I. Tablets 1.

Tablet w/in a tablet

- solid dosage forms usually prepared (TwT, core and shell)
with the aid of suitable pharmaceutical 2. Layered tablet (L
excipients. tabs)
- Most tablets are used in the oral C. Sugarcoated Tablets
administration of drugs.  water soluble coating which
- Tablets are prepared primarily by quickly dissolves upon
compression, with a limited number swallowing
prepared by molding.  Compressed tablets may be
- Some tablets that are not scored are coated with a colored or an
not intended to be broken or cut by the uncolored sugar layer.
patient since they may have special  protects the enclosed drug
coatings and/or drug release features from the environment
that would be compromised by altering  provides a barrier to
the tablet's physical integrity. objectionable taste or odor.
 enhances the appearance
II. Types of Tablets of the compressed tablet
A. Compressed Tablets  permits imprinting of
 usually contain a number of identifying manufacturer's
pharmaceutical excipients information
X time and expertise are
1. Diluents or fillers- required
add the necessary bulk X the increase in size, weight,
2. Binders or adhesives- and shipping costs.
promote adhesion for X Sugarcoating may add 50%
granulation to the weight and bulk of
3. Disintegrants or the uncoated tablet
disintegrating agents- promote
breakup of the tablets after D. Film-Coated Tablets
admin.  compressed tablets coated
4. Antiadherents, glidants, with a thin layer of a
lubricants, or lubricating agents- polymer capable of forming
flow enhancer, minimize wear, a skin-like film (usually
prevent sticking, and sheen colored)
tablets  Desired location: GI tract
5. Miscellaneous adjuncts-  TwT type
colorants and flavorants  more durable, less bulky,
B. Multiple Compressed and less time-consuming to
Tablets apply than sugarcoating
 prepared by subjecting the
E. Gelatin-Coated Tablets
fill material to more than a
 recent innovation
single compression
 Gelcap- capsule-shaped
 2 types:
compressed tablet
  allows the coated product  enable oral absorption of
to be about one-third drugs that are destroyed by
smaller than a capsule filled the gastric juice and/or are
with an equivalent amount poorly absorbed from the
of powder. gastrointestinal tract.
 more tamper evident than  Buccal Tablets- erode
unsealed capsules. slowly
 The gelatin coating aids in  Sublingual Tablets- dissolve
swallowing rapidly and provide rapid
 E.g., Tylenol Cold Multi- drug effects
Symptom Daytime (McNeil  Lozenges- disc-shaped solid
Consumer) dosage forms containing a
medicinal agent and
F. Enteric-Coated Tablets generally a flavoring
 delayed-release features substance in a hard candy
 designed to pass or sugar base. They are
unchanged through the intended to be slowly
stomach to the intestines dissolved in the oral cavity,
 The most important factor usually for local effects,
to consider for enteric although some are
coated tablets is the pH. formulated for systemic
 Gastric acidity is 1.5 - 3.5 pH absorption. (e.g., Mycelex
 So some enteric coatings troches of Bayer Consumer
 are designed to dissolve at Care.
pH = 4.8 and greater
 employed when: H. Chewable Tablets
a. the drug sub. is  have a smooth, rapid
destroyed by gastric disintegration when
acid chewed or allowed to
b. drug sub. is irritating to dissolve in the mouth
the gastric mucosa  pleasant-tasting tablets
c. bypass of the stomach formulated to disintegrate
substantially enhances smoothly in the mouth with
drug absorption or without chewing.
 E.g., Ecotrin tablets and  have a creamy base, usually
caplets (GlaxoSmithKline of specially flavored and
Beecham). colored mannitol.
 prepared by wet
G. Buccal and Sublingual granulation and
Tablets compression, using only
 flat, oval tablets intended minimal degrees of
to be dissolved in the pressure to produce a soft
buccal pouch or beneath tablet.
the tongue (sublingual  Mannitol
tablets)
  Mannitol is about 70% dissolution of the active
as sweet as sucrose, drug.
with a cool feel in the  E.g., Alka-Seltzer Original
mouth resulting from tablets (Bayer Consumer
its negative heat of Care) and Zantac
solution. EFFERdose
 a white crystalline (GlaxoSmithKline)
hexahydric alcohol, is
used as the excipient in
J. Molded Tablets
 very soft and soluble tablets
most chewable tablets.
that are designed for rapid
 50% or more of
dissolution
chewable tablets
 The mold is made of hard
weight
rubber, hard plastic, or
 do not contain disintegrants
metal.
