ISSN: Pathan et al., World Journal of Pharmacy 2015; 3(2): S. K. CHAKRAVATI, J. K. PATHAN, S. MALVIYA, A. KHARIA, N. KHAN, S.

Transcription

1 ISSN: Pathan et al., World Journal of Pharmacy 2015; 3(2): PROCESSING TECHNOLOGY FOR PHARMACEUTICAL EXCIPIENTS BASED ON TABLET: A REVIEW S. K. CHAKRAVATI, J. K. PATHAN, S. MALVIYA, A. KHARIA, N. KHAN, S. VYAS

2 Research Article World Journal of Publisher Research & Review World Journal Of Pharmacy PROCESSING TECHNOLOGY FOR PHARMACEUTICAL EXCIPIENTS BASED ON TABLET: A REVIEW Sudhanshu K Chakravati1, *Javed Khan Pathan1, Sapna Malviya1, Anil Kharia1, Neelam Khan2, Savita Vyas3 1.Modern Institute of Pharmaceutical Sciences, Indore 2.RKDF College of Pharmacy, Indore 3.MGM Medical College, Indore Corresponding Author: J. K. Pathan, Mobile No. :+91- Received on 01 June, 2015; Revised on 05 June, 2015; Accepted on ABSTRACT The aim of study was made to a review an Excipients substance mixed with a medicine to give it consistent and play an important role in formulating a dosage form. These are the ingredients which along with Active Pharmaceutical Ingredients make up the dosage forms. Excipients act as protective agents, bulking agents and can also be used to improve bioavailability of drugs in some instances, the following review discusses the various types and with their uses, and these can be used for different activities. Specific excipients are best suited for a particular dosage form; the selection criterion for excipients and various interactions that an excipient can undergo during its course of stay in formulation has been discussed in this review. A tablet is a compressed solid dosage form containing medicaments with or without exponents. Pharmaceutical oral solid dosage forms have been used widely for decades mainly due to their convenience of administration and suitability for delivery of drugs for systemic effects. Tablet may be defined as solid pharmaceutical form containing drug substances with or without suitable diluents and prepared by either compression or molding method. Molding tablet and compressed tablet can be further World Journal of Publisher 473 Available Online at

3 classified as directly compressible tablet, chewable tablet and controlled release tablet (osmotic tablet, bilayer tablet, matrix tablet, floating tablet). Keywords: Types of Excipients and tablet, Selection of Excipients in tablet, Excipients with concentration INTRODUCTION: The formulation of a drug substance frequently involves it being blended with different excipients to improve manufacturability, and to maximize the product s ability to administer the drug dose effectively. Excipients are known to facilitate administration and modulate release of the active component [1].Selection of appropriate excipients for formulation of drug substances is vitally important in ensuring final product stability and efficacy. As formulation scientists, it is imperative that we develop pharmaceutical products that have acceptable chemical and physical stability during the time period of their distribution, storage, and use. It is not uncommon that an API (active pharmaceutical ingredient) will be stable as a bulk drug but unstable when blended with the excipients required for formulation of dosage forms. Therefore, understanding the reactivity of the API in the solid state when mixed with excipients is critical to commercial formulation development [2]. With the increasing interest in polymers of natural origin, the pharmaceutical world has compliance to use most of them in their formulations. Pharmaceutical formulation development involves various components in addition to the active pharmaceutical ingredients. The plant derived gums and mucilages comply with many requirements of pharmaceutical excipients as they are nontoxic, stable, easily available, associated with less regulatory issues as compared to their synthetic counterpart and inexpensive; also these can be easily modified to meet the specific need. Most of these plant derived gums and mucilages are hydrophilic and gelforming in nature. The traditional concept of the excipients as any component other than the active substance has undergone a substantial evolution from an inert and cheap vehicle to an essential constituent of the formulation [3].These components are generally termed as excipients and according to the international pharmaceutical excipient council, Excipient is defined as Any substance other than active drug or pro-drug World Journal of Publisher 474 Available Online at

