Pharmaceutical Excipients and their role

 Pharmaceutical Excipients and their uses:

1. Acacia
Synonyms
Acaciae gummi; acacia gum; arabic gum; E414; gum acacia; gummi africanum; gum arabic;
gummi arabicum; gummi mimosae; talha gum.

Functional Category
Emulsifying agent; stabilizing agent; suspending agent; tablet binder; viscosity-increasing agent.

Applications in Pharmaceutical Formulation or Technology:

Acacia is mainly used in oral and topical pharmaceutical formulations as a suspending and
emulsifying agent, often in combination with tragacanth. It is also used in the preparation of
pastilles and lozenges, and as a tablet binder, although if used incautiously it can produce
tablets with a prolonged disintegration time. Acacia has also been evaluated as a bioadhesive;
(1) and has been used in novel tablet formulations, (2) and modified release tablets. (3) Acacia
is also used in cosmetics, confectionery, food products, and spray-dried flavors.

Uses of Acacia
Use Concentration (%)
Emulsifying agent 10–20
Pastille base 10–30
Suspending agent 5–10
Tablet binder 1–5

2. Cellulose, Microcrystalline
Synonyms
Avicel PH; Cellets; Celex; cellulose gel; hellulosum microcristallinum; Celphere; Ceolus KG;
crystalline cellulose; E460; Emcocel; Ethispheres; Fibrocel; MCC Sanaq; Pharmacel; Tabulose;
Vivapur

Functional Category
Adsorbent; suspending agent; tablet and capsule diluent; tablet disintegrant.

Applications in Pharmaceutical Formulation or Technology

Microcrystalline cellulose is widely used in pharmaceuticals, primarily as a binder/diluent in oral
tablet and capsule formulations where it is used in both wet-granulation and direct-compression
processes. (1–7) In addition to its use as a binder/diluent, microcrystalline cellulose also has
some lubricant (8) and disintegrant properties that make it useful in tableting. Microcrystalline
cellulose is also used in cosmetics and food
products;

Uses of microcrystalline cellulose.

Use Concentration (%)
Adsorbent 20–90
Antiadherent 5–20
Capsule binder/diluent 20–90
Tablet disintegrant 5–15
Tablet binder/diluent 20–90

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Pharmaceutical Excipients and their role

3. Copovidone
Synonyms
Acetic acid vinyl ester, polymer with 1-vinyl-2-pyrrolidinone; copolymer of 1-vinyl-2-pyrrolidone
and vinyl acetate in a ratio of 3:2 by mass; copolyvidone; copovidonum; Kollidon VA 64;
Luviskol VA; Plasdone S-630; poly (1-vinylpyrrolidone-co-vinyl acetate); polyvinylpyrrolidone-
vinyl acetate copolymer; PVP/VA; PVP/VA copolymer.

Functional Category
Film-forming agent; granulation aid; tablet binder.

Applications in Pharmaceutical Formulation or Technology

Copovidone is used as a tablet binder, a film-former, and as part of the matrix material used in
controlled-release formulations. In tableting, copovidone can be used as a binder for direct
compression (1–3) and as a binder in wet granulation. (4,5) Copovidone is often added to
coating solutions as a film-forming agent. It provides good adhesion, elasticity, and hardness,
and can be used as a moisture barrier.

Uses of copovidone.
Use Concentration (%)
Film-forming agent 0.5–5.0
Tablet binder, direct compression 2.0–5.0
Tablet binder, wet granulation 2.0–5.0

4. Corn Starch and Pregelatinized Starch

Synonyms
StarCap 1500.

Functional Category
Binding agent; compression aid; disintegrant; tablet and capsule diluent; tablet and capsule
filler.

Applications in Pharmaceutical Formulation or Technology

Corn starch and pregelatinized starch can be used in both capsules and tablets to improve
flowability, enhance disintegration and improve hardness.

5. Ethyl Acetate
Synonyms
Acetic acid ethyl ester; acetic ester; acetic ether; acetoxyethane; aethylis acetas; aethylium
aceticum; ethyl ethanoate; ethylis acetas; vinegar naphtha.

Functional Category
Flavoring agent; solvent.

