TABLET

DOSAGE FORM
Pharmaceutics II-B (Dosage form sciences)
 TABLETS INTRODUCTION
 Tablets are solid dosage forms usually prepared with the aid of suitable pharmaceutical excipients. They may
vary in size, shape, weight, hardness, thickness, disintegration, and dissolution characteristics and in other
aspects, depending on their intended use and method of manufacture. Most tablets are used in the oral
administration of drugs. Many of these are prepared with colorants and coatings of various types. Other
tablets, such as those administered sublingually, buccally, or vaginally, are prepared to have features most
applicable to their particular route of administration.
 Tablets are prepared primarily by compression, with a limited number prepared by molding. Compressed
tablets are manufactured with tablet machines capable of exerting great pressure in compacting the powdered
or granulated material. Their shape and dimensions are determined by the use of various shaped punches and
dies . Molded tablets are prepared on a large scale by tablet machinery or on a small scale by manually
forcing dampened powder material into a mold from which the formed tablet is then ejected and allowed to
dry.
 TABLETS INTRODUCTION
 Some tablets are scored, or grooved, which allows them to be easily broken
into two or more parts. This enables the patient to swallow smaller portions
as may be desired, or when prescribed, it allows the tablet to be taken in
reduced or divided dosage. Some tablets that are not scored are not intended
to be broken or cut by the patient since they may have special coatings
and/or drug-release features that would be compromised by altering the
tablet’s physical integrity.
 TYPES OF TABLETS
1. COMPRESSED TABLETS: The physical features of compressed tablets are well known such as they
may be round, oblong or unique in shape, thick, thin, large or small in diameter, flat or convex, unscored
or scored in halves, engraved or imprinted with an identifying symbol or code number, coated or
uncoated, colored or uncolored, one, two or three layer. Tablet diameter and shapes are determined by the
dies and punches used in compression. Monograms may be placed on one or both sides of a tablet
depending on the punches.
2. Multiply compressed tablets:
Multiply compressed tablets are prepared by subjecting the fill material to more than a single
compression. The result may be a multiple-layer tablet or a tablet within a tablet, the inner tablet being the
core and the outer portion being the shell. 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 two-layered or three layered
tablets, depending on the number of separate fills. Each layer may contain a different medicinal agent,
separated for reasons of chemical or physical incompatibility, staged drug release, or simply for the unique
appearance of the layered tablet. E.g Norgesic tablets like Orphenadrine, Paracetamol.
 TYPES OF TABLETS
3. Sugar coated tablets:
Compressed tablets may be coated with a colored or an uncolored sugar layer. The coating is water soluble
and quickly dissolves after swallowing. The sugarcoat protects the enclosed drug from the environment and
provides a barrier to objectionable taste or odor. The sugarcoat also enhances the appearance of the
compressed tablet and permits imprinting of identifying manufacturer’s information. Among the
disadvantages to sugarcoating tablets are the time and expertise required in the coating process and the
increase in size, weight, and shipping costs. Sugarcoating may add 50% to the weight and bulk of the
uncoated tablet.
4. Film coated tablets:
Film-coated tablets are compressed tablets coated with a thin layer of a polymer capable of forming a skin
like film. The fi lm is usually colored and has the advantage over sugar coatings in that it is more durable,
less bulky, and less time consuming to apply. By its composition, the coating is designed to rupture and
expose the core tablet at the desired location in the gastrointestinal tract.
 TYPES OF TABLETS
5. Gelatin coated tablets:
A recent innovation is the gelatin-coated tablet. The innovator product, the gelcap, is a capsule shaped
compressed tablet. The gelatin coating facilitates swallowing, and gelatin-coated tablets are more tamper
evident than unsealed capsules. Examples include Extra Strength Tylenol PM Gelcaps.

6. Enteric coated tablets:

Enteric-coated tablets have delayed-release features. They are designed to pass unchanged through the
stomach to the intestines, where the tablets disintegrate and allow drug dissolution and absorption and/or
effect. Enteric coatings are employed when the drug substance is destroyed by gastric acid or is particularly
irritating to the gastric mucosa. Examples include Ecotrin Tablets and Caplets.
 TYPES OF TABLETS

7. Buccal and sublingual tablets:

Buccal and sublingual tablets are flat, oval tablets intended to be dissolved in the buccal pouch (buccal
tablets) or beneath the tongue (sublingual tablets) for absorption through the oral mucosa. They enable oral
absorption of drugs that are destroyed by the gastric juice and/or are poorly absorbed from the gastrointestinal
tract. Buccal tablets are designed to erode slowly, whereas those for sublingual use (such as nitroglycerin)
dissolve promptly and provide rapid drug effects. Lozenges or troches are disc-shaped solid dosage forms
containing a medicinal agent and generally a flavoring substance in a hard candy or sugar base. They are
intended to be slowly dissolved in the oral cavity, usually for local effects, although some are formulated for
systemic absorption. An example would be Mycelex Troches.
 TYPES OF TABLETS

8. Chewable tablets:
Chewable tablets, which have a smooth, rapid disintegration when chewed or allowed to dissolve in the
mouth, have a creamy base, usually of specially flavored and colored mannitol. Chewable tablets are
especially useful for administration of large tablets to children and adults who have difficulty swallowing
solid dosage forms. Examples include Pepcid Chewable Tablets and Rolaids Chewable Tablets.

