Semisolid Dosage Forms PDF

SEMISOLID DOSAGE FORMS
Phr. Bibek Singh Mahat

M. Pharm. (Industrial)
6/27/2012 bibekmahatsingh@gmail.com 1
y Ointments:-Type of ointments, classification and
selection of dermatological vehicles. Preparation and
stability of ointments by the following processes: (i)
Trituration, (ii) Fusion, (iii) Chemical reaction, (iv)
emulsification.
y Pastes: Differences between ointments and pastes.

Bases of p
pastes. Preparation
p of ppastes and their
preservation.
y Jellies: An introduction to the different types of jellies

and their preparation.
y An elementary study of poultice.

Ointments are soft semisolid preparations meant
for external application to the skin or mucous
membrane.
b
They usually contains medicament which is either

dissolved or suspended in the base.
They have emollient and protective action.
Creams are semisolid emulsions and are generally

of softer consistency and lighter than ointments.
They are less greasy and are easy to apply.

Pastes are semisolid preparations for external application
that differ from similar products in containing a high
proportion of finely powdered medicaments.
They are stiffer and are usually employed for their protective
action and for their ability to absorb serous discharges from
skin lesions.
Thus when protective,

protective rather than therapeutic action is
desired, the formulation pharmacists will favour a paste, but
when therapeutic action is required, he will prefer ointments
and creams.
Jellies are transparent or translucent, non-greasy, semisolid

preparation mainly used externally.The
externally The gelling agent may be
gelatin, starch, tragacanth, sodium alginate or cellulose
derivative (e.g. carboxy methyl6/27/2012
cellulose).
bibekmahatsingh@gmail.com 4
OINTMENT
y Definition:
y Ointments are semisolid preparations for

application to the skin or mucosae.
y The ointment bases are almost always

anhydrous and generally contains one or more
medicaments in suspension or solution.
OINTMENT
Characteristics of an ideal ointment:
1. It should be chemically and physically stable.
2. It should be smooth and free from grittiness.
3 It should melt or soften at body temperature
3.
and be easily applied.
4. The
Th base
b should
h ld bbe non-irritant
i i and
d should
h ld
have no therapeutic action.
5. The medicament should be finely divided and
uniformly distributed throughout the base.
Classification of ointments
According to their therapeutic properties
based on p penetration of skin.
Ointments classified according to their
therapeutic properties based on penetration
are as follows:
(a) Epidermic,
(b) Endodermic,
E d d i
(c) Diadermic
(a) Epidermic ointments
y These ointments are intended to produce

their action on the surface of the skin and
produce local effect.
y They are not absorbed.
y Theyy acts as pprotectives, antiseptics

p and
parasiticides.
(b) Endodermic ointments
y These ointments are intended to release the
medicaments that penetrate into the skin.
y They are partially absorbed and acts as
emollients, stimulants and local irritants.
(c) Diadermic ointments

y These ointments are intended to release the
medicaments that pass through the skin and
produce systemic effects.
According to therapeutic uses the ointments are classified as follows:
y (i) Acne treatment :resorcinol, sulfur.
y (ii) Antibiotics :Used to kill microorganisms.

y e.g. bacitracin, chlortetracycline, neomycin.
y (iii) Antieczematous :Used to stop oozing and exudation from

vesicles on the skin.
y e.g. hydrocortisone, coal tar, ichthamol, salicylic acid.
y (iv) Antifungal :Used to inhibit or kill the fungi.

y e g benzoic acid
e.g. acid, salicylic aid
aid, nystatin,
nystatin clotrimazole,
clotrimazole etc.
etc
y (v) Anti-inflammatory :Used to relieve inflammatory, allergic and

pruritic conditions of the skin
y e.g. betamethasone valerate, hydrocortisone, triamcinolone
acetonide
y (vi) Antipruritic :Used to relieve itching.
y e.g.
g benzocaine,, coal tar.
y (vii) Antiseptic :Used to stop sepsis.

y e.g. ammoniated mercury, zinc oxide.
y (vii) Astringent :Reduces the secretion of glands or discharge from

skin surface.
y e.g. calamine, zinc oxide, aluminium acetate and subacetate, acetic
acid and tannic acid.
y (ix) Counter irritant These are applied locally to irritate the intact
skin, thus reducing or relieving another irritation or deep seated
pain. e.g. capsicum oleoresin, iodine (Iodex), methyl salicylate.
y (x) Dandruff treatment :e.g. salicylic acid and cetrimide (cetyl

trimethyl ammonium bromide) 6/27/2012 bibekmahatsingh@gmail.com 11
y (xi) Emollient :Used to soften the skin (for example in the dry season).
y e.g. soft paraffin
y (xii) Keratolytic Used to remove or soften the horny layer of the skin.
y e.g. resorcinol, salicylic acid and sulfur.
y (xi) Keratoplastic :Tends to increase the thickness of horny layer e.g. coal
tar.
y (xii) Parasiticide :These ointments destroy or inhibit living infestations such

as lice and ticks.
y e.g. benzyl benzoate, gamma
gamma-benzene
benzene hexachloride (GBH), sulfur etc.
y (xiii) Protective :Protects the skin from moisture, air, sun rays or other
substances such as soaps or chemicals.
y e.g. silicones, titanium dioxide, calamine, zinc oxide, petrolatum.
OINTMENT BASES
y The ointment base is that substance or part of an ointment
preparation which serves as carrier or vehicle for the
medicament.
medicament
y An ideal ointment base should be inert, stable, smooth,

compatible with the skin, non-irritating and should release the
incorporated medicaments readily.
Classification of ointment bases:

y 1.
1 Oleaginous bases
y 2. Absorption bases
y 3. Water
Water-miscible
miscible bases
y 4. Water soluble bases
OINTMENT BASES
y OLEAGINOUS BASES
y These bases consists of oils and fats.

fats The most important are the
Hydrocarbons i.e. petrolatum, paraffins and mineral oils.
y The animal fat includes lard.
y The
Th combination
bi ti off ththese materials
t i l can produce d a productd t off
desired melting point and viscosity.
(a) Petrolatum (Soft paraffin)
y This is a purified mixture of semi-solid hydrocarbons obtained from
petroleum or heavy lubricating oil.
y Yellow soft paraffin (Petrolatum; Petroleum jelly)
y This a purified mixture of semisolid hydrocarbons obtained from
petroleum.
y It may contain suitable stabilizers like, antioxidants e.g. a a-tocopherol
tocopherol
(Vitamin E), butylated hydroxy toluene (BHT) etc.
y Melting range : 38 to 56C.
OINTMENT BASES
y OLEAGINOUS BASES
White soft paraffin (White petroleum jelly, White petrolatum)
y This a purified
Thi ifi d mixture
i off semisolid
i lid hydrocarbons
h d b obtained
b i d
from petroleum, and wholly or partially decolorized by
ppercolatingg the yellow
y soft paraffin
p through
g freshlyy burned
bone black or adsorptive clays.
y Melting range : 38 to 56C