4 that is included in the manufacturing process or is contained in finished pharmaceutical dosage forms [4]. The US pharmacopoeia- National formulary (USPNF) categorizes excipients according to the functions they perform in the formulations e.g. Binders, disintegrants etc. Excipients can be classified on the basis of their origin, use in dosage form, and functions they perform as follows [5]. Excipients is a used as a means of its administration [12] TABLET (6, 7 ) Tablet may be defined as solid pharmaceutical dosage form containing medicament with or without suitable excipients and prepared either by compression or moulding. Classification of Tablet Based on the route of administration or the function, the tablets are classified as follows Tablets ingested orally a) Standard compressed tablet b) Multiple compressed tablet c) Layered tablet d) Osmotic tablet e) Compressed coated tablet f) Repeat action tablet g) Delayed action and enteric coated tablet h) Sugar and chocolate coated tablet i) Film coated tablet j) Chewable tablet k) Targeted tablet Floating tablet Colon targeted tablet Tablets used in the oral cavity a) Buccal tablet b) Sublingual tablet c) Troches and Lozenges d) Dental cones e) Mouth dissolving tablet 1.2. EXCIPIENT [8] Pharmaceutical excipients can be defined as non-active ingredients that are mixed with therapeutically active compound to form medicines. The ingredient which is not an active compound is regarded as an excipient.the formulation of a drug substance frequently involves it being blended with different excipients to improve manufacturability, and to maximize the product s ability to administer the drug dose effectively. Excipients are known to facilitate administration and modulate release of the active component. They can also stabilize it against degradation from the environment. Classification of Excipients [5, 9, 10, 13] Diluents World Journal of Publisher 475 Available Online at

5 Diluents are components that are incorporated into tablet or capsule dosage forms to increase dosage form volume or weight. Sometimes referred to as fillers, diluents often comprise a significant proportion of the dosage from, and the quantity and type of diluents selected often depends on its physical and chemical properties. Because the diluents may comprise a large portion of the dosage from, successful manufacturing and dosage from performance depend on the measurement and control of these critical attributes. Example:- Calcium carbonate, Dicalcium anhydrous, Lactose spray process, Mannitol, Microcrystalline, Sorbitol, Starch, Sucrose Binders Binders are incorporated into formulations to facilitate the agglomeration of powder into granule during mixing with a granulating fluid such as water, hydroalcoholic mixture, or other solvents. Example:-Hypromellose (hpmc), Povidone, Pregelatinized starch Disintegrants They are employed in tablet formulation to facilitate the breakdown of the tablet into granules when it come in contact with GIT fluid. In case of enteric coated tablet or controlled release tablets disintegrantes are an essential formulation component, enabling tablet disintegration to occur within the specifications defined I the various pharmacopoeias (typically disintegration of conventional tablets must occur within 15 minutes). Example:- Alginic acid, Crospovidone, Microcrystalline celluse, Pregelatinized starch, Sodium croscarmellose, Sodium starch glycolate, Starch Lubricants They are typically used to reduce the fictional forces between particles and metal contact surfaces of manufacturing equipment such as tablet punches and dies used in the manufacture of solid dosage forms. Example:- Magnesium stearate, Calcium stearate, Stearic acid, Sodium steryl fumerate, Polyethylene glycol, Sodium laury sulfate, Starch Glidant and Anticaking Agents They are used to promote power flow and to reduce the caking or clumping that can occur when powders are stored in bulk. Example:-Colloidal silicon dioxide, Calcium silicate, Magnesium silicate, Talc Solubilizing Agents The solubility of a drug that is normally insoluble or poorly soluble in water can World Journal of Publisher 476 Available Online at

