Excipient Profile

Excipient Profile

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5. EXCIPIENT PROFILE

5.1 β-CYCLODEXTRIN

Figure 7. Structure of Beta cyclodextrin

1. Nonproprietary Names BP:

Beta cyclodextrin

PhEur: Beta cyclodextrin USP:

Beta cyclodextrin

2. Synonyms β - cyclodextrin, beta-cycloamylose; betadex; beta –

dextrin.

3. Chemical Name and CAS registry Number β-

cyclodextrin : [7585-39-9]

4. Empirical Formula and Mol. Weight

C42H70O35; 1135

5. Functional Category Stabilizing agent,

solubilizing agent.

Excipient Profile

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5.2.Applications in Pharmaceutical Formulation or Technology

Cyclodextrins are crystalline, nonhygroscopic, cyclic oligosaccharides derived from

starch. Cyclodextrins are used to form inclusion complexes with a variety of drug

molecules resulting primarily in improvements to dissolution and bioavailability

due to enhanced solubility and improved chemical and physical stability.

Cyclodextrin inclusion complexes have also been used to mask the unpleasant taste

of active materials and to convert a liquid substance into a solid material. β –

cyclodextrin is the most commonly used cyclodextrin although it is the least soluble.

It is least expensive cyclodextrin, is commercially available from number of sources,

and is able to form inclusion complexes with a number of molecules of

pharmaceutical interest. However, β – cyclodextrin should not be used in parenteral

formulations since it is nephrotoxic, and considered to be nontoxic when taken

orally and has thus primarily used in tablet and capsule formulations. In oral tablet

formulations β – cyclodextrin may be used in both wet granulation and dry

compression process.

5.3. Typical

properties

Bulk Density:

0. 0.

0.523gm/cm

Tapped Density: 0.754

gm/cm3 Melting point: 255 -2 65ºC

Solubility: Soluble in 200 parts of Propylene glycol, 1 in 50 parts of water at 20ºC,

practically insoluble in acetone.

Stability and storage conditions Stable in the solid state

if protected from high humidity.

Incompatibilities

The activity of some antimicrobial preservatives in aqueous solutions can be reduced

in the presence of hydroxypropyl - β – cyclodextri

Excipient Profile

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5.4 MICROCRYSTALLINE CELLULOSE

1. Non-proprietary names

BP: Microcrystalline cellulose

JP: Microcrystalline cellulose

PhEur: Cellulose Microcrystallinum

USP: Microcrystalline cellulose

2. Synonyms

Avicel; cellulose gel; crystalline cellulose; E460; Emcocel; Fibrocel; Tabulose;

Vivacel

3. Chemical Name and CAS Registry

Number Cellulose [9004–34–6]

4. Empirical Formula and Mol.

weight (C6H10O5)n | 36,000 . Where

n = 220

5. Functional category Adsorbent; suspending agent, tablet and

capsule diluent; tablet disintegrant.

6. Applications in pharmaceutical formulation or technology

MCC 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 process. In addition to its use as a binder/ diluent, MCC

also has some lubricant and disintegrant properties that make it useful in

tabletting. Also used in cosmetics and food products.

Excipient Profile

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Use

Concentration (%)

1. Adsorbent 20-90

2. Anti-adherent 5-20

3. Capsule binder / diluents 20-90

4. Tablet disintegrant 5-15

5. Tablet binder / diluents 20-90

7. Description

MCC is purified, partially depolymerized cellulose that occurs as a white,

odourless, tasteless, crystalline powder composed of porous particles.

It is commercially available in different particle sizes and moisture grades,

which have different properties and applications.

8. Typical properties

1) PH: 5.0 - 7.0

2) Density (true): 0.32g/cm3

3) M.P. : Chars at 260-270oC

4) Moisture content: typically, less than 5% w/w. It is hygroscopic.

5) Solubility: slightly soluble in 5% w/v sodium hydroxide solution, insoluble in

Excipient Profile

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9. Stability and storage conditions

MCC is a stable, though hygroscopic material. The bulk material should be

stored in a well-closed container in a cool, dry place.

10. Incompatibilities Incompatible

with strong oxidizing agents.

11. Safety

MCC is widely used in oral pharmaceutical formulations and food products

and is generally regarded as a non-toxic and non-irritant material.

Excipient Profile

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5.5 LACTOSE

1. Non-proprietary Names BP:

Lactose monohydrate PhEur:

Lactosum

USP: Lactose monohydrate

2. Synonyms Fast – Flo; Lactohem; Microtose;

Pharmatose.

