This document summarizes a seminar presentation on taste masking methods in pharmaceutical formulations. It discusses factors to consider when selecting and developing taste masking technologies, including drug properties and dosage form requirements. Various taste masking approaches are described, such as using sweeteners and flavors, polymer coatings, inclusion complexes, ion exchange resins, solid dispersions, and microencapsulation. Evaluation techniques for taste masked formulations are also mentioned.
This power point presentation is about the Taste Masking Techniques. Among the various techniques, few of them are discussed here with the criteria and factors determining their selection. It will be useful for B.Pharm and M.Pharm students.
This power point presentation is about the Taste Masking Techniques. Among the various techniques, few of them are discussed here with the criteria and factors determining their selection. It will be useful for B.Pharm and M.Pharm students.
Directly Compresible Vehicle By Mr. Vishal ShelkeVishal Shelke
Directly Compresible Vehicle By Mr. Vishal Shelke
https://youtube.com/vishalshelke99
https://instagram.com/vishal_stagram
Introduction
These are the diluents or fillers designed to make up the required bulk of the tablets.
These are inactive ingredients that are added to tablets in addition to the active drug.
Some very common diluents in tablets include lactose and their derivatives, starch, cellulose derivatives.
Used in the direct compression of the tablets.
Requirements For A Good DCV :
Non-toxic and acceptable to the regulatory agencies.
Low cost.
Physiologically inert.
Must be color-compatible
Stability.
Controlled particle size.
Good flowability.
What is Direct compression ?
Direct compression (DC) is the tabletting of a blend of ingredients i.e. the compression mix, without a preliminary granulation or aggregation process.
The compression mix contains the active pharmaceutical ingredient (API) blended with one or more excipients.
The excipients may include binders, fillers/diluents, disintegrant and lubricants.
Advantages of DC :
More Economic compare to wet granulation since it requires fewer unit operations.
Documentation and validation requirements are reduced.
It requires less equipment, and space, time.
lower power consumpation , and less labor leading to reduce production cost of tablets.
More suitable for moisture and heat sensitive APIs, since it eliminates wetting and drying steps.
Lower microbial contamination
Faster drug release.
Disadvantages of DC :
Segregation because of the difference in the density of the API and excipients.
The dry state of the material during mixing may induce static charge and lead to segregation. due to this problems like weight variation and content uniformity may occur.
APIs that have poor flow properties and low bulk density is difficult to process by direct compression.
DC excipients are costly because these are prepared by spray drying, fluid bed drying, roller drying or co-crystallization.
Classification of DCV:
Disintegrants And Poor Flow:
ex. Microcrystalline cellulose , Starch.
Free-flowing Materials That Do Not Disintegrate :
ex. Dicalcium phosphate dihydrate.
Free-flowing Powders That Disintegrate By Dissolution:
ex. Lactoses,Sucrose, Dextrose Sorbitol , Mannitol
Co-processed exicipients :
ex. Ludipress
REFERENCES -
* Pharmaceutical dosage forms tablet Vol-II second edition lachman leon, lieberman H.A. Page.No 77-160.
* www.authorstream.com
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
The tablet compression process involves different steps of the rearrangement of particles within the die cavity and initial elimination of voids. It is very necessary for the academicians, students, production chemists, managers in the pharma background, to have the idea about the physics behind the tablet compression process.
Directly Compresible Vehicle By Mr. Vishal ShelkeVishal Shelke
Directly Compresible Vehicle By Mr. Vishal Shelke
https://youtube.com/vishalshelke99
https://instagram.com/vishal_stagram
Introduction
These are the diluents or fillers designed to make up the required bulk of the tablets.
These are inactive ingredients that are added to tablets in addition to the active drug.
Some very common diluents in tablets include lactose and their derivatives, starch, cellulose derivatives.
Used in the direct compression of the tablets.
Requirements For A Good DCV :
Non-toxic and acceptable to the regulatory agencies.
Low cost.
Physiologically inert.
