Tablets

Solid medicaments may be administered orally as powders, pills, sachets, capsules or tablets.
These dosage forms contain a quantity of drug which is given as a single unit and they are known
collectively as solid unit dosage forms, even in the case of sustained action, preparations which,
technically, contain the equivalent of several normal doses of drug. The stringent formulation
requirements of modern medicaments, the many advantages of tablet and capsule medication,
coupled with expanding health services and the commitment need for large‐scale economic
manufacture, have led to a steady decline in the prescribing of powders and pills. Tablets and
capsules, on the other hand, currently account for well over two third of the total number and cost
of medicines produced all over the world.
Tablet is defined as a compressed solid dosage form containing medicaments with or without
excipients. According to the Indian Pharmacopoeia, Pharmaceutical tablets are solid, flat or
biconvex dishes, unit dosage form, prepared by compressing a drugs or a mixture of drugs, with or
without diluents. They vary in shape and differ greatly in size and weight, depending on amount
of medicinal substances and the intended mode of administration.
It is the most popular dosage form and 70% of the total medicines are dispensed in the form of
Tablet. All medicaments are available in the Tablet form except where it is difficult to
formulate or administer.
The advantages of the Tablet dosage form are:
1. They are unit dosage form and offer the greatest capabilities of all oral dosage form for the
greatest dose precision and the least content variability.
2. Cost is lowest of all oral dosage form.
3. Lighter and compact.
4. Easiest and cheapest to package and strip.
5. Easy to swallowing with least tendency for hang‐up.
6. Sustained release product is possible by enteric coating.
7. Objectionable odor and bitter taste can be masked by coating technique.
8. Suitable for large scale production.
9. Greatest chemical and microbial stability over all oral dosage form.
10. Product identification is easy and rapid, requiring no additional steps when employing
an embossed and/or monogrammed punch face.
Disadvantages of Tablet dosage form are:
1. Difficult to swallow in case of children and unconscious patients.
2. Some drugs resist compression into dense compacts, owing to amorphous nature, low
density character.
3. Drugs with poor wetting, slow dissolution properties, optimum absorption high in GIT
may be difficult to formulate or manufacture as a tablet that will still provide adequate or
full drug bioavailability.
4. Bitter testing drugs, drugs with an objectionable odor or drugs that are sensitive to
oxygen or moisture may require encapsulation or coating. In such cases, capsule may offer
the best and lowest cost.
General properties of Tablet dosage forms:
1. A tablet should have elegant product identity while free of defects like
chips, cracks, discoloration, and contamination.
2. Should have sufficient strength to withstand mechanical shock during its
production packaging, shipping and dispensing.
3. Should have the chemical and physical stability to maintain its physical
attributes over time.
4. The tablet must be able to release the medicinal agents in a predictable and
reproducible manner.
5. Must have a chemical stability over time so as not to follow alteration of
the medicinal agents.
Different types of Tablets
(A) Tablets ingested orally:
1. Compressed tablet, e.g. Paracetamol tablet
2. Multiple compressed tablet
3. Delayed release tablet, e.g. Enteric coated Bisacodyl tablet
4. Sugar coated tablet, e.g. Multivitamin tablet
5. Film coated tablet, e.g. Metronidazole tablet
6. Gelatin coated tablet e.g. Tylenol PM gelcaps
7. Chewable tablet, e.g. Antacid tablet
(B) Tablets used in oral cavity:
1. Buccal tablet, e.g. Vitamin‐c tablet
2. Sublingual tablet, e.g. Vicks Menthol tablet
3. Troches or lozenges
4. Dental cone
(C) Tablets administered by other route:
1. Implantation tablet
2. Vaginal tablet, e.g. Clotrimazole tablet
(D) Tablets used to prepare solution:
1. Effervescent tablet, e.g. Dispirin tablet (Aspirin)
2. Dispensing tablet: compounding tablets because the pharmacist used them to compound
prescriptions e.g. Enzyme tablet (Digiplex)
3. Hypodermic tablet
4. Tablet triturates e.g. NTG tablet
(E) Instant-release tablets (rapidly dissolving tablets, or RDTs): are characterized by disintegrating
or dissolving in the mouth within 1 minute, some within 10 seconds e.g., Claritin Reditabs
[loratadine].
Tablet Ingredients
In addition to active ingredients, tablet contains a number of inert materials known as additives or
excipients. Different excipients are:
1. Diluent
2. Binder and adhesive
3. Dis-integrents
4. Lubricants and glidants
5. Colouring agents
6. Flavoring agents
7. Sweetening agents
Diluent: Diluents are fillers used to make required bulk of the tablet when the drug dosage itself is
inadequate to produce the bulk. Secondary reason is to provide better tablet properties such as
improve cohesion, to permit use of direct compression manufacturing or to promote flow. A
diluent should have following properties:
1. They must be non toxic and acceptable to all countries.