3. Chemial Name and CAS Registry Number O-β-D-Galatopyranosyl-(1 - 4 )-

α-D-gluopyranose monohydrate [64044-51-5]

4. Empirical Formula and Molecular Weight

C12H22O11 .H2O 360.31 (monohydrate)

5. Functional category Tablet

and capsule diluents

6. Applications in pharmaceutial industry

Lactose is widely used as a filler or diluent in tablets, capsules, and to a more limited

extent in lyophilized produts and infant feed formulas. Usually, fine grades of

lactose are used in the preparation of tablets by the wet granulation method or when

milling during proessing is carried out, since the fine size permits better mixing with

other formulation ingredients and utilizes the binder more efficiently.

7. Desription

White to off-white crystalline partiles or powder. Lactose is odorless and slightly

sweet-tasting; α-lactose is approximately 15 % as sweet as sucrose, while α-lactose is

sweeter than the α-form.

Excipient Profile

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8. Other properties

Density: 1.540 for α-lactose monohydrate

Bulk density: 0.619 g/cm3

Tapped density: 0.935 g/cm3

Melting point: 201-202ºC

9. Stability and storage conditions

Under humid conditions (80 % relative humidity and above), mold growth may occur.

Lactose may develop a brown coloration on storage, the reation being accelerated by

warm, damp conditions. The purity of different latoses can vary and color

evaluation may thus be important, particularly if white tablets are being formulated.

Lactose should be stored in a well closed container in a cool, dry place.

10. Incompatibilities

A Maillard type condensation reaction is likely to occur between lactose and

compounds with a primary amine group to form brown colored produts. This

reation occurs more readily with the amorphous material rather than with crystalline

lactose. Lactose is incompatible with amino acids, aminophylline and

amphetamines.

11. Safety

Widely used in pharmaeutial formulations as a diluent in oral capsules and tablet

formulations

Excipient Profile

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5.6 CROSPOVIDONE

1. Non-proprietary Names BP:

Crospovidone

PhEur: Crospovidone

USP: Crospovidone

2. Synonyms Cross-linked providone,

kollidon CL.

3. Chemical name & CAS Registry Number

Ethenyl-2-pyrrolidinone homopolymer [9003-39-8]

4. Empirical Formula and Molecular weight

(C9H9NO)n > 10,00,000

CP is a water-insoluble synthetic cross-linked homopolymer of N-vinyl 2-

pyrrolidinone. An exact determination of the molecular weight has not been

established because of the insolubility of the material.

5. Functional category

Tablet disintegrant

6. Applications in pharmaceutical formulations and technology

Water insoluble tablet disintegrant used at 2-5% concentration in tablets prepared by

direct compression or wet and dry granulation methods. It rapidly exhibits high

capillary activity and pronounced hydration capacity with little tendency to form

gels.

7. DescriptionIt is a white to creamy white, finely divided, free-flowing, practically

tasteless, odorless or nearly odorless, hygroscopic powder.

Excipient Profile

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8. Pharmacopoeial specifications

1) pH: 5.0 - 8.0

2) Density: 1.22 g/cm3

3) Solubility: Practically insoluble in water and most common organic solvents.

4) Moisture content: Maximum moisture absorption is approx. 60%.

9. Stability and storage conditions

Crospovidone is stable. However, since it is hygroscopic it should be stored in

an airtight container in a cool, dry place.

10. Incompatibilities

Compatible with most organic and inorganic pharmaceutical ingredients. When

exposed to a high water level CP may form molecular adducts with some

materials.

11. Safety

CP is used in oral pharmaceutical formulations and is generally regarded as a

non-toxic and non-irritant material.

Excipient Profile

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5.7 MAGNESIUM STEARATE

1. Non-proprietary Names

BP : Magnesium stearate

PhEur : Magnesium stearate

US : Magnesium stearate

2. Synonyms 572, Magnesium octadecanoate; stearic acid magnesium

salt; octadecanoic acid, magnesium salt.

3. Chemical name and CAS Registry

Number Octadecanoic acid magnesium salt

[557-04-0]

4. Empirical Formula & Molecular weight

C36H70MgO4; 591.34

USP describes magnesium stearate as a compound of magnesium with a

mixture of solid organic acids and consists chiefly of variable proportions of

magnesium stearate & magnesium palmitate (C32H62MgO4)

5. Structural Formula

[CH3(CH2)16COO]2 Mg

6. Functional category

Tablet & capsule

lubricant.

7. Applications in pharmaceutical Formulation or Technology Mg 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 0.25-5.0%. It is also used in barrier creams.

Excipient Profile

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8. Description

Fine, white, precipitated or milled, impalpable powder of low bulk density,

having a faint odour of stearic acid and a characteristic taste. The powder is

greasy to the touch and readily adheres to the skin.

