PHARMACEUTICAL DOSAGE

FORMS LABORATORY
TROCHES
Troches, also known as lozenges
or pastilles, are discoid shape
solids containing the medicinal
agent in a suitably favoured
base.
The base may be a hard sugar
candy, glycerinated gelatin, or
the combination of sugar with
sufcient mucilage to give it
form.
Troches are placed in the mouth
where they slowly dissolve,
liberating the active ingredient.
PEPPERMINT TOCHES
Sugar
.. g
Tragacanth ..
....! g
"eppermint #il $.s.
"uri%ed water $.s.
Trochisci &enthae "iperitae
USE' (lavoured Troches base
PILLS
)re small round solid dosage
forms containing a medicinal
agent and are intended for oral
administration.
Substances which are bitter or
unpleasant to the taste, if not
corrosive or delin$uescent, can
be administered in this form if
the dose is not too large.
ALOE PILLS
)loe ..
..*.
+g
,ard soap..
.*.+g
"uri%ed water
"ill -+
).#/' the dried late0 of leaves of )loe
barbadensis
USE' 1athartic
2 The action of aloe is accompanied by
intestinal griping and pelvic vascular
congestion.
SUPPOSITORIES
Solid dosage forms intended for
insertion into body ori%ces where they
melt, soften, or dissolve and e0ert
localized or systemic e3ects.
.atin' supponere meaning 4to
place under5
Sub' under
Ponere' to place
Rectal:
)dult 2 bullet, torpedo, little %nger 2 !g
6nfants and children 2 pencil2like 2 half
the weight of adult dose
Vaginal:
)ka pessaries 2 globular, oviform,
cone2shaped 7 8g
Uretral:
)ka bougies2 pencil shaped 2 male2 9g,
female2 !g
SUPPOSITORY BASES
:"lays an important role in the release
of the medication they hold and
therefore in the availability of the drug
for absorption for systemic e3ects or
for localized action.
:#ne of the %rst re$uisites for a
suppository base is that it remains
solid at room temperature but softens,
melts, or dissolves readily at body
temperature.
CLASSIFICATION OF A
SUPPOSITORY BASE
(atty or oleaginous
;ater soluble or water miscible
&iscellaneous
FATTY !r OLEAGINOUS BASES
"rincipally the most fre$uently
employed suppository base.
E"AMPLES:
1ocoa butter
"alm kernel oil
1ottonseed oil
<lyceryl monostearate
<lyceryl monopalmitate
COCOA BUTTER NF
The fat obtained from the
roasted seed of Theobroma
cacao.
)t room temperature it is a
yellowish, white solid having a
faint, agreeable chocolate2like
odor.
&elts between *
o
1 to =
o
1
#ATER SOLUBLE an$ #ATER
MISCIBLE BASES
<lycerinated gelatin
"olyethylene glycols
GLYCERINATED GELATIN
&ost fre$uently used in the
preparation of vaginal
suppositories.
ADVANTAGES:
Slower to soften and mi0 with
the physiologic fuids than is cocoa
butter and therefore provides a more
prolonged release.
DISADVANTAGES:
,ave a tendency to absorb
moisture due to the hygroscopic
nature of glycerine, they must be
protected from atmospheric moisture
for them to maintain their shape and
consistency. >ue to the hygroscopicity
of glycerine, the suppository may have
a dehydrating and be irritating to the
tissue upon insertion.
POLYETHYLENE GLYCOLS
"olymers of ethylene o0ide and
water, prepared to various chain
lengths, molecular weights and
physical state.
"/< **, 9**, =**' clear,
colorless li$uid
"/< +*** and up' wa0like white
solid whose hardness increases
with an increase in the
molecular weights.
ADVANTAGES
>o not melt at body
temperature but rather dissolve
slowly in the body?s fuid.
1onvenient storage
"ermits slow insertion without
fear that they will melt in the
%ngertips.
>o not leak in the ori%ce.
DISADVANTAGE
"olyethylene glycol do not
contain at least !*@ water and
therefore moisture is withdrawn
from the tissues and causes a
stinging sensation
MISCELLANEOUS BASES
&i0tures of oleaginous and
water2soluble or water2miscible
materials.