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Pharmaceutical Excipients and their role
Applications in Pharmaceutical Formulation or Technology
In pharmaceutical preparations, ethyl acetate is primarily used as a solvent, although it has also
been used as a flavoring agent. As a solvent, it is included in topical solutions and gels, and in
edible printing inks used for tablets.

6. Gelatin
Synonyms
Byco; Cryogel; E441; gelatina; gelatine; Instagel; Kolatin; Solugel; Vitagel.

Functional Category
Coating agent; film-forming agent; gelling agent; suspending agent; tablet binder; viscosity-
increasing agent.

7. Colloidal Silica
Synonyms
Aerosil R972; silica dimethyl silylate; silica hydrophobica colloidalis; silicic acid, silylated; silicon
dioxide, silanated.

Functional Category
Anticaking agent; emulsion stabilizer; glidant; suspending agent; thermal stabilizer; viscosity-
increasing agent.

Applications in Pharmaceutical Formulation or Technology

Hydrophobic colloidal silica has nano-sized primary particles and a large specific surface area,
1)which provide desirable flow characteristics in dry powders used in tableting (2–4) and
capsule filling. (3) The hydrophobic grades absorb less moisture (5) and may offer an
advantage in moisture-sensitive formulations.

8. Hydroxyethyl Cellulose
Synonyms
Cellosize HEC; cellulose hydroxyethyl ether; cellulose 2-hydroxyethyl ether; cellulose
hydroxyethylate; ethylhydroxy cellulose; ethylose; HEC; HE cellulose; hetastarch; 2-
hydroxyethyl cellulose ether; hydroxyethylcellulosum; hydroxyethyl ether cellulose; hydroxyethyl
starch; hyetellose; Natrosol; oxycellulose; Tylose H; Tylose PHA.

Functional Category
Coating agent; suspending agent; tablet binder; thickening agent; viscosity-increasing agent.

Applications in Pharmaceutical Formulation Technology

Hydroxyethyl cellulose is a nonionic, water-soluble polymer widely used in pharmaceutical
formulations. It is primarily used as a thickening agent in ophthalmic (1) and topical
formulations, (2) although it is also used as a binder (3) and film-coating agent for tablets. (4) It
is present in lubricant preparations for dry eye, contact lens care, and dry mouth. (5) The
concentration of hydroxyethyl cellulose used in a formulation is dependent upon the solvent and
the molecular weight of the grade. Hydroxyethyl cellulose is also widely used in cosmetics.

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Pharmaceutical Excipients and their role
9. Hydroxyethylmethyl Cellulose
Synonyms
Cellulose, 2-hydroxyethyl methyl ester; Culminal MHEC; HEMC; hydroxyethyl methylcellulose;
hymetellose; MHEC; methylhydroxyethylcellulosum; Tylopur MH; Tylopur MHB; Tylose MB;
Tylose MH; Tylose MHB.

Functional Category
Coating agent; suspending agent; tablet binder; thickening agent; viscosity-increasing agent.

Applications in Pharmaceutical Formulation or Technology

Hydroxyethylmethyl cellulose is used as an excipient in a wide range of pharmaceutical
products, including oral tablets and suspensions, and topical gel preparations. (1) It has similar
properties to methylcellulose, but the hydroxyethyl groups make it more readily soluble in water
and solutions are more tolerant of salts and have a higher coagulation temperature.

10. Hypromellose
Synonyms
Benecel MHPC; E464; hydroxypropyl methylcellulose; HPMC; hypromellosum; Methocel;
methylcellulose propylene glycol ether; methyl hydroxypropylcellulose; Metolose; MHPC;
Pharmacoat; Tylopur; Tylose MO.

