1 Final Intro VBHV

INTRODUCTION
INTRODUCTION:
An ideal dosage regimen in the drug therapy of any disease is the one, which
immediately attains the desire therapeutic concentration of drug in plasma (or at the site of
action and maintains it constant for the entire duration of treatment! This is possi"le through
administration of con#entional dosage form in a particular dose and at a particular fre$uency!
Thus drug may "e administered "y #ariety of routes in a #ariety of dosage forms!
%
Drugs are more fre$uently ta&en "y oral administration! Compared with alternate
routes, the oral route of drug administration is the most popular and has "een successfully
used for con#entional deli#ery of drug! It is considered most natural, uncomplicated,
con#enient, safe means of administering drugs, greater fle'i"ility in dosage form design, ease
of production!

Among the drugs that are administered orally, solid dosage form represent the
preferred class of product! They are #ersatile, fle'i"le in dosage strength, relati#ely sta"le,
present lesser pro"lem in formulation, pac&aging and it is con#enient to manufacture, store,
handle and use! (olid dosage form pro#ides "est protection to the drug against light,
temperature, humidity, o'ygen, and stress during transportation

! Amongst the solid oral
dosage form ta"lets are widely used!

1 ) TABLETS

:
Ta"lets may "e defined as solid pharmaceutical dosage forms containing
medicament or medicaments with or without suita"le e'cipients ) prepared either "y
compression or molding!
*
[Formulation development and evaluation of oro-dispersible tablet by direct
compression Method ] Page 1
INTRODUCTION
1 (a) Advantages of tablets
2
:
(ome of the potential ad#antages of ta"lets are as follows!
They are the unit dosage form ha#ing greatest capa"ilities amongst all the oral dosage
form for the dose precision and least content #aria"ility!
Their cost is lowest amongst all the oral dosage forms!
They are the lightest and the most compact amongst all the oral dosage form!
They are easiest and cheapest for pac&aging and transportation!
They lend themsel#es to certain special release profile products such as enteric or delayed
release products!
Ta"lets are "etter suited to large+scale production than other unit oral dosage forms!
They ha#e the "est+com"ined properties of chemical, mechanical, micro"iological
sta"ility amongst all the oral dosage forms!
1(b) Classf!aton of tablets:
,ased on the route of administration or the function, the ta"lets are classified as follows!
-
% Ta"lets ingested orally!
Compressed ta"let
.ultiple compressed ta"let
i /ayered Ta"let
ii Compression coated Ta"let
Repeat action Ta"let
Delayed action and enteric+coated Ta"let
(ugar and chocolate+coated ta"let
a 0ilm coated ta"let
" Chewa"le Ta"let
1 Ta"lets used in the oral ca#ity!
,uccal Ta"let
(u"lingual Ta"let
Troches and /o2enges
INTRODUCTION
Dental cones
* Ta"lets administered "y other routes!
Implantation Ta"let
3aginal Ta"lets
- Ta"lets used to prepare solution!
4ffer#escent Ta"let
Dispensing Ta"let
5ypodermic Ta"let
Ta"lets Triturates
1) !) Tablet "an#fa!t#$ng "et%ods
Ta"lets are manufactured "y 6et granulation, Dry granulation or Direct compression
method!
7
& 'et ($an#laton:
6et granulation is the process in which a li$uid is added to a powder in a #essel
e$uipped with any type of agitation that will produce agglomeration or granules! These
granules after drying are compressed to form ta"lets!
& D$) ($an#laton:
In this techni$ue, there is no use of li$uids! The process in#ol#es the formation of
slugs! Then the slugs are screened or milled to produce granules! The granules formed are
then compressed to form ta"lets!
& D$e!t Co*+$esson:
The term direct compression is used to define the process "y which ta"lets are
compressed directly from powder "lends of acti#e ingredient and suita"le e'cipients, which
will flow uniformly in the die ca#ity ) forms a firm compact!
INTRODUCTION
Table No,1,1: 8rocessing (teps Commonly re$uired in the 3arious Ta"let 9ranulation
preparation techni$ues
7
-$o!essng
ste+s
'et ($an#laton D$)
($an#laton
D$e!t Co*+$esson
Raw materials
6eight
(creen
.i' +
Compress
(slug
+ +
6et mass + +
.ill + +
Dry + +
.ill +
.i' +
Compress
1)d) Advantages of D$e!t Co*+$esson "et%od
.
:/
This process is more economical! It re$uires fewer manufacturing steps, less
processing time ) thus reduces la"our cost ) less process #alidation!
The processing steps re$uired no need of moisture, heat, and high compaction
pressure!
There is an optimi2ation of ta"let disintegration, in which each primary drug particle
is li"erated from the ta"let mass ) is a#aila"le for dissolution!
Disintegrating agents li&e starch are more effecti#e when processed "y direct
compression than wet granulation techni$ue!
In the present aging society, easy+to+use dosage forms for elderly patient, whose
swallowing function is often decreased, are in great demand
*-
! The use of con#entional
ta"lets, capsules, and li$uid or syrup preparations were not always easy+to+use dosage forms
INTRODUCTION
for elderly patients "ecause of there decrease motor function! (imilarly the use of
con#entional ta"lets is challenging to pediatric, geriatric, and uncooperati#e patients who
may ha#e difficulty to swallow ta"lets and is also pro"lematic when water is una#aila"le or
when patients ha#e a persistent cough or gag+reflu'!
These pro"lems ha#e "een addressed "y the recent introduction of orally
disintegrating ta"lets(ODT which also &nown as A $uic&+dissol#ing ta"let (also &nown as
fast+dissol#ing, fast+dissol#ing multiparticulate, rapid+dissol#ing, mouth+dissol#ing, fast+
melting, orodispersing ta"lets is an oral ta"lets that does not re$uire water for swallowing!
.any patients e'press difficulty in swallowing ta"lets and capsules tending to noncompliance
) ineffecti#e therapy!
1, A) 0AST DISSOL1IN( 2 DISINTE(RATIN( TABLET:
Orally Disintegrating ta"lets are also called as Oro+dispersi"le ta"lets, :uic&
disintegrating ta"lets, .outh dissol#ing ta"lets, 0ast disintegrating ta"lets, Rapid dissol#ing
ta"lets, 8orous ta"lets and Rapimelts!
;
A B C
0g#$e 1,1: A+ Disintegration of Oro dispersi"le ta"let after 7 seconds
,+ Disintegration of Oro dispersi"le ta"let after %< seconds
C+ Disintegration of Oro dispersi"le ta"let after 1< seconds
Ad#antages of this drug deli#ery system includes administration without water ,accuracy of
dosage form , easy porta"ility ,alternati#e to li$uid dosage form ,ideal for pediatric )
geriatric patients and rapid onset of action !