y Use: The white form is used when the medicament is
colourless white or a pastel shade.
colourless, shade
y This base is widely used in
1. Dithranol ointment B.P.
2. Ammoniated Mercury and Coal tar ointment B.P.
3. Zinc ointment B.P. 6/27/2012 bibekmahatsingh@gmail.com 15
OINTMENT BASES
y OLEAGINOUS BASES
y (b) Hard paraffin (Paraffin)
y This is a mixture of solid hydrocarbons obtained

from petroleum.
y It is colourless or white, odorless, translucent, wax-
like substance.
y It solidifies between 50 and 57C and is used to
stiffen ointment bases.
OINTMENT BASES
(c) Liquid paraffin (Liquid petrolatum,; White mineral
oil)
y It is a mixture of liquid , hydrocarbons obtained from petroleum. It

is transparent, colourless, odourless, viscous liquid.
y On long storage it may oxidize to produce peroxides and therefore,
it may contain tocopherol or BHT as antioxidants.
y It is used along with hard paraffin and soft paraffin to get a desired
consistency of the ointment.
y Tubes for eye, rectal and nasal ointments have nozzles with narrow
orifices
ifi through
h h which
hi h iit iis diffi
difficult
l to expell very viscous
i ointments
i
without the risk of bursting the tube.
y To facilitate the extrusion up-to p 25% of the base mayy be replacedp byy
liquid paraffins.
OINTMENT BASES
Advantages of hydrocarbons bases:
1. They are not absorbed by the skin.
2. They remain on the surface as an occlusive layer that
restricts the loss of moisture hence, keeps the skin soft.
3 They are sticky hence ensures prolonged contact between
3.
skin and medicament.
4. They are almost inert. They consist largely of saturated
hydrocarbons, therefore, very few incompatibilities and little
tendency of rancidity are there.
5 They can withstand heat sterilization
5. sterilization, hence
hence, sterile
ophthalmic ointments can be prepared with it.
6. Theyy are readilyy available and cheap.p
OINTMENT BASES
Disadvantages of hydrocarbon bases;
1. It may lead to water logging followed by maceration of the
skin
ki if applied
li d ffor a prolonged
l d period.
i d
2. It retains body heat, which may produce an uncomfortable
feeling of warmth.
3. They are immiscible with water; as a result rubbing onto the
surface and removal after treatment both are difficult.
4. they are sticky, hence makes application unpleasant and leads
to contamination of clothes.
5 Water absorption capacity is very low,
5. low hence,
hence these bases are
poor in absorbing exudates from moist wounds.
OINTMENT BASES
ABSORPTION BASE
y The term absorption base is used to denote the water
absorbing
b bi or emulsifying
l if i property off these
h bases
b and
d not to
describe their action on the skin.
y These bases (some times called emulsifiable ointment bases)

are generally anhydrous substances which have the property of
absorbing
b b ((emulsifying)
l f ) considerable
d bl quantity off water yet
retaining its ointment-like consistency.
y Preparations of this type do not contain water as a

component of their basic formula but if water is incorporated
a W/O emulsion results.
OINTMENT BASES
ABSORPTION BASE
Wool Fat (anhydrous lanolin)
y It is the purified anhydrous fat like substance obtained from
the wool of sheep.
y It
It is practically insoluble in water but can absorb water upto
50% of its own weight.
y Therefore it is used in ointments the proportion of water or
aqueous liquids to be incorporated in hydrocarbon base is too
large.
y Due to its sticky nature it is not used alone but is used along
with other bases in the preparation of a number of ointments.
y e.g.
g Simple
p ointment B.P. contains 5% and the B.P. eyey ointment
base contains 10% woolfat.
OINTMENT BASES
y Hydrous Wool Fat (Lanolin)
y It is a mixture of 70 % w/w wool fat and 30 % w/w purified water. It
is a w/o emulsion. Aqueous liquids can be emulsified with it.
y It is used alone as an emollient.
y Example:- Hydrous Wool Fat Ointment B.P.C., Calamine Coal Tar
Ointment.
y Wool Alcohol
y It is the emulsifying fraction of wool fat.
y Wool alcohol is obtained from wool fat by treating it with alkali and
separating the fraction
f containing cholesterol and other alcohols.
y It contains not less than 30% of cholesterol.
y Use:-
y It is used as an emulsifying agent for the preparation of w/o
emulsions and is used to absorb water in ointment bases.
y It is also used to improve the texture, stability and emollient
properties
ti off o/w
/ emulsions.
li
y Examples :- Wool alcohol ointment B.P. contains 6% wool
alcohol and hard, liquid and soft paraffin.
OINTMENT BASES
Beeswax
y It is purified wax, obtained from honey comb of bees.
y It contains small amount of cholesterol.
y It is of two types: (a) yellow beeswax and (b) white beeswax.
Use:-
y Beeswax is used as a stiffening agent in ointment preparations.
y Examples:-Paraffin ointment B.P.C. contains beeswax.
Cholesterol
y It is widely distributed in animal organisms.
organisms
y Wool fat is also used as a source of cholesterol.
y Use:- It is used to increase the water absorbing power of an
ointment base.
base
y Example:- Hydrophilic petroleum U.S.P. contains:
y Cholesterol 3%
y Stearyl alcohol 3%
y White beeswax 8%
y White soft paraffin 86% 6/27/2012 bibekmahatsingh@gmail.com 23
OINTMENT BASES
Advantages of absorption bases:
1. They are less occlusive nevertheless, are good emollient.
2. They assist oil soluble medicaments to penetrate the skin.
3. They are easier to spread.
4 They
4. Th are compatible tibl with
ith majority
j it off th
the medicaments.
di t
5. They are relatively heat stable.
6 The base may be used in their anhydrous form or in
6.
emulsified form.
7. They can absorb a large quantity of water or aqueous
substances.
Disadvantages: Inspite of their hydrophilic nature, absorption
bases are difficult to wash.
wash
OINTMENT BASES
WATER MISCIBLE BASES
y They are miscible with an excess of water.
y Ointments
Oi made
d ffrom water-miscible
i ibl bbases are easilyil removed
d after
f
use.
y There are three official anhydrous
y water-miscible ointment bases:-
y Example:-
1. Emulsifying ointment B.P. - contains anionic emulsifier.
2. Cetrimide
C emulsifying
f ointment B.P. - contains cationic emulsifier
f
3. Cetomacrogol emulsifying ointment B.P. - contains non-ionic
emulsifier
y Uses: they are used to prepare o/w creams and are easily removable
ointment bases
y e.g. C
Compound dB
Benzoic i A
Acid
id Ointment
Oi t t (Whitfields
(Whitfi ld Ointment)
Oi t t) -
used as antifungal ointment.
OINTMENT BASES
WATER MISCIBLE BASES
y Advantages of water miscible bases:

1. Readily miscible with the exudates from lesions.
2
2. R d d interference
Reduced i t f with
ith normall skin
ki ffunction.
ti
3. Good contact with the skin, because of their surfactant
content.
4. High cosmetic acceptability, hence there is less likelihood of
the patients discontinuing treatment.
5. Easy removal from the hair.
OINTMENT BASES
y WATER SOLUBLE BASES
y Water soluble bases contain only the water soluble

ingredients and not the fats or other greasy substances, hence,
they are known as grease
grease-less
less bases.
y Water soluble bases consists of water soluble ingredients such

as polyethylene glycol polymers (PEG) which are popularly
known as carbowaxes and commercially known as
macrogols.
macrogols .
y Theyy are a range

g of compounds
p with the general
g formula:
CH2OH . (CH2OCH2) n CH2OH
OINTMENT BASES
y WATER SOLUBLE BASES
y The PEG
Th PEGs are mixtures
i t off polycondensation
l d ti products
d t off
ethylene and water and they are described by numbers
representing their average molecular weights.
y Like the paraffin hydrocarbons they vary in consistency from
viscous liquids to waxy solids.
y Example:-
p
1. Macrogols 200, 300, 400 - viscous liquids

