Paperwork under the course of Pharmacy Practice that discusses the technique and advantages/disadvantages of different topical dosage forms. Created by: Annisa Hayatunnufus Bachelor of Pharmacy Management & Science University

1. SCHOOL OF PHARMACY
Subject: PHARMACY PRACTICE 1
Subject code: SPH1023
Assignment: COMPOUNDING TOPICAL DOSAGE FORMS
Prepared by : ANNISA HAYATUNNUFUS (012014052438)
Lecturer’s Name : SIR NIZAM GHANI
Date of submission : 12th
MARCH, 2015

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TABLE OF CONTENT
I. Table of Content ....................................................................2
II. Introduction ...........................................................................3
III. Discussions..........................................................................7
A. Ointment.......................................................................7
1. General Procedure................................................7
2. Problems & How to Overcome Them....................8
3. Additives ...............................................................9
B. Cream.........................................................................10
1. General Procedure..............................................10
2. Problems & How to Overcome Them..................10
3. Additives .............................................................11
C. Lotion .........................................................................11
1. General Procedure..............................................11
2. Problems & How to Overcome Them..................12
3. Additives .............................................................12
IV. References ........................................................................14

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I. INTRODUCTION
In extemporaneous compounding, it is important to consider which dosage
form suits the patient best. If a wrong or unsuitable dosage form was sent, the
drug may not be distributed properly to the site of action and become
therapeutically ineffective, or in worst case—it may not be safe and subsequently
worsen the patient’s condition.
The dosage form itself may vary according to the drug’s functions and the
patient’s needs. It may correlate with the complexity of the administration route,
the location of site of action, or the patient’s needs such as ability to swallow, skin
sensitivity, and others.
The type of dosage form that is going to be discussed here is the dosage
form for the topical route of administration. ‘Topical’ refers to a type of medication
that is applied directly to the skin, as opposed to being taken by mouth. (Topical
medications can also be put in the eye or ear). Three examples of this dosage
form are lotion, cream, and ointment.
Ointments, creams, and lotions are different ways to formulate over-the-
counter products or medicines. An ointment is 80% oil and 20% water. A cream is
50% oil and 50% water. A lotion is similar to a cream, but it is an even lighter or
less thick formulation. Any of these can be used with different over-the-counter
products or drugs, depending on the dryness or oiliness of one’s skin.
Lotions are similar to solutions but are thicker and tend to be
more emollient in nature. They are usually oil mixed with water, and more often
than not have less alcohol than solutions. Lotions can be drying if they contain a
high amount of alcohol. There is a significant variability in the ingredients of base
of generic lotions when compared to brand name lotions.
Lotion is commonly applicated to inflamed ulcerated skin and is able to cool
the skin by evaporation of solvents. They absorb very quickly and feel very light
on the skin. They are easier to distribute on hairy areas. Most over-the-counter
body moisturizers are lotions, where they are often packaged in a pump.

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Cream is semisolid emulsion of oil and water with equal proportions. It
contains an emulsifying base and is used for external use, penetrating
the stratum corneum outer layer of skin well. Cream is thicker than lotion, and
maintains its shape when removed from its container. It tends to be moderate in
moisturizing tendency as it reasonably hydrates without feeling too heavy on the
skin. It has a high rate of acceptance by patients. There is a great variation in
ingredients, composition, pH, and tolerance among generic brands.
Two main types of cream are oil in water (o/w) cream and water in oil (w/o)
cream. o/w cream is more comfortable and cosmetically acceptable as they are
less greasy and more easily water washable. o/w creams that are readily rub into
the skin are termed as vanishing cream. Meanwhile, w/o creams accommodate
and release better lipophilic API. They are also more commonly used for topical
steroid products.
Creams are always packaged in a tub or a tube; they are too thick to be
dispensed in a pump. Creams for external use are stored in wide-mouth jars with
lid. The mouth of the jar should be covered with a disc of greaseproof paper.
Collapsible metal or plastic tubes are sometimes preferred for cream as these
reduce the risk or contamination.
Creams are often used to treat acne in patients whose skin is somewhat dry,
as the creams promote hydration. Creams are also more beneficial in darker skin,
which in general is more easily irritated than lighter skin.
An ointment is a homogeneous, viscous, semi-solid preparation, most
commonly a greasy, thick oil (oil 80% - water 20%) with a high viscosity, that is
intended for external application on a variety of body surfaces. These include
the skin and the mucous membranes of the eye (an eye ointment), chest, vulva,
anus, and nose.
Ointments are ‘occlusive,’ which means they trap moisture and heat in very
well and good for dry skin. They have a low risk of sensitization due to having few
ingredients beyond the base oil or fat, and low irritation risk. Ointments promote
medication absorption over all other formulations. If an ingredient is in an
ointment, it is always more potent than the exact same ingredient packaged in a
cream or lotion.