Functional Category
Bioadhesive material; coating agent; controlled-release agent; dispersing agent; dissolution
enhancer; emulsifying agent; emulsion stabilizer; extended-release agent; film-forming agent;
foaming agent; granulation aid; modified-release agent; mucoadhesive; release-modifying
agent; solubilizing agent; stabilizing agent; suspending agent; sustained-release agent; tablet
binder; thickening agent; viscosity-increasing agent

Applications in Pharmaceutical Formulation or Technology

Hypromellose is widely used in oral, ophthalmic, nasal, and topical pharmaceutical formulations.
In oral products, hypromellose is primarily used as a tablet binder, (1) in film-coating, (2–7) and
as a matrix for use in extended release tablet formulations. (8–12) Concentrations between 2%
and 5% w/w may be used as a binder in either wet- or dry-granulation processes. High-viscosity
grades may be used to retard the release of drugs from a matrix at levels of 10–80% w/w in
tablets and
capsules. Hypromellose is also used in liquid oral dosage forms as a suspending and/or
thickening agent at concentrations ranging from 0.25–5.0%.

11. Lanolin
Synonyms
Adeps lanae; cera lanae; E913; lanolina; lanolin anhydrous; Protalan anhydrous; purified
lanolin; refined wool fat.

Functional Category
Emulsifying agent; ointment base.

Applications in Pharmaceutical Formulation or Technology

Lanolin is widely used in topical pharmaceutical formulations and cosmetics. Lanolin may be
used as a hydrophobic vehicle and in the preparation of water-in-oil creams and ointments.
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Pharmaceutical Excipients and their role
When mixed with suitable vegetable oils or with soft paraffin, it produces emollient creams that
penetrate the skin and hence facilitate the absorption of drugs. Lanolin mixes with about twice
its own weight of water, without separation, to produce stable emulsions that do not readily
become rancid on storage.

12. Lecithin
Synonyms
E322; egg lecithin; LSC 5050; LSC 6040; mixed soybean phosphatides; ovolecithin; Phosal 53
MCT; Phospholipon 100 H; ProKote LSC; soybean lecithin; soybean phospholipids; Sternpur;
vegetable lecithin.

Functional Category
Emollient; emulsifying agent; solubilizing agent.

Applications in Pharmaceutical Formulation or Technology

Lecithins are used in a wide variety of pharmaceutical applications; see Table I. They are also
used in cosmetics (2) and food products. Lecithins are mainly used in pharmaceutical products
as dispersing, emulsifying, and stabilizing agents, and are included in intramuscular and
intravenous injections, parenteral nutrition formulations, and topical products such as creams
and ointments.
Lecithins are also used in suppository bases, (3) to reduce the brittleness of suppositories, and
have been investigated for their absorption-enhancing properties in an intranasal insulin
formulation. (4) Lecithins are also commonly used as a component of enteral and parenteral
nutrition formulations.

13. Magnesium Stearate

Synonyms
Dibasic magnesium stearate; magnesium distearate; magnesia stearas; magnesium
octadecanoate; octadecanoic acid, magnesium salt; stearic acid, magnesium salt; Synpro 90.

Functional Category
Tablet and capsule lubricant.

Applications in Pharmaceutical Formulation or Technology

Magnesium stearate is widely used in cosmetics, foods, and pharmaceutical formulations. It is
primarily used as a lubricant in capsule and tablet manufacture at concentrations between
0.25% and 5.0% w/w. It is also used in barrier creams.

14. Mannitol
Synonyms
Cordycepic acid; C*PharmMannidex; E421; Emprove; manna sugar; D-mannite; mannite;
mannitolum; Mannogem; Pearlitol.

Functional Category
Diluent; plasticizer; sweetening agent; tablet and capsule diluent; therapeutic agent; tonicity
agent.

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Pharmaceutical Excipients and their role
Applications in Pharmaceutical Formulation or Technology
Mannitol is widely used in pharmaceutical formulations and food products. In pharmaceutical
preparations it is primarily used as a diluent (10–90% w/w) in tablet formulations, where it is of
particular value since it is not hygroscopic and may thus be used with moisture-sensitive active
ingredients. (1,2) Mannitol may be used in direct-compression tablet applications, (3,4) for which
the granular and spray-dried forms are available, or in wet granulations. (5,6) Granulations
containing mannitol have the advantage of being dried easily. Specific tablet applications
include antacid preparations, glyceryl trinitrate tablets, and vitamin preparations. Mannitol is
commonly used as an excipient in the manufacture of chewable tablet formulations because of
its negative heat of solution, sweetness, and ‘mouth feel’.