2. Macrogols 1500 - greasy semi-solids
3. Macrogols 1540, 3000, 4000, 6000 - waxy solids.
y Different PEGs are mixed to get an ointment of desired

consistency. 6/27/2012 bibekmahatsingh@gmail.com 28
OINTMENT BASES
Advantages of PEGs as ointment base:
1. They are water soluble; hence, very easily can be removed

from the skin and readily miscible with tissue exudates.
2
2. Helps in good absorption by the skin.skin
3. Good solvent properties. Some water-soluble dermatological
drugs, such as salicylic acid, sulfonamides, sulfur etc. are
soluble in this bases.
4. Non-greasy.
5. Th do
They d not hydrolyze,
h d l rancidify
idif or support microbial
i bi l
growth.
6. Compatibility with many dermatological medicaments.
OINTMENT BASES
Disdvantages of PEGs as ointment base:
1. Limited uptake of water. Macrogols dissolve when the

proportion of water reaches about 5%.
2
2. Reduction in activity of certain antibacterial agents,
agents ee.g.g
phenols, hydroxybenzoates and quaternary compounds.
3. Solvent action on polyethylene and bakelite containers and
closures.
4. Certain other substances which are used as water soluble
ointment bases include tragacanth,
tragacanth gelatin
gelatin, pectin
pectin, silica gel
gel,
sodium alginate, cellulose derivatives, etc.
OINTMENT BASES
FACTORS GOVERNING SELECTION OF
AN IDEAL OINTMENT BASE
1. DERMATOLOGICAL FACTORS
2. PHARMACEUTICAL FACTORS
Factors Governing Selection (Ideal Ointment Base)
D
Dermatological
l i l factors
f
y (a) Absorption and Penetration:

y P
Penetration
i means passage off theh drug
d across the
h skin
ki i.e.
i cutaneous
penetration, and absorption means passage of the drug into blood
stream.
y Medicaments which are both soluble in oil and water are most readilyy
absorbed though the skin.
y Whereas animal and vegetable fats and oils normally penetrate the skin.
y Animals fats, e.g. lard and wool fat when combined with water, penetrates
th skin.
the ki
y o/w emulsion bases release the medicament more readily than greasy
bases or w/o emulsion bases.
y (b) Effect on the skin

y Greasy bases interfere with normal skin functions i.e. heat radiation and
sweating. They are irritant to the skin.
y o/w emulsion bases and other water miscible bases produce a cooling
effect due to the evaporation of water.
Dermatological factors
y ( ) Mi
(c) Miscibility
ibilit with
ith skin
ki secretion
ti and
d serum
y Skin secretions are more readily miscible with emulsion bases than with
greasy bases. Due to this the drug is more rapidly and completely
released
l d to the
h skin.
ki
y (d) Compatibility with skin secretions:

y The bases used should be compatible with skin secretions and should
have pH about 5.5 because the average skin pH is around 5.5. Generally
neutral ointment bases are preferred.
y (e) Non-irritant
y All bases should be highly pure and bases specially for eye ointments
should be non-irritant and free from foreign particle.
Dermatological factors
y (f) Emollient properties

y Dryness and brittleness of the skin causes discomfort to the skin
therefore, the bases should keep the skin moist. For this purpose water
and humectants such as glycerin, propylene glycol are used. Ointments
should prevent rapid loss of moisture from the skin.
y (g) Ease of application and removal

y The ointment bases should be easily applicable as well as easily removable
from the skin by simple washing with water. Stiff and sticky ointment
b
bases require
i muchh force
f to
t spread
d on the
th skin
ki and d during
d i rubbing
bbi newlyl
formed tissues on the skin may be damaged.
Pharmaceutical factors
y (a) Stability
y Fats and oils obtained from animal and p plant sources are prone
p to
oxidation unless they are suitably preserved. Due to oxidation
odour comes out. This type of reactions are called rancidification.
Lard, from animal origin, rancidify rapidly. Soft paraffin, simple
ointment and paraffin ointment are inert and stable. Liquid paraffin
is also stable but after prolonged storage it gets oxidized.
Therefore, an antioxidant like tocopherol (Vit -E) may be
i
incorporated.
t d Other
Oth antioxidants
ti id t those
th may be
b used d are butylated
b t l t d
hydroxy toluene (BHT) or butylated hydroxy hydroxy anisole
(BHA).
y (b) Solvent properties

y Most of the medicaments used in the preparation of ointments are
insoluble in the ointment bases therefore, they are finely powdered
and are distributed uniformly throughout the base.
Ph
Pharmaceutical
i l factors
f
y (c) Emulsifying properties

y Hydrocarbon bases absorbs very small amount of water.
y Wool fat can take about 50% of water and when mixed with other
fats can take up several times its own weight of aqueous solution.
y Emulsifying ointment, cetrimide emulsifying ointment and
cetomacrogol emulsifying ointment are capable of absorbing
considerable amount of water, forming w/o creams.
y (d) Consistency
y The ointments produced should be of suitable consistency. They
should neither be hard nor too soft.
soft They should withstand
climatic conditions. Thus in summer they should not become too
soft and in winter not too hard to be difficult to remove from the
container and spread on the skin.
y The consistency of an ointment base can be controlled by varying
the ratio of hard and liquid paraffin.
End Of
Part 1
Ointment Base
Part 2
Preparation Of Ointments
PREPARATION OF OINTMENTS
A well-made ointment is :-
a. Uniform throughout i.e. it contains no lumps of separated

high melting point ingredients of the base, there is no
tendency for liquid constituents to separate and insoluble
powders are evenly dispersed.
b. Free from grittiness, i.e. insoluble powders are finely

subdivided and large lumps of particles are absent. Methods
of preparation must satisfy this criteria.
PREPARATION OF OINTMENTS
Two mixing techniques are frequently used in making

ointments:
1. Fusion, in which ingredients are melted together and stirred

to ensure homogeneity.
2. Trituration, in which finely-subdivided insoluble

medicaments are evenly distributed by grinding with a small
amount of the base or one of its ingredients followed by
dilution with gradually increasing amounts of the base.
1. Ointments prepared by Fusion method:-
method:-
y When an ointment base contains a number of solid
ingredients such as white beeswax, cetyl alcohol, stearyl
alcohol, stearic acid, hard paraffin, etc. as components of the
base, it is required to melted them. The melting can be done
in two methods:
Method I
Method-I
y The components are melted in the decreasing order of their
melting point i.e. the higher m. p. substance should be melted
first the substances with next melting point and so on.
first, on
y The medicament is added slowly in the melted ingredients

and stirred thoroughly until the mass cools down and
homogeneous product is formed.
y This will avoid over-heating of substances having low melting

point. 6/27/2012 bibekmahatsingh@gmail.com 40
method:-
y Method-II
y All the components are taken in subdivided state and melted

together.
y The maximum temperature

p reached is lower than Method-I,,
and less time was taken possibly due to the solvent action of
the lower melting point substances on the rest of the
ingredients.
ingredients
method:-
Cautions:-
Melting time is shortened by grating waxy components (i.e.