 Lubricants and binders that
 Upper part is the die
do not detract from the
portion and the lower part
texture or desired hardness
is the punches portion
of the tablet may be used.
 The die portion is a flat
 for children and adults who
plate with the thickness of
have difficulty swallowing
the tablets to be produced,
solid dosage forms.
with 50 to 200 uniformly
 these tablets tend to be
drilled and evenly spaced
more fragile than standard
circular holes
compressed tablets, they
 The base for molded tablets
are generally packaged in
is generally a mixture of
more sturdy materials to
finely powdered lactose
prevent damage.
with or without a portion of
 E.g., Pepcid AC chewable
powdered sucrose
tablets (J&J Merck) and
 addition of sucrose = fewer
Rolaids chewable tablets
brittle tablets
(Pfizer Consumer
 Molded tablets are
Healthcare).
intended to dissolve rapidly
I. Effervescent Tablets in the mouth.
 compressed granular  do not contain
effervescent salts disintegrants, lubricants, or
 release gas when in contact coatings to slow their rate
with water of dissolution
 contain medicinal  e.g., Tablet Triturates
substances that dissolve
rapidly when added to
K. Tablet Triturates
 small, usually cylindrical,
water
molded, or compressed
 The “bubble action” can
tablets containing small
assist in breaking up the
tablets and enhancing the
 amounts of usually potent rate-controlling features,
drugs such as special coatings and
 most of these produced by other techniques
tablet compression.
 minimal amount of O. Rapidly Disintegrating or
pressure is applied during Dissolving Tablets
their manufacture  disintegrates or dissolves in
 Diluent: Sucrose + Lactose the mouth within 1 minute,
 Some are inserted in a some within 10 seconds
capsule for accurate (e.g., Clarinex Reditabs
amount of API [loratadine], Schering)
 Used by pharmacists in  designed for children and
compounding the elderly or for any
 e.g., NTG Tablets patient who has difficulty in
swallowing tablets
L. Hypodermic Tablets  liquefy on the tongue, and
 for extemporaneous the patient swallows the
preparation of parenteral liquid
solutions  Preparation techniques
 dissolved in a suitable o Lyophilization
vehicle, sterility attained, Technique (e.g., Zydis,
and the injection performed R.P. Scherer),
X difficulty in achieving o Soft Direct
sterility Compression (e.g.,
X the availability of Wow-Tab, Yamanouchi
prefabricated injectable Shaklee Pharma)
products eliminated the o Other methods (e.g.,
need for these tablets. Quicksolv, Janssen)
 prepared using very water-
M. Dispensing Tablets
soluble excipients designed
 A.K.A “Compounding
to wick water into the
Tablets”
tablet for rapid
 contained large amounts of
disintegration or dissolution
highly potent drug
 have the stability
substances
characteristics of other
 not dispensed as such to
solid dosage forms
the patient due to the
 Original RDT were molded
dangerous potential of
tablets for sublingual use
being inadvertently
 API + Lactose moistened
dispensed
with an alcohol-water
N. Immediate-Release Tablets mixture
 designed to disintegrate  used for drugs that are
and release their destroyed in the
medication with no special gastrointestinal tract, such
 as testosterone,  prepared by compression
administered sublingually and shaped to fit snugly on
for absorption to minimize plastic inserter devices that
the first-pass effect accompany the product
 more convenient to carry  contain antibiotics and
and administer than an oral antifungals
liquid
 generally packaged in cards III. Method of Preparation
or bubble-type packaging
A. Lyophilized Foam
with each individual tablet
 foamed mixture of gelatin +
in its own cavity
sugar/s + drug + others +
 General Def: drug that
molding = RDTs
dissolves in the mouth
X taste masking can be a
within approximately 15
problem in this method
seconds (slower = not an
X drugs can be sometimes
RDT)
difficult to remove from the
X drug loading
packaging
X taste masking
 e.g., Claritin Reditabs,
- remedied by a flavoring
Maxalt-MLT (Merck),
technique or by
Zofran ODT
microencapsulation or
(GlaxoSmithKline), Zyprexa
nanoencapsulation
Zydis (Eli Lilly) tablets, and
X problem in friability
Tylenol Meltaways Jr.