Must be color-compatible
Stability.
Controlled particle size.
Good flowability.
What is Direct compression ?
Direct compression (DC) is the tabletting of a blend of ingredients i.e. the compression mix, without a preliminary granulation or aggregation process.
The compression mix contains the active pharmaceutical ingredient (API) blended with one or more excipients.
The excipients may include binders, fillers/diluents, disintegrant and lubricants.
Advantages of DC :
More Economic compare to wet granulation since it requires fewer unit operations.
Documentation and validation requirements are reduced.
It requires less equipment, and space, time.
lower power consumpation , and less labor leading to reduce production cost of tablets.
More suitable for moisture and heat sensitive APIs, since it eliminates wetting and drying steps.
Lower microbial contamination
Faster drug release.
Disadvantages of DC :
Segregation because of the difference in the density of the API and excipients.
The dry state of the material during mixing may induce static charge and lead to segregation. due to this problems like weight variation and content uniformity may occur.
APIs that have poor flow properties and low bulk density is difficult to process by direct compression.
DC excipients are costly because these are prepared by spray drying, fluid bed drying, roller drying or co-crystallization.
Classification of DCV:
Disintegrants And Poor Flow:
ex. Microcrystalline cellulose , Starch.
Free-flowing Materials That Do Not Disintegrate :
ex. Dicalcium phosphate dihydrate.
Free-flowing Powders That Disintegrate By Dissolution:
ex. Lactoses,Sucrose, Dextrose Sorbitol , Mannitol
Co-processed exicipients :
ex. Ludipress
REFERENCES -
* Pharmaceutical dosage forms tablet Vol-II second edition lachman leon, lieberman H.A. Page.No 77-160.
* www.authorstream.com
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
The tablet compression process involves different steps of the rearrangement of particles within the die cavity and initial elimination of voids. It is very necessary for the academicians, students, production chemists, managers in the pharma background, to have the idea about the physics behind the tablet compression process.
Pulsatile drug delivery are the system in which rapid & transient release of an active molecule within a short time period immediately after a predetermined off release period. i.e. lag time
The Pulsatile effect i.e. the release of drug as a “pulse” after a lag time has to be designed in such a way that complete and rapid drug release should follow the lag time. Such systems are also called time-controlled as the drug release is independent of the environment.
About two-thirds of all prescriptions are dispensed as solid dosage forms, and half of these are compressed tablets. A tablet can be formulated to deliver an accurate dosage to a specific site; it is usually taken orally, but can be administered sublingually, buccally, rectally or intravaginally. The tablet is just one of the many forms that an oral drug can take such as syrups, elixirs, suspensions, and emulsions. Medicinal tablets were originally made in the shape of a disk of whatever color their components determined, but are now made in many shapes and colors to help distinguish different medicines. Tablets are often stamped with symbols, letters, and numbers, which enable them to be identified. Sizes of tablets to be swallowed range from a few millimeters to about a centimeter. Some tablets are in the shape of capsules, and are called "caplets". Other products are manufactured in the form of tablets which are designed to dissolve or disintegrate; e.g. cleaning and deodorizing products.
Polysaccharide Based Drug Delivery System for Periodontitis-PPT.pptxVasundharaPatil12
Project aimed to develop a biocompatible In-situ gel for reducing inflammation caused due to Periodontitis and enhancing bioavailability of drug. Developed a biocompatible in-situ gel utilizing Tamarind Seed Polysaccharide (TSP) as the primary material and natural polymer.
Focused on enhancing gel adhesion to Periodontal tissues, reducing inflammation, and swelling associated with Periodontitis.
Conducted in-vitro studies to evaluate the effectiveness of the drug delivery system.
Demonstrated a 65% improvement in targeted drug delivery, indicating the efficacy of the developed formulation.