These materials may be
chemical or physical mi0tures.
Some are preformed emulsion,
generally of the water2in2oil
type, or they may be capable of
dispersing in a$ueous fuids.
POLYO"YL %& STEARATE
) surface active ingredient that
is employed in a number of
commercial suppository bases.
) mi0ture of the monostearate
and distearate of mi0ed
polyo0ythelene diols and the
free glycols.
The average polymer length is
e$uivalent to about 9*
o0yethylene units.
;hite to light tan wa0y solid
that is water soluble.
&elting point' A
o
1 to 98
o
1
PREPARATION OF SUPPOSITORIES
&#.>6B< from a melt
1#&"C/SS6#B
,)B> C#..6B< and S,)"6B<
&#.>6B< (C#& ) &/.T
&ost fre$uently employed both
on a small scale and on an
industrial scale.
Dases suitable for preparation
by molding'
2 1ocoa butter
2 <lycerinated gelatin
2 "olyethylene glycol
STEPS:
+. &elting the base
!. 6ncorporating any re$uired
medicaments.
. "ouring the melt into the mold
9. )llowing the melt to cool and
congealed into suppositories
8. Cemoving the formed
suppositories from the mold.
SUPPOSITORY MOLDS
2 Ma$e !' (tainle(( (teel)
al*+ini*+) ,ra(() !r -la(tic
Te+-!rar. +!l$(:
(ormed by pressing heavy aluminun
foil about an obEect having the shape
of the desired suppository, then
carefully removing the obEect.
glass stirring rods' Frethral
suppositories
round pencils and pens' rectal
suppositories
cone2shaped obEect' vaginal
suppositories
LUBRICATION OF THE MOLD
.ubrication of the mold is
sometimes re$uired to facilitate
clean and easy removal of the
molded suppositories.
.ubrication is seldom necessary
when the base is cocoa butter
or polyethylene glycol, as these
materials contract sufciently
on cooling to separate from the
inner surfaces and allow easy
removal.
<lycerinated gelatin re$uires
lubrication' mineral oil
PREPARATION BY COMPRESSION
ADVANTAGES
Suited for making suppositories
that contain heat2labile
medicinal substances or a great
deal of substances that are
insoluble in the base.
Bo likelihood of insoluble matter
settling during manufacture.
DISADVANTAGE
Special suppository machine is
re$uired and there is some
limitation as to shapes of
suppositories that can be made.
PREPARATION BY HAND ROLLING
AND SHAPING
;ith the ready availability of
suppository molds of
accommodating shapes and
sizes, there is little re$uirement
for today?s pharmacist to shape
suppositories by hand.
GLYCERIN SUPPOSITORIES USP
<lycerin
..A+g
Sodium stearate.
...Ag
"uri%ed water.
.+g
To make
about...+**g
<lycerin
2 .a0ative
Sodium Stearate
2 Solidifying agent
USES: .a0ative, especially in
infants and children.
2 (ecal evaluation usually occurs
within +8 to * minutes after
insertion.
2 )ct by stimulating the rectal
mucosa and by softening
inspissated fecal material.
2 To establish habit time.
STORAGE' Tight containers,
preferably at temperatures below
!8
#
1
GLYCERINATED GELATIN
SUPPOSOTORIES
&edicinal agent GtrisulfapyrimidineH..
..*.8g
<elatin,
granular.
..!*g
"uri%ed
water
.+*g
<lycerin
I*g
Trisulfapyrimidine
2 sulfadiazine, sulfamerazine and
sulfamethazine
2 )ntibacterial
<elatin GI*@H
2 Solidifying agentJvehicle
<lycerine G!*@H
2 .ubrication
USES' "reparation of vaginal
suppositories
STORAGE: glycerine suppositories
and glycerinated gelatin suppositories
are packaged in tightly closed glass
containers to prevent a moisture
change in the content of the
suppositories.
