Suppositories

Semisolid Dosage Forms-

Suppositories and Pessaries
Definition
Suppositories are solid dosage forms intended for insertion into body cavities other than mouth. They may
be inserted into rectum, vagina or nasal cavity. These are available in different shapes, sizes and weights.
Suppositories they will melt, soften, or dissolve and exert localized or systemic effects

Advantages
1) Suppositories are unit dosage form of drugs.
2) Can exert local effect on rectal mucosa.
3) Used to promote evacuation of bowel.
4) Avoid any gastrointestinal irritation.
5) Can be used in unconscious patients (e.g. during fitting).
6) Can be used for systemic absorption of drugs and avoid first-pass metabolism.
7) Children or old people who cannot swallow oral medication.
8) Post-operative people who cannot be administered oral medication.
9) Can be given to People suffering from severe nausea or vomiting.
10) drugs in suppositories are slowly absorbed giving sustained action
1. The problem of patient acceptability.
2. Suppositories are not suitable for patients suffering from diarrhea.
3.
4. Disadvantages
5. the irritant drug can’t be administered by this route
6. Incomplete absorption may be obtained because suppository usually promotes evacuation of the bowel
7. the suppositories are required to be stored at low temperature (100C to 200C).
8. suppositories cannot be prepared easily

Type of suppositories
a. Rectal suppositories
 they are introduced into the rectum for the systemic effect
 these are made from theobroma oil and available in various size and shapes
 For adults weigh 2 gm and are torpedo shape.
 Children's suppositories weigh about 1 gm.

b.Vaginal suppositories or Pessaries

 these are meant for introduction into vagina and used for their local action
 these are also known as pessaries
 Weight about 4-8gm and are moulded in globular, rod shaped or oviform shape or compressed on
a tablet press into conical shapes.
 now days vaginal tablets and vaginal capsules are also available

c. Urethral suppositories
 These are meant for introduction into urethra and also called bougies
 These are pencil shape. Those intended for males weigh 4 gm each and are 100-150 mm long.
 Those for females are 2 gm each and 60-75 mm in length.

d. Nasal suppositories
1
D.S.K.C.P Sangli
Suppositories
 these are meant for introduction into nasal cavity and also called nasal bougies or buginaria
 They are prepared with glycerogelatin base.
 They weigh about 1 gm and length 9-10 cm.
e. Ear cones
 They meant for introduction into ear and also known as aurinaria
 Rarely used and these are thin, long and cylindrical in shapeand weight about 1gm
 Theobroma oil is used as base.
 Prepared in urethral bougies mould and cut according to size.
5

New trends of suppositories

1. Tablet suppositories
 This type of tablets suppositories are prepared by compression like tablets.
 Such type of suppositories used for rectal & vaginal purposes.
 Pessaries tablet suppositories are present in almond like shape.
 Rectal tablets covered with thin layers of materials such as polyethylene glycol for protecting.
2. Layered suppositories

 In these type of suppositories contains different drugs in different layers.

 So that, incompatibility drugs can be separated from each other.
 Similarly drugs having different melting points can be incorporated to control the absorption rate.

3. Coated suppositories
 These type of suppositories are coated with polyethylene glycol, cetyl alcohol etc. by simply dipping
in solution.
 coating helps to control the release of medicament
 These suppositories provide protection action during storage and impart lubricant properties.