Recently, 4uropean 8harmacopoeia has used the term Oro+dispersi"le ta"lets that
disperses readily and within * min in mouth "efore swallowing!
;,%*
compression Method ] Page
INTRODUCTION
United (tate 0ood and Drug Administration (0DA defined Oro+dispersi"le
ta"lets as, =A solid dosage form containing medicinal su"stance of acti#e ingredient which
disintegrates usually within a matter of seconds when placed upon the tongue!>
;
30ast dissol#ing ta"lets is solid dosage form that contains medicinal su"stances
and that disintegrate and dissol#e rapidly without water (within seconds when placed on the
tongue!>
The need for deli#ering drugs to patients efficiently and with few side effects has
prompted pharmaceutical companies to engage in the de#elopment of new drug deli#ery
systems! A solid dosage form that dissol#es or disintegrates rapidly in oral ca#ity, resulting
in solution or suspension without the need of water is &nown as fast dispersing dosage form
or mouth dissol#ing ta"lets! 6hen this type of ta"let is placed into the mouth, the sali#a will
ser#e to rapidly dissol#e the ta"let!
Target populations for these new fast+dissol#ing?disintegrating dosage forms ha#e
generally "een pediatric, geriatric, "edridden or de#elopmentally disa"led patients! 8atient
with persistant nausea, who are tra#eling or who ha#e little or no access of water are also
good candidates for fast dissol#ing ? disintegrating ta"lets

. Other groups that may e'perience
pro"lems using con#entional oral dosage form include the mentally ill and patients who are
uncooperati#e! A difficulty in swallowing (dysphagia ta"lets or capsules is common pro"lem
among all age groups, especially in elderly and pediatrics! 0or this reasons, ta"lets that can
dissol#e or disintegrate in oral ca#ity, ha#e attracted a great deal of attention!
Orally disintegrating ta"lets are characteri2ed "y high porosity, and low hardness, when
administered an in+situ suspension is created in the oral ca#ity as the ta"let disintegrates and
is su"se$uently swallowed!

(ome ta"lets are designed to dissol#e in sali#a remar&a"ly fast,
within a few seconds, and are true fast+dissol#ing ta"lets! Others contain agents to enhance
the rate of ta"let disintegration in the oral ca#ity, and are more appropriately termed fast+
disintegrating ta"lets, as they may ta&e up to a minute to completely disintegrate! 6hen put
on tongue, this ta"let disintegrates instantaneously, releasing the drug, which dissol#es or
disperses in the sali#a! (ome drugs are a"sor"ed from the mouth, pharyn' and oesophagus as
the sali#a passes down into the stomach! In such cases, "ioa#aila"ility of drug is significantly
greater than those o"ser#ed from con#entional ta"let dosage form
%%
!

The disintegration time
of these ta"lets depend largely on si2e and hardness parameters!
compression Method ] Page !
INTRODUCTION
On placing orodispersi"le ta"let in the mouth, sali#a ser#es to rapidly dissol#e the
dosage form! The sali#a containing the dissol#ed or dispersed medicament is then swallowed
and the drug is a"sor"ed in the normal way! (ome drugs are a"sor"ed from the mouth,
pharyn' and oesophagus as the sali#a passes down into the stomach ) it may produce rapid
onset of action!
%%
1, B) / ) Advantages of Oro-dispersible Tablets
Orally disintegrating ta"lets offer all ad#antages of solid dosage forms and li$uid
dosage forms along with special ad#antages, which include
%1
@
4ase of administration to patients who cannot swallow, such as the elderly, stro&e
#ictims and "edridden patientsA patients who should not swallow, such as renal
failure patientsA and who refuse to swallow, such as paediatrics, geriatric and
psychiatric patients!
8atientBs compliance for disa"led "edridden patients and for tra#elling and "usy
people who do not ha#e ready access to water!
9ood mouth feel property of .DDD( helps to change the "asic #iew of
medication as C"itter pillC, particularly for paediatric patients due to impro#ed
taste of "itter drugs!
Con#enience of administration and accurate dosing as compared to li$uid
formulations!
.ore rapid drug a"sorption from the pre+gastric area i!e! mouth, pharyn' and
oesophagus which may produce rapid onset of action!
8re+gastric a"sorption can result in impro#ed "ioa#aila"ility, reduced dose and
impro#ed clinical performance "y reducing side effects!
1,B) / ) Dsadvantages of O$o/ds+e$sble Tablet
Orally disintegrating ta"lets offer following disad#antages
%*
@+
Ta"lets are #ery fragile and lac& physical resistance! ,ecause the ta"lets are #ery
porous and low compression forces are used to prepare them! They cannot "e
pac&ed in con#entional strips or in "ottles and special pac&aging is re$uired!
,itter drugs ha#e to "e taste mas&ed "y #arious techni$ues which in turn increases
the time and cost of production
The growing importance of fast dissol#ing ?disintegrating ta"let was under lined recently
when 4uropean 8harmacopoeia adopted the term =Oro+dispersi"le Ta"let> as a ta"let that to
"e placed in the mouth where it disperses rapidly "efore swallowing
,
compression Method ] Page "
INTRODUCTION
1,B)/) BASIC A--ROAC4ES TO DE1ELO- "DTS
The fast+dissol#ing property of the .DTs is attri"uted to $uic& ingress of water into
ta"let matri' resulting in rapid disintegration! 5ence, the "asic approaches to de#elop mouth
dissol#ing ta"lets include
%-
@
.a'imi2ing the porous structure of the ta"let matri'!
Incorporating the appropriate disintegrating agent?agents!
Using highly water+solu"le e'cipients in the formulation!
1,B) / v) +ossble benefts of o$all) dsnteg$atng d$#gs,
Cln!al:
Impro#ed drug a"sorption!
0aster onset of action!
.inimi2ed first pass effect!
Impro#ed "ioa#aila"ility!
"ed!nal:
No ta"let or capsule to swallow or chew!
,etter taste, no water needed!
Impro#ed safety and efficacy!
Impro#ed compliance!
Te!%n!al:
.ore accurate dosing than li$uid products!
Can use sugars and other e'cipients that are generally recogni2ed as safe!
Impro#ed sta"ility "ecause of unit+dose pac&aging!
.anufactured with common process and con#entional e$uipment!