beeswax, wool alcohols, hard-paraffin, higher fatty alcohols and
emulsifying waxes) by stirring during melting and by lowering the
dish as far as possible into the water bath so that the maximum
surface area is heated.
The surface of some ingredients discolors due to oxidation e.g.

eg
wool fats and wool alcohols and this discolored layers should be
removed before use.
After melting, the ingredients should be stirred until the ointment

is cool, taking care not to cause localized cooling, e.g. by using a
cold spatula or stirrer, placing the dish on a cold surface (e.g. a
plastic bench top) or transferring to a cold container before the
ointment has fully set. If these precautions are ignored, hard
lumps may separate.
method:-
Cautions:-
Vigorous-stirring, after the ointment has begun to thicken, causes

excessive aeration and should be avoided.
Because of their greasy nature, many constituents of ointment

bases pickup dirt during storage, which can be seen after melting.
This is removed from the melt by allowing it to sediment and
decanting the supernatant, or by passage through muslin
supported by a warm strainer. In both instances the clarified
liquid
qu iss co
collected
ecte in another
a ot e hot
ot basin.
bas .
If the product is granular after cooling, due to separation of high

m p constituents,
m.p. constituents it should be re
re-melted,
melted using the minimum of
heat, and again stirred and cooled.
method:-
Example:
(i) . Simple ointment B.P. contains
1
1. Wool fat 50g
2. Hard paraffin 50g
3. Cetostearyl alcohol 50g
4. White soft paraffin 850g
y Type of preparation: Absorption ointment base
Procedure:
y Hard p paraffin and cetostearyl
y alcohol on water-bath.
y Wool fat and white soft paraffin are mixed and stirred until
all the ingredients are melted.
y If required decanted or strained and stirred until cold and
packed in suitable container.
method:-
(ii) Paraffin ointment base
y Type of preparation : Hydrocarbon ointment base
(iii) WWooll alcohols
l h l ointment
i t t B.P.
BP
y Type of preparation: Absorption base
(iv) Emulsifying ointment B.P. BP
y Type of preparation: Water-miscible ointment base.
((v)) Macrogol
g ointment B.P.C
y Type of preparation: Water soluble ointment base
y Formula: Macrogol 4000
y Liquid Macrogol 300
y Method: Macrogol 4000 is melted and previously warmed
li id macrogoll 300 is
liquid i added.
dd d
y Stirred until cool.
2. OINTMENT PREPARED BY TRITURATION
y This method is applicable in the base or a liquid present in
small amount.
1. Solids are finelyy ppowdered are ppassed through
g a sieve (# (
250, # 180, #125).
2. The powder is taken on an ointment-slab and triturated
with a small amount of the base.
base
3. A steel spatula with long, broad blade is used.
4. To this additional quantities of the base are incorporated
and triturated until the medicament is mixed with the base.
5. Finally liquid ingredients are incorporated.
6
6. To avoid loss from splashing
splashing, a small volume of liquid is
poured into a depression in the ointment an thoroughly
incorporated before more is added in the same way.
7
7. S l hi iis more easily
Splashing il controlled
t ll d iin a mortar
t ththan on a
tile.
2. OINTMENT PREPARED BY TRITURATION
y Example:
(i) Whitfield ointment
((Compound
p benzoic acid ointment B.P.C.))
1. Formula: Benzoic acid, in fine powder 6gm

2. Salicylic acid, in fine powder 3gm
3. Emulsifying ointment 91gm
y Method:
1. Benzoic acid and salicylic acid are sieved through No. 180
sieves.
2. They are mixed on the tile with small amount of base and
levigated
g until smooth and dilute ggradually.
y
(ii) Salicylic acid sulphur ointment B.P.C.

3. OINTMENT PREPARATION BY CHEMICAL REACTION
y Chemical reactions were involved in the preparation of
several famous ointments of the past, e.g. Strong Mercuric
Nitrate Ointment, both of the 1959 B.P.C.
((a)) Ointment containing g free iodine

y Iodine is only slightly soluble in most fats and oils but readily
soluble.
y Iodine
I d is readily
d l soluble
l bl in concentrated d solution
l off
potassium iodide due to the formation of molecular
p
complexes KI.I2, KI.2I2, KI.3I2 etc.
y These solutions may be incorporated in absorption-type
ointment bases.
y e.g. Strong Iodine Ointment B.Vet.C
y Strong Iodine Ointment B. Vet. C

((British Veterinaryy Pharmacopoeia)
p ) is used to treat ringworm
g
in cattle. It contains free iodine.
y At one time
ti thi
this ttype off ointments
i t t were used
d as counter-
t
irritants in the treatment of human rheumatic diseases but
they were not popular because:-
y (i) They stain the skin a deep red color.
y (ii) Due to improper storage the water dries up and the

iodine crystals irritate the skin, hence glycerol was some
ti
times to
t di
dissolve
l the
th iiodine-potassium
di t i iiodide
did complex
l
instead of water.
y Example: Strong Iodine Ointment B.Vet. C.
1. Iodine
2
2. Wool fat
Wool-fat
3. Yellow soft paraffin
4. Potassium iodide
5. Water
Strong Iodine Ointment B.Vet. C.
y Procedure:
P d
y (i) KI is dissolved in water. I2 is dissolved in it.
y (ii) Wool-fat
Wool fat and yellow soft paraffin are melted together
over water bath. Melted mass is cooled to about 40C.
y (iii) I2 solution is added to the melted mass in small quantities
at a time with continuos stirring until a uniform mass is
obtained.
y (iv) It is cooled to room temperature and packed.
packed
y Use: - Ringworm in cattle.
(b) Ointment containing combined iodine
y Fixed
Fi d oils
il and
d many vegetable
bl and
d animal
i l ffats absorb
b b iiodine
di
which combines with the double bonds of the unsaturated
constituents, e.g.
g
y CH3.(CH2) 2.CH = CH.(CH2) 7.COOH + I2 CH3.(CH2)
2.CHI CHI.(CH2) 7.COOH
y Oleic acid di-iodostearic acid
y Example: Non-staining Iodine Ointment B.P.C. 1968 Iodine