4. Capsule suppositories
 Soft gelatine capsules of different shapes & size are prepared in these type of suppositories.
 Capsule suppositories are filled with liquids, semisolids or solids.
 there is great demand of such capsule suppositories

5. Disposable suppositories

 moulds are made up of plastic material or tin foils

 suppository material are poured into mould and cooled after that excess of mass is trimmed off with
help of sharp knife or blade and mould ate sealed
 they are cheaper and elegant
 the shape of suppositories can be changed at lower cost
 advantage of disposable mould is when suppositories mass melts during storage it will remain in the
mould and reconverted into suppositories after cooling

Suppository bases

2
D.S.K.C.P Sangli
Suppositories
Definition Suppositories bases are used to prepared suppositories, so that they can retain its shape, and
firmness during storage and administration. Suppositories they will melt, soften, or dissolve in body cavity
fluids, when inserted into body cavity

Ideal Suppository Base

1. It should melt at rectal temperature (360C) or dissolve or disperse in body fluid.
2. Release medicaments easily.
3. Shape should remain intact while handling.
4. Non-toxic and non-irritant to sensitive and inflammed mucous membrane.
5. It should be stable on storage i.e. it does not change colour, odour, or drug release pattern.
6. Compatible with drug and other additives.
7. It should shrink so that it comes out easily from the mould without the use of any lubricants.
8. it should be stable if heated above its melting point
9. it should be easily moulded and not adhere to the mould
10. it should be good in appearance
11. it should be easily mouldable by pouring or cold compression

Classification of suppository bases

1. Fatty bases: They melt at body temperature.
eg. theobroma oil, emulsified theobroma oil, hydrogenated oils.
2. Water-soluble or water miscible base: They dissolve or disperse in rectal secretions.
eg. glycero-gelatin base, soap-glycerin baase, polyethylene glycols
3. Emulsifying bases: They emulsifies small amount of aqueous solution of drug.
eg. witepsol, massa estarinum, massuppol

1. Fatty Bases:
Designed to melt at body temperature.
Example: Theobroma oil (Cocoa butter), Synthetic fats.

A) Theobroma oil (Cocoa butter):

• It is a yellowish-white solid with an odour of chocolate obtained from crushed and roasted seeds of
theobroma cocoa and is a mixture of glyceryl esters of stearic, oleic palmitic and other fatty acids.
it is known as cocoa butter and it has butter like consistency having melting point of 30-350C
Advantages
1. A melting range of 30-36°C (solid at room temperature but melts in the body).
2. Readily melted on warming, rapid setting on cooling.
3. Miscible with many ingredients.
4. Non-irritating.

Disadvantages
1. Polymorphism:
 When melted and cooled it solidifies in different crystalline forms, depending on the temperature of
melting, rate of cooling and the size of the mass.
 If melted at not more than 36°C and slowly cooled it forms stable beta crystals with normal
melting point.
 If over-heated then cooled it produce unstable gamma crystals which melt at about 15°C or
alpha crystals melting at 20°C.
3
D.S.K.C.P Sangli
Suppositories
 Cocoa butter must be slowly melted over a warm water bath to avoid the formation of the unstable
crystalline form.
2. Adherence to mould
Because theobroma oil does not contract enough on cooling to loosen the suppositories in the mould,
sticking may occur, particularly if the mould is worn. This is prevented by lubricating the mould before use.
3. Softening point too low for hot climates
To raise the softening point, whit beeswax may be added to theobroma oil suppositories intended for use in
tropical and subtropical countries.
4. Melting point reduced by soluble ingredients
Substances, such as chloral hydrate, that dissolve in theobroma oil, may lower its melting point to such an
extent that the suppositories are too soft for use. To restore the melting point, a controlled amount of white
beeswax may be added.
5. Slow deterioration during storage
This is due to oxidation of the unsaturated glycerides.
6. Poor water absorbing capacity
This fault can be improved by the addition of emulsifying agents.
7. Leakage from the body
Sometimes melted base escapes from the rectum or vagina. This is most troublesome with pessaries because
of their larger size, and therefore, these are rarely made with theobroma oil. so theobroma oil only used to
prepare rectal suppositories
8. Relatively high cost

