*~ Tablets ~*

TABLETS
• solid pharmaceutical dosage form containing
drug substance with or without suitable
diluents
• their shapes and dimensions are determined by
use of various shaped punches and dies

• tablets are prepared primarily by compression, with

limited number prepared by molding

• vary in size, shape, weight, hardness,

thickness,disintegration depending upon use & method
of manufacturing

• some tablets are scored, or grooved, which

allows them to be easily broken into 2 or
more parts
• for oral tablets – colorants, flavorants and coating of
various type

• for oral, buccal, sublingual, or vaginal

administration may be prepared by compression and
have different adjuncts

• layered tablets are prepared by initial compaction

of a portion of fill material in a die followed by
additional fill material and compression to
form 2 or 3 layered tablets

• tablets that are not scored are not intended to be

broken or cut
• Accurate dosage since each tablet represent one dosage units

• Preference of manufacturers due to rapid mass production

• Lease expensive of the solid dosage forms and as to lightest in

weight and therefore cheapest to pack.

• Easy to carry (capsules may come open)

• Compact and easy for the pharmacist to store

• Chemically stable

• Can provide control of drug release

In Summary Solid Dosage Forms, Most Notably Tablets Provide Advantages

in storage, dispensing,
and control

To the pharmacist

convenience of use

To the patient
 of product identification,
dosage accuracy and precision,
improved control and more
reliable therapy
To the physician

cheaper due to mass production

and easier to manufacture,
simplicity, economy, stability,
and convenience

To the manufacturer
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COMPRESSED EXTENDED RELEASE

MULTIPLE COMPRESSED INSTANTLY DISINTEGRATING

SUGAR - COATED CHEWABLE

VAGINAL
CHOCOLATE - COLORED

FILM COATED TABLET TRITURATE

MOLDED HYPODERMIC

ENTERIC COATED TIMED-RELEASE

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BUCCAL / SUBLINGUAL PILLS Examples oF

Official Tablets
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Prepared by single compression, occur in various shapes and sizes and
usually contain in addition to the medicinal substance/s a number of
pharmaceutical adjuncts including:

1. Essential components - those that impart satisfactory

characteristics to the formulation such as:
a. Diluent or bulking agent - those substances that make up
the major portion of the tablet
b. Binders or granulators - those substances that “glue”
powders together and cause them to form granules. They
impart cohesive qualities to the powdered material.
C. Disintegrants - material that help the tablet break up and
dissolved to release the medicament for rapid dissolution
2. Compression Aids - those materials which impart
satisfactory compression characteristics such as:
a. Glidants - materials added to the formulation to
enable the granules to flow from hopper on the tablet
press to the die and for consistent and uniform fill.

b. Lubricants - materials which aid in

releasing the compressed tablet from the die

c. Antiadhesives - materials needed to prevent

the formation of residue films of tablets granulation in
the punches
3. Supplementary Components - those that give
additional desirable physical characteristics to the finished
tablets

a. Colors - materials added to a tablet for its

aesthetic value, to provide a control during manufacture,
and to distinguish one product from another.

b. Flavors - materials added for the same reason

above

c. Sweetening Agents - those that are added to

enhance the taste of the finished tablet especially when
chewed.
Examples OF Diluents
1. Lactose USP - It is the principal bulking agent used
Advantages:
1. Inexpensive 4. Not softened by the friction forces
2. Readily soluble of compression
3. Stable and generally inert

2. Starches - wheat, corn, rice, potato - use as binders and

disintegrants

3. Mannitol
Advantages
1. Highly desirable for water-sensitive drugs
2. Appropriate for chewable tablets because of its taste

4. Sorbitol - use for direct tableting

5. Sucrose - serve as binder because of its cohesive property, and additional

sweetness
Example Of Diluents
1. Starch Paste - aqueous solution of corn starch - 10 to 20% w/w
2. Aqueous Gelatin Solution - 10 to 20% w/w
3. Aqueous Glucose Solution - 25 to 50% w/w
4. Alcoholic Solution of ethylcellulose - 5% w/w

Examples Of Disintegrants

1. Starches - corn and potato

2. Clays - betonite and beegum

3. Cellulose - methylcellulose, sodium CMC

4. Algins - alginic acid and sodium alginate

5. Gums - locust bean, karaya, agar, tragacanth

 A Well Made Compressed Tablets Possesses These
Attributes
1. Ability to withstand the rigors of the mechanical treatment
involved in the production, packaging, shipment and
dispensing.
2. Freedom from defects such as cracks, chipped edges,
discoloration, specking and contamination.
3. Reasonable chemical and physical stability during
average storage conditions.
4. Ability to release the medicament in a reproducible and
predictable manner.

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Are prepared by subjecting to more than a single
compression. The result maybe multiple layered tablet or
tablet within tablet, the inner tablet being the core and the
outer portion being the shell.

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 Are compressed tablets which may be coated with colored or
uncolored sugar.

The coating is water-soluble and is quickly dissolved after

swallowing

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Advantages:
1. It serves the varied purposes and protecting
the drug from air and humidity.
2. Provides the taste or smell barrier to
objectionable tasting or smelling drugs.
3. It enhances the appearance of many CT

Disadvantages:
1. Time and expertise required by the
process
2. Increase in size and weight of the
CT which may be 50% larger and
heavier than the original uncoated
tablet.
 Basic Steps In Sugar Coating Of Compressed Tablets and
Granules

1. Sealing - This done to separate the core from the water that is used in the
coating process. Waterproofing materials - cellulose acetate, zein,
shallac, and resins are adhesive in nature, therefore, dusting powders
such as asbestos-free talc and terra alba are applied in between two seals coats up to six
seal coats to prevent the tablets from sticking with one another and to
the coating pan.

