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LOZENGES FORMULATION AND EVALUATION: A REVIEW

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IJAPR Review Article

Available Online through
www.ijapronline.org ISSN: 2230 – 7583

LOZENGES FORMULATION AND EVALUATION: A REVIEW

Renuka Pothu1, Madhusudan Rao Yamsani*
Vaagdevi college of Pharmacy, Kishanpura, Warangal, A.P.
Received on 03 – 04 - 2014 Revised on 10 –04- 2014 Accepted on 25– 04 – 2014
ABSTRACT
Lozenges, or troches, are experiencing a renewed popularity as a means of delivering many different drug products.
Lozenges have various advantages and disadvantages. Different types of lozenges and their methods of preparation
along with ingredients used in their preparation are discussed. The selection criteria for flavoring agents and
preservatives are mentioned, packing, quality control tests, storage, dispensing of lozenges have been reviewed in
this. Examples of different lozenge formulations and different marketed products can be known from this review.
Lozenges have bright future as a novel method of delivering drugs for local action and systemic effect. The
acceptance for lozenges as a dosage form is high by adults and also more by children.
Key Words: Lozenge, Troches, Excipients, Sweeteners.

INTRODUCTION
Lozenges are solid preparations that contain one
or more medicaments, usually in a flavored,
sweetened base, that are intended to dissolve or
disintegrate slowly in the mouth. They can be
prepared by molding (gelatin and/or fused sucrose
and sorbitol base) or by compression of sugar-based
tablets. Molded lozenges are sometimes referred to as
pastilles, whereas compressed lozenges may be
referred to as troches. They are used for patients who
cannot swallow solid oral dosage forms well as for
medications designed to be released slowly to yield a
constant level of drug in the oral cavity or to bathe
the throat tissues in a solution of the drug. Lozenges
historically have been used for the relief of minor
sore throat pain and irritation and have been used
extensively to deliver topical anesthetics and
antibacterial.
Author for Correspondence
Prof. Y. Madhusudan Rao
Director, Vaagdevi College of pharmacy,
Kishanpura, Warangal, Andhra Pradesh
India-506001
Mobile No; 9493873284
E. Mail: ymrao123@yahoo.com
Today they are used for of drugs like analgesics,
anesthetics, antimicrobials, antiseptics, antitussives,
aromatics, astringents, corticosteroids, decongestants,
and demulcents and other classes and combinations.
They are easy to handle, the dose has been
apportioned, and the excipients have a demulcent
effect on throat since the ingredients are released
slowly and spread uniformly over the affected
mucosal membrane.
The USP [1] currently recognizes Cetyl
pyridinium Chloride Lozenges and Nystatin
Lozenges. However, more than five dozen over-the-
counter (OTC) lozenge products are currently
marketed. [2]
A BRIEF HISTORY
James Loft house was born in Lancaster
(England, UK) in 1842 and opened his pharmacy in
Fleetwood on the Fylde coast in 1865. At that time
Fleetwood was a growing fishing port and home of
the North Atlantic fishing trawlers teeming with
fishermen suffering from various bronchial
complaints. Seizing the opportunity, James
formulated an extra strong bronchial mixture
containing menthol, eucalyptus oil; capsicum and
liquorice designed to be dropped onto sugar cubes
and sucked. Unfortunately, glass bottles were not the
ideal containers for his customers, who complained
that they broke in rough seas. Consequently, he