2. They must be commercially available in acceptable grade
3. There cost must be low
4. They must be physiologically inert
5. They must be physically & chemically stable by themselves & in combination with the drugs.
6. They must be free from all microbial contamination.
7. They do not alter the bioavailability of drug.
8. They must be color compatible.
Commonly used tablet diluents
1. Lactose‐anhydrous and spray dried lactose: anhydrous no Maillard reaction but absorb
moisture, can become dark in presence of amine drug base or salts of alkaline compounds.
2. Directly compressed starch‐StaRx 1500 can act as binder, disintegrating agent. Itself act
as lubricant but needs lubricant when mix with drug.
3. Hydrolyzed starch‐Emdex and Celutab: 90-92% dextrose + 3-5% maltose. Can be used
in place of mannitol in chewable tablets due to their sweet and smooth taste.
4. Microcrystalline cellulose‐Avicel (PH 101and PH 102): good flow properties and
excellent compression characteristics, also acts as disintegrating agent, expensive in high
concentration.
5. Dibasic calcium phosphate dehydrate
6. Calcium sulphate dihydrate
7. Mannitol: expensive but –ve heat of dissolution, slow solubility and sweet
taste- chewable tablets. Nonhygroscopic good vitamins, poor flow requires
fairly high lubricant.
8. Sorbitol: with mannitol to reduce cost, however hygroscopic.
9. Sucrose‐Sugartab, DiPac, Nutab: problem with diabetic patients, picks up
moisture at high temp.
10. Dextrose or Cerelose to replace lactose when it darkens.
Binders and Adhesives: These materials are added either dry or in wet‐form to form granules or
to form cohesive compacts for directly compressed tablet. Example:
• Acacia, tragacanth‐ Solution for 10‐25% Conc. Better in solution than dry pd, variable in
composition and performance and contaminated with bacteria.
• Gelatin‐ 10‐20% solution: either alone or with acacia
• Glucose‐ 50% solution, common wet granulating agent
• Starch paste‐10‐20% solution, by dispersing in water followed by heating. Transluscent
• Cellulose derivatives‐ Methyl cellulose, Hydroxy propyl methyl cellulose, Hydroxy propyl
cellulose, dry as binder and wet as adhesives.
• Polyvinylpyrrolidone (PVP)‐ 2% conc. Either as aq, solution or ethanol sol. Can also use as dry
binder.
• Sodium alginate
• Sorbitol
Disintegrants: Added to a tablet formulation to facilitate its breaking or disintegration when it
contact in water in the GIT. Function by drawing water into the tablet to burst apart.
Example:
• Starch‐ 5‐20% of tablet weight. Cost effective
• Starch derivative – Primogel and Explotab (1‐8%)
• Clays‐ Veegum HV, bentonite 10% level in coloured tablet only.
• Cellulose
• Cellulose derivatives‐ Ac‐ Di‐Sol (sodium carboxy methyl cellulose) cross linked polymer of
sodium carboxy methylcellulose.
• cross‐linked PVP (Polyvinylpyrrolidone).
Superdisintegrants: Swells up to ten fold within 30 seconds when contact water. Example:
Crosscarmellose‐ cross‐linked cellulose, Crosspovidone‐ cross‐linked povidone (polymer),
Sodium starch glycolate‐ cross‐linked starch. A portion of disintegrant is added before granulation
and a portion before compression, which serve as glidants or lubricant. Evaluation of carbon
dioxide in effervescent tablets is also one way of disintegration.
Lubricant, anti-adherents and Glidants: Lubricants are intended to reduce the friction
during tablet ejection, Anti-adherents reduces the stickiness or adhesion of the any of the
tablet granulation or powder to the punch or die wall. Glidants are intended to promote flow
of granules or powder material by reducing the friction between the particles.
Example: Lubricants‐ Stearic acid, Stearic acid salt ‐ Stearic acid, Magnesium stearate,
Talc, PEG (Polyethylene glycols). The finer the particle size of lubricant, the more effective
the lubricant action is likely to be.
Antiadherents: most of the lubricants except those are water soluble, also work as
lubricants. Ex. Talc, magnesium stearate and starch derivatives. In addition various colloidal
silicas also function as antiadherents.
Surfactants Glidants‐ Corn Starch – 5‐10% conc., Talc‐5% conc., Silica derivative ‐
Colloidal silicas such as Cab‐O‐Sil, Syloid, Aerosil in 0.25‐3% conc
Coloring agent: The use of colors and dyes in a tablet has three purposes: (1) Masking of
off color drugs (2) Product Identification (3) Production of more elegant product
All coloring agents must be approved and certified by FDA. Two forms of colors are used
in tablet preparation – FD &C and D&C dyes. These dyes are applied as solution in the
granulating agent or Lake form of these dyes. Lakes are dyes absorbed on hydrous oxide
and employed as dry powder coloring. Example: FD&C yellow 6‐sunset yellow, FD&C
yellow 5‐ Tartrazine, FD&C green 3‐ Fast Green, FD&C blue 1‐ Brilliant Blue, FD&C
blue 2 ‐ Indigo carmine, D&C red 3‐ Erythrosine, D&C red 22 - Eosin Y.
Flavoring agents: For chewable tablet‐ flavor oil are used, 0.5-0.75%
Sweetening agents: For chewable tablets: Sugar, mannitol.
Saccharine (artificial): 500 time’s sweeter than sucrose Disadvantage: Bitter aftertaste and
carcinogenic
Aspartame (artificial) Disadvantage: Lack of stability in presence of moisture.
Evaluation of Tablet