y Arachis Oil
y Yellow Soft Paraffin
y Method:
1. Iodine is finely powdered in a glass mortar and required amount
is added to the oil in a glass
glass-stoppered
stoppered conical flask and stirred
well.
2. The oil is heated at 50C in a water-bath and stirred continually.
Heating is continued until the brown color is changed to
greenish-black; this may take several hours.
3. From 0.1g of the preparation the amount of iodine is determined
by B.P.C. method and the amount of soft paraffin base is
calculated to give the product the required strength.
4. Soft pparaffin is warmed to 40C. The iodized oil is added and
mixed well. No more heat is applied because this causes
deposition of a resinous substance.
5
5. The preparation is packed in a warm,
warm wide-mouthed,
wide mouthed amber color color,
glass bottle. It is allowed to cool without further stirring.
4. PREPARATION OF OINTMENTS BY EMULSIFICATION
y An emulsion
A l system contain an oill phase,
h an aqueous phase h and
d an
emulsifying agent.
y For o/w emulsion systems the following emulsifying agents are
used:
1. water soluble soap
2. cetyl alcohol
3
3. glyceryl
l l monostearate
t t
4. combination of emulsifiers: triethanolamine stearate + cetyl
alcohol
5
5. non ionic emulsifiers: glyceryl monostearate,
non-ionic monostearate glyceryl monooelate, monooelate
propylene glycol stearate
y For w/o emulsion creams the following emulsifiers are used:
1
1. polyvalent ions e.g
e g magnesium,
magnesium calcium and aluminium are used. used
2. combination of emulsifiers: beeswax + divalent calcium ion
y The viscosity of this type of creams prevent coalescence of the
emulsified phases and helps in stabilizing the emulsion.
emulsion
y Example:
y Cold cream: 6/27/2012 bibekmahatsingh@gmail.com 54
4. PREPARATION OF OINTMENTS BY EMULSIFICATION
y Cold cream:
y Procedure:
1. Water immiscible components e.g. oils, fats, waxes are

melted together over water bath (70C).
2. Aqueous solution of all heat stable, water soluble
components are heated (70C).
3. Aqueous solution is slowly added to the melted bases with
continuous stirring until the product cools down and a
semi-solid
semi solid mass is obtained.
1. N.B. The aqueous

q pphase is heated otherwise high
g meltingg
point fats and waxes will immediately solidify on addition of
cold aqueous solution.
End Of
Part 2
Preparation Of Ointments
Part 3
Stability Of Ointments
STABILITY OF OINTMENTS
y The ointments should remain stable from the time of
preparation to the time when the whole of it is consumed by
the user.
y ( ) To stop
(i) p microbial ggrowth ppreservatives are added.
Preservatives for ointment includes : p-hydroxy benzoates,
phenol, benzoic acid, sorbic acid, methyl paraben, propyl
paraben quaternary ammonium compounds,
paraben, compounds mercury
compounds etc.
y (ii) The preservatives should not react with any of the

component of the formulation. Plastic containers may absorb
the preservative and thereby decreasing the concentration of
preservative available for killing the bacteria.
STABILITY OF OINTMENTS
y (iii) Some ingredients like wool fat and wool alcohols are
susceptible to oxidation. Therefore, a suitable antioxidant may
be incorporated to protect the active ingredients from
oxidation.
y (iv) Incompatible drugs, emulsifying agents and preservatives
must be avoided. The drugs which are likely to hydrolyze
must be dispensed in an anhydrous base.
y (v) Humectants such as,
as glycerin
glycerin, propylene glycol and
sorbitol may be added to prevent the loss of moisture from
the preparation.
y (vi) Ointment must be stored at an optimum temperature
otherwise separation of phases may take place in the
emulsified pproducts which mayy be veryy difficult to remix to
get a uniform product.
PASTE
Syllabus:
y Differences between ointments and pastes.
pastes
y Bases of pastes
y Preparation
p of ppaste and their ppreservation.
PASTE
y Differences between pastes and ointments;
y Pastes generally
P ll contains
i a llarge amount (50%) off fifinely
l
powdered solids. So they are often stiffer than ointments.
y When applied to the skin pastes adhere well, forming a thick

coating protects and soothes inflamed and raw surfaces and
minimizes the
h d damage ddone by
b scratching
h in itchyh conditions
d
such as chronic eczema.
y it is comparatively easy to confine pastes to the diseased
areas whereas ointments, which are usually less viscous, tend
to spread on to healthy skin, and this may result in sensitivity
reactions
ti if th
the preparations
ti contain
t i a powerful
f l medicament
di t
such as dithranol.
PASTE
y Differences between pastes and ointments;
y Because off the

B h powder
d contents pastes are porous; hence,
h
perspiration can escape. Since the powders absorbs exudate,
ppastes with hydrocarbon
y base are less maceratingg than
ointments with a similar base.
y They are lless greasy than

Th h ointments bbut since their
h efficacy
ff
depends on maintaining a thick surface layer they are far from
y
attractive cosmetically.
y Most of the pastes are unsuitable for treating scalp

conditions because they are difficult to remove from the hair.
JELLIES
y Definition: Jellies are transparent or translucent, non-greasy,
semisolid preparation generally applied externally. They are
used for medication, lubrication and some miscellaneous
applications.
y Types of jellies:
1 Medicated jellies
1.
y (i) Water soluble drugs like local anaesthetics, spermicides
and antiseptics are suitable for incorporation in the jellies.
y (ii) They are easy to apply and evaporation of the water
content produces a pleasant cooling effect. The medicinal film
usually adheres well and gives protection but is easily
removed by washing when the treatment is complete.
y e.g. ephedrine sulfate jelly - used to arrest bleeding from nose.
y pramoxine HCl , a local anaesthetic - relieves discomfort of pruritis
and haemorrhoids.
y phenylmercuric nitrate - as spermicidal contraceptive
JELLIES
2. Lubricant jelly
y Catheters,
C h i
items off eletrodiagnostic
l di i equipment,
i such
h as
cystoscopes, and rubber gloves or finger stalls used for rectal
and other examinations require
q lubrication before use.
y The lubricants must be sterile for articles inserted into

sterile
l regions off the
h bbody,
d suchh as urinary bl
bladder.
dd
y For painful investigations a local anaesthetic may be included

as in Lignocaine Gel B.P.C.
JELLIES
The following are more specialized jellies -
y (a) Patch testing
y Here the jjelly
y is the vehicle for allergens
g applied
pp to the skin to
detect sensitivity.
y Several allergens may be applied on one person.

person
y The viscosity of the jelly and it leaves on drying help to keep the
particles
ti l separate.
t
y (b) Electrocardiography
y to reduce electrical resistance between the patients skin and
electrodes of the cardiograph, an electrode jelly may be applied.
This contains NaCl to provide good conductivity and often pumice
powder which, when applied onto the skin, removes part of the
horny layer of the epidermis, the main layer of electrical resistance.
JELLIES
The following are more specialized jellies
y (b) Electrocardiography
El t di h
y To reduce electrical resistance between the patients skin and

electrodes of the cardiograph, an electrode jelly may be
applied.
y This contains NaCl to provide good conductivity and often

pumice powder which,
which when applied onto the skin
skin, removes
part of the horny layer of the epidermis, the main layer of
electrical resistance.
JELLIES
y FORMULATION
y Pharmaceutical jellies are usually prepared by adding a
thickening agent such as tragacanth or carboxy
methylcellulose (CMC) to an aqueous solution in which drug
has been dissolved.
y The mass is triturated in a mortar until a uniform product is

obtained.
obtained
y For the preparation of jellies whole gum is preferred rather

