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FEDERAL UNIVERSITY OYE-EKITI

MINERAL MATTERS USED AS

DRUG EXCIPIENTS
Mrs Olorunsola Olufunke

Books
1. Introduction to modern phy
2. Internet resource materials
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Course Outline
1. Mineral matter used as drugs excipients
2. Unorganized crude dugs( Animal substances; Gelatin)
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Mineral matter used as drug excipients

• Excipients are agents or substances, which have no or

little therapeutic activity but are included along with the
drug being formulated in a dosage form so as to impart
specific qualities to them.
• Pharmaceutical excipients are substances other than the
active pharmaceutical ingredient (API) that have been
appropriately evaluated for safety and are intentionally
included in a drug delivery system.”
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• Excipient are inactive substances used as a vehicle or medium for a drug or

active ingredient and likewise assist in the administration of active substances
that may not be easily administered or absorbed by the patient.

• Excipient are an integral process in drug development, but it is important to

choose the right excipient or a combination of excipient for the drug in focus. It
is important for the stabilization of medicinal drugs and administration.
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IDEAL PROPERTIES OF AN EXCIPIENTS

• It should be physically, chemically and biologically inert.
• It can range from simple to complex substances.
• It should be cost effective i.e commercially available at low cost
• It has no interaction with other drugs
• It should be organoleptically acceptable
• It is feasible
• It is chemically stable
• It is compatible with primary packaging materials
• It can conform to regulatory agency requirements
• Absence of pathogenic microbial organisms
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ROLE OF EXCIPIENTS
• It controlled the consistency of drug release and bioavailability
• It promotes ease of administration
• It prevent denaturation
• It enables stability, bioavailability, patient acceptability
• It enhances product identification and overall safety
• It provide bulk to the formulation
• Note: the excipient choosen, the concentration and interaction with the active
pharmaceutical ingredient will determine the physical, chemical and biological
properties of the drug product.
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Categorization of excipients
• Pharmaceutical excipients are categorized into different types;
• 1. By route of administration e.g Oral excipient, topical excipient and
Parenteral excipient.
• 2. By origin i.e
• Animal source e.g Beewax,Gelatin, Honey, Musk, Lanolin
• Plant source e.g Starch, Tumeric, Peppermint, Guargum, Acacia
• Mineral source e.g Talc, Kaolin, Parrafin, Calcium phosphate
• Synthetic source e.g Boric acid, Sacchrin, Lactic acid

• 3. By functionality e.g Fillers, binders, disintegrants, Lubricants, anticaking

agent, flavoring agent, sweetening agent, coating agent, diluent, sorbents e.t.c
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Excipient used in solid Excipient used in liquid Excipients in semi

dosage form form solid form

Diluent Solvents/ Cosolvents Suspending agent

Disintegrants Buffering agents Gelling agent
Binders Antioxidants Suppository base
Lubricants Wetting agent Emollient
Glidants Antifoaming agents
Coating agents Thickening agent
Sorbents Preservatives
Flavoring agent Emulsifying agent
Sweeteners Thickening agent
Colouring agent Chelating agent
Plasticizers Surfactant
Plasticizers Humectant
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Disintegrants
• They aid tablet formulation to facilitate its breaking or disintegration when it
contact in water in the gastrointestinal tract.
• These smaller fragments have greater surface area which will increase the
dissolution of the drug. Two mechanism of disintegrations are proposed:
•  By breaking into fragments: When the tablet comes in contact with the
liquid, the liquid penetrates into the pores of the tablets and breaks it into
fragments.
•  By swelling: When the tablet comes in contact with the water it swells and
ruptures the tablet into small particles.

• Example: starch, starch derivatives, cellulose, alginates.

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Mechanism of action for disintegrants

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Super disintegrants
• They are effective at low concentration and have greater disintegrating
efficiency.
• But they are hygroscopic in nature. Therefore, they not used with moisture
sensitive drugs.
• These cross-linked products swell upto ten fold within 30 seconds when in
• contact with water.
• • A portion of disintegrant is added before granulation and a portion before
• compression, which serve as glidants or lubricant. Evaluation of carbon
• dioxide in effervescent tablets is also one way of disintegration

• Example: Cross-linked polymers, cross carbamalose, cross povidone.

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Binders
• Binders promote the adhesion of particles of the formulation. Such adhesion
enables preparation of granules and maintains the integrity of the final tablet.
• It impart cohesive qualities to powdered material.
• It holds the ingredients in a tablet together. Binders ensure that tablets and
granules can be formed with required mechanical strength.