Formulation and evaluation of antifungal ketoconazole emulgelShwetaKate3
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Presentation by Gajanan S. Lahade
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Mask bitter aftertaste for a sweeter pill to swallow! Patients’ compliance and the therapeutic benefit are supported by a pleasant taste of pharmaceutical formulations. With the high intensity sweeteners Neotame and Sucralose, you have efficient tools at hand which are superior to other sweeteners in many aspects:
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Taste masking methods in pharmaceutical formulations
1. A
Seminar on
Taste Masking Methods in
Pharmaceutical Formulations
Presented by
Sagar B. Thoke
M. Pharm IInd Semester
[Dept. of Pharmaceutics]
Guided by
Prof . Y. P. Sharma
S.N.D. College of Pharmacy, Babhulgaon.
2. Introduction
Introduction
Factors Affecting Selection of Taste Masking Technology
Factors Consideration During The Taste-Masking Formulation
Process
Ideal Characteristics of Taste Masking Process & Formulation
Taste Masking Approaches
Evaluation Techniques
2
7/16/2012
3. Introduction
Need to Formulate Taste Masked Oral formulations.
Children, older persons-
Trouble swallowing tablets or capsules
Prefer liquid or sublingual/ Chewable solid
form dosage form
Undesirable taste-
Important formulation problems in case of Oral formulation
Patient compliance
3
7/16/2012
4. Anatomy & Physiology of Tongue
Vasculature
Lingual artery
Jugular vein
Nerve supply
Facial nerve CN VII
Glossopharyngeal nerve CN IX
Musculature Fig. Physiology of Taste Bud
Intrinsic
Extrinsic
Tongue physiology
Taste buds (taste cells)
Sense different tastes 4
7/16/2012
5. Four fundamental sensations of taste
Sweet and salty, mainly at the tip
Sour, at the sides
Bitter, at the back
fifth is Umami (2002)
Taste Signaling Pathways Fig. Taste Points in Tongue
1. Drug (tastant) binds with G-PCR in the cells
2. triggering the release the release of G-Protein (Gustducin)
5
7/16/2012
7. Factors Affecting Selection of Taste Masking
Technology
Conventional taste masking techniques alone are often
inadequate in masking the taste of highly bitter drugs such as
quinine, celecoxib.
Coating imperfections, reduce the efficiency of the technique.
Microencapsulation of potent bitter azithromycin is insufficient
to provide taste masking of liquid oral suspensions.
7
7/16/2012
8. Factors Consideration During The Taste-Masking
Formulation Process
1. Extent of the bitter taste of the API & Required dose load.
2. Drug particulate shape and size distribution.
3. Drug solubility and ionic characteristics.
4. Required disintegration and dissolution rate of the finished
product.
5. Desired bioavailability & release profile.
6. Required dosage form.
8
7/16/2012
9. Ideal Characteristics of Taste Masking Process & Formulation
It should
1. Involve least number of equipments and processing steps.
2. Effectively mask taste with as few excipients which are
economically and easily available.
3. No adverse effect on drug bioavailability.
4. Least manufacturing cost.
5. Can be carried out at room temperature.
6. Require excipients that have high margin of safety.
7. Rapid and easy to prepare. 9
7/16/2012
10. Taste Masking Approaches
Two approaches are commonly utilized
1. By reducing the solubility of drug in the pH of saliva
(5.6 - 6.8).
2. By altering the affinity and nature of drug which will
. interact with the taste receptor.
10
7/16/2012
11. Taste Masking Technologies
Taste masking patents and
patent applications are
contributed from
Asia-49.34%
North America- 41.45% of
which 62.67% were filed in
USA and
Europe- 9.30%.
Fig. Geographical distribution of taste masking patents &
patent application filed in the period of year 1997 to 2007. 11
7/16/2012
12. Fig. Taste masking technology filed in the period of
year 1997 to 2007.
12
7/16/2012
13. Fig. Taste Masking Technologies uses in liquid and solid dosage forms
13
7/16/2012
14. 1. Taste Masking with Sweeteners and Flavor's
Flavors
Natural Flavors-
Juices – Raspberry, Extracts – Liquorices, Tinctures – Ginger,
Spirits - Lemon & Orange, Syrups – Blackcurrant,
Aromatic waters - Anise & Cinnamon, Aromatic Oils –
Peppermint & Lemon.