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A medicament would usually be incorporated in the ointment. Sometimes it
can also contain a mixture of medicaments that is dissolved or dispersed in the
base. Ointment bases may be divided into oligeanous (hydrocarbon), absorptive,
water-miscible, and hydrophilic. The choice of a base depends upon the clinical
indication for the ointment.
1. Hydrocarbon bases
Hydrocarbon bases are immiscible with water and are not absorbed
by the skin. They usually consist of soft paraffin or mixtures of soft paraffin
with hard paraffin or liquid paraffin. There would be a greasy waterproof film
on the skin that is formed by the paraffin. This would stop water loss from
the skin, hence would improve the skin hydration. This is particularly
important in the treatment of dry scaly medical conditions such as psoriasis.
Examples of this base are hard paraffin, soft paraffin, microcrystalline
wax and ceresine.
2. Absorption bases
These bases can act as good emollients and are less occlusive. It is
easier to apply than hydrocarbon bases. Absorption bases can be divided
into non-emulsified bases and water-in-oil emulsions.
Non-emulsified bases are bases that absorb water to form water-in-oil
emulsions. They consist of a hydrocarbon base combined with a water-in-oil
emulsifier such as Wool Acohols BP or Wool fat BP. Water-in-oil emulsions
are similar to non-emulsified bases but are capable of absorbing more
water. The components of emulsified bases include Hydrous Wool Fat BP
and Oily Cream BP.
3. Water-miscible/emulsifying bases
These are anhydrous bases that contain oil-in-water emulsifying
agents, which make them miscible in water and therefore washable and
easily removed after use. There are three emulsifying ointments that are
used as water-miscible bases which are emulsifying ointment BP, cetrimide

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emulsifying ointment BP, and cetomacrogol emulsifying ointment BP. Since
the bases mix readily with the aqueous secretions of the skin, it makes the
ointment to be easily washed out. So they are particularly suitable for use
on the scalp. Examples of this base are emulsifying wax and cetrimide
4. Hydrophilic bases
Hydrophilic bases are developed from polyethylene glycols
(macrogols). They mix readily with skin secretions and are non-occlusive.
These bases are also easily removed upon washing. Macrogol bases are
commonly used with local anesthetics such as Lidocaine BP.

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II. DISCUSSIONS
A. OINTMENT
1. General Procedure
In general, there are two methods of preparation in making an
ointment: the fusion method and trituration method.
Fusion method usually involves the compounding of many semisolid
preparations that may be hard to blend with each other such as oily
materials. Some materials are even solid at room temperature and
available in a size too large than what is needed. Therefore, fusion
method will make it easier to blend by melting it first.
Meanwhile, trituration method involves insoluble solids or liquids,
which are incorporated into the bases. The kind of solid that is suitable for
the trituration method is a coarse powder because it easy to be decreased
in size into a fine powder. More detailed procedures of the trituration &
fusion methods are as stated below:
 Trituration: With this method, finely subdivided insoluble medicaments
are evenly distributed by grinding with a small amount of the base,
followed by dilution with gradually increasing amounts of the base.
a) To avoid grittiness, powders should be passed through a 180µm
sieve before weighing.
b) This method is done on a glazed porcelain or glass ointment slab
or tile. A flexible spatula is used to mix the material together.
c) Powders are placed on the tile and using doubling-up technique,
the powders are incorporated into the base. In order to avoid
‘crumbling’, it is necessary to have two or three times the volume
of base to powder.
d) If a liquid is present, it is often present in small amounts. To
incorporate a liquid, a portion of the base is placed on the slab and
a recess made to hold the liquid. Then, mix well the liquid and the
base.

