Excipients used in oral solid dosage forms


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Excipients used in oral solid dosage forms:

Excipients used in oral solid dosage forms Presented by: Abhilash Mund M.pharm, 1 st Sem. (Pharmatechnology) Royal College of Pharmacy & Health Sciences

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What is Excipient ? The term comes from Latin word “excipiens” which means to receive or to take out . “ IT IS AN INERT SUPPORT OF THE ACTIVE PRINCIPLE ” According to International Pharmaceutical Excipient Council (IPEC) : These are the process aids or any substances other then the Active Pharmaceutical Ingredient (API) or prodrug that is included in pharmaceutical dosage forms.

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Selection of excipients for solid oral dosage forms:

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Ideal characteristics…. Nontoxic Pharmacologically inert. Physically and chemically stable. Acceptable to the Regulatory agencies in all countries. Commercially available. Have pleasing organoleptic properties. Must be colour compatible. Economical

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Physical Physicochemical and Biopharmaceutical property Basic requirements of a modern pharmaceutical Excipients: API vs. Excipients: For both safety and quality. For API therapeutic efficacy. For Excipients functionality.

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What are the functionalities of Excipient? Impart weight, consistency and volume: It’s allow accuracy of dose. Improve solubility. Increase stability. Enhance bioavailability. Modifying drug release. Assist in product identification. Increase patient acceptability. Facilitate dosage form design.

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Classification of excipients… Primary Excipients Diluents (Filler) Binders (Adhesives) Disintegrants Lubricants Antiadhesives Glidents Excipients Secondary excipients Colouring agents Flavours Sweeteners Coating agents Plasticizers Wetting agents Miscellaneous Excipients Buffers Adsorbents Waxes

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Diluents (Filler): Diluents are used to increase the bulk volume of a tablet or capsule when the drug dosage itself is inadequate to produce tablets of adequate weight and size. Usually the range of diluent may vary from 5-80% . The tablet size should be kept above 2-3 mm . Minimum tablet weight is typically ~50mg . Actual API doses can be as low as ~20 µg. Functions of diluent: To facilitate tablet handling during manufacture. To achieve targeted content uniformity. To provide improved cohesion. To allow direct compression manufacturing. To enhance flow. To adjust weight of tablet as per die capacity.

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Classification of diluents… Four major classes: Natural Diluents: Starch Native starch ( PharmGel, StarCap 1500, Sta-Rx 1500 ) Hydrolyzed starch (Emdex, Celutab) Partially pregelatinized starch ( Lycatab ) Soyabean powder (newly introduced) Organic Diluents: Lactose α-lactose monohydrate ( trade name Pharmatose and Respitose) . Spray dried lactose (Spray Process 315) Anhydrous lactose (Pharmatose DCL 21) Sucrose ( Sugartab, Dipac, Nu tab ) Mannitol ( Parteck M, Pearlitol ) Sorbitol ( Sorbifin, Sorbidex and Neosorb ) Xylitol ( Xylisorb - used in chewable tablets ) Erythritol (Zerose) Powdered cellulose ( Elcema G-250 ) Microcrystalline cellulose ( Avicel- [PH 101, 102, 105 ] , Emcocel, Tabulose )

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Inorganic Diluents: Dibasic calcium phosphate dihydrate ( Di-Tab, Emcompress ) Dibasic calcium phosphate anhydrate (A-Tab, Fujicalin) Tribasic calcium phosphate (Tri-Tab) The inorganic diluents, do not exhibit binding properties when used in wet granulation and direct compression. Co-processed Diluents: Co-processing means combining two or more materials by an appropriate process. It provide better tableting properties than a single substance . According to solubility in water: INSOLUBLE DILUENTS SOLUBLE DILUENTS Starch Powdered cellulose Microcrystalline cellulose Calcium phosphates, etc. Lactose Sucrose Mannitol Sorbitol, etc.

