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168
upper-center punch is then retracted to create space, into which the core powder is
introduced and pre-compressed by the upper-center punch. In the end, the lower-
outer punch descends, permitting the second-outer layer powder to ll and encase
the pre-compressed core and rst-outer layer. The combination of the core and rst-
outer layer, along with the second-outer layer, is compressed utilizing the upper and
lower punches, with the center punches and outer punches functioning coopera-
tively (Ozeki etal. 2004).
Advantages of OSDrC
®
Technology
• Improves the safety and efcacy of drugs
• Enhanced pharmaceutical treatment
• Improved branding and product distinction
• Enhanced controlled-release formulations
6.8 Defects ofTablet Coating
The tablet coating has several defects, including blistering, chipping, picking, twin-
ning, pitting, orange peel, and mottling. These defects and their remedies are sum-
marized in Table6.1.
Table 6.1 Overview of defects of tablets, their denitions, reasons, and remedies
Defects
Denition Reason Remedies
Reference
Blistering It is a localized
separation of the
lm from the
substrate’s
surface that
results in a blister
Gas retention in
the lm as a
result of
excessive heat
throughout
spraying as well
as the nal step
of the coating
process
In this case, slower drying
conditions are necessary
Ganguly
etal.
(2022)
Chipping It is a problem in
which the lm
appears chipped
and dented,
typically along
the tablet’s edges
Reduced
uidizing air or
a decrease in
drum rotation
speed in pan
coating
Exercise caution to avoid
excessive drying of the tablets
during the preheating phase,
as this could render the tablets
fragile and encourage capping
Ganguly
etal.
(2022)
Picking This problem
occurs when
certain regions of
the lm detach
from the surface
due to tablets
adhering together
and subsequently
separating
Similar to
cratering, an
excessively
moist tablet bed
can cause
subsequent
tablets to fuse
together before
breaking
The issue is typically resolved
by slowing down the liquid
application speed or
enhancing the drying air heat,
air volume, and temperature
of the air
Ganguly
etal.
(2022)
N. N. Jitendra et al.
169
6.9 Conclusion
Tablets have long been a preferred pharmaceutical dosage form because of their
convenience, stability, and ease of administration. Remarkable advancements in
tablet production and coating technologies have revolutionized the pharmaceutical
Table 6.1 (continued)
Defects
Denition Reason Remedies
Reference
Twinning Two tablets that
adhere to one
another are
referred to as
twinning
This issue
generally arises
in capsule-
shaped tablets
If preserving the tablet shape
is a priority, the issue can be
resolved by adjusting the
interplay between the pan
speed and the spray rate.
Experiment with decreasing
the spray rate while elevating
the pan speed. Occasionally, it
might be essential to slightly
alter the tooling design by
making a subtle adjustment to
the radius. This modication,
nearly imperceptible,
effectively mitigates the
occurrence of tablet adhesion
Ganguly
etal.
(2022)
Pitting This aw entails
the formation of
indentations on
the tablet core
surface, even
when there is no
apparent damage
to the lm
coating
The
temperature of
the tablet core
is higher than
the materials’
melting points
when the tablets
are made
During the entire production
process, regulate the
temperature of the tablet core
Ganguly
etal.
(2022)
Orange
peel
This surface
irregularity leads
to a lm texture
that is uneven and
lacks glossiness,
resembling the
appearance of an
orange peel
Improperly
applying the
coating solution
before it has
dried
This issue might be resolved
by adding more solvent to thin
the solution
Ganguly
etal.
(2022)
Mottling The term
“mottling”
describes an
uneven
distribution of
color over the
tablet’s surface,
leaving spots that
are both deeper
and brighter
It is primarily
caused by
excipients with
varied
colorations or
tablets with
colored
degradation
products
An adequate amount of
coating solution is prepared
Ganguly
etal.
(2022)
6 Advances inTablet Production andTablet Coating
170
and nutraceutical industries in recent years. Advancements in granulation methods
such as spray drying, uid bed granulation, and hot-melt extrusion have improved
drug content uniformity, dissolution rates, and overall product stability. The adop-
tion of these technologies promises continued progress in the eld of tablet manu-
facturing, offering new opportunities for personalized medicine and enhanced
therapeutic outcomes. Coating technologies have also evolved signicantly to
enhance tablet appearance, taste-masking, and drug release proles. Automation
involves the utilization of machinery and tools to execute both physical and cogni-
tive tasks within a production process, substituting the need for human involvement.
Acknowledgments The authors thank the National Institute of Pharmaceutical Education and
Research-Raebareli (NIPER-R), Department of Pharmaceutics, Ministry of Chemicals and
Fertilizers, Govt. of India for the entire support. Also, the NIPER-Raebareli has provided the
communication number for this manuscript and the communication number is NIPER-R/
Communication/567.
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175
7
Formulation Evaluation
andDevelopment ofSpecialized Tablets
SofiyaTarannum andKeertiJain
Abstract
Oral solid formulations are the most popular and convenient among all kinds of
dosage forms available in the market. Tablets are the solid dosage forms that
ensure xed dose, tamper resistance, and easy handling and administration. The
merits of tablets make them survive in the pharmaceutical market with huge
prot. Tablets have been modied from time to time into several types to be
accepted by all groups and kinds of patients. Based on release prole, tablets are
basically divided into immediate, sustained, delayed release, and many more.
Chewable, effervescent, and orodispersible tablets hold a specic position in the
market. In this chapter we have discussed formulation, evaluation, and develop-
ment of these specialized tablets to cater needs of particular groups of patients in
brief. The future of the tablets starts with the exploration of the world of 3D
printing which makes the customized tablets easily available for the patients as
per their needs, hence improving the patient compliance and acceptability.
