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CARRIER PROFILE
66Carriers ProfileCarriers Profile
6.1 Lactose, Monohydrate
1. Nonproprietary Names
BP: Lactose
PhEur: Lactose Monohydrate
JP: Lactose Hydrate
USP-NF: Lactose Monohydrate
2. Synonyms
CapsuLac; GranuLac; Lactochem; lactosum monohydricum;
Monohydrate; Pharmatose; PrismaLac; SacheLac; SorboLac;
SpheroLac; SuperTab 30GR; Tablettose.
3. Chemical Name O-β -D-Galactopyranosyl-(1→4)-α-D-glucopyranose monohydrate.
4. Empirical Formula C12H22O11.H2O
Molecular Weight 360.31
5. Structural Formula
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6. Functional Category
Dry powder inhaler carrier; lyophilization aid; tablet binder; tablet
and capsule diluent; tablet and capsule filler.
7. Applications in Pharmaceutical Formulation or Technology
Lactose is widely used as a filler and diluent in tablets and capsules, and to a more limited
extent in lyophilized products and infant formulas.(1–9) Lactose is also used as a diluent
in dry-powder inhalation; seeLactose, Inhalation. Various lactose grades are commercially
available that have different physical properties such as particle size distribution and flow
characteristics. This permits the selection of the most suitable material for a particular
application; for example, the particle size range selected for capsules is often dependent on
the type of encapsulating machine used.
L
Lactose, Monohydrate
Usually, fine grades of lactose are used in the preparation of tablets by the wet-granulation
method or when milling during processing is carried out, since the fine size allows better
mixing with other formulation ingredients and utilizes the binder more efficiently.
Other applications of lactose include use in lyophilized products, where lactose is added to
freeze-dried solutions to increase plug size and aid cohesion. Lactose is also used in
combination with sucrose (approximately 1 : 3) to prepare sugar-coating solutions. It may
also be used in intravenous injections.
Lactose is also used in the manufacture of dry powder formulations for use as aqueous
film-coating solutions or suspensions. Direct-compression grades of lactose monohydrate
are available as granulated/agglomerated a-lactose monohydrate, containing small
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CARRIER PROFILE
amounts of anhydrous lactose. Direct-compression grades are often used to carry lower
quantities of drug and this permits tablets to be made without granulation.
Other directly compressible lactose are spray-dried lactose and anhydrous lactose.
8. Description
In the solid state, lactose appears as various isomeric forms, depending on the
crystallization and drying conditions, i.e. α lactose monohydrate, β-lactose anhydrous, and
α-lactose anhydrous. The stable crystalline forms of lactose are α-lactose monohydrate, β-
lactose anhydrous, and stable α-lactose anhydrous. Lactose occurs as white to off-white
crystalline particles or powder. Lactose is odorless and slightly sweet-tasting; α-lactose is
approximately 20% as sweet as sucrose, while β-lactose is 40% as sweet.
9. Typical Properties
Table 6.2
Properties of Hypromellose
Properties Range
pH 5.5 -6.5
Ash 1.5 - 3.0 %
Bulk density 0.75 g/cm3
Tapped density 0.88 g/cm3
True density 1.545 g/cm3
Melting point 219 oC
Specific gravity 1.525
10. Solubility
Soluble in water and practically insoluble in chloroform, ether and ethanol.
6.2 Cellulose Microcrystalline43
1. Nonproprietary Names
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CARRIER PROFILE
BP: Microcrystalline cellulose
JP: Microcrystalline cellulose
PhEur: Cellulosum microcristallinum
USPNF: Microcrystalline cellulose
2. Synonyms
Avicel PH, Celex, cellulose gel, Celphere, Ceolus KG, crystalline cellulose, E460,
Emcocel, Ethispheres, Fibrocel, Pharmacel, Tabulose, Vivapur.
3. Chemical Name Cellulose
4. Empirical Formula (C6H10O5)n where n = 220 Molecular Weight 36000
5. Structural Formula
6. Functional Category
Adsorbent, suspending agent, tablet and capsule diluent, tablet disintegrant.