B#sness:
/ifecycle .anagement@ re+formulation is a strategy to prolong mar&et e'clusi#ity as
it may delay or reduce generic erosion at patent e'piry!
Differentiation in a crowded mar&et
3alue+added product line e'tension
compression Method ] Page #
INTRODUCTION
0or generic companies it offer the prospect of superior generic drugs in order to gain
mar&et dominance upon the e'piration of patents
Cost effecti#e drug de#elopment!
1, C) Salent feat#$e of fast dssolvng D$#g Delve$) S)ste*
%D,1<
%! 4ase of administration for patients who are mentally ill, disa"led and uncooperati#e!
1! Re$uires no water
*! :uic& disintegration and dissolution of the dosage form!
-! O#ercomes unaccepta"le taste of the drugs!
7! Can "e designed to lea#e minimal or no residue in the mouth after administration and

also to pro#ide a pleasant mouth feel!

E! Allows high drug loading!

D! A"ility to pro#ide ad#antages of li$uid medication in the form of solid preparation!
;! Adapta"le and amena"le to e'isting processing and pac&aging machinery
1, D) C%a$a!te$st!s of 0ast Dssolvng Delve$) S)ste*s
1<
:
&/ Ease of ad*nst$aton:
0ast Dissol#ing Deli#ery (ystems are easy to administer and handle hence,
leads to "etter patient compliance! Usually, elderly people e'perience difficulty in swallowing
the con#entional dosage forms (ta"lets, capsules, solutions and suspensions "ecause of
tremors of e'tremities and dysphasia! 0ast Dissol#ing Deli#ery (ystems may offer a solution
for these pro"lems!
&/"o#t% feel:
.outh feel is critical, and patients should recei#e a product that feels pleasant!
Any large particles from the disintegrating ta"let that are insolu"le or slowly solu"le in sali#a
would lead to an unpleasant gritty feeling! This can "e o#ercome "y &eeping the maFority of
the particles "elow the detecta"le si2e limit! In some cases, certain fla#ors can im"i"e an
impro#ed mouth feel perception, resulting in a product that is percei#ed as "eing less gritty,
compression Method ] Page $
INTRODUCTION
e#en if the only change is the fla#our ! 4ffer#escence can "e added to aid disintegration and
impro#e mouth feel "y reducing the =dryness% of a product&
& Taste of t%e "ed!a*ent
As most drugs are unpalata"le, mouth dissol#ing deli#ery systems usually
contain the medicament in taste mas&ed form! Deli#ery systems dissol#e or disintegrate in
patientBs mouth, thus releasing the acti#e ingredients which come in contact with the taste
"uds and hence, taste mas&ing of the drugs "ecomes critical to patient compliance!
v& / 4)g$os!o+!t):
(e#eral fast dissol#ing dosage forms are hygroscopic and cannot maintain
physical integrity under normal condition from humidity which calls for speciali2ed product
pac&aging!
v&/0$ablt):
In order to allow fast dissol#ing ta"lets to dissol#e in the mouth, they are
made of either #ery porous or soft+ moulded matrices or compressed into ta"lets with #ery
low compression force, which ma&es the ta"lets fria"le and?or "rittle, which are difficult to
handle, often re$uiring speciali2ed peel+off "lister pac&aging! To o#ercome this pro"lem,
some companies introduced more ro"ust forms of fast dissol#ing ta"lets! such as 6owta" "y
Gamanouchi+(ha&lee and Durasol# "y CI.A la"s!
1, E) "e!%ans* of tablet dsnteg$ants
%D, *%
The ta"let "rea&s to primary particles "y one or more of the mechanisms listed "elow@+
I! ,y capillary action
II! ,y swelling
III! ,ecause of heat of wetting
I3! Due to disintegrating particle?particle repulsi#e forces
3! Due to deformation
compression Method ] Page 1'
INTRODUCTION
3I! Due to release of gases
3II! ,y en2ymatic action
I) B) !a+lla$) a!ton:
Disintegration "y capillary action is always the first step! 6hen we put the ta"let into suita"le
a$ueous medium, the medium penetrates into the ta"let and replaces the air adsor"ed on the
particles, which wea&ens the intermolecular "ond and "rea&s the ta"let into fine particles!
6ater upta&e "y ta"let depends upon hydrophilicity of the drug ?e'cipient and on ta"leting
conditions! 0or these types of disintegrants maintenance of porous structure and low
interfacial tension towards a$ueous fluid is necessary which helps in disintegration "y
creating a hydrophilic networ& around the drug particles!
II) B) s5ellng:
8erhaps the most widely accepted general mechanism of action for ta"let
disintegration is swelling Ta"lets with high porosity show poor disintegration due to lac& of
ade$uate swelling force! On the other hand, sufficient swelling force is e'erted in the ta"let
with low porosity! It is worthwhile to note that if the pac&ing fraction is #ery high, fluid is
una"le to penetrate in the ta"let and disintegration is again slows down!
0g,no,1,2: Dsnteg$aton of tablet b) 5!6ng and s5ellng
INTRODUCTION
III) Be!a#se of %eat of 5ettng (a$ e7+anson)
6hen disintegrants with e'othermic properties gets wetted, locali2ed stress is
generated due to capillary air e'pansion, which helps in disintegration of ta"let! This
e'planation, howe#er, is limited to only a few types of disintegrants and cannot descri"e the
action of most modern disintegrating agents!
I1) D#e to dsnteg$atng +a$t!le 2 +a$t!le $e+#lsve fo$!es
Another mechanism of disintegration attempts to e'plain the swelling of ta"let
made with Hnon+swella"leB disintegrants! 9uyot+5ermann has proposed a particle repulsion
theory "ased On the o"ser#ation that non+swelling particle also cause disintegration of
ta"let! The electric Repulsi#e force "etween particle are the mechanism of disintegration and
water is re$uired for it! Researchers found that repulsion is secondary to wic&ing!
1) D#e to defo$*aton,
5ess had pro#ed that during ta"let compression, disintegranted particles get
deformed and these deformed particles get into their normal structure when they come in
contact with a$ueous media or water! Occasionally, the swelling capacity of starch was
impro#ed when granules were e'tensi#ely deformed during compression! This increase in
si2e of the deformed particles produces a "rea& up of the ta"let! This may "e a mechanism of
starch and has only recently "egun to "e studied!
INTRODUCTION
0g,1, 8, Dsnteg$aton b) defo$*aton and $e+#lson
1I) D#e to $elease of gases
Car"on dio'ide released within ta"lets on wetting due to interaction "etween
"icar"onate and car"onate with citric acid or tartaric acid! The ta"let disintegrates due to
generation of pressure within the ta"let! This effer#escent mi'ture is used when pharmacist
needs to formulate #ery rapidly dissol#ing ta"lets or fast disintegrating ta"let! As these
disintegrants are highly sensiti#e to small changes in humidity le#el and temperature ,strict
control of en#ironment is re$uired during manufacturing of the ta"lets !The effer#escent
"lend is either added immediately prior to compression or can "e added in to two separate
fraction of formulation!
1II) B) en9)*at! $ea!ton
5ere, en2ymes presents in the "ody act as disintegrants! These en2ymes
destroy the "inding action of "inder and helps in disintegration!
1,2) 0#nda*entals of fast dssolvng 2 dsnteg$atng tablets:
INTRODUCTION
0or rapid dissolution or disintegration of dosage form, water must
rapidly penetrate into the ta"let matri' to cause $uic& disintegration ) instantaneous
dissolution of the ta"let! (e#eral techni$ues are used to achie#e these fundamentals, to
formulate mouth+dissol#ing ta"let! (ome of the techni$ues are descri"ed "elow!
: Te!%nologes e*+lo)ed fo$ t%e *o#t% dssolvng tablets
%D, %;, *%
@
I! .olding
II! Direct compression method!
III! 0ree2e drying technology (2ydis technology
I3! (pray Drying
3! (u"limation technology!
3I! (ugar "ased e'cipients!
I &/Tablet "oldng
;,%1,%D;*%
:
In this technology, water+solu"le ingredients are used so that ta"let disintegrate
and dissol#e rapidly! The powder "lend is moistened with a hydro alcoholic sol#ent and is
molded in to ta"let using compression pressure lower than used in con#entional ta"lets
compression! The sol#ent is then remo#ed "y air+drying! .olded ta"lets ha#e a porous
structure that enhances dissolution! Two pro"lems commonly encountered are mechanical
strength and poor taste mas&ing characteristics! Using "inding agents such as sucrose, acacia
or poly #inyl pyrrolidone can increase the mechanical strength of the ta"let!
To o#ercome poor taste mas&ing characteristic 3an (coi&! incorporated drug
containing discrete particles, which were formed "y spray congealing a molten mi'ture of
hydrogenated cottonseed oil, sodium "icar"onate, lecithin, polyethylene glycol and acti#e
ingredient into a lactose "ased ta"let triturate form! Ta"lets prepared "y this method are solid
dispersions! 8hysical form of drug in the ta"lets depends on whether and to what e'tent it
dissol#es in the wetted mass! The drug can e'ist as discrete particles or micro particles in the
matri'! Different moulding techni$ues can "e used to prepare mouth+dissol#ing ta"lets@
a, Co*+$esson *o#ldng: The powder mi'ture pre#iously wetted with a sol#ent i&e
ethanol?water is compressed into mould plates to form a wetted mass!
b, 4eat *o#ldng: A molten matri' in which drug is dissol#ed or dispersed can "e directly
moulded into orodispersa"le Ta"lets!
INTRODUCTION
!, No va!##* l)o+%l9aton: This process in#ol#es e#aporation of sol#ent from a drug
solution or suspention at a standard pressure!
.oulded ta"lets posess porous structure, which facilitates rapid disintegration and
easy dissolution! .oulded ta"lets offer impro#ed taste due to water+solu"le sugars present in
dispersion matri'! ,ut moulded ta"lets lac& good mechanical strength and can undergo
"rea&age or erosion during handling and opening of "lister pac&s!