1. General Appearance: The general appearance of a tablet, its identity and general elegance is essential for
consumer acceptance, for control of lot‐to‐lot and tablet‐to‐tablet uniformity. The control of general appearance
involves the measurement of size, shape, colour, presence or absence of odour, taste etc.

2. Size & Shape: It can be dimensionally described & controlled. Tablet thickness is consist batch to batch or
within a batch only if the tablet granulation or powder blend is adequately consistent in particle size and size
distribution, if the punch tooling is of consistent length, and if the tablet press is clean and in good working
condition. The thickness of a tablet is only variables. Tablet thickness can be measured by micrometer or by other
device. Tablet thickness should be controlled within a ±5% variation of standard value.

3. Unique identification marking: These marking utilize some form of embossing, engraving or printing. These
markings include company name or symbol, product code, product name etc.

4. Organoleptic properties: Colour distribution must be uniform with no mottling (nonuniformity is generally
referred to as “mottling”). For visual colour comparison compare the colour of sample against standard colour using
reflectance spectrophotometer, tristimulus colorimetric measurements and the use of micro-reflectance photometer
to measure the colour uniformity and gloss on a tablet surface.

The presence of an unusual odour in a batch of tablets could indicate a stability problem, however the presence is
also characteristic of a kind of tablets
5. Hardness: Tablet requires a certain amount of strength or hardness and resistance to
friability to withstand mechanical shakes of handling in manufacture, packaging and
shipping as well as customers' handling. Hardness generally measures the tablet crushing
strength. The hardness is related to tablet disintegration, and drug dissolution release rate.
6. Friability: Friability of a tablet can determine
in laboratory by Roche friabilator. This consist of
a plastic chamber that revolves at 25rpm,
dropping the tablets through a Distance of six
inches in the friabilator, which is then operate for
100 revolutions. The tablets are reweighed.
Compress tablet that lose less than 0.5 to 1.0% of
the Tablet weight are consider acceptable. Worn
out punches results in whiskering at the tablet
edge, which have higher friability value. Tablet
friability is also influenced by moisture content Varian Friabilator testing apparatus for rolling
and impact durability. Tablets are weighed
which acts as binder.
and placed in the acrylic drums, in which a
curved baffle is mounted. When the motor is
activated by setting the timer, the tablets roll
and drop.
Drug Content and Release:
(I) Weight Variation test (U.S.P.) : Take 20 tablet and weighed individually. Calculate average
weight and compare the individual tablet weight to the average. The tablet pass the U.S.P. test if no
more that 2 tablets are outside the percentage limit and if no tablet differs by more than 2 times the
percentage limit.
(II) Content Uniformity Test: Randomly select 30 tablets. 10 of these assayed individually. The
Tablet pass the test if 9 of the 10 tablets must contain not less than 85% and not more than 115% of
the labelled drug content and the 10th tablet may not contain less than 75% and more than 125% of
the labelled content. If these conditions are not met, remaining 20 tablet assayed individually and
none may fall outside of the 85 to 115% range.
(III) Disintegration Test (U.S.P.) : The U.S.P. device to test
disintegration uses 6 glass tubes that are 3”long; open at the top
and 10 mesh screen at the bottom end. To test for disintegration
time, one tablet is placed in each tube and the basket rack is
positioned in a 1‐L beaker of water, simulated gastric fluid or
simulated intestinal fluid at 37±20°C such that the tablet remain
2.5 cm below the surface of liquid on their upward movement
and not closer than 2.5 cm from the bottom of the beaker in their
downward movement. Move the basket containing the tablets up
and down through a distance of 5‐6 cm at a frequency of 28 to
32 cycles per minute. Floating of the tablets can be prevented by
placing perforated plastic discs on each tablet.
According to the test the tablet must disintegrate and all
particles must pass through the 10 mesh screen in the time
specified. If any residue remains, it must have as oft mass.
Disintegration time: Uncoated tablet: 5‐30 minutes
Entric Coated tablet: 1‐2 hours
Dissolution Test: In vitro dissolution testing of solid dosage forms is important for a
number of reasons
• Dissolution studies in the early stages of a product’s development allow differentiation
between formulations and correlations identified with in vivo bioavailability data.
• The conduct of such testing from early product development through approval and
commercial production ensures control of any variables of materials and processes that
could affect dissolution and quality standards.
• Consistent in vitro dissolution testing ensures bioequivalence from batch to batch.
• It is a requirement for regulatory approval of marketing for products registered with the
FDA and regulatory agencies of other countries. New drug applications (NDAs)
submitted to the FDA contain in vitro dissolution data generally obtained from batches
used in pivotal clinical and/or bioavailability studies and from human studies conducted
during product development.
• The goal of in-vitro dissolution testing is to provide insofar as is possible a