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TRADE NAME OF DILUENTS COMPOSITION Fast Flo lactose Crystalline α-lactose monohydrate and amorphous lactose. Microcellac 75% lactose and 25% MCC Ludipress 93% α- lactose monohydrate, 3.5% polyvinylpyrrolidone, and 3.5% crospovidone. Nu-Tab Sucrose 95-97%, invert sugar 3-4% and magnesium- stearate 0.5% Di-Pac Sucrose 97% and modified dextrins 3% Sugartab Sucrose 90-93% and invert sugar 7-10%. Emdex Dextrose 93-99% and maltose 1-7% Cal-Tab Calcium sulfate 93% and vegetable gum 7% Cal Carb Calcium carbonate 95% and maltodextrins 5% Calcium 90 Calcium carbonate 90-91% and Starch 9-10%

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Binders (Adhesives) Binders are used to hold the active pharmaceutical ingredient and inactive ingredients together in a cohesive mix. (5-25%) Binders ensure the mechanical strength. Exhibit cohesive and adhesive force. Classification of binder: According to their application: Dry binders : Direct powder compression. Dry granulation (roller compaction, slugging). As a solution or paste: Wet granulation

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Granulating fluid used: Water and occasionally with ethanol . According to their solubility: Insoluble in water e.g. starch Soluble in water e.g. HPMC Soluble in water and ethanol e.g. Povidone According to their chemical source: Saccharides and their derivatives: Disaccharides: sucrose, lactose Polysaccharides and their derivatives: Starches : Starch paste, pregelatinized starch. Modified cellulose: microcrystalline cellulose. Cellulose ethers: hydroxypropyl cellulose, HPMC. Sugar alcohols: xylitol, sorbitol etc. Naturl gums: acacia, tragacanth. Protein: gelatin Synthetic polymer: polyvinylpyrrolidone(PVP), polyethyiene glycol

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DISINTEGRANT AND SUPER-DISINTEGRANT Disintegrants cause rapid break up of the tablet compact upon exposure to moisture. Superdisintegrant: the simplest way to achieve quick disintegration. Used intragranulerly or extragranularly or both for better action . Mode of action : Swelling : e.g.- Cellulose and its derivatives Porosity and Capillary Action (Wicking): e.g.- Microcrystalline cellulose Deformation By enzymatic reaction: enzymes destroy the binding action of binder and helps in disintegration. ENZYMES BINDER Amylase Starch Protease Gelatin Cellulase Cellulose derivatives Invertase Sucrose

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BRAND NAMES CONC. IN % CATEGORIES Starch USP 5-20 Native starch Starch 1500 5-15 Modified starch Avicel (PH 101, PH 102) 10-20 Microcrystalline cellulose Solka floc 5-15 Purified wood cellulose Alginic acid NF 1-5 Acts by swelling Na alginate 2.5-10 Acts by swelling Explotab , Primojel 2-8 Sodium starch glycolate, (superdisintegrant) Polyplasdone (XL ) 0.5-5 Crosslinked PVP Amberlite (IPR 88) 0.5-5 Ion exchange resin Methyl cellulose, Na CMC, HPMC 5-10 Cellulose derivatives AC-Di-Sol 1-3 Direct compression Polyplasdone Miscellaneous category Types of disintegrant:

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SUPERDISINTEGRANTS EXAMPLE OF MECHANISM OF ACTION Crosscarmellose Ac-Di-Sol Vivasol Primellose Crosslinked cellulose -Swells 4-8 folds in < 10 seconds. -Swelling and wicking both. Crosspovidone Crosspovidon M Kollidon Polyplasdone Crosslinked PVP -Swells very little and returns to original size after compression but act by capillary action Sodium starch glycolate Explotab Primogel Crosslinked starch -Swells 7-12 folds in <30  seconds Alginic acid NF Satialgine Crosslinked alginic acid -Rapid swelling in aqueous medium or wicking action Soypolysaccharides Emcosoy Natural super disintegrant Swelling Calcium silicate -Wicking action LIST OF SUPERDISINTEGRANTS

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LUBRICANTS, ANTIADHESIVES AND GLIDENTS Lubricants are used in formulations to: S mooth ejection of tablet from die cavity. P revent sticking of powder on punch faces. Reduce interparticle friction during compression. I mprove flow of powder blend and granules into the die cavity. Usual range (0.1-5%) Under-lubricated blends - compression sticking problems. Over-lubricated blends - adversely affect tablet hardness and dissolution rate. A ccording to functionality: (1) G lidant : enhance flow property of powder blend by overcoming powder cohesiveness. (2) A ntiadherent: prevent sticking to the punch. (3) Die wall lubricant: reduce the friction between the tablet surface and the die wall during and after compaction to enable easy ejection.