5owe#er, adding sucrose,
acacia or poly#inyl pyrrolidone can increase mechanical strength!
II &/D$e!t Co*+$esson "et%od
%D,1<
:
It is the easiest way to manufacture ta"lets! Con#entional e$uipment, commonly
a#aila"le e'cipients and a limited num"er of processing steps are in#ol#ed in direct
compression! Also high doses can "e accommodated and final weight of ta"let can easily
e'ceed that of other production methods! Directly compressed ta"letIs disintegration and
solu"ilisation depends on single or com"ined action of disintegrates, water solu"le e'cipients
and effer#escent agent! Disintegrate efficacy is strongly affected "y ta"let si2e and hardness!
/arge and hard ta"lets ha#e disintegration time more than that usually re$uired! As
conse$uences, products with optimal disintegration properties often ha#e medium to small
si2e and ?or high fria"ility and low hardness! ,rea&age of ta"let edges during handling and
ta"let rupture during the opening of "lister al#eolus, all result from insufficient physical
resistance!
Disintegrants ha#e maFor role in the disintegration and dissolution process of .outh
Dissol#ing Ta"lets made "y direct compression! To ensure a high dis+ integration rate, choice
of suita"le type and an optimal amount of disintegrant is important! Other formulation
components such as water solu"le e'cipients or effer#escent agents can further enhance
dissolution or disintegration properties! ,ut main draw"ac& of using effer#escent e'cipients
is their highly hygroscopic nature!
The understanding of disintegrant properties and their effect on formulation has ad#anced
during last few years, particularly regarding so called super+disintegrants! Disintegration
efficiency is "ased on force e$ui#alent concept, which is the com"ined measurement of
swelling force de#elopment and amount of water a"sorption! 0orce e$ui#alent e'presses the
capa"ility of disintegrant to transform a"sor"ed water into swelling force! The optimi2ation
of ta"let disintegration was defined "y means of disintegrant critical concentration! ,elow
INTRODUCTION
this concentration, the ta"let disintegration time is in#ersely proportional to disintegrate
concentration and a"o#e that disintegration time remains appro'imately constant or e#en
increases
0g#$e 1,<@
Conceptual diagram of disintegration of ta"let "y disintegranting
III &/0$ee9e D$)ng Te!%nolog) (=)ds Te!%nolog))
%;,*%
/yophili2ation can "e used to prepare ta"lets that ha#e #ery porous open
matri' networ& into which sali#a rapidly mo#es to disintegrate lyophili2ed mass after it is
placed in mouth!
The drug is entrapped in a water solu"le matri' which is free2e dried to produce a unit which
rapidly disperses when placed in mouth! Apart from the matri' and acti#e constituents, the
final formulation may contain other e'cipients, which impro#e the process characteristics or
enhance the $uality of final product! These include suspending agents, wetting agents,
preser#ati#es, antio'idants, colors and fla#ors! The preferred drug characteristics for free2e
drying formulations are water insolu"le, low dose, chemically sta"le, small particle si2e and
tasteless!
Cor#eleyn and Remon in#estigated the influence of #arious formulation and process
parameters on the characteristics of rapidly disintegrating ta"lets in lyophili2ed form using
hydrochlorthia2ide as a model drug! They ha#e concluded that maltod'trins are useful in the
formulation of fast dissol#ing ta"lets made "y free2e+drying!
compression Method ] Page 1!
INTRODUCTION
/yophili2ation is relati#ely e'pensi#e and time consuming manufacturing process! Other
draw"ac& includes fragility, which ma&e the use of con#entional pac&ing difficult and poor
sta"ility during storage under stressful condition!
I1&/S+$a) D$)ng
;, %1, %;
(pray dryers are widely used in pharmaceuticals and "iochemical processes!
Due to processing sol#ent is e#aporated rapidlyA spray drying can produce highly porous, fine
powder! (pray drying can "e used to prepare rapidly disintegrating ta"lets! This techni$ue is
"ased on a particulate support matri', which is prepared "y spray drying an a$ueous
composition containing support matri' and other components to forma highly porous and fine
powder! This is then mi'ed with acti#e ingredients and compressed into ta"lets!
Allen et al used a spray drying techni$ue to prepare fast dissol#ing ta"lets! The ta"lets made
from this technology are claimed to disintegrate within 1< seconds!
1 &/S#bl*aton Te!%nolog)
%;
The "asis of this techni$ue is to add inert solid ingredients that #olatili2e
readily, (e!g! camphor, ammonium "icar"onate, naphthalene, urea, urethane etc to other
ta"let e'cipients and the mi'ture is then compressed into ta"lets! 3olatile material is then
remo#ed #ia su"limation, which generate a porous structure!
Joi2umi et al applied the su"limation techni$ue to prepare highly porous compressed ta"lets
that were rapidly solu"le in sali#a! .annitol and camphor were used as a ta"let matri'
material and su"liming the material respecti#ely! Camphor was iminated "y su"liming in
#acuum at ;<
<
C for *< minutes to de#elop pores in the ta"lets!
.a&ino et al descri"ed a method of producing a fast dissol#ing ta"let using water as a pore
forming material! A mi'ture containing acti#e ingredient and car"ohydrates (glucose,
manitol, 'ylitol etc were moistened with water (%+ * Kw?w and compressed into ta"lets!
The water was then remo#ed yielding highly porous ta"let that e'hi"ited e'cellent A
compression Method ] Page 1"
INTRODUCTION
0g No 1,> Ste+s nvolved n S#bl*aton Te!%nolog)
1I &/S#ga$ Based E7!+ents
%;
(ugar "ased e'cipients e!g! sor"itol, manitol, de'trose, 'ylitol, fructose,
maltose etc! ha#e "een used as a "ul&ing agents! ,ecause of their high a$ueous solu"ility and
sweetness, which impart a pleasant mouth feel and good taste mas&ing properties, can "e
used to formulate sugar+"ased mouth dissol#ing ta"let! 5owe#er, not all sugar+"ased material
ha#e fast dissolution rate and good compressi"ility!
Table No 1,2: Co**e$tall) avalable *o#t% dssolvng tablets:
t$ade na*e a!tve ng$edent Catego$) *an#fa!t#$e$
8epcid R8D 0amotidine Antihistamine .erc& ) Co!,NL,U(A
Nimulid .DT Nimesulide Antipyretic 8anacea ,iotech,New+Delhi,India
Romilast .ontelu&ast Antiasthamatic Ran"a'y /a"s /td, New Delhi, India!
Olane' Insta" Olan2apine Antipsychotic Ran"a'y /a"s /td!New Delhi India!
A maFor component of success in orally disintegrating ta"lets (ODT is good taste! If the
product does not taste good, patients and physicians will find another ODT or other product
that does taste good! ODT technology is relati#ely new to the industry and has had a
significant impact on patients of all ages!
1,8, (USTATION: SENSE O0 TASTE
compression Method ] Page 1#
