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Excipients Definition: Excipients in pharmaceuticals are substances other than the active pharmaceutical ingredient (API).
To produce a drug substance in a final dosage form requires pharmaceutical excipients.
For example, in the preparation of solutions, one or more solvents are used to dissolve the drug substance, flavors and sweeteners are used to make the product more palatable, colorants are added to enhance the appeal, preservatives may be added to prevent microbial growth, and stabilizers, such as antioxidants and chelating agents, may be used to prevent decomposition.
For the preparation of tablets, diluents or fillers are commonly added to increase the bulk of the formulation, binders to cause adhesion of the powdered drug and pharmaceutical substances, anti-adherent or lubricants to assist smooth tablet formation, disintegrating agents to promote tablet breakup after administration, and coatings to improve stability, control disintegration, or enhance appearance.
Ointments, creams, and suppositories acquire their characteristic features from their pharmaceutical bases. Thus, for each dosage form, the pharmaceutical ingredients establish the primary features of the product and contribute to the physical form, texture, stability, taste, and overall appearance.
PHARMACEUTICAL EXCIPIENTS/INGREDIENTS
| ngredient/ Excipient | Example | Example | Conc.(%) | |
| Preservatives: Used in liquid and semisolid preparations to prevent growth of Micro-organism. | Based on chemical Class | Acidic | Phenol | 0.2-0.5 |
| Chlorocresol | 0.05-0.1 | |||
| O-Phenyl phenol | 0.005-0.1 | |||
| Alkyl ester of parahydroxybezoic acid | 0.001-0.2 | |||
| Benzoic acid & its salts | 0.1-0.3 | |||
| Boric acid & Its salt | 0.5-1.0 | |||
| Sorbic acid & Its salt | 0.05-0.2 | |||
| Neutral | Chlorobutanol | 0.5 | ||
| Benzyl alcohol | 0.1 | |||
| Beta- Phenylethyl alcohol | 0.2-1.0 | |||
| Mercurial | Thimerosal | 0.001-0.1 | ||
| Phenylmercuric acetate & Nitrate | 0.002-0.005 | |||
| Nitromersol | 0.000-0.1 | |||
| QAC (Quaternary Ammonium Compound) | Benzalkonium chloride | 0.004-0.02 | ||
| Cetypyridimium | 1.01-0.02 | |||
| Based on Micro-organism | Antifungal | ButylparabenEthylparabenMethylparabenBenzoic acidPropylparabenSodium benzoateSodium propionate | ||
| Antimicrobial | Benzoic acid & Its salt Ex.Benzalkonium chloride etc | |||
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| Antioxidant: Used to prevent deterioration of preparations byoxidation | Compounds | Reducing agent Antioxidant | Ascorbic acid | 0.02-0.1 |
| Sod. Bisulfite | 0.1-0.15 | |||
| Sod. Metasulfite | 0.1-0.15 | |||
| Sof. Formaldehyde sulfoxylate | 0.1-0.15 | |||
| Thoiurea | 0.005 | |||
| Blocking agent Antioxidant | Ascorbic acid esters | 0.1-0.15 | ||
| BHT (Butyl hydroxytoluene), BHA | 0.005-0.02 | |||
| Tocopherol/vit E | 0.05-0.075 | |||
| Chelating agent as antioxidant | EDTA (Ethylenediaminetetraacetic acids) | 0.01-0.075 | ||
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| Synergists antioxidant | Ascorbic acis | 0.01-0.05 | ||
| Citric acid | 0.005-0.01 | |||
| Citraconic acid | 0.03-0.45 | |||
| Phosphoric acid | 0.005-0.01 | |||
| Tartaric acid | 0.01-0.02 | |||
| Air displacement | Nitrogen gas | Agent employed to displace air (oxygen) in a hermetically sealed container to enhance product stability | ||
| Ingredient/ Excipient | Definition | Example |
| Adsorbent | An agent capable of holding other molecules onto its surface by physical or chemical (chemisorption) means | Powdered celluloseActivated charcoal |
| Acidifying agent | Used in liquid preparations to provide acidic medium for product stability | Citric acidAcetic acidFumaric acidHydrochloric acidNitric acid |
| Alkalinizing agent | Used in liquid preparations to provide alkaline medium for product stability | Ammonia solutionAmmonium carbonateDiethanolamineMonoethanolaminePotassium hydroxideSodium bicarbonateSodium borateSodium carbonateSodium hydroxideTrolamine |
| Aerosol propellant | Agent responsible for developing the pressure withinan aerosol container and expelling the product whenthe valve is opened | Carbon dioxideDichlorodifl uoromethaneDichlorotetrafl uoroethaneTrichloromonofl uoromethane |