reasonable prediction of or correlation with the product’s in-vivo bioavailability.
The system relates combinations of a drug’s solubility (high or low) and its
intestinal permeability (high or low) as a possible basis for predicting the
likelihood of achieving a successful in-vivo–in-vitro correlation (IVIVC). Using
this system, drugs are placed into one of four categories as follows:
I II
High Solubility and High Low Solubility and High
Permeability Permeability
III IV
High Solubility and Low Low Solubility and Low
Permeability Permeability
• A number of formulation and manufacturing factors can affect the disintegration and
dissolution of a tablet, including particle size of the drug substance; solubility and
hygroscopicity of the formulation; type and concentration of the dis-integrant, binder, and
lubricant; manufacturing method, particularly the compactness of the granulation and
compression force used in tableting; and any in-process variables. Together, these factors
present a set of complex interrelated conditions that have a bearing on a product’s
dissolution characteristics. Therefore, batch-to-batch consistency is vitally important to
establish dissolution test standards and controls for both materials and processes and to
implement them during production and in final testing.
• In addition to formulation and manufacturing controls, the method of dissolution testing
must be controlled to minimize important variables such as paddle rotational speed,
vibration, and disturbances by sampling probes. Dissolution testing for oral dosage forms
has been a component of evaluating product quality in the USP since 1970, when only 12
monographs contained such a requirement.
Dissolution Test (U.S.P.):
Two set of apparatus:
Apparatus‐1: A single tablet is placed in a small wire mesh basket attached to the bottom
of the shaft connected to a variable speedmotor. The basket is immersed in a dissolution
medium (as specified in monograph) contained in a 100 ml flask. The flask is cylindrical
with a hemispherical bottom. The flask is maintained at 37±0.5°C by a constant temperature
bath. The motor is adjusted to turn at the specified speed and sample of the fluid are
withdrawn at intervals to determine the amount of drug in solutions.
Apparatus‐2: It is same as apparatus‐1, except the basket is replaced by a paddle. The
dosage form is allowed to sink to the bottom of the flask before stirring. For dissolution test
U.S.P. specifies the dissolution test medium and volume, type of apparatus to be used, rpm
of the shaft, time limit of the test and assay procedure for. The test tolerance is expressed as
a % of the labelled amount of drug dissolved in the time limit.
Dissolution testing and interpretation can be continued through three stages if necessary. In stage 1,
6 tablets are tested and are acceptable is all of the tablets are not less the monograph tolerance limit
plus 5%. If stage 1st fails then an additional 6 tablets are tested. The tablets are acceptable if the
average of the twelve tablets is greater than or equal to Q and no unit is less than Q minus 15%. If
the tablets still fail the test, an additional 12 are tested. The tablets are acceptable if the average of
all 24 tablets is greater than or equal to Q and if not more than 2 tablets are less than q minus 15%.
Granulation
The granulation process allows the particles to stick together more firmly. It increases the particle
size of the constituents used, which are mostly very fine powders. The greater the particle size of a
constituent, greater will be its compressive or binding ability.
Good flow properties- spheres- aggregates called granules
Size of granules: effect of granule size and size distribution on processability and tablet quality
features. Have to checked for each formulation and manufacturing process.
Surface area of granules
Density, strength and friability, flow properties(- repose angle, hopper flow rate), compaction
 Wet granulation is a widely employed method for the production of compressed tablets.
The steps required are
(a) weighing and blending the ingredients,
(b) preparing a dampened powder or a damp mass with binder (in powder form or in
solution form)- crumbling mass followed by milling,
(c) screening the dampened powder or damp mass into pellets or granules,
(d) drying the granulation to remove solvent,
(e) sizing the granulation by dry screening,
(f) adding lubricant and blending, and
(g) forming tablets by compression.
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.
Slugging or compression-granulation: 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 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.
Roller Compaction: Instead of slugging, powder
compactors may be used to increase the density of a
powder by pressing it between rollers at 1 to 6 tons
of pressure. The compacted material is broken up,
sized, and lubricated, and tablets are prepared by
compression in the usual manner. The roller
compaction method is often preferred to slugging.
Binding agents used in roller compaction
formulations include methylcellulose or hydroxy
methylcellulose (6% to 12%), which can produce
good tablet hardness and friability.
ALL-IN-ONE GRANULATION METHODS: The fluid bed granulator performs the
following steps: (a) preblending the formulation powder, including active ingredients,
fillers, and disintegrants, in a bed with fluidized air; (b) 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; and (c) 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.