INTRODUCTION
Taste is mainly a function of the taste buds in the mouth, "ut it is common
e'perience that oneBs sense of smell contri"utes strongly to taste perception! In addition the
te'ture of the food, as detected "y tactual senses of the mouth, greatly conditions the taste
e'perience
11
! There are fi#e primary tastes, which can "e distinguished as@ sweet, sour, salty,
bitter and umani. Chochlate, pepper and coffee, these fla#ours are com"inations of the fi#e
primary tastes, plus accompanying olfactory and tactile (touch sensations
1*
!
Anato*) of Taste B#ds and -a+llae
0igure %!E@8apillae and taste "uds
The receptors for sensation of taste are located into the taste "uds! The
nearly %<,<<< taste "uds of a young adult ate mainly on the tongue, "ut they are also found on
the soft palate ("ac& portion of roof of mouth, laryn' and pharyn'! The num"er of taste "uds
decline with age! 4ach taste "ud is an o#al "ody consisting of three &inds of epithelial cells!
The supporting cells form a capsuleA inside are a"out 7< gustatory receptor cells! A single,
hair li&e gustatory receptor cell to the e'ternal surface through the taste pore! ,asal cells are
found at the periphery of the taste "ud near the connecti#e tissue layer! These epithelial cells
produce supporting cells, which then de#elop into gustatory receptor ells that ha#e life span
of a"out %< days! At their "ase, the receptor cells synapse with dendrites of sensory ner#e
fi"res that form the first part of the gustatory pathway!
Taste "uds are found in ele#ation on the tongue called papillae! The papillae gi#e the
upper surface of the tongue its rough appearance! Circum#allate papillae, the largest type, are
circular and form an in#erted 3+ shaped row at the posterior portion of the tongue! 0ungiform
compression Method ] Page 1$
INTRODUCTION
papillae are &no"li&e ele#ations found primarily on the tip and sides of the tongue! All
cicum#allate and most fungiform papillae contain taste "uds!
1,8,(a) -%)solog) of (#staton
17
Chemicals that stimulate gustatory receptor cells are &nown as tastants!
Once a chemical is dissol#ed in sali#a, it can ma&e contact with the plasma mem"rane of the
gustatory hairs, which ate the presumed site of taste transduction! The result is a receptor
potential, which is thought to cause the release of neurotransmitter "y e'ocytose of synaptic
#esicles within gustatory receptor cells! Ner#e impulses first arise in the neurons that synapse
with gustatory receptor cells!
The sodium ions (Na
M
in a salty food enter gustatory receptor cells #ia NaN channels
in the plasma mem"rane! The accumulation of NaM inside causes depolari2ation, which opens
Ca1M channels! In turn, inflow of ca1M triggers e'ocytosis of synaptic #esicles and li"eration
of neurotransmitter! The hydrogen ions in sour tastants may flow into opening and closing of
other types of ion channels!
Other tastants, responsi"le for stimulating sweet, "itter and umani tastes, do not themsel#es
enter gustatory receptor cells! Rather they "ind to receptor on the plasmamem"rane that is
lin&ed to 9 protein!
0g#$e 1,?: .echanism of taste perception
1E
1,8,(b) T%e (#stato$) -at%5a)
1D
Three cranial ner#es include a'on of first+order gustatory neurons from
taste "uds! The facial ner#e ser#ers the anterior two+third of the tongue, the glossopharyngeal
ner#e ser#es the posterior one Othird of the tongue, and the #agus ner#e ser#es the throat and
epiglottis! 0rom taste "uds, impulse propagates along this cranial ner#e to the medulla
INTRODUCTION
o"longata! 0rom the medulla, some a'ons carrying taste signal proFect to the lim"ic system
and the hypothalamus, whereas others proFect from the thalamus to the primary gustatory area
in the parietal lo"e of thee cere"ral corte' gi#e rise to the conscious perception of taste!
1,<) TASTE
Taste is an important parameter in administering drugs orally! Undesira"le taste is
one of the important formulation pro"lems that are encountered with many drugs!
Administration of "itter drugs orally with accepta"le le#el of palata"ility is a &ey issue for
health care pro#iders! 8ro#en methods for "itterness reduction and inhi"ition ha#e resulted in
impro#ed palata"ility of oral pharmaceuticals!
1*
The "iological definition of taste (gustation is a chemical reaction deri#ed from
sensory responses from the four main taste perceptions@ salt, sour, "itter, and sweet! Two
other perceptions (umami and trigeminal should "e included when considering taste! Umami
is deri#ed from the presence of glutamate, such as monosodium glutamate, resulting in the
fullness sensation from certain foods! Trigeminal is the "urning sensation deri#ed from such
foods as spices and peppers! 0igure % shows the location of the sensors for these si'
perceptions around the tongue!
Fig.1.8 Location of sensors.
(mell (olfaction contri"utes significantly to the taste of something! This is
due to aromas "eing released into the nasal passages as food is "eing chewed! The "rain
interprets the com"ined signals from "oth the nasal passages and the taste "uds into one
taste?fla#or response! The human tongue is pac&ed with ner#es, and many of these detect
INTRODUCTION
su"tle differences in the consistency of the food "eing masticated! 6hether the food is
creamy, rough, granular, or stic&y, the tongue is a master in differentiating those
characteristics! Conse$uently, changing the fla#or to something new may act against the
product, e#en if the effecti#eness is the same!
TASTE "AS@IN(
Worst te taste of te medication, te better te cure! was once the pre#ailing
attitude
1;
! Today this trend has changed and great importance is gi#en to the organoleptic
characteristics of pharmaceutical products i!e! mainly appearance, odor and taste! .as&ing
the unpleasant taste of a drug impro#es the compliance of the patient and product #alue!
Administration of a drug orally ha#ing "itter and o"no'ious taste with accepta"le le#el of
palata"ility is a challenge to the pharmacist in the present world, especially in paediatric and
geriatric formulation! Thus taste mas&ing in the present day pharmaceutical industry has
"ecome a potential tool to impro#e patient compliance and commercial success of the
product!
0ormulationBs organoleptic properties i!e!taste ,mouth feel and appearance are of considera"le
importance in differentiating products in the mar&et and can ultimately determine the success,
or otherwise, of a product!
.ore than 7<K of the pharmaceutical products are administered orally for se#eral
reasons, of which "etter patient compliance and e'istence of highly de#eloped technology are
most important!
Taste mas"ing is defined as a percei#ed reduction of an undesirable taste tat would
oterwise e$ist.