B) Hydrogenated oils:
As a substitute of theobroma oil, a number of hydrogenated oils.
e.g. hydrogenated edible oil, arachis oil, coconut oil, palm kernel oil, stearic and a mixture of oleic and
stearic acids are recommended.
Advantages
1. Their solidifying points are unaffected by overheating.
2. They have good resistance to oxidation because their unsaturated fatty acids have been reduced.
3. Their emulsifying and water absorbing capacities are good.
4. No mould lubricant is required because they contract significantly on cooling.
5. They produce colorless, odourless and elegant suppositories. 19
Disadvantages
1. They should not be cooled in refrigerator because they become brittle if cooled quickly.
2. They are more fluid than theobroma oil when melted and at this stage greater sedimentation of the
added substances. This difficulty can be overcome by adding some thickening agent such as bentonite,
magnesium stearate etc.

C) Emulsified theobroma oil

This may be used as a base when large quantities of aqueous solution are to be incorporated. The use of 5%
glyceryl monostearate, 10% lentte wax, 2-3% cetyl alchol, 4% beeswax and 12% spermaceti is
recommended to prepare emulsified theobroma oil suppositories.

A) Glycero-Gelatin Base:
 This is a mixture of glycerol and water made into a stiff jelly by adding gelatin.
 It is used for the preparation of jellies, suppositories and pessaries. The stiffness of the mass depends
upon the
 Proportion of gelatin used which is adjusted according to its use.
4
D.S.K.C.P Sangli
Suppositories
 Depending upon the compatibility of the drugs used a suitable type of gelatin is selected for the
purpose. Two types of gelatins are used as suppository base.
 Type-A or Pharmagel-A which is acidic in nature and used for acidic drugs having iso-electric
point (7-9)
 Type-B or Pharmagel-B which is alkaline in nature and used for alkaline drugs having iso-
electric point (4.7 to 5.0)
Disadvantages:
Glycerogelatin base suppositories are less commonly used than the fatty base suppositories because:
 Glycerol has laxative action.
 They are more difficult to prepare and handle.
 They are hygroscopic, hence must be carefully stored.
 Gelatin is incompatible with drugs those precipitate with the protein e.g. tannic acid, ferric
chloride, gallic acid, etc.

B) Soap-Glycerin Suppositories:
 In this case gelatin and curd soap or sodium stearate which makes the glycerin sufficiently hard
for
 suppositories and a large quantity of glycerin up to 95% of the mass can be incorporated.
 Further the soap helps in the evacuation of glycerin.
 The soap glycerin suppositories have the disadvantage that they are very hygroscopic, therefore
they must be protected from atmosphere and wrapped in waxed paper or tin foil.

C) Polyethylene glycol bases/Macrogol bases (Carbowaxes)

 Depending on their molecular weight they are available in different physical forms.
 the marogols having molecular weight less than 1000 are liquids and those with molecular weight
higher than 1000 are wax like solids.
 By choosing a suitable combination a suppository base with the desired characteristics can be
prepared.
Advantages
1. they are chemically stable
2. they are non-irritant
3. they do not allow the bacterial mould growth to take place
4. they are physiologically inert substance
5. The mixtures generally have a melting point above 420C, hence, does not require cool storage
and they are satisfactory for use in hot climate.
6. Because of the high melting point they do not melt in the body cavity, rather they gradually
dissolve and disperse, releasing the drug slowly.
7. They do not stick to the wall of the mould since they contract significantly on cooling.
8. the suppositories made from macrogols have clean and smooth appearance
Disadvantages
1. they are hygroscopic and hence require special storage condition to store them
2. They are incompatible with certain drugs like tannins, phenols etc.
3. high solubility of macrogols lead to supersaturation which in turn make crystals and fracture the
product on storage
4. Its good solvent properties can result in retention of the drug in the liquefied base, in the body,
thereby reducing their therapeutics activity.
3. Emulsifying Bases:
These are synthetic bases and a number of proprietary bases of very good quality are available, few of
which are described below:

5
D.S.K.C.P Sangli
Suppositories
A) Witepsol: They consist of triglycerides of saturated vegetable acids (chain length C12 to C18)
with varying proportions of partial esters.

 a small amount of beeswax is added for use in hot climates

 It should not be cooled rapidly as it become brittle and fracture.
 Lubrication is required.

B) Massa Esterium: This is another range of bases, consisting of a mixture of di-, tri- and mono-
glycerides of saturated fatty acids with chain lengths of C11 to C17.

 It is a white, brittle, almost odourless and tasteless solid.

 It has a melting.point . 33.5 to 35.50C.
 They are available in various grades but grade B is commonly used in dispensing.

C) Massuppol: It consists of glyceryl esters mainly of lauric acid, to which a small amount of
glyceryl monostearate has been added to improve its water absorbing capacity.

Advantages of these bases over cocoa butter:

1. Overheating does not alter the physical characteristics.
2. They do not stick to the mould. They do not require previous lubrication of the mould
3. They solidify rapidly.
4. They are less liable to get rancid.
5. They can absorb fairly large amount of aqueous liquids.
Disadvantages
1. They should not be cooled rapidly in a refrigerator because they become brittle.
2. They are not very viscous on melting, so medicaments incorporated with the base settle down rapidly

Preparation of suppositories
1. Rolling method
2. Hot process or fusion method
3. Cold compression method

1. Rolling method
1. It is the oldest and simplest method of suppository preparation and may be used when only a few
suppositories are to be prepared in a cocoa butter base.
2. It has the advantage of avoiding the necessity of heating the cocoa butter.
3. A plastic-like mass is prepared by triturating grated cocoa butter and active ingredients in a mortar.
4. The mass is formed into a ball in the palm of the hands, then rolled into a uniform cylinder with a
large spatula or small flat board on a pill tile.
5. The cylinder is then cut into the appropriate number of pieces which are rolled on one end to produce
a conical shape.
6. Effective hand rolling requires considerable practice and skill.

2. Hot process or fusion method

Hot process or Fusion method is commonly used method for Preparation of suppositories.
a. Thoroughly Clean & lubricate the mould with suitable lubricant. Keep it on ice in inverted
position to cool & drain excess lubricant.

6
D.S.K.C.P Sangli
Suppositories
b. Heat the china dish over water bath. To this add required quantityof suppository base after
taking into account the displacement value of medicament. & calculating for two extra
suppositories for unavoidable wastage.
c. Remove the dish from water bath, when 2/3rd of base melts & stir thoroughly until whole mass
melts. To avoid overheating.
d. Place the weighed quantity of medicament on an ointment tile. Pour about half of melted base
over it. Mix it thoroughly with spatula.
e. Transfer the mixed mass again to china dish, mix it thoroughly& warm china dish over water
bath for few seconds with constant stirring.
f. Pour the melted mass into the cavities of suppository mould. Kept over ice. Fill each cavity to
over flowing, to prevent the formation of holes in suppositories.
g. Remove excess of mass with the help of sharp knife.
h. Open the mould& remove suppositories.
i. Wipe off the suppository lightly with a clean cloth or filter paper.
j. Wrap the individual suppository in a wax paper.

3. Cold compression method of preparation of suppositories.

Compression moulding is a method of preparing suppositories from a mixed mass of grated suppository
basesand medicaments which is forced into a special compression mould using suppository making machines.
1. The suppository basesand the other ingredients are combined by thorough mixing.
2. The friction of the process causing the basesto soften into a past-like consistency.
3. In the compression machine, the suppository mass is placed into a cylinder which is then closed.
4. Pressure is applied from one end to release the mass from the other end into the suppository mould or
die.
5. When the die is filled with the mass, a movable end plate at the back of the die is removed and when
additional pressure is applied to the mass in the cylinder, the formed suppositories are ejected.
6. The end plate is returned, and the process is repeated until all of the suppository mass has been used.

7
D.S.K.C.P Sangli
Suppositories
Storage and packaging
 Suppositories are usually packed in tin or aluminum, paper or plastic.
 Poorly packed suppositories may give rise to staining, breakage or deformation by melting.
 Both cocoa butter and glycerinated gelatin suppositories stored preferably in a refrigerator.
 Polyethylene glycol suppositories stored at usual room temperature without the requirement of
refrigeration.

Define “displacement value”. Write its Importance in suppository

Definition: Displacement value of a medicament is defined as “The quantity of the drug which displaces
one part of the base.”
 Importance:
 The volume of suppository from a particular mould is uniform but its weight will vary because the
densities of medicaments usually differ from the density of the base with which the mould is calibrated
 For preparation of uniform suppositories, accurate weight, allowance must be made for the change in
density of the mass due to added medicament. For this purpose displacement value of the medicament
is taken into consideration.

How will you dispense following prescription

Boric acid ………………………………10 gr
Coca Butter …………………………......q.s.
Preapare 5 pessaries.
Capacity of mould is 120 grains
Problem Solution – (4 marks)
Calculate for 6 pessaries.
Weight of Cocoa butter for 6 pessaries. = 720 grains
Weight of Boric acid for 6 pessaries. = 60 grains
Displacement Value of Boric acid = 1.5
The quantity of Cocoa butter required = Total amount of base – Total amount of drug / Displacement Value
= 720 – 60/ 1.5

= 720- 40 = 680 grains

Formula for 6 Suppositories is
Boric acid 60 grains
Cocoa butter 680 grains
Or
Calculate for 6 pessaries.
Weight of Cocoa butter for 6 pessaries. = 120 X 65X6 = 46.8 g
Weight of Boric acid for 6 pessaries. = 60 x 65 = 3.9g
Displacement Value of Boric acid = 1.5
The quantity of Cocoa butter required = Total amount of base – Total amount of drug / Displacement Value
= 46.8 – 3.9/ 1.5
= 46.8- 2.6 = 44.2g
Formula for 6 Suppositories is
Boric acid 3.9 g
Cocoa butter 44.2 g

8
D.S.K.C.P Sangli
Suppositories

Calculate the displacement value of ZnO in theobroma oil suppositories containing 40% of ZnO and is
prepared in 1 gm mould. The weight of 08 suppositories is 11.74 gm.
Calculation: (3M)
1. Weight of 8 suppositories containing Theobroma oil = 1X 8 = 8 gm.
2. Weight of 8 suppositories containing 40% Zinc Oxide = 11.74 gm.
3. Amount of theobroma oil present in 8 suppositories = 60/100 X 11.74 = 7.044 gm.
4. Amount zinc oxide present in 8 suppositories = 40/100 X 11.74 = 4.696gm

5. Qty of theobroma oil displaced by Zinc oxide = 8 – 7.044 = 0.956 gm

6. Displacement value = Amount of drug/ qty of base displaced = 4.696/0.956 = 4.912 ≈ 5

Prepare and dispense the Iodoform suppositories

Iodoform 3grains
Cocoa butter sufficient quantity
Make suppositories
Prepare 12 suppositories of each 15 grain
Note: displacement value of Iodoform is 4.0

Ans
Calculate for 3 extra suppositories
Weight of Cocoa butter for 1 Suppository = 15 grains
Weight of Cocoa butter for 15 Suppositories = 15 X 15 = 225 grains
Weight of iodoform for 1 Suppository = 3 grains
Weight of iodoform for 15 Suppositories = 15 X 3 = 45 grains
Displacement Value of iodoform = 4.0
The quantity of Cocoa butter required = Total amount of base – Total amount of drug / Displacement Value
= 225 grains - 45 / 4
=213.75 grains = 214 grains

Pessaries
 Pessaries are a type of suppository intended for vaginal use.
 The larger size moulds are usually used in the preparation of pessaries such as 4 g and 8 g moulds.
 pessaries are also available as tablet and capsules and are known as vaginal tablet and capsule
respectively.
 moulded pessaries are packed similar to glycerol-gelatin suppositories while tablet container are
suitable for the compressed type pessaries.
 sometime instruction are given on the label to moisten pessaries with water before insertion into
vagina to reduce the stinging caused by osmotic withdrawal of the water from the tissues during
solution in the vagina.
 di-iodohydroxyquinoline and nystatin, pessaries should always be labelled with this advice
 Pessaries are used almost exclusively for local medication, the exception being prostaglandin
pessaries that do exert a systemic effect.

Differentiate between suppositories and pessaries

9
D.S.K.C.P Sangli
Suppositories
Suppositories
They are solid dosage form meant
for insertion into body cavities
other than mouth
They are available in different
shapes sizes and weight
The weight differs depending on
purpose for which it is use
Base used mostly cocoa butter
Suppositories used for systemic and
local action
Ex. Dulcolax suppositories
D.S.K.C.P Sangli
Pessaries
They are solid dosage form meant
for insertion into the vagina
They are available in conical,
wedge shape or rod shape
The weight ranges from 4 to 8gms
Base used glycerol-gelatin
Pessaries are used only for local
action.
Ex. Fluconazole pessaries.
10
Suppositories
What is HLB. Give its significance.

 [HLB] – Griffin developed a system to assists making systematic decisions about the amounts and types
of surfactants needed in stable emulsion. The system is called the HLB System (hydrophillic – Lipophilic
Balance)
 System and has an arbitrary scale of 1-18 HLB numbers are experimentally determined for different
emulsifiers in laboratory.
 An emulsifier having a low HLB number indicates that the number of hydrophilic groups present in the
molecule is less and it has a lipophillic character. For eg. spans generally have low HLB number & they
are oil soluble. Because of their oil soluble character, they favours w/o emulsion.
 A higher HLB number indicated that the emulsion has a large number of hydrophilic group & hence it is
hydrophilic in character. Therefore it favours o/w emulsion

HLB Range Application

4-6 w/o emulsifying
Agents
8-18 o/w Emulsifying
agents

Explain methods of evaluation of suspension.

Method of evaluation:
1. Sedimentation Method:
2. Rheological Method:
3. Electrokinetic's Method:
4. Micrometrics Method:
1. Sedimentation Method
1. Sedimentation volume is the most important parameter in the evaluation of the stability of
suspension
2. It is determined by keeping a measured volume of the suspension in a graduated cylinder in an
undisturbed position for a definite period of time and noted the ultimate height (Hu) of the sediment
and initial height of the total suspension.
3. The sedimentation volume F is the ratio of the ultimate height and initial height .(Hu/Ho)
4. The sedimentation volume plotted against time, the graph indicates the sedimentation pattern of
suspension on storage.
5. A stable suspension shows a horizontal or less steep curve.
6. The evaluation of redispersibility can also be determined by shaking the suspension and again find
out the sedimentation volume ( Hu/Ho).
2. Rheological Method:
1. The viscosity of the suspension is studied at different time intervals by using a good quality of
viscometer.
2. It provide useful information regarding stability of suspension.
3. Electrokinetic's Method:
1. The determination of surface electric charge or zeta potential is helpful to find out the stability of
suspension.
2. Certain zeta potentials produce more stable suspensions because of controlled flocculation.
3. Zeta potential can be calculated from the migration velocity of the particles measured by the
electrophoretic method.
4. Micrometrics Method:
1. The stability of suspension depends on the particle size of the disperse phase.
2. The size of the particle in a suspension may grow and may ultimately leads to the formation of lumps
or cracking.
11
D.S.K.C.P Sangli
Suppositories
3. So any change in the particle size with reference to time will provide useful information regarding
the stability of a suspension.
4. A change in particle size distribution and crystal habit may be studied by microscopy and coulter
counter method.

12
D.S.K.C.P Sangli