Pharmaceutical Excipients

Adsorbent

Capable of retaining large quantities of liquids without becoming wett.

⇨ Bentonite

⇨ Powdered cellulose

⇨ Colliloidal silicon dioxide

⇨ Anhydrous calcium phosphate

⇨ Kaolin

⇨ Magnesium oxide

⇨ Magnesium silicate

⇨ Silicon di-oxide (also act as glidant)

Antiadherents

Prevent materials from sticking to punches and die walls.

⇨ Cornstarch

⇨ DL-luicine

⇨ Magnesium stearate

⇨ Coloidal  Silicon dioxide

⇨ Silicon oil

⇨ Sodium lauryl sulfate

⇨ Talc

Anticaking agent

Prevent cake formation.

⇨ Calcium phosphate tribasic

⇨ Magnesium silicate

⇨ Magnesium trisilicate

⇨ Colliloidal silicon dioxide

⇨ Talc

Antioxidants

(Protect drug from undergoing oxidation.)

⇨ Alpha tocopherol

⇨ Anisole

⇨ Ascorbic acid

⇨ Ascorbyl palmitate

⇨ Butylated hydroxy anisole (BHA)

⇨ Butylated hydroxy toluene (BHT)

⇨ Butyl paraben

⇨ Citric acid

⇨ EDTA (Ethylene diamine tetra acetic acid)

⇨ Hydroquinone

⇨ Norhydroguaiaretic acid

⇨ Propyl gallate

⇨ Sodium dioxide

⇨ Sodium bisulfite

⇨ Sodium metabisulfite

⇨ Sodium sulfite

⇨ Sodium thiosulfite

⇨ Sodium formaldehyde

⇨ Tartaric acid

1. Antioxidants for aqueous systems

⇨ Sodium dioxide

⇨ Sodium formaldehyde

⇨ Sodium sulfite

⇨ Sofium bisulfite

⇨ Sodium metabisulfite

⇨ Sodium thiosulfite

2. Antioxidants for oil system:

⇨ Ascorbyl palmitate

⇨ Hydroquinone

⇨ Propyl gallate

⇨ Norhydroguaiaretic acid

Binders/ Binding agents

⇨ Binders hold the ingredients in a tablet together.

⇨ Binders ensure that tablets and granules can be formed with required mechanical strength and give volume to low active dose tablets.

Classification of binders:

1. Sugars:

⇨ Liquid glucose

⇨ Sucrose

2. Natural Binders:

⇨ Alginic acid

⇨ Cellulose

⇨ Gelatin

⇨ Pregelatinized starch

⇨ Starch Paste

3. Synthetic Polymer binders:

⇨ Copovidone

⇨ Crosspovidone

⇨ Ethyl cellulose

⇨ Hydroxyethyl Cellulose

⇨ Hydroxyethylpropyl cellulose

⇨ Hydroxypropyl Cellulose

⇨ Hydroxy propylmetyl cellulose

⇨ Methyl Cellulose

⇨ Sodium carboxy methyl cellulose

⇨ Polythylene glycol

⇨ Polyvinyl pyrolidone

Buffering agents

⇨ Calcium carbonate

⇨ Sodium bicarbonate

⇨ Sodium Citrate

⇨ Histidine

⇨ Phosphate

⇨ Succinate

⇨ Tris [ Shortening of tris(hydroxymethyl)aminomethane.]

Chelating agents

⇨ Inactivating the catalytic activity of heavy metal ions by forming conplexes with that metals.