| Buffering agent | Used to resist change in pH upon dilution or addition of acid or alkali | Potassium metaphosphatePotassium phosphate,Monobasic Sodium acetateSodium citrate, Anhydrous and dihydrate |
| Chelating agent | Substance that forms stable water-soluble complexes (chelates) with metals; used in some liquid pharmaceuticals as stabilizers to complex heavy metals that might promote instability. In such use, they are also called sequestering agents | Edetic acidEdetate disodium |
| Colorant | Used to impart color to liquid and solid (e.g., tablets and capsules) preparations | Caramel, Ferric oxide & Regulatory approved color |
| Clarifying agent | Used as a filtering aid for its adsorbent qualities | Bentonite |
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| Emulsifying agent | Used to promote and maintain dispersion of finely subdivided particles of liquid in a vehicle in which it is immiscible. End product may be a liquid emulsion or semisolid emulsion | AcaciaCetomacrogolCetyl alcoholGlyceryl monostearateSorbitan monooleatePolyoxyethylene 50 stearate |
| Encapsulating agent | Used to form thin shells to enclose a drug for ease of administration | Gelatin |
| Flavorant | Used to impart a pleasant flavor and often odor to a preparation. In addition to the natural flavorants listed, many synthetic ones are used | Anise oilCinnamon oilCocoaMentholOrange oilPeppermint oilVanillin |
| Humectant | Used to prevent drying of preparations, particularly ointments and creams | GlycerinPropylene glycolSorbitol |
| Levigating agent | Liquid used as an intervening agent to reduce the particle size of a powder by grinding, usually in a mortar | Mineral oilGlycerinPropylene glycol |
| Ointment base | Semisolid vehicle for medicated ointments | LanolinHydrophilic ointmentPolyethylene glycol ointmentPetrolatumHydrophilic petrolatumWhite ointmentYellow ointmentRose water ointment |
| Plasticizer | Component of fi lm-coating solutions to make fi lm more pliable, enhance spread of coat over tablets, beads, and granules | Diethyl phthalateGlycerin |
| Solvent | Used to dissolve another substance in preparation of a solution; may be aqueous or not (e.g., oleaginous). Cosolvents, such as water and alcohol (hydroalcoholic) and water and glycerin, may be used when needed. Sterile solvents are used in certain preparations (e.g., injections) | AlcoholCorn oilCottonseed oilGlycerinIsopropyl alcoholMineral oilOleic acidPeanut oilPurifi ed waterWater for injectionSterile water for injectionSterile water for irrigation |
| Stiffening agent | Used to increase thickness or hardness of a preparation, usually an ointment | Cetyl alcoholCetyl esters waxMicrocrystalline waxParaffi nStearyl alcoholWhite waxYellow wax |
| Suppository base | Vehicle for suppositories | Cocoa butterPolyethylene glycols (mixtures)PEG 3350 |
| Surfactant (surface active agent) | Substances that absorb to surfaces or interfaces to reduce surface or interfacial tension. May be used as wetting agents, detergents, or emulsifying agents | Benzalkonium chlorideNonoxynol 10Octoxynol 9Polysorbate 80Sodium lauryl sulfateSorbitan monopalmitate |
| Suspending agent | Viscosity-increasing agent used to reduce sedimentationrate of particles in a vehicle in which they are not soluble; suspension may be formulated for oral, parenteral, ophthalmic, topical, or other route | AgarBentoniteCarbomer (e.g., Carbopol)Carboxymethylcellulose sodiumHydroxyethyl celluloseHydroxypropyl celluloseHydroxypropyl methylcelluloseKaolinMethylcelluloseTragacanthVeegum |
| Sweetening agent | Used to impart sweetness to a preparation | AspartameDextroseGlycerinMannitolSaccharin sodiumSorbitolSucrose |
| Tablet-Antiadherents | Prevent tablet ingredients from sticking to punches and dies during production | Magnesium stearate |
| Tablet binders | Substances used to cause adhesion of powder particles in tablet granulations | AcaciaAlginic acidCarboxymethylcellulose sodiumCompressible sugar (e.g., Nu-Tab)EthylcelluloseGelatinLiquid glucoseMethylcellulosePovidonePregelatinized starch |
| Tablet and capsule diluent | Inert filler to create desired bulk, fl ow properties, and compression characteristics of tablets andcapsules | Dibasic calcium phosphateKaolinLactoseMannitolMicrocrystalline cellulosePowdered cellulosePrecipitated calcium carbonateSorbitolStarch |