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 Madhusudan Rao Yamsani. et al. /International Journal of Advances in Pharmaceutical Research
reformulated the mixture into a solid form – a
lozenge consisting of the same ingredients dispersed
in a sugar and gum base massed with water, which
was then rolled, cut into shapes and oven dried. Such
was the popularity of this formulation that fishermen
constantly came into his pharmacy requesting ‘an
ounce of friends’ or ‘a bag of fisherman’s lozenges’ –
hence the origin of the famous brand name
‘Fisherman’s Friend’ [3]
Advantages
It is easy to administer to both pediatric and geriatric
patients.
It has a pleasant taste and will extend the time a
quantity of drug remains in the oral cavity to
elicit local activity.
Systamic absorption of drugs can be possible through
buccal cavity.
It can be prepared with minimal equipment.
Taste of the drugs can be masked by sweetners and
flavours used in the formulation.
Disadvantages
It could be mistakenly used as candy by children.
Parents should be cautioned not
associate medications with candy and to keep the
product out of the reach of children. Some drugs may
not be suitable with aldehyde candy bases eg;
benzocaine.
Heat stable drugs are suitable.
Children having above 6 years of age can use lozenges
safely.
Drugs having minimum bitter taste are suitable.
Types and Definitions
Lozenges are various-shaped, solid
dosage forms usually containing a medicinal agent
and a flavoring substance, intended to be dissolved
slowly in the oral cavity for localized or systemic
effect. They are also called troches or pastilles.
Pastilles have a softer texture and a high percentage
of a sugar or a combination of a gelatin and sugar.
Many lozenges have hard candy bases of sugar and
syrup and often incorporate an adhesive substance
such as acacia. Commercial lozenges (troches) may
be made on a tableting machine using high
compression pressures. Lozenges are designed to
dissolve slowly in the mouth. They are designed to
dissolve and not to disintegrate. Ingredients should be
heat-stable if they are to be incorporated into
extemporaneously-prepared lozenges. Recently, soft
lozenges and chewable lozenges have been re-
introduced into pharmacy and are enjoying increased
popularity. The soft lozenges generally have a
polyethylene glycol base and the chewable lozenges
have a glycerinated gelatin base. These usually are
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
chewed and are a means of delivering the product to
the gastrointestinal tract for systemic absorption.
Hard candy Lozenges
Hard candy lozenges are mixtures of sugar and
other carbohydrates in an amorphous (no crystalline)
or glassy condition. These can be considered solid
syrups of sugars and Lozenges historically have been
used for the relief of minor sore throat pain and
irritation and have been used extensively to deliver
topical anesthetics and antibiotics. Lozenges are
various-shaped, solid dosage forms usually
containing a medicinal agent and a flavoring
substance, intended to be dissolved slowly in the oral
cavity for localized or systemic effects. Usually they
have a moisture content of 0.5 to 1.5% Hard
lozenges should provide a slow, uniform dissolution
or erosion over 5 to 10 minutes, not disintegrate, have
a smooth surface texture and have a pleasant flavor
masking the drug taste. A primary disadvantage of
hard candy lozenges is the high temperature required
for their preparation. Hard candy lozenges generally
weigh between 1.5 to 4.5 gm. Excipients such as
to sorbitol and sugar have demulcent effects, which
relieve the discomfort of abraded tissue resulting
from irritation due to cough and sore throat. A
portion of the active drug product actually may be
absorbed through the buccal mucosa, thereby
escaping the first-pass metabolism which occurs
when a drug is swallowed and absorbed through the
gut.
All hard candy type lozenges
eventually become grainy but the speed at which this
occurs is dependent upon the ingredients that are
used. The incorporation of corn syrup solids at a
greater than 50% concentration decreases the
graining tendencies but can increase moisture
absorption tendencies which increase product
stickiness and interactions of medicaments. Using
greater than 70% sucrose solids tends to increase
graining tendencies and the rapidity of crystallization.
Formulations that contain between 55 and 65% sugar
and 35 to 45% corn syrup solids generally offer the
best compromise among the resistance to graining,
reduction of moisture absorption and realistic
preparation time. Acidulents, such as citric, tartaric,
fumaric and malic acid may be added to candy base
to strengthen the flavor characteristics of the finished
product and to control pH to preserve the stability of
the incorporated medication. Regular hard candy has
a pH of about 5.0 to 6.0 but with the addition of
acidulents, it may be as low as 2.5 to 3.0. Calcium
carbonate, sodium bicarbonate and magnesium
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trisilicate can be added to increase the lozenge pH to
as high as 7.5 to 8.5.
Soft Lozenges
Soft lozenges have become popular because
of the ease of extemporaneous preparation and
applicability to a wide variety of drugs. The bases
usually consist of a mixture of various polyethylene
glycols, acacia or similar materials. One form of
these soft lozenges is the pastille, which is defined as
a soft variety of lozenge, usually transparent,
consisting of a medication in a gelatin, glycerogelatin
or acacia: sucrose base. Pastilles may be colored and
flavored and can be either slowly dissolved in the
mouth or chewed, depending upon the action desired
for the particular incorporated drug.
Soft lozenges are similar to a
historical form of medication that is making a
comeback: the “confection”. Confections are defined