6 often is improved by addition of a surfaceactive agent Example:-Sodium lauryl sulfate, Docusate sodium, Lecithin, Poloxamer, Polysorbate Coating Agents Reasons for coating pharmaceutical drug delivery system include masking unpleasant tastes ordors, improving ingestion, improving appearance, protecting active ingredient from the environment, controlling the rate of release of the active ingredient and controlling drug release in the gastrointestinal tract. Example:-Hypromellose, Ethylcellulose, Methylcellulose, Ammonio methacrylate copolymer, Sucrose Drug release modifying agents An ideal dosage resimen in the drug therapy of any disease is the one which immediately attains the desired therapeutic concentration of drugin plasma and maintains it constant for the entire duration of treatment. Example:-Hypromellose, Hydroxypropyl methylcellulose acetate succinate, Ethylcelluse acetate phthalate, Methacrylic acid copolymer, Polymethylcelluse, Polyvinylchloride, Polyvinyllacetate 2.0 SELECTION OF EXCIPIENT IN TABLET 2.1. Excipient based on Excipients use in preparation of tablet [4,5] 2.2. Excipient based on used in the manufacture of tablet [10] 2.3. Excipient based on Excipients use in method of tablet [5, 11] Wet granulation The wet granulation technique uses the same preparatory and finishing step (careening or milling, and mixing) as the two previously discussed granulation techniques. The unique portion of wet granulation process involved the wet massing of the powders, wet sizing or milling, and drying. The theory, equipment, methods associated with drying and compression DRY GRANUATION When tablet ingredient are sensitive to moisture and/or unable to withstand elevated temperature during drying and when the tablet ingredient have insufficient cohesive properties slugging may b used to form granules. This method is referred to as dry granulation. This technique I used in preparation of aspirin, aspirin combination acetophenetidin enlisted the execipients used in dry granulation. 2.5DIRECT COMPRESSION The manufacture of tablets using wet granulation or dry granulation method World Journal of Publisher 477 Available Online at

7 requires series of unit operations both time consuming and potentially costly A potentially more attractive option for the manufacture of tablets involves powder mixing and subsequent compression of the powder mix, thereby obviating the need for granulation (and related unit operations) This process is termed direct compression the mechanisms of particle-particle interactions in tablets produced by direct compression are similar to those operative in tablets produced by dry granulation and roller compaction. Enlisted the execipients used in direct granulation. 3.0 EXCIPIENT BASED ON IT S USE IN COLORING AGENTS OF TABLET They are incorporated into dosage form in order to produce a distinctive appearance that may serve to different a particular formulation from others that have a similar physical appearance. These substances are subdivided into dyes (water soluble substances) lakes insoluble form of a dye that result from its irreversible adsorption onto a hydrou metal oxide). Inorganic pigments (substances such as titanium dioxide or iron oxides), and natural colorants (colored compounds not considered as dye such as riboflavin). In the Federal Food, Drug, and Cosmetic Act of 1938, three categories of coloring agents were created: 4.0 EXCIPIENT BASED ON IT S USE IN COATING MATERIAL OF TABLET 5.0 CONCLUSION Excipients being an indispensible component of medicinal products must be evaluated for their safety and stability. The various excipent interactions like drug- excipient interactions, excipient-excipient interactions and package- excipient interactions may render the excipient harmful for use in formulation. In order to avoid the use of incompatible excipients and to assure that that the excipients are safe and stable for use in the designing of the formulation, various stability testing procedures are carried out where the excipients are subjected to extreme conditions of temperature, humidity etc. if the stability testing data is in favor of the use of excipient in formulation the excipients are further tested for assuring safety, which is the most important feature of any formulation intended to be used in humans or animals. As new excipients emerge, it s important to recognize their potential use in various complex delivery systems, and the IPEC procedure subjects new excipients for potential use in humans to World Journal of Publisher 478 Available Online at

8 a thorough safety assessment. The safety assurance of excipients helps the formulator to design an effective and safe dosage form with the use of efficient and safe excipients, thus for an excipient to be in a formulation it must be highly stable, safe and efficacious, and above all it must comply with the expected performance in the formulation. 6.0 ACKNOWLEDGEMENT I offer my sincere & graceful gratitude to the Modern Institute of Pharmaceutical Sciences, to provide the healthy environment for research. In my daily work I have been get helping hands of my colligues. I am grateful to get such an enthusiastic environment. 7.0 REFERENCES 1. Sonali S. Bharate, Sandip B. Bharate, Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review, J. Excipients and Food Chem., 2010; 1 (3),pp Kumar Pragati B., Sahu Kiran Ravi, K.V.Ramana Murthy, Subba Rao,.B.Ramu, A Review on Mechanism, Importance and Methods of Compatibility Testing in the Formulation of Dosage Forms, Journal of Chemical and Pharmaceutical sciences, 2011; Volume 4, pp Dharmendra. S, Surendra K J, Natural Excipients- A Review, International Journal of Pharmaceutical & Biological Archives, 2012; 3(5), pp Chaudhari P Shilpa, Pharmaceutical Excipients: A review, International Journal of Advances in Pharmacy, Biology and Chemistry, 2012; Volume 1(1). 5. Goutam Rath, Amit K Goyal, Suresh P. Vyas, Hand book of pharmaceutical dosage form, 1st ed, Delhi; Vallabh Prakashan, 2011; pp Haur Harbir, Processing technology for pharmaceutical tablets, International Research Journal of Pharmacy, 3(7), pp S.P. Vyas, V. Sihorkar,V. Mishra, Controlled and targeted drug delivery strategies towards intraperiodontal pocket diseases, Journal of Clinical Pharmacy and therapeutics,2000, 25 (1), pp Bharate, Sonali S, Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review, IPEC- Americas Inc, Sinko J Patrick, Martin s Physical Pharmacy and Pharmaceutical Sciences, World Journal of Publisher 479 Available Online at