- an inherent problem
(McNeil Consumer)
- balance must be
 Claritin Reditabs use diff.
achieved b/w friability
formulation
and the speed of
 Its excipients are:
dissolution
a. mannitol
X problem in manufacturing
b. microcrystalline
costs
cellulose
X problem in stability of the
c. pregelatinized starch
product
d. sodium starch glycolate
P. Extended-Release Tablets e. magnesium stearate
 designed to release their f. butylated methacrylate
medication in a copolymer
predetermined manner g. crospovidone
over an extended period. h. aspartame
i. citric acid
Q. Vaginal Tablets j. sodium bicarbonate
 A.K.A. “Vaginal Inserts” k. colloidal silicon dioxide
 uncoated, bullet-shaped, or l. ferric oxide red
ovoid tablets inserted into m. tutti-frutti flavoring
the vagina for local effects
B. Compression - by Yamanouchi Pharma;
 uses standard tableting used in Benadryl
technology Fastmelt
 enhances fluid uptake and
tablet disintegration and IV. Example Chewable
dissolution Dispersible Tablets
 tablets are compressed a
 generally packaged in more sturdy
little thinner than standard
materials to prevent damage
tablets to allow for a larger
 Lamictal chewable dispersible tablets
surface area exposed to the
for oral administration contain 2, 5, or
saliva in the mouth
25 mg of lamotrigine
 DuraSolv and OraSolv
 Excipients:
technologies (Tempra
Quicklets action is done/ a. black currant flavor
- slower than the Zydis b. calcium carbonate
tablet, taking about 30 c. low-substituted hydroxypropyl
to 45 seconds, unless cellulose
some tongue pressure d. magnesium aluminum silicate
is used. e. magnesium stearate
- Examples of Comp. f. povidone
Products g. saccharin sodium
o Dimetapp ND orally h. sodium starch glycolate
disintegrating  Lamotrigine is also available as standard
tablet swallow tablets for oral administration
o Alavert (Wyeth) in strengths of 25, 100, 150, and 200 mg
o NuLev FasTabs  Lamotrigine is an antiepileptic drug
(Schwarz Pharma) chemically unrelated to existing drugs in
o Symax FasTabs this therapeutic class.
(Capellon)  Didanosine (Videx) is available in three
o Remeron SolTabs dosage forms: a chewable dispersible
(Organon) buffered tablet, buffered powder for
o Triaminic Softchews oral solution, and a pediatric powder
(Novartis Consumer for oral solution.
Health)  Didanosine (2′,3′-dideoxyinosine) is
o Abilify Discmelt unstable
(Otsuka America), o in acidic solutions
o Tylenol Meltaways o at a pH lower than 3 at body temp.
(McNeil Consumer)  10% of didanosine decomposes to
o Zomig ZMT hypoxanthine in less than 2 minutes.
(AstraZeneca)
 Flashtab technology V. Compressed tablets
- by Ethypharm; used in  Physical features:
Excedrin QuickTabs a. round, oblong, or unique in shape
 Wowtab technology b. thick or thin
 c. large or small in diameter 1. 10 tablets are weighed
d. flat or convex individually
e. unscored or scored in halves, thirds, 2. the average weight is
or quadrants calculated
f. engraved or imprinted 3. The tablets are
g. coated or uncoated assayed, and the content of
h. colored or uncolored active ingredient in each of
i. one, two, or three layered the 10 tablets is calculated
 Tablet diameters and shapes are assuming homogeneous drug
determined by the die and punches
distribution
used in compression
a. flat face, B. Content Uniformity
b. shallow cup  10 dosage units are
c. standard cup individually assayed for
d. deep cup their content according to
e. modified ball the method described in
the individual monograph.