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e) If we are dealing with a large quantity, then using the same
method, the liquid is added little at a time.
f) Theoretically, it is possible to recover all material from the slab but
it is normal to allow up to 10% excess for losses. Using a mortar
with a flat base and a pestle with a flat head, this process can be
carried out.
 Fusion: In this method, the ingredients are melted together in
descending order of their melting points. Then they are stirred to
ensure homogeneity.
a) This method is done in an evaporating dish on a water-bath or hot
plate.
b) High temperature is not required; 60-70ºC is adequate.
c) Waxy solids must first be grated before weighed. Then it should be
added first, so the melting can start whilst other ingredients are
being prepared.
d) The basin from the water-bath is removed when all the ingredients
are melted. It is then stirred until cold.
e) In order to avoid bubbles and formation of lumps, the mixing
should be done gently.
f) Medicaments may be added at different stages of the preparation
depending on its properties. A soluble and stable medicament can
be added when the base is molten. A less stable or insoluble but
easy to disperse can be added during cooling. However, if it is
unstable and difficult to disperse, it should then be added when it
is cold—using mixing by trituration.
g) It is important to make an excess of about 10% because when
evaporating basins are being used, the recovery of the entire
product is not possible.
2. Problems & How to Overcome Them
The primary indication of instability for semisolid topical dosage forms
is either discoloration or a noticeable change in consistency or odor.

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Specifically for ointment, the common signs of instability are changes
in particle size, hydration state, consistency, and drug release rate. In
such case, one of the ways to prevent those instabilities is to design the
product based on proper pre-formulation studies.
Sometimes, excessive ‘bleeding’ (i.e., separation of excessive
amounts of liquid) and formation of granules or grittiness (caking or
coalescence) will occur. Accurate preparation of ointment may reduce this
problem.
Also, some people may develop a hypersensitivity reactions to
ointments that are given to them. This is due to the presence of some
minor impurities. Other times, this problem also arises when a patient has
an allergy to a certain ingredient used in the dosage form. That is why
other dosage form may also develop the same problem.
In dealing with this hypersensitivity reaction problem, combinations of
bases are sometimes used to acquire better stability.
3. Additives
Ingredients Usage
Hydrocarbons / Vegetable
Oils / Animal Fat /
Hydrogenated and
Sulphated Oils / Alcohols,
Acids, Esters / Silicones
Oleaginous Bases
Fragrant oils To add fragrance if necessary
Vitamin E oil / Rosemary
Frond Extract
Antioxidants
Bithional / Ethyl Paraben /
Sorbic Acid
Preservatives
Citric Acid / Maleic Acid /
Phosphoric Acid
Chelating Agent

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B. CREAM
1. General Procedure
The pharmacist may be asked to prepare extemporaneous dilutions of
proprietary creams. Dilutions should be carried out only if the diluent to be
used is the stated in the manufacturer’s data sheet (this is usually quoted
in the BNF). The creams must be freshly prepared without heat and with
strict hygienic precaution. Meanwhile, the following is the general
procedure to make a cream from the basic ingredients:
a. Creams are prepared by heating the components of the oily phase
(including the emulsifying agents) until molten at 60 – 70ºC.
b. The components of aqueous phase are mixed separately and also
heated to 60 – 70ºC.
c. The aqueous mixture is then poured into the oily phase at the same
temperature. The resultant mixture is then stirred until cool.
2. Problems & How to Overcome Them
One of the main concerns of using cream dosage form is that it is
prone to lose water, especially in the oil/water type. The more water that
are lost, the easier it is for cream to become dry and ultimately shrinks
due to evaporation or come in contact with too much acid. This problem
can be dealt with proper storage such as making sure that the lid was
properly closed or keeping the cream in a controlled room temperature.
Aside from that, creams also have the problems of emulsion breakage,
crystal growth, and gross microbial contamination. Especially for the case
of microbial contamination, it can be prevented by using a suitable quality
of raw materials, good manufacturing practices, adequate preservation,
and the use of noninvasive packages (such as tubes, pumps, or narrow
orifice containers).

