PHARMACEUTICAL EXCIPIENTS/INGREDIENTS & THEIR USES

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Classification of excipients

To produce a drug substance in a final dosage form requires pharmaceutical ingredients.

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 INGREDIENTS/ EXCIPIENTS

Ingredient/ 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

Butylparaben

Ethylparaben

Methylparaben

Benzoic acid

Propylparaben

Sodium benzoate

Sodium propionate

 

Antimicrobial

Benzoic acid & Its salt Ex.Benzalkonium chloride etc

 

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Antioxidant: Used to prevent deterioration of preparations by

oxidation

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 cellulose

Activated charcoal

Acidifying agent

Used in liquid preparations to provide acidic medium for product stability

Citric acid

Acetic acid

Fumaric acid

Hydrochloric acid

Nitric acid

Alkalinizing agent

Used in liquid preparations to provide alkaline medium for product stability

Ammonia solution

Ammonium carbonate

Diethanolamine

Monoethanolamine

Potassium hydroxide

Sodium bicarbonate

Sodium borate

Sodium carbonate

Sodium hydroxide

Trolamine

Aerosol propellant

Agent responsible for developing the pressure within

an aerosol container and expelling the product when

the valve is opened

Carbon dioxide

Dichlorodifl uoromethane

Dichlorotetrafl uoroethane

Trichloromonofl uoromethane

Buffering agent

Used to resist change in pH upon dilution or addition of acid or alkali

Potassium metaphosphate

Potassium phosphate,

Monobasic Sodium acetate

Sodium 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 acid

Edetate 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

Acacia

Cetomacrogol

Cetyl alcohol

Glyceryl monostearate

Sorbitan monooleate

Polyoxyethylene 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 oil

Cinnamon oil

Cocoa

Menthol

Orange oil

Peppermint oil

Vanillin

Humectant

Used to prevent drying of preparations, particularly ointments and creams

Glycerin

Propylene glycol

Sorbitol

Levigating agent

Liquid used as an intervening agent to reduce the particle size of a powder by grinding, usually in a mortar

Mineral oil

Glycerin

Propylene glycol

Ointment base

Semisolid vehicle for medicated ointments

Lanolin

Hydrophilic ointment

Polyethylene glycol ointment

Petrolatum

Hydrophilic petrolatum

White ointment

Yellow ointment

Rose 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 phthalate

Glycerin

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)

Alcohol

Corn oil

Cottonseed oil

Glycerin

Isopropyl alcohol

Mineral oil

Oleic acid

Peanut oil

Purifi ed water

Water for injection

Sterile water for injection

Sterile water for irrigation

Stiffening agent

Used to increase thickness or hardness of a preparation, usually an ointment

Cetyl alcohol

Cetyl esters wax

Microcrystalline wax

Paraffi n

Stearyl alcohol

White wax

Yellow wax

Suppository base

Vehicle for suppositories

Cocoa butter

Polyethylene 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 chloride

Nonoxynol 10

Octoxynol 9

Polysorbate 80

Sodium lauryl sulfate

Sorbitan monopalmitate

Suspending agent

Viscosity-increasing agent used to reduce  sedimentation

rate of particles in a vehicle in which they are not soluble; suspension may be formulated for oral, parenteral, ophthalmic, topical, or other route

Agar

Bentonite

Carbomer (e.g., Carbopol)

Carboxymethylcellulose sodium

Hydroxyethyl cellulose

Hydroxypropyl cellulose

Hydroxypropyl methylcellulose

Kaolin

Methylcellulose

Tragacanth

Veegum

Sweetening agent

Used to impart sweetness to a preparation

Aspartame

Dextrose

Glycerin

Mannitol

Saccharin sodium

Sorbitol

Sucrose

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

Acacia

Alginic acid

Carboxymethylcellulose sodium

Compressible sugar (e.g., Nu-Tab)

Ethylcellulose

Gelatin

Liquid glucose

Methylcellulose

Povidone

Pregelatinized starch

Tablet and capsule diluent

Inert filler to create desired bulk, fl ow properties, and compression characteristics of tablets and

capsules

Dibasic calcium phosphate

Kaolin

Lactose

Mannitol

Microcrystalline cellulose

Powdered cellulose

Precipitated calcium carbonate

Sorbitol

Starch

Tablet coating agent

Used to coat a tablet to protect against decomposition

by 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. Some

water-insoluble coatings (e.g., ethylcellulose) are used to slow the release of drug in the gastrointestinal tract

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Sugar coating

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Liquid glucose

Sucrose

Film coating

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Hydroxyethyl cellulose

Hydroxypropyl cellulose

Hydroxypropyl methylcellulose

Methylcellulose

(e.g., Methocel)

Ethylcellulose (e.g., Ethocel)

Enteric coating

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Cellulose acetate phthalate

Shellac (35% in alcohol,

pharmaceutical glaze)

Tablet direct compression

excipient

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 or

dissolved

Alginic acid

Polacrilin potassium

(e.g., Amberlite)

Sodium alginate

Sodium starch glycolate

Starch

Tablet glidant

Used in tablet and capsule formulations to improve flow properties of the powder mixture

Colloidal silica

Cornstarch

Talc

Tablet lubricant

Used in tablet formulations to reduce friction during tablet compression

Calcium stearate

Magnesium stearate

Mineral oil

Stearic acid

Zinc 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 wax

White 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

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Acacia syrup

Aromatic syrup

Aromatic elixir

Cherry syrup

Cocoa syrup

Orange syrup

Syrup

Oleaginous

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Corn oil

Mineral oil

Peanut oil

Sesame 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 acid

Bentonite

Carbomer

Carboxymethylcellulose

Sodium

Methylcellulose

Povidone

Sodium alginate

Tragacanth

Mode of Action/Mechanism of action of Preservatives

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 PreservativesModes/Mechanism of action
Benzoic acid, boric acid, p-hydroxybenzoatesDenaturation of proteins
Phenols and chlorinated phenolic compoundsLytic and denaturation action on cytoplasmic membranes and for chlorinated preservatives, also by oxidation of enzymes
AlcoholsLytic and denaturation action on membranes
Quaternary compoundsLytic action on membranes
MercurialsDenaturation of enzymes by combining with thiol (-SH) groups)
mode of action of preservative

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