 Content uniformity is met if
VI. 7 Quality Standards and the amount of API in the
Compendial Requirements dosage unit lies w/in the
 tablets must meet other physical range of 85% to 115% of
specifications and quality standards. the label claim and
a. weight standard dev. is <6%
b. weight variation  If one or more dosage units
c. content uniformity do not meet these criteria,
d. thickness additional USP test is
e. hardness required.
f. disintegration
g. dissolution C. Tablet Thickness
 determined by:
A. Tablet Weight and USP a. the diameter of the die
Weight Variation Test b. the amount of fill
 The quantity of fill in the die permitted to enter the
of a tablet press determines die
the weight of the tablet. c. the compaction
 During production, sample characteristics of the fill
tablets are periodically material
removed for visual d. the force or pressure
inspection and automated applied during
physical measurement compression
 For uniform thickness, care
must be exercised to
employ the same factors of
fill, die, and pressure during
and between batch
 productions for the same  Friabilator- used to
formulation measure a tablet's
 Pressure affects not only durability; determines the
thickness but also hardness tablet's friability, or
of the tablet (hardness is tendency to crumble, by
more important criterion allowing it to roll and fall
since it has something to do within the drum (e.g.,
with the disintegration and Varian friabilator)
dissolution)  Resistance to loss of
 can be measured by a hand weight indicates the
gauge during production or tablet's ability to withstand
by automated equipment abrasion in handling,
packaging, and shipment
D. Tablet Hardness and  Maximum weight loss of
Friability not more than 1% generally
 Tablet press produces force is considered acceptable for
as little as 3,000 and as most products.
much as 40,000 lb
 the characteristics of the E. Tablet Disintegration
granulation also have a  tablet disintegration
bearing on hardness. provides drug particles with
 the greater the pressure an increased surface area
applied, the harder the for activity.
tablets  All USP tablets must pass a
 tablets should be test for disintegration,
sufficiently hard to resist which is conducted in vitro
breaking during normal using a testing apparatus
handling and yet soft  a tablet is placed in each of
enough to disintegrate the six tubes of the basket,
properly after swallowing and through the use of a
 Special dedicated hardness mechanical device, the
testers or multifunctional basket is raised and
systems are used to lowered in the immersion
measure the degree of fluid at 29 to 32 cycles per
force required to break a minute, the wire screen
tablet. always below the level of
 4kg is the minimum the fluid.
pressure for a satisfactory  For uncoated tablets,
tablet. buccal tablets, and
 Multifunctional automated sublingual tablets:
equipment can determine water at about 37°C serves
weight, hardness, thickness, as the immersion fluid
and diameter of the tablet. unless another fluid is
specified in the individual
monograph.
  Complete disintegration= a. Guides: formulation
any residue of the unit, and product
except fragments of development toward
insoluble coating or capsule product optimization
shell, remaining on the b. Monitors: quality of the
screen of the test apparatus process of
is a soft mass having no manufacturing
palpably firm core c. Ensures: drug
 Tablets must disintegrate bioequivalence from
within the times set forth in batch to batch
the individual monograph, d. A requirement for
usually 30 minutes, but regulatory approval of
varying from about 2 marketing the drug
minutes for NTG tablets to product
up to 4 hours for buccal  Goal: provide prediction of
tablets. or correlation with the
 If one or more dosage units product's in vivo
do not meet these criteria, bioavailability.
additional USP test is  The system relates
required. combinations of a drug's
 For enteric-coated tablets, solubility (high or low) and
the tablets are tested in its intestinal permeability
simulated gastric fluid for 1 (high or low) as a possible
hour, after which no sign of basis for predicting the
disintegration, cracking, or likelihood of achieving a
softening must be seen and successful in vivo–in vitro
then, they are actively correlation.