<lycerinated gelatin
suppositories are best stored at
temperatures below 8
#
( and
can routinely be stored at
controlled room temperature
G!*2!8
#
1J=K2II
#
(H
OINTMENTS
Semisolid preparations intended
for e0ternal application to the
skin or mucous membranes.
&ay be medicated or non2
medicated. Bonmedicated
ointments are used for the
physical e3ects that they
provide as protectants,
emollients or lubricants.
PREPARATION OF OINTMENTS
Two general methods'
Inc!r-!rati!n
2 6ncorporation of soild
2 6ncorporation of li$uid
F*(i!n
INCORPORATION
1omponents are mi0ed until a
uniform preparation is attained.
)pparatusL
2 &ortar and pestle
2 Spatula and ointment slab
INCORPORATION OF SOLIDS
The ointment is prepared by
thoroughly rubbing and working
the components together on
hard surface until the product is
smooth.
) small portion of the powder is
mi0ed with the portion of the
base until uniform. <eometric
dilution is continued until all
portions of the powder and base
are combined and thoroughly
and uniformly blended.
"owder or crystalline materials
are reduced before
incorporation into the ointment
base so the %nal product will not
be gritty. This may be done by
levigating, or mi0ing the solid
material in a vehicle in which it
is insoluble to make a smooth
dispersion.
Le/igating agent0
Mineral !il: for bases in which
oils are the e0ternal phase.
Gl.cerin: for bases in which
water is the e0ternal phase.
INCORPORATION OF LI1UIDS
.i$uid substances or solutions
of drugs are added to an
ointment only after due
consideration of an ointment
base?s capacity to accept the
volume re$uired.
FUSION
Dy the fusion method, all or
some of the components of an
ointment are combined by
being melted together and
cooled with constant stirring
until congealed.
1omponents not melted are
added to the congealing
mi0ture as it is being cooled
and stirred.
,eat2labile substances and
many volatile components are
added last when the
temperature of the mi0ture is
low enough not to cause
decomposition or volatilization
of the components.
Substances can be added to the
congealing mi0ture as solutions
or insoluble powders levigated
with the portion of the base.
&edicated ointments and
ointment bases containing
components as beeswa0,
parafn, stearyl alcohol, and
high molecular weight
polyethylene glycols, which do
not lend themselves well to
mi0ture by incorporation, are
prepared by fusion.
METHODS
A2 The materials with the highest
melting points are heated to the
lowest re$uired temperature to
produce a melt.
The additional materials then are
added with constant stirring during
cooling of the melt until the mi0ture is
congealed.
6n this way, not all of the components
are subEected to the highest
temperature.
B2 &elting the component having the
lowest melting point %rst and adding
the remaining components in order of
their melting points or simply melting
all the components together under
slowly increasing temperature.
Dy these method, a lower temperature
is re$uired is usually sufcient to
achieve fusion due to the solvent
action e0erted by the %rst melted
components on the others.
C2 6n the preparation of
ointments having an emulsion base,
the method of manufacture involves
melting and an emulsi%cation process.
The water2immiscible
components such as the oil and wa0es
are melted together in a steam bath to
about I* to I8
#
1.
&eantime, an a$ueous
solution of the heat2stable, water2
soluble components is prepared and
heated to the same temperature as
the oleaginous components.
Then the a$ueous solution is
slowly added, with mechanical stirring
to the melted oleaginous mi0ture.
The temperature is
maintained for 8 to +* minutes and
the mi0ture is slowly cooled with the
stirring continued until congealed.
OINTMENT BASES
1lassi%ed by the FS" into four
general groups.
2 H.$r!car,!n ,a(e(
2 A,(!r-ti!n ,a(e(
2 #ater3re+!/a,le ,a(e(
2 #ater (!l*,le ,a(e(
SELECTION OF THE APPROPRIATE
BASE
Selecti!n !' te ,a(e t! *(e in te
'!r+*lati!n !' an !int+ent
$e-en$( !n care'*l a((e((+ent !'
a n*+,er !' 'act!r() incl*$ing te
'!ll!4ing:
>esired release rate of the drug
substance
>esirability of topical or
percutaneous drug absorption
>esirability of occlusion of
moisture from the skin
Stability of the drug in the
ointment base
/3ect, if any, of the drug on the
consistency or other features of
the ointment base
>esire for a base easily
removed by washing with water.