2. Subcoating - this is to round off the tablet - to improve the bond between
seal coat and the sugar coat, and to standardized tablet size.

Examples: solutions of gelatin and/or acacia

3. Syruping - It usually involves 3 basis phases such as grossing, heavy sugar

coating, and regular syrup coating.
3 BASIC PHASES
a. Grossing - the application of a syrup solution with sub coating powder dispersed in it
and with dye added to develop a color base for the final syrup application

b. Heavy sugar coating - application of a syrup concentrate to build up a solid

rapidly and attain a specific tablet volume.

C. Regular syrup coating - applied just prior to finishing without permitting the
tablets to become as dusty as the previous two syruping stage.

4. Finishing - This initiated when the desired colors is attained. Three or four coats of
regular syrup are applied rapidly without permitting the the tablet bed to become dusty.

5. Polishing - Is done in canvas polishing pan by allowing the coated tablets to roll in wax
solution until high luster is produced.
Are mainly of historic importance since chocolate was
once used to color and coat compressed tablets.
Today, chocolate has been replaced by the other
chocolate like iron oxides to stimulates the chocolate
color.

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Are compressed tablets coated with a thin layer of a
water-insoluble polymeric substances capable of
forming a film over tablet. The film coat is usually
colored.

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 Advantages over Sugar Coated Tablets
1. It is more durable
2. Less bulky
3. Less time consuming to apply/ reduction in coating
time/material cost
4. No significant increase in tablet weight
5. No undercoat or water proof coat required
6. Resistance to chipping and cracking
7. Allows monogramming identification of product
8. Provides effective protection to light, air and moisture
9. Pharmaceutically elegant
10. Provides the opportunity to use non-aqueous coating solutions
• rapid dissolving tablets or RDT are characterized by
disintegrating or dissolving in the mouth within 1
minute, some within 10 seconds ( Claritin Reditabs -
Loratadine )

• designed for children and the elderly, patient with

difficulty in swallowing tablets

• liquefy on the tongue, and the patient swallows the liquid

EFFERVESCENT TABLETS
These are prepared by compressing granular effervescent salts or other materials having
the capacity to release gas when in contact with water.

DISPENSING TABLETS
Might be better termed “compounding tablets” . Since they are used by the pharmacists
in compounding and are never dispensed as such to the patient.

Characteristics:
1. Contain relatively large amount of highly potent drugs substances
2. The diluent or base of the tablet is usually water soluble to permit the
preparation of clear aqueous solutions.
3. Dispensing tablets may be prepared by either molding or compression.
4. Disintegrating agents water-insoluble lubricants, colorants, flavorants, and
coating are not used in the preparation of dispensing tablets.

NOTE: These tablets are no longer used today due to potential hazards.
 Techniques to prepare the RDT

1. Lyophilization - Zydis by R.P. Echerer

2. Soft direct compression - Wow-tab by Yamanouchi

Shaklee Pharma

3. Other method - Quicksolv by Janssen

CHARACTERISTICS OF RDTs

• tablets are prepared using water-soluble excipients to wick water into

tablet for rapid dissolution and disintegration
•no standards that define RDT, but one possibility is dissolution in the
mouth within approximately 15 to 30 seconds; anything slower would
not be categorized as rapidly dissolving

Disadvantages and difficulties in formulating RDTs: drug loading, taste

masking, friability, manufacturing costs, and stability of the product
•drug loading = is incorporation of the drug into dosage forms
• taste masking = since dissolved in the mouth, taste must be
covered, either (1) flavoring technique, (2) microencapsulation or
nanoencapsulation
•friability = is an inherent problem in RDTs, since dissolve instantly, it
may be quite friable, making it more firm and less friable may increase
dissolution time.
 Lyophilized Foam
• Zydis was the first entry into the RDt
• Prepared by foaming a mixture of gelatin, sugars, drug, and any
other components and pouring the foam into a mold.
• the mold also serves as the unit dose dispensing package, the
foam is lyophilized and packaged
• Claritin (loratadine) rapidly disintegrating tablet (Reditabs)
contain 10 mg of micronized loratadine in a base containing
citric acid, gelatin, mannitol, and mint flavor formed with Zydis
technology
• Claritin Reditabs are blister packaged tablets that should be
stored in a dry place at 20 to 250C.They should be used within 6
months of opening the laminated foil, each foil pouch contains
one blister card containing 10 individually sealed tablets.
• Examples: (Zydis technology) : Maxalt-MLT (Merck), Zofran
ODT (GlaxoSmithKline), and Zyprexa Zydis (Eli Lilly) tablets
 Compression
in the mouth, the disintegrant starts wicking water into
the tablet. The effervescent materials start dissolving and
aid in the breakup. This continues until the tablet has
disintegrated
 Example: Dimetapp ND Orally Disintegrating Tablet
(Non-DrowsyAllergy Tablets)
Using DuraSolv and OraSolv technologies - Tempra
Quicklets: acetaminophen 80 mg, aspartame, citric acid,
D&C Red No.27 Lake, FD&C Blue No.1 Lake, flavor,
magnesium stearate, mannitol, potassium carbonate.

 Another examples: Alavert; NuLev; Remeron SolTabs;

Triaminic Softchews; Zomig Rapidmelt
 Using Flashtab technology: Excedrine QuickTabs
 Using Wowtab technology: by Yamanouchi Pharma -
(click to return) Benadryl Fastmelt
 sometimes called controlled release (CR) tablets
are designed to release their medication is a
predetermined manner over an extended period.