15. Methylcellulose
Synonyms
Benecel; Cellacol; Culminal MC; E461; Mapolose; Methocel; methylcellulosum; Metolose;
Tylose; Viscol.

Functional Category
Coating agent; emulsifying agent; suspending agent; tablet and capsule disintegrant; tablet
binder; viscosity-increasing agent.

Applications in Pharmaceutical Formulation or Technology

Methylcellulose is widely used in oral and topical pharmaceutical formulations. In tablet
formulations, low- or medium-viscosity grades of methylcellulose are used as binding agents,
the methylcellulose being added either as a dry powder or in solution. (1–3) Highviscosity
grades of methylcellulose may also be incorporated in tablet formulations as a disintegrant. (4)
Methylcellulose may be added to a tablet formulation to produce sustained-release
preparations.

16. Propylene Glycol

Synonyms
1,2-Dihydroxypropane; E1520; 2-hydroxypropanol; methyl ethylene glycol; methyl glycol;
propane-1,2-diol; propylenglycolum.

Functional Category
Antimicrobial preservative; disinfectant; humectant; plasticizer; solvent; stabilizing agent; water-
miscible cosolvent.

Applications in Pharmaceutical Formulation or Technology

Propylene glycol has become widely used as a solvent, extractant, and preservative in a variety
of parenteral and nonparenteral pharmaceutical formulations. It is a better general solvent than
glycerin and dissolves a wide variety of materials, such as corticosteroids, phenols, sulfa drugs,
barbiturates, vitamins (A and D), most alkaloids, and many local anesthetics. As an antiseptic it
is similar to ethanol, and against molds it is similar to glycerin and only slightly less effective
than ethanol. Propylene glycol is commonly used as a plasticizer in aqueous film-coating
formulations. Propylene glycol is also used in cosmetics and in the food industry as a carrier for
emulsifiers and as a vehicle for flavors in preference to ethanol, since its lack of volatility
provides a more uniform flavor.

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Pharmaceutical Excipients and their role
17. Shellac
Synonyms
Blonde; Bulls Eye Shellac; CertiSeal FC 300A; Crystalac; E904; Excelacs 3-Circles; Excelacs 3-
Stars; Gifu Shellac GBN-PH; Gifu Shellac Pearl-811; lac; lacca; Mantrolac R-49; Mantrolac R-
52; Marcoat 125; Opaglos R; Sepifilm SN; SSB Aquagold; SSB 55 Pharma; SSB 56 Pharma;
SSB 57 Pharma; Swanlac.

Applications in Pharmaceutical Formulation or Technology

Shellac is widely used as a moisture barrier coating for tablets and pellets due to its low water
vapor and oxygen permeability. It has usually been applied in the form of alcoholic or aqueous
solutions (pharmaceutical glazes). However, due to stability problems with
alcoholic shellac solutions, it has had limited use in the pharmaceutical industry for modified
release or enteric coatings

Functional Category
Coating agent; encapsulating agent; film-forming agent; matrixforming agent; modified-release
agent.

18. Sodium Lauryl Sulfate

Synonyms
Dodecyl alcohol hydrogen sulfate, sodium salt; dodecyl sodium sulfate; dodecylsulfate sodium
salt; Elfan 240; lauryl sodium sulfate; lauryl sulfate, sodium salt; monododecyl sodium sulfate;
natrii laurilsulfas; sodium dodecyl sulfate; sodium n-dodecyl sulfate; sodium laurilsulfate; sodium
monododecyl sulfate; sodium monolauryl sulfate; SDS; SLS; sulfuric acid monododecyl ester,
sodium salt; Texapon K12P.

Functional Category
Anionic surfactant; detergent; emulsifying agent; skin penetrant; tablet and capsule lubricant;
wetting agent.

Applications in Pharmaceutical Formulation or Technology

Sodium lauryl sulfate is an anionic surfactant employed in a wide range of nonparenteral
pharmaceutical formulations and cosmetics; It is a detergent and wetting agent effective in both
alkaline and acidic conditions. In recent years it has found application in analytical
electrophoretic

Uses of sodium lauryl sulfate.