as heavily saccharinated, soft masses containing
medicinal agents. The improvement in their current
use is largely due to the use of polymers
(polyethylene glycols) as the matrix for the dosage
form. They are easy to use, convenient to carry, easy
to store (room temperature), and are generally
pleasant tasting. Polyethylene glycol-based lozenges
may have a tendency to be hygroscopic and may
soften if exposed to high temperatures. Consequently,
storage in a cool, dry place should be recommended.
Chewable Lozenges
Soft, chewable candies have been on the
market for a number of years. They are very highly
flavored and many often contain a slightly acidic
taste. They are an excellent way of administering
drug products as the taste of the drug often can be
masked very effectively with fruit-flavored products.
They are relatively easy to prepare
extemporaneously. The most difficult part involves
the preparation of the gelatin base which is described
below. These are especially used for pediatric
patients and are a very effective means of
administering medications for gastrointestinal
absorption and systemic use.
One of the more popular lozenges for
pediatric use is the chewable lozenge, or “gummy-
type” candy lozenge. The gelatin base for these
chewable lozenges is similar to the former Glycerin
Suppositories, or Glycerinated Gelatin Suppositories,
which consisted of 70% glycerin, 20% gelatin and
10% purified water. Some of the earlier pastilles
consisted of a gelatin or a glycerogelatinm base.
These gelatin-based pastilles were prepared by
pouring the melt into molds or out onto a sheet of
uniform thickness. The dosage forms were then
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
“punched out” using various shaped punches. The
last step often included the “dusting” of the product
with corn starch or powdered sugar to decrease
tackiness. These pastilles should be stored in a
refrigerator, depending upon the active drug content.
Hard Candy Lozenges
Raw Materials
The types of raw materials used in medicated
lozenges may vary according to a number of factors.
Most medicated lozenges contain sugar, corn syrup,
acidulant, colorant, flavor, and the medicament.
1. Sucrose
Sucrose, a disaccharide of glucose and fructose, is
obtained from sugarcane or beet. The choice of beet
or cane sugar is based on availability and
geographical considerations. Sucrose and sucrose
products are used in medicated lozenges because of
their value as neutral sweeteners, their ready
solubility, and their function as a ‘‘drier’’ to reduce
the weight of the confection through crystallization.
2. Invert sugar
Invert sugar, derived from sucrose, possesses the very
desirable physical property of controlling the
crystallization of concentrated sugar solutions and
maintaining freshness of the finished product through
its humectant properties.
3. Corn syrup
Corn syrup is used in almost every type of confection
to control sucrose and dextrose crystallization, which
may lead to crumbling.
Corn syrup in appropriate proportion with sucrose
and dextrose allows the formation of an amorphous
glass and produces a candy with the desirable
appearance.
The following physical properties of corn syrup are
extremely important in the preparation of medicated
candies: density, dextrose equivalent (DE),
hygroscopicity, sugar crystallization, viscosity,
freezing point depression, and osmotic pressure.
4. Isomalt
Isomalt is an almost equimolar mixture of 6-
glucopyranosyl-sorbitol (6- GPS) and 1-
glucopyranosyl-mannitol (1-GPM), and the weight
percentage can vary between 43 to 57% of 6-GPS to
57% to 43% of 1-GPM. Isomalt has properties like a
binding agent, i.e. to a certain extent it is capable of
establishing binding between the individual particles
in the composition and further in the binding during
the kneading step in the process of preparing a
lozenge. Isomalt is beyond being a binding agent also
a suitable softener. The lozenges prepared with a
binding agent comprising isomalt are softer than
lozenges that do not contain any isomalt.
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5. Colorants
Colorants are incorporated into medicated lozenges
for appearance, product identification, and masking
of physical degradation.
6. Dyes and other organic colorants
Dyes and other organic colorants may degrade by
heat or light via oxidation, hydrolysis, photo
oxidation, etc., and their compatibility with drug,
excipients, and process conditions should be studied
before selection. Suppliers of colors are excellent
sources of information on current regulatory status of
colorants.
7. Acidulants
Acidulants are generally added to medicated lozenges
to fortify and strengthen their flavor profile. Organic
acids such as citric, malic, fumaric, and tartaric acids
are most commonly used. Citric acid alone or in
combination with tartaric acid is the most common.
Another use of acids in medicated lozenges is to alter
the pH to maintain the integrity of the drug.
Regular conversion corn syrup has a pH of 5.0–6.0.
Addition of a weak organic acid to improve flavor
lowers it to 2.5–3.0, a pH at which some
medicaments exhibit maximum stability. If
necessary, some drugs can be stabilized by adjusting
the pH to 7.0–8.0 with a suitable weak base such as
calcium carbonate.
Some research has shown that excessive use of acidic
lozenges could have the potential to enhance existing
dental erosion, and that low pH (2.6–3.7) leads to
dissolution of calcium and phosphorous from
hydroxyapatite. Others have shown that excessive use
of citric and tartaric acids may affect bioavailability
of zinc in zinc lozenges. Another report indicated that
the activity of cetyl pyridinium chloride in candy-
base lozenges is influenced by pH, with >5.5 being
most desirable. Acceptable taste is necessary to
ensure patient acceptability, and this can be the
determining factor between commercial success and