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• also called vaginal inserts, are uncoated bullet-
shaped or ovoid tablets inserted into the
vagina for local effects

•prepared by compression and shaped to fit

snugly on plastic inserter devices

• contain antibacterials for the treatment of

vaginitis caused by Haemophilus vaginalis or
antifungals for the treatment of vulvovaginitis
candidiasis caused by Candida albicans
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Quality Standards and Compendial Requirements
1. Tablet Weight and USP Weight Variation Test
 to yield the desired weight and content
 to have dosage form uniformity by weight variation
 10 tablets are weighed individually and the average weight
calculated and assayed
2. Content Uniformity
 85% to 115% of the label claim and the standard deviation is less
than 6%.
3. Tablet Thickness
 tablet thickness maybe measured by hand gauge during
production or by automated equipment
4. Tablet Hardness and Friability
 are used to measure the degree of force (in kg, pounds, or in arbitrary units
required to break a tablet. A force of about 4 kg is considered the minimum
requirement for a satisfactory tablet
durability - use of a friabilator - determines the tablet’s friability, or tendency
to crumble, by allowing it to roll and fall within the drum
  The tablets are weighed before and after a specified number of rotations and
any weight loss determined
 Resistance to loss of weight indicates the tablet’s ability to withstand abrasions
in handling, packaging and shipment.
 A maximum weight loss of not more than 1% generally is considered
acceptable for most product

5. Tablet Disintegration
.
 tablet disintegrating apparatus = the tablets is placed in each test tubes
of the basket, and through the use of mechanical device, the basket is
raised and lowered in the immersion fluid at 29 to 32 cycles per minute,
the wire screen always below the level of the fluid
disintegration defined = that state in which any residue of the unit,
except fragments of insoluble coating or capsule shell, remaining on the
screen of the test apparatus is a soft mass having no palpably firm core
 tablets must disintegrate within the times set forth in the individual
monograph, usually 30 minutes; but 2 minutes for nitroglycerin up to 4
minutes for buccal tablets
5. Tablet Dissolution
Reasons/Importance
1. It guides formulation and product development toward product optimization
2. Manufacturing may be monitored by dissolution testing as a component of the overall
quality assurance program
3. Consistent in vitro dissolution testing ensures bioequivalence from batch to batch
4. It is a requirement for regulatory approval of marketing for products
registered with the FDA/BFAD

Predicting the likelihood of achieving a successful in vivo-vitro correlation

(IVIVC). Considered are drugs determined to have
1. High solubility and high permeability
2. Low solubility and high permeability
3. High solubility and low permeability
4. Low solubility and low permeability
 D issolution T esting D evices
 Vessels are surrounded by a warm water bath to maintain biologic al
temperature for up to 96 hours
 Stirring rods are used to simulate biological contractions & mix ing
 Ports for monitoring pH, temp
 Dosage form must sit in the bottom of the vessel, if it floats, is must be
fixed to the bottom of the vessel
Weighing and Blending
 mixed the active ingredient, diluent or filler, and disintegrating agent by mechanical
powder blender or mixer until uniform
 Filler = lactose, microcrystalline cellulose, starch, powdered sucrose,
calcium phosphate; the choice is based on experience and compatibility
Example: calcium salts must not be used as fillers with tetracycline antibiotics
because of an interaction between 2 agents that results in reduced tetracycline absorption from GT
Lactose are preferred because of its solubility and compatibility
 Disintegrating agents = croscarmellose, corn and potato starches, sodium starch
glycolate, sodium carboxymethylcellulose, polyvinyl polypyrrolidone (PVP), alginic, etc.
 Croscarmellose (2%) and Sodium starch glycolate (5%) are often used
because of their high water uptake and rapid action; Sodium starch glycolate swell
up to 300% of its volume in water
Preparing the Damp Mass
 a liquid binder is added to the powder mixture to facilitate adhesion of
the powder particles
 a damp mass resembling dough is formed and used to prepare the granulation
 Binding agent= povidone, an aqueous preparation of cornstarch (10-
20%), glucose solution (25-50%), molasses, methyl cellulose (3%),
carboxymethylcellulose and microcrystalline cellulose
care must be exercised not to overwet = too hard for proper tablet
formation; underwetting = too soft and tend to crumble
Screening to damp Mass Into Pellets or Granules
 wet mass is pressed through a screen (usually 6 to 8 mesh) to prepare
the granules. This may be done by hand or with special equipment that
prepares the granules.
Drying the Granulation
 granules may be dried in thermostatically controlled ovens that
constantly record the time, temperature, and humidity.
Sizing the Granulation by Dry Screening
 after drying, the granules are passed through a screen of a smaller
mesh than that used to prepare the original granulation
  size depends on the punches to be used
 the smaller the tablet to be produced, the smaller the granules
 screens of 12 to 20 mesh size are generally used for this purpose
Adding Lubrication and Blending
 after dry screening, a dry lubricant is dusted over the spread-out granulation
through a fine mesh screen
 Lubricants = improve the flow of the granulation in the hopper to the die cavity,
they prevent adhesion to the punches and dies during compression; they reduce
friction between the tablet and the die wall during the ejection of the tablet from the
machine; they give a sheen to the finish tablet
Example of lubricants = magnesium stearate, calcium stearate, stearic acid,
talc, and sodium stearyl fumarate. Magnesium stearate is commonly used. Quantity of
lubricant = ranges from 0.1 to 5% of the weight of the granulation
All -in-One Granulation Methods
 technologic advances now allow the entire process of granulation to be
completed in continuous fluid bed process, using a single piece of equipment, the
fluid bed granulator
Steps of Fluid Bed Granulator
1. Preblending the formulation powder, including active ingredients, filler, disintegrants,
in a bed with fluidized air
2. Granulating the mixture by spraying onto the fluidized powder bed, a
suitable liquid binder, such as an aqueous solution of acacia, hydroxypropyl
cellulose, or povidone
3. Drying the granulated product to the desired moisture content

Another method, Microwave Vacuum processing, also allows the powders to be mixed,
wetted, agglomerated, and dried within the confines of a single piece of equipment.