Use Concentration (%)
Anionic emulsifier, forms self-emulsifying bases 0.5–2.5
with fatty alcohols
Detergent in medicated shampoos 10
Skin cleanser in topical applications 1
Solubilizer in concentrations greater than critical >0.0025
micelle concentration
Tablet lubricant 1.0–2.0

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Pharmaceutical Excipients and their role

19. Sodium Stearyl Fumarate

Synonyms
Fumaric acid, octadecyl ester, sodium salt; natrii stearylis fumaras; Pruv; sodium monostearyl
fumarate.

Functional Category
Tablet and capsule lubricant.

Applications in Pharmaceutical Formulation or Technology

Sodium stearyl fumarate is used as a lubricant in capsule and tablet formulations at 0.5–2.0%
w/w concentration. (1–9) It is also used in certain food applications;

20. Starch
Synonyms
Amido; amidon; amilo; amylum; C*PharmGel; Eurylon; fecule; Hylon; maydis amylum; Melojel;
Meritena; oryzae amylum; Pearl; Perfectamyl; pisi amylum; Pure-Dent; Purity 21; Purity 826;
solani amylum; tritici amylum; Uni-Pure.

Functional Category
Tablet and capsule diluent; tablet and capsule disintegrant; tablet binder; thickening agent.

Applications in Pharmaceutical Formulation or Technology

is utilized as a binder, diluent, and disintegrant. As a diluent, starch is used for the preparation
of standardized triturates of colorants, potent drugs, and herbal extracts, facilitating subsequent
mixing or blending processes in manufacturing operations. Starch is also used in dry-filled
capsule formulations for volume adjustment of the fill matrix, (1) and to improve powder flow,
especially when using dried starches. Starch quantities of 3–10% w/w can act as an
antiadherent and lubricant in tableting and capsule filling.

21. Pregelatinized Starch

Synonyms
Amylum pregelificatum; compressible starch; C*PharmGel; Instastarch; Lycatab C; Lycatab
PGS; Merigel; National 78-1551; Pharma-Gel; Prejel; Sepistab ST200; Spress B820; Starch
1500 G; Tablitz; Unipure LD; Unipure WG220.

Functional Category
Tablet and capsule diluent; tablet and capsule disintegrant; tablet binder.

Applications in Pharmaceutical Formulation or Technology

Partially pregelatinized starch is a modified starch used in oral capsule and tablet
formulations as a binder, diluent, (2,3) and disintegrant. (4) In comparison to starch,
partially pregelatinized starch may be produced with enhanced flow and compression
characteristics such that the Pregelatinized material may be used as a tablet binder in
dry-compression or direct compression processes. (5–15) In such processes,
pregelatinized starch is self-lubricating. However, when it is used with other excipients it
pg. 8
Pharmaceutical Excipients and their role
may be necessary to add a lubricant to a formulation. Although magnesium stearate
0.25% w/w is commonly used for this purpose, concentrations greater than this may
have adverse effects on tablet strength and dissolution. Therefore, stearic acid is
generally the preferred lubricant with pregelatinized starch

22. Talc
Synonyms
Altalc; E553b; hydrous magnesium calcium silicate; hydrous magnesium silicate; Imperial;
Luzenac Pharma; magnesium hydrogen metasilicate; Magsil Osmanthus; Magsil Star;
powdered talc; purified French chalk; Purtalc; soapstone; steatite; Superiore; talcum.

Functional Category
Anticaking agent; glidant; tablet and capsule diluent; tablet and capsule lubricant.

Applications in Pharmaceutical Formulation or Technology

Talc was once widely used in oral solid dosage formulations as a lubricant and diluent, (1–3)
although today it is less commonly used. However, it is widely used as a dissolution retardant in
the development of controlled-release products. Talc is also used as a lubricant in tablet
formulations;(7) in a novel powder coating for extended-release pellets; (8) and as an
adsorbant.
Uses of talc.

Use Concentration (%)

Dusting powder 90.0–99.0
Glidant and tablet lubricant 1.0–10.0
Tablet and capsule diluent 5.0–30.0

Reference:
handbook-of-pharmaceutical-excipients-6th-edition

pg. 9