• Binders can be in powder form and liquid form:

•  Powder binders : cellulose, methyl cellulose, polyvinyl pyrrolidine,
•  PEG Solution binders: gelatin, PVP, sucrose, starch.
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• Natural binders like acacia and tragacanth are used in solution form in the
concentration of 10-25%, alone (or) in combination for wet granulation and
they can be added as powder for the direct compression process.
• Example:
• Saccharides and their derivatives:
•  Disaccharides: sucrose, lactose;
•  Polysaccharides and their derivatives: starches, cellulose
•  Protein: gelatin
•  Synthetic polymers: polyvinyl pyrrolidone (PVP)
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LUBRICANTS
• They are intended to prevent adhesion of the tablet materials to the surface of
dies and punches, reduce inter particle friction and may improve the rate of
flow of the tablet granulation.
• Lubricants interpose a film of low shear strength that interface between the
tableting mass and die wall, and are used in small quantities. It can be
hydrophobic or hydrophilic in nature. Many of them are hydrophobic.
• Example: Talc, Stearic acid, Magnesium stearate, Calcium stearate,
surfactants.
• NOTE:Magnesium stearate is by far the most extensively used tableting
• lubricant
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GLIDANTS
• They are used to improve the flow property of the formulation; it reduces the
friction between the particles and between the hopper and particles and die
cavity and particles.
• Glidants are intended to promote flow of granules or powder material by
reducing the friction between the particles.
• Corn Starch – 5-10% conc., Talc-5% conc., Silica derivative -Colloidal silicas
such as Cab-O-Sil, Syloid, Aerosil in 0.25-3% conc.
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DIFFERENCES BETWEEN LUBRICANT AND GLIDANT

GLIDANT LUBRICANT
Usually glidant are solid. Lubricant may be liquid.
It improves the flow ability of the powder It ensures tablet formulation and ejection with low
fraction.
The glidant is often added to a granulation before Lubricant gives action after tableting.
tableting
They adhere particle surface of the other ingredients They adhere to the die wall.
and improve flow.
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Preservatives
• Preservatives are substances that commonly added to various foods and
pharmaceutical products in order to prolong their shelf life.
• Preservatives prevents an increased risk of contamination by opportunistic
microbial pathogens.
• Exert a wide spectrum of antimicrobial activity at low inclusion levels.
• It maintain activity throughout product manufacture, shelf life and usage.
• It is not adversely affect patient safety or tolerance of the product.
• Example: Methyl & Ethyl parabens, Propyl paraben, Benzoic acid, BHA, BHT.
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Buffering agent
• These materials when dissolved in solvent will enable the solution to resist any
change in pH should an acid or an alkali be added. It maintains pH of the
formulation.
• It maintaining/optimizing chemical stability, anti-microbial effectiveness, ensure
physiological compatibility
• Example: Phosphate buffers, Acetate buffers.
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Solvents/Cosolvent
Solvents work by breaking of bonds and reducing effective charge on ions thus
increasing Solute Solvent forces of attraction which are eventually greater than
Solute-Solute and Solvent-Solvent forces of attraction.
• Examples: Water, alcohol, acetic acid.

• Co-solvents Increase the solubility of solute in solvents, Reduce dose volume.

• Example: Ethanol, Sorbitol, Glycerin.
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Suppository base
• Suppository base used to form base for dissolving active ingredient.
• Example: Cocoa butter, glycerin, coconut oil, gelatin
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Suspending agent
• They function by keeping small particles of active, and possibly other
excipients, suspended during the shelf life of the product.
• It helps to prevent cake formation in suspension .
• It helps in the formation of stabilized system of deflocculated system. Used for
easy redistribution.
• Reduce the rate of sedimentation of particles .
• Uniform dispersion system formation.

• Example: Acacia, Agar.

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MINERAL MATTER USED AS EXCIPIENT

• TALC : it is a sheet silicate mineral associated with clay. The formula of Talc is
Mg3Si4O10(OH)2, Magnesium Silicate Hydroxide.