9. Effervescent tablets:
Effervescent tablets are prepared by compressing granular effervescent salts that release gas when in
contact with water. These tablets generally contain medicinal substances that dissolve rapidly when added to
water. The “bubble action” can assist in breaking up the tablets and enhancing the dissolution of the active
drug. Examples include Alka-Seltzer Original and Extra-Strength Tablets (Bayer) and Zantac EFFER
dose.
 TYPES OF TABLETS
10. Hypodermic tablets:
Hypodermic tablets are no longer available in the United States. They were originally used by
physicians in extemporaneous preparation of parenteral solutions. The required number of tablets was
dissolved in a suitable vehicle, sterility attained, and the injection performed. The tablets were a
convenience, since they could be easily carried in the physician’s medicine bag and injections prepared to
meet the needs of the individual patients. However, the difficulty in achieving sterility and the availability
of prefabricated injectable products, some in disposable syringes, have eliminated the need for hypodermic
tablets.
11. Immediate release tablets:
Immediate-release tablets are designed to disintegrate and release their medication with no special rate-
controlling features, such as special coatings and other techniques.
 TYPES OF TABLETS
12. Extended release tablets:
Extended-release tablets (sometimes called controlled-release tablets) are designed to release their
medication in a predetermined manner. E.g Venlafaxine.

13. Vaginal tablets:

Vaginal tablets, also called vaginal inserts, are uncoated, bullet-shaped or ovoid tablets inserted into the
vagina for local effects. They are prepared by compression and shaped to fi t snugly on plastic inserter
devices that accompany the product. They contain antibacterials for the treatment of nonspecific vaginitis
caused by Haemophilus vaginalis or antifungals for the treatment of vulvovaginitis candidiasis caused by
Candida albicans and related species.
 EXCIPIENTS USED IN TABLET FORMULATION
In addition to the medicinal agent or agents, compressed tablets usually contain a number of pharmaceutical
adjuncts, including the following:
 Diluents or fillers: Diluents or fillers, which add the necessary bulk to a formulation to prepare tablets of
the desired size. E.g, starch.
 Binders or Adhesive: Binders or adhesives, which promote adhesion of the particles of the formulation,
allowing a granulation to be prepared and maintaining the integrity of the final tablet. These agents
provide cohesive strength to the particles e.g, gelatin, Lactose, cellulose derivatives such as methyl
cellulose, ethyl cellulose, Hydroxypropyl methyl cellulose, Hydroxypropyl starch, Polyvinyl
pyrrolidone (Povidone), Sodium Alginate, Acacia e.t.c
Lubricants: Lubricants are used to reduce the friction between the die wall and tablet, prevent the
adhesion of tablet material to dies and punches and they also help in the easy ejection of tablets from the
die cavity. Some of the examples include insoluble stearic acid, Magnesium stearate, Calcium
stearate, Talc, Paraffin, Sodium Lauryl sulphate, Sodium Benzoate e.t.c.
 EXCIPIENTS USED IN TABLET
FORMULATION
Lubricants are classified into two types:
1. Glidents
2. Anti-adherents

Glidents: It helps in the free flowing of granules from hopper to die cavity. They also minimize the friction
between the particles e.g, Mg stearate, colloidal silicone dioxide (Aerosil), Corn starch., Talc e.t.c.

Antiadherents: These are added to prevent the adhesion of tablet material to punches and dies e.g Talc.
 EXCIPIENTS USED IN TABLET FORMULATION
 Disintegrants or disintegrating agents: These promote breakup of the tablets after
administration to smaller particles for ready drug availability. Some of examples include
starch, Sodium Carboxy methyl cellulose, Cros carmellose.
 Super disintegrants: These agents are added so when they come in contact with water
or fluids in the oral cavity/ gastrointestinal tract breakdown into smaller particles very
quickly. Some of the examples include Cros Povidone (polyplasdone), Sodium starch
glycolate, Cros carmellose Sodium e.t.c.
 COMPRESSED TABLET MANUFACTURING
Compressed tablets may be made by three basic methods:
1. Wet granulation method
2. Dry granulation method
3. Direct compression method

Most powdered medicinal agents require addition of excipients such as diluents, binders, disintegrants, and
lubricants to provide the desired characteristics for tablet manufacture and efficacious use. One important
requirement in tablet manufacture is that the drug mixture flows freely from the hopper of the tablet press into
the dies to enable high-speed compression of the powder mix into tablets. Granulations of powders provide
this free flow. Granulations also increase material density, improving powder compressibility during tablet
formation.
 COMPRESSED TABLET MANUFACTURING

