12

-
Semisolid Dosage Forms -
Suppositories and Pessaries
,u tJ. ~ '//f!J. i:: '//II ,,. ~ flS ' ~ • ' ... :::0 flj ,ti!, ;;:- ~ ... ':ii "'- "' f; -;:

SUPPOSITORIES
Suppositories are semisolid dosage fonn of medicament for insertion
into body cavities other than mouth. They may be inserted into rectum,
vagina or nasal cavity. The medicament is incorporated into the sup-
pository base and the product is fonnulated in such a way that they will
either melt or dissolve in the body cavity fluid to release the medica-
ment. Suppositories are available in different shapes, sizes and weights.
Suppositories are used to produce local, systemic and mechanical action.
Advantages

(1) These .can be easily administered to children, old persons and to

unconscious patients who cannot swallow the drug easily.
(2) These are inserted into body cavity to produce local effect of the
medicament incorporated in the base.
(3) These are inserted into the rectum to exert a direct and rapid
action on the rectum.
(4) These are inserted into the rectum to promote evacuation of the
bowel.
(5) Suppositories are unit dosage form of drugs.
(6) These are convenient mode of administration of drugs which
irritate gastro-intestinal tract, cause vomiting and destroyed in
the acidic pH of the gastric juice of stomach.
(7) The drugs in suppositories are slowly absorbed giving sustained
action.
Disadvantages

by this route. _
2 The irritant drugs can't be administered
(l)
( ) Suppositories cause embarrassment to the patient, when~ drug is
administered by inserting a suppository into a body cavity.

263
 DISPENSING PH A lh,. Cfl'J'.Z
264
re ctal
- ~ '-''-LYLA.Cy

(3) These cannot be prepared easily. ,rtie ctioo

prate Jj8
(4) The suppositories are required to be store~ adt low temperatUre
ranging from 10° to 20°C. These are require
. . .
to be stored .
1n a
z..
s 10
d
refrigerator, which 1s costly for poor patients. dfllg i..avi
s 1•'
dfl.l~ tO C'
Types of Suppositories rate oSl·tor
1. Rectal suppositories : These are meant for introduction into the suPP f rn
rectum for their systemic effect. These are generally made from theo- eo
tYP d 00e
broma oil and are available in various sizes to meet the needs of infant adde
children and adults. Rectal suppositories are usually available in Weig~~ 3. C
about 1-2 g. They are either cone or torpedo shaped. sbapes a~
2. Vaginal suppositories : These are meant for introduction into 'f}1e }i~Ul
the vagina. These suppositories are also known as pessaries and are r11ere 1s
larger than rectal suppositories. The vaginal suppositories may be 4. C
conical, rod-shaped or wedge shaped and are usually available in weight the soluti
about 4-8 g. Vaginal suppositories are mainly used for their local action cetyl alco
on the vagina. Nowadays, vaginal tablets and vaginal capsules are also These are
available which has substituted the vaginal suppositories. to provid
- 3. Nasal suppositories : These are meant for introduction into the the releas
nasal cavity and are also known as nasal bougies. These are similar to
urethral suppositories. These are thin and cylindrical in shape and are
plastic m
always prepared with glycero-gelatin base. Nasal suppositories are about
disposabl
9- 10 cm long and weigh about 1.0 g.
with the
4. Urethral suppositories : These are meant for introduction into then pack
the urethra and are also known as urethral bougies. These are thin, long Their sha
and cylindrical forms rounded at one end to facilitate insertion. Their
weight varies from 2 to 4 g. These suppositories are very rarely used.
5. Ear cones : These are meant for introduction into the ear and
are also known as aurinaria. Nowadays, these are rarely used. These
suppositories are thin, long and cylindrical in shape and weigh about 1
gram. Ear cones are usually prepared with theobroma oil. The v
tones, so
New Trends of Suppositories adlllinistr
In recent years a_new concept of suppositories have been introd~ced When.ins
in regard to its formulation and packaging. Some of these are descnbed
have the
as under:-
1. It
1. Tablet suppositories : Nowadays, the rectal suppositories and b
pessaries are prepared by compression just like compressed tablets. ~e 2. I
compressed pessaries are generally almond shape for ease in inse~on
and to provide a large surface area for disintegration and absorpuon, 3. I
4. l
 sFMISOl II) DOSAUF FORMS SIJPl'OSl'l'Ol< ll!S & J>liSSt\RIES 265
Ch 12