• Talc is a metamorphic mineral that results from the metamorphism of

Magnesium minerals such as serpentine, pyroxene, amphibole, and olivine, in
the presence of carbon dioxide and water.
• Talc is primarily formed by hydration and carbonation by this reaction:
• 2Mg3Si2O5(OH)4 + 3CO2 → Mg3Si4O10(OH)2 + 3MgCO3 +3H2O
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Properties of Talc
• Color is usually white, gray, yellow and green.
•  It can also be stained brown by iron oxides.
•  Luster is greasy to dull, but pearly on cleavage
• surfaces.
• Transparency: Crystals are mostly translucent to
• opaque.
• Fracture is uneven or splintery.
• Hardness is 1 - 1.5 (soft enough to be scratched by a
• fingernail).
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White Talc Green Talc Gray Talc

Yellow Talc
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• Due to its low shear strength, talc is one of the oldest known solid lubricants.
Talc finds use as a cosmetic (talcum powder), as alubricant, and as a filler in
paper manufacture.
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TYPES OF TALC
• PLATY TALC: It contains predominately (>90%) the mineral talc.
Platy talc's can be further classified as microcrystalline or macro crystalline,
• MICRO CRYSTALLINE: These varieties are naturally small in plate size and
comprise compact, dense ores.
• b) MACRO CRYSTALLINE: These varieties contain relatively large, higher
aspect ratio plates.
TREMOLITIC TALC: It is most often a natural blend of talc, tremolite,
serpentine and anthophyllite. The size of an individual talc platelet (= a few
• thousand elementary sheets) can vary from approximately 1 micron to over
100 micronsdepending on the deposit.
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KAOLIN
• Synonyms: China clay, Kaolinumproderesum, porcelain clay.
• Source: It is purified native hydrated aluminiumsilicate free from gritty
particles. It is obtained by powdering the native kaolin elutriating and collecting
the fraction, which complies with the requirement of particle size.
• The different types of Kaolin are as follows:
• 1.Heavy Kaolin: It is purified hydrated aluminiumsilicate powdered so as to
make free from gritty particles by elutriation.
• 2.Light Kaolin: It is identical to heavy kaolin, but is limited to certain particle
size and contains suitable dispersing agent.
• 3.Natural light Kaolin: it is also a native hydrated aluminiumsilicate free from
gritty particles, but devoid of dispersing agent.
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• Chemical constituents:
• Kaolin is anhydrous aluminium silicate with a chemical formula
Al2O22SiO22H2O.
• The composition are as follow:
• Silicon dioxide, Iron oxide, titanium dioxide aluminium oxide etc. It is used as
diluent; binder; disintegrant; and pelletizing, granulating,amorphizing, particle
film coating, emulsifying and suspending agents
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Excipient and Kaolin Grade

EXCIPIENT KAOLIN GRADE
Diluent Light and heavy kaolin
Disintegrant Heavy kaolin
Suspending agent and anticaking agent Heavy kaolin
Wetting and emulsifying agent Light kaolin
Granulating agent Heavy and Light Kaolin
Pelletizing agent Heavy kaolin
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Acacia
• Synonyms: Gum acacia, Gum arabica,
• Indian gum.
• Biological Source: It is the dried gummy
• exudates obtained from the stem and branches of Acacia arabicabelonging to
Family Leguminosae.
• Uses; it is used as an emulsifying agent, binding agent, suspending agent
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Beewax
• Synonyms: Beeswax, Cera-flava.
• Biological Source: It is purified wax obtained by melting the walls of the
honey comb of the bees Apis mellifera and other species of Apis, belonging
to Family Apidae
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Tragacanth
• Synonyms: Gum tragacanth,
• Tragacanth.
• Biological Source: It is dried gummy exudates obtained by incision from
stems and branches of Astragalus gummifer belonging to Family
Leguminosae.
• Uses:
• •Demulcent, adhesive.
• •Emollient.
• •Used as thickening, suspending and emulsifying agent.
• •Used binding agent in tablets & excipients in pills.
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AGAR
AGAR
• •Synonyms: agar-agar, japanese-isinglass, vegetable gelatin.
• •Biological Source: It is the dried gelatinous substance obtained from
Gelidium amansiibelonging to Family Gelidaceae.
• Uses:
• •Used as emulsifying agent, bulk laxative.
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Guar gum

• Synonyms: Guar flour, Jaguar gum.

• Biological Source:It is the powder of
• endosperm of the seeds of Cyamopsis tetragonolobus belonging to Family
Leguminosae.
• Uses:
• •It reduces blood glucose concentration in diabetic patients and serum
concentration in hyper lipidaemia.
• •Used as binding agent and disintegrating agent in tablet formulations.
• •bulk laxatives and as appetite depressant.
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References

• Ms. Pranita Sunar, Pharmaceutical Aids

• Hak-kim Chan, 2002, Excipients: Powder And Solid Dosage Forms
• DIPTO KUMER SARKER , 2018; Excipients
• Shagufta Farooqui, Herbal excipients
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Happy reading !!!!!!!