failure of an OTC product.
8. Flavors
Flavors used in medicated lozenges must be
compatible with the drug and excipients and capable
of withstanding the rigors of the manufacturing
conditions.
Flavors consist of numerous chemicals that may
interact with excipients or medicaments and that
degrade by heat and light. Aldehydes, ketones, and
esters may react with drugs. A classic example of
flavor–drug interaction is that of a primary amine
drug (benzocaine, phenylpropanolamine) with
aldehyde containing flavor components like cherry,
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
banana, etc., resulting in the formation of a Schiff
base, drug decomposition, and loss of efficacy.
Adjustment of lozenge base pH to accentuate certain
flavors (e.g., citrus) may also result in incompatibility
with some medicaments (e.g., benzocaine).
9. Salvage
The last major ingredient in lozenges is salvage
obtained from lozenge batches rejected because of
imperfect shape or size, presence of air bubbles, or
unacceptable drug concentration. Salvage, if properly
heated, can be reused in finished products without
altering color, texture, lozenge base composition, or
drug concentration.
Before any salvage can be used as part of a
medicated lozenge base, it should be adjusted to a pH
of 4.5–7.5 to prevent excessive and uncontrolled
formation of reducing sugars, and the stability of the
drug at cooking cycles should be determined.
Candy-Base Manufacturing
The first step in the manufacture of
medicated lozenges is the preparation of candy base,
followed by the addition of medicament, flavor,
acidulants, colors, etc., and finally by lozenge
formation. Irrespective of process, the manufacture of
medicated lozenges involve the cooking of candy
base, mixing, batch forming, ‘‘rope’’ sizing,
adjustment of weight, lozenge formation, cooling,
and storage of lozenges. [3]
Candy base is prepared from liquid sugar
(67% sugar) and corn syrup (liquid glucose, 80%
solids) in a ratio of about 60: 40. Precooking is
initiated under vacuum at controlled temperature.
The precooked solution is transferred
into the steam heated coil, where it is boiled and from
which it is moved to the intermediate chamber where
final mixture is produced. The final moisture content
of candy base should be about 1%, its temperature
about 135ºC, and its consistency plastic-like. The
candy base is transferred into a kettle mounted on a
suitable scale and, if necessary, batch weight is
adjusted.
Heat-stable colors are added at this
point as cubes or paste. The colored candy base is
transferred to a cold stainless-steel cooling plate for
the mixing operation.Mixing can be manual or
mechanical, using a series of plows and rollers, or a
mixer consisting of two arms, a plunger, and a slowly
rotating table top. The temperature of the mixing
table is maintained at 40–50ºC. Flavor, medicament,
acidulant, and ground salvage are added to the
colored candy mass when mixing is initiated. After
completion, the medicated candy base is transferred
to a warm slab and allowed to equilibrate to a
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uniform temperature. The mass is cut into workable
portions, properly tempered, and placed into batch-
forming (holding) machines. For candy formers
requiring a flat sheet, heated tables are used. For
candies requiring cylindrical pieces to be fed into the
batch formers, batch rollers are used.
A plastic-like mass is formed into a sugar cone and
transferred at a predetermined rate to the sizing roller.
The operation of the batch former is synchronized
with the rope sizer. In order to maintain a
temperature at which the outer shell of the candy
would not crack, the batch formers are kept at the
height to which the batch formers are adjusted and
the amount of material in them dictates the delivery
rate of the candy flowing as a rope from the batch
former to the sizing rollers. The sizers consist of sets
of successively smaller forming rolls. The thickness
of the rope is determined by the diameter of the
sizing rollers and governs the weight and size of the
candy. The sizers are generally heated to maintain
temperatures of 50–60ºC, preventing the candy from
cracking by rapid cooling. For the formation of the
final lozenge, the candy rope is discharged into a
forming machine. The formed lozenges are then fed
onto the distribution belt, which provide intensive
cooling and shaking to prevent deformation of the
still plastic lozenge. [5]
The formed candy must be cooled as quickly as
possible to prevent loss of shape. The candy is
usually cooled on a conveyor belt made of chain or
canvas. Multi belt coolers are designed in such a way
that the first narrow belt (15–20 cm wide) runs as
rapidly as the candy-forming machine. At the end of
the first belt, a breaker separates the candy and
distributes the lozenges uniformly across a wider,
slower-moving second belt. The third belt is still
wider and travels even more slowly, allowing enough
time to cool the lozenge to the desired temperature
(below 35ºC). [4]
In the sizing operation, the medicated lozenges are
collected as they leave the cooling belt and
transferred to a series of counter rotating rollers
separated via caliper adjustment. [5]
The sizing operation removes all oversized and
undersized lozenges, ensuring uniformity. The
properly sized lozenges are collected and stored in a
climate-controlled room at 15–20ºC and a relative
humidity of 25–35% until the product is cleared by
the quality control unit for packaging.
Recent technological advances in lozenge
manufacture include a patent that teaches a
continuous process for producing dextromethorphan
lozenges. A new lozenge cutter apparatus consisting
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
of a drum with an array of cutter elements is
described in a 1997 patent. [6] [7]
A distributing device for feeding lozenges (or other