he rectal tab!cts are . gcm•~·ally t·oated with polyethylen e glycol for

'frotcction and its easy 111s0rt1011 into the rectum.
p
2. Layered suppos1·t ones . :
These s11ppm;itorics contain different
us in different layers to avoid itH·ompatihility hctween them. The
dfll t>
drugs having d.I f'f'crent me Itu~g
.
point or dissolution rate can be incorpo-
rated to control the rate of release of' medicament . These types of
5tl Pp
ositories can he prepared by partially rilling the mould with one
. l
type of mat~na • WI1en tt .
gets solidified, then the other materials are
added one after the other as a separate layer.
3. Capsule suppositories : The soft gelatin capsules of different
shapes and sizes. are. used for. insertion into the rectum or the vagina.
The liquids, sem1-sohds or sohds can be filled in soft gelatin capsules.
There is great demand of such capsules nowadays.
4. Coated suppositories : Suppositorie s are coated by dipping in
the solution of the coated materials, such as, polyethylen e glycol and
cetyl alcohol etc. until the coats of desired thickness have been obtained.
These are then dried. These suppositorie s impart lubricant properties or
to provide protection action during storage. They also helps to control
the release of medicamen t.
5. Disposable moulds : The disposable moulds are made up of
plastic material or tin foils. The suppository material is poured into the
disposable moulds and cooled. The excess of the mass is trimmed off
with the help of sharp knife or blade and moulds are sealed. These are
then packed in cartons. The disposable moulds are cheaper and elegant.
Their shapes can be changed at a lower cost. Moreover, when supposi-
tories mass melts during storage, it will remain in the mould itself and
can be reconverted into suppositorie s after cooling.

SUPPOSITORY BASES
The various types of suppositorie s bases are used to prepare supposi-
tories, so that they can retain its shape, and firmness during storage and
administration. They should melt or dissolve in body cavity fluids,
when inserted into the body cavity. An ideal suppository base should
have the foJlowing properties:-
]. It should melt at body temperature or dissolve or disperse in
body fluids.
2. It should keep its shape when being ham.lied.
3. It should release the medicamen t readily.
4 . It should be non-toxic and non- irritant to the mucous membrane.
266 DISPE\S IXG PIIAR..\t,\cy

5 _ It should be stable on storage.

6. It should be compat ible with large number of drugs.
7. It should be stable if heated above its melting point
8 _ It should be easily moulde d and it should not adhere to the
mould.
9. It should be good in appearance.
10. It should be easily moulda ble by pouring or cold compression.

Classification of Suppository Bases

Suppository bases can be broadly classifi ed into three categor ies:-
1. Fatty bases
2. \Yater soluble and water miscibl e bases
3. Emulsi fying bases
1. Fatty Bases
' i) Theobroma oil : It is a yellowi sh white solid obtained from
crushed and roasted seeds of TI1eobroma cocoa. It is also knoV1-"I1 as
cocoa butter. It has butter like consist ency haYing melting point of 30-
35 ::c. It is a mixture of glycery l esters of stearic. oleic. palmitic and
other fatty acids.
Theobrorna oil melts at body tempera ture and release the medica-
ment for rapid absorption. It is conside red a most suitable base for
rectal suppositories but not suitable for pessari es. nasal and urethral
bougies because after melting it has a tendenc y to leak out of the cavities
and also it is immisc ible with mucous secretio ns. It is readily liquefy on
warming and quickly settle on cooling.
Disadvantages Cocoa butter has most of the qualities of an ideal
suppository base but still, it has a number of serious disadvantages
which are as follow :-
(a) It shows the phenom ena of polymo rphism i.e., when theobroma
oil is melted and cooled, it gets solidifi ed into different crystal-
line forms depend ing upon melting tempera ture, rate of cooling
and size of the mass.
(b) It become s rancid and melts in warm weathe r.
(c) It has a tendenc y to stick to the sides of the mould when
solidifi ed.
(d) The leakage from body cavities on melting can take place.
(e) It is relatively costly.
(0 It is immiscible with body fluids.
 '()I II> r>C>SA<11~ H>H.MS SIJJ>P<,sno r<JES & PESSARIES 267
s1:tvf IS •
('It I l •
('er tain dr 11gs such as chloral hydrate, lactic acid etc. when
(g) , 1,or.itcd with cocoa h111ter, liquefacti on take place. To
111CO
llt ·iin the desired consisten cy, the beeswax can be added.
11lill '
: ufaifi, d rJ,,,ohroma oil : This may be used as a base when
1