Synthetic Flavors-
Alcoholic solutions, aqueous solutions, Powders.
Sweeteners
Complement flavors associated with sweetness
Soothing effect on the membranes of the throat
14
7/16/2012
16. 2. Polymer Coating of Drug
Coating acts as a physical barrier to the drug particles, by
minimizing interaction between the drug and taste buds.
Powders (50 mm) is fluidized by
heated, high-velocity air, and the
drug particles are coated with a
coating solution introduced from
the top as a spray through a
nozzle.
Nontoxic polymer that is
insoluble at pH 7.4 and soluble
at acidic pH are used.
chewable tablet of crystalline
ibuprofen and methacrylic acid
Fig. Coating process copolymer coating. 16
7/16/2012
17. 3. Formation of Inclusion Complexes
Complexation of guest molecule with host form a stable complex.
1. Decreasing its oral solubility or
2. Decreasing the amount of drug particles exposed to taste buds.
most suitable only for low dose drugs.
β-CD cyclic oligosaccharide obtained from starch.
Fig. Scanning electron micrograph of uncoated (bitter) and
coated (taste masked) paracetamol particles. 17
7/16/2012
18. 4. Ion Exchange Resin Complexes (IER)
IERs- high mole. weight polymers with cationic and anionic
functional groups.
Most drugs possess ionic sites in their molecule.
Drug-resin complex does not dissociate at salivary pH conditions.
Classification
Strong cation exchanger- sulphuric acid sites
Weak cation exchanger- carboxylic acid moieties
Strong anion exchanger- quaternary amine ionic sites
Weak anion exchanger- predominantly tertiary amine substituents
e.g. Indion 204, 234, 244, 254; Tulsion T-335, T- 339, T-334;
Amberlite IRC 50, IRP 69, IRP 88, IR 120; Dowex 50.
Not used- Amberlite IR400; Amberlite IR4B; Dowex 1;
Indion 454; Duolite AP143. 18
7/16/2012
19. 5. Solid Dispersion
One or more active ingredients Dispersed in an inert carrier or
matrix at solid state.
Carriers used- povidone, PEG, HPMC, urea, mannitol and
ethylcellulose.
Methods of Preparation
Melting method
Solvent method
Melting solvent method
Dimenhydrinate with polyvinyl acetate phthalate solid dispersion .
19
7/16/2012
20. 6. Microencapsulation
Thin coating to small particles of solids, droplets of liquids and
dispersions.
Reduce its solubility in saliva &
Act as physical barrier between drug and taste buds
Coating agents e.g.
• Gelatin, povidone, hydroxyethyl cellulose, ethyl cellulose,
bees wax, carnuba wax acrylics and shellac.
• water insoluble polymers- cellulose ethers, cellulose
ester, polyvinyl acetate and
• water soluble polymers- cellulose acetate
butyrate, PVP, hydroxyethyl cellulose.
Clarithromycin with combination of gelatine and acrylic resins
(Eudragit L-100, Eudragit S-100 & E-100). 20
7/16/2012
21. 7. Multiple Emulsions
API entrapped in internal phase of w/o/w or o/w/o emulsion.
w/o/w or o/w/o emulsion of chloroquine phosphate.
8. Development of Liposome
Liposomes- simple microscopic vesicles in which aqueous
volume (drug or biological agent) is entirely closed by a
membrane composed of lipid molecules.
lipid bilayers mainly composed of natural or synthetic
phospholipids.
e.g. phosphatidic acid, phosphatidylinositol, soy lecithin.
