EXCIPIENT PROFILE

CHAPTER-5
EXCIPIENT PROFILE

Magnesium Stearate

Nonproprietary Name: Magnesium Stearate

Synonyms:Magnesium octadecanoate; octadecanoic acid, magnesium salt.

Chemical Name: Octadecanoic acid magnesium salt

Empirical Formula: C36H70MgO4

Molecular Weight: 591.24

Functional Category: Tablet and capsule lubricant.

Description: Magnesium stearate is a very fine, light white, precipitated or milled,

impalpable powder of low bulk density, having a faint odor of stearic acid and a
characteristic taste. The powder is greasy to the touch and readily adheres to the skin.

Solubility: Practically insoluble in ethanol, ethanol (95 %), ether and water; slightly
soluble in warm benzene and warm ethanol (95 %).

Stability and Storage Conditions: Magnesium stearate is stable and should be stored in
a well-closed container in a cool, dry place.

Applications: 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.

Related Substances: Calcium stearate; magnesium aluminum silicate; stearic acid; zinc
stearate.

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Microcrystalline cellulose

Nonproprietary Name: Microcrystalline Cellulose.

Synonyms: Avicel PH; celex; cellulose gel; crystalline cellulose; emcocel; tabulose.

Chemical Name: Cellulose

Empirical Formula: (C6H10O5) n where n ~ 220

Molecular Weight: ~36 000mg

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

Description: Microcrystalline cellulose is a purified, partially depolymerized cellulose

that occurs as a white, odorless, tasteless, crystalline powder composed of porous
particles. It is commercially available in different particle sizes and moisture grades that
have different properties and applications.

Solubility: Slightly soluble in 5 % w/v sodium hydroxide solution; practically insoluble

in water, dilute acids, and most organic solvents.

Stability and Storage Conditions: Microcrystalline cellulose is a stable though

hygroscopic material. The bulk material should be stored in a well-closed container in a
cool, dry place.

Applications: 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. It also has some lubricant and disintegrant
properties that make it useful in tableting. It is also used in cosmetics and food products.

Related Substances: Microcrystalline cellulose and carrageenan; microcrystalline

cellulose and carboxy methyl cellulose sodium; microcrystalline cellulose and guar gum;
powdered cellulose.

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Sodium Bicarbonate

Nonproprietary Names: Sodium bicarbonate, Natrii hydrogenocarbonas

Synonyms: Baking soda,E500, effer-soda, monosodium carbonate, sodium acid

carbonate, sodium hydrogen carbonate.

Chemical Name and CAS Registry Number : Carbonic acid monosodium salt

[144- 558]

Empirical Formula and Molecular Weight : NaHCO3 84.01

Functional Category : Alkalizing agent, therapeutic agent.

Description: Sodium bicarbonate occurs as an odorless, white, crystalline powder with a

saline, slightly alkaline taste. The crystal structure is monoclinic prisms. Grades with
different particle sizes, from a fine powder to free-flowing uniform granules, are
commercially available.

Stability and Storage Conditions: When heated to about 50°C, Sodium bicarbonate
begins to dissociate into carbon dioxide, sodium carbonate, and water; on heating to 250–
300°C, for a short time, Sodium bicarbonate is completely converted into anhydrous
sodium carbonate. The effects of relative humidity and temperature on the moisture
sorption and stability of Sodium bicarbonate powder have been investigated. detrimental
effects on stability.

Applications: Sodium bicarbonate is generally used in pharmaceutical formulations as a

source of carbon dioxide in effervescent tablets and granules. It is also widely used to
produce or maintain an alkaline pH in a preparation. Tablets may also be prepared with
Sodium bicarbonate alone since the acid of gastric fluid is sufficient to cause
effervescence and disintegration. Sodium bicarbonate is also used in tablet formulations
to buffer drug molecules that are weak acids, thereby increasing the rate of tablet
dissolution and reducing gastric irritation.