1. The wet mass is dried by gentle mixing, vacuum, and microwave

2. The use of microwave reduces drying time considerably, of ten by one- fourth.
3. The total batch production time is usually in the range of 90 minutes.
4. After adding lubricants and screening, the batch is ready for tablet
formation or capsule filling
Dry Granulation
Slugging
 after weighing and mixing the ingredients, the powder
mixture is slugged, or compressed into large flat tablets or
pellets about 1 inch in diameter
 the slugs are broken up by hand or by mill and passed
through a screen of desired mesh for sizing
 lubricants is added
 tablets are prepared by compression
 aspirin, which is hydrolyzed on exposure to moisture,
may be prepared into tablets after slugging
Roller Compaction
 instead of slugging, powder compactors may be
used to increase density of a powder by pressing it
between rollers at 1 ton to 6 tons of pressure
 the compacted material is broken up, sized, and
lubricated, and tablets are prepared by compression
 the roller compaction method is often preferred to
slugging
 binder use in these method: methylcellulose or
hydroxymethylcellulose (6-12%), which can produce
good tablet hardness and friability
Tablet Granulation
machines compress a tablet formulation within a steel
die cavity by the pressure exerted by the movement
of two steel punches, a lower punch and an upper
punch
 single punch tablet press describes the basic
mechanical process. As the lower punch drops,
the feed shoe filled with granulation from the hopper
is positioned over and fills the die cavity. The feed shoe
retracts, scrapes away the excessive granulation, and
levels the fill in the die cavity.
 the upper punch lowers and compresses the fill,
forming the tablet
 the upper punch retracts as the lower punch rises
with the formed tablet to the precise level of the
stage
Tablet Granulation
 the feed shoe moves over the die cavity, shoves the tablet
aside, and once again fills the cavity with granulation to
repeat the process.
 the tablet fall into a collection container
 a Rotary tablet machines equipped with multiple punches
and dies operate via continuous rotating movement punches
 a consequences of high speed production is the increased
occurrence of lamination (horizontal striations) and tablet
capping, in which the top of the tablet separates
from the whole because the fill material does not have
enough time to bond after compression. Reduced speed
remedies the problem
Direct Compression Tableting
 some granular chemicals, like potassium chloride, possess free
flowing and cohesive properties that enable them to be
compressed directly in a tablet machine without need of
granulation
lacking this quality - excipients include fillers, disintegrating
agents, lubricants and glidants

Tablet Dedusting

 to remove traces of loose powder adhering to

tablets following compression, tablets are
conveyed directly from the tableting machine to a
deduster. The compressed tablets may then be
coated.
The Non-aqueous Film Coating Generally Contain The Following:
1. A film former capable of producing smooth, thin films reproducible
under conventional coating conditions and applicable to variety of tablet shapes.
Examples: cellulose, acetate phthalate
2. An alloying substance providing water solubility or permeability to the film to ensure
penetration by the body fluids and therapeutic availability of the drug.
Example: polyethylene glycol
3. A plasticizer to produce flexibility and elasticity of the coating and thus provide
durability.
Example: Castor oil
4. A surfactant to enhance spreadability of the film during application.
Example: polyoxyethylene sorbitan derivatives
5. Opaquants and colorants to make the appearance of the coated tablets handsome and
distinctive.
Examples: Opaquant- titanium dioxide, colorant - FD and C or DC
The Non-aqueous Film Coating Generally Contain The
Following:
6. Sweeteners, flavors, and aromas - to enhance the acceptability of the
tablet to the patient.
Examples: sweeteners - saccharin, flavors and aromas - vanillin
7. A glossant - to provide luster to the tablets without a separate polishing
operation.
Example: beeswax
8. A volatile solvent to allow the spread of the other components over the
tablets while allowing rapid evaporation to permit an effective yet
speedy operation
Example: alcoholic acetone mixture, for water based, colloidal
coating dispersion is called AQUACOAT - contains 30% ethyl cellulose
pseudolatex
The Typical Aqueous Film-Coating Formulations
Contains The Following:

1. Film Forming Polymer (7-18%).

Examples: cellulose ether polymers, hydroxypropyl
methylcellulose, hydroxypropylcellulose, and methyl cellulose

2. Plasticizer (0.5 - 2.0%)

Examples: glycerin, propylene glycol, polyethylene glycol, and
dibutyl subacetate

3. Colorant and Opacifier (2.5 - 8%)

Examples: FD and C or D and C

4. Vehicle (100%)
Example: water
 Problems Attendant To Aqueous Film Coating
1. Picking the appearance of small amounts of film fragments flaking from the
tablet surface

2. Peeling the appearance of large amounts of film fragments flaking from the
tablet surface

3. Orange peel effect - roughness of the tablet surface due to failure of spray
droplets to coalesce

4. Mottling - an uneven distribution of color on the tablet surface

5. Bridging - filling - in of the score -line or intended logo on the tablet film

6. Tablet Erosion -disfiguration of the core tablet when subjected for too long a
period of time to the coating solution
 Are tablets with a coating which resists
dissolution or disruption in the stomach but not in
the intestine, thereby allowing for tablet transit
that the stomach in favor of tablet disintegrations
and drug absorption from the intestines.

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 PROCEDURE FOR ENTERIC COATING
 Capsules were automatically weighed and
loaded into the coating chamber through airlock
pinch valves.