immersed in the simulated  Four categories
intestinal fluid for the time (S=solubility; P=
stated in the individual permeability)
monograph, during which 1. High S and High P (cat. I)
time the tablets - IVIVC is expected; dissoln
disintegrate completely for rate < gastric emptying rate
a positive test. 2. Low S and High P (cat. II)
- IVIVC is expected;
F. Tablet Dissolution dissolution may be the rate-
 component of evaluating limiting step for absorption
product quality in the USP 3. High S and Low P (cat. II)
since 1970, when only 12 - limited IVIVC; perm. is the
monographs contained rate-limiting step
such a requirement. Today, 4. Low S and Low P (cat. IV)
the requirement is standard - Oral drug delivery
for tablets and capsules problems
 Important for a number of
reasons:
 Factors affecting dissol. and b. a cylindrical stainless-
disint. of a tablet steel basket on a stirrer
a. particle size of the drug shaft (USP Apparatus 1)
substance or a paddle as the
b. solubility and stirring element (USP
hygroscopicity of the Apparatus 2)
formulation c. a 1,000-mL vessel of
c. type and concentration glass or other inert
of the disintegrant, transparent material
binder, and lubricant; fitted with a cover
d. manufacturing method having a center port for
e. any in-process variables the shaft of the stirrer
 batch-to batch consistency and three additional
is vitally important to ports, two for removal
establish dissolution test of samples and one for
standards and controls for a thermometer
both materials and d. a water bath to
processes and to maintain the
implement them during temperature of the
production and in final dissolution medium in
testing. the vessel
 the method of dissolution  The samples are submerged
testing must be controlled in the dissolution liquid
to minimize important with a temp. of 37 oC ± 0.5
o
variables C
a. paddle rotational speed  >85% of the labeled
b. vibration amount is dissolved in 30
c. disturbances by minutes
sampling probes  inconsistencies in
 The USP includes seven dissolution occur between
apparatus designs for drug batches or between
release and dissolution products from different
testing of immediate- manufacturers
release oral dosage forms,  Pooled Dissolution Testing-
extended-release products, dosage units within a batch
enteric-coated products, are tested together.
and transdermal drug
delivery devices. Compressed Tablet Manufacture
 Apparatus 1 and USP  Free-flowing property of
Apparatus 2 are the primary the drug mixture is vital in
interest here tablet manufacture for
 The equipment consists of: high-speed compression of
a. a variable speed stirrer the powder mix into tablets
motor  Benefits of granulation:
a. Provides free flow
 b. increase material by the free-
density flowing
c. improves powder granules
compressibility during o Voids or air
tablet formation spaces left by
 3 methods: too large a
a. wet granulation granulation
 widely employed result in the
method production of
 Steps: uneven tablets
1. weighing and 6. adding lubricant
blending the and blending
ingredients o Stea-L
2. preparing a substances and
dampened powder Talc
or a damp mass 7. forming tablets
o Overwetting = by compression.
Too Hard  Spraying methods
Granules a. Top spray
o Underwetting=
b. Bottom spray
Too Soft Tablets
(Wurster)
3. screening the
c. Tangential
dampened powder
spray
or damp
 Fillers-
mass into pellets or
1. lactose
granules.
2.microcrystalline
o #6-#8 meshes
3.cellulose
4. drying the
4.starch
granulation
5. powdered
5. sizing the
sucrose
granulation by dry
6.calcium
screening
phosphate
o the smaller the
tablet to be
(most pref are
produced, the
lactose and
smaller the
microcrystalline
granules
cellulose)
o #12-#20
 Disintegrating
meshes
agents-
o Sizing of the
croscarmellose,
granules is for corn and potato
completely and starches, sodium
rapidly filling of starch glycolate,
the die cavities sodium
 carboxymethylcellul  for materials that
ose, cannot be prepared
polyvinylpyrrolidon by wet granulation
e (PVP), because they
crospovidone, degrade in
cation exchange moisture or the
resins, alginic acid, elevated
and others (often temperatures
pref are required for drying
Croscarmellose the granules.