Chloroquine phosphate in HEPES (N-2-hydroxyetylpiperzine-N’-
2- ethane sulfonic acid) buffer was masked at pH 7.2. by
incorporating into egg phosphatidyl choline. 21
7/16/2012
22. 9. Prodrug Approach
Chemically modified inert drug precursor upon biotrans-
formation liberates the pharmacologically active parent
compound.
changing the molecular configuration of the parent molecule
taste receptor‐substrate adsorption constant may be modified.
Increase or decrease the aqueous solubility, mask bitterness,
increase lipophilicity, improve absorption, decrease local side
effects, and alter membrane permeability of the parent molecule.
Examples of Prodrugs with improved taste
Parent Drug Prodrug
Erythromycin Erythromycin Propionate
Clindamycin Clindamycin palmitate ester
22
Chloramphenicol Chloramphenicol palmitate ester 7/16/2012
23. 10. Taste Masking by Adsorption
Adsorbate of Drug are less saliva soluble versions of drugs.
Solution of the drug mix with an insoluble powder that will
absorb the drug, removing the solvent, dry it.
e.g. veegum, bentonite, silica gel and silicates.
Loperamide and phenyl propanolamine Suspension-
adsorbed on magnesium aluminium silicates (Veegum F).
11. Taste Masking with Lipophilic Vehicles like Lipids
and Lecithins
Oils, surfactants, polyalcohols, and lipids effectively increase the
viscosity in the mouth and coat the taste buds.
Talampicillin HCl- Magnesium aluminum silicate with soybean
lecithin. 23
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24. 12. Taste Suppressants and Potentiators
Suppressants (bitter taste blockers) compete with bitter
substances to bind with the G-protein coupled (GPCR) receptor
sites.
Not affecting taste due to the sugars, amino acids, salts or
acids.
Bitter substances (hydrophobic) contributes greatly to their
binding and inter-action with the receptor sites.
• Lipoproteins (phosphatidic acid and β-lactoglobulin)
• adenosine monophosphate
• Phospholipid (BMI-60)
• hydroxyl flavanones & γ-aminobutanoic acid
Mixture of cooling (e.g. eucalyptol) and warming agents (e.g.
methyl salicylate) was used for taste masking of thymol. 24
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25. Potentiators increase the perception of the taste of sweeteners.
• thaumatine,
• neohesperidine dihydrochalcone (NHDC) and
• glycyrrhizin
Increase the perception of sodium or calcium
saccharinates, saccharin, aspartyl-phenyl-alanine, cyclamates.
Desensitizing agents desensitize the taste buds by interfering
with taste transduction.
• phenols
• sodium phenolates
25
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26. 13. Taste masking by gelation
Water insoluble gelation on the surface of tablet containing
bitter drug .
Sodium alginate- form water insoluble gelation in presence of
bivalentmetal ions.
In presence of saliva, sodium alginate react with bivalent
calcium and form water insoluble gel and thus taste masking
achieved
Amiprolose hydrochloride tablet undercoat of sodium alginate
and overcoat of calcium gluconate.
26
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27. 14. Formation of salt and derivative
Salt formation decreasing the solubility of drug (less soluble in
saliva).
• N, N- dibenzyl ethylenediamine diacetate salts or
• N, N bis (deyhdroabiety) ethylene diamine salts is tasteless.
Ibuprofen water-soluble salts using alkaline metal bicarbonate
(sodium bicarbonate).
Aspirin tablets with magnesium salt of aspirin.
Sodium salts- sodium chloride, sodium acetate, sodium
gluconate
27
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28. 15. Use of Amino Acids and Protein Hydrolysates
Amino acids or their salts with bitter drugs.
• sarcosine,
• alanine,
• taurine,
• glutamic acid, and
• glycine.
Ampicillin taste improved by its granules with glycine and
additional quantity of glycine, sweeteners, flavors at final
compression step.
28
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29. 16. Miscellaneous
a) By effervescent agents
It comprises
chewing gum base
an orally administrable medicament
Taste masking generator of carbon dioxide
optionally a taste bud desensitizing composition e.g. oral
anaesthetics (benzocaine and spilanthol) and
other non active material, (sweeteners, flavours, and fillers).
