Poonam et al - Galaxy of Pharmaceutical Innovations

Transcription

Poonam et al - Galaxy of Pharmaceutical Innovations
Poonam et al
Review article
Galaxy of Pharmaceutical Innovations
(Journal for Pharmaceutical Innovators)
Home page: www.gopionline.com
Volume 1, Issue 1, February-March 2015
Taste masking technology for pharmaceutical dosage forms: a review
Poonam Mandawat
Dept. of Pharmaceutics, Shrinathji institute of Pharmacy, Nathdwara, Rajasthan-313301
*
E-mail: [email protected]
ARTICLE INFO
ABSTRACT
Article History
Received 17 March 2015
Revised 23 March 2015
Accepted 27 March 2015
Keywords
Taste
Oral
Mask
Approaches
Pharmaceutical, nutraceutical, nutritional, and other active
materials typically have an objectionable taste which
creates challenges for some forms of oral delivery. If it is
confined to a tablet or capsule that is swallowed whole, the
material can pass the taste buds without significant
detection. When the material is formulated as a chewable
tablet, a fast-dissolve lozenge or film, solution or
suspension, objectionable taste is often the primary cause of
patient non-compliance with a dosing requirement. The
present review article provides different approaches for
masking the taste of bitter taste drugs.
INTRODUCTION
Taste is one of the most important parameters
governing patient compliance. Undesirable
taste is one of several important formulation
problems that are encountered with certain
drugs. Oral administration of bitter drugs with
an acceptable degree of palatability is a key
issue for health care providers, especially for
pediatric
patients.
Several
oral
pharmaceuticals, numerous food and beverage
products, and bulking agents have unpleasant,
bitter-tasting
components.
So,
any
pharmaceutical formulation with a pleasing
taste would definitely be preferred over a
competitor's product and would translate into
better compliance and therapeutic value for the
patient and more business and profits for the
company.
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The desire of improved palatability in these
products has prompted the development of
numerous formulations with improved
performance and acceptability1
Sense of taste
Taste, or gustatory perception, is one of our
basic senses. It tells us from early childhood
what is edible and what is not, what is good
for our body and what can be potentially
dangerous. Taking into account how important
the sense of taste is for us, it is surprising how
little we know about the underlying
neurological mechanisms that produce the
sensation of taste2.
Different Types of taste
Scientists describe seven basic tastes: bitter,
salty, sour, astringent, sweet, pungent (eg
chili), and umami. There are however five
basic tastes that the tongue is sensitive to: salt,
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sweet, bitter, sour, and umami, the taste of
MSG. Umami is a Japanese word meaning
"savory" or "meaty" and thus applies to the
sensation of savoriness -- specifically, to the
detection of glutamates, which are especially
common in meats, cheese and other proteinheavy foods. The action of umami receptors
explains why foods treated with monosodium
glutamate often taste fuller or just better3.
PHYSIOLOGY OF TASTE
The sense of taste is mediated by taste receptor
cells which are bundled in clusters called taste
buds. Taste receptor cells sample oral
concentrations of a large number of small
molecules and report a sensation of taste to
centers in the brainstem. Taste buds are
composed of groups of between 50 and 150
columnar taste receptor cells bundled together
like a cluster of bananas. The taste receptor
cells within a bud are arranged such that their
tips form a small taste pore, and through this
pore extend microvilli from the taste cells. The
microvilli of the taste cells bear taste
receptors4.
The sense of taste affords an animal the ability
to evaluate what it eats and drinks. At the most
basic level, this evaluation is to promote
ingestion of nutritious substances and prevent
consumption of potential poisons or toxins.
