation and drying takes place in same equipment
- can be used for coating
When is granulation not required? what is used instead?
drugs/excipients that possess free flowing and cohesive properties; direct compression
What are 3 potential problems in compression process?
- capping or splitting (soft granulation, excess fines, worn/imperfect punches)
- lamination
- reduced disintegration and/or dissolution
CLASS ACTIVITY: Your marketing department is insisting on filling a drug with 700 mg dose formulation into size 0 Capsule? What can be done?
-change the formulation–> add a binder to change the bulk density (INCREASE BULK DENSITY) so it can be compressed
Tablet Coating (3)
- protect from air/moisture
- taste masking/identification
- improve product appearance
Gelatin is a ______ in capsules, but a ____ in tablet
capshell lubricant; binder
Types of Tablet Coating (3)
- sugar
- film
- compression
(coating pans (warm air supply) or fluid bed processing equipment or modified tablet machines)
(first step is water proofing)
Sugar Coating is a multistep process that involves:
- sealing
- subcoating (to build up the mass/weight)
- smoothing
- color coating
- polishing & printing (wax applied)
SUGAR COATING:
Sealing coat applied using alcoholic solution of resin such as _____
shellac
Film Coating
-preferred method applies thin, uniform coating on tablet
What has allowed the use of aqueous application?
transition to vented pans and fluid-bed equipment
The formulation for FILM COATING contains: (4)
- polymer
- plasticizer
- colorant
- solvent
HPMC: Hydroperoxy methyl cellulose….
a binder
Glycerin, PG, PEG, or dibutyl subacetate are…..
used as plasticizers
What are possible problems with coating?
- picking and peeling
- orange peel effect
- mottling
- bridging
picking and peeling
flaking of the film fragments
orange peel effect
roughness of the surface
mottling
uneven distribution of color
bridging
filming in of the scoring line
All dosage forms must be taken with _____; and should be taken at least ___ hour before retiring
water; one
When can prefabricated dosage forms be used for compounding special needs…
when bulk drug is not available (i.e you can use a tablet to make a suspension if not soluble and solution if soluble)
Components of quality control for tablets? (4)
- specifications
- uniformity of dosage form
- disintegration test
- dissolution test
SPECIFICATIONS:
Tablet Hardness
- measure the force when the tablet breaks
- made in house–>USP does not make recommendations b/c it can vary
SPECIFICATION:
Tablet Friability
how much powder the tablet will shed; should not be more than 1%
Tablet ____ and ____ both have in house specifications
thickness and hardness
CLASS ACTIVITY:A company started to make tablets on a rotary press but during the initial run, tablets are too friable. What can be done?
- add a binder
- the upper punch may not be coming down to compress properly
CLASS ACTIVITY: A weight variation test on a tablet batch shows individual tablet weighs of 97mg, 101 mg, 103 mg, 98 mg. Can we be sure the patient is expected to receive correct drug dose from this formulation?
-No, this is not okay. Even though the weights are similar the amount of drug and excipient may vary between the tablets
Disintegration vs. Dissolution
- A basket rack assembly with open ended glass tubes held vertically on a 10-mesh screen
- A mechanical device raises and lowers the tubes
- Typically 15-30 minutes
disintegration test
Disintegration vs. Dissolution
-A stirrer shaft with a paddle or cylindrical basket moves in the dissolution media at 37 deg C (used to stimulate the body temperature)
dissolution test
Dissolution test equipment:
Type 1…..
Type 2…..
Type 1: Basket
Type 2: Paddle
Dissolution Test is used toL
- guide formulation development
- monitor process
- establish bioequivalence from batch to batch
IVIVC
in vitro in vivo correlation(drug absorption in the body)
Successful IVIVC depends on (2)
- drug solubility
- permeability
Which BCS (biopharmaceutic classification system) is the best?
Category 2: best correlation: low solubility and high permeability (they are absorbed quickly)