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3. Additives
Ingredients Usage
Wool Fat / Waxes /
Bivalent Soaps / Sorbitan
Esters / Wool Alcohol
Emulsifying agent for w/o creams
Polysorbates / Methyl
Cellulose / Monovalent
soap / Acacia / Tragacanth
/ Triethanolamine Oleate
Emulsifying agent for o/w creams
Cocoamide Dea /
Propylene Glycol / Sodium
Lauryl Sulfate / Sodium
Lauryl Fluoride
Add scent if necessary
Organic Acids / Esters of
Parahydroxybenzoid Acid /
Chlorocresol /
Phenoxyethanol /
Quaternary Ammonium
Compounds / Organic
Mercurial Compounds
Preservatives (same as lotion’s)
C. LOTION
1. General Procedure
The following procedure is an example of the compounding of
Calamine Lotion, therefore some points or ingredients added may only be
valid to this particular lotion. The procedure is as follow:
a. Weigh all ingredients accurately
b. Transfer the weighed bentonite (suspending agent) to the mortar
c. Add the zinc oxide (active ingredient with antiseptic properties)
using the doubling-up technique, then triturate with pestle
d. Add calamine powder (active ingredient for itching & irritation)
using doubling-up technique, then triturate with pestle
e. Add sodium citrate (pH buffer/chelating agent/antioxidant) to the
mortar, mix with pestle to form a smooth paste

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f. Add glycerol (for humectant effect) & liquefied phenol (for cooling
effect) to the paste, mix with pestle until the mixture is pourable
g. Transfer the contents to a conical measure or the final container
h. Rinse the mortar with water and add to the final container
i. Make up to volume with any remaining water
j. Label appropriately and dispense
2. Problems & How to Overcome Them
Certain lotions tend to separate or stratify on long standing. In such
case, they require a label directing that they should be shaken well before
each use. This will help mixing the lotion again so that the ingredient is
spread evenly.
Just like other dosage form, microorganisms may grow in lotions if no
preservative is included. However, a lotion that are microorganism-free
might still be contaminated after usage. Therefore, extra care should be
taken to avoid contaminating the lotion during preparation, even if a
preservative is present.
3. Additives
Ingredients Usage
Water Decrease greasiness
Bentonite Suspending agent
Methyl Cellulose/Sodium
Carboxymethyl Cellulose
Holds active ingredient in contact with the
affected site & at the same time rinsed off
easily with water.
Alcohol
Accentuate drying & cooling effect of a
lotion
Glycerin Gives a humectant (moisture preservative)
effect
Sodium Citrate pH buffer/chelating agent/antioxidant
Organic Acids / Esters of
Parahydroxybenzoid Acid /
Chlorocresol /
Phenoxyethanol /
Preservatives (same as cream’s)

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Quaternary Ammonium
Compounds / Organic
Mercurial Compounds

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III. DISCUSSIONS
 Bellevue Acne Clinic. What is the Difference between Cream, Ointment, and
Lotion?. [Online] Available from: http://bellevueacneclinic.com/what-is-the-
difference-between-cream-ointment-and-lotion.html [Accessed on 24th
February 2015].
 Wikipedia Organization. Topical Medication. Wikipedia. [Online] Available
from: http://en.wikipedia.org/wiki/Topical_medication#Ointment [Accessed on
24th
February 2015].
 Michel McDonald, M.D. Vanderbilt University Medical Center. (2009). What’s
the Difference between an Ointment, A Cream, and A Lotion?. Abc NEWS.
Available from:
http://abcnews.go.com/Health/WellnessResource/story?id=6858390.
[Accessed on 24th
February 2015].
 Sahudin, S., Rabi, R., Fern, N.G.S., & Paraidathathu T. (2011). Pharmacy
Practice: Guide to Compounding and Dispensing. Selangor: Penerbit
Universiti Kebangsaan Malaysia.
 Premjeet, S., Ajay, B., Sunil, K., Bhawana, K., Sahil, K., Divashish, R., &
Sudeep, B. (2012). Additives in Topical Dosage Forms. International Journal
of Pharmaceutical, Chemical, and Biological Sciences, 2(1), 78-96. ISSN:
2249-9504. Available from: http://www.ijpcbs.com/files/08.pdf [Accessed on
26 th
February 2015].
 Dash, A.K., Singh, S., Tolman, J. (2013). Pharmaceutics: Basic Principles
and Application to Pharmacy Practice. United States: Academic Press.
 Hunt, Desmond G (1991). Stability Considerations in Dispending Practice.
United States Pharmacopeia. Available from:
http://www.pharmacopeia.cn/v29240/usp29nf24s0_c1191.html [Accessed on
9th March 2015]
 Okeke, I.N. and Lamikanra, A. (2001), Bacteriological quality of skin-
moisturizing creams and lotions distributed in a tropical developing country.

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Journal of Applied Microbiology, 91: 922–928. doi: 10.1046/j.1365-
2672.2001.01456.x
 Remington, J. P. (1995). Remington, the science and practice of pharmacy.
Easton, Pa: Mack Pub. Co.