Fentanyl and prochlorperazine effervescent tablets for
buccal, sublingual, and gingival absorption.
29
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30. b) Rheological modification
Rheological modifier (gums or carbohydrates)-
lower the diffusion of bitter substances from the saliva.
For administration of liquid preparation.
High viscosity induced by thickening agents
• PEG and
• sodium CMC
Acetaminophen suspension using xanthan gum (0.1‐0.2%) and
microcrystalline cellulose (0.6‐1%).
Mirtazapine (antidepressant) aqueous suspension using methonine
(stabilizer) and maltitol (thickening agent).
Terbutaline cough syrups given in doses of 4mg/5ml.
30
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31. c) Continuous multipurpose melt (CMT) technology
Continuous granulation and coating of API.
d) Wet Spherical Agglomeration (WSA)
Microencapsulation process combined with wet spherical
agglomeration (WSA).
E.g. Enoxacin taste masking.
31
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32. e) Freeze Drying Process
Used to develop FDT.
Zydis and Lyoc technology- drug is physically entrapped in
matrix composed of saccharide e.g. mannitol and a polymer.
piroxicam, loperamide, ondansetron, chlorpheniramine are
various drugs taste-masked by Zydis technology.
32
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33. Evaluation Techniques
Taste masking efficiency as
Quality control parameter and
Determining the rate of release of drug from taste-masked
complex.
Asses by
in vivo and
in vitro.
To quantitatively evaluate taste sensation, following methods
have been reported
a. Human Panel testing (human subjects)
b. Multichannel taste sensor/ magic tongue
c. Spectrophotometric evaluation/ D30’s value 33
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34. In vivo Evaluation
a. Human Panel testing (human subjects)
5‐10 healthy volunteers with organoleptic sense.
Taste evaluation using reference solutions ranging from
tasteless to very bitter.
Place the dosage form in mouth for 10 seconds.
Demands large panels and elaborate analysis.
raises safety and scheduling issues.
time consuming and expensive.
Two sensory analysis methods used-
Flavor Profile and
Profile Attribute Analysis
34
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35. Bitterness recorded against pure drug using a numerical scale.
seven point scale
1 = no bitterness,
2 = very slight bitterness,
3 = slight bitterness,
4 = slight to moderate bitterness,
5 = moderate bitterness,
6 = moderate to strong bitterness, and
7 = strong bitterness.
untrained taster would perceive an objectionable and/or
noticeable bitterness if the bitterness score is greater than or
equal to 3.
37
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36. In vitro Evaluation
b. Multichannel Taste Sensor / Magic tongue
automated taste sensing device to detect the magnitude of
bitterness.
“E-Tongue” electronic sensor array technology recognizes three
levels of biological taste including
1. receptor level (Taste buds in humans, probe membranes in
E-Tongue),
2. circuit level (neural transmission in humans, transducer in E-
. Tongue), and
3. Perceptual level (cognition in the thalamus humans, computer
. and statistical analysis in the E Tongue).
38
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37. Seven (7) sensors designated by Alpha MOS
ZZ, AB, BA, BB, CA, DA, and JE.
chemically modified sensors- field effect transistors (Chem
FET), similar to an ion selective FET but are coated with a
proprietary coating/membrane.
Ag/AgCl reference electrode
probes consist of a silicon transistor with proprietary organic
coatings.
measurement done potentiometrically.
taste profile and statistical software interprets the sensor data
into taste patterns.
39
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38. Reference electrode and sensors are dipped in a beaker
containing a test solution for 120 seconds.
40
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41. c. Spectrophotometric Method
known quantity of formulation mixed with 10 ml of distilled
water in 10 ml syringe by revolving the syringe, end to end;
five times in 30 seconds.
filtered through a membrane filter & spectrophotometric
determination of the concentration of the drug in the filtrate.
If this concentration is below the threshold concentration, it
may be concluded that the bitter taste would be masked in vivo.