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Die-wall lubricants are of two classes : Fluid lubricants: work by separating moving surfaces completely with a layer of lubricant. Boundary lubricants: work by forming a thin solid film at the interface of die and tablet. According to solubility: Hydrophobic: Most widely used lubricants in use today. Hydrophilic: Generally poor lubricants, no glidant or anti-adherent properties. HYDROPHILIC HYDROPHOBIC Boric acid Magnesium , calcium and sodium stearate Sodium chloride Stearic acid DL- Lucine Sterotex Carbowax 4000, 6000 Sterowet Sodium lauryl sulfate Aerocil

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CATEGORIES CONCENTRATIONS USED IN % Glidant Talc Fumed silicon dioxide Native starch Aerosil 1-5 0.1-0.5 1-10 1-3 Antiadherent Talc Cornstarch Cab-O- Sil ( Fumed Silicon Dioxide ) Syloid DL- Leucine 1-5 3-10 0.1-0.5 0.1-0.5 3-10 Fluid lubricants Light mineral oil Vegetable oils (Sterotex, Lubritab) Glyceryl Behenate (Compitrol 888) 1-3 2-5 Boundary lubricants Metallic stearate Sodium stearyl fumarate Polyethylene glycol Sodium lauryl sulfate 0.2 - 2 0.5 - 2 2 - 20 1 - 3

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COLOuRING AGENTS Colours are incorporated into tablets generally for : Identification of similar-looking products. Minimize the possiblity of mixups. Increase aesthetic value or their marketing value. FD&C and D&C dyes and lakes are mostly used. Dyes are relatively unstable because : 1 ) light sensitive 2) By oxidizing and reducing agents 3) Microorganisms 4) Trace metals 5) pH 6) High temperatures .

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COLOURS COMMON NAMES FD&C blue #1 FD&C blue #2 D&C blue #4 D&C blue #9 FD&C green #3 D&C green #5 D&C green #6 D&C green #8 D&C orange #4 D&C orange #5 D&C orange #10 FD&C red #3 FD&C red #4 D&C red #7 D&C red #17 Brilliant blue FCF Indigotine Alphazurine Indanthrene blue Fast green FCF Alizarin cyanine green F Quinizarine green SS Pyranine concentrated Orange II Dibromofluorescein Diiodofluorescein Erythrosine Ponceau Lithol rubin Toney red

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FLAVORS AND SWEETENERS Flavors and sweeteners are commonly used to improve mouth feel . Flavors have found little acceptance due to their lesser stability upon aging . Types of flavor: Water soluble (solution) Volatile oils Dry flavors e.g.:- Bitter product - mint , cherry or anise may be used. Salty product - peach , apricot or liquorice may be used. Sour product - raspberry or liquorice may be used. Excessively sweet product - vanilla may be used.

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Sweeteners are added to make the ingredients more palatable. SWEETENERS COMMENTS Mannitol 72% as sweet as sugar Saccharin 400 times sweeter then sucrose. Artificial sweetener Carcinogenic Bitter after taste Cyclamate Carcinogenic Aspartame 180 times sweeter then sucrose. Unstable in presence of moisture Sucrose ,dextrose etc Not sufficiently mask the test

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COATING AGENTS : COATING TYPE POLYMERS TRADE NAME Enteric Coatings Cellulose Acetate Phthalate HPMC Aquacoat CPD Sepifilm LP Polymer Extenders Hydroxypropylcellulose Klucel EF and LF Immediate Release Coatings HPMC Ethylcellulose Microcrystalline Cellulose Carrageenan Methylcellulose Sepifilm LP Aquacoat ECD Lustre Clear Metolose SM-4 Sustained Release Coatings Ethylcellulose Aquacoat ECD Aqualon Subcoat Hydroxypropylcellulose Klucel Pellet Coating Methylcellulose Metolose SM-4

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PLASTICIZERS FOR COATING Used for physical modification of coating polymer . Plas II : composed of: Glyceryl Monostearate Polysorbate 80 Triethylcitrate Methyl Parabens Propyl Parabens Citrate Esters Triethyl citrate Acetyltriethyl Citrate Acetyltri-n-butyl Citrate Dibutyl Sebacate Diethyl phthalate Triacetin

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ADSORBENTS Silicon dioxide (Syloid, Cab-O- Sil, Aerosil) Bentonite Kaolin Magnesium silicate Tricalcium phosphate Magnesium carbonate Magnesium oxide WAXES (Polishing agent ) C arana uba Yellow Beeswax White Beeswax Paraffin Naphtha Miscellaneous components BUFFERS (Maintain a required pH for stability) Sodium bicarbonate Sodium citrate Calcium carbonate

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Physicochemical Tests for Excipients Flow rate Gel strength (binders) Lubricity (frictional) Microbiological status Moisture sorption Particle hardness Particle size distribution: (1) sieve analysis (2) air permeability Porosity Shear rate Tensile strength Bulk volume Water absorption

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