TASTE MASKING & PARTICLES COATING WHAT IS TASTE ? Four main taste perceptions: salt, sour, bitter, and sweet. Two other perceptions (umami and trigeminal). Umami is derived from the presence of glutamate, such as monosodium glutamate, resulting in the

fullness sensation. Trigeminal is the burning sensation derived from such foods as spices and peppers. BRIJESH PATEL 2 FACTORS AFFECTING THE PERCEPTION OF BITTERNESS Taste Interactions. Medium of Presentation. Viscosity. Temperature. Taste Modifiers. Salivary Status. Age.

BRIJESH PATEL 3 METHODS OF IMPROVING THE PALATABILITY Chemical Physical Complexatio n Pro-drug Less soluble derivative Precipitation Emulsion Viscous vehicle

Physiological Anaesthetic action Effervescence Cooling effect BRIJESH PATEL Maski ng & Blendi ng 4 Techniques Employed

for Taste Masking BRIJESH PATEL 5 1 -Use of Flavours & Sweeteners Natural Flavours

Juices - Raspberry Extracts - Liquorice Spirits - Lemon & Orange Syrups - Blackcurrant Tinctures - Ginger Aromatic waters - Anise & Cinnamon Oils - Lemon & Orange Synthetic Flavours Alcoholic solutions Aqueous solutions Powders BRIJESH PATEL 6 2 - Use of sweeteners

Natural Sucrose, glucose, fructose mannitol, glycerol Sweeten Sorbitol, Honey, liquorice er Artificial sweeten er Advanta ge of Artificial Sweeten

Saccharin, saccharin sodium Aspartame Intense sweetener Sugar free preparation Enhance degree of sweetness Disadvantage bitter or metallic aftertaste BRIJESH PATEL 7 FDA approved NonNutritive Sweeteners Asparatame

Sucralose Neotame BRIJESH PATEL Saccharin 8 3 - Applying polymers Coating of drugs using a suitable polymer offer an excellent method of concealing the drug from the taste buds.

The coated incorporated pharmaceutical composition into much may be number

of formulations, BRIJESH PATEL including 9 3. 1. Coating Polymers Eudragit E100, is finding fairly broad utility in taste-masking drugs when a rapid release is needed. Neutral polymers like methacrylate copolymers,

ethyl cellulose or cellulose acetate butyrate, Eudragit RS can also provide sufficient time delay for use in taste-masking. BRIJESH PATEL 10 3.2 Meltable Coatings BRIJESH PATEL

11 3.3. Coating of Drug Particles 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. Taste-masking of Ibuprofen has been successfully achieved

by this technique to form microcapsules. Starches, polyvinyl pyrrolidones BRIJESH PATEL 12

3.4. Camouflage Technology Polymeric taste High drug masking process Simple to use Cost effective Colorless Tasteless, taste masking Sugar free

BRIJESH PATEL loading Dissolves rapidly Non-systemic absorption of polymer Enhances stability Used in approved products 13

Microencapsula Uses various coating agents, such as tion 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, air suspension, coacervation -phase separation, spray drying and congealing, BRIJESH PATEL pan coating, solvent evaporation

14 3.6. Complexation with ion exchange resins The adsorption of bitter drugs onto synthetic ion exchange resins to achieve taste coverage has been well documented. Extreme bitterness of quinolones has been achieved by ion

exchange resin such as methacrylic acid polymer cross linked with di-vinyl benzene. Drugs with cationic functionality (e.g. -COOH or Na / K salts) DUOLITE AP143. BRIJESH PATEL 15 3.7. Inclusion complex with cyclodextrins

Cyclodextrin is the most widely used complexing agent for inclusion complex formation which is capable of masking the bitter taste of the drug. By decreasing the

amount of drug particles exposed to taste buds there by reducing its perception of bitter taste. BRIJESH PATEL 16 3.8. Taste Masking by Ionic Interaction For this technology, two combinations are possible: using an anionic drug and a cationic polymer, or a cationic drug together with an anionic polymer.