9 South Asian Edition, India; Published By Wolters Kluwer Pvt Ltd, 2011, pp Goutam Rath, Amit K. Goyal and Suresh P. Vyas, Hand book of pharmaceutical dosage form, 1st ed., Delhi; Vallabh Prakashan : 2011,pp Lachman Leon, Lieberman A Herbert. The theory and practice of industrial pharmacy, 4th ed., Bombay; Varghese publishing house: 1991, pp The chamber dictionary, New Delhi; Allie Chamber Limited: 1996, pp Brahankar M D, Jaiswal B Sunil, Biopharmaceutics and Pharmacokinetics a treatise, 2nd ed., Delhi; Vallabh Prakashan: 2009, pp World Journal of Publisher 480 Available Online at

10 Table 1: Mechanism Physical properties with examples in preparation of tablet Excipients Functions Examples Diluent To act as a bulking agent or filling material Sugars, lactoe, mannitol, orbital, sucroe Inorganic salts primarily calcium salts Polysaccharided, Binders and To hold powder together to Sugars, glucose, syrup, polymers, natural adhesives form granules for tableting gums, starch, gelatin or synthetic celluloses polyvinylpyrrolpyrrolidone (PVP) poly-methycrylate (EudragitTM) Glidants To improve the flow of granule from the hopper to the die cavity to ensure uniform fill for each tablet Disintegrants To facilitate the breakup of a tablet in the gastrointestinal tract Lubricants To reduce the friction between the granules and the die wall during compression and ejection of the tableting process Antiadherents To minimize the problem of picking i.e. portion, of the tablet face picked out and adhered to the punch face during tableing Colorants For identification purpose and visual marketing values. Flavours and sweeteners To improve the taste of chewable tablets Fine silica, magnesium stearate, purified talc Starch and derivatives (polyplasdone XL) Microcrystalline cellulose Claysm, algins gums, surfactant Water insoluble metal stearates, stearic acid, talc water soluble boric acid, sodium chloride, benzoate and acetate sodium or magnesium lauryl sulfate Carbowax 4000 or 6000 Talc, cornstarch metal stearates, sodium lauryl sulfate Natural pigment synthetic dyes Natural e.g. mannitol Artificial e.g. aspartames World Journal of Publisher 481 Available Online at

11 Table 2: Excipients Mechanism of function, concentration and incompatibility Excipients Functions Concentration Incompatibility Lactose monohydrate NF EP JP powder, various mesh Lactose monohydrate NF modified spray dried Lactose anhydrous NF: DT direct tableting Lactose anhydrous NF powder Microcrytalline celluloe (MCC) NF, EP, JP: 101, 102, 12 (DC) etc. Cellulose powder NF Maximum 65-85% Maillard reaction primary amines Range depends on compressibility of drug Range depends on compressibility of drug Range depends on compressibility of drug Same as for lactose monohydrate NF Same as for lactose monohydrate NF Same as for lactose monohydrate NF 20-90% Strong oxidizing agents same as for Disintegrant 5-15% MCC Absorbent 20-90% 0-100% Binder 5-25% Glidant 1-2% Disintegrant 5-15% Starch NF Starch pregelatinized NF Sucrose NF Filler Ranges Incompatibilities Binder 2-25% owing to impurities in sugar Disintegrant 3-15% Filler Binder Same as starch NF but more compressible Not very compressible 2-20% dry 50-67%(wet) Same as for starch Incompatibilities owing to impurities in sugar Coating 50-67% syrup World Journal of Publisher 482 Available Online at