Examples:

⇨ EDTA

⇨ Dihydroxy ethyl glycine

⇨ Citri acid

⇨ Tartaric acid

Coating agents

Classification of coating agents:

1. Enteric coating agents

2. Non-enteric coating agents

1. Enteric Coating agents:

⇨ Acetyltributyl citrate

⇨ Cellulose acetate phthalate

⇨ Hydroxypropyl methylcellulose acetate phthalate

⇨ Polyvinyl acetate phthalate

⇨ Shellac

⇨ Zein

2. Non-enteric film coating agents:

⇨ Hydroxy methyl ethyl cellulose

⇨ Hydroxy propyl cellulose

⇨ Hydroxy propyl methyl cellulose

⇨ Methyl cellulose

⇨ Polyvinyl phthalate

⇨ Polyethylene glycol

Diluents

1. Diluents for Tablets/Capsules

⇨ Used to make required bulk of the tablet when the drug dosage itself is inadequate to produce the bulk.

⇨ To improve cohesion

⇨ To permit use of direct compression manufacturing

⇨ To promote flow

Examples:

⇨ Ammonium alginate

⇨ Calcium Carbonate

⇨ Calcium phosphate dibasic

⇨ Calcium phosphate tribasic

⇨ Calcium sulfate

⇨ Cellulose

⇨ Dextrates

⇨ Dextrose

⇨ Fructose

⇨ Lactilol

⇨ Lactose Anhydrous

⇨ Lactose monohydrate

⇨ Maltitol

⇨ Maltodextrin

⇨ Maltose

⇨ Mannitol

⇨ Microcrystalline cellulose -Avicel

⇨ Microcrystalline cellulose silicified

⇨ Sorbitol

⇨ Starch-1500

⇨ Sucrose

⇨ Sugar (Compressible, Spheres)

⇨ Sunflower oil

⇨ Talc

⇨ Xylitol

2. Diluents for dry powder inhaler:

⇨ Lactose

⇨ Mannitol

3. Diluents for Liquids:

⇨ Maltitol [a disaccharide polyol used as a sugar substitute, produced through the hydrogenation of maltose]

⇨ Sunflower oil

Disinfectants 

(Kill germs or viruses)

⇨ Benzalkonium chloride

⇨ Benzethonium chloride

⇨ Calcium sulfate

⇨ Cresol

Disintegrants 

(To facilate a breakup or disintegration of tablet)

⇨ Disintegrants are agents added to tablet formulations to promote the breakup of the tablet into smaller fragments in an aquous environment

⇨ Promoting a more rapid release of the drug substance

⇨ Alginic acid

⇨ Bentonite

⇨ Calcium Alginate

⇨ Crosspovidone

⇨ Crosscarmellose

⇨ Polyvinyl pyrrolidone

⇨ Primogel

⇨ Sodium bicarbonate

⇨ Sodium carboxy methyl cellulose

⇨ Starch-1500

Superdisintegrant 

(Swell up to 10 fold within 30 seconds)

⇨ It swell up to ten fold within 30 seconds when contact with water

⇨ Crosspovidone

⇨ Crosscarmellose

⇨ Primogel (Sodium starch glycolate)

⇨ Sodium carboxy methyl cellulose (Ac-Di-Sol)

⇨ Starch-1500

Dissolution Enhancers 

(Enhance dissolution rate)

⇨ Fructose

⇨ Povidone [ A powdered form of polyvinylpyrrolidone that is used as a dispersing and suspending agent in drugs.]

⇨ Surfactants

Dissolution retardant 

(Used when control release of drug is required)

Waxy materials such as-

⇨ Stearic acid

⇨ Sodium Stearate

Emulsifying agents

⇨ Calcium alginate

⇨ Lecithin

⇨ Sodium phosphate

Fillers

⇨ Calcium carbonate

⇨ Glucose

⇨ Lactose

⇨ Magnesium stearate

⇨ Mannitol

⇨ Sorbitol

⇨ Sucrose

Reason for using fillers

⇨ Fill out the size of a tablet or capsule, making it practical to produce and convenient for the consumer to use.