( II) I, ,Illtitics. .
of aqucrnis solulJCm<.; arc to be incorpora ted. The u-;e of
l' qu,111
1arf! . ·ryl ,nonostca rat c, l 0% Jenette wax, 2-Y,f, cety1 alcohol.
"¼ g1ye,:, .
-' " . ·w·ix and 12'¾ spcrmacct1 1s re;commended to prepare emulsifie d
4% bL'l s , . .
• , 1 oil supposrto ncs.
th~ohtolll,
... ) f tvdrof!.<'t1ated oil\ : These are obtained by hydrogen ation of
111
.< . vegetable oils,· sue.: h as arac h'1s 01·1 , cotton seed 01·1 , coconut 01·1 •
vanous . . . .
- ,·tc It is used as a suhst1tutc for thcobrom a ml because 1t has a
p·1I111 0 11 " .
' t ,. • of advantage s over thcobrom a oil. These are:-
nun1 )v1
(a) They arc resistant to oxidation .
(b) Lubricatio n of the mould is not required.
(c) Overheati ng docs not affect the solidifyin g point.
(d) They produce colourless , odourless and elegant supposito ries.
(c) The emulsifyi ng and water absorbing capacities are good.

Disadvantages
(a) The supposito ries become brittle on rapid cooling in a refrigerat or.
(b) They are more fluid than theobrom a oil when melted so there is
greater sedimenta tion of the added substance s. This difficulty
can be overcome by adding some thickenin g agent such as
bentonite, magnesiu m stearate etc.

2. Water Soluble and Water Miscible Bases

(i) Glycero-gelatin base : It is a mixture of glycerin and \Vater
which is made stiff by the addition of gelatin. The base may be used for
preparing all type of supposito ries but it is particular ly used for making
pessaries.
h_The supposito ries prepared from glycero-g elatin base are translucen t.
; ich t~nd to dissolve or disperse slowly in the body cavity and release
g ~ n_iedicament. Hence, the base is preferred over fatty base: Glycero-
h~:tin base is well suited for supposito ries containin g boric acid, chloral
rate, bromides, iodides, iodoform , opium etc.
are To avoid incompat ible reactions , any one of the two types of gelatin
used as suppositor y base.
l. T~p~ A or Pharmage l A. It is prepared by acid hydrolysis. It is
ac~dic in nature and used for acidic drugs having iso-electr ic
Point (7-9).
 DISPENSING PliAlh.
268 ''-lYIACy
or Pharmagel B which is alkaline in nature and us d
2. T ype B . . (4 7 e for
alkaline drugs having iso-electnc pomt . to 5 .0).

Disadvantages
(a) The solution time depends on the content and quality of gelatin
used.
(b) Gelatin is incompa~ible . with many drugs, such as, tannic acid,
ferric chloride, galhc acid etc.
(c) There are more chances of bacterial and mould growth. Ther _
fore, a suitable preservative is required to preserve tie (c)
suppositories.
(d) The suppositories prepared with glycero-gelatin base are
hygroscopic and hence require special storage containers. (d)
turn
(e) They have a physiological action (Glycerol-suppository B.P. is
used as a laxative).
3. Emu
(f) They are more difficult to prepare and handle.
proprietarY s
(ii) Soap-glycerin suppositories : In glycero-gelatin base, the gelatin are described
is replaced with either curd soap or sodium stearate which makes the (i) Wite
base sufficiently hard to prepare good quality of suppositories. Soap
fatty acid wi
also helps in the evacuation action of glycerin.
beeswax is
The main disadvantage of this base is that they are very hygroscopic. with witepso
Therefore, the suppositories prepared with this base must be protected them from
from atmosphere and wrapped in waxed paper or tin foil. properly 1ub
(iii) Polyethylene glycols : Polyethylene glycol polymers are com- (ii) Mas
monly known as carbowaxes or polyglycols or macrogols. The physical of saturate
character of these carbowaxes varies according to the molecular weight.
C17H35COO
The macrogols having molecular weight less than 1000 are liquids and
those with molecular weight higher than 1000 are wax like solids. It is a wl
m.p. 33.5 to ·
Advantages
commonly u~
(a) They are chemically stable.
· (iii) Masd
(b) They are non-irritant. Whi
. ch sma11 1

(c) They do not allow the bacterial or mould growth to take place. lts '
Water abs◄
(d) They are physiologically inert substances.
. . of the base can be changed ding to thed Advanta1
(e) Physical properties accor
(a) They
need by combining the different proportion of high and low an
high melting point polymers. . tb Cb) They
lt JJ1 e (c) The
(t) They provide prolonged action because they do not roe
body cavity but dissolve slowly for a long time. (d) Over
 PO SIT OR IES & PESSARIES 269
servfJSOLID DO SAG E FO RM S-S UP
•
c11-tZ mould.
) TheY do not stic k to the sid e of the
The sup pos ito rie s ma de fro m ma cro gol s hav e clean and smooth
(:)
( appearance.