| Tablet coating agent | Used to coat a tablet to protect against decompositionby atmospheric oxygen or humidity, to provide a desired release pattern, to mask taste or odor, or for aesthetic purposes. Coating may be sugar, fi lm, or thick covering around a tablet. Sugar-coated tablets generally start to break up in the stomach. Film forms a thin cover around a formed tablet or bead. Unless it is enteric, film dissolves in the stomach. Enteric coating passes through the stomach to break up in the intestines. Somewater-insoluble coatings (e.g., ethylcellulose) are used to slow the release of drug in the gastrointestinal tract | Content provided by https://thepharmapedia.com/ |
| Sugar coating | Content provided by https://thepharmapedia.com/ | Liquid glucoseSucrose |
| Film coating | Content provided by https://thepharmapedia.com/ | Hydroxyethyl celluloseHydroxypropyl celluloseHydroxypropyl methylcelluloseMethylcellulose(e.g., Methocel)Ethylcellulose (e.g., Ethocel) |
| Enteric coating | Content provided by https://thepharmapedia.com/ | Cellulose acetate phthalateShellac (35% in alcohol,pharmaceutical glaze) |
| Tablet direct compressionexcipient | Used in direct compression tablet formulations | Dibasic calcium phosphate(e.g., Ditab) |
| Tablet disintegrates | Used in solid forms to promote disruption of the mass into smaller particles more readily dispersed ordissolved | Alginic acidPolacrilin potassium(e.g., Amberlite)Sodium alginateSodium starch glycolateStarch |
| Tablet glidant | Used in tablet and capsule formulations to improve flow properties of the powder mixture | Colloidal silicaCornstarchTalc |
| Tablet lubricant | Used in tablet formulations to reduce friction during tablet compression | Calcium stearateMagnesium stearateMineral oilStearic acidZinc stearate |
| Tablet or capsule opaquant | Used to render a coating opaque. May be used alone or with a colorant | Titanium dioxide |
| Tablet polishing agent | Used to impart an attractive sheen to coated tablets | Carnauba waxWhite wax |
| Tonicity agent | Used to render solution similar in osmotic-dextrose characteristics to physiologic fluids, e.g., in ophthalmic, parenteral, and irrigation fluids | Sodium chloride |
| Vehicle | Carrying agent used in formulating a variety of liquids for oral and parenteral administration Generally, oral liquids are aqueous (e.g., syrups) or hydroalcoholic (e.g., elixirs). Solutions for intravenous use are aqueous, whereas intramuscular injections may be aqueous or oleaginous | |
| Flavoured, sweetened | Content provided by https://thepharmapedia.com/ | Acacia syrupAromatic syrupAromatic elixirCherry syrupCocoa syrupOrange syrupSyrup |
| Oleaginous | Content provided by https://thepharmapedia.com/ | Corn oilMineral oilPeanut oilSesame oil |
| Viscosity-increasing agent | Used to render preparations more resistant to fl ow. Used in suspensions to deter sedimentation, in ophthalmic solutions to enhance contact time (e.g., methylcellulose), to thicken topical creams, etc. | Alginic acidBentoniteCarbomerCarboxymethylcelluloseSodiumMethylcellulosePovidoneSodium alginateTragacanth |
Preservatives interfere with microbial growth, multiplication, and metabolism through one or more of the following mechanisms:
- Modify cation of cell membrane permeability and leakage of cell constituents (partial lysis)
- Lysis and cytoplasmic leakage
- Irreversible coagulation of cytoplasmic constituents (e.g., protein precipitation)
- Inhibition of cellular metabolisms, such as by interfering with enzyme systems or inhibition of cell wall synthesis
- Oxidation of cellular constituents
- Hydrolysis
| Name of Preservatives | Modes/Mechanism of action |
|---|---|
| Benzoic acid, boric acid, p-hydroxybenzoates | Denaturation of proteins |
| Phenols and chlorinated phenolic compounds | Lytic and denaturation action on cytoplasmic membranes and for chlorinated preservatives, also by oxidation of enzymes |
| Alcohols | Lytic and denaturation action on membranes |
| Quaternary compounds | Lytic action on membranes |
| Mercurials | Denaturation of enzymes by combining with thiol (-SH) groups) |