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Bentonite

Nonproprietary Names: Bentonite

Synonyms: ilkinite;wilkonite;Optigel WM

Chemical name: Sodium bentonite; Bentonite, sodian;

Emperical formula: Al2H2Na2O13Si4

Molecular weight: 422.286

Functional category: Adsorbent; stabilizing agent; suspending agent; viscosity

increasing agent

Description: Bentonite is a crystalline, claylike mineral, and is available as an odorless,

pale buff, or cream to grayish-colored fine powder, which is free from grit. It consists of
particles about 50–150 mm in size along with numerous particles about 1–2 mm.
Microscopic examination of samples stained with alcoholic methylene blue solution
reveals strongly stained blue particles. Bentonite may have a slight earthy taste.

Stability and storage conditions: Bentonite is hygroscopic, and sorption of atmospheric

water should be avoided. Aqueous bentonite suspensions may be sterilized by
autoclaving. The solid material may be sterilized by maintaining it at 170 0C for 1 hour
after drying at 1080C. Bentonite should be stored in an airtight container in a cool, dry
place.

Applications: Bentonite is a naturally occurring hydrated aluminum silicate used

primarily in the formulation of suspensions, gels, and sols, for topical pharmaceutical
applications. It is also used to suspend powders in aqueous preparations and to prepare
cream bases containing oil-in-water emulsifying agents. Bentonite may also be used in
oral pharmaceutical preparations, cosmetics, and food products, see Section 18. In oral

preparations, bentonite, and other similar silicate clays, can be used to adsorb cationic
drugs and so retard their release.Adsorbents are also used to mask the taste of certain
drugs. Bentonite has been investigated as a diagnostic agent for magnetic resonance
imaging. Therapeutically, bentonite has been investigated as an adsorbent for lithium
poisoning

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HPMC

Non proprietary name: Hydroxyethylmethylcellulose, Methylhydroxyethyl cellulosum

Synonyms: Cellulose, 2-hydroxyethyl methyl ester

Chemical name: Hydroxyethylmethylcellulose

Emperical formula: O-methylated and O-(2-hydroxyethylated) cellulose.

Molecular weight: 1261.45

Functional category: Coating agent; suspending agent; tablet binder; thickening

agent; viscosity-increasing agent.

Description: A white, yellowish-white or grayish-white powder or granules,

hygroscopic after drying.

Stability and storage conditions: Hydroxyethylmethyl cellulose is hygroscopic and

should therefore be stored under dry conditions away from heat.

Applications: Hydroxyethylmethyl cellulose is used as an excipient in a wide range of

pharmaceutical products, including oral tablets and suspensions and topical gel
preparations. 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.

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ETHYL CELLULOSE

Non proprietary name: Ethylcellulose, Ethylcellulosum

Synonyms: Aquacoat ECD; Aqualon; E462

Chemical name: Cellulose ethyl ether

Emperical formula: C12H23O6(C12H22O5)nC12H23O5

Molecular weight: 454.51

Functional category: Coating agent; flavoring fixative; tablet binder; tablet filler;

viscosity-increasing agent.

Description: Ethylcellulose is a tasteless, free-flowing, white to light tan colored powder

Stability and storage conditions: Ethylcellulose is a stable, slightly hygroscopic

material. It is chemically resistant to alkalis, both dilute and concentrated, and to salt
solutions, although it is more sensitive to acidic materials than are cellulose esters.

Ethylcellulose is subject to oxidative degradation in the presence of sunlight or UV light

at elevated temperatures. This may be prevented by the use of antioxidant and chemical
additives that absorb light in the 230–340nm range. Ethylcellulose should be stored at a
temperature not exceeding 328C (908F) in a dry area away from all sources of heat. It
should not be stored next to peroxides or other oxidizing agents.

Applications: The main use of ethylcellulose in oral formulations is as a hydrophobic

coating agent for tablets and granules.Ethylcellulose coatings are used to modify the
release of a drug, to mask an unpleasant taste, or to improve the stability of a formulation;
for example, where granules are coated with ethylcellulose to inhibit oxidation.
Modifiedrelease tablet formulations may also be produced using ethylcellulose as a
matrix former.(11–14) Ethylcellulose, dissolved in an organic solvent or solvent mixture,
can be used on its own to produce water-insoluble film

GELATIN
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Non proprietary name: Gelatin, Gelatina

Synonyms: Byco, Cryogel

Chemical name: Gelatin

Functional category: Coating agent; film-former; gelling agent; suspending agent;

tablet binder; viscosity-increasing agent.

Description: Gelatin occurs as a light-amber to faintly yellow-colored,vitreous, brittle

solid. It is practically odorless and tasteless and is available as translucent sheets and
granules, or as a powder.

Stability and storage conditions: Dry gelatin is stable in air. Aqueous gelatin solutions
are also stable for long periods if stored under cool, sterile conditions. At temperatures
above about 508C, aqueous gelatin solutions may undergo slow depolymerization and a
reduction in gel strength may occur on resetting. Depolymerization becomes more rapid
at temperatures above 658C, and gel strength may be reduced by half when a solution is
heated at 808C for 1 hour. The rate and extent of depolymerization depends on the
molecular weight of the gelatin, with a lower-molecular-weight material decomposing
more rapidly.

Applications: Gelatin is widely used in a variety of pharmaceutical formulations,

including its use as a biodegradable matrix material in an implantable delivery system,(1)
although it is most frequently used to form either hard or soft gelatin capsules.(2–4)
Gelatin capsules are unit-dosage forms that are filled with an active drug and are
generally designed for oral administration. Although gelatin is poorly soluble in cold
water, a gelatin capsule will swell in gastric fluid to rapidly release its contents. Hard
capsules are manufactured in two pieces by dipping stainless steel pins into a gelatin
solution, which is distributed evenly around the pin. The gelatin is then set with a blast of
chilled air and dried to remove moisture. The capsule halves are then removed, trimmed
and filled before they are joined and closed with a tamper-evident seal. The USPNF 23
permits gelatin that is used to produce hard capsules to contain various coloring agents,
antimicrobial preservatives, and sodium lauryl sulfate. Manufacturers may also add a
hardening agent, such as sucrose, to hard gelatin capsules. Capsules varying in size from
0.13 to 1.37mL volume are commercially available.

Lactose

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Non proprietary name: Anhydrous lactose,Anhydrous lactose,Lactosum anhydricum

Synonyms: Anhydrous Lactose NF 60M; Anhydrous Lactose

Chemical name: O-b-D-galactopyranosyl-(1!4)-b-D-glucopyranose

Emperical formula: C12H22O11

Molecular weight: 342.30

Functional category: Binding agent; directly compressible tableting excipient;

lyophilization aid; tablet and capsule filler.

Description: Lactose occurs as white to off-white crystalline particles or powder. Several

different brands of anhydrous lactose are commercially available which contain
anhydrous b-lactose and anhydrous a-lactose. Anhydrous lactose typically contains 70–
80% anhydrous b-lactose and 20–30% anhydrous alactose.Stability and storage
conditions

Applications: Anhydrous lactose is widely used in direct compression tableting

applications and as a tablet and capsule filler and binder. Anhydrous lactose can be used
with moisture-sensitive drugs due to its low moisture content.

Talc

Non proprietary name: Purified Talc, Talcum

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Synonyms: Altalc; E553b; hydrous magnesium calcium silicate;

Chemical name: Talc

Emperical formula: Mg6(Si2O5)4(OH)4

Molecular weight: 379.25

Functional category: Anticaking agent; glidant; tablet and capsule diluent; tablet and
capsule lubricant.

Description: Talc is a very fine, white to grayish-white, odorless, impalpable,

unctuous, crystalline powder. It adheres readily to the skin and

is soft to the touch and free from grittiness.

Stability and storage conditions: Talc is a stable material and may be sterilized by
heating at 1600C for not less than 1 hour. It may also be sterilized by exposure to ethylene
oxide or gamma irradiation.(10) Talc should be stored in a well-closed container in a
cool, dry place.

Applications: Talc was once widely used in oral solid dosage formulations as a lubricant
and diluent, 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, in a novel powder coating for extended-release
pellets, and as an adsorbant.

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