1haracteristics of the surface to
which it is applied.
HYDROCARBON OINTMENT BASE
Al(! ter+e$ a( 5!leagin!*(
,a(e(6
On a--licati!n t! te (7in:
they have an emollient e3ect,
protect against the escape of
moisture
e3ective as occlusive dressings
Cemain on the skin for
prolonged period of time
without 4drying out5
6mmiscible with water therefore
difcult to wash o3.
;ater and a$ueous
preparations may be
incorporated into them, but only
in small amounts and with some
difculty.
;hen powdered substances are
to be incorporated into
hydrocarbon bases, a levigating
agent should be used.
E8a+-le(:
"etrolatum
;hite petrolatum
;hite ointment
Mellow ointment
#HITE OINTMENT:
;hite
wa0
..8*g
;hite
petrolatum..
A8*g
To
make
.+***g
Oint+ent USP "I0 Si+-le Oint+ent
Pre-arati!n' (usion
6t is permissible to vary the
proportions of the wa0 to obtain a
suitable consistency of the ointment
under di3erent climatic conditions.
USES: an e+!llient an$ /eicle '!r
!ter !int+ent(
#ite -etr!lat*+:
;hite petroleum EellyL white soft
parafn
) puri%ed mi0ture of semisolid
hydrocarbons obtained from
petroleum, and wholly or nearly
decolorized.
USES' similar to yellow petrolatum but
often is preferred because its freedom
from color. 6t is employed as
protective, a base for ointments and
cerates and to form the basis for burn
dressings.
#ite 4a8:
Dleached Deeswa0L ;hite beeswa0L
bleached wa0
The product of bleaching and purifying
yellow wa0 that is obtained from the
honeycomb of the bee.
USES' a sti3ening agent in many
preparations such as cerates, pastes
and ointments.
YELLO# OINTMENT
Mellow wa0.
..8*g
"etrolatum..
..A8*g
To make.
.+***g
Pre-arati!n: F*(i!n
USES: an emollient and vehicle for
other ointments. Doth white and
yellow ointment are known as 4simple
ointment5.
;hite ointment should be used to
prepare white ointments and yellow
ointments should be used to prepare
colored ointments when simple
ointment is prescribed.
Yell!4 4a8:
Deeswa0L Mellow beeswa0
The puri%ed wa0 from the
honeycomb of the bee.
FS/S' ) sti3ening agent in
many pharmaceutical
preparations.
Petr!lat*+:
Mellow soft parafnL amber
petrolatumL yellow petrolatumL
petroleum EellyL parafn Eelly
) puri%ed mi0ture of semisolid
hydrocarbons obtained from
petroleum.
FS/S' a base for ointments. 6t is
highly occlusive and therefore a
good emollient but it may not
release some drugs readily
ABSORPTION BASES
Fseful as pharmaceutical
adEuncts to incorporate small
volumes of a$ueous solutions
into hydrocarbon bases.
Fsed as emollients although
they do not provide the degree
of occlusion a3orded by the
hydrocarbon bases.
Bot easily removed from the
skin with water since the
e0ternal phase of the emulsion
is oleaginous.
Two types'
Those that permit the
incorporation of a$ueous
solutions resulting in the
formation of water2in2oil
emulsions.
2 /0' hydrophilic petrolatum
Those that are water2in2oil
emulsions Gsyn' emulsion basesH
and permit the incorporation of
additional $uantities of a$ueous
solutions.
2 /0' .anolin
,M>C#",6.61 "/TC#.)TF&
1holesterol
.. *g
Stearyl
)lcohol....
*g
;hite wa0.
..K*g
;hite "etrolatum.
..K=*g
To
make
+***g
Pre-arati!n: (usion
USES' a protective and water2
absorbable ointment base.
6t will absorb a large amount of
water from a$ueous solutions of
medications, forming ;J# type
of emulsion.