Recent years ha#e seen a tremendous progress in the techni$ue of mas&ing the
unaccepta"le taste of orally administered pharmaceuticals, such as filling in capsules,
con#entional granulation, coating with water insolu"le polymers or p5 dependent water
solu"le polymer, adsorption on ion+e'change resin , micro encapsulation with #arious
polymers comple'ing with cyclode'trin, chemical modification such as use of insolu"le
prodrugs , effer#escent systems, salt formation, free2e drying process, multiple emulsions,
liposomes and use of e'cipients li&e fla#ors, sweeteners, gelatin, gelatini2ed starch, lecithin
li&e su"stances and surfactants

!

INTRODUCTION
8harmaceutical companies are commercially moti#ated to in#est time, money and resources
in de#eloping palata"le, pleasant tasting products "ecause good tasting products
*;
@
4nhance patient compliance
8ro#ide a competiti#e ad#antage when a therapeutic category is crowded with
similar products e!g! anti+infecti#e category etc!
8ro#ide "rand recognition to com"at pri#ate+la"el competition!
Taste mas&ing technologies rely on pre#enting interaction "etween the drug molecule
and the oral mucosal surface! ,y creating a physical "arrier around each particle, drug
su"stance can "e pre#ented from going into solution and interacting directly with taste
receptors!
In the pharmaceutical industry, taste+mas&ing science "roadly co#ers physiological
and physicochemical approaches to pre#ent Acti#e 8harmaceutical Ingredient (A8I or drugs
from interacting with taste "udsA there"y eliminating or reducing negati#e sensory response!
1,>) (ene$al a++$oa!%es to taste *as6ng
*%, *P, -<, -1
a) 0lavo#$ng as a *eans of taste *as6ng
Addition of fla#ours and sweeteners is the foremost and simplest
approach for taste mas&ing especially in the case of paediatric formulations! This approach is
howe#er not #ery successful for highly "itter and highly water solu"le drugs! ,esides taste
mas&ing, this approach is also used to impro#e the aesthetic appeal of the product especially
to ma&e it more attracti#e for the paediatric patients as well as used for the li$uid
formulations and the chewa"le ta"lets!
b) Taste *as6ng #sng s5eetene$s
(weeteners play an important role in taste mas&ing of "itter su"stances!
Aspartame is a prominent sweetener for "itterness reduction! A concentration of as small as
<!;K was effecti#e in reducing the "itterness of Acetaminophen! (tarch, lactose and mannitol
are diluents &nown for their taste mas&ing characteristics! Artificial sweetener li&e
neohesperidine dihydrochalcone, which is a "itterness suppressor and fla#our modifier, elicits
a #ery intense sweet tasteA hesperidine dihydrochalcone -B+Q+D+glucoside has the a"ility to
reduce the perception of "itterness!
!) Taste *as6ng b) n%btng btte$ness
INTRODUCTION
/ipoproteins composed of phosphatidic acid and "eta+lacto glo"ulin
were effecti#e in suppressing the "itter taste of drugs such as caffeine, propranolol,
prometha2ine and $uinine! The salty taste of sodium chloride and sweet taste of sucrose were
not inhi"ited "y the lipoproteins! The addition of phosphorylated amino acids such as
phosphotyrosine and phosphoserine to mi'tures of I"uprofen, Acetaminophen,
De'tromethorphan hydrochloride, 8seudoephedrine hydrochloride and Chlorpheniramine
maleate inhi"ited the unpleasant taste of drugs without su"stantially affecting the o#erall true
taste of the formulations!
d) Taste *as6ng b) !oatng
-1
Coating is an e'tremely useful techni$ue for a num"er of applications
in the pharmaceutical field! Although it is used primarily for production of sustained release,
gastro+resistant dosage forms, it also has maFor application in mas&ing the unpleasant taste!
.erely applying thic&er layer of coating material can "e ineffecti#e in taste mas&ing of
certain drugs with o"Fectiona"le taste! Thic& coating can cause pro"lems "oth in terms of si2e
and coat apart from "eing pro"lematic in getting the desired release profile of the drug! Taste
mas&ing of I"uprofen has "een successfully achie#ed "y using the air suspension coating
techni$ue to form microcapsules, which comprises of a pharmaceutical core of crystalline
I"uprofen and a methacrylic acid copolymer coating that pro#ides chewa"le taste mas&ed
characteristics! The methacrylic acid copolymer has a rapid rate of dissolution at a p5 of
a"out 7!7!
e) Taste *as6ng b) $%eolog!al *odf!aton
-1
A$ueous dispersions of gums such as acacia, tragacanth, 'anthan gum or
synthetic polymers such as polyethylene glycols, hydro'ypropyl methyl cellulose, hydro'yl
ethyl cellulose, are used to increase the #iscosity, which lowers diffusion of "itter su"stances
from the sali#a to the taste "uds! Com"ination of polyethylene glycol (849 and sodium
car"o'y methyl cellulose (Na+C.C were used to mas& the unpleasant taste of drugs such as
guaifenesin, pseudoephedrine hydrochloride, de'tromethorphan and I"uprofen!
f) Taste *as6ng b) salt +$e+a$aton o$ f#n!tonal g$o#+ *odf!aton
This approach in#ol#es taste mas&ing of the "itter drugs "y either
decreasing solu"ility or "y increasing hydropho"icity and there"y reducing contact of "itter
drugs with the taste "uds! This approach differs from others in that attempt is made to modify