pisadvantages .
uir e special storage condi-
They are hyg ros cop ic and hen ce req
(a) tions to sto re the m.
s
(b) They are inc om pat ibl e wit
h cer tain drugs like tannins, phenol
etc. .
results in retention of the drug in
(c) Its good sol ven t pro per ties . can
body, thereby reducing their
the liq uef ied bas e, the n m the
therapeutic act ivi ty.
Hig h sol ubi lity of ma cro gol s lea ds to supersaturation which in
(d)
tum ma ke cry sta ls and fra ctu re
the pro duc t on storage.

synthetic bases and a num ber of

3, Emulsifying Ba ses : Th ese are
le in the market. So me of these
proprietary syn the tic bas es are ava ilab
are described as un de r:-
lyc eri des of saturated vegetable
(i) Witepsol : Th ey con sis t of trig
acid wit h var yin g per cen tag e of par tial esters. A sm all am oun t of
fatty
ate s. Th e suppositories pre par ed
beeswax is add ed for use in ho t clim t
coo led rapidly, in ord er to pre ven
with witepsol bas es sho uld not be
ctu re. Th e mo uld sho uld also be
them from bec om ing bri ttle and fra
es of suppositories.
properly lubricated to get goo d qua liti
Ma ssa est ari num : It is a mi xtu re of mo no, di- and triglycerides
(ii)
ted fat ty aci ds ha vin g the for mu la C 11 H2 3C OO H to
of sat ura
as ade ps solidus.
C17H35COOH. Th is is als o kno wn
ess and tas tele ss solid. It has a
It is a white, bri ttle , alm ost odo url
le in var iou s gra des but grade B is
m.p. 33.5 to 35. 5°C . Th ey are ava ilab
commonly used in dis pen sin g.
(iii) Ma ssu ppo l : It con sis ts of gly cer yl est ers ma inl y of lauric acid to
wh·
sma]I am oun t of gJy cer yl mo nos tea rat e has bee n add ed to improve
. ich
rts Water absorbing cap aci ty.
Advantages ove r the ob rom a oil
(a) They sol idi fy rap idl y.
(b) They are non -irr itan t.
req uir ed.
(c) The lub ric atio n of mo uld is not
phy sic al properties of the base.
(d) Overheating doe s not aff ect the
270 DISPENSING PHAD~ •.
-~ uuVV\Cy