Sparfloxacin granules, with threshold concentration being
100μg/ml.
Generally the taste evaluation involves
objective or analytical method and
subjective or hedonic method 44
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42. Conclusion
Taste masking of bitter drugs has been a challenge to the scientist.
There are numbers of technologies available, which effectively
mask the objectionable taste of drugs. Selection of technology
depends upon the bitterness of drugs and their compatibility with
taste masking agents that does not affect the bioavailability of
drug. With application of these techniques and proper evaluation
of taste masking effect one can improve product preference to a
large extent. Moreover, the development of taste masking
methodology requires great technical skill, and the need for
massive experimentation. 45
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43. References
1) Gupta A. K., Practical Approaches for Taste Masking of Bitter Drug: A Review,
International Journal of Drug Delivery Technology (April-June 2010), Vol. 2, Issue 2,
Page no.- 56-61.
2) S. B. Ahire, A Review: Taste Masking Techniques in Pharmaceuticals, An International
Journal of Pharmaceutical Sciences (2011), Page no.- 1645-1657.
3) Aditi Tripathi, Taste Masking: A Novel Approach for Bitter and Obnoxious Drugs,
Journal of Pharmaceutical Science and Bioscientific research (Nov-Dec 2011), Vol. 1,
Issue 3, Page no.- 136-142.
4) Vijay D. Wagh, Taste Masking Methods and Techniques in Oral Pharmaceuticals:
Current Perspectives, Journal of Pharmacy Research (2009), Vol. 2, Issue 6, Page no.-
1049-1054.
5) Vijay A. Agrawal, Taste Abatement Techniques to Inprove Palatability of Oral
Pharmaceuticals: A Review, International Journal of Pharma Research and Development
(Sep. 2010), Vol. 2, Issue 7, Page no.- 1-10. 46
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44. 6) Vinod M. Sonawane, An Update of Taste Masking Methods and Evaluation
Techniques, Scholars Research Library, Der Pharmacia Lettre (2010), Vol. 2, Issue 6,
Page no.- 1-15.
7) Sidharth Puri, Taste Masking: A Novel Approch For Bitter And Obnoxious Drugs,
International Journal of Biopharmaceutical & Toxicological Research (May 2011), Vol.
1, Issue 1, Page no.- 47-56.
8) J.K. Lorenz et al., Evaluation of a Taste Sensor Instrument (electronic tongue) for Use
In Formulation Development, International Journal of Pharmaceutics (2009), Page no.-
65–72.
9) K Gowthamarajan, Taste-Masking Technologies for Bitter Drugs, General Article
Resonance (December 2004), Page no.- 25-32.
10) Arvind K. Bansal, Trends in Pharmaceutical Taste Masking Technologies: A Patent
Review, Recent Patents on Drug Delivery & Formulation (2009), 3, Page no.- 26-39.
47
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45. 11) A. M. Suthar, Ion Exchange Resin As An Imposing Method For Taste Masking: a
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no.- 6-11.
12) Sanjay Daharwal, Taste Masking Method for Bitter Drug and Tasteless Dispersible
Tablet: An Overview, Page no.- 1-9.
13) Rajesh Agrawal, Cyclodextrins – A Review on Pharmaceutical Application for Drug
Delivery, International Journal of Pharmaceutical Frontier Research (Jan-Mar 2012), Vol.
2, Issue 1, Page no.- 95-112.
14) K.P. Sampath Kumar, Taste Masked Suspension, www.thepharmajournal.com
(2012), Vol. 1 No. 2, Page no.- 1-6.
15) S. T. Birhade, Preparation and Evaluation of Cyclodextrin Based Binary Systems for
Taste Masking, International Journal of Pharmaceutical Sciences and Drug Research
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16) Inderbir SINGH, Scientific Review Ion Exchange Resins: Drug Delivery and
Therapeutic Applications, FABAD J. Pharm. Sci. (2007), 32, Page no.- 91-100. 48
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