Fluid bed coating of solid particles. A. Top spray. B. Bottom spray (Wurster). C. Tangential spray.
Tableting of granulation: Basic parts -a steel die cavity by the pressure exerted by the
movement of two steel punches, a lower punch and an upper punch.
Basic mechanical process. With 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. 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 tablets fall into a collection container.
Rotary tablet machines equipped with multiple punches and dies
operate via continuous rotating movement of the punches. A single
rotary press with 16 stations (16 sets of punches and dies) may
produce up to 1,150 tablets per minute. Double rotary tablet
presses produce two tablets for each die.
Problems with Tablet: capping, splitting, laminating,
• The capping, splitting, or laminating of tablets is sometimes related to air entrapment
during direct compression. When air is trapped, the resulting tablets expand when the
pressure of tableting is released, resulting in splits or layers in the tablets. Forced or
induced feeders can reduce air entrapment, making the fill powder more dense and
amenable to compaction.
• Capping also may be caused by punches that are not immaculately clean and perfectly
smooth or by a granulation with too much fines, or fine powder. Fine powder, which
results when a dried granulation is sized, is generally 10% to 20% of the weight of the
granulation. Some fine powder is desired to fill the die cavity properly. However, an
excess can lead to tablet softness and capping.
Tablet Compression Machine
Tablets are made by compressing a formulation containing a drug or drugs with excipients on
stamping machine called presses. Tablet presses are designed with following basic components:
1) Hopper for holding and feeding granulation
2) Dies that define the size and shape of the tablet.
3) Punches for compressing the granulation within the dies.
4) Cam tracks for guiding the movement of the punches.
5) A feeding mechanism for moving granulation from hopper into the dies
Working of rotary tableting machine.
https://www.youtube.com/watch?v=4xggZRckfTE
Tablet Coating
Tablet coatings perform one or more of the following functions. They may:
• mask the taste of unpalatable drugs,
• Provide chemical and physical protection for the drug,
• separate incompatible ingredients,
• control the release of medicament in the gastrointestinal tract,
• and provide an elegant or distinctive finish to the tablet.
The materials used for coating may largely comprise sucrose (sugar coating), water‐soluble
film‐forming polymers (film coating) or substances which are soluble in the intestinal secretions
but not in those of the stomach (enteric coating). These types of coating can all be applied by the
pan or fluid‐bed processes; the compression coating technique is suitable for sugar and enteric
coatings, but not for film coating.
Required tablet properties:
• Must be resistant to abrasion and chipping
• Smooth surface and curved surface of the tablet
• Wetting of the surface of the tablet
Tablet coating is the application of a coating composition to a moving bed of tablets with the
concurrent use of heated air to facilitate evaporation of the solvent. The distribution of the coating
is accomplished by the movement of the tablets either perpendicular (coating pan) or vertical (air
suspension coater) to the application of the coating composition.
Coating process: Pan coating, Fluid Bed Coating, Compression coating
Mostly coating processes use one of the three general types of coating pans (1) Standard coating
pan, (2) perforated coating pan and (3) the fluidized bed
Perforated coating pans: to maximize the interaction between the tablet bed and the drying air, which
it does by drawing the air through the tumbling product bed as opposed to supplying air to the bed
surface only.
Mixing efficiency is achieved by the use of appropriately designed baffles on the pan surface.
Perforated coating pans come in various designs depending on the vendor, but the intention is to
maximize the drying capability of the machine so as to minimize core penetration at high spray rates.
Examples of perforated coating pans include:
1. Accela-cota (Thomas Engineering, USA)
2. Hi-coater (Freund-Vector Japan and USA)
3. Driacoater (Driam Metallprodukt GmbH, Germany)
4. Glatt perforated coating pan (Glatt., Switzerland, Germany and USA)
5. Huttlin Butterfly Pan, HBP (G S, Italy)
6. IDA Coating equipment (Dumoulin, France
Fluidized bed equipment: the most efficient drying of any product that is possible in any existing coating
equipment.