Figure 1. Three-dimensional simulated drawing of tablets suspended in the coating chamber of

the Supercell coater during coating.
 PROCEDURE FOR ENTERIC
COATING
 The coating dispersion was delivered
using precision syringe pumps.
 PROCEDURE FOR ENTERIC
COATING
 The capsules were coated and then
discharged using a rapid vacuum
extraction system.
 PROCEDURE FOR ENTERIC
COATING
 Two different batch sizes (15 and 30 g)
and two different sizes (Size 1 and 00) of
capsules were evaluated. For each
capsule and batch size, the capsules were
coated to different theoretical coating
levels (5.0 – 13.0%) weight gain).
 PRINCIPLES OF ENTERIC DRUG
PENETRATION TO THE BODY
 The drugs immediately release a portion into the
stomach while allowing a portion of the drug to
pass into the duodenum wherein the enteric
coating dissolves and the drug is thereby slowly
absorbed by the intestines.
PRINCIPLES OF ENTERIC DRUG
PENETRATION TO THE BODY
 The unprotected portion of the drug rapidly
dissolves in the stomach and that portion of the
drug dose quickly enters the bloodstream.

The enterically coated portion of the drug begins to

dissolve in the small intestine where a
substantial increase in pH occurs to then
controllably release the remainder of the active.
PRINCIPLES OF ENTERIC DRUG
PENETRATION TO THE BODY
 In the intestines, the enteric coating or
membrane dissolves or disperses in the
intestinal fluid. Depending upon the relatively pH
solubility of the active agent, the percentage of
total active inside or outside of the enteric
coating can be adjusted so that excess plasma
drug concentrations are minimized and steady
long-term release of the drug is maximized.
This technique is employed in instances in which the drug
substance is:
1. Destroyed to the gastric acid
2. Is irritating to the gastric mucosa
3. When by passing the stomach enhances drug absorption from
the intestines to a significant extent
Fluid - Bed or Air Suspension Coating
This process involves the spray coating of pellets, beads,
granules, powders, or tablets held in suspensions by a column
of air.
3 Types:
1. Top spray
2. Bottom spray
3. Tangential spray technique - used in rotary fluid-bed
coaters.
                                                                                                  
                                                                                                
                                                                             
Principle: Principle: Principle:
Batch fluid bed Batch fluid bed Batch fluid bed
coating Top Spray coating Bottom coating Tangential
Spray Spray
(Wurster coating) (Rotor pellet
coating)
 Compression Coating
Similar to the preparation of multiple
compressed tablets having an inner core and
an outer shell of drug material, core tablets
maybe sugar coated by compression.
 Gelatin Coated Tablets
A recent innovation called GELCAPS,
the innovator product is a gelatin-coated
capsule shaped tablet. Compared to dry-
filled, unsealed capsules, GELCAPS are
more tamper-resistant and tamper-
evident.
 Are generally flat, oval tablets intended to be dissolved in the buccal
pouch (buccal tablet - side of cheek or between lips and gums) or beneath
the tongue (sublingual tablet) for absorption through the oral mucosa.
USE: provides for the absorption of the drugs that are destroyed by gastric
juice and/or poorly absorbed from GIT.

Characteristics: buccal administration (a progesterone tablet) are prepared to

erode or to dissolved slowly while those for sublingual use (nitroglycerin tablet)
dissolved very promptly to give rapid drug effects.

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 Are compressed tablets which have a smooth, rapid
disintegration when chewed or allowed to dissolve in the mouth
and contains a creamy base of a specially flavored and colored
mannitol.
These are useful in formulations for children -
multivitamins tablets and for adults - antacids and
antibiotics.
Prepared by wet granulation and compression
Example Of Typical Chewable Antacid

Aluminum hydroxide 325.0 mg

Mannitol 812.0 mg
Sodium saccharin 0.4 mg
Sorbitol (10% w/v solution) 32.5 mg
Magnesium stearate 35.0 mg
Mint flavor concentrate 4.0 mg

Preparation:

(1) Blend the aluminum hydroxide, mannitol, and sodium saccharin.

(2) Prepare a wet granulation with sorbitol solution.

(3) Dry at 120 0C and screen through a 12 mesh screen.

(4) Add the flavor and magnesium stearate, blend, and compress into
tablets.
  prepared by wet granulation and compression
 do not contain disintegrants - chew the tablets
thoroughly and not swallow them whole.
 Mannitol is used excipient in most chewable tablet;
70% as sweet as sucrose, with a cool feel in the mouth,
accounts 50% or more of the weight of many chewable
tablet formulations
 other sweetening agents = sorbitol, lactose, dextrose,
crystalline maltose, and glucose, may be substituted for
apart or all of the mannitol.
 Xylitol may be used in the preparation of sugar-free
chewable tablets. Xylitol is sweeter than mannitol.

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CHEWABLE TABLET
lubricant and binders must not affect the texture or
desired hardness of the tablet
 colorant and tart or fruity flavorants are commonly
employed to enhance the appeal of the tablets
 Examples of chewable tablets: Calcium carbonate
- antacids; Erythromycin - antibiotics; Didanosine -
anti-infectives; Carbamazepine - anticonvulsants;
Isosorbide dinitrate - vasodilator; Acetaminophen -
analgesics; various vitamins and cold-allergy
combination tablet
• certain tablets, such as tablet triturates, may be prepared by
molding
• the resultant tablets are very soft and soluble and are designed for rapid
dissolution
• original fast-dissolving tablets were molded tablets for sublingual use.
• they generally consisted of active drug and lactose moistened with alcohol-
water mixture to form a paste, then molded, dried and packaged
example: nitroglycerin - placed under the tongue -to provide
rapid onset of action
example: testosterone - destroyed in the GT - administered
sublingually for absorption to minimize the first-pass effect.
MOLDED TABLETS
 commercial preparation of tablets by molding has been
replaced by tablet compression
 molded or tablet triturate still prepared on a small laboratory
scale
Procedure:
1. The mold is made of hard rubber, hard plastic, or metal
2. It has 2 parts, the upper part or die portion, and the lower part,
containing squat, flat punches
3. The die portion is a flat plate the thickness of the tablets to be
produced with 50 to 200 uniformly drilled and evenly spaced circular
holes
4. The lower part of the mold has corresponding punches that fit the
holes precisely
5. When the die is filled with material and placed atop the punches,
the punches, gently lift the fill material from the holes to rest upon the
punches for drying
@ the base for molded tablets is generally a mixture of finely
powdered lactose with or without a portion of powdered sucrose (5-
20%). The addition of sucrose results in less brittle tablets
@ In preparing the fill, the moisture is wetted with a 50%
mixture of water and alcohol sufficient only to dampen the
powder so that may be compacted; water= binds the powder mixture
upon drying; alcohol = hastens drying
6. The upper mold is placed on a clean flat glass surface and the damp
mass added by a rubbing motion. When each opening is filled
completely and smoothed, top and bottom, the mold is fitted on the
punch portion of the mold and pressed down, leaving the tablets raised
on the pegs to dry.
TABLET COATING
REASONS:
1. Protect the medicinal agents against destructive exposure to air or humidity
2. To provide special characteristics of drug release ( enteric coatings )
3. To provide aesthetics or distinction to the product
4. To prevent inadvertent contact with the drug substance and the effects of drug
absorption