(2%) and sodium  Example: Aspirin
starch glycolate Slugging
(5%))  Ways of dry
 All-in-One granulation:
Granulation 1. Slugging
Methods - compressed into
- continuous fluid large flat tablets or
bed process by the pellets about 1 inch
fluid bed in diameter
granulator 2. Roller
- microwave Compaction
vacuum processing - more pref. than
allows the powders slugging because it
to be mixed, is a continuous
wetted, process
agglomerated, and - pressing it
dried within the between rollers at 1
confines of a single to 6 tons of
piece of equipment; pressure
drying speed  A consequence of
increases by ¼ due high-speed
to the help of the production is the
microwave increased
b. dry granulation occurrence of
 the powder mixture lamination
is compacted in (horizontal
large pieces and striations) and
subsequently tablet capping
broken down or c. direct compression
sized into granules  For granular
 the API or the chemicals that
excipient must possess free-
have cohesive flowing and
properties cohesive properties
 The capping, adhering to tablets
splitting, or following
laminating of compression.
tablets is
sometimes related Tableting: Steps of mechanical
to air entrapment process of a single punch
during direct operation and facts about the
compression rotary tablet machines
 Forced or induced 1. The lower punch
feeders can reduce drops to give more room for
air entrapment, the die cavity as the feed shoe
making the fill fills it with granules.
powder denser and 2. Excess granules are
more amenable to
scraped off by the feed shoe
compaction.
as it retracts.
 Capping also may
3. The upper punch
be caused by
compresses the granules to
punches that are
not immaculately
form a tablet, then the upper
clean and perfectly punch simultaneously rises
smooth or by a with the lower punch.
granulation with 4. The feed shoe moves
too much fines or the tablet aside to fill the die
fine powder. cavity again
 Fine powder is Rotary tablet machines
generally 10% to equipped with multiple
20% of the weight punches and dies operate
of the granulation via continuous rotating
 Adequate amount movement
of fine powder = Single Rotary Press w/ 16
proper filling of the stations = 1,150 tablets/min
die cavity Double rotary tablet
 Excessive amount presses with 27, 33, 37, 41,
of fine powder = or 49 sets of punches and
tablet softness and dies are capable of
capping producing two tablets for
 Aged and each die.
improperly stored A consequence of high-
tablets= splitting or speed production is the
other physical increased occurrence of
deformations. lamination (horizontal
 Tablet Dedusting- striations) and tablet
remove traces of capping. The solution to
loose powder
 this problem is decrease in 1. Waterproofing and
speed. sealing if necessary
shellac or a polymer
Tablet Problems Warm air is for fast
1. Capping- separation drying and prevent
of the top or bottom surface the tablet from
5. Lamination- sticking to one
Separation into 2 or more another
distinct layers 2. Subcoating
6. Picking- sticking to a coating of sugar-
punch face based syrup for
rounding and a
7. Sticking- adherence to
primer for the sugar
the die wall.
coating
8. Mottling- uneven 3. Smoothing and final
coloring rounding
Tablet Coating addition of 5-10
 all tablets are visually or additional coatings
electronically inspected for of a thick syrup for
physical imperfection smoothening and
 Functions: final rounding
1. protect the medicinal dusting powder is
agent against used in between
destructive exposure to coating
air and/ or humidity 4. Finishing and coloring if
2. mask the taste of the desired
drug attaining the final
3. provide special smoothness and
characteristics of drug the appropriate
release color to the tablets
4. provide aesthetics or 5. Imprinting
distinction to the 1995 FDA
product regulation: all solid
5. prevent inadvertent dosage forms for
contact with the drug human
substance and the consumption,
effects of drug including both
absorption (e.g., prescription only
Proscar tablets must and over-the-
not be touched/inhaled counter drug
by a woman who has a products, must be
male fetus) imprinted with
product-specific
Sugarcoating Tablets identification codes
 Steps:
 Embossed- mark X Varying sizes from batch to
above the surface batch and within a batch
Debossed- mark
