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AMYLUM

Starch is used as an excipient primarily in oral solid-dosage formulations where it is utilized


as a binder, diluent, and disintegrant As a diluent, starch is used for the preparation of
standardized triturates of colorants or potent drugs to facilitate subse!uent mixing or blending
processes in manufacturing operations Starch is also used in dry-filled capsule formulations
for "olume ad#ustment of the fill matrix$%&
'n tablet formulations, freshly prepared starch paste is used at a concentration of ()*(+ w,w
in tablet granulations as a binder Selection of the !uantity re!uired in a gi"en system is
determined by optimization studies, using parameters such as granule friability, tablet
friability, hardness, disintegration rate, and drug dissolution rate Starch is one of the most
commonly used tablet disintegrants at concentrations of -)%(+ w,w$*).& /owe"er,
unmodified starch does not compress well and tends to increase tablet friability and capping
if used in high concentrations 'n granulated formulations, about half the total starch content
is included in the granulation mixture and the balance as part of the final blend with the dried
granulation Also, when used as a disintegrant, starch exhibits type '' isotherms and has a
high specific surface for water sorption$%0& Starch has been in"estigated as an excipient in
no"el drug deli"ery systems for nasal,$%%,%*& oral,$%-)%1& periodontal,$%2& and other site-
specific deli"ery systems$%3,%.& Starch is also used in topical preparations4 for example, it is
widely used in dusting powders for its absorbency, and is used as a protecti"e co"ering in
ointment formulations applied to the s5in Starch mucilage has also been applied to the s5in
as an emollient, has formed the base of some enemas, and has been used in the treatment of
iodine poisoning 6herapeutically, rice starch-based solutions ha"e been used
in the pre"ention and treatment of dehydration due to acute diarrheal diseases
Mg S67A8A6
Magnesium stearate is widely used in cosmetics, foods, and pharmaceutical formulations 't
is primarily used as a lubricant in capsule and tablet manufacture at concentrations between
0*(+ and (0+ w,w 't is also used in barrier creams
Magnesium stearate is hydrophobic and may retard the dissolution of a drug from a solid
dosage form4 the lowest
possible concentration is therefore used in such formulations$()%0& 9apsule dissolution is
also sensiti"e to both the
amount of magnesium stearate in the formulation and the mixing time4 higher le"els of
magnesium stearate and long mixing times can result in the formation of hydrophobic powder
beds that do not disperse after the capsule shell dissol"es$%%,%*& An increase in the
coefficient of "ariation of mixing and a decrease in the dissolution rate ha"e been obser"ed
following blending of magnesium stearate with a tablet granulation 6ablet dissolution rate
and crushing strength decreased as the time of blending increased4 and magnesium stearate
may also increase tablet friability :lending times with magnesium stearate should therefore
be carefully controlled$%-)*.& 6he existence of "arious crystalline forms of magnesium
stearate has been established$-0)-;& A trihydrate, a dihydrate,
and an anhydrate ha"e been isolated,$(,-*,--,-(& and an amorphous form has been obser"ed
$-1& <hile the hydrate
forms are stable in the presence of moisture, the anhydrous form adsorbs moisture at relati"e
humidity up to (0+, and at higher humidities rehydrates to form the trihydrate 6he
anhydrate can be formed by drying either of the hydrates at %0(
o
9
't has not been conclusi"ely established which form of pure magnesium stearate possesses the
best lubricating properties$-%,-*,-1,-2& 9ommercial lots of magnesium stearate generally
consist of mixtures of crystalline forms$-*,-;,-1);0& :ecause of the possibility of
con"ersion of crystalline forms during heating, consideration should be gi"en to the
pretreatment conditions employed when determining physical properties of magnesium
stearate powders such as surface area
6here is e"idence to suggest that the hydrophobic nature of magnesium stearate can "ary
from batch to batch owing to the presence of water-soluble, surface-acti"e impurities such as
sodium stearate :atches containing "ery low concentrations of these impurities ha"e been
shown to retard the dissolution of a drug to a greater extent than when using batches that
contain higher le"els of impurities$;*& =ne study related lubricity to the fatty acid
composition $stearate > palmitate& of lubricant lots for tablet formulations based on
compaction data and tablet material properties$;2& /owe"er, other studies ha"e indicated
that fatty acid composition has no influence on lubricant acti"ity$-*& and high-purity
magnesium stearate was as effecti"e a lubricant as the commercial material$%0& Moisture
sorption at different relati"e humidities can result in morphological changes in the
magnesium stearate
LA96=SA
Anhydrous lactose is widely used in direct compression tableting applications and as a tablet
and capsule filler and binder Anhydrous lactose can be used with moisture-sensiti"e drugs
due to its low moisture content
Lactose is widely used as a filler or diluent in tablets and capsules, and to a more limited
extent in lyophilized products and infant formulas$%)%-& Lactose is also used as a diluent in
dry-powder inhalation$%;)%1& ?arious lactose grades are commercially a"ailable that ha"e
different physical properties such as particle size distribution and flow characteristics 6his