1. Wet granulation method:

Wet granulation is a widely employed method for the production of compressed tablets. The steps
required in this method are:
 Weighing and blending: Specified quantities of active ingredient, diluent or filler, and disintegrating
agent are initially weight and then brought to the granulation section where they are mixed by mechanical
powder blender or mixer until uniform.
Fillers include lactose, microcrystalline cellulose, starch, powdered sucrose, and calcium phosphate. The
choice of filler usually is based on the experience of the manufacturer with the material, its relative cost,
and its compatibility with the other formulation ingredients.
Disintegrating agents include croscarmellose, corn and potato starches, sodium starch glycolate, sodium
carboxymethylcellulose, polyvinylpyrrolidone (PVP), crospovidone, alginic acid, and other materials that
swell or expand on exposure to moisture and effect the rupture or breakup of the tablet in the
gastrointestinal tract.
 COMPRESSED TABLET MANUFACTURING
 Preparing the damp mass:

A liquid binder is added to the powder mixture to facilitate adhesion of the powder particles. Either a
dampened powder formed into granules or a damp mass resembling dough is formed and used to prepare the
granulation. A good binder results in appropriate tablet hardness and does not hinder the release of the drug
from the tablet.
Among binding agents are solutions of Povidone, an aqueous preparation of cornstarch (10% to 20%),
glucose solution (25% to 50%), methylcellulose (3%) etc.
The binding agent contributes to adhesion of the granules to one another and maintains the integrity of the
tablet after compression. However, care must be exercised not to overwet or underwet the powder.
Overwetting can result in granules that are too hard for proper tablet formation, and underwetting can result
in tablets that are too soft and tend to crumble. When desired, a colorant or flavorant may be added to the
binding agent to prepare a granulation with an added feature.
 COMPRESSED TABLET MANUFACTURING

 Screening the damp mass into pellets or granules:

The dampened powder granules are screened, or the wet mass is pressed through a screen (usually 6 or 8
meshes) to prepare the granules. This may be done by hand or with special equipment that prepares the
granules by extrusion through perforations in the apparatus. The resultant granules are spread evenly on large
lined trays and dried to consistent weight or constant moisture content.
 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. The degree to which the granules are reduced depends on the size of the punches to be
used. In general, the smaller the tablet to be produced, the smaller the granules. Screens of 12- to 20-mesh
size are generally used for this purpose. Sizing of the granules is necessary so that the die cavities for tablet
compression may be completely and rapidly filled by the free-flowing granulation. Voids or air spaces left by
too large a granulation result in the production of uneven tablets.
 COMPRESSED TABLET MANUFACTURING
 Adding lubrication and blending:

After dry screening, a dry lubricant is dusted over the spread-out granulation through a fine-mesh screen.
Lubricants contribute to the preparation of compressed tablets in several ways:
i. They improve the flow of the granulation in the hopper to the die cavity
ii. They prevent adhesion of the tablet formulation to the punches and dies during compression.
iii. They reduce friction between the tablet and the die wall during the ejection of the tablet from the
machine.
Among the more commonly used lubricants are magnesium stearate, calcium stearate, stearic acid, talc, and
sodium stearyl fumarate. Magnesium stearate is most used. The quantity of lubricant used varies from one
operation to another but usually ranges from about 0.1% to 5% of the weight of the granulation.
 COMPRESSED TABLET MANUFACTURING

2. Dry granulation method:

By the dry granulation method, the powder mixture is compacted in large pieces and subsequently broken down or sized
into granules. For this method, either the active ingredient or the diluent must have cohesive properties. Dry granulation
is especially applicable to materials that cannot be prepared by wet granulation because they degrade in moisture or the
elevated temperatures required for drying the granules. Steps are following:
 Weighing and blending: In the first step specified quantities of the active ingredient and excipients are
accurately weight and subject to blending in a specified blender for specified period of time.
 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 a mill/granulator and passed through a screen of desired
mesh for sizing. Lubricant is added in the usual manner, and tablets are prepared by compression. Aspirin, which is
hydrolyzed on exposure to moisture, may be prepared into tablets after slugging.
 COMPRESSED TABLET MANUFACTURING

3. Direct compression method:

Some granular chemicals, like potassium chloride, possess free-flowing and cohesive properties that enable
them to be compressed directly in a tablet machine without any need of granulation. For chemicals lacking
this quality, special pharmaceutical excipients may be used to impart the necessary qualities for the production
of tablets by direct compression. These excipients include fillers, such as spray-dried lactose, microcrystals of
alpha-monohydrate lactose, sucrose–invert sugar–corn starch mixtures, microcrystalline cellulose, crystalline
maltose, and dicalcium phosphate; disintegrating agents, such as direct compression starch, sodium
carboxymethyl starch, cross-linked carboxymethylcellulose fibers, and cross-linked polyvinylpyrrolidone;
lubricants, such as magnesium stearate and talc; and glidants, such as fumed silicon dioxide.