Film forming agents

⇨ Ammonium alginate

⇨ Chitosan

⇨ Copovidone

⇨ Ethyl cellulose

⇨ Hydroxyethyl cellulose

⇨ Hydroxypropyl cellulose

⇨ Gelatin

Glidants 

(Improve flow properties)

⇨ Improve flow properties of the material

⇨ Calcium silicate

⇨ Powdered cellulose

⇨ Magnesium silicate

⇨ Colloidal silicon dioxide

⇨ Starch (as additional value of disintegrant)- up to 10%

⇨ Talc (Superior to starch)

Reason for using Glidants

To improve flow properties of material during early stages of compression

Humectants

Ammonium alginate

Propylene glycol

Reason for using humectants

Absorb moisture

Prevent degradation of API by moisture.

Hygroscopic Materials (Maintain proper moisture level)

⇨ Methylcellulose

⇨ Polyethylene glycol-4000

⇨ Sorbitol

Lubricants

⇨ Act by reducing friction by interposing an intermediate layer between the tablet constituents and the die wall during compression and ejection.

1.Water insoluble lubrcants

Calcium stearate

Magnesium stearate

Sodium stearate

Zinc Stearate

Talc

Waxes

Liquid paraffin

2. Water soluble lubricants

Boric acid

Sodium acetate

Sodium benzoate

Sodium oleate

Sodium lauryl sulfate

Magnesium lauryl sulfate

Reason for using lubricants

For reducing friction between tablet constituents and die wall during compression and ejection by interposing an intermediate layer btw tablet & die wall

Plasticizers (for soft, flexibility, easily bent,  mold)

Acetyltributyl citrate

Benzyl benzoate

Polyethylene glycol

Propylene glycol

Tween-80

Reason for using Plasticizer

For increase pliability (Flexibility)

Plymers

1. Natural polymers

2. Synthetic polymers

1. Natural Polymers

Gelatin

Methyl Cellulose

Ethyl Cellulose

Hydroxyethyl Cellulose

Hydroxyethyl-methyl cellulose

Hydroxypropyl Cellulose

Hydroxyethylpropyl cellulose

2. Synthetic Polymers

Polyacrylic acid

Poly vinyl acetate phthalate

Poly vinyl alcohol

Polyvinyl Pyrrolidone

Preservatives (Prevent growth of microorganism in tablet formulation)

Alcohol

Benzalkonium chloride

Benzoic acid

Benzyl alcohol (vagnal)

Boric acid

Butyl paraben

Butyl para hydroxy benzoate

Cresol (For intradermal)

Benzyl paraben

Butyl paraben

Methyl paraben

Propyl paraben

Sodium benzoate (For Dermal)

Sodium bisulfite

Sodium metabisulfite

For Otic: Benzalkonium chloride

For vaginal: Benzoic acid, Benzyl alcohol

For Rectal: Benzoic acid, Butyl paraben

For intradermal: Cresol

For Dermal: Sodium benzoate

Antimicrobial Preservatives

Alcohol

Benzalkonium chloride

Benzoic acid

Boric acid

Preservatives for Parenteral products

Benzyl alcohol

Chlorobutanol

Methyl paraben

Propyl paraben

Phenol

Sodium bisulphite

Sodium metabisulphite

Preservatives for Opthalmic products

Benzalkonium chloride

Methyl paraben

Propyl paraben

Thiomersal [used as an antiseptic and antifungal agent, especially in vaccines.]

Preservatives for Oral products

Methyl paraben

Propyl paraben

Sodium benzoate

Preservatives for Creams

Benzoic acid

Benzyl alcohol

Chlorocresol

Methyl paraben

Propyl paraben

Sorbic acid [an unsaturated aliphatic carboxylic acid]

Reason for using Preservatives

To prevent the growth of microorganisms in tablet formulation.