than powdered gum because the former gives a clear
preparation of uniform consistency.
JELLIES
The ffollowing
Th ll gelling
ll agents are used d ffor the
h preparation off jellies.
ll
y (i) Tragacanth
y the main hydrophilic component of tragacanth that gels in water
h been
has b named d bassorin
b i - hence,
h tragacanthh jellies
j lli are sometimes
i
called bassorin paste.
y The amount of gum required for a preparation varies with its use:
a)) For
F lubricating
l b i ti jjelly ll 2 tto 3%
3%.
b) For dermatological vehicles about 5%.
c) For incorporation of ichthamol, resorcinol, salicylic acid and
other medicaments
medicaments, about 5% is generally used used. All formulations
contain alcohol and/or glycerol and/or a volatile oil to disperse
the gum and prevent lumpiness when water is added.
d) They vary in viscosity, due to the natural origin of the gum and
variations in milling and storage.
e) The film left on the skin tends to flake.
f)) Viscosity y is rapidly
p y lost outside the ppH range g of 4.5 to 7.0;; for
example if benzoic acid is used as the preservative.
g) They are susceptible to microbial growth.
JELLIES
The following gelling agents are used for the preparation of
jellies.
2. Sodium alginate
y Uses:
Uses:- As lubricant - 1.5 to 2 % is used.
y As dermatological vehicle - 5 to 10 % is used.
y A trace of Ca - salt (CaCl2) may be added to increase the
viscosity and most formulations contain glycerol as a
dispersing agent.
y Advantage: Sodium alginate has an advantage over tragacanth
that is available in several grade or standardized viscosity.
JELLIES
The following gelling agents are used for the preparation of
jellies.
3 Pectin
3.
y Pectin is a very good gelling agent and is used in the
ppreparation
p of manyy types
yp of jjellies includingg edible jjellies.
y Glycerin is used as a dispersing agent and humectant in
dermatological jellies.
y Jellies
J ll must bbe packed
k d in well-closed
ll l d containers because
b they
h
lose water rapidly by evaporation and this lose water rapidly
byy evaporation
p and this is increased byy the susceptibility
p y of
pectin gels to syneresis (i.e. exudation of the aqueous phase
as a result of contraction of the gel).
JELLIES
The following gelling agents are used for the preparation of jellies.
4. Starch
y Starch in combination with gelatin and glycerin is commonly used
for preparations of jellies.
y Glycerin in 50% may act as preservative.
y Medicaments are incorporated in the cold jelly by trituration.
5. Gelatin
y Insoluble in cold water but swell and softens in it.
it It is soluble in
hot water.
y Hot solution contain 2% gelatin forms a jelly on cooling.
y Very stiff (15%) jellies are melted before used and after cooling to
desired temperature are applied with a brush to the affected area.
y The area is covered with bandage and the dressing may be left in
place for several weeks.
JELLIES
6. Cellulose derivative
y Methyl cellulose and sodium carboxy methyl cellulose
y 1.
1 produce neutral jellies of stable viscosity.
viscosity
y 2. Have good resistance against microbial growth.
y 3. Clear due to freedom from insoluble impurities.
y 4. Produce strong film after drying on the skin.
y Use: Sodium carboxy methyl cellulose can be used to
prepare lubricating jellies and sterile jellies.
jellies
y e.g. lignocine gel - because it can withstand autoclaving
temperature.
y N.B. Other cellulose derivatives are
Hydroxy propyl methyl cellulose (Hypermellose)
Carbomer
Polyvinyl alcohols.
JELLIES
7. Clays
y Gels
G l containing
i i 7 to 20 % off bentonite
b i can be
b used
d as
dermatological bases.
y Disadvantages:
y 1. They are opalescent and lack attractiveness.
y 2. Their pH is about 9.0 i.e. not suitable for application on the
skin.
y 3R
3. Residue
id on the h skin
ki iis powdery
d andd rather
h silky.
ilk
POULTICE
y Definition: Poultice are paste-like preparations used
externally to reduce inflammation because they retain
heat well. After heating, the preparation is spread thickly
on a dressing and applied, as hot as the patient can bear
it, to the affected area.
y Uses;
y (i) Glycerol, because of its hygroscopic nature, is believed to
draw infected materials from the tissues when the poultice is
used for boils and similar infections.
infections
y (ii) Methyl salicylate (an antirheumatic drug),
thymol (a powerful bactericide),
boric acid (a weak antimicrobial agent),
and peppermint oil (which contributes to the smell) are
used for different purposes.
purposes
POULTICE
y M h d off applying
Method l the
h poultice:-
l
1. For use, the poultice is heated, with occasional stirring, until it can only be
tolerated on the back of the hand.
2. Then it is spread thickly on lint or other dressing and applied to the
affected area which is sometimes first covered with muslin to facilitate
removal after use.
3
3. A thick
thi k llayer off cotton
tt wooll iis applied
li d tto retain
t i the
th hheatt and
d a covering
i off
oiled silk may be added to protect clothing.
y Example:p
y The only example given in the pharmacopoeia is Kaolin Poultice B.P.C.
Formula:
Heavy kaolin, finely sifted and dried at 100C 52.7 g
Boric acid, finely sifted 4.5 g
Methyl salicylate 0.2 ml
Thymol 50 mg
Peppermint oil 0.05 ml
Glycerin 42.5 g
SUPPOSITORY:
y It is a small solid medicated mass, usually cone-shaped ,that is

inserted either into the rectum ((rectal suppository),
pp y) vagina
g ((vaginal
g
suppository or pessaries) where it melts at body temperature .
SUPPOSITORY
Types of suppositories, Suppository bases,

classification, pproperties,
p preparation
p p and packaging
p g g
of suppositories.
Use of suppositories for drug absorption.
SUPPOSITORY
y Definition:
y SSuppositories
i i are specially
i ll shaped
h d solid
lid dosage
d form
f off
medicament for insertion into body cavities other than
mouth.
y They may be inserted into rectum, vagina or the urethra.
y This products are so formulated that after insertion, they will