the chemical composition of the drug su"stance itself, so as to render it less solu"le in sali#a
INTRODUCTION
and there"y less stimulating to the taste "uds, or to o"tain a tasteless or less "itter form! The
al&ylo'yal&yl car"onates of Clarithromycin ha#e remar&a"ly reduced!
g) Taste *as6ng b) n!l#son !o*+le7aton
In inclusion comple' formation, the drug molecule fits into the ca#ity of
a comple'ing agent i!e! the host molecule forming a sta"le comple'! The comple'ing agent is
capa"le of mas&ing the "itter taste of drug "y either decreasing its oral solu"ility on ingestion
or decreasing the amount of drug particles e'posed to taste "uds, there"y reducing the
perception of "itter taste! 3an der 6aals forces are mainly in#ol#ed in inclusion comple'es!
R+Cyclode'trin is most widely used comple'ing agent for inclusion type comple'es! It is
sweet, nonto'ic, cyclic oligosaccharide o"tained from starch!
%) Taste abate*ent b) Ion E7!%ange Resns
-1
.ost of the "itter drugs ha#e nitrogen atom and amine as a functional
group, which is the cause of their o"no'ious taste! If the nitrogen atom and functional groups
are "loc&ed "y comple' formation the "itterness of the drug reduces drastically!
8harmaceutical industry has done this type of comple' formation "y con#erting the drug to
stearates and estolate! ,ut now days the use of ion e'change resin is done to "loc& the
functional group responsi"le for causing the "itter taste "y forming comple' "etween ion
e'change resin and the drug! 0urther "ecause of the comple', the drug doesnBt release in the
sali#a! Thus the resin reduces the drug and taste "uds interaction!
A drug@ resin comple' is made from the "itter drugs ) ion + e'change resins!
The nature of the drug@ resin comple' is such that the a#erage p5 of E!D and Cation
concentration of a"out -< me$? lit in sali#a are not a"le to "rea& the drug@ resin comple' "ut
it is wea& enough to "e "ro&en down "y the hydrochloric acid present in the stomach! Thus
the drug@ resin comple' is a"solutely tasteless and sta"le, with no after taste, "ut at the same
time its "ioa#aila"ility is not affected!
6ith taste mas&ing technology it is possi"le to ma&e ITasteless Drug@ resin Comple'I
of #arious "itter drugs and can "e used these drug@ resin comple' in formulating not only the
con#entional dosage forms li&e ta"lets and capsules, "ut also other dosage forms li&e
dispersi"le ta"lets, chewa"le ta"lets and oral suspensions!
1,. ) ION/EAC4AN(E RESIN (IER)
INTRODUCTION
Ion e'change can "e define as a re#ersi"le process in which ions of li&e sign are
e'changed "etween li$uid and solid, a highly insolu"le "ody in contact with it
71
! Ion+
e'change resins are water+insolu"le, cross+lin&ed polymers containing co#alently "ound
salt forming groups in repeating positions on the polymer chain!
7*
Ion e'change resin may "e define as a special type of a polyelectrolyte and consists of free
dimensional polymeric hydrocar"on networ& to which are "onded a large num"er of
electrically charged groups, such as O(O
*
+
((ulphonate group or a ON(C5
*
-
M
(:uarernary
ammonium group!
7-
The most common properties of all ion e'changers which ha#e "een
used&
They are almost insolu"le in water and organic sol#ents, li&e "en2ene,
car"on tetrachloride, ether, etc!
They are comple' in nature and in fact they are polymeric!
They contain acti#e of counter ions that will e'change re#ersi"ility
with other ions in a surrounding solution without any su"stantial change in
the materials!

0igure %!P@ Classf!aton of Ion E7!%ange Resns
>
1,.,a) T%eo$) of on e7!%ange :
compression Method ] Page 2!
INTRODUCTION
Ion e'change is a stoichiometric process in which any counter ions that lea#e the
ion e'change are replaced "y an e$ui#alent amount of other counter ions! This is a
conse$uence of the electro neutrality re$uirement! The ion e'change is essentially a
diffusion process, "ut also has relation to chemical reaction &inetics! Usually the ion
e'changers are selecti#eA they ta&e up some counter ions in preference to others! The rate+
determining step in ion e'change is diffusion either within the ion+e'changer itself or in
the diffusion "oundary layer! Rechen"erg proposed that at low concentration of counter
ion, the rate of e'change is controlled "y film diffusion and at high concentrations "y
particle diffusion! The e$uili"rium distri"ution of the drug species "etween the resin and
e'ternal solution phases results from "oth electrostatic and hydropho"ic interactions! In the
ion e'change resins the ions are &nown to "ind to the ion+e'changer "y two mechanisms!
Drug in an ionic form (usually in solution is mi'ed with the appropriate I4R to
form a comple' , &nown as HresinateB! The performance of resinate is go#erned "y se#eral
factor, such as
--@
p5 and temperature of the drug solution
.olecular weight and charge intensity of the drug and I4R
.i'ing speed
Ionic strength of the drug solution
Degree of cross lin&ing and particle si2e of the I4R
Nature of sol#ent
Contact time "etween the drug species and the I4R
Drug release from Drug@ resin comple' (Resinate depends upon two factors
-1
@
%! The ionic en#ironment (i!e! p5 and electrolyte concentration within the
gastrointestinal tract!
1! The properties of resin