Example: Proscar tablets (finasteride) are coated for just this

reasons. For treatment of benign prostatic hyperplasia
Instruction: women who pregnant or may become pregnant should
not come into contact with it. Drug contact can occur through handling broken
tablets. If finasteride is absorbed by woman who is pregnant with a male baby, the
drug has the potential to adversely affect the developing male fetus
Sugar Coating Tablets
1. Waterproofing and Sealing Coats
 components are affected by moisture - waterproofing substance is applied
( shellac or a polymer); then subcoating of the tablet
 waterproofing solution ( usually alcoholic ) is gently poured or sprayed on the
compressed tablets rotating in the coating pans
 warm air is blown into the pan during the coating to hasten the drying and to
prevent tablets from sticking together
2. Subcoating
 after the tablets are waterproofed if needed, 3 to 5 subcoats of sugar-based syrup
are applied
 This bonds the sugar coating to the tablet and provides rounding
 the sucrose and water syrup also contains gelatin, acacia or polyvinylpyrrolidone
(PVP) to enhance coating
 when the tablets are partially dry, they are sprinkled with a dusting powder,
( mixture of powdered sugar and starch but sometimes talc, acacia or precipitated
chalk )
 warm air is applied to the rolling tablets, then dry, the process is repeated until
desired shapes size is obtained.
3. Smoothing and Final Rounding
 after the tablets are subcoated, 5 to 10 additional coatings of a thick syrup are applied to
complete the rounding and smooth the coating
this syrup is sucrose based, with or without additional components such as starch and
calcium carbonate.
 as the syrup is applied, the operator moves his or her hand through the rolling tablets to
distribute the syrup and to prevent the tablets from sticking to one another
 a dusting powder is often used between syrup applications
 warm air is applied to hasten the drying time of each coat

4. Finishing and Coloring

 to attain final smoothness and the appropriate color to the tablets, several coats of thin
syrup containing the desired colorant are applied in the usual manner.
 this step is performed in a clean pan, free from previous coating materials

5. Imprinting
 to impart identification codes and other distinctive symbols
radiopharmaceuticals, other products because of their size, shape, texture, make imprinting
technologically not feasible.
6. Polishing
coated tablets may be polished in several ways

a. Special drum-shaped pans or ordinary coatings pans lined with canvas or other cloth
impregnated with carnauba wax or beeswax, may be used to polish as they tumble in the
pan
b. Pieces of wax may be placed in a polishing pan and the tablets allowed to tumble over
the wax until the desired sheen is attained.
C. Light spraying of the tablets with wax dissolved in a nonaqueous solvent
 two or three coats of wax may be applied, depending upon the desired gloss
 after each coat has been applied, the addition of a small amount of talc to the
tumbling tablets contributes to their high luster
Example: Coated, polished, and monogrammed tablets = Premarin
0.625 and 1.25 mg

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 Are small, usually cylindrical molded MTT or
compressed CTT tablets containing small amounts of
usually potent drugs.

Characteristics:
1. Must be readily and completely soluble in water,
thus when prepared by compression a minimal
amount of pressure is exerted.
2. The diluent is usually a combination of sucrose
and lactose avoiding any water-insoluble
material.
USES:
1. Used for oral administration of drugs and some
sublingual.
2. Used in compounding procedures in the
preparation of other solid or liquid dosage forms.
Example: The tablet may easily inserted into
capsules to provide accurate amounts of potent
drugs
3. Use to fortify liquid preparations as prescribed
by dissolving the appropriate number of
tablets in a small portion of water the
bringing the preparation to the required volume
with the liquid being fortified.
 Are tablets triturates for use by the
physician in his extemporaneous preparation of
parenteral administration.

(click to return)
 Also called “controlled release, sustained
release, prolong release, timed release, slow
release, sustained action, prolong action,
extended action, and rate controlled” tablets or
capsules

 are solid dosage forms designed to release

the drug slowly for more prolonged drug
release and sustained action.
Characteristics:
1. Exhibit neither very slow nor very fast rates of absorption
and excretion.
2. Uniformly absorbed from the GIT.
3. Administered in relatively small doses.
4. They possess good margin of safety.
5. Used in the treatment of chronic rather than acute
conditions.