Keywords
Chewable tablet · Effervescent tablet · Orodispersible tablet · 3D printing
S. Tarannum · K. Jain (*)
Drug Delivery and Nanomedicine Research Laboratory, Department of Pharmaceutics,
National Institute of Pharmaceutical Education and Research (NIPER)—Raebareli,
Lucknow, Uttar Pradesh, India
e-mail: keertijain.02@niperraebareli.edu.in
176
Abbreviations
3D Three-dimensional
API Active pharmaceutical ingredient
BCS Biopharmaceutics Classication System
DSC Differential scanning calorimetry
ET Effervescent tablet
FLX Fluoxetine
HPMC Hydroxypropyl methylcellulose
ODT Orodispersible tablet
PVP Polyvinylpyrrolidone
PXRD Powder X-ray diffraction
RH Relative humidity
SARS-CoV-2 Severe acute respiratory syndrome coronavirus 2
STP Stiripentol
SUPAC IR Scale-up and Post-Approval Changes Immediate Release
US FDA United States Food and Drug Administration
USP United States Pharmacopeia
7.1 Tablet Dosage Form
Orally administered solid dosage forms are highly preferred forms of medication in
recent times. Solid dosage forms that are administered orally have accurate dosages
as well as stable components. The most appreciable advantages of solid dosage
forms are patient compliance, tamper resistance, and ease of handling and use
(Hemamanjushree and Tippavajhala 2020). Tablets are well-designed in appear-
ance, and they are produced with some identication using distinctive embossing
and debossing on their surface. They are economical formulations as their produc-
tion is simple and highly robust and appropriate for packaging, shipping, as well as
transportation. The tablets are the utmost stable dosage form compared to the liquid
capsules, solutions, or suspensions in terms of physicochemical and microbial char-
acteristics. Tablets are swallowed conveniently and processing steps in their produc-
tion are quite few as well as simple (Arshad etal. 2021).
7.2 History ofTablet
In 1500BCE (Before the Common Era), the most basic oral solid dosage form,
pills, came into the picture. In 4000BCE, medical preparations like liquid, herbs,
spices, plant powders and metals were mostly prescribed as compared to solids.
In primitive Egypt, the pills were mentioned on papyruses. Pills at that time were
composed of honey, grease, and bread dough. Pills were handmade with the help
S. Tarannum and K. Jain
177
of medicated constituents like plant powders or spices. Medications were referred
to as katapotia by the ancient Greece people (Advankar etal. 2019). Pills were
termed as pilula (little ball) by the Roman scholar Pliny. Slimy constituents of
plants were utilized for coating the pills in the olden days. Sugar coating and
gelatin coating were invented in 1800 as gelatin capsules.
William Brockedon shaped the pills, lozenges, and other oral dosage forms using
a device that applies pressure in dies and patented the same (Bueno and Nozal
2010). This machine can compact the powder in the form of a tablet with no use of
adhesive. In 1844 the rst compacted tablets were formulated by Professor
Brockedon in England. The produced tablets were exceptionally hard with no men-
tion of their solubility and disintegration time. The inspiration for compressing the
medications and additives in the form of tablets came from compressing the lead for
making pencils. Thereby, he carried out the compaction of potassium hydrogen car-
bonate and sodium hydrogen carbonate which became the rst illustration of mod-
ern tablet compression. The tablets then came into the market in England and
managed to have decent sales (Skaftason and Jóhannesson 2013). Messrs. Newbery
procured William Brockedon’s business in 1871. At the same time, Jacob Dunton
from Philadelphia started the compaction of several formulations, like quinine tab-
lets, using Brockedon’s die-compression methods (Salawi 2022).
In the mid-nineteenth century, compressed powders were becoming very popular
as they could be easily administered. The negligible use of liquid in these formula-
tions makes them very stable as compared to conventional pills; the ease of storage,
as well as transportation, makes them highly desirable in military pharmacies.
Conventionally the production of pills and lozenges at the industrial scale is much
more complicated than the manufacturing of tablets by powder compression. From
the 1870s to the present, several kinds of tablets were manufactured. The manufac-
turing was signicantly accelerated by the Burroughs Wellcome Company, estab-
lished in the year 1879 by S. M. Burroughs and H. S. Wellcome (Helmstaedter
2020). In 1872, John Wyeth & Brother and Mr. Henry Bower developed an advanced
nonautomatic instrument that could produce tablets at a cheaper rate (Kebler 1914).
Dr. Robert R.Fuller from NewYork rst suggested the lling of molds with medi-
cated milk sugar. In 1883, Mr. Fraser manufactured molded tablets entirely in the
exact approach it is manufactured today (Wood 1906).
Between the 1940s and 1990s, polymers of synthetic and semisynthetic nature
became popular for enteric coating. This comprises the oral sustained-release for-
mulations by Smith, Kline & French utilizing the Spansule mechanism: Dexedrine
(dextroamphetamine sulfate) (1952) (Maurya etal. 2014; Park 2016). Within the
time span of the 1970s and 1980s, the creation and marketing of osmotic drug deliv-
ery systems via the oral route were carried out by the Alza Corporation (Santus and
Baker 1995). Tablets are leading pharmaceutical dosage form globally as compared
to other kinds of pharmaceutical formulations. Its market analysis is described in
brief in below section.
7 Formulation Evaluation andDevelopment ofSpecialized Tablets