below the surface Film-Coating Tablets
Engraved- cut into  places a thin, skin-tight
the surface coating of a plastic-like
6. Polishing material over the
carnauba wax and compressed tablet
beeswax  same weight, shape, and
Linings with size as the originally
polishing agent compressed tablet
Tumbling of tablets  thin enough to reveal any
on the pieces of identifying monograms
wax embossed in the tablet
light spraying of  far more resistant to
with wax destruction by abrasion
 Conducted in a series of than are sugarcoated
mechanically operated tablets
acorn-shaped coating pans  Contents of the non-
of galvanized iron, stainless aqueous solution for film-
steel, or copper. coating
 The pans operate at about a 1. Film Former- produces
40-degree angle to contain smooth, thin films
the tablets while allowing 2. Alloying Substance-
the operator visual and provides water
manual access. solubility or
 Each coat is applied only permeability
after the previous coat has 3. Plasticizer- flexibility
dried. and elasticity
 Tablets intended to be 4. Surfactant- enhance
coated are manufactured to spreadability
be thin edged and highly 5. Opaquants and
convex to allow the colorants
coatings to form rounded 6. Sweeteners, flavors,
rather than angular edges. and aromas- for patient
X tedious acceptability
X time-consuming 7. Glossant- luster
X specialized 8. Volatile Solvent- the
X requiring the expertise of spread of the other
highly skilled technicians components over the
X Tablets are twice the size tablets while allowing
and weight of the original rapid evaporation to
uncoated tablets. permit an effective yet
speedy operation
 Aqueous solutions are more to the intestines and may
preferred due to relatively be accomplished through
cheaper cost and coatings of sufficient
environmental-friendliness thickness.
compared to non-aqueous  based on factors of pH
kinds. However, this has  Resist gastric dissolution
slower water evaporation but yield to intestinal
than the latter. Solution: digestion
Aquacoat (greater coating  The coatings may be
ability and a relatively low applied in multiple portions
viscosity). to build a thick coating or as
 Contents of the aqueous a thin film coat
solution for film-coating  The coating system may be
1. Film-forming polymer aqueous or organic solvent
2. Plasticizer based and effective so long
3. Colorant and opacifier as the coating material
4. Vehicle resists breakdown in the
 Problems attendant on gastric fluid.
aqueous film coating  Materials for enteric-
* Result of the Orange Peel coating
Effect 1. Shellac
- failure of spray droplets 2. hydroxypropyl
to coalesce= flaking + methylcellulose
roughness phthalate
1. Picking- small amount 3. polyvinyl acetate
of film fragments phthalate
2. Peeling- large amount 4. diethyl phthalate
of film fragments 5. cellulose acetate
3. Mottling- uneven dist. phthalate
of color
Fluid Bed or Air Suspension
4. Bridging- filling-in of the
score line or indented
Coating
 spray coating of powders,
logo
granules, beads, pellets, or
5. Tablet erosion-
tablets held in suspension
disfiguration of the core
by a column of air
tablet
 Factors affecting the quality
Enteric Coating of coating
 pass through the stomach 1. Method of spraying
intact to disintegrate and 2. Spray nozzle distance
release their drug content from spraying bed
for absorption along the 3. Droplet size
intestines 4. Spray rate
 Design: based on the transit 5. Spray pressure
time required for passage
 6. Volume of the air Compression Coating
column  The coating material, in the
7. Batch Size form of a granulation or
8. Method and time for powder, is compressed
drying onto a tablet core of drug
9. Air Temperature with a special tablet press.
10. Moisture Content  More uniform and uses less
 3 types of fluidized bed coating material
systems  Lighter, smaller, and easier
1. Top-spray method to swallow tablets
taste masking,  Less expensive to package
enteric release, and and ship
barrier films on
particles or tablets. Impact of manufacturing
provides greater changes in solid dosage forms
capacity, up to  Changes in Formulation
1,500 kg, than the 1. starting raw materials
other air susp. with varying chemical
coating methods. or physical
most effective characteristics than the
when coatings are original components.