12 Sucrose compressible NF More compressible than sugar Calcium phosphate dibasic USP: direct compression Calcium phosphate anhydrous USP powder & DC grade Calcium carbonate USP powder, DC, or with gum or starch Mannitol USP, powder DC, grades, pyrogen free Sorbitol NF, powder and DC grades Filler Maximum 65%- 75%needs lubricant Maximum 65%- 75%always needs lubricant Maximum 65%- 75%always needs lubricant Same as for sugar Tetracycline indomethacin aspirin ampicillin aspartame, etc. Same as for calcium phosphate dibasic USP Acids and ammonium salts 10-90% chew tablets None reported in dry state Both direct compressible and regular available Form chelates, watersoluble metal ions, PEG Dextrose NF Dextrin NF Aacia NF, spraydried Methyl cellulose NF Fthyl celluloe NF Depends on compressibility of drug Depends on compressibility of drug Maillard reaction primary amines; strong oxidizing agents; warfarin sodium etc. Strong oxiding agents Binder 1-5% Amidopyrine, apomorphine,ethano l etc, oxidizing effects Binder disintegrant Binder Binder coating 1-5% 2-10% Aminacrine HCL chlorocresol, parabens 1-3% Paraffin waxes Microencapsulation 10-20% Sustained release 3-20% Coating 1-3% World Journal of Publisher 483 Available Online at

13 Alginic acid NF Sodium starch Glycolate NF, EPJRS vivastar Croscarmelloe sodim NF, EP: JRS vivasol Magnesium stearate NF, powder, regular and vegetable Disintegrant Binder Control release Super disintegrant Super disintegrant 1-5% Alkaline earth metals 2-8% Ascorbic acid Tablets 0.5-5% Strong acids soluble iron salts Capsule 10-25% Lubricant/glidant % Strong acids alkalis, and iron salts strong oxidizing agents Calcium stearate NF powder Lubricant/glidant 1% and less Same as for magnesium Zinc tearate NF powder Lubricant/glidant % Decomposed by strong acids Stearic acid triple pressed NF FCC powder regular and vegetable Lubricant/glidant 1-3% Metal hydroxides and oxidizing agents naproxen Hydrogenated vegetable oil NF Lubricant/glidant 0.1-2% Oxidizing activity PEG polyethylene glycol NF EP, all molecular weights Lubricant/glidant coating Soluble tablets 5-15% Oxidizing activity softening of solids Silicon dioxide colloidal NF Lubricant/glidant % Diethlstilbesterol Talc USP EP Mineral oil NF light Lubricant/glidant Lubricant/glidant preparations 1-2% Strong oxidizing agents Polysorbate NF FCC various grades Sodium lauryl sulfate NF Wetting agent 0.1-3% Reduces activity of paraben preservatives Wetting agent 1-2% 1-2% Reacts with cations lubricant Table 3: Mechanism Physical properties with examples in wet granulation Mechanism Physical properties Examples: Diluents role is to impart The primary properties relevant to Calcium Carbonate, desirable manufacturing tablet diluents are those that can have Kaolin Starch, properties (e.g. powder flow, tablet compaction strength, wet or dry granule formation, and homogeneity) and performance a direct effect on diluents and formulation performance. These include: Lactose, Pregelatinized starch, Modified Cellulose, Tapioca World Journal of Publisher 484 Available Online at

14 (e.g. content uniformity, disintegration, dissolution, tablet integrity, friability, and physical and chemical stability) some diluents (e.g., microcrystalline cellulose) are occasionally referred to as dry binders because of the high degree of tablet strength they impart to the final compressed tablet. (1)Particle size and size distribution, (2) particle shape, (3) bulk/tapped/true density, (4) specific surface area, (5) crystallinity, (6) moisture content, (7) powder flow, (8) solubility, and (9) compaction properties for tablet dosage forms. Cellulose, Powered Maltodextrin Starch, Wheat starch Maltose, Sucrose Dextrin Mannitol, Sugar etc. Table 4: Manly used tablet diluents and their specific role in tablet production Commonly Used Tablet Diluents and Their Specific Role in Tablet Production Lactose Available as anhydrous and monohydrate; anhydrous material used for direct compression due to superior compressibility Microcrystalline Commonly used for direct compression now often included in cellulose granules due to its excellent compressibility Dextrose, glucose Direct compression diluents, often used in chewable tablets Starch and derivatives Versatile material that can be used as filler Dicalcium phosphate Excellent flow properties Magnesium carbonate Direct compression diluents Table 5: Mechanism Physical properties with Examples in wet granulation Mechanism: Physical properties Examples: Tablet binders are soluble or Dispersion or Acacia, Alginic, Acid, partially soluble in the granulating dissolution of binder Ammonio Methacrylate solvent or, as in the case of native in the granulation Copolymer, Carbomer starches, can be made soluble. The liquid depends on its Copolymer, Gelatin, concentrated binder solutions also physical properties Glucose, Guar Gum, have adhesive properties. Upon like surface tension, Hydroxypropyl, Cellulose addition of liquid, binders typically particle size, size Maltodextrin, Maltose, facilitate the production of moist granules (agglomerates) by altering distribution, solubility, and Methylcelulose, Povidone, Starch, Corn Starch, Potato interparticle adhesive. viscosity are among the more important. starch. World Journal of Publisher 485 Available Online at