either melt or dissolve in the cavity fluids to release the
medicament.
SUPPOSITORY
y Advantages of rectal suppositories:
1. Mechanical action: The rectal suppositories are extensively used
as a mechanical aid to bowel evacuation which produce its action
by either irritating the mucous membrane of the rectum (e.g.
glycerol and bisacodyl) or by lubricating action or by mechanical
lubrication.
2. Local action: The rectal suppositories may be used for soothing,
antiseptic, local anaesthetic action or for astringent effect.
Therefore, they may contain soothing e.g. zinc oxide, local
anaesthetic-
th ti e.g. cinchocaine,
i h i benzocaine,
b i astringents
ti t e.g. bi
bismuth
th
subgallate, hamamelis extract and tannic acid antiinflammatory
e.g. hydrocortisone and its acetate.
3
3. T provide
To id systemic
t i action:
ti SSuppositories
it i are convenienti t moded
of administration of drugs which irritate the gastrointestinal tract,
cause vomiting, are destroyed by the hepatic circulation, or are
destroyed in the stomach by pH changes
changes, enzymes etc
etc.
SUPPOSITORY
y Partial bypass: The lower portion of the rectum affords a large
absorption surface area from which the soluble substances can
absorb and reach the systemic circulation.
y e.g. aminophylline used in asthmatic and chronic bronchitis.
y morphine a powerful analgesic
y ergotamine
g tartarate used to treat migraine
g
y indomethacin and phenyl butazone analgesic and antiinflammatory
actions.
y Systemic treatment by the rectal route is of particular
value for
y (a) treating patients who are unconscious, mentally disturbed or
unable to tolerate oral medication because of vomiting or
pathological conditions of the alimentary tract.
y (b) administering drugs, such as aminophylline, that cause gastric
irritation and
irritation,
y (c) treating infants.
PESSARIES
y Pessaries are solid medicated preparations for introducing
into the vagina, where they melt or dissolve and exert a local
action.
y They are used mainly for vaginitis (inflammation of the
vagina) and leucorrhoea (unpleasant vaginal discharge).
Vaginitis may be caused by a variety of micro-organisms or
key old age. The medicaments in official pessaries are:
1
1. acetarsol an antiprotozoal agent
2. di-iodohydroxyquinoline for yeast and protoplast infections.
3. lactic acid often useful in leucorrhoea
4. nystatin for yeast infections
5. crystal violet for various microbial infections.
PESSARIES
y TYPES OF SUPPOSITORIES:
y 1. Rectal suppositories
y Th
These are meant for
f introduction
i d i into i the
h rectum for
f their
h i
systemic effect. They are tapered at one or both ends and
usuallyy weigh
g about 2 gm.g The rectal suppositories
pp meant for
children are smaller in size and weight is 1 gm.
y 2.Vaginal suppositories:
y Th are meant ffor introduction
They d into vagina.
y They are larger than rectal suppositories and vary in weight
from 3 to 6 gm or more.
y They may be conical, rod-shaped or wedge shaped.
y Theyy a re exclusivelyy used for their local action on vagina.
g
PESSARIES
y 3. Urethral Suppositories (or Urethral bougies)
y Th are meant ffor iintroduction
They d i into i the
h urethra.
h
y Their weight varies from 2 to 4 gm and length from 2 to 5
inch. Urethral suppositories are very rarely used.
y 4. Nasal suppositories (Nasal bougies)

y They are meant for introduction into nasal cavity.
y They are similar in shape to urethral bougies.
y Their weight is about 1 gm and length 9-10 cm.
y They are always prepared with glycero-gelatin base.
PESSARIES
y 5 Ear
5. E cones (aurinaria)
( i i )
y They are meant for information into the ear.

ear
y Generally theobroma oil is used as a base.
y Theyy are prepared
p p in an urethral bougies
g mould and cut
according to the required size.
PESSARIES
y Properties of an Ideal Suppositories Base
1. It should melt at body temperature or dissolve or disperse
in bodyy fluids.
2. It should release any medicament readily.
3. It should keep its shape when being handled.
4. It should be non-toxic and non-irritant to the mucous
membrane.
5. It should be stable on storage.
g
6. It should be compatible with any added medicament.
7. It should be stable if heated above its melting point.
8. It should be easily moulded and should not adhere to the
mould.
9. It should be easilyy mouldable byy ppouringg or cold
compression.
PESSARIES
1. Since it is not possible to get all the above mentioned
qualities in a single base, so a combination of bases is used
to get a product of required qualities.
2. A number of ppatent improved

p suppository
pp y bases are
available. Most of these are mixtures of fats, waxes and/or
esters in specific proportions according to the desired
qualities of the product to be obtained.
obtained
3. Glycerogelatin
y g and ppolyethylene
y y glycols
gy are beingg widelyy
used as suppository bases, though theobroma oil is
extensively used in extemporaneous preparations but it is
losing its importance because it is unstable to heat and has
undesirable physical properties.
PESSARIES
y Types of Suppository Bases
y 11. Fatty
F bases
b - these
h melt
l at body
b d temperature.
y 2. Water-soluble or water miscible bases - these dissolve or
disperse in rectal secretions.
y 3. Emulsifying bases
PESSARIES
y FATTY BASES
y Theobroma oil (Cocoa butter)
y I iis a yellowish-white
It ll i h hi solid lid with
i h a chocolate-like
h l lik odour.
d It
I is
i a
mixture of glyceryl esters of stearic, palmitic, oleic and other
fattyy acids. Its valuable characteristics include -
y Advantages:
y (a) A melting point range of 30 to 36 0C; hence it is solid at
normall room temperatures bbut melts l in the
h body.
b d
y (b) Ready liquefaction on warming and rapid setting on
cooling.
y (c) Miscibility with many ingredients.
y ((d)) Blandness i.e. does not pproduce irritation
PESSARIES
y FATTY BASES
y Disadvantages:
y (a) Polymorphism
y When melted and cooled it solidifies in different crystalline
forms, depending on the temperature of melting, rate of
cooling
li and d size
i off th
the mass.
y If melted at not more than 360C and slowly cooled it forms
stable beta crystals with normal melting point, but if over-
heated it may produce, on cooling, unstable gamma crystals,
which melt at about 150C, or a-crystals, melting at about
200C.
y These unstable forms eventually return to the stable
condition but this may take several days and meanwhile, the
suppositories may not set at room temperature or, if set by
cooling, may remelt in the warmth of the patients home.
PESSARIES
y (b) Adherence to mould
y Because theobroma oil doesnt 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.
y (c) Softening point too low for hot climates

y To raise the softening point, whit beeswax may be added to
theobroma oil suppositories
pp intended for use in tropical
p and
subtropical countries.
y (d) Melting point reduced by soluble ingredients

y 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.
use To restore the melting point,
point a
controlled amount of white beeswax may be added.
PESSARIES
y (e) Slow deterioration during storage
y This is due to oxidation of the unsaturated glycerides.
y (f) Poor water absorbing capacity

y This fault can be improved by the addition of emulsifying
agents.
y (g) Leakage from the body

y Sometimes melted base escapes from the rectum or vagina.
This is most troublesome with pessaries because of their
l
larger size,
i and d therefore,
th f these
th are rarely
l made
d with
ith
theobroma oil.
y (h) Relatively high cost

PESSARIES
y Synthetic fats
y As a substitute of theobroma oil a number of hydrogenated
oils,, e.g.
g hydrogenated
y g edible oil,, arachis oil,, coconut oil,, ppalm
kernel oil, stearic and a mixture of oleic and stearic acids are
recommended.
y N.B. Synthetic suppositories bases are by hydrogenation and

subsequent heat treatment of vegetable oils such as palm oil
and
d arachis
hi oil.
il
y The oils are ggenerallyy esters of unsaturated fattyy acids.

