WHAT IS TASTE Four main taste perceptions salt
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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
Chemical Physical • Complexation • Pro-drug • Less soluble derivative • Precipitation • Emulsion • Viscous vehicle Physiological • Anaesthetic action • Effervescence • Cooling effect BRIJESH PATEL Masking & Blendin g 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 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 BRIJESH PATEL 7
FDA approved Non-Nutritive 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 composition may be incorporated into much number of pharmaceutical formulations, including chewable tablet, effervescent tablets, BRIJESH PATEL powder, and liquid dispersion etc. 9
3. 1. Coating Polymers � Eudragit E 100, is finding fairly broad utility in tastemasking 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. � Water-soluble polymers such as HPMC may be used PATEL to decrease barrier. BRIJESH properties of taste-masking 10
3. 2 Meltable Coatings Hydrogenated vegetable oils, Vegetable waxes BRIJESH PATEL Saturated fatty acids such as stearic acid 11
3. 3. Coating of Drug Particles � Powders as fine as 50 micron are fluidized in an expansion chamber by means of heated, highvelocity 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 (povidone) of various molecular methylcellulose, weights, hydroxyl gelatin, methylcellulose, BRIJESH PATEL 12
3. 4. Camouflage Technology Polymeric taste masking � � process � Simple to use � Cost effective � � Colorless � Tasteless, taste masking � � Sugar free � High drug loading � Dissolves rapidly Non-systemic absorption of polymer Enhances stability Used in approved products BRIJESH PATEL 13
� � 3. 5. Microencapsulation Uses various coating agents, such as gelatin, povidone, HEC, 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, � pan coating, solvent evaporation � multi-orifice centrifugation techniques. � It has been reported that the bitter taste of PATEL 14 paracetamol was BRIJESHcompletely masked on
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™ AP 143. � Drugs with anionic functionality (-NH 2, HCl salts etc. ) AMBERLITE™ IRP 64. 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. � Bitter taste of ibuprofen has been effectively masked by BRIJESH PATEL cyclodextrin. 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 completely masked by the formation of a molecular complex of caffeine BRIJESH PATEL and gentisic acid in 1: 1 and 1: 2 molar ratios. 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 of solid dispersion are described below. Melting method: Solvent method: BRIJESH PATEL 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. � D-chlorpheniramine maleate is a taste-masked salt of chlorpheniramine. 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 improved markedly by preparing its granules with glycine and mixing them with additional quantity of glycine, sweeteners, flavors BRIJESH PATEL 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 tasting medicines. 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 formulation. BRIJESH PATEL 25
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 tasteassessment requires Trained taste panel and sophisticated interpretation. E- Tongue E- Nose Olfactory Gas Chromatography In vitro cell Cultures 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 formulations. 5. Serving a quality control function for flavored product and excipient. BRIJESH PATEL 32
Use of Electronic Nose to Optimize Flavor Profile Company that commercially produce e-nose : Alpha M. O. S. (De. Motte, IN), Aroma. Scan (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 simulated brain consisting of a computer BRIJESH PATEL 33 and sophisticated software.
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 to describe our perception of stimuli. BRIJESH PATEL 34
Olfactory Gas Chromatographic Technique � Olfactory GC techniques permitted the division of identified volatiles into odor-active and non-odoractive. � 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
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Applications of particle coating 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 BRIJESH PATEL 37
Cont… Dispersibility Hydrophilic/Hydrophobic Properties Electrostatic/Electric/Magnetic/Optic al Characteristics Achieve sphericity Solid Phase reactivity BRIJESH PATEL 38
Various Particles Coating Techniques BRIJESH PATEL 39
Microencapsulation v Versatile for individual particles coating v The type and level of membrane applied is determined by release rate requirements, organoleptic features and the dosage form application. v Microcaps particles can be incorporated into different dosage forms including fast melt tablets, sachets, sprinkles and reconstitutable and temporary suspensions. BRIJESH PATEL 40
Spray Drying Inexpensive methods for coating particles. Suspension is spray dried BRIJESH PATEL 41
Spray drying systems Open spray drying system Aseptic spray drying system Closed spray drying system Semi-closed spray drying system BRIJESH PATEL 42
Fluid bed coating techniques v It is used to dry the wet products, agglomerate particles, improve flow properties, produce coated particles for controlled release or taste masking v Ease of scale up BRIJESH 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 BRIJESH PATEL Arm head Scraper 50
Hybridizer BRIJESH PATEL 51
Theta Composer Capacity : 40 cc ; Powder occupied Volume : 20 % Outside Vessel : 30 rpm ; Rotor : 500 ~ 3000 rpm 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) Guest Collar coil 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) 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 BRIJESH PATEL 56
“ The greatest discovery of our generation is that a human being can alter his life by altering his attitude of mind “ k n a h T BRIJESH PATEL 57
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