flat products) via a feed conveyor to a ‘‘user’’
machine, such as a packager, is described in a 1993
Patent. [8]
Compressed Tablet Lozenges
Commercially, the preparation of lozenges by tablet
compression is less important than hard-candy
manufacturing techniques. Essentially, lozenge
tablets differ from conventional tablets only in their
organoleptic and non-disintegrating properties and
slower dissolution rate.
The associated attributes of pleasant taste with or
without matching color, smoothness, and mouth feel
during prolonged dissolution on the tongue, and the
physical consideration of holding the tablet in the
mouth while swallowing its dissolved components,
Unusual formulation requirements are to be met
by lozenges compared to those of tablets intended for
swallowing or chewing. The commonly used drugs
mentioned previously tend to be bitter, unpleasant
tasting compounds. The desire to release these agents
slowly in the mouth, in constant contact with the
tongue, demands a formulation approach unlike that
found in any other dosage form.
Processing and Excipients
Any of the common tablet-processing methods, such
as wet granulation, dry granulation, or direct
compaction, may be utilized in the production of
lozenge tablets. However, because the tablets should
dissolve very slowly without disintegration, wet
granulation is preferable because it generally
provides better control. Through the judicious use of
wet binders that retard dissolution, it should be
possible to design a formulation having the
appropriate dissolution rate.
Formulating for slow dissolution, plus
smoothness and good mouth feel, these require
careful excipient selection and appropriate process
development to ensure that the controlling variables
are dealt with correctly. Several important aspects of
lozenge tablet manufacture are critical to all of the
desired performance attributes of the finished
product. These include assurance of necessary
particle size and distribution, maintenance of correct
moisture content, and achievement of proper tablet
hardness. Process development and scale up
considerations must be thoroughly explored to ensure
the establishment of proper specifications for these
parameters.
As always when the process involves wet
granulation, the extent of wetting and the rate and
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extent of drying must be defined. Over wetting
almost certainly produces harder granules that may
have poor compression characteristics, resulting in
softer and more friable tablets unacceptable for
lozenge application. Because of the lesser degree of
particle deformation, such granulations produce
tablets having a gritty mouth feel. Over wetting also
leads to longer drying times in order to achieve the
desired moisture level or, to a higher moisture level
due to failure to compensate through adjustment of
the drying cycle.[9]
Lozenge tablets are generally formulated
as relatively large-diameter (>12.5 mm), flat-faced
(beveled edge), heavy (>700 mg) tablets with high
hardness (>15 kp). These physical attributes lead to
ease of use in the mouth and contribute to the desired
slow dissolution.
The formulation factors primarily
responsible for controlling dissolution, hardness, and
mouth feel are the presence of a high strength,
dissolution retarding binder and the absence of a
disintegrate. Several commonly employed binders
meet these criteria and provide the added benefit of
delivering a demulcent-like action in the throat.
Gelatin
Gelatin (in the form of a warm 10% aqueous
solution) and acacia gum (in the form of an aqueous
mucilage) in wet granulation form very hard tablets
with slow dissolution. Guar gum, used as aqueous
thixotropic mucilage, exhibits behavior similar to that
of acacia gum
Sugar bases
The sugar bases frequently associated with lozenge
tablets are sucrose or compressible sugar, dextrose,
mannitol, and sorbitol, which are available in special
tableting grades from a variety of excipient
manufacturers. Generally intended for direct
compaction applications, they may also be utilized
with the above binders in wet-granulation systems.
A nonnutritive sweetener is a synthetic or
natural sugar substitute whose sweetness is higher
than or comparable to sucrose. Table 1 lists examples
of nonnutritive sweeteners and their relative
sweetness values.
Lactose
Lactose, because of its extremely low
sweetness (15% of sucrose), is limited for use in
lozenges because it would require the addition of an
artificial sweetener of sufficient potency to overcome
its blandness.
Xylitol
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
Xylitol is relatively sweet and has an
advantage in lozenge formulation with respect to its
lack of caries production.
Artificial sweeteners
Artificial sweeteners are of significant
importance to lozenge tablet formulations. As noted
above, some sugars may not be sweet enough to
mask the bitterness or sourness of many drugs.
Presently, there is considerable regulatory
disagreement worldwide concerning these materials;
some are approved for use in certain Countries but
not others.
Aspartame, asulfame-K, cyclamate, saccharin, and
sucralose appear to be technically usable, but their
selection requires care from the regulatory
perspective.
All have potency (sweetness) levels orders of
magnitude higher than that of sucrose, permitting the
use of very low concentrations (less than 1%) to
cover most bitter drugs. Semisynthetic sweeteners,
derived from glycyrrhiza, have enjoyed some degree
of popularity over the years. They are much sweeter
than sucrose, but less sweet than saccharin. It is
strongly recommended that the formulator validate
the current regulatory acceptance of the intended
sweetener prior to its use for a particular product and
market country. In addition, a recent report suggests
that the common lubricant, magnesium stearate,