Hydrogenation saturates the unsaturated fatty acids and heat
treatment splits some of the triglycerides into fatty acids and
partial esters (mono
(mono- and di di-glycerides).
glycerides).
y
PESSARIES
y Advantages of these synthetic fats over theobroma oil:
y 1. Their solidifying points are unaffected by overheating.
y 2 They have good resistance to oxidation because their
2.
unsaturated fatty acids have been reduced.
y 3. Their emulsifying and water absorbing capacities are good.
[They usually contain a proportion of partial glycerides some
of which, e.g. glyceryl monostearate, are w/o emulsifying
agents and, therefore, their emulsifying and water absorbing
capacity are good.
y 4. No mould lubricant is required because they contract
significantly on cooling.
y 5. They produce colorless, odourless and elegant
suppositories.
suppositories
y
PESSARIES
y Disadvantages:
y 11. Th
They should
h ld not bbe cooled
l d iin refrigerator
fi bbecause they
h
become brittle if cooled quickly. Certain additives e.g. 0.05 %
ppolysorbate80,
y helpp to correct this fault.
y 2. They are more fluid than theobroma oil when melted and
at this
h stage sedimentation
d rate is greater. Thickeners
Th k suchh as
magnesium stearate , bentonite and colloidal silicon dioxide,
mayy be added to reduce this.
PESSARIES
y WATER SOLUBLE AND WATER MISCIBLE BASES
y Glycero-Gelatin base
y Thi iis a mixture
This i off glycerol
l l and
d water maded into
i a stiff
iff jelly
j ll
by adding gelatin.
y 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.
use
y The base being hydrophilic in nature, slowly dissolves in the
q
aqueous secretions and pprovide a slow continuous release of
medicament. Glycerogelatin base is well suited for
suppositories containing belladonna extract, boric acid,
chloral hydrate,
hydrate bromides,
bromides iodides,
iodides iodoform,
iodoform opium,
opium etc
etc.
PESSARIES
y WATER SOLUBLE AND WATER MISCIBLE BASES
y Glycero-Gelatin base
y 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
y (i) Type-A or Pharmagel-A which is made by acid hydrolysis

(has isoelectric point between 7 to 9 and on the acid side of
the range behaves as a cationic agent, being most effective at
pH 7 to 8. ) is used for acidic drugs.
y (ii) Type-B or Pharmagel-B which is prepared by alkaline

hydrolysis (having an isoelectric point between 4.7 to 5 and
on the alkaline side of the range behaves as an anionic agent,
agent
being most effective at pH 7 to 8 ) is used for alkaline drugs
PESSARIES
y Soap-Glycerin Suppositories
y In this case gelatin and curd soap or sodium stearate which
makes the glycerin sufficiently hard for suppositories and a
large quantity of glycerin upto 95% of the mass can be
incorporated.
y Further the soap helps in the evacuation of glycerin.
y 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.
y Polyethylene glycol bases / Macrogol bases (Carbowaxes)

PESSARIES
y EMULSIFYING BASES
y These are synthetic bases and a number of proprietary bases of
very good quality are available, few of which are described below:
y Witepsol
y They consist of triglycerides of saturated vegetable acids (chain
length C12 to C18) with varying proportions of partial esters.
y Massa Esterium
y This is another range of bases,
bases consisting of a mixture of di
di-, tri
tri-
and mono- glycerides of saturated fatty acids with chain lengths of
C11 to C17.
y M
Massuppol l
y 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.

PESSARIES
y PREPARATION OF SUPPOSITORIES
y Suppositories are prepared by two processes: moulding (hot
pprocess or fusion process)
p ) and cold compression.
p
y Mould
y Various types and sizes of suppository moulds are available.
y In the dispensary suppository moulds with six or twelve
cavities with desired shape and size may be used. For large
scale production moulds up to 500 cavities may be used.
y Moulds are made up of stainless steel, nickel-copper alloy,
brass, aluminium or plastic.
y For cleaning,
cleaning lubrication and removal of suppositories the
mould can be opened longitudinally by removing the screw in
the centre of the plates.
y Th nominal
The i l capacities
iti off th
the common mouldsld are 11g, 2g,
2 4g4
and 8g.
PESSARIES
y Calibration
C lib i off the h mould ld
y The nominal capacity of a mould is not always correct. It will vary
for different bases. Each mould should be calibrated before use by
preparing a set of suppositories or pessaries using the base alone,
alone
weighing the products and taking the mean weight as the true
capacity. This is repeated for each base and the value is recorded
for future use.
y Displacement value
y The volume of a suppository from a particular mould is uniform
but its weight will vary because the densities of medicaments
usually
ll diff
differ ffrom the
h ddensity
i off the
h base
b with
i h which
hi h the
h mould ld
was calibrated.
y To prepare products accurately, allowance must be made for the
change in density of the mass due to added medicaments
medicaments. For this
purpose the displacement value of a medicament is taken into
consideration.
y Definition: The number of pparts of medicament (drug)
( g) that
displaces one part by weight of the base is known as the
displacement value of that drug.
THE END

Semisolid Dosage Forms PDF

Uploaded by

Document Information

Original Title

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Semisolid Dosage Forms PDF

Uploaded by

Copyright:

Available Formats

SEMISOLID DOSAGE FORMS

Phr. Bibek Singh Mahat

y Pastes: Differences between ointments and pastes.

y Jellies: An introduction to the different types of jellies

y An elementary study of poultice.

They usually contains medicament which is either

They have emollient and protective action.

Creams are semisolid emulsions and are generally

They are less greasy and are easy to apply.

Thus when protective,

Jellies are transparent or translucent, non-greasy, semisolid

y Ointments are semisolid preparations for

y The ointment bases are almost always

y These ointments are intended to produce

y They are not absorbed.

y Theyy acts as pprotectives, antiseptics

(c) Diadermic ointments

y (ii) Antibiotics :Used to kill microorganisms.

y (iii) Antieczematous :Used to stop oozing and exudation from

y (iv) Antifungal :Used to inhibit or kill the fungi.

y (v) Anti-inflammatory :Used to relieve inflammatory, allergic and

y (vii) Antiseptic :Used to stop sepsis.

y (vii) Astringent :Reduces the secretion of glands or discharge from

y (x) Dandruff treatment :e.g. salicylic acid and cetrimide (cetyl

y (xii) Parasiticide :These ointments destroy or inhibit living infestations such

y An ideal ointment base should be inert, stable, smooth,

Classification of ointment bases:

y These bases consists of oils and fats.

y Melting range : 38 to 56C

y (b) Hard paraffin (Paraffin)

y This is a mixture of solid hydrocarbons obtained

y It is a mixture of liquid , hydrocarbons obtained from petroleum. It

y These bases (some times called emulsifiable ointment bases)

y Preparations of this type do not contain water as a

y Advantages of water miscible bases:

y Water soluble bases contain only the water soluble

y Water soluble bases consists of water soluble ingredients such

y Theyy are a range

1. Macrogols 200, 300, 400 - viscous liquids

y Different PEGs are mixed to get an ointment of desired

1. They are water soluble; hence, very easily can be removed

1. Limited uptake of water. Macrogols dissolve when the

y (a) Absorption and Penetration:

y (b) Effect on the skin

y (d) Compatibility with skin secretions:

y (f) Emollient properties

y (g) Ease of application and removal

y (b) Solvent properties

y (c) Emulsifying properties

a. Uniform throughout i.e. it contains no lumps of separated

b. Free from grittiness, i.e. insoluble powders are finely

Two mixing techniques are frequently used in making

1. Fusion, in which ingredients are melted together and stirred

2. Trituration, in which finely-subdivided insoluble

y The medicament is added slowly in the melted ingredients

y This will avoid over-heating of substances having low melting

y All the components are taken in subdivided state and melted

y The maximum temperature

Melting time is shortened by grating waxy components (i.e.

The surface of some ingredients discolors due to oxidation e.g.

After melting, the ingredients should be stirred until the ointment

Vigorous-stirring, after the ointment has begun to thicken, causes

Because of their greasy nature, many constituents of ointment