In a fluid bed system, the objects being coated are suspended in an upward stream of air, maximizing the surface
available for coating. The coating is applied by an atomizer, and this is dried by the fluidizing air.

Film coating can be applied to the fluidized material by a variety of techniques – top spray, bottom spray and
tangential spray. The selection of a particular technique is often determined by the nature and intended
functionality of the coating applied; for example

1. Top spray (granulation or conventional mode) is used predominately for taste and odour masking purposes,
where drug release rates are not critical since films produced by this method are not uniform in thickness.
Additionally, it is suitable for the application of hot-melt coatings.

2. Bottom spray (Wurster) is preferred for the application of rate-controlling polymers to a wide variety of
multi-particulates. The process is also suitable for drug layering when the drug dose is in the low-to-medium
range.

3. Tangential spray (rotary granulator) is suitable for the application of modified-release film coatings to a wide
range of multiparticulate products. The process is ideal for drug layering when the dose is medium to high. It is
also useful as a spheronizing process for producing spheroidal pellets from powders.
Spray application system: high pressure and low pressure
Compression coating: In a manner similar to the preparation of multiple compressed
tablets having an inner core and an outer shell of drug material, core tablets may be
sugarcoated by compression. The coating material, in the form of a granulation or powder,
is compressed onto a tablet core of drug with a special tablet press. Compression coating is
an anhydrous operation and thus may be safely employed in the coating of tablets
containing a drug that is labile to moisture. Compared to sugarcoating using pans,
compression coating is more uniform and uses less coating material, resulting in tablets that
are lighter, smaller, and easier to swallow and less expensive to package and ship.
• Irrespective of the method used in coating, all tablets are visually or electronically
inspected for physical imperfections.
Sugar coating: It involves the application of sugar solution with color for several times to give –
• It prevents unpleasant odor,
• Give sweet taste to tablet by masking bitter taste,
• Highly elegant and glossed tablets are obtained.
Sugar coating involves following steps –
Sealing
Sub-coating
Syruping (smoothing)
Polishing
The tablet having deep convex surfaces with thin rounded edges are suitable for sugar coating. In
sugar coating, the tablet should be resistant to breakage, chipping, and abrasions because sugar
coating tends to be long and vigorous.
Sealing: It prevents moisture penetration in to the tablet core. Why: Sugar-coatings are aqueous
formulations which allow water to penetrate directly into the tablet core and thus potentially
affecting product stability and possibly causing premature tablet disintegration. It enables
sugar-coated product to exhibit modified- release pattern (extended release or delayed "enteric"-
release characteristics). To protect the tablet core from adverse effect of moisture

Seal coating agents - shellac, zein, Oleic acid, PG, PEG4000, alcohol, methylene chloride. Zein
is alcohol-soluble protein derivative. Shellac is more effective (because of polymerization of
shellac), But it lengthens tablet disintegration and dissolution times.

Sub coating: To form uniform edges, To build up the tablet size. Sub coating increases the tablet
weight from 50 to 100%. It is done to provide the sealed tablet cores with round edges and to
build up the core weight. It is achieved by adding a bulking agent such as Calcium carbonate, to
the sucrose solution. Antiadherents e.g. Talc may be added after partial drying to prevent sticking
of the tablets together.
Examples- Gelatin, sugarcane powder, corn syrup, syrup , distilled water, Gum acacia.
It involves application of binder solution to the Tablets followed by dusting of sub coating with powders
and drying until the tablet edges have been covered & the desired thickness is achieved.
Syrup Coating: It is done to cover the imperfections in the Tablet surface caused during sub coating step.
Syrup coating constituents- colorant, sub coating powder, calcium carbonate, cane sugar powder, corn
starch, syrup, distilled water. It involves-
• Application of syrup coating with grossing syrups followed by the addition of dilute colorants to provide
tinted base.
• In subsequent steps, the syrup solution containing dye are applied until final size and color are achieved.
• The final step a clear syrup coat without dye are applied.
No colour is added until the tablets are quit smooth, Premature application to the rough tablets can produce
a Mottled appearance in the final coated tablets.
Polishing: The desired luster to the tablet is obtained by polishing. Tablets are polished in a Standard
coating pans by application of carnauba wax (yellow), bees wax (white), paraffin wax (or) warm solutions
of waxes in naphtha (or) suitable volatile solvent.
Film coating: It is the process of polymeric solution to bring a uniform film. It gives a tablet with less weight
and small size. The film formed is very thin. In film coating engravings are possible on tablet surface which are
not possible in sugar coating. Better mechanical strength is obtained. The cost of the film coated tablets is less.