Solubilizing agents

Benzalkonium chloride

Benzethonium chloride

Benzyl alcohol

Benzyl benzoate

Stabilizing agents

Bentonite

Calcium alginate

Carboxymethylcellulose calcium

Carboxymethylcellulose sodium

Sodium alginate

Emulsion stabilizers

Colloidal silicon dioxide

Polyethylene glycol

Polymethylvinyl ether

Sequestering agents

sequestering agent is an organic compound capable of linking metal ions or molecules together to form complex ring-like

Citric acid

Potassium citrate

Phosphoric acid

Sodium phosphate

Surfactants

Sodium dodecyl sulfate

Sodium lauryl sulfate

Suspending agents

Acacia

Agar

Alginic acid

Calcium stearate

Gelatin

Sustained release agents

Acetyltributyl citrate

Agar

Alginic acid

Castor oil

Sweetening Agents

Aspartame

Cyclamate

Saccharin

Dextrose

Glycerin

Maltose

Mannitol

Sorbitol

Thickening agents

Agar

Ammonium alginate

Calcium alginate

Hydroxyethyl cellulose

Hydroxypropyl cellulose

Viscosity increasing agent

Bentonite

Sodium alginate

Methyl cellulose

Carboxy Methyl Cellulose

Wetting agents

⇨ Aid water uptake during disintegration and assist drug dissolution.

Benzalkonium chloride

Benzethonium chloride

Sodium lauryl sulfate (SLS)

Sodium diisobutyl sulfosuccinate

Reason for using Adsorbents

Capable of retaining large quantities of liquids without becoming wett

Reason for using Antiadherents (Silicon dioxide)

To prevent sticking & picking problem of tablet to punches and die walls

Reason for using Anticaking agent

⇨ Prevent cake formation

Reason for using Binder

Binders are used in tablet formulations to make powders more compressible and produce tablets that are more resistant to breakage during handling.

For holding ingredients in tablet together.

For require necessary mechanical strength 

To make powder more compressible

To produce tablets that are more resistant to breakage during handling

Binding agent গুলো Granulating solution এর সাথে যোগ না করে Dry powder এর সাথে যোগ করার কারণ

⇨ To overcome pouring difficulites of granulating solution

Reason for using Buffers

To maintain a required pH

Reason for using Chelating agents

To inactivate catalytic activity in the oxidation of medicaments.

Reason for using Coloring agents

⇨  Masking of Off color drugs

⇨ Product identification

⇨ Production of more elegant product

Reason for using Disintegrants

For promote the breakup of tablet into smaller fragments in aqueous environment⇨ increase surface area⇨ Promote more rapid release of drug substances.

Reason for using Superdisintegrants

For swelling tablets up to ten fold within 30 seconds when contact with water

Reason for using dissolution enhancers

To enhance the dissolution rate of API

Reason for using dissolution retardants

for controlled release of drug

⇨ To stablies an emulsion by reducing interfacial tension between two immisvible liquids

Reason for using Flavoring agents

⇨ To increase patient acceptance.

⇨ To mask unpleasant tasting 

Reason for using sufractants

⇨ Decrease the surface tension or interfacial tension between two liquids, a liquid and a gas, or a liquid and a solid.

⇨ Surfactants may function as emulsifiers, wetting agents, detergents, foaming agents, or dispersants.

Reason for using suspending agents

increase the viscosity of the dispersion medium to slow down the sedimentation speed of particles, 

and adsorb on the surface of the particles to become a barrier to prevent the aggregation and agglomeration of particles.

Reason for using Wetting agents

To aid water uptake during disintegration and assist drug dissolution

Used when hydrophobic drugis to be formulated into tablet

Function of various types of Excipents

Function of Ammonium Alginate

⇨ Diluent

⇨ Film former

⇨ Humectant

⇨ Emulsifier

⇨ Thickening agent.

⇨ Stabilizing agent

Functions of Calcium alginate

⇨ Disintegrant

⇨ Emulsifying agent

⇨ Thickening agent

⇨ Stabilizing agent

Function of Sodium alginate

⇨ Binder

⇨ Disintegrant

⇨ Suspending agent

⇨ Viscosity increasing agent.