ORIGINAL FORMULATION:
&elt the steary alcohol, white
wa0, and white petrolatum
together on a steam bath, then
add the cholesterol, and stir
until it completely dissolves.
Cemove from the water bath,
and stir until it congeals.
C!le(ter!l
2a steroid alcohol widely
distributed in the animal
organisms
2 FS/S' to enhance
incorporation and emulsi%cation
of medicinal products
2 ) pharmaceutical necessity for
hydrophilic petrolatum, in which
it enhances water2absorbing
capacity.
Stear.l alc!!l
2FS/S' a surface active agent
used to stabilize emulsions and
increase their ability to retain
large $uantities of water.
#ite 4a8
2 Sti3ening agent
#ite -etr!lat*+
2 #intment base
LANOLIN USP
#btained from the wool of
sheep G#vis ariesH
) puri%ed, wa02like substance
that has been cleaned,
deodorized, and decolorized.
GyellowishH
1ontains not more than *.!8@
water.
)dditional water may be
incorporated into lanolin by
mi0ing.
#ATER3REMOVABLE OINTMENT
BASES
#il2in2water emulsion
resembling creams in
appearance.
/asily washed from the skin and
are often called 4water2
washable5 bases.
,ave the ability to absorb
serous discharge.
/0ample' hydrophilic ointment
FS"
HYDROPHILIC OINTMENT
&ethylparaben
*.!8g
"ropylparaben
......*.+8g
Sodium lauryl
sulfate..+*g
"ropylene
glycol..+!*
g
Stearyl
alcohol.!
8*g
;hite "etrolatum.
..!8*g
"uri%ed water, a sufcient $uantity
To
make
+***g
Pre-arati!n' (usion
USES' ) water2removable
ointment base for the so2called
4washable5 ointments. This is
an #J; emulsion.
Met.l-ara,en
2 )ntimicrobial preservative
Pr!-.l-ara,en
2 )ntimicrobial preservative
S!$i*+ La*r.l S*l'ate
2 )n emulsifying agent, detergent
and wetting agent in ointments
Pr!-.lene gl.c!l
2 ) surfactant. 6t is particularly
useful as dispensing agent for
perfume oils or oil2soluble
vitamins in water, and in
cosmetic preparations.
Stear.l alc!!l
2 ) surface active agent used to
stabilize emulsions and increase
their ability to retain large
$uantities of water.
#ite -etr!lat*+
2 #intment base
#ATER SOLUBLE BASES
1ompletely water2washable and
often are referred to as
4greaseless5
>o not contain oleaginous
components.
Soften greatly with the addition
of water therefor large amounts
of a$ueous solutions are not
e3ectively incorporated into
these bases.
&ostly used in incorporation of
solid substances.
POLYETHYLENE GLYCOL OINTMENT
NF
"olyethylene glycol 8*.
.9**g
"olyethylene glycol 9**.
=**g
Pre-arati!n' (usion
The combining of "/< 8*, a
solid, with "/< 9**, a li$uid
results in a very pliable
semisolid ointment.
6f a %rmer ointment is desired,
the formula may be altered to
contain up to e$ual parts of the
two ingredients.
;hen a$ueous solutions are to
be incorporated into the base,
the substitution of 8*g of the
"/< 8* with an e$ual amount
of stearyl alcohol is
advantageous in rendering the
%nal product more %rm.
USE: ;ater soluble base.
SULFUR OINTMENT USP
"recipitated sulfur.
..+**g
&ineral oil..
..+**g
;hite
ointment
K**g
To make.
.+***g
Pre-arati!n' 6ncorporation
Preci-itate$ (*l-*r
2 )ctive ingredient
Mineral !il
2 .evigating agent
#ite !int+ent
2 Dase
USES: "arasiticideJScabicide
"rolonged use of sulfur may
result in a characteristic
dermatitis
venenataGinfammation of the
skin of e0ternal originH
DOSE' Topical, as a +*@
ointment every night fro
nights
STORAGE: "reserved in a well
closed container and avoid
prolonged e0posure to
e0cessive heat
ICHTHAMMOL OINTMENT NF
6chthammol...
..+**g
)nhydrous lanolin.