9. Typical properties

1) Crystalline forms: high purity Mg. st. has been isolated as a trihydrate, a

dihydrate and an anhydrate.

2) Bulk density: 0.159 g/cm3

3) Flow ability: poorly flowing, cohesive powder.

4) Melting range: 117-150oC (commercial samples)

126-130oC (high purity Mg. stearate.)

5) Solubility: Practically insoluble in ethanol, ethanol (95%), ether and H2O,

slightly soluble in warm benzene and warm ethanol (95%).

10. Stability and storage conditions

Mg. stearate is stable and should be stored in a well-closed container in a cool,

dry place.

11. Incompatibilities: Incompatible with strong acids, alkalis and iron salts,

can’t be used in products containing aspirin, some vitamins and most alkaloid

salts.

12. Safety: Widely used as a pharmaceutical recipient and is generally regarded

as being non-toxic following oral administration

Excipient Profile

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5.8. SODIUM HYDROXIDE

Sodium hydroxide, also known as lye or caustic soda, it is a highly caustic metallic base. It is

a white solid available in pellets, flakes, granules, and as a 50% saturated solution

It is highly soluble in water, with a lower solubility in ethanol and methanol, but is insoluble

in ether and other non-polar solvents.

1) Synonym: Caustic Soda

2) Chemical Name: Sodium Hydroxide

3) Chemical Formula: NaOH

4) Physical state and appearance: Solid.

5) Odor: Odorless

6) Molecular Weight: 40 g/mole

7) Color: White.

8) pH (1% soln/water): 13.5 [Basic.]

9) Specific Gravity: 2.13 (Water = 1)

Uses

Sodium hydroxide is the principal strong base used in the chemical industry. In bulk it is

most often handled as an aqueous solution, since solutions are cheaper and easier to handle.

Sodium hydroxide, a strong base, is responsible for most of these applications. Another

strong base such as potassium hydroxide is likely to yield positive results as well.

56% of sodium hydroxide produced is used by the chemical industry, with 25% of the same

total used by the paper industry. Sodium hydroxide is also used for the manufacture of

sodium salts and detergents, for pH regulation, and for organic synthesis. It is used in the

Bayer process of aluminium production.

Sodium hydroxide is used in many scenarios where it is desirable to increase the alkalinity of

a mixture, or to neutralize acids.

Excipient Profile

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5.9. Sodium lauryl sulfate

sodium lauryl sulfate is commonly used as a detergent, wetting agent, and emulsifying agent

in many of the products that we all use on a daily basis. It is an ingredient used in shampoos,

conditioners, dish soap, hand soap, and even toothpaste. Sodium lauryl sulfate is a crystal like

salt derived from sulfated lauryl alcohol.

1) Synonym: Sodium dodecyl sulfate

2) Chemical Name: Sulfuric acid, monododecyl ester, sodium salt

3) Chemical Formula: CH3(CH2)10CH2OOSOONa

4) Physical state and appearance: Solid. (Crystals solid.)

5) Odor: Characteristic. Faint odor of fatty substances (Slight.)

6) Molecular Weight: 288.38 g/mole

7) Color: White to yellowish.

8) Melting Point: 204°C (399.2°F) - 207° C

9) Solubility: Soluble in cold water, hot water. Solubility in water: 1g/10 ml water

Uses

There is controversy over whether this salt is safe for people to use. Many believe that

sodium lauryl sulfate is carcinogenic and could be hazardous to humans. There is still no

concrete evidence that sodium lauryl sulfate is connected with cancer. Companies take

advantage of this and package their products to consumers as free of sodium lauryl sulfate.

Sodium lauryl sulfate is added to many of the items we come across it in because it produces

an exceptional lather and makes substances become thicker. This chemical is widely used

because it is relatively low in cost, has a long shelf life and for its multi use. Sodium lauryl

sulfate is also used as an ingredient in certain pesticide products to dehydrate and kill insects.

It works effectively on ticks, bed bugs, lice, mites, and aphids. Sodium lauryl sulfate

dissolves in water easily and can be sprayed right on the insect you wish to eradicate from

your home of place of work. Sodium lauryl sulfate will also biodegrade at a faster rate than

other products. It is listed as a “minimum risk’ pesticide with the EPA and is considered a

safer alternative.

Sodium lauryl sulfate will strip the protective oils from the top layer of your skin and can be

irritating to the eyes. A lot of organic products use a less harsh detergent referred to as

ammonium lauryl sulfate. Products containing this chemical may be a better option for you

and your family if those with sodium lauryl sulfate cause your skin to become irritated.

Normally, inexpensive shampoos and soaps have sodium lauryl sulfate as one of their

ingredients, although some higher priced cleansers have this chemical in them as well.