EXCIPIENT PROFILE

EXCIPIENT PROFILE
MAGNESIUM STEARATE
Synonyms : Magnesium octadecanoate; Octadecanoic acid, magnesium salt;
Stearic acid, magnesium salt.
Functional Category : Tablet and capsule lubricant.
Description : It 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.
Flowability : Poorly flowing, cohesive powder.
Melting range : 117150C (commercial samples);
126130C (high purity magnesium stearate).
Solubility : Practically insoluble in ethanol, ethanol (95%), ether and
water; slightly soluble in warm benzene and warm ethanol (95%).
Stability and Storage : It is stable and should be stored in a well-closed container
in a cool, dry place.
Incompatibilities : Incompatible with strong acids, alkalis, and iron salts. Avoid
mixing with strong oxidizing materials. It cannot be used in products containing
aspirin, some vitamins, and most alkaloidal salts.
Safety : Nontoxic following oral administration. However, oral consumption of
large quantities may produce a laxative effect or mucosal irritation.

Uses : It 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.

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CROSS POVIDONE
Nonproprietary Names
BP: Crospovidone
PhEur: Crospovidone
USP-NF: Crospovidone
Synonyms
Crospovidonum; Crospopharm; crosslinked povidone; E1202; Kollidon CL;
Kollidon CL-M; Polyplasdone XL; Polyplasdone XL-10;
polyvinylpolypyrrolidone; PVPP; 1-vinyl-2-pyrrolidinone homopolymer.
Chemical Name
1-Ethenyl-2-pyrrolidinone homopolymer [9003-39-8]
Empirical Formula and Molecular Weight
(C6H9NO)n >1 000 000
The USP32NF27 describes crospovidone as a water-insoluble synthetic
crosslinked homopolymer ofN-vinyl-2-pyrrolidinone. An exact determination of
the molecular weight has not been established because of the insolubility of the
material.
Structural Formula

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Functional Category
Tablet disintegrant.
Applications in Pharmaceutical Formulation or Technology
Crospovidone is a water-insoluble tablet disintegrant and dissolution agent used at
25% concentration in tablets prepared by directcompression or wet- and dry-
granulation methods.
It rapidly exhibits high capillary activity and pronounced hydration capacity,with
little tendency to form gels. Studies suggest that the particle size of crospovidone
strongly influences disintegration of analgesic tablets.
Larger particles provide a faster disintegration than smaller particles. Crospovidone
can also be used as a solubilityenhancer. With the technique of co-evaporation,
crospovidone can be used to enhance the solubility of poorly soluble drugs. The
drug is adsorbed on to crospovidone in the presence of a suitable solvent and the
solvent is then evaporated. This technique results in faster dissolution rate.
Description
Crospovidone is a white to creamy-white, finely divided, freeflowing, practically
tasteless, odorless or nearly odorless, hygroscopic powder.
Typical Properties
Acidity/alkalinity pH = 5.08.0 (1% w/v aqueous slurry)
Density 1.22 g/cm3
Density (bulk) seeTable II.
Density (tapped)

Table II: Density values of commercial grades of crospovidone.

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Commercial grade Density (bulk) (g/cm3) Density

(tapped) (g/cm3)
Kollidon CL 0.30.4 0.40.5
Kollidon CL-M 0.150.25 0.30.5
Polyplasdone XL 0.213 0.273
Polyplasdone XL-10 0.323 0.461
Moisture content Maximum moisture sorption is approximately 60%.
Particle size distribution Less than 400mm forPolyplasdone XL;less than 74mm
forPolyplasdone XL-10. Approximately 50% greater than 50mm and maximum of
3% greater than 250mmin size forKollidon CL. Minimum of 90% of particles are
below 15mm forKollidon CL-M.The average particle size for Crospopharmtype A
is 100mm and forCrospopharmtype Bit is 30mm.
Solubility Practically insoluble in water and most common organic solvents.
Stability and Storage Conditions
Since crospovidone is hygroscopic, it should be stored in an airtight container in a
cool, dry place.
Incompatibilities
Crospovidone is compatible with most organic and inorganic pharmaceutical
ingredients. When exposed to a high water level,crospovidone may form molecular
adducts with some materials.