BRIJESH PATEL 17 3.10. Pelletization 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). BRIJESH PATEL 19 3.11. Molecular Complexes of Drugs

The solubility and absorption of drugs can be modified by the formation of molecular complexes. Lowering drug solubility through molecular complexation can decrease the intensity of bitterness. The bitterness of caffeine was BRIJESH PATEL completely masked by the formation of a 20

3.12. Solid Dispersions 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. HPMC, mannitol and ethylcellulose. Approaches for

preparation dispersion are described below. Melting method: BRIJESH PATEL of solid 21 3.13. Formation of Salts or Derivatives 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. Aspirin tablets can be rendered tasteless by making magnesium salt of aspirin. BRIJESH PATEL 22

3.14. Use of Amino Acids 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 markedly by preparing BRIJESH PATEL its

improved granules 23 3.15. Taste-masking by Viscosity Modifications Increasing the viscosity with thickening agents can lower the diffusion of bitter substances from the saliva to the taste buds. This provides a taste masked liquid preparation for administration of a relatively large amount of unpleasant BRIJESH PATEL

24 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 BRIJESH PATEL 25 formulation. 3.18 Multiple emulsions Another novel technique employing multiple emulsions has also been reported. By dissolving drug in the inner aqueous phase of w/o/w emulsion In one of the method drugs with bitter taste

are combined with nonionic surfactants to form composites by hydrophobic interactions resulting in taste masking. BRIJESH PATEL 26 3.18. Freeze drying process

Various drugs have been taste masked by zydis technology. This includes the drugs like lorazepam, piroxicam, loperamide, ondansantron, rizatriptan, loratadine, olanzapine, selegiline etc. BRIJESH PATEL 27 Oralance technology

The Oralance technology efficiently hides the taste of the most difficult molecules even formulated in aqueous media BRIJESH PATEL 28 Evaluation of Taste Masking Effect BRIJESH PATEL 29 4.1. Pharmaceutical taste-assessment

requires BRIJESH PATEL 30 4.2. How does e-tongue works ? 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 BRIJESH PATEL Probe membranes Transducer Computer and statistical analysis E-tongue

31 Key benefit of e- tongue evaluation 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 BRIJESH PATEL 32 Use of Electronic Nose to Optimize Flavor Profile Company that commercially produce e-nose : Alpha M.O.S. (DeMotte, IN), AromaScan (Hollis, NH), and Neotronics (Gainesville, GA). Human nose: 10,000 odor sensors (nonspecific)

but can be very sensitive to certain odors. Signals from human olfactory sensors are transmitted to the brain for processing. The brain then interprets what the sum of all these signals is describing in terms of odor. Electronic Nose instruments attempt to do the same with many fewer sensors and a BRIJESH PATEL

33 Use of Cell Cultures & Receptors Cloning of receptor proteins, individual receptors or the whole sensory organ may produce detection systems with similar function to the human sensory organs. However, it will be necessary to deconvolute the signals obtained from these systems to convert them into terms typically used toBRIJESH describe our PATEL

34 Olfactory Gas Chromatographic Technique Olfactory GC techniques permitted the division of identified volatiles into odoractive and non-odor-active. 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 BRIJESH PATEL

35 PARTICLES COATING BRIJESH PATEL 36 Applications of particle coating BRIJESH PATEL 37 Cont BRIJESH PATEL 38

Various Particles Coating Techniques BRIJESH PATEL 39 Microencapsulation 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

BRIJESH PATEL 40 Spray Drying BRIJESH PATEL 41 Spray drying systems Open spray drying system Closed spray drying system Aseptic spray drying system Semi-closed spray drying system

BRIJESH PATEL 42 Fluid bed coating techniques 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 upBRIJESH PATEL 43 CLosed system

Open system Batch fluid bed system BRIJESH PATEL 44 Bottom spray coater BRIJESH PATEL 45 Wuster coater :- industry recognized coating for precision application of film coat to particulate material like powder, crystal, granule BRIJESH PATEL 46

Thin Precision coating technique for fine powders BRIJESH PATEL 47 Dry Particle coating Equipments HIGH INTENSITY MACHINES : Hybridizer Mechanofusion Theta Composer FLUIDIZATION BASED DEVICES : Magnetically Assisted Impaction Coating ( MAIC)

Rotating Fluidized Bed coater ( RFBC) BRIJESH PATEL 48 DRY PARTICLE COATING Mechanical Forces Guest particle Discrete coating Continuous coating Host particle BRIJESH PATEL 49

Mechanofusion Use high mechanical force between the fixed arm head and rotating chamber Wall for embedding guest particles onto host particles. Rotating Chamber BRIJESHhead PATEL Arm Scraper 50 Hybridizer

BRIJESH PATEL 51 Theta Composer 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

BRIJESH PATEL 52 Rotating Fluidized bed coater BRIJESH PATEL 53 Vertical Rotating Fluidized bed coater BRIJESH PATEL 54 Magnetically Assisted Impact Coating (MAIC) Collar coil

Guest Host N-S Oscillating magnetic field S-N AC Power supply Guest Particle Chamber Magnetic particle Host particle BRIJESH PATEL

55 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) 137148. 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 (23) (2001) 159167. 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 Coaters 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 BRIJESH PATEL 56 The greatest discovery of our generation is that a human being can alter his life by altering his attitude of mind BRIJESH PATEL a h T 57

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