There is no doubt that animals, including
humans, develop taste preferences. That is,
they will choose certain types of food in
preference to others. Interestingly, taste
preference often changes in conjunction with
body needs. Taste Receptor Cells, Taste Buds
and Taste Nerves
TASTE MASKING TECHNOLOGY
Taste masking is defined as a perceived
reduction of an undesirable taste that would
otherwise exist. The ideal solution to reduce or
inhibit bitterness is the discovery of a
universal inhibitor of all bitter tasting
substances that does not affect the other taste
modalities such as sweetness or saltiness. Two
comprehensive reviews to control bitter taste
have already been presented along with
thoughts on the discovery of a universal
bitterness inhibitor5,6
An appreciable amount of success has been
achieved in the development of bitterless,
tasteless, and taste‐masked formulations in
recent years. Various techniques available for
masking bitter taste of drugs include taste
masking with ingredients such as flavors,
sweeteners, and amino acids; taste masking by
polymer
coating;
taste
masking
by
conventional granulation; taste masking with
ion‐exchange resins; taste masking by spray
congealing with lipids; taste masking by
formation of inclusion complexes with
cyclodextrins; taste masking by the
freeze‐drying process; taste masking by
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making multiple emulsions; and taste masking
with gelatin, gelatinized starch, liposomes,
lecithins
or
lecithin‐like
substances,
surfactants, salts, or polymeric membranes7.
Selection of Taste Masking Technique
Appropriate selection of a taste masking
technique is a must for developing a palatable
and economical formulation. For instance, a
drug that is extremely bitter cannot be taste
masked with sweeteners or flavorants alone,
and intermediary techniques like coating or
matrix entrapment should be used. An ionic
drug can be taste masked with ion exchange
resins. A lipophilic drug can be taste masked
by entrapping it into a lipoidal matrix.
Although variations are possible, in general
simple techniques are more economical as
compared to intermediary ones.
Ideal Taste Masking Process


Involve least number of equipments
and processing steps.
Require
minimum
number
of
excipients
for
an
optimum
formulation.
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





No
adverse
effect
on
drug
bioavailability.
Require excipients that are economical
and easily available.
Least manufacturing cost.
Can be carried out at room
temperature.
Require excipients that have high
margin of safety
Rapid and easy to prepare8
Factors That Are Taken Into
Consideration during the TasteMasking Formulation Process
Extent of the Bitter Taste of the API
With aggressively bad tasting medicaments
even a little exposure is sufficient to perceive
the bad taste. For example, sweeteners could
not achieve taste masking of oral formulation
of ibuprofen due to its dominating taste.
Coating is more efficient technology for
aggressively bitter drugs even though coating
imperfections, if present, reduce the efficiency
of the technique9.
Similarly, microencapsulation of potent bitter
active agents such as azithromycin is
insufficient to provide taste masking of liquid
oral suspensions10.Conventional taste masking
techniques such as the use of sweeteners,
amino acids and flavoring agents alone are
often inadequate in masking the taste of highly
bitter drugs such as quinine, antibiotics like
levofloxacin,
ofloxacin,
sparfloxacin,
ciprofloxacin, cefuroxime axetil, erythromycin
and clarithromycin11.
Required dose load
Dose of a drug may dictate whether a
particular formulation strategy would be
suitable to achieve taste masking. In paediatric
formulations, the dose is small enough so as to
allow the usage of flavouring agents to mask
the taste of the medicine. For example, low
dose palatable paediatric aspirin oral
formulation was developed by adding
sweeteners, but the same approach failed to
address the problem of drugs like
acetaminophen because of its high dose. In
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such cases, coating is preferred to achieve taste
masking along with sweeteners to attain an
acceptable final dosage form size 12 .
Drug particulate
distribution
shape
and
size
Particle characteristics of the drug would
affect the taste masking process efficiency.
Core materials with irregular shapes and small
particle size lead to poor taste masking
efficiency and varying dissolution of coated
particles. Fines, abrasion and variable coating
thickness can lead to situations wherein the
taste mask coating is compromised. Multilayer
coating using inner spacing layer to sequester
the drug from taste masking layer helps to
reduce
or
eliminate
such
coating
imperfections. Taste masked granules of
gatifloxacin and dextromethorphan were
formulated by multilayer coating consisting of
inner spacing layer followed by outer taste
masking layer.13
Drug solubility
Physicochemical properties of the drug play an
important role in the selection of taste masking
technology. For example, ondansetron has a
relatively lower water solubility at higher pH,
based on which a rapidly disintegrating taste
masked composition of ondansetron was
formulated by adding an alkalizing
agent(sodium bicarbonate) to reduce the water
solubility and the consequent taste perception14
Ionic characteristics of the drug
Ionic characteristics of drugs govern the
selection of ion exchange resin polymers and
the suitability of the drug candidate for this
technology. For example, anionic polymers
(e.g. alginic acid) are good candidates for
cationic drugs like donepezil hydrochloride,
and the cationic polymers are choice of
excipients for anionic drugs like sildenafil15,16
Required dosage form
It is estimated that 50% of the population have
problem of swallowing tablets, especially the
paediatric and geriatric population. Chewable
tablets and liquid oral dosage forms have been
used to address these problems. However, it is
difficult to formulate some drugs in these
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dosage forms due to their poor palatability. For
formulations which are swallowed unchewed:
capsules, coated tablets and slowly
disintegrating hard tablets have been used as
.
preferred
taste
masking
technologies.
Chewable tablets and liquid oral formulations
are preferable in case of large dose drugs for
an ease of intake17,18
DIFFERENT
TASTE
TECHNOLOGY
flavors for masking the taste of ammonium
chloride and other saline drugs has also been
established. The various imitation flavor
concentrates used are grape, maple, raspberry,
and wild cherry, etc. These have been
compared to some of the official flavored
syrups and recognized as good masking agents
for saline drugs24.
Flavors
Natural Flavors
 Juices – Raspberry
 Extracts – Liquorices
 Spirits - Lemon & Orange
 Syrups – Blackcurrant
 Tinctures –Ginger
 Aromatic waters - Anise & Cinnamon
 Aromatic Oils – Peppermint &
Lemon.
Synthetic Flavors
 Alcoholic solutions
 Aqueous solutions
 Powders
Sweetners
 Complement flavors associated with
sweetness
 Soothing effect on the membranes of
the throat
Natural Sweetener
 Sucrose, glucose, fructose
 Sorbitol, mannitol, glycerol
 Honey, liquorice
Artificial Sweetener
 Saccharin, Saccharin sodium
 Aspartame
 Nutritive: Sucrose, Fructose and
Glucos
 Polyols: Mannitol, Sorbitol, Xylitol,
Erythritol, Maltitol.
 Non-Nutritive: Aspartame, Sucralose,
Neotame and Saccharin24
MASKING
Taste
Masking
with
Sweeteners, and Amino Acids
Flavors,
This technique is the foremost and the simplest
approach for taste masking, especially in the
case of pediatric formulations, chewable
tablets, and liquid formulations. But this
approach is not very successful for highly
bitter and highly water soluble drugs. Artificial
sweeteners and flavors are generally being
used along with other taste‐masking
techniques to improve the efficiency of these
techniques. Numerous pharmaceuticals such as
dentifrices and mouthwashes applied to the
oral
cavity
elicit
unpleasant
taste
perceptions19. The unpleasant taste of certain
formulations like mouthwashes and cough
drops containing medicinal and bitter tasting
substances such as eucalyptus oil can be
masked by adding fenchone, borneol, or
isoborneol. These taste masking agents
significantly suppress the perception of
unpleasant organoleptic sensations of the
volatile oil20. The cooling effect of the taste
masking agents also aids in reducing the
bitterness. Sweetening compositions of
di‐D‐fructofuranose 1,2′: 2,3′‐di‐anhydride are
also useful for dentifrices, mouthwashes, and
foods. Menthol reduces the bitter taste, and
low‐calorie formulations show beneficial
anticaries effects21. Nonbitter dentifrices are
prepared by sweetening benzethonium
chloride with stevia‐based sweetener extract
and glycerin. It exhibits 100% bactericidal
activity against E. coli22. Anethole and
menthofuran in various dentifrices are not only
used to mask the bitterness but also to improve
the low temperature stability of the
formulation23. The use of some imitation
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Taste masking by microencapsulation
It is important to understand that only soluble
portion of the drug can generate the sensation
of taste. And it is possible, or even likely, that
coating the active drug with a properly
selected polymer film can reduce its solubility
in saliva in thus taste could be masked.Coating
the drug particles created a physical barrier
between the drug and the taste buds and this
taste of active could be masked.
Microencapsulation is a process by which very
tiny droplets or particles of liquid or solid
material are surrounded or coated with film or
polymeric material25.