SODIUM STARCH GLYCOLATE (SSG)

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1. Synonyms:
Explotab; Primogel; Vivastar. Carboxymethyl starch, sodium salt.
2. Chemical Name:
Sodium carboxymethyl starch.
3. Description:
It is a white or almost white free-flowing very hygroscopic powder. The PhEur
states that when examined under a microscope it is seen to consist of: granules
irregularly shaped, ovoid or pear-shaped, 30100 mm in size, or rounded,1035
mm in size; compoundgranules consisting of 24 components occur occasionally;
the granules have an eccentric hilum and clearly visible concentric striations.
Between crossed nicol prisms, the granules show a distinct black cross intersecting
at the hilum; small crystals are visible at the surface of the granules. The granules
how considerable swelling in contact with water.
4. Functional Category:
Tablet and capsule disintegrant.
5. Solubility:
Practically insoluble in water and insoluble in most organic solvents.
6. Incompatibilities:
Sodium starch glycolate is incompatible with ascorbic acid.
7. Stability and Storage Conditions:
Tablets prepared with sodium starch glycolate have good storage
properties.Sodium starch glycolate is stable although very hygroscopic, and should
be stored in a well-closed container in order to protect it from wide variations of
humidity and temperature, which may cause caking. The physical properties of
sodium starch glycolate remain changed for up to 3 years if it is stored at moderate
temperatures and humidity

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8. Applications in Pharmaceutical Formulation :

Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in
capsule and tablet formulations. It is commonly used in tablet prepared by either
direct compression or wet granulation processes.

CROSCARMELLOSE SODIUM

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1. Nonproprietary Name: Croscarmellose sodium

2. Synonyms:
Ac-di-sol; carmellosum natricum conexum; Crosslinked carboxymethylcellulose
sodium; Explocel:modified cellulose gum; Nymcel ZSX; Pharmacel XL;
Primellose; Solutab; Vivasol.
3. Chemical Name: Cellulose, carboxy methyl ether, sodium salt.
4. Functional Category: Tablet and capsule disintegrant.
5. Description: Croscarmellose sodium occurs as an odorless, white or grayish-
white powder.
6. Solubility:
Insoluble in water, although Croscarmellose sodium rapidly swells to 4-8 times its
original volume on contact with water. Practically insoluble in acetone, ethanol and
toluene.
7. Stability and Storage Conditions:
Croscarmellose sodium is a stable though hygroscopic material. A model tablet
formulation prepared by direct compression, with Croscarmellose sodium as a
disintegrant, showed no significant difference in drug dissolution after storage at
3000C for 14 months. Croscarmellose sodium should be stored in a well closed
container in a cool, dry place.
8. Incompatibilities:
The efficacy of disintegrant such as Croscarmellose sodium, may be slightly
reduced in tablet formulations prepared by either the wet-granulation or direct
compression process that contain hygroscopic excipients such as sorbitol.
Croscarmellose Sodium is not compatible with strong acids or with soluble salts
of iron and some other metals such as aluminum, mercury and zinc.

9. Applications:

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Croscarmellose sodium is used in oral pharmaceutical formulations as a

disintegrant for capsules, tablets and granules. In tablet formulations,
Croscarmellose sodium may be used in both direct-compression and wet-
granulation processes. When used in wet granulations, the Croscarmellose sodium
should be added in both the wet and dry stages of the process (intra and extra-
granularly) so that the wicking and swelling ability of the disintegrant is best
utilized. Croscarmellose sodium at concentrations up to 5% w/w may be used as
tablet disintegrant, although normally 2% w/w is used in tablets prepared by direct
compression and 3%w/w in tablet prepared by wet granulation process.
10.Related Substances: Carboxy methyl cellulose calcium: Carboxy methyl
cellulose sodium.

Microcrystalline cellulose

Nonproprietary Name: Microcrystalline Cellulose.

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

Empirical Formula: (C6H10O5) n where n ~ 220
Molecular Weight: ~36 000
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.
Incompatibilities: Microcrystalline cellulose is incompatible with strong oxidizing
agents.
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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MENTHOL
Nonproprietary Names
BP: Racementhol
PhEur: Mentholum racemicum
USP: Menthol

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Synonyms
Hexahydrothymol; 2-isopropyl-5-methylcyclohexanol; 4-isopropyl-1-
methylcyclohexan-3- ol; 3-p-menthanol; p-menthan-3-ol; dl-menthol; peppermint
camphor; racemic menthol.