permits the selection of the most suitable material for a particular application4 for example,
the particle size range selected for capsules is often dependent on the type of encapsulating
machine used Usually, fine grades of lactose are used in the preparation of tablets by the wet-
granulation
method or when milling during processing is carried out, since the fine size permits better
mixing with other formulation ingredients and utilizes the binder more efficiently =ther
applications of lactose include use in lyophilized products, where lactose is added to freeze-
dried solutions to increase plug size and aid cohesion Lactose is also used in combination
with sucrose $approximately % > -& to prepare sugar-coating solutions
@irect-compression grades of lactose monohydrate are a"ailable as granulated,agglomerated
a-lactose monohydrate, containing small amounts of anhydrous lactose @irect-compression
grades are often used to carry lower !uantities of drug and this permits tablets to be made
without granulation =ther directly compressible lactoses are spray-dried lactose and
anhydrous lactose
A?A
Although po"idone is used in a "ariety of pharmaceutical formulations, it is primarily used in
solid-dosage forms 'n tableting, po"idone solutions are used as binders in wetgranulation
processes$*,-& Ao"idone is also added to powder blends in the dry form and granulated in
situ by the addition of water, alcohol, or hydroalcoholic solutions Ao"idone is used as a
solubilizer in oral and parenteral formulations and has been shown to enhance dissolution of
poorly soluble drugs from solid-dosage forms$;)1& Ao"idone solutions may also be used as
coating agents
Ao"idone is additionally used as a suspending, stabilizing, or "iscosity-increasing agent in a
number of topical and oral suspensions and solutions 6he solubility of a number of poorly
soluble acti"e drugs may be increased by mixing with po"idone
Special grades of pyrogen-free po"idone are a"ailable and ha"e been used in parenteral
formulations4
Ao"idone has been used in pharmaceutical formulations for many years, being first used in
the %.;0s as a plasma expander, although it has now been superseded for this purpose by
dextran$3& Ao"idone is widely used as an excipient, particularly in oral tablets and solutions
<hen consumed orally, po"idone may be regarded as essentially nontoxic since it is not
absorbed from the gastrointestinal tract or mucous membranes$3& Ao"idone additionally has
no irritant effect on the s5in and causes no sensitization 8eports of ad"erse reactions to
po"idone primarily concern the formation of subcutaneous granulomas at the in#ection site of
intramuscular in#ections formulated with po"idone$.& 7"idence also exists that po"idone
may accumulate in the organs of the body following intramuscular in#ection$%0& A temporary
acceptable daily inta5e for po"idone has been set by the </= at up to *( mg,5g body-
weight$%%& L@(0 $mouse, 'A&> %* g,5g$%*&
AMA8=6A:
Aregelatinized starch is a modified starch used in oral capsule and tablet formulations as a
binder, diluent,$%,*& and disintegrant$-& 'n comparison to starch, grades of pregelatinized
starch may be produced with enhanced flow and compression characteristics such that the
pregelatinized material may be used as a tablet binder in dry compression or direct
compression processes$;)%;& 'n such processes, pregelatinized starch is selflubricating
/owe"er, when it is used with other excipients it may be necessary to add a lubricant to a
formulation Although
magnesium stearate 0*(+ w,w is commonly used for this purpose, concentrations greater
than this may ha"e ad"erse effects on tablet strength and dissolution 6herefore, stearic acid
is generally the preferred lubricant with pregelatinized starch$%(& Aregelatinized starch may
also be used in wet granulation processes$%1&
A8'M=B7L
Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in capsule$%)
1& and tablet formulations$2)%0& 't is commonly used in tablets prepared by either
directcompression$%%)%-& or wet-granulation processes$%;)%1& 6he usual concentration
employed in a formulation is between *+ and 3+, with the optimum concentration about ;+,
although in many cases *+ is sufficient @isintegration occurs by rapid upta5e of water
followed by rapid and enormous swelling$%2)*0& Although the effecti"eness of many
disintegrants is affected by the presence of hydrophobic excipients such as lubricants, the
disintegrant efficiency of sodium starch glycolate is
unimpaired 'ncreasing the tablet compression pressure also appears to ha"e no effect on
disintegration time$%0)%;& Sodium starch glycolate has also been in"estigated for use as a
suspending "ehicle$*%,**&
6ALC
6alc was once widely used in oral solid dosage formulations as a lubricant and diluent, see
6able ',$%)-& although today it is less commonly used /owe"er, it is widely used as a
dissolution retardant in the de"elopment of controlled-release products$;)1& 6alc is also used
as a lubricant in tablet formulations4$2& in a no"el powder coating for extended-release
pellets4$3& and as an adsorbant$.& 'n topical preparations, talc is used as a dusting powder,
although it should not be used to dust surgical glo"es4 see Section %; 6alc is a natural
material4 it may therefore
fre!uently contain microorganisms and should be sterilized when used as a dusting powder4
see Section %%
6alc is additionally used to clarify li!uids and is also used in cosmetics and food products,
mainly for its lubricant properties