applied from 2. Different quantities of
aqueous solutions, the same excipients in a
latexes, or hot formulation
melts 3. Addition of a new
2. Bottom-spray method excipient to a
(Wurster process) formulation
drug layering and 4. Different
control drug release pharmaceutical
for batches of small excipients
amounts  Changes in the Method of
3. Tangential spray Manufacture
technique 1. Different design of
side-spraying processing or
layering coatings manufacturing
and for sustained- equipment
release and enteric- 2. Change in the steps or
coated products order in the process or
Used in rotary fluid method of manufacture
bed coaters 3. Different in-process
controls, quality tests,
or assay methods
4. Different batch sizes
 5. Different product are prone to decomposition
reprocessing by moisture
procedures  Placed in light-resistant
6. Different containers: for drugs that
manufacturing site are adversely affected by
 Changes such as these may light
be proposed or  Properly stored = stable for
implemented: several years or more
1. During the product  In dispensing: use a similar
development stage type of container as
2. During scale-up of provided by the
product manufacture manufacturer of the
before NDA approval product.
3. After NDA approval and  For patients: keep the drug
product marketing. in the container dispensed
 Minor changes  the hardness of certain
- do not affect product tablets may change upon
quality aging, usually resulting in a
- do not require prior decrease in the
FDA approval disintegration and
- e.g., New Color dissolution rates of the
 Major Changes product.
- affect product quality  Increase in hardness:
and performance increased adhesion of the
- require prior FDA binding agent and other
approval formulative components
- e.g., use of a within the tablet (e.g.,
substantially different aluminum hydroxide,
quantity or grade of an sodium salicylate, and
excipient or use of a phenyl butazone)
piece of manufacturing  For tablets containing
equipment that volatile drugs like NTG=
changes the X Packing materials like
methodology of cotton and rayon
manufacture X Storage of a container
next to a heat source
Packaging and Storing  Preserved in tight
Tablets containers, preferably
 stored in tight containers, in of glass
places of low humidity, and  Controlled room
protected from extremes in temperature
temperature.  Be dispensed in the
 Package with a desiccant original unopened
packet: for products that container
  Close tightly is a sugar-based
immediately after use lozenge on a stick and
 Place RDTs in special contains fentanyl
packagings due to their citrate
softness. - Actiq is designed to aid
in controlling
Other Solid Dosage Forms breakthrough pain in
for Oral Administration cancer patients
 Lozenges (Troches) - Breakthrough cancer
- designed to dissolve or pain occurs in about
disintegrate slowly in 50% of cancer pain
the mouth patients and is a
- designed to dissolve or component of chronic
disintegrate slowly in cancer pain that is
the mouth particularly difficult to
- used for both local and treat because of its
systemic action severity, rapid onset,
- can be made by and frequent
compression or molding unpredictability
- Compressed lozenges: - immediate relief for 15
made using a tablet minutes (long enough
machine and large, flat for the relief of
punches breakthrough pain)
- subjected to greater - The concern about this
compression; harder product being
than ordinary tablets so accidentally used by
that they dissolve or children is addressed by
disintegrate slowly in special packaging that
the mouth requires scissors to
- Medicinal substances open
that are heat stable  Pellets
may be molded into - small, solid particles of
hard sugar candy uniform shape
lozenges by candy- sometimes called beads
making machines - being spherical is not a
- . To slow the rate of requirement
dissolution, - provide physical
polyethylene glycols separation for
and hypromellose are chemically or physically
sometimes added. incompatible materials,
 Lollipops extended release of an
- Fentanyl Actiq active pharmaceutical
(Cephalon) is a ingredient (API), or
raspberry lollipop that delayed release to
 protect an acidlabile
API from degradation in
the stomach or to
protect stomach tissues
from irritation
- usually placed inside a
hard-shell capsule
- Capsule sizes are
usually #1 (5 gr) and #0
(7.5 gr)
 Bolus Tablets
- large, usually elongated
tablets intended for
administration to large
animals.
- higher compression
forces may be
necessary due to their
larger size
 Pills
- small, round solid
dosage forms
containing a medicinal
agent
- intended to be
administered orally
- replaced by
compressed tablets and
capsules
- Excipients are selected
for pills based on their
ability to produce a firm
and plastic mass