Packaging and Storage: Stored in tight containers

in places of low humidity and protect from extreme
temperature. Packed with dessicant to avoid
decomposition by moisture and packaged in light resistant
containers.
 METHODS OF PREPARATIONS
1. Dry methods
a. Direct Compression
b. Granulation by compression
2. Wet methods
a. Wet granulation
b. Special procedures/related
granulation processes
Dry Granulation Method
1. Weighing of ingredients
2. Mixing of ingredients in suitable mixer blender
3. Slugging by using flat face punches 7/8 to 1 inch
diameter
4. Dry screening of slugs through a mesh screen (by
hand) or through a Fitzpatrick comminuting mill
5. Lubrication through a suitable blender
6. Compression into final tablets
Note: Slugging has the advantage of utilizing less
equipment and space than wet granulating, no binder
solution and subsequent drying
 DRUG ADJUVANT

BLEND
GRIND

PELLET

COMPRESS
LUBRICANT CRUSH

TABLET

BLEND

SCREEN
Tablet Granulations
Granulation is the pharmaceutical process that
attempts to convert powdered materials into
aggregates called “granules”.
Granules Must Possess:
1. Fluidity: the property necessary for the
transport of material through the hopper into
the feed frame
2. Compressibility: the property of forming a
stable compact mass when pressure is applied
Accordingly, a good tablet granulation should:
1. Contain particles which approach spherical shape.
2. Present a range of particle size that resembles a normal
distribution curve, with a small percentage of coarse and
fine particles and with the rest in a narrow range between.
3. Have a uniform distribution of all the ingredients in
the formulation.
4. Possess compressible components that will confer
physical strength and form to the tablet.
 Tablet Granulation
 The mixture is then
placed on the lower
punch.
 The upper punch then
compress the tablet at
the same time taking out
the air.
WET METHOD
Is the most widely used. The general method
of preparing tablet granulation that will satisfy the
physical requirements for the compression of good
tablets.
Disadvantages:
1. It involves several steps (separate)
2. Requires longer processing time
3. Labor cost is high
Steps Of Wet Method
1. Weighing of the ingredients
2. Mixing them in a suitable mixer or blender
3. Granulation into a damp mass by the addition of a
binding solution
4. Screening the mass by forcing through a 6 to 8 mesh
screen
5. Drying in suitable ovens or fluid bed dryers
6. Dry screening through smaller mesh screen
7. Lubrication in a suitable blender
8. Compression into final tablets
 DRUG ADJUVANT LIQUIDID
IDS

BLEND AGGLOMERATE
GRIND

LUBRICAN
PELLET
T

COMPRESS

TABLET BLEND

SCREEN
DRY
Processing Problems

1. Chipping - the separation of a small piece

of tablet surface after ejection
2. Capping - the partial or complete separation of
the top or bottom of a tablet from the main body
3. Lamination - the separation of a tablet into
one or more distinctive layer
 Factors that may cause splitting of tablets
1. Excess “fine” or powder which entraps air in the tablet mixture
2. Deep markings on tablet punches. Many designs or “scores” on
punches are too broad and deep.
3. Worn and imperfect punches. Punches should be smooth and buffed.
4. Worn dies. Dies should be replaced or reversed.
5. Too much pressure on the machine
6. Unsuitable formula
7. Moist and soft granulation. It will not flow into the dies, thus giving
uneven weight and soft or capped tablets
8. Poorly machined punches.
Picking and Sticking
Picking describes the removal of material from the
surface of the tablet and its adherence to the face of the
punch. (same as chipping). The main difference is that
it occurs before the ejection of tablets.
Sticking describes the adhesion of granulation to
the die wall.

REMEDIES:
1. Design lettering as large as possible, particularly on
punches with small diameters
2. Reformulate to produce a larger tablets
REMEDIES
3. Plate the punch faces with chromium to produce smooth,
non adherent face
4. Add a polishing agent such as colloidal silica
5. Add more binder or change the binder to make granules
more cohesive
6. Dilution of low melting active ingredients/additives
7. Refrigeration of the press and granulation containing high
concentration of low melting medicament.(e.g. stearic acid and
polyethylene glycols) with high melting materials will prevent
softening of the granules due to heat of compression and
many increase tablet size
8. Re-dry the granulation
Reasons Of Coating Tablets
1. To mask unpleasant taste
2. To improve appearance
3. To separate reactive ingredients
4. Protect components from atmospheric degradation
5. Control drug release
6. Surface modification
7. Sustained action
8. Prevent contact with the drug which is
irritating/allergies
Tablet Coatings Are Classified Into Four
1. Sugar coating
2. Film coating
3. Compression
4. Other new concepts
a. Pan coating
b. Air suspension coating
c. Dip coating
d. Tablet compression coating
Processes used in the application of coatings