reduced the effectiveness of cetylpyridinium chloride
in compressed tablet lozenges, and that the
concentration of this ingredient in such a formulation
should be maintained at not more than 0.3%.[10]
Flavoring
Some correlations can be made between
flavors/odors and chemical structure. For example, a
sour taste is associated with hydrogen ions, saltiness
with both anions and cations present, bitterness with
high molecular weight salts, sweet with polyhydroxyl
compounds/polyhalogenated compounds and alpha
amino acids, a sharp, biting taste with unsaturation, a
camphoraceous odor with a tertiary carbon atom, a
fruity odor with esters and lactones, and a pleasant
odor with ketones. The causative factors for taste
include the following: a hot taste is due to a mild,
counterirritant effect, an astringent taste is due to
tannins and acids, coarseness/grittiness is due to
texture, and coolness is due to a negative heat of
solution. In flavor formulation development, there are
usually the requirements for an immediate flavor
identity, a rapid full flavor development, compatible
mouth feel, no “off” notes, and a short aftertaste.
Some techniques commonly used in flavoring include
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blending, overshadowing, physical methods,
chemical methods, and physiological methods.
Blending:
Blending incorporates the use of a
characteristic common to both the flavor and drug,
for example the use of a fruit flavor to blend in with a
sour/acid taste (orange flavor to blend with ascorbic
acid). Salty/sweet/sour flavors can be used to blend
with a bitter taste. Also, the use of a slight salty taste
will actually decrease sourness and increase
sweetness. It has also been found that adding a sour
flavor may help overcome a bitter taste
Over shadowing:
Methyl salicylate and glycyrrhiza, with their
strong essences,can overshadow or overpower many
products.
Flavor selection guide
Taste Flavors That Can Be Used
Salty; Butterscotch, Maple, Nutty, Buttery,
Spice
Bitter Wild Cherry, Licorice, Chocolate
Mint, Grapefruit, Coffee, Cherry, Peach,
Acrid/ Raspberry, Fruits, Berries, Acacia
Sour Syrup
Oily Peppermint, Anise, Wintergreen
Sweet Fruit, Berry, Vanilla
Acid; Citrus Metallic Berries, Mint, Grape,
Marshmallow
Preservatives
Since these are solid dosage forms, there
usually is no need to incorporate preservatives.
However, since hard candy lozenges are hygroscopic,
the water content may increase and bacterial growth
may occur if they are not packaged properly. Since
the water that is present would dissolve some
sucrose, the resulting highly concentrated sucrose
solution is bacteriostatic in nature and would not
support bacterial growth. A few comments are in
order concerning the flavors and effects of
preservatives. For example, a 0.08% solution of
methylparaben has an odor described as “floral”,
“gauze pad”, or “face powder” sweet. A 0.015%
solution of propylparaben has an effect that is tongue
numbing, producing a slight sting and a minimal
aroma. A 0.125% butyl paraben solution has the least
aroma of all. Preservatives may have a tendency to
partition into flavors since preservatives are not
always very water soluble and most flavors are oily
in nature
Packaging
Hard candies are hygroscopic and usually prone to
absorption of atmospheric moisture. Considerations
JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298
must include the hygroscopic nature of the candy
base, storage conditions of the lozenges, length of
time they are stored and the potential for drug
interactions. These products should be stored in tight
containers to prevent drying. This is especially true of
the chewable lozenges that may dry out excessively
and become difficult to chew. If a disposable mold
with a cardboard sleeve is used, it is best to slip this
unit into a properly labeled, sealable plastic bag.
QUALITY CONTROL
Lozenges require the same quality assurance
and control measures as any pharmaceutical dosage
form. Because of their unique composition, however,
certain additional methods are necessary.
In Process Testing
In addition to all of the common in-process tests
used for all dosage forms, certain specialized
procedures are necessary for hard candy lozenges.
These include checking the corn syrup and sugar
composition, temperature, steam pressure, and the
cooking speed of pre cooker and cooker; analysis of
the candy base and its moisture content, and
determination of the sugar to- corn syrup ratio using
the dextrose equivalent method, percent-reducing
sugar (by reacting candy with copper sulfate and
alkaline cupric tartrate and titrating with dextrose
solution), pH, cooked candy batch weight, lozenge
weight, and lozenge size.
The usual in-process tests for compressed tablets
apply to lozenge tablets, including particle-size
distribution, moisture content, flow, blend
uniformity, tablet weight and thickness control,
hardness, etc.
Batch-Release Testing
In addition to the usual quality control procedures
and the above in-process tests, batch-release testing
includes dosage uniformity and a test for grittiness,
performed by partially dissolving lozenges under
running tap water until one-third to one-half has been
removed. No grittiness must be felt when rubbed
between thumb and forefinger.
Test procedures that are
ordinarily applied to compressed tablets are also
employed for lozenge tablets. However, because the
lozenge is intended to dissolve slowly in the mouth,
typical disintegration and dissolution testing is
inappropriate. Lozenges should be non-
disintegrating; therefore, there is no need for
disintegration testing. Dissolution specifications
should be developed on the basis of a minimum and
maximum time to physically dissolve, rather than on
the basis of minimum percent drug released in the
maximum time interval.
296
 Madhusudan Rao Yamsani. et al. /International Journal of Advances in Pharmaceutical Research