The film forming agents tablet coating are classified into:

Non enteric film formers: They are incorporated to give uniform film with desired mechanical strength which
are as follows: 1. HPMC (Hydroxy propyl methyl cellulose) 2. MHEC (Methyl hydroxyl ethyl cellulose) 3. EC
(Ethyl cellulose) 4. HPC (Hydroxy propyl cellulose) 5. POVIDONE 6. SCMC 7. PG 8. Acrylate polymers

Enteric film formers: To protect acid-labile drugs from gastric fluid e.g. Enzymes & certain Antibiotics. To
prevent gastric distress or nausea due to irritation from the drug. e.g., Sodium salicylate. To deliver drugs
intended for local action in the intestines, e.g. Intestinal antiseptics. To deliver drugs that are optimally absorbed
in the small intestine to their primary absorption site. To provide a delayed-release component for repeat-action
tablets. Eg. CAP (Cellulose acetate phthalate), ACRYLATE POLYMERS, HPMCP (Hydroxypropyl methyl
cellulose phthalate), PVAP (Polyvinyl acetate phthalate)
Coating composition: It involves 1. Solvent 2. Plasticizers 3. Colorants 4. Opaquant-extenders

Solvent to dissolve or disperse the polymers and other additives and convey them to the substrate surface. The
ideal requirements of the solvent are

• It should either dissolve or disperse the polymer system.

• It should have no environmental impact.

• It should easily disperse other coating solution components in to the solvent system.