15 Table 6: Commonly used tablet binders and their specific role in tablet production Commonly used Tablet Binders and Their Specific Role in Tablet Production Starch The most commonly used binder, starch has to be prepared as paste, just before use Pre-gelatinised starch Soluble in cold water so easier to prepare than starch Acacia Required preparation of paste prior to use; retard disintegration time if used at high concentration Polyvinyl pyrrolidone Available in range of molecular weight and viscosities; soluble in water and ethanol Hydroxyl propyl methyl cellulose Low viscosity grades most widely used and Methyl cellulose Table 7: Mechanism Physical properties with Examples in wet granulation Mechanism Physical properties Examples They are insoluble in water and facilitating the transport of liquid into the core of the tablet, with the consequence that the tablet breaks into fragments. Disintegrates may increase the porosity and wet ability of the compressed tablet matrix. In so doing gastrointestinal fluids may readily penetrate the tablet matrix and thereby enable tablet breakdown to occur. Disintegrates may operate by swelling in the presence of aqueous fluids, thereby expediting tablet disintegration due to the increase in the internal pressure within the tablet matrix. They are often referred as super disintegrans. Tablet disintegration may also be mediated by the production of gas whenever the tablet contacts aqueous fluids. This is the mechanism of disintegration of effervescent tablets. They are insoluble in water and swell, facilitate the disintegration of the tablets. Tablets containing a mixture of sodium bicarbonate and organic acids such as tartaric or citric acid will effervesce when added to water. Starch, MCC, Gelatin, Gums and Sodium starch. Sodium starch glycolate croscarmellose sodium (a cross-linked sodium carboxymethylcellulose ) and crospovidone glycolate Sodium bicarbonate and organic acids such as tartaric or citric acid. World Journal of Publisher 486 Available Online at

16 Table 8: Commonly used tablet disintegrants and their specific role in tablet production Commonly used Tablet Disintegrates and Their Specific Role in Tablet Production Starch Probably works by capillary action and swelling minimal at body temperature Microcrystalline cellulose Strong capillary action Alginic acid Swell like gum but form less viscous gels Sodium starch glycolate Swell when comes in contact with water and strong Croscar- capillary action. malose sodium Table 9: Mechanism Physical properties with examples in wet granulation Mechanism: Physical properties Examples Lubricants function by adhering to solid surfaces (granules and machine parts) and reducing the particleparticle friction or the particle-metal friction. The primary physical properties that are possible important for boundary lubricants include particle size, surface area, hydration state, and polymorphic form. Calcium Stearate, Sodium Lauryl Sulfate, Talc, Sodium Stearyl Fumarate, Vegetable Oil, Hydrogenated, Magnesium Stearate, Starch Zinc Stearate Mineral Oil, Light Stearic Acid, Polyethylne Glycol Table 10: Commonly used tablet lubricants and their specification in tablet production Commonly used Tablet Lubricants and Their Specification in Tablet Production Talc Silicon dioxide Starch Sodium lauryl sulphate Fine, crystalline powder; Widely used as diluents has small particle size and large surface area help in covering imperfection of granules. Flowability; used for adsorbent, antitacking agen disintegrant and glidant Mainly used for binder, disintegrant and diluents but also used for glidant Anionic surfactant, lubricant and wetting agent World Journal of Publisher 487 Available Online at

17 Magnesium stearte and Mineral oil Hydrophobic can be applied to either formulation or tooling Table 11: Mechanism Physical properties with examples in wet granulation Mechanism: Physical properties Examples Guidants probably work by a combination of adsorption onto the surface of larger particles adhesive and cohesive forces, thus allowing particles to move more easily relative to one another. Primary physical properties of potential importance for glidants and anticaking agents are particle size, particle size distribution and surface aera. They may be slightly hygroscopic. Calcium silicate, silicon dioxide, colloidal Magnesium silicate, Talc Table 12: Commonly used tablet glidants and their specific role in tablet production Commonly used Tablet Glidants and Their Specific Role in Tablet Production Talc Fine, crystalline powder; widely used as lubricant has small particle size and large surface area helps to improve flowability Silicon Flowability : used for adsorbent, antitacking agent, disintegrant and dioxide glidant Table 13: Mechanism Physical properties with examples in wet granulation Mechanism Physical properties Examples Sweetening agents bind to receptors on the tongue that are responsible for The primary physical properties relevant to Acesulfame, Aspartame, Maltose, the sensation of wetness. The longer sweetness relate to Sucrose Saccharin the sweetener molecule remains their compatibility Sugar dextrose attached to the receptor, the sweeter with the other saccharin, Fructose, the substance is perceived to be. The ingradients in the Sorbitol Galactose standard for wetness is sucrose. formulation and Sorbitol Solution World Journal of Publisher 488 Available Online at

18 Table 14: Diluents, disintegrants, lubricants, glidants used in dry granuation Diluents /filler Disintegrants Lubricants Glidants Miscellaneous Anhydrous lactose or lactose monohydrate starch Dibasic calcium Starch MCC, sodium starch glycolate, Crocarmellose sodium and crospovidone Talc colloidal silicon dioxide Colours, sweetening agents etc. Colours, sweetening agents etc. Table 15: Diluents, disintegrants, lubricants, glidants used in direct compression Diluents /filler Disintegrants Lubricants Glidants Spray dried lactose (e.g. MCC (e.g. Avicel, Magnesium Talc lactopress spray dried, Pregelatinised starch stearte, Colloidal lactopress) Spray dried 250 (e.g. starch 15000) stearic Silicon Dicalcium phosphate (e.g. sodium starch acid, dioxide Encompress grades) glycolate sodium Mannitol, Sorbitol, MCC croscarmelloe and stearyl sodium crospovidone) fumarate Table 16: Mechanism Physical properties with examples Mechanism: Physical properties Examples Particle size and size ditributionof dyes and lakes can influence product processing times (blending and dissolution), color intensity and uniformity of appearance Water soluble dyes are usually dissolved in a granulating fluid for use, although they may also be adsorbed onto carriers such as starch, lactose or sugar from Ferric oxide red, Ferric, Oxide Yellow Ferric Oxide blends Caramel World Journal of Publisher 489 Available Online at

19 The coating system forms a layer on the substrate e.g. a particle or unit dosage form, and changes its appearance, on contact with the secretions of the gastrointestinal tract, the coating makes the product slide more easily over mucosal surfaces and helps control the rate and site of drug release. Table 17: Mechanism Physical properties with examples Mechanism Physical properties Examples The necessary physical properties for a coating system include adequate mechanical strength. The film must be strong enough to withstand tumbling during the coating process and to resist film erosion. The solubility of the coating material must be adequate in either aqueous or nonaqueous solvents, depending on the nature of the material. Carboxymethylcellulose, Cellulose Acetate, Celluloe Acetate Phthalate, Ethylcellulose, Gelatin, hydroxypropyl Cellulose, Methacrylic Acid Copolymmer, Methylcellulose, Polyethylen Glycol, Polyvinyl Acetatehthalate, shellac starch wax, carnauba wax and Microcrystalline wax. Table 18: Coating materials and their specific role in tablet production Commonly used tablet coating materials and their specific role in tablet production Methyle cellulose Ethyl cellulose Hydroxyl propyl methyl cellulose Sodium carboxy methyl cellulose Soluble in cold water, GI fluids and a range of organic solvents Soluble in organic solvents, insoluble in water and GI fluids used aione in modified release formulation and in combination with water soluble cellulose for immediate release formulation Soluble in cold water, GI fluids alcohols, Soluble in water and polar solvents World Journal of Publisher 490 Available Online at