⇨ Stabilizing agent

Function of Colloidal Silicon dioxide

⇨ Antiadharent 

⇨ Adsorbents

⇨ Anticaking agent

⇨ Glidant

⇨ Disintegrant

⇨ Emulsion stabilizer

⇨ Suspending agent

⇨ Thermal Stabilizer

⇨ Viscosity increasing agent

Functions of Carbon dioxide

⇨ Aerosol Propellant

⇨ Air Displacement

Function of Calcium Sulfate (CaSO4)

⇨ Diluent 

⇨ Desiccant (Used as a drying agent)

Function of Calcium Stearate

⇨ Lubricant

Function of Magnesium stearate

⇨ Lubricant

Function of Zinc Stearate

⇨ Lubricant

Function of Magnesium Stearate

⇨ Lubricant

Function of Benzalkonium chloride

⇨ Preservative

⇨ Antiseptic

⇨ Disinfectant

⇨ Wetting agent

⇨ Solubilizing agent

Function of Benzethonium chloride

⇨ Preservative

⇨ Antiseptive (Stop or slow down the growth of microorganisms)

⇨ Disinfectant

Function Sodium Benzoate

⇨ Preservative

⇨ Lubricant

Functions of Bentonite

⇨ Adsorbent (Capable of retaining large quantities of liquids without becoming wett)

⇨ Suspending agent

⇨ Viscosity increasing agent

⇨ Stabilizing agent

Function of Butyl Paraben

⇨ Preservative

Function of Methyl Paraben

⇨ Preservative

Function of Propyl paraben

⇨ Preservative

Function of Boric acid

⇨ Preservative

Function of Butyle hydroxy anisole (BHA)

⇨ Antioxidant

Functions of Butyle hydroxy toluene (BHT)

⇨ Antioxidant

Functions of Calcium phosphate dibasic

⇨ Diluent

Functions of Calcium Phosphate Tribasic

⇨ Diluent

⇨ Buffering agent

⇨ Anticaking agent

⇨ Glidant

Functions of Calcium Carbonate

⇨ Diluent

⇨ Buffering agent

⇨ Coating agent

Function of Various types of Cellulose

Function of Powdered Cellulose

⇨ Diluent

⇨ Adsorbent

⇨ Glidant

⇨ Disintegrant

⇨ Suspending agent

Function of Microcrystaline Cellulose

⇨ Diluent

⇨ Adsorbent

⇨ Disintegrant

⇨ Suspending agent

Functions of Carboxy methyl Cellulose

⇨ Binder

⇨ Coating agent

⇨ Disintegrant

⇨ Water absorbing agent

⇨ Suspending agent

⇨ Viscosity increasing agent

⇨ Stabilizing agent

Function of Methyl cellulose

⇨ Binder

⇨ Coating agent

⇨ Disintegrant

⇨ Emulsifying agent

⇨ Suspending agent

⇨ Viscosity increasing agent

Function of Copovidone

⇨ Film forming agent

⇨ Binder

⇨ Granulating agent

Function of Cresol

⇨ Antimicrobial preservative

⇨ Disinfectant

Function of Crospovidone

⇨ Superdisintegrant

Function of Croscarmelose

⇨ Super-disintegrant

Functions of Magnesium Silicate

⇨ Anticaking agent

⇨ Glidant

Functions of Magnesium Trisilicate

⇨ Anticaking agent

⇨ Glidant

Function of Shellac

⇨ Coating agent

Function of Talc

⇨ Anticaking agent

⇨ Glidant

⇨ Lubricant

⇨ Diluent

Function of Tween 80/ Polysorbate 80

⇨ Emulsifying agent

⇨ Non-ionic surfactant

⇨ Dispersing/Suspending agent

⇨ Wetting agent

⇨ Solubilizing agent

Function of Tragacanth

⇨ Suspending agent (Increase viscosity of dispersion medium)

⇨ Viscosity increasing agent

Function of Zein

⇨ Binder

⇨ Coating agent

⇨ Extended release agent