• It should have rapid drying rate (ability to coat 300kg load in 3-5 hours) 67

• It should be Colorless, tasteless, odorless, Inexpensive, nontoxic, inert and Non-inflammable and rapid drying
Rate. Examples- Water, Ethanol, Methanol, Isopropanol, Chloroform, Acetone, Methylene chloride, Methylene
ethyl ketone.
Plasticizers: to modify the quality of the film. Plasticizing techniques involve internal plasticizers and
external plasticizers.
Internal plasticizers involves chemical modification of the basic polymer that alters the physical properties of
the polymers.
Chemical plasticizers: Additives of the Coating solution to achieve the desire effect of the film (flexibility,
tensile Strength, adhesive properties)
Level of plasticizers ranges from 1-50% by weight of film former. Examples: Castor oil, Propylene glycol,
Glycerin, Surfactants e.g., Polysorbate(tweens), sorbitan esters(spans), organic acid esters.
Colorants: It is to provide the distinct color and Elegance to the dosage form. To achieve the proper
distribution of suspended colorants in the coating solutions requires. Use of fine powdered colorants (<10
microns). The concentration of colorants in the coating solution depends on the color shade, desired the type
of dye and the concentration of the opaquant extenders.
For very light shade conc. Lt 0.01% For dark shade Conc. Mt 2.0% is required. The most common colorants
in use are certified by FOOD DRUG AND COSMETICS (FD&C) or DRUG AND COSMETIC (D&C)
Colorants. These are lakes and dyes. Lakes are derived from dyes by precipitating with carriers e.g., Alumina
or talc.
The inorganic materials and the natural colorants are- Iron oxides, Caramel, Carotenoid,
Chlorophyll, indigo, Flavones, Turmeric and carminic acid. A variety of products that
are Commercially available are- Opalux- Opaquant color concentrate for sugar coating.
Opaspray -for film coating. Opadry- complete film coating concentrate.
OPAQUANT-EXTENDERS These are very fine inorganic powders used In the coating
solution formulation to provide more pastel colors and increase film coverage. Provide
white coating or mask the color of the tablet core. Examples: Titanium dioxide, Silicates
like (Talc, Aluminium silicate) Carbonates like-magnesium carbonate, Sulphates like
calcium sulphate.
Pan pour Process: This method is relatively slow and relies heavily on the skill and
technique of the operator to balance the steps to produce an acceptable product.
Requires additional drying to remove latent solvents. Aq. based film coatings are not
suitable due to localised over-wetting.
Pan spray methods: More efficient and versatile than pan pour method. Spray patterns are
selected for continuous bed across the tablet bed surface. Broad flat patterns are usually
chosen by selection of appropriate nozzle systems.
Pan variables Process air Spray variables
Pan design/ baffling Air quality rate
Speed temperature Degree of atomization
Pan load Airflow rate/vol/balance Spray pattern
Nozzle to bed distance
Fluidized spray process: In this system fluidization of the tablet mass is achieved in a
columnar chamber by the upward flow of drying air. The air flow is controlled, so that more
air enters the center of the column, causing the tablets to rise in the center. The movement of
tablets is upward through the center of the chamber. They then fall towards the chamber wall,
Move downwards to re-enter the air stream at the bottom of the chamber. Coating solutions
are applied from a spray nozzle which is located at the bottom of the chamber or are sprayed
onto the top of the Cascading tablet bed by nozzles located in the upper region of the chamber
Determination of the quality of a tablet coat involves studying of the film and the film- tablet
.
interactions. The following test methods can be employed;
• Adhesion test with tensile strength testers are used to measure the force needed to peel the
film from the tablet surface.
• Diametric crushing strength of the coated tablets is determined using a tablet hardness
tester.
• The rate of coated tablet disintegration and dissolution should also be studied.
• Exposure to elevated humidity and measurement of tablet weight gain provide relative
information on the protection provided by the film.
• Stability studies can be conducted on coated tablets to verify whether temperature and
humidity changes would result in film defects.
• Determination of film surface roughness, hardness and color uniformity.
• Resistance of coated tablet to abrasion is done by merely rubbing the coated tablet on white
paper sheet. Film should remain intact and no color transferred to paper.
1. Picking and sticking: This defect is occurs when the coating removes a piece of the
tablet from the core. It is caused by over-wetting the tablets, by under-drying, or by poor
tablet quality.
2. Bridging: This occurs when the coating fills in the lettering or logo on the tablet and is
typically caused by excess application of the solution, poor design of the tablet
embossing, high coating viscosity, high percentage of solids in the solution, or improper
atomization pressure.
3. Erosion: This can be the result of soft tablets, an over- wetted tablet surface, inadequate
drying, or lack of tablet surface strength.
4. Twinning: This is the term for two tablets which stick together, and it’s a common issue
with capsule shaped tablets. If you don’t want to change the tablet shape, you can solve
this problem by changing the pan speed and spray rate. Try lowering the spray rate or
increasing the pan speed. The change is almost impossible to see, but it solves the
twinning problem.
 5. Peeling and frosting: This is a defect where the coating peels away from the tablet surface in a sheet.
Peeling indicates that the coating solution did not lock into the tablet surface. This could be due to a defect
in the coating solution, over-wetting, or high moisture content in the tablet core.

6. Blistering: Too rapid evaporation of solvent from the coated tablets and the effect of high temperature on
the strength and elasticity of the film may cause blistering. Milder conditions are required in this case.

7. Mottled color: This can happen when the coating solution is improperly prepared, the actual spray rate
differs from the target rate, the tablet cores are cold, or the drying rate is out of spec.

8. Orange peel: This refers to a coating texture that resembles the surface of an orange. It is usually the result
of high atomization pressure in combination with spray rates that are too high.

9. Capping: The main cause of this defect is improper compression of the tablet. This defect will not be
revealed unless the coating is initiated. This defect occurs due to excessive drying in pre-heating stage.

10. Chipping: Chipping is caused due to high pan speed, a friable tablet core or coating solution that lacks
good plasticizer.
Electrostatic coating: For conductive substances. A strong electrostatic charge is applied to
the substrate. The coating material containing conductive ionic species of opposite charges is
sprayed onto the charged substate. Complete and uniform coating of corners.
Dip coating: by dipping in coating solution followed by drying in coating pans, alternate
dipping and drying. Lacks the speed, versatility and reliability of spray coating.
Vacuum film coating: In a air sealed pan, heating by surrounding water, coating in airless
spray system. Energy requirement is low with high coating efficiency. Very apt for organic
solvents.
Bioequivalence is the similarity of two drugs that share the same desired outcome for patients.
Pharmacokinetic studies must be done to determine whether a commercially available brand
and a potential generic version share core attributes.
Bioavailability is used to describe the fraction of an administered dose of unchanged drug that
reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs.