Transcript Slide 1

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Four main taste perceptions: salt, sour, bitter, and sweet.
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Two other perceptions (umami and trigeminal).
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Umami is derived from the presence of glutamate, such as
monosodium glutamate, resulting in the fullness sensation.
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Trigeminal is the burning sensation derived from such foods
as spices and peppers.
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Taste Interactions.
Medium of Presentation.
Viscosity.
Temperature.
Taste Modifiers.
Salivary Status.
Age.
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Chemical
Physical
• Complexation
• Pro-drug
• Less soluble
derivative
• Precipitation
• Emulsion
• Viscous vehicle
Physiological
• Anaesthetic action
• Effervescence
• Cooling effect
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Masking
&
Blending
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Natural Flavours
• Juices - Raspberry
• Extracts - Liquorice
• Spirits - Lemon & Orange
• Syrups - Blackcurrant
• Tinctures - Ginger
• Aromatic waters - Anise & Cinnamon
• Oils - Lemon & Orange
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Synthetic Flavours
• Alcoholic solutions
• Aqueous solutions
• Powders
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Natural
Sweetener
• • Sucrose, glucose, fructose
• • Sorbitol, mannitol, glycerol
• • Honey, liquorice
Artificial
sweetener
• • Saccharin, saccharin sodium
• • Aspartame
Advantage
of Artificial
Sweetener
• • Intense sweetener
• • Sugar free preparation
• • Enhance degree of sweetness
• • Disadvantage – bitter or metallic aftertaste
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Asparatame
Sucralose
Neotame
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Saccharin
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Coating of drugs using a suitable polymer offer an excellent
method of concealing the drug from the taste buds.
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The coated composition may be incorporated into much
number of pharmaceutical formulations, including chewable
tablet, effervescent tablets, powder, and liquid dispersion etc.
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Eudragit E100, is finding fairly broad utility in tastemasking drugs when a rapid release is needed.
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Neutral polymers like methacrylate copolymers, ethyl
cellulose or cellulose acetate butyrate, Eudragit RS can also
provide sufficient time delay for use in taste-masking.
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Water-soluble polymers such as HPMC may be used to
decrease barrier properties of taste-masking coatings.
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Hydrogenated
vegetable oils,
Vegetable
waxes
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Saturated fatty
acids such as
stearic acid
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Powders as fine as 50 micron are fluidized in an
expansion chamber by means of heated, high-velocity
air, and the drug particles are coated with a coating
solution introduced usually from the top as a spray
through a nozzle.
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Taste-masking of Ibuprofen has been successfully
achieved by this technique to form microcapsules.
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Starches, polyvinyl pyrrolidones (povidone) of various
molecular weights, gelatin, methylcellulose, hydroxyl
methylcellulose, microcrystalline cellulose and ethyl
cellulose.
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Polymeric taste masking
process
Simple to use
Cost effective
Colorless
Tasteless, taste masking
Sugar free
High drug loading
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Dissolves rapidly
Non-systemic absorption of
polymer
Enhances stability
Used in approved products
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Uses various coating agents, such as gelatin, povidone, HEC,
EC, bees wax, carnuba wax and shellac.
Bitter-tasting drugs can be first encapsulated to produce free
flowing microcapsules, which are then blended with other
excipients and compressed into tablets.
Microencapsulation also increases the stability of the drug and
release pattern can be modified .
It can be accomplished by a variety of methods,
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air suspension,
coacervation -phase separation,
spray drying and congealing,
pan coating, solvent evaporation
multi-orifice centrifugation techniques.
It has been reported that the bitter taste of paracetamol was
completely masked on microencapsulation using cellulose-wax
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combination.
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The adsorption of bitter drugs onto synthetic ion exchange resins to
achieve taste coverage has been well documented.
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Extreme bitterness of quinolones has been achieved by ion exchange resin
such as methacrylic acid polymer cross linked with di-vinyl benzene.
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Drugs with cationic functionality (e.g. -COOH or Na / K salts)
DUOLITE™ AP143.
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Drugs
with
anionic
functionality
(-NH2,
HCl
salts
etc.)
AMBERLITE™ IRP64.
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Cyclodextrin is the most widely
used complexing agent for
inclusion complex formation
which is capable of masking the
bitter taste of the drug.
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By decreasing the amount of drug
particles exposed to taste buds there
by reducing its perception of bitter
taste.
Bitter taste of ibuprofen has
been effectively masked by
cyclodextrin.
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For this technology, two combinations are possible: using an
anionic drug and a cationic polymer, or a cationic drug
together with an anionic polymer.
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Taste masking is achieved when the bitter value (short: BV) is decreased three
times by the power of ten.
BV is determined as the reciprocal drug concentration that tastes slightly
unpleasant (according to German Pharmacopeias DAB 10).
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The solubility and absorption of drugs can be modified by
the formation of molecular complexes.
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Lowering drug solubility through molecular complexation
can decrease the intensity of bitterness.
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The bitterness of caffeine was completely masked by the
formation of a molecular complex of caffeine and gentisic
acid in 1:1 and 1:2 molar ratios.
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They are dispersions of one or more active ingredient in an
inert carrier or matrix in solid state, and insoluble or bland
matrices may be used to mask the taste of bitter drugs.
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HPMC, mannitol and ethylcellulose.
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Approaches for preparation of solid dispersion are described
below.
 Melting method:
 Solvent method:
 Melting-solvent method:
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In this approach, an attempt is made to modify the chemical
composition of the drug substance itself, so as to render it
less soluble in saliva and thus make it less sensitive to the
taste buds.
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Aspirin tablets can be rendered tasteless by making
magnesium salt of aspirin.
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D-chlorpheniramine maleate is a taste-masked salt of
chlorpheniramine.
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By combining amino acids or their salts with bitter drugs, it
is possible to substantially reduce the bitterness.
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Some of the preferred amino acids include sarcosine, alanine,
taurine, glutamic acid, and glycine.
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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 tablets.
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Increasing the viscosity with thickening agents can
lower the diffusion of bitter substances from the saliva
to the taste buds.
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This provides a taste masked liquid preparation for
administration of a relatively large amount of
unpleasant tasting medicines.
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3.16. Incorporation of drugs into vesicles or liposomes
 Incorporation of drugs into vesicles or liposomes
is although an ideal technique, yet a challenge to
formulate without altering the regulatory status of
the product
3.17. Anesthetizing agent
 Anesthetizing
agent like sodium phenolate,
which numb the taste buds sufficiently within 4-5
seconds is helpful in inhibiting the perception of
bitter taste of the formulation.
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3.18 Multiple emulsions
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Another novel technique employing multiple emulsions has
also been reported.
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By dissolving drug in the inner aqueous phase of w/o/w
emulsion
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In one of the method drugs with bitter taste are combined
with nonionic surfactants to form composites by hydrophobic
interactions resulting in taste masking.
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3.18. Freeze drying process
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Various drugs have been taste masked by zydis technology.
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This includes the drugs like lorazepam, piroxicam,
loperamide,
ondansantron,
rizatriptan,
loratadine,
olanzapine, selegiline etc.
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The Oralance ® technology efficiently hides the taste of
the most difficult molecules even formulated in aqueous
media
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Trained taste panel and
sophisticated interpretation.
E- Tongue
E- Nose
Olfactory Gas Chromatography
In vitro cell Cultures
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The e- tongue mirrors the three levels of biological taste recogination:
Taste buds
Neural
transmission
Cognition in
the thalamus
Human Tongue
The
Receptor
level
The
Circuit
level
The
Perceptual
level
Probe
membranes
Transducer
Computer and
statistical analysis
E-tongue
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1.
Help to quantify bitterness of drug actives when limited basic
taste information is available, especially if the drug supply is
limited.
2.
Developing suitable matching bitter placebos for blinded
clinical testing
3.
Conduct comparator studies (Benchmark analysis)
4.
Developing optimized taste- masked formulations.
5.
Serving a quality control function for flavored product and
excipient.
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Company that commercially produce e-nose :
Alpha M.O.S. (DeMotte, IN),
AromaScan (Hollis, NH), and
Neotronics (Gainesville, GA).
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Human nose: 10,000 odor sensors (nonspecific) but can be very sensitive
to certain odors.
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Signals from human olfactory sensors are transmitted to the brain for
processing.
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The brain then interprets what the sum of all these signals is describing
in terms of odor.
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Electronic Nose instruments attempt to do the same with many fewer
sensors and a simulated brain consisting of a computer and
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sophisticated software.
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Cloning of receptor proteins, individual receptors or the whole
sensory organ may produce detection systems with similar
function to the human sensory organs.
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However, it will be necessary to deconvolute the signals
obtained from these systems to convert them into terms
typically used to describe our perception of stimuli.
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
Olfactory GC techniques permitted the division of identified
volatiles into odor-active and non-odor-active.
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Deal with measurements of volatile release in the mouth by a
novel nose sampler and oral vapor GC. These useful tools clarify
the effects of breathing, chewing, and saliva flow on flavor
release
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Modification of particles to mask flavors, odor
& color
Modification of reactivity, solubility and
wetting properties
Taste masking with modified release
Separation of incompatibilities
Conversion of liquids to solids
Sustained release
Flowability
Partice size distribution
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Cont…
Dispersibility
Hydrophilic/Hydrophobic
Properties
Electrostatic/Electric/Magnetic/Op
tical Characteristics
Achieve sphericity
Solid Phase reactivity
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 Versatile for individual particles coating
 The type and level of membrane applied is determined by
release rate requirements, organoleptic features and the dosage
form application.
 Microcaps particles can be incorporated into different dosage
forms including fast melt tablets, sachets, sprinkles and
reconstitutable and temporary suspensions.
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Inexpensive
methods for
coating particles.
Suspension is
spray dried
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Open spray drying system
Aseptic spray drying system
Closed spray drying system
Semi-closed spray drying system
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 It is used to dry the wet products, agglomerate particles,
improve flow properties, produce coated particles for
controlled release or taste masking
 Ease of scale up
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CLosed system
Open system
Batch fluid bed system
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Bottom spray coater
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Wuster coater :- industry recognized coating for
precision application of film coat to particulate
material like powder, crystal, granule
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Thin Precision coating technique for fine powders
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
HIGH INTENSITY MACHINES :
 Hybridizer
 Mechanofusion
 Theta Composer
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FLUIDIZATION BASED DEVICES :
 Magnetically Assisted Impaction Coating ( MAIC)
 Rotating Fluidized Bed coater ( RFBC)
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Mechanical Forces
Guest particle
Discrete coating
Continuous coating
Host particle
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Use high mechanical force between the fixed arm head and
rotating chamber Wall for embedding guest particles onto
host particles.
Rotating
Chamber
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Arm head
Scraper
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Capacity : 40cc ;
Powder occupied Volume : 20 %
Outside Vessel : 30 rpm ;
Rotor : 500 ~ 3000rpm
Slow revolution of outside vessel:
Promotion of favourable bulk mixing
High speed rotation of inside rotor :
high shear stress required for coating.
Elliptical Shape:
Stress & relaxation
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Rotating Fluidized bed coater
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Vertical Rotating Fluidized bed coater
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Guest
Collar coil
Host
N-S
Oscillating
magnetic
field
S-N
AC Power supply
Guest Particle
Chamber
Magnetic particle
Host particle BRIJESH PATEL
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References
1. Michelle Ramlakhan, C.-Y. Wu, Satoru Watano, R.N. Dave, Robert Pfeffer,
Dry particle coating using magnetically assisted impaction coatings:
modification of surface properties and optimization of system operating
parameters, Powder Technology 112 (2000) 137–148.
2. P. Singh, T.K.S. Solanky, R. Mudryy, R. Pfeffer, R.N. Dave, Estimation of
coating time in the magnetically assisted impaction coating process,
Powder Technology 121 (2–3) (2001) 159–167.
3. Nethersole, Douglas C.; Dudley, Michael A.; Parthasarathy, Mellapalayam 4.
R.; United States Patent 4069792
Rodriguez L, Albertini B, Passerini N, Cavallari C, Giovannelli L. Hot air
coating technique as a novel method to produce microparticles. Drug Dev
Ind Pharm. 2004; 30(9):913-23.
5. Powder Coater’s Manual 1/98
6. www. biophan - nanotechwire_com - the online resource for nano
technology and research
7. www. ventilex.htm
8. www. caleva.co.uk
9. www. coating place.inc.htm
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“ The greatest discovery of our generation is that a human
being can alter his life by altering his attitude of mind “
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