As with hard candy lozenges, microbial testing may Formula for 10 lozenges
be appropriate, especially when wet granulation has Drug 1 gm
been used in processing the materials and high Polyethylene glycol1000 10 gm
concentrations of carbohydrates are present. Aspartame 20 gm
Stability Mint extracts 1 ml
For both hard candy lozenges and compressed Color q.s
tablet lozenges, stability considerations extend to
areas not usually of concern with other types of Chewable Lozenge
tablets. These products should not only conform to Formula for 40 lozenges
chemical and physical specifications, but should also Drug 0.5 gm
exhibit satisfactory stability of organoleptic attributes Glycerin 70 ml
at elevated temperatures and elevated humidity. Gelatin 18 gm
Because lozenges are flavored, flavor stability is Water 12 ml
important. There is, however, no objective method Methylparaben 0.4 gm
for measuring flavor stability in a finished dosage Flavoring oil 3 to 4 drops
form, although gas chromatography may be used for Color q.s
chemical analysis of flavor compounds.
Even subjective methods such as tasting are MARKETED PRODUCTS
difficult because formal taste panels are needed to There are several marketed products for different
acquire reliable data. Suitable changes in flavor with uses. They are as follows
time, although not affecting product performance,
may have a significant impact on product market Brand name
acceptability. This could also be true of minor Use
changes (increase or decrease) in tablet hardness, Difflam
color, odor, taste; grains formation affects dissolution anti inflamatory Androlex
time and therefore acceptability. c,
Storage antiseptic, anti inflammatory
These preparations should be stored away from heat Strepsils,
and out of the reach of children. They should be antiseptic CORLAN
protected from extremes of humidity. Depending on (Hydrocortisone) 2.5 mg lozenges
the storage requirement of both the drug and base, antiulcer
either room temperature or refrigerated temperature Fungilin (Amphotericin B)
is usually indicated. antifungal
Cold-EEZE® Zinc Gluconate Lozenge ,
Dispensing zinc supplement
The patient should receive counseling about the Strepfen Anti-inflammatory Lozenges (sugar free)
purpose of a hard lozenge/troche which is to provide anti anti inflammatory etc
a slow, continual release of the drug over a prolonged Potters lozenges
period of time. Soft and chewable lozenges are to be decongestant
taken only as directed and not considered as candy. Duro-Tuss Cough Lozenges
They should be kept out of the reach antitussive
Nicorite
EXAMPLES OF FORMULATIONS smoking suppresent
Hard Lozenge
Formula for 30 lozenges There are several sugar free lozenges available in the
Drug 1 gm market they are as follows
Powdered sugar 42 gm Bosisto’s Eucalyptus Drops (sugar free)
Corn Syrup 16 gm Difflam Anti-Inflammatory Anti Bacterial Lozenges
Water 24 ml (sugar free)
Mint extracts 1.2 ml Double ‘D’ Eucalyptus Drops (sugar free)
Color q.s Fisherman’s Friend (sugar free)
Soothers (sugar free)
Soft Lozenge Strepfen Anti-inflammatory Lozenges (sugar free)

JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298 297

 Madhusudan Rao Yamsani. et al. /International Journal of Advances in Pharmaceutical Research

strepsils (sugar free) (3) Ramond c.Rowe, Astrazenca, 2002.Formulating

Vicks Vital Vitamin C Throat Lozenges etc. fortunes-the tale of medicated lozenges,Drug
discovery today.7,286-287.
Table 1: Non-nutritive Sweeteners (4) Peters, D. Medicated lozenges. In Pharmaceutical
Sweetener Sweetn Sweete Sweetness1 Dosage Forms: Tablets, 2nd Ed.; Lieberman, H.A.,
1
ess ner Lachman, L., Schwartz, J.B., Eds.; Marcel Dekker,
Saccharin 400- Invert 1.1-1.2 Inc.: New York, 1989; I, 419–463.
500 sugar (5) Technical bulletin. In Machines, Production Lines
Cyclamate 30-40 Palantin 0.4-0.5 and Process Technologies for the Confectionery
ose Industry; Robert Bosch Corp.: Bridgman, MI; 1998.
Aspartame 100- Xylitol 1.0 (6) Beahm, J.S. Dextromethorphan Continuous
200 Lozenge Manufacturing Process. US Patent
Acesulfam 200 0.5-0.6 5,302,394, April 12, 1994.
e Sorbitol (7) Duchow, R.W. Lozenge Cutter Apparatus. US
Monellin 2500 Mannit 0.4-0.6 Patent 5,676,982. Oct 14, 1997.
ol (8) Spatafora, M.; Gamberini, A. Distributing Device
Neohesperi 1000 -- for Feeding Flat Products to a User Machine. US
dine -- Patent 5,199,546, April 6, 1993.
Palatinit 0.4-0.5 -- -- (9) Bandelin, F.J. Compressed tablets by wet
granulation. In Pharmaceutical Dosage Forms:
Tablets; Lieberman, H.A., Lachman, L., Schwartz,
REFERENCES J.B.,, Eds.; Marcel Dekker, Inc.: New York, 1989; I,
(1). United States Pharmacopeia 24/National 160–164.
Formulary 19; United States Pharmacopeial
Convention, Inc.: Rockville; 1999. (10) Richards, R.M.; Xing, J.Z.; Mackay, K.M.
(2). Non-Prescription Drug Products: Formulations & Excipient interaction with cetylpyridinium chloride
Features; Knodel, L.C., Ed.; American activity in tablet based lozenges. Pharm. Res. 1996,
Pharmaceutical Association: Washington; 1998. 13 (8), 1258–1264.

INTERNATIONAL CONGRESS IN PHARMACY AND HEALTH SCIENCES

Pharma Science Tech Association, Foundation No: AP/PSTA/56/2012.
Please visit for Details: www.icphsmembership.com
Totally three types
FICPHS (Fellowship in International Congress in Pharmacy and Health Sciences), MICPHS (Member in International Congress in
Pharmacy and Health Sciences), AMICPHS (Associate Member in International Congress in Pharmacy And Health Sciences)

Eligibility
FICPHS: Ph.D in Chemistry/ Pharmacy / M.Sc / M.Pharm with 2 years experience, MICPHS: M.Sc / M.Pharm (or) B.Sc / B.Pharm with
2 years experience, AMICPHS: B.Sc (or) B.Pharmacy

JAPR /May 2014/ Vol. 5 /Issue 5 /290 – 298 298

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