..+**g
petrolatum .
K**g
To make.
.+***g
Pre-arati!n' 6ncorporation
Icta++!l
2 )ctive ingredient
2 6chthyol
)nhydrous lanolin
2 ;ool fat
2 Sti3ening agent
Petr!lat*+
2 Dase
2 USE: )ntibacterial agent with
moderate emollient and
demulcent properties.
2 DOSE: Topical, to the skin as +*
to !*@ ointment or e0ternal
ear canal as +*@ ointment.
PAC9AGING) STORAGE) an$
LABELING
#intments and other semi2solid
preparations are packaged
either in large2mouth ointments
Ears or in metal or plastic tubes.
Semisolid preparations must be
stored in well2closed containers
to protect against
contamination and in a cool
place to protect against product
separation in heat. ;hen
re$uired, light sensitive
preparations are packaged in
opa$ue or light2resistant
containers.
FS" directs the labelling for
certain ointments and creams
include the type of base used.
CREAMS
Semisolid preparations
containing one or more
medicinal agents dissolved or
dispersed in either an oil2in2
water emulsion or in another
type of water washable base.
4Nanishing creams5 #J;
emulsions containing large
percentages of water and
stearic acid.
2 )fter application of the cream,
the water evaporates leaving
behind a thin residue %lm of
stearic acid.
1reams are preferred than
ointments because they are
easier to spread and remove
than many ointments.
COLD CREAM
1etyl esters
wa0..+!8
g
;hite
wa0
+!*g
&ineral
oil
8=*g
Sodium
borate
8g
"uri%ed
water
+A*ml
To make.
+,**
Petr!lat*+ R!(e #ater
Oint+ent USP "VI
Cet.l e(ter 4a8
2 4 Synthetic Spermaceti5
2 ) replacement for spermaceti
used to give consistency and
te0ture to ointments.
#ite 4a8
2 Sti3ening agent
Mineral !il
S!$i*+ ,!rate
2 )lkalanizing agent
USES' useful as an emollient,
cleansing cream and ointment
base.
6t resembles rose water
ointment, di3ering only in that
the mineral oil is used in place
of almond oil and omitting the
fragrance. This change
produces an ointment base
which is not subEect to rancidity
like one containing a vegetable
oil.
6f the ointment has been chilled,
warm it slightly before
attempting to incorporate other
ingredients.
;J# emulsion
ROSE #ATER OINTMENT
1old creamL <alen?s cerate
#riginated by <alen, the famous
roman physician2pharmacist of
the +
st
century )>, was known
for many centuries by the name
unguentum or ceratum
refrigerans.
)n emollient and ointment
base.
;J# emulsion.
PASTES
Semisolid preparations intended
for application to the skin.
1ontains a larger amount of
solid materials than ointments
and therefore are sti3er.
;hen prepared with an
oleaginous base they are less
greasy than their counterpart
ointments due to the reduced
amount of base.
"repared in the same manner as
ointment, however, when a
levigating agent is to be used to
render the powdered
component smooth, a portion of
the base is often used rather
than a li$uid, which would
soften the base.
ADVANTAGE
2 Decause of the sti3ness,
remains in the place after
application and are e3ectively
employed to absorb serous
secretions.
DISADVANTAGE
2 Decause of their sti3eness and
impenetrability, pastes are not
suited for application to hairy
parts of the body.
:INC O"IDE PASTE
Oinc o0ide.....
..!8*g
Starch...
..!8*g
;hite petrolatum.
8**g
To make.
.+***g
Synonyms'
.assar?s "lain Oinc "aste
"asta Oinci #0idi
1ompound "aste of Oinc #0ide
USES' protectant, mild J weak
astringentL
Fsed in dermatologic disorders where
there are more lesions as compared to
Oinc #0ide ointment
La((ar;( Pa(te' Oinc #0ide "aste
with Salicylic Acid Ghas keratolytic
e3ectH
1ontains not less than !9@ but not
more than !=@ of Oinc #0ide
STORAGE' well closed containers,
avoid prolonged e0posure to
temperature e0ceeding *P1