Pan coating - This process in both sugar and film coating. It makes use of coating pans
provided with a hot and cold air input system and exhaust system to remove
moisture and fine powder generated during the coating operation.
Air Suspension Coating - This process has become one of the most
dependable methods for applying film coats. The coating is atomized and
applied to tablets as they are suspended inside the columnar coating and applied to
means of a stream of hot air
Dip Coating - Materials to be coated are usually placed in baskets and
dipped into containers of coating solutions. The wet tablets are then agitated or tumbled
in coating pans during drying to prevent adherence to each other. The process is repeated
a number of times after each coat is sufficient dry.
Compression Coating - Compression coating makes possible some special dosage forms.
Two incompatible drugs may be separated by placing one in the core,
the other in the coating.
Subcoatings Are Either
1. Debossed - imprinted with a mark below the dosage
form surface
2. Embossed - raised above the surface of the dosage
form
3. Engraved - imprinted with a code that is cut into the
dosage form surface after it has fabricated
Evaluation Of Tablets
1. Hardness - mechanical hardness (Strong cobb tester,
Stokes Monsato)
2. Dissolution rate -knowing the length of time by
which the tablet has dissolved in the media
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 EVALUATION OF TABLETS
3. Friability - is tested by a Roche Friabilator which
induces shock and friction of the tablet
4. Disintegration time - to assure product uniformity; 5-
30 minutes is required for disintegration time
5. Weight variation - 130 mg or less - 10 %; 130- 134 mg
- 4.5% ; 324 over - 5% allowances
6. Thickness - micrometer caliper; determination of
length and width
7. Content uniformity - to detect homogeneity of the
distribution of the drug content
Examples Of Some Official Tablets
Official Tablet Commercial Tablet Strengths Category
Products usually available
Acetaminophen Tylenol 325 mg Analgesic and antipyretic
Allopurinol Zyloprim 100, 300 mgAntigout, antiurolithic
Amitriptyline HCl Elavil HCl 10,25,50,100, Antidepressant
150 mg
Bisacodyl Dulcolax 5 mg Cathartic; E. Coated
Carbamazepine Tegretol 200 mg Anticonvulsanr
Chlorambucil Leukeran 2 mg Antineoplastic
Chlorpheniramine Chlor-Trimeton 4,8, and 12 mg Antihistamine;
maleate maleate controlled release
Chlorpropamide Diabinese 100, 250 mgAntidiabetic
Cimetidine Tagamet 200, 300 mgHistamine H2 receptor
antagonist
Diazepam Valium 2,5,10 mg Sedative; skeletal
muscle relaxant
Digoxin Lanoxin 0.125, 0.25, 0.5 Cardiotonic
Examples Of Some Official Tablets
Official Tablet Commercial Tablet Strengths Category
Products usually available
Dimenhydrinate Dramamine 50 mg Antinauseant
25, 30 mg Bronchodilator
Vasoconstrictor
Furosemide Lasix 20,40, 80 mg Diuretic;
antihypertensive
GriseofulvinFulvicin U/F 250,500 mg Antifungal
Haloperidol Haldol 0.5,1,2,5,10,20 Tranquilizers
Hydrochlorothiazide Hydro-Diuril 25,50,100 mg Diuretic,
antihypertensive
Ibuprofen Motrin 300,400,600, Analgesic,
800 mg Antipyretic
Levodopa Larodopa 100,250,500 Antidyskinetic
Meclizine HCl Antivert 12.5, 25,50 Antivertigo
Meperidine HCl Demerol 50 and 100 mg Narcotic analgesic
Meprobamate Equanil 200, 400 mgSedative,hypnotic
Methyldopa Aldomet 125,250,500 Antihypertensive
Examples Of Some Official Tablets
Official Tablet Commercial Tablet Strengths Category
Products usually available
Metronidazole Flagyl 250, 500 mgAntiamebic,
antitrichomonal
Nitroglycerin Nitrostat 0.150,0.30,0.4,0.6 Anti-anginal
Penicillin V Pen Vee 250, 500 mgAntibacterial
Potassium
Prednisone Deltasone 1 mg Adrenocorticoid
Prochlorperazine Compazine 5,10,25 mg Antiemetic
Maleate
Propanolol Inderal 10,20,40,60,80 Antianginal;
HCl 90 mg Antiarrhythmic
Antihypertensive
Sulindac Clinoril 150 and 200 mg Antirheumatic
Antiinflammatory
Terbutaline sulfate Brethine 2.5 and 5 mg Antiasthmatic
Tolbutamide Orinase 250 and 500 mg Antidiabetic
Warfarin Coumadin 2, 2.5, 7.5, 10 Anticoagulant (click to return)
 Are small round dosage forms containing a medicinal agent and intended to be
administered orally. Pills may be coated or uncoated

Today pills have largely replaced by compressed tablets and capsules.

Example: Hexylresorcinol pills NF – as antihelmintic.

.
 Characteristics:
1. Adhesiveness - retain shape
2. Firmness to retain shape; hold its shape when molded into
pills
3. Plasticity - capable of being worked upon but not sticky
enough to our hand, tools or mixing machine
4. Disintegration - disintegrates readily in gastric or
intestinal fluids
TYPES:
1. Compressed Pills
2. Dispensing Pills
Four Classes Of Pills According To Weight
1. Parvules - potent substance with coloring agent,
small pills; 20 mg- less
2. Granules - it contain sugar; 20 mg to 60 mg
3. Pills - comes in variety of sizes, shapes, coatings
and colors; 60-500 mg
4. Boluses - for veterinary use; big pills; 700 to
2000 mg
 OTHER SOLID DOSAGE FORMS

1. Lozenges/ Pastilles or Troches - Are

disk-shaped, solid dosage forms containing a medicinal
agent and generally a flavoring substances and
intended to be slowly dissolved n the oral cavity or localized
effects.
Examples: Cepachol, Strepsils, Fisherman’s
Friend, Dequadin
Classification Of Ingredients
1. Active ingredient - antiseptic, local anesthetics,
antibiotic
2. Flavored base - hard sugar candy, glycerinated
gelatin
Methods Of Preparation
1. Compression - for heat labile active ingredients
2. Hard candy base - for heat labile stable active
drug
 2. Cachets or Konseal or Wafer
Capsules –
are related to capsules, in as much as they provide an
edible container for the oral administration of solid
drugs, cachets were formerly used in pharmacy. They
vary in size, from 3/4 to 1/8 of an inch in diameter
and consisted of 2 concave pieces of wafer made of
flour and water.

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3. Pellets or Inserts –
are small, sterile cylinders about 3.2 mm in diameter
by 8 mm in length which are formed by
compression from medicated masses. They are
used by implantation.
Examples: Testosterone, estradiol, ordesoxycorticosterone
pellet desired for prolonged and continuous
absorption. Norplat (Wyeth-Ayers)
4. Vaginal or Inserts –
are specially formulated and shaped tablets
intended to be placed in the vagina by special
applicators, where the medication is released,
generally for localized effects
5. Lollipops - Fentanyl Actiq - is a
raspberry lollipop that differs from Fentanyl
Oralet. It is a sugar-base lozenge on a stick
and contains fentanyl citrate . Actiq is the
first product designed to aid in controlling
breakthrough pain in cancer