7. 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. In addition to its use as a binder/diluent, microcrystalline cellulose
also has some lubricant and disintegrant properties that make it useful in tableting.
Table 6.3Uses of Microcrystalline Cellulose
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Use Concentration (% w/w)
Adsorbent 20-90
Antiadherent 5-20
Capsule binder/diluent 20-90
Tablet disintegrant 5-15
Tablet binder/diluent 20-90
8. 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.
9. Solubility
Slightly soluble in 5 % w/v sodium hydroxide solution, practically insoluble in water,
dilute acids, and most organic solvents.
10. Typical Properties
Table 6.4Grade Nominal mean
particle size (μm)Paricle size analysis Moisture
content (%)Mesh size Amount retained
(%)
Avicel PH -101 50 60≤ 1.0 ≤ 5.0
Properties of Microcrystalline Cellulose
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6.3 Povidone43
1. Nonproprietary Names
BP: Povidone
JP: Povidone
PhEur: Povidonum
USP: Povidone
2. Synonyms
E1201, Kollidon, Plasdone, poly[1-(2-oxo-1-pyrrolidinyl)ethylene], polyvidone,
polyvinylpyrrolidone, PVP, 1-vinyl-2-pyrrolidinone polymer.
3. Chemical Name 1-Ethenyl-2-pyrrolidinone homopolymer.
4. Empirical Formula (C6H9NO)n Molecular Weight 2500-3000000
PVP K-30 50000
5. Structural Formula
BBDNITM, LUCKNOW Page 33
Properties Range
pH 5.0 -7.5
Angle of repose 49 o
Bulk density 0.32 g/cm3
Tapped density 0.45 g/cm3
True density 1.512-1.668 g/cm3
Melting point 260 - 270 oc
Specific surface area 1.06-1.12 m2/g for Avicel PH-101
CARRIER PROFILE
6. Functional Category
Disintegrant, dissolution aid, suspending agent, tablet binder.
7. Applications in Pharmaceutical Formulation or Technology
Although povidone is used in a variety of pharmaceutical formulations, it is primarily used
in solid-dosage forms. In tableting, povidone solutions are used as binders in wet-
granulation processes. Povidone is also added to powder blends in the dry form and
granulated in situ by the addition of water, alcohol, or hydroalcoholic solutions. Povidone
is used as a solubilizer in oral and parenteral formulations and has been shown to enhance
dissolution of poorly soluble drugs from solid-dosage forms. Povidone solutions may also
be used as coating agents.
Povidone is additionally used as a suspending, stabilizing, or viscosity-
increasing agent in a number of topical and oral suspensions and solutions. The solubility
of a number of poorly soluble active drugs may be increased by mixing with povidone.
Table 6.5Uses of Povidone
Use Concentration (%)
Carrier for drugs 10-25
Dispersing agent Up to 5
Eye drops 2-10
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Suspending agent Up to 5
Tablet binder, tablet diluent, or coating agent 0.5-5
8. Description
Povidone occurs as a fine, white to creamy-white colored, odorless or almost odorless,
hygroscopic powder.
9.Solubility
Freely soluble in acids, chloroform, ethanol , ketones, methanol, and water; practically
insoluble in ether, hydrocarbons, and mineral oil.
10. Typical Properties
Table 6.6Properties of Povidone
6.4 Colloidal Silicon Dioxide43
1. Nonproprietary Names
BP: Colloidal anhydrous silica
PhEur: Silica colloidalis anhydrica
USPNF: Colloidal silicon dioxide
2. Synonyms
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Properties Range
pH 3.0 - 7.0
Bulk density 0.29-0.39 g/cm3
Tapped density 0.39-0.54 g/cm3
True density 1.180 g/cm3
Melting point 150oC
CARRIER PROFILE
Aerosil, Cab-O-Sil, Cab-O-Sil M-5P, colloidal silica, fumed silica, light anhydrous silicic
acid, silicic anhydride, silicon dioxide fumed, Wacker HDK.
3. Chemical Name Silica
4. Empirical Formula SiO2 Molecular Weight 60.08
5. Structural Formula SiO2
6. Functional Category
Adsorbent, anticaking agent, emulsion stabilizer, glidant, suspending agent, tablet
disintegrant, thermal stabilizer, viscosity-increasing agent.
7. Applications in Pharmaceutical Formulation or Technology
Colloidal silicon dioxide is widely used in pharmaceuticals, cosmetics, and food products.
Its small particle size and large specific surface area shows desirable flow characteristics
that are exploited to improve the flow properties of dry powders in a number of processes
such as tableting
Table 6.8Uses of Colloidal silicon dioxide
Use Concentration (%)
Aerosols 0.5-2.0
Emulsion stabilizer 1.0-5.0
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Glidant 0.1-0.5
Suspending and thickening agent2.0-10.0
8. Description
Colloidal silicon dioxide is a submicroscopic fumed silica with a particle size of about
15 nm. It is a light, loose, bluish-white-colored, odorless, tasteless, nongritty amorphous
powder.
9. Solubility
Practically insoluble in organic solvents, water, and acids, except hydrofluoric acid,
soluble in hot solutions of alkali hydroxide. Forms a colloidal dispersion with water.
10. Typical Properties
Table 6.9
Properties of Colloidal silicon dioxide
Properties Range
pH 3.5-4.4
Bulk density 0.029-0.042 g/cm3
Tapped density 0.05 g/cm3
Specific surface area 200 ± 25 m2/g
6.5 Magnesium Stearate
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1. Nonproprietary Names
BP: Magnesium Stearate
JP: Magnesium Stearate
PhEur: Magnesium Stearate
USP-NF: Magnesium Stearate
2. Synonyms
Dibasic magnesium stearate; magnesium distearate; magnesia stearas; magnesium
octadecanoate; octadecanoic acid, magnesium salt; stearic acid, magnesium salt; Synpro
90.
3. Chemical Name Octadecanoic acid magnesium salt.
4. Empirical Formula C36H70MgO4
5. Functional Category
Tablet and capsule lubricant.
6. 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.
7. 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.
8.Solubility
Practically insoluble in ethanol, ethanol (95%), ether and water; slightly soluble in warm
benzene and warm ethanol (95%).
9. Typical Properties
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Table 6.10
Properties of Talc
Properties Range
Bulk Density 0.159 g/cm3
Tapped Density 0.286 g/cm3
True Density 1.092 g/cm3
Melting Point 117–150°C
6.6 Sodium Starch Glycolate1.Nonproprietary Names
BP: Sodium Starch Glycolate
PhEur: Sodium Starch Glycolate
USP-NF: Sodium Starch Glycolate
2 Synonyms
Carboxymethyl starch, sodium salt; carboxymethylamylum natricum; Explosol;
Explotab; Glycolys; Primojel; starch carboxymethyl ether, sodium salt; Tablo; Vivastar P.
3 Chemical Name
Sodium carboxymethyl starch.
4. Empirical Formula
The USP32–NF27 describes two types of sodium starch glycolate, Type A and Type B,
and states that sodium starch glycolate is the sodium salt of a carboxymethyl ether of
starch or of a crosslinked carboxymethyl ether of starch.
The PhEur 6.0 describes three types of material: Type A and Type B are described as the
sodium salt of a crosslinked partly Ocarboxymethylated potato starch. Type C is described
as the sodium salt of a partly O-carboxymethylated starch, crosslinked by physical
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dehydration. Types A, B, and C are differentiated by their pH, sodium, and sodium
chloride content. The PhEur and USP–NF monographs have been harmonized for Type A
and Type B variants.
5. Molecular Weight
The molecular weight is typically 5 x105–1x106 .
6. Structural Formula :
7. Functional Category:
Tablet and capsule disintegrant.
8 Appilication in pharmaceutical Formulation or Technology
Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in
capsule and tablet formulations. It is commonly used in tablets prepared by either direct-
compression or wet-granulation processes. The usual concentration employed in a
formulation is between 2% and 8%, with the optimum concentration about 4%, although
in many cases 2% is sufficient. Disintegration occurs by rapid uptake of water followed by
rapid and enormous swelling. Although the effectiveness of many disintegrants is affected
by the presence of hydrophobic excipients such as lubricants, the disintegrant efficiency of
sodium starch glycolate is unimpaired. Increasing the tablet compression pressure also
appears to have no effect on disintegration time.
Sodium starch glycolate has also been investigated for use as a suspending vehicle.
9.Description
Sodium starch glycolate is a white or almost white free-flowing very hygroscopic powder.
The PhEur 6.0 states that when examined under a microscope it is seen to consist of:
granules, irregularly shaped, ovoid or pear-shaped, 30–100 mm in size, or rounded, 10–35
mm in size; compound granules consisting of 2–4 components occur occasionally; the
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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 show considerable swelling
in contact with water.
10 Typical Properties
Table 6.10
Properties of Talc
Properties Range
Bulk Density 0.75 g/cm3
Tapped Density 0.90 g/cm3
True Density 1.90 g/cm3
Melting Point Chars at 200°C
Solubility
Practically insoluble in methylene chloride. It gives a translucent suspension in water.
6.6 Polyoxyethylene Sorbitan Fatty Acid Esters1.Nonproprietary Names
BP: Polysorbate 80
PhEur: Polysorbate 80
USP-NF: Polysorbate 80
2 Synonyms
Polysorbate 80 Atlas E; Armotan PMO 20; Capmul POE-O; Cremophor PS 80; Crillet 4;
Crillet 50; Drewmulse POE-SMO; Drewpone 80K; Durfax 80; Durfax 80K; E433; Emrite
6120; Eumulgin SMO; Glycosperse O-20; Hodag PSMO-20; Liposorb O-20; Liposorb O-
20K; Montanox 80; polyoxyethylene 20 oleate; polysorbatum 80; Protasorb O-20;
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Ritabate 80; (Z)-sorbitan mono-9-octadecenoate poly(oxy1,2- ethanediyl) derivatives;
Tego SMO 80; Tego SMO 80V; Tween 80.
3 Chemical Name
Polysorbate 80 Polyoxyethylene 20 sorbitan monooleate.
4. Empirical Formula
C64H124O26
5. Molecular Weight
1310
6. Structural Formula :
7. Functional Category:
Dispersing agent; emulsifying agent; nonionic surfactant; solubilizing agent; suspending
agent; wetting agent.
8 Appilication in pharmaceutical Formulation or Technology
Polyoxyethylene sorbitan fatty acid esters (polysorbates) are a series of partial fatty acid
esters of sorbitol and its anhydrides copolymerized with approximately 20, 5, or 4 moles
of ethylene oxide for each mole of sorbitol and its anhydrides. The resulting product is
therefore a mixture of molecules of varying sizes rather than a single uniform compound.
Polysorbates containing 20 units of oxyethylene are hydrophilic nonionic surfactants that
are used widely as emulsifying agents in the preparation of stable oil-in-water
pharmaceutical emulsions. They may also be used as solubilizing agents for a variety of
substances including essential oils and oil-soluble vitamins, and as wetting agents in the
formulation of oral and parenteral suspensions. They have been found to be useful in
improving the oral bioavailability of drug molecules that are substrates for P-glycoprotein.
Polysorbates are also widely used in cosmetics and food products.
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9.Description
Polysorbates have a characteristic odor and a warm, somewhat bitter taste. At 25°C it is
yellow oily liquid.
.
10 Typical Properties
Table 6.10
Properties of Talc
Properties Range
pH 6.0-8.0
HLB Value 15.0
Specific gravity 1.08
Viscosity 42.5 mPa s
Surface Tension 42.5 mN/m
Acid Value 2.0
Hydroxyl Value 65-80
Moisture Content 3.0
Saponification Value 45-55
Solubility
Soluble in water and ethanol . Insoluble in mineral oil and vegetable oil.
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