Taste
masking
complexation
by
inclusion
In inclusion complex formation,the drug
molecule fits into the cavity of a complexin
agent ,i.e. the host molecule,forming a stable
complex. The complexing agent is capable of
masking the bitter taste of drug by either
decreasing its oral solubility on ingestion or
decreasing the amount of drug particles
exposed to taste buds, thereby reducing the
perception of bitter taste. This method is most
suitable only for low dose drugs. Vander Walls
forces are mainly involved in inclusion
complexes. β-cyclodextrin is the most widely
used complexing agent for inclusion type
complexes. It is a sweet, non-toxic, cyclic
oligosaccharide obtained from starch. The
strong bitter taste of carbetapentane citrate
syrup was reduced to approximately 50% by
preparing a 1:1 complex with cyclodextrin1.
Palatable ibuprofen solutions are prepared by
forming a 1:11 to 1:15 inclusion complex with
Ibuprofen and hydroxy propyl Bcyclodextrin,
respectively.
Taste Masking by
Hydrophilic Vehicles
Coating
with
This is the simplest and most feasible option to
achieve taste masking. The coating acts as a
physical barrier to the drug particles, thereby
minimizing interaction between the drug and
taste buds. Coating of chewable tablets
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provides excellent taste masking while still
providing acceptable bioavailability. A
specialized technique, i.e., micro emulsion
technology, has been used for taste masking of
powders, chewable tablets, and liquid
suspensions.
Taste Masking By Granulation
Granulation is a less expensive, rapid
operation and an easily scalable taste masking
technology. This step can be exploited as a
mean for taste masking of slightly bitter
tasting drug. Granulation lowers the effective
surface area of the bitter substance that come
in contact with the tongue upon oral intake.
Liquid and low melting point waxes such as
glycerol palmitostearate, glyceryl behenate
and hydrogenated castor oil are commonly
used ingredients during the granulation to
achieve taste masking.26
Taste masking by ion exchange resins
Based on Complexation of drugs with ion
exchange resins. Ion exchange resins are water
insoluble, cross linked high molecular weight
polyelectrolytes containing salt forming
groups in repeating position on the polymer
chain which exchange their mobile ion of
equal charge with the drug molecule. As taste
perception of bitter drugs is experienced in the
mouth at taste buds, complexed drugs resinate
does not release drug in mouth due of scarcity
of exchangeable ions (at pH 6.7) in the saliva
and when complex comes in contact with GIT
fluids (at acidic pH),complex is broken down
quickly and drug is release. Resins being
polyelectrolyte have extensive binding sites
leading to very high drug loading ability Ion
exchange resins have received considerable
attention because of their versatile properties
as drug delivery vehicles, chemically inert and
free from local and systematic side effects
possess long-term safety even while ingesting
large doses and also compatible with all
conventional solid, semisolid and liquid
dosage forms.
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Use of Amino Acids And Protein
Hydrates
By combining amino acids or their salts with
bitter drugs, it is possible to substantially
reduce the bitterness. Some of the preferred
amino acids include sarcosine, alanine, taurine,
glutamic acid, and glycine. The taste of
ampicillin improved markedly by preparing its
granules with glycine and mixing them with
additional quantity of glycine, sweeteners,
flavors and finally compressing them into
tablets27.
Taste masking by bitterness inhibitors
The development of a specific universal
inhibitor for bitter taste has been widely
required in the fields of taste physiology and
pharmaceutical sciences, but no such inhibitors
has been available.One difficulty in
discovering of universal inhibitor for bitter
taste is that substances that inhibits bitterness
of one compound will not influence the
bitterness of a second because many different
classes of compound impart bitterness. Sodium
salts such as sodium chloride, sodium acetate,
sodium gluconate have been shown to be
potent inhibitors of some bitter compounds.
The mechanism is not known, however,
research shows that sodium act at peripheral
taste level rather than a cognitive effect. Bitter
substances are commonly hydrophobic in
nature hence lipoprotein (PA?LG) composed
of phophatidic acid and β lactoglobulin can
mask the target sites for bitter substances on
the taste receptor membrane without affecting
responses to salts, acids, sugars or sweet
amino acids.28.
Viscosity modification
Enhancement of viscosity in liquid
formulations by thickening agents such as
natural gums or carbohydrates can mask the
unpleasant taste of drug by formulating a
covering layer on the tongue and act as barrier
between drug particles and taste buds, thus
lowering the diffusion of drug from saliva into
the taste buds13. For viscosity enhancement in
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liquid formulations, polyethylene glycols and
carboxy methylcellulose are induced which
not only increases the stability of liquid
formulation but surprisingly, provides taste
masking of unpleasant tasting medicines. For
examples, in cough syrups, terbutaline given in
doses of 4mg/5ml can be effectively
administered by increasing the viscosity of the
formulation29.
Taste masking by prodrug approach
Chemical modification, including prodrug
design is an effective method for reducing
solubility, and thereby improving taste. A
prodrug is chemically modified inert drug
precursor which upon biotransformation
liberates the pharmaceutically active parent
compound. Bitterness of a molecule may be
due to the efficiency of the taste receptor
substrate adsorption reaction, which is related
to the molecular geometry of the substrate. If
alteration of the parent molecule occurs by
derivative formation, the geometry is altered,
affecting the adsorption constant. Thus the
magnitude of a bitter taste response or taste
receptor-substrate adsorption constant may be
modified by changing the molecular
configuration of the parent molecule. The
extremely bitter antibiotics have been the
focus of much work in reversible drug
modification30.
Taste masking by gelation
Water insoluble gelation on the surface of
tablet containing bitter drug can be used for
taste masking. Sodium alginate has the ability
to cause water insoluble gelation in presence
of bivalent metal ions. Tablet of amiprolose
hydrochloride have been taste masked by
applying a undercoat of sodium alginate and
overcoat of calcium gluconate. In presence of
saliva, sodium alginate reacts with bivalent
calcium and form water insoluble gel and thus
taste masking achieved31.
Development of liposome
Another way of masking the unpleasant taste
of therapeutic agent is to entrap them into
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liposome. For example, incorporating into a
liposomal formulation prepared with egg
phosphatidyl choline masked the bitter taste of
chloroquine phosphate in HEPES (N-2hydroxyetylpiperzine-N‟- 2- ethane sulfonic
acid) buffer at pH 7.232.
solubility
through
molecular
complex
formation can decrease the intensity of
bitterness of drug Higuchi and Pitman,
reported that caffeine forms complexes with
organic acids that are less soluble than xanthan
and as such can be used to decrease the bitter
taste of caffeine35
Taste masking by adsorption
Adsorbates are commonly used in taste
masking technologies. Adsorbate of bitter
tasting drug can be considered as the less
saliva soluble versions of these drugs.
Adsorption involves preparing a solution of
the drug and mixing it with an insoluble
powder that will adsorb the drug, removing the
solvent, drying the resultant powder, and then
using these dried adsorbates in the preparation
of the final dosage form. Many substrates like
veegum, bentonite, silica gel and silicates can
be used for the reparation of adsorbate of bitter
drugs.The bitter taste of ranitidine is masked
by forming an adsorbate with a synthetic
cation exchange resin33.
Use of multiple emulsion
A novel technique of taste masking of drug
employing multiple emulsions. The w/o/w or
o/w/o type multiple emulsion are vesicular
systems in which active ingredients can be
entrapped in internal phase. The entrapped
substances can be transferred from internal
phase to external phase through the membrane
phase. This phase controls the release of drug
from system. These system could be used for
controlled-release delivery of pharmaceuticals.
If the system is stable enough for a reasonable
shelf life, the formulation could also mask the
taste of drug. Both w/o/w or o/w/o multiple
emulsion of chloroquine phosphate have been
prepared and reported to be partially effective
in masking the bitter taste of drug34.
Molecular complexes of drug with other
chemicals
The solubility and adsorption of drug can be
modified by formation of molecular
complexes. Consequently lowering drug
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Mass extrusion method
This technology involves softening the active
blend using the solvent mixture of watersoluble polyethylene glycol, using methanol
and expulsion of softened mass through the
extruder or syringe to get a cylinder of the
product into even segments using heated blade
to form tablets.The dried cylinder can also be
used to coat granules of bitter tasting drugs
and thereby masking their bitter taste36.
Use of salts or derivatives
In this approach, an attempt is made to modify
the chemical composition of the drug
substance itself, so as to the taste buds. Aspirin
tablets can be rendered tasteless by making
magnesium
salt
of
aspirin.