Chemical Name :(1RS,2RS,5RS)-()-5-Methyl-2-(1-methylethyl)cyclohexanol

Empirical Formula and Molecular Weight: C10H20O, 156.27 g/mol

Structural Formula

Functional Category: Flavoring agent; therapeutic agent.

Solubility:Very soluble in ethanol (95%), chloroform, ether, fatty oils and liquid
paraffin; soluble in acetone and benzene; very slightly soluble in glycerin;
practically insoluble in water.

Description
Racemic menthol is a mixture of equal parts of the (1R,2S,5R)- and (1S,2R,5S)-
isomers of menthol. It is a free-flowing or agglomerated crystalline powder, or
colorless, prismatic, or acicular shiny crystals, or hexagonal or fused masses with a

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strong characteristic odor and taste. The crystalline form may change with time
owing to sublimation within a closed vessel. The USP 28 specifies that menthol
may be either naturally occurring l-menthol or synthetically prepared racemic or
dl-menthol. However, the JP 2001 and PhEur 2005, along with other
pharmacopeias, include two separate monographs for racemic and l-menthol.

Typical Properties
Boiling point: 212C
Flash point: 91C
Melting point: 34C
Refractive index: n20D = 1.4615

Stability and Storage Conditions

A formulation containing menthol 1% w/w in aqueous cream has been reported to

be stable for up to 18 months when stored at room temperature. Menthol should be
stored in a well-closed container at a temperature not exceeding 25C, since it
sublimes readily.

Incompatibilities

Incompatible with: butylchloral hydrate; camphor; chloral hydrate; chromium

trioxide; - naphthol; phenol; potassium permanganate; pyrogallol; resorcinol; and
thymol.

Applications:

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Menthol is widely used in pharmaceuticals, confectionery, and toiletry products as

a flavoring agent or odor enhancer. When used to flavor tablets, menthol is
generally dissolved in ethanol (95%) and sprayed onto tablet granules and not used
as a solid excipient. Menthol has been investigated as a skin-penetration enhancer
and is also used in perfumery, tobacco products, chewing gum and as a therapeutic
agent (Raymond C.et al., 2009).

CAMPHOR
Synonyms:
1,7,7-trimethyl bicyclo (2,2,1)-heptan-2-one, 2-bornanone, 2-camphanone, 2-keto-
1,7, 7-trimethylnorcamphane, 2-oxo-bornane, alcanfor, camfora, camphor-natural,
camphor-synthetic, formasa-camphor, Gum camphor, Japan camphor, l,7,7-
trimethy1norcamphor, laurel camphor, matricaria camphor, root bark oil, spirit of
camphor, tramfer.

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Functional category: Rubefacient/counter-irritant

Brand names, Trade names: Camphora synthetic tablets, camphora.

Solubility in water: 0.125 g/100 m1 (25 C) Soluble in ethanol, ethylether,

turpentine, and essential oils

Physical properties

Properties of the substance Normal state at room temperature: solid,

translucent crystals.
Colour: white crystals.
Odour: penetrating, aromatic. There are dangers associated with the
vapour, its dispersion, and possible ignition. There is a moderate risk of fire
if camphor is exposed to heat or flame, but spontaneous combustion does
not occur.
Boiling point: 204 C
Melting point: 176 to 180 C .Sublimes appreciably at room temperature
and normal atmospheric pressure
Flash point: 65C
Relative density: 0.99 (specific gravity)
Relative molecular mass: 152.2.
Shelf-life of the substance :Five years.

Storage conditions: Store in airtight containers at a temperature not above 25C.

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Applications: Camphor is used:

as a rubefacient
as a plasticizer for cellulose esters and ethers
in the manufacture of plastics (especially celluloid)
in lacquers and varnishes
in explosives and pyrotechnics
as a moth repellent
in the manufacture of cymene
as a preservative in pharmaceuticals and cosmetics.

When camphor is applied on the skin, it is analgesic. It is also used in liniments as

a counter-irritant in fibrositis, neuralgia, and similar conditions. In dermatology,
when it is applied as lotion (0.1 to 3%), it is an anti-pruritic and surface anaesthetic
(when applied gently,it creates a feeling of coolness). In dentistry, it is prepared
with parachlorophenol 35% (and 65% camphor) and used as an antibacterial for
infected root canals (Raymond C.et al., 2009).

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