(e) They can absorb fairly large amount of water or aqueous li

uids.1 q-
(f) The white, odourless, clean and attractive suppositories are Pro-
duced.
(g) They are less liable to get rancid.
Disadvantages
(a) They should not be cooled rapidly in a refrigerator because the
~~~~- y
(b) They are not very viscous on melting, so the medicaments
incorporated with the base settle down rapidly.

PREPARATION OF SUPPOSITORIES
The ~uppositories are prepared by any of the following methods:-
(A) Rolling method
(B) Hot process or fusion method
(C) Cold compression method
(A) Rolling method : It is an ancient method of preparing the
suppositories. The suppository base is rolled and then desired shape is
given with the hand. The method is not used nowadays.
(B) Hot process or fusion method: This method is commonly used
in the preparation of suppositories for dispensing purposes. The sup-
pository base is melted, the medicament is incorporated in it and filled
in lubricated mould. On cooling, suppositories are formed which are
removed from the suppository mou~d. /
Suppository mould The suppository mould of various types and
sizes are available in the market for commercial use. In dispensing, the
suppository mould having 6-12 cavities, with desired shape and size may
be used. These moulds are generally made up of stainless steel, nickel
copper alloy, brass, aluminium or plastic. (Fig. 12.1)

0
Fig. 12.1 Dispensing suppository mould
0
 JD DOSAGE FOR MS-S UPP OSIT ORIE S & PESSARIE
seMJSOL S 2 71
c~-11- ositofY mou ld can be open ed longitudinally by rem
ovin g the
fbe suPP ectr e of the plat es. The mou ld is open
c ~ ed at the time of
eW 1·11 the bric atio n and rem ova1 o f supp osito. .
nes. .
·g' 1u mov
scrans111 1 The mou ld is
d.
ing the p ates an unm ersed'm hot wate r cont ..
1 auun g
\:aned by Ar~ter was hing with wate r, the mou ld is drie
c ent d thor ough ly.
deterg · lubr ican t is appl ied. Eve ry care shou ld
be taken, so that the
fben ~~e of the cav~ties of the mou ld ~o not
have any scra tch,
inner ~urf ppos itori es with unev en surf ace will be
rW1se su prod uced .
ottie . tion of mou ld The lubr icati on of the supposito
Lubr1ca ry mou ld is
. . case coco a butt er, or g1ycer o-ge latm . .
base is used for the
essenua.1 in of supp osito ries. Tab le 12.1 show s diffe
aration rent type s of lubri-
prep .
d for diffe rent type s of supp osito ry base.
cants use

--s.No.
l.
Name of the Bas e

Cocoa butte r
TAB LE 12.1

Lub rica nt Used

Soft soap 10 g
Glyc erin 10 g
Alco hol 90% 50 ml
2. Glycero-gelatin Liqu id para ffin or Arac his oil
3. Emulsifying base (Syn theti c base ) No lubri cant is used .

The lubricant shou ld be appl ied with the help of

a brus h or a swa b
made of gauze. Cott on woo l shou ld not be used
beca use the cott on
fibres get detached from it. Exc essi ve lubr icati on
of the mou ld shou ld
be avoided. The exce ss of lubr ican t can be drai ned
by clos ing the mou ld
and put it in the inve rted posi tion on a whi te tile.
Calibration of the mou ld · Gen eral ly a stan
dard mou ld of one
gramme capacity is used . The calib ratio n of the
mou ld is nece ssar y,
because the size of the supp osito ry from a part icul
ar mou ld rem ains the
~~:e, but the weig ht vari es. This is due to the reas
on, that dens ity of
/ .ebrent bases and med icam ents are diffe rent . So
a11 rated fo . d. . d the mou ld shou ld be
ing rm ivi ual base and med icam ents . This is don
e by prep ar-
thena;et of supp osito ries usin g the base , weig hing
nd the supp osito ries and
lllout;_ the aver age mea n whi ch will indi cate the
true capa city of the
Oisplac
lar mould .eme ~t valu es The volu me of a supp
osito ry from a part icu-
llledicain is umf orm but its wei ght will vary beca use
the dens ities of the
lllould wents usua lly diff er from the dens ity of the
base with whi ch the
as calibrated. To prep are the supp osito ries of
unifo!ID and
272 DISPENSING PH A l h -
-~ AC'f
accurate weight, allowance must be made for the change in d .
the mass due to added medicaments. For this purpose, the dis e1nsity of
. . ak . 'd . p acenient
value of the med1cament 1s t en mto cons1 eration.
Displacement value is defined as "The quantity of the d .
displaces one part of the base". The displacement
. . . .h ~
values of s::g
Which
me of th
medicament used m suppos1tones wit re1erence to cocoa b t e
. . u ter ar
given m Table 12.2. e
TABLE 12.2

S.No. Name of the Medicament Displacement Value.__

1. / Aminophylline 1.5
2. Boric acid 1.5
3. Castor oil 1.0
4. Chloral hydrate 1.5
0
5. Cocaine hydrochloride 1.5
6. H ydrocortisone acetate 1.5
7. Ichthammol 1.0
8. ✓ Iodoform 4.0
9. Morphine hydrochloride 1.5
10. Phenobarbitone 1.0
11. Resorcinol 1.0
12. Tannie acid 1.0
13. Zinc oxide 5.0

The displacement value of a given medicament may be determined as

follows:-
1. Prepare and weigh 6 suppositories containing theobroma oil (or
other base) = a gramme.
2. Prepare and weigh 6 suppositories containing, say 40 per cent
medicament = b gramme.
3. Calculate the amount of theobroma oil present in medicated
suppositories.
60
=-- =
x b c gramme
100
. dicated
4. Calculate the amount of medicament present m the me
suppositories.
40
=-- x b =d gramme
100
 serJJSOLID DOSAGE FORMS-SUPPOSITORIES & PESSARIES 273

calculate the amount of theobroma oil displaced by d g of

5. rnedicarnent == (a - c) gramme
d
Displacement value of the medicament = ___
a-c

le 12.l Calculate the displacement value of zinc oxide in

· · 40% of zmc
· · contalnmg
EiaJJlP oil suppos1tones · ·
oxide and is pre-
theobr?rna g mould. The weight of 8 suppositories is 11 .7 4 gramme.
ared in a 1 . . . .
p Weight of 8 suppos1tones contammg theobroma oil = I x 8 = 8 g
Weight of 8 suppositories containing 40% of zinc oxide = 11.74 g
60
Amount of theobroma oil present is 8 suppositories == - - x 11.74
100
= 7.044 g
40
Amount of medicament present in 8 suppositories =- -x
100
11.74

= 4.696 g
Amount of theobroma oil displaced by 4.696 g of medicament
= 8 - 7.044 = 0.956 g
4.696
Displacement valua'= - - - = 4.912 = Approx. 5
0.956

Method of Preparation
(1) Thoroughly clean and lubricate the mould with a suitable lubri-
cant. Keep it on ice in the inverted position to cool and drain an excess
of the lubricant. The lubrication of the mould is not required in case the
emulsifying base or synthetic base is used.
(2) Heat the china dish over water bath. To this add the required
quantity
. .
of cocoa b utter or any other base af ter taki ng mto account the
d~~ .
ab! 1 ment value of the medicament. Allowance 1s made for unavo1d-
.

e wastage d unng. . .
preparation by calculating for two extra suppos1tones.
bas?) Remove the china dish from water bath, when two-third of the
Procelllelts and stir thoroughly until whole of the mass melts. The
ss prevents over heating of the base.
. . of powdered medicament . ·
corp(4) Place the weighed quantity to be m-
0 rated • the suppository base on an ointment tile. Pour about
With
ha!f of
spatula the melt~ base over it. Mix it thoroughly with a flexible
so that· Transfer the mixed mass to the china dish and mix thoroughly
a ho ·
·
mogenous mass is formed.
 274 DISPENSING PfiARMAcy

(5) Warm the china dish over water bath for a few seconds With
constant stirring, so that mass becomes pourable.
(6) Pour the melted mass into the cavities uf the suppository mould
kept over the ice. Fill each cavity to overflowing, in order to prevent th~
formation of hollows in the tops of the finished suppositories because
cocoa butter contracts on cooling and hollows are formed at the top of
the suppositories. The precautions must be taken while pouring the mass
· into the cavities. It must be continuously stirred to ensure even distribu-
tion of the medicament in all the suppositories.
(7) Remove the excess of mass with the help of sharp knife or blade
when the mass is properly set.
(8) Keep the mould over ice or in cool place for 10 to 15 minutes.
(9) Open the mould and remov e the suppositories.
(10) Wipe off the suppository lightly with a clean cloth or filter
paper.
(11) Wrap the individual suppository in a wax paper.

Example 12.2 Prepare and dispense the iodoform suppositories.

13c
Iodofo rm 0.9 g
Cocoa butter sufficient quantity
Make the suppositories.
Send 8 suppositories of 2 g each.
Direction : One suppository to be inserted into rectum at bed time.
Note : Displacement value of iodoform is 4.0
Calculation : Calculate for 2 extra suppositories
Weigh t of cocoa butter for one suppository = 2 g
:. Weigh t of cocoa butter for 10 suppositories = 2 x 10 = 20 g
Weigh t of iodoform for one suppository = 0.9 g
:. Weigh t of cocoa butter for 10 suppositories = 0.9 x 10 = 9 g
Displa cemen t value of iodoforrn = 4.0
The quantity of cocoa Total amoun t Total amount of drug
butter required = of base
Displacement value
9.0
= 20
4.0
=-= 20 - 2.25 = 17.75 g
 sons oLID DOSAGE FOR.\.IS-SCPPOSITORJES & PESS
ARIES 275

~ula for 10 supp ositories is as unde r-

·
foi= 9.0 g
Iodo form
coco a butte r 1"7.7 5 g

thermola-
C Cold com pres sion m etho d : The method is usefu l for
• 9 d insoluble drug s beca use
1 heat ing and stirring of the base with
;,ile an . d Th e vano . us steps invo lved in this meth od
~ . arnent is not reqm re .
;nediC
,,, under:-
?re ...., d with an equa l
- 1 Cocoa butter is grate d. The ingredients are mixe
' •i\- of Qrated coco a butte r.
•
Add the rema ining amount of e!ITated
Jllafi□ L, ...,
a butte r to be
.:·ocoa burrer. \\nil e cal~ ulau ng the amo unt of coco
e for unav oid-
c.:orporared wi~ the medicam~nts. allowances are mad
::ble wascage dunn g the preparatrnn.
on hand or
2 Toe com pres sion of the prep ared mass is done
is plac ed in
po,;i.·er-operated com pres sion machines. The prep ared mass
"c.-linder ' C and force d throu gh a narro\Y opening ·o·
by means of a
mou ld ·G · are
pis;on ·p- into a mould. The threads of mass passing into
On the remo val
;:cmpressed until a hom ogen eous fused mass is formed.
o: retaining stop plate ·S · the suppositories are
eject ed by furth er
ramm atica lly in
pressure. The operation of the mach ine is show n diag
F1g 12.2.

I STOP
I s I
PLATE
=; I ~

I
MOULD
~ -
G NARR OW
>c C
OPENING

PREPARED
MASS
0

CYLINDER
C

_ P__ PISTON

- ....-

--- - .....
Fig. 12.2 Cold comp ressi on nach ine for suppositories
276 DISPENSING PHARMAcy

The moulds are of different sizes and contain. several cavities. The
mass and the compression cylinder o~ the machme may _be chilled to
prevent heat of compression from making the mass too flmd.
The method is not suitable for suppositories in which glycero-gelatin
base or any other base in which melting is essential for its preparation.

Packaging and Storage

Suppositories are usually packed in shallow partitioned card board
boxes which can hold them in upright position and do not allow them to
come in contact with each other. Many commer cial suppositories are
packed separately in aluminium foil or PVC polythene strip. Glycero-
gelatin suppositories are often packed in tightly closed screw capped
glass cont:iiners. Nowadays, suppositories are directly moulded into
primary packaging made of plastic material or aluminium foils. The
moulds are sealed. The excess is trimmed off and finally packed in
/
cartons.
The suppositories are required to be stored in a cold place so that
they can retain their shape at the room temperature.

Mechanism of Drug Actions by Suppositores

Suppositories are used for following types of action.
1. Local action : when suppository is inserted into a body it may
either get melted or dissolved and the medicam ent present in it is carried
to the tissue. The medicament thus retain in the cavity for its localised
effect.
Rectal suppositories are used for their localised action to relieve
constipation pain, irritation, itching and inflammation due to hemorrhoids
(piles) or other anorectal condition. Rectal suppositories containing
local anesthetics, vasoconstrictiors, astringents, analgesics, soothing emol-
lients and protective agents are very popular for their localised effects.
Vaginal suppositories are commonly used to provide localised anti-
septic effect in the vaginal cavity against micro-o rganism s like
Trichomonas vaginalis, Candida alicans etc.
Uretheral suppositories arc used for its local anaesthetic and antibac-
terial action.

2. Systemic action : The suppository on its insertion into a bodY

cavity, gets melted or dissolved. The drug released is distributed throu~h-
out the tissues of mucous membrane and get absorbed. Systemic ac~on
of drug from suppository can be obtained through the rectum or vagtn•
but rectal route provides the best site for the drug absorption.
fr~-- "
..
LID DOSAGE fOR.'-fS-SCPPOS ITORIES & PESSARIES
,C'\fJ.:>0
277

Or , ffecting Drug Absorption from Rectal Suppositories

f .,ctof'S ..~ .i·na t-actors a..ffects the drue: absorption when it is adminis-
. ....
" .;10]lo\' == .
fhe . the
c ..,.,.., of rectal supposnones.
101J..U

:e.--et in hvsical factors.: Human rectum is 15-~0 cm in length. There

1, p · ,-ascularity m the sub-mucosal rcg10n of the rectum wall 1
is JbUD~t and jsmphatic Yessel. The following factors affect the
"dl blOO • ~
\\1 rpooc from the re\. rum .
.i.,o(; [ircu.'ar rowe : In rectal ab sorpn?n . 1anon
. of dru.g. pos tal _circu .
. 1s
~-
b,-passed giYing_ an adY~tage of preYentrng the b10n:ansfo~a-
-~n of drugs m the liver. The lower hemorrh01dal vems
~urrounding the colon receiYe the absorbed drug and initiate its
;ircularion throughout the body by passing the liver. Lymphatic
circulation also assist rectal drug absorption.
lii Colonic conrenr : An empty rectum has more efficiency to
absorb drug than from one that contain fecal matter because
drug has better opportunity to make contact with the absorbing
surface of the recmm. It is ad\isable to eYacuate the rectum by
giYing suitable enema before administering any medicated sup-
pository.
(iiiJ PH and :ack of buffering capacity of rectal fluid : pH of the
rectal fluid is - to S and no buffering capacity. Hence there is
no chemica: chane:e of administered drue: in the rectum.
- V

2. Physico-Chemicai factors : The following physico-chemic al

factors affects the absorption of drug administered in the form of sup-
pository.
Particle si::,e : The smaller the particle size of the dispensed drug
(i)
in the base. the more readil: the dissolution of the particle and
hence greater the chance for rapid absorption e.g. aspirin sup-
positories prepared in cocoa butter base absorb readily when
aspirin is present in small particle size than large size particles.
Cii) l'·.1ature of the base : The nature of the suppository base which
may either softens. melts or dissolYe. affects the release of drug
from it. If the base interacts with the drug. inhibits its release
aoct ultimately drug absorption is hindered.~
(iii)
;ipi~-water solubility of drug : The lipid-water partition co-
s fficie~t of a drug is an important factor affecting selection of
t~Ppository base. A lipophilic drug dispersed in a fatty supposi-
bo1 base_ has less tendency to escape to the surrounding aqueous
Wh'y fluids than a hydrophilic drug dispersed in a fatty base
ich forms a condition of saturation.
2?S DISPE NSING PHAPJviAcy

Wate r soluble base such as polye thyle ne glycols dissolve

i
anorectal fluids, release for absorption both wate r soluble and
~
soluble drugs. The rate of absor ption of a drug is not chang0
ed
beyond a certain limit of incre ase in drug concentration.
(iv) Presence of adjuncts in base : Adjun_cts such _as surfa
ctants may
be added to !he suppository bases to impr ove its water absor
bing
property. Thus more polar drugs or their solutions can
be
incorporated in the base. They may also enha nce the rate
of
dissolution by retarding the surfa ce tensi on betw een the
fatty
base and the aqueous body fluids and then impr oves the rate
of
absorption.

PESSARIES
They are mean t for intro ducti on into the vagina. They are
larger than
rectal suppositories and vary in weig ht from 4 to 8 gram
me or more.
The pessaries may be conical, wedg e shape d or rod shaped.
Nowadays,
speci al shape d suppositories are manu factu red and are
supplied with
applicators to facilitate inser tion into the vagina.
The pessaries are also available as tablets and capsules
and are
know n as vagin al tablets and capsules respe ctive ly. The
pessaries of
ichthammol, crystal violet, lactic acid are manu factu red by
using glycero-
gelatin base.
Mou lded pessaries are pack ed simil ar to glyce ro-ge latin suppo
sitories
while table t containers are suita ble for the comp resse d type
pessaries.
Sometimes instructions are given on the label to mois ten
pessaries with
wate r befor e insertion into vagin a to reduc e the stinging
caused by
osmo tic withd rawa l of the wate r from the tissu es during solut
ion in the
vagina. Di-io dohy droxy quino line and nysta tin, pessaries shoul
d always
be label led with this advice. Pessaries shou ld be store d in
a cool place.
Example 12.3 Prepa re and dispe nse 8 lactic acid pessaries B.P.C.
f3c
Lactic acid 5 g
Glyc erin suppositories mass 100 g
Mak e the pessaries.
Send 8 pessaries.
Direction : One to be inser ted at night.
Note : Pessaries conta ining 5 per cent of lactic acid and prepa
red in
8 g moul d are supp lied when no stren gth is presc ribed .
,~•~- z serv11s0LID DOSAGE FORMS-SUPPOSITORIES & PESSARIES 279
c~-l fbe quantity of glycero-gelatin base for 10 pessaries
= 10 X 8 X 1.2 = 96.0 g
flence, 100 g is the convenient amount to prepare 10 pessaries.
100 X 5
acid required = 5
Am0 Unt of lactic 100 1 = g

formula . 5g
Lactic acid
Glycero-gelatin base 100 g

!Jethod
l. Lubricate the mould with liquid paraffin or arachis oil. Invert
and cool.
2. Heat the glycerin in a china dish at 100°C and keep it hot on a
water bath.
3. Add the gelatin to the water. Stir gently to wet the material
thoroughly. Add the hot glycerin, stir again and heat the china
dish on boiling water bath for 15 minutes or until a clear
solution is made. Glycero-gelatin base is prepared. Adjust its
weight to 100 g by evaporating the water.
4. Remove 5 g of the base with a metal spoon or spatula. Add 5.0
g of lactic acid. Stir well and pour into a chilled mould. Mould
should be opened as long as possible because lactic acid lowers
the setting point of the glycero-gelatin mass.
5. Wrap the individual pessary in a metal foil or waxed paper, as
lactic acid pessaries are very hygroscopic. Pack in a well-closed
Jar.

MARKETED SEMISOLID DOSAGE FORMS

(A) Suppositories
1. Dulcolax suppositories (Germany Remedies) : contains Bisacodyl
5 mg (Infants) and 10 mg (Adults) in suppository base.
2· Conlax suppositories (Bliss Chemicals and Pharmceuticals In-
dia) : contains Bisacodyl 5 mg & 10 mg in suppositories base.

(B) Pessaries
1. Betadine pessaries (Win Medicare) : contains Po vidone Iodine
200 mg.
2· Canesten vaginal tablets (Bayer India) : contains Clotrlmazole
100 mg.
280 DISPENSING PHAR'•
,v1Acy
3. Jmidil vaginal tablets (Lyka Lah.) : contains Clotrimazole
100
mg.
4. Tinicide- V pessaries (Blue Cross Laboratories) : conta·
Clotrimazole 200 mg and Tinidazole 500 mg). ins
5. Kemicetine vaginal suppositories (Mac Laboratories) ; contains
Chloramphenicol.
6. Candizole-T vaginal tablets (M.M. Labs) : contains Tinidazole
500 mg, Micronazole nitrate 100 mg, Neomycin sulphate equiva~
lent to Neomycin 20 mg.
7. Wokadine vaginal pessaries (Wockhardt) : Each contains Povi-
done iodine 200 mg.