Dchlorpheniramine maleate is taste-masked salt
of chlorpheniramine. The alkyloxy alkyl
Carbonates of Clarithromycin have remarkably
viated bitterness and improved bioavailability
when administered[65]. Sodium salts such as
sodium chloride, sodium acetate, sodium
gluconate have been shown to be potent
inhibitors of some bitter compound. The
mechanism is not known, however, research
shows that sodium act at peripheral taste level
rather than a cognitive effect 37
Use of desensitizing agents
Desensitizing agents like phenols, sodium
phenolates desensitize the taste buds by
interfering with taste transduction the process
by which taste message from the mouth to the
brain and thus mask the taste of drug.38
Wet spherical agglomeration (WSA)
Technique
(CMT)
and Continuous Multipurpose
Technology.
A
novel
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microencapsulation process combined with the
wet spherical agglomeration (WSA) technique
was used to mask the bitter taste of enoxacin.
The microcapsules prepared were bioequivalent to the commercial Enoxacin 100
mg tablets in beagle dogs. The CMT method
was developed for the continuous granulation
and coating of pharmacologically active
substances. It was concluded that this method
could be successfully applied for taste masking
of bitter drugs39
pH modifiers
Many natural and synthetic polymers, resins
and waxes alone or in combination have been
employed for taste masking. The enteric
polymers like eudragit L are used for taste
masking but the pH of saliva is near 5.8 and
these polymers solubilize at pH beyond 5.5 so
there is a possibility of drug being partially
leached. Therefore there is a need for the
development of taste masking polymer such
that the bitter taste is completely masked by
the polymer at the pH of saliva in mouth and
in the reconstitution medium as in case of the
liquid orals and further which is able to protect
the drug in a biologically active form, from the
moisture in the dosage form and releasing the
drug rapidly in the stomach without affecting
its absorption and bioavailability.40.
Miscellaneous taste masking approaches
by effervescent agents
Effervescent agents have been shown to be
useful
and
advantageous
for
oral
administration of drugs and have been
employed for use as taste masking agents for
dosage forms that are not dissolved in water
prior to administration. A chewing gum
composition of bitter medicament was
formulated to supply the medicament to oral
cavity for local application or for buccal
absorption. It comprise a chewing base, an
CONCLUSION
Taste masking of bitter drugs has significantly
improved the quality of treatment provided to
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orally administrable medicament, a taste
masking generator of carbon dioxide, and
optionally a taste bud desensitizing
composition (e.g., oral anesthetic such as
benzocaine) and other non active material such
as sweeteners, flavoring components, and
fillers.Recently, effervescent tablets of
fentanyl and prochlorperazine were developed
to supply these drugs to the oral cavity for
buccal, sublingual, and gingival absorption.
The formulation contains the drug in
combination with effervescent agent to
promote their absorption in the oral cavity and
to mask their bitter taste. An additional pH
adjusting substance was also included in
fentanyl formulation for further promotion for
absorption 41.
Rheological modification
Increasing the viscosity with rheological
modifier such as gums or carbohydrates can
lower the diffusion of bitter substances from
the saliva to the taste buds. Acetaminophen
suspension can be formulated with xanthan
gum (0.1?0.2%) and microcrystalline cellulose
(0.6?1%) to reduce bitter taste. The
antidepressant drug mirtazapine is formulated
as an aqueous suspension using methonine
(stabilizer) and maltitol (thickening agent).
Maltitol is stable in the acidic pH range of 2 to
3 and besides masking the unpleasant taste of
the drug, it also inhibit its undesirable local
anesthetic effect 42
Continuous multipurpose melt (cmt)
technology
The cmt method was developed for the
continuous granulation and coating of
pharmacologically active substances. It was
concluded. That this method could be
succesfully applied for taste masking of bitter
drugs43
suffering patients, especially children. The
word „medicine‟ for a child is synonymous
with bad taste. Oral pharmaceuticals have been
GOPI, Vol 1(1) feb-mar 2015
Poonam et al
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continually adapted for making their “bitter
taste better”, especially to the pediatric and the
geriatric consumers. There are so many
effective techniques and methodologies that
are constantly being researched and developed
in the pharmaceutical field in response to the
need of taste masking. Applicability of all
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these approaches varies from drug to drug and
depends on the type of dosage form required.
The ideal solution to bitterness reduction or
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