Drug molecules attached to the resins are released "y appropriate
charged ions in the gastrointestinal tract, followed "y diffusion of free drug molecules
out of the resin as shown "elow!
Resin
+
Drug
M
M S
M
T Resin
+
+++++S
M
M Drug
M
Resin
+
Drug
M
M G
M
T Resin
+
++++++G
M
M Drug
M
compression Method ] Page 2"
INTRODUCTION
6here S and G are ions in the gastrointestinal tract
0g#$e 1,1B: 0actors that affect I4R process in#ol#ed in the deli#ery of cationic drug
--
1,.,b) -$o+e$tes of Ion E7!%ange Resns
--
1, -a$t!le s9e: The rate of ion e'change reactions depends on the si2e of resin particles!
Decreasing the si2e significantly decreases the time re$uired for the reaction to reach
e$uili"rium with surrounding medium! I4Rs are a#aila"le in wide si2e range from 1 to *
mm spherical "eads to powder as fine as few microns!
2, -o$ost) and s5ellng: 8orosity is defined as the ratio of the #olume of the material to
its mass! The limiting si2e of ions that can penetrate into the resin matri' depends strongly
on the porosity, which depends mainly on the amount of cross +lin&ing agent, and also on
polymeri2ation process! (welling is directly proportional to num"er of hydrophilic
functional groups and in#ersely proportional to degree of cross+lin&ing!
8, C$oss/ln6ng: 8ercentage of cross+lin&ing affects purely physical structures of resin
particles! Resins with low cross+lin&ing can swell into structure that is soft and gelatinous
when ta&e up water, while resins with high cross lin&age are somewhat hard and "rittle!
<, Avalable !a+a!t): The capacity of an ion e'changer is a $uantitati#e measure of its
a"ility to ta&e up counter ions and is therefore of maFor importance! This depends mainly
on accessi"ility of the drug to the site of e'change!
compression Method ] Page 2#
INTRODUCTION
>, A!d base st$engt%: Resin containing sulfonic, phosphoric or car"o'ylic acid e'change
groups ha#e appro'imate pJa #alues of 1+*, -+E respecti#ely! Anionic e'changers are
$uaternary, tertiary or secondary ammonium groups ha#ing apparent pJa #alues of U%*, D+
P and 7 to P respecti#ely! Acid "ase strength is significant for the reason that the strength
of "ond and su"se$uent rate of release of drug depends on this strengthA also the p5
en#ironment needed for loading and release of drug can "e predicted!
., Sele!tvt) of $esn fo$ !o#nte$ on: (ince ion e'change in#ol#es electrostatic forces,
selecti#ity mainly depends on relati#e charge, and ionic radius of hydrated ions competing
for an e'change site and to some e'tent on hydropho"icity of competitor ion!
?, Stablt): The I4Rs are remar&a"ly inert su"stances! They are resistant to attac& "y
chemicals and heat to large e'tent! The limitation is degradation in presence of strong
gamma rays!
C, To7!t): The resins are insolu"le solids that are not a"sor"ed "y the "odyA hence, they
do not ha#e significant associated side effects or to'icity! 5owe#er, commercial products
canBt "e used as such as they contain impurities that can cause to'icity! Therefore careful
purification of resins is re$uired prior to treatment with drugs,
1,.,!) ED#lb$#* +%eno*enon
( drug can be loaded onto an ion-e)change resin by an
e)changing reaction* and hence a drug-resin comple) is formed& The
principal properties of these resins are their e'change capacity to e'change its insolu"le
ions with those in solution! (olu"le ions may "e remo#ed from the solution through
e'change with the counter ions a"sor"ed on the resin as illustrated in this e$uation@
Re+ (o*
+
Na
M
Drug
M
T Re+ (o*
+
Drug
M
M Na
M
Re+N (C5**cl
+
MDrug
M
T Re+N(C5**
M
+Drug
+
M cl
O
These are e$uili"rium reactions in which e'tent of e'change is go#erned "y the
relati#e affinity of the resin for particular ions! Relati#e affinity "etween ions may "e
e'pressed as a selecti#e coefficient deri#ed from the mass action e'pression as gi#en
"elow!
J
D.
N VDW
r
V.W
(
? VDW
(
V.W
r
compression Method ] Page 2$
INTRODUCTION
6here,
VDW
r
N drug concentration in resin!
V.W
(
N counter ion concentration in the solution!
VDW
(
N drug concentration in the solution
V.W
r
N counter ion concentration in resin!
1,.,d) E7!%ange !a+a!t)
The e'change capacity refers to num"er of ionic sites per unit weight of or #olume
of ion e'change resin (me$! per gram! The weight "asis #alue (me$! per gram is
generally much higher than the #olume "ased e'change capacity since the wet resin is
highly hydrated! The e'change capacity may limit the amount of drug that may "e
a"sor"ed on a resin and hence the potency of a comple'! Car"o'ylic acid resins are
deri#ed from the acrylic acid polymer and ha#e higher e'change capacities (a"out %< me$!
per gram than sulfonic acid (a"out - me$! per gram or amine resins "ecause of "ul&ier
ionic su"stitute and polystyrene matri'! Therefore, higher drug percentage may often "e
achie#ed with car"o'ylic acid resins!
1.7 ) Ion E7!%ange Resn : A++l!atons n D$#g Delve$) Resea$!%
%! Taste mas&ing
1! Ta"let disintegration
*! Drug sta"ili2ation
-! (ustained release
7! Targeted drug deli#ery
Table No, 1,8: Drugs taste mas&ed "y #arious grades of ion e'change resin
-1
!
Na*e of t%e d$#g
Ion e7!%ange $esn
Ciproflo'acin Indion+1*-
A2ithromycin Indion+1%-
Chloro$uine 8hosphate Indion+1*-
Oflo'acin Tulsion+**7
De'tromethorphan 5ydro"romide Indion+1*-
:uinine (ulphate Indion+1<-, Indion+1*-
Norflo'acin Indion+1<-
Ro'ithromycin Tulsion+**7
INTRODUCTION

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INTRODUCTION

.ore accurate dosing than li$uid products!

Impro#ed sta"ility "ecause of unit+dose pac&aging!

.anufactured with common process and con#entional e$uipment!

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