EXCIPIENTS

Mrs. Pruthvi N
Associate Professor
RRCOP
Herbal Excipients:

• Excipients are any component other than the active substance(s)

intentionally added to formulation of a dosage form. Generally, they
are known as Pharmaceutical excipients which are non-active
ingredients. These ingredients are mixed with the therapeutically
active compounds and form a medicine.
 • Some of the ideal properties of the excipients are like:
(a) They should be biologically stable.
(b) They should be odourless, tasteless, and elegant.
(c) They should be pharmaceutically acceptable, high flexibility,
sterilizable and thermostable.
(d) They should be approved by regulatory bodies.
(e) They should be easily available and economical.
(f) They should be physically, chemically and therapeutically inert.
(h)They should be non-toxic.
(i) They should be compatible & should make formulation stable and
reproducible.
• There are various types of excipients that are used in pharmaceutical
preparations.
• They semi-synthetic as well as natural plant based. Natural based
excipients and derivatives occur are listed.
• There are various types of Pharmaceutical excipients such as
synthetic, ubiquitously throughout the plant and animal kingdoms.
There polymers such as natural gums and mucilage are
biocompatible, cheap and easily available.
• More over, they are quite safe than synthetic and semi-synthetic
excipients based on low toxicity, low cost, availability, soothing action
and non-irritant nature.
• There are various types of natural excipients available that are shown.
CLASSIFICATION OF PHARMACEUTICAL AIDS
• Colour: caramel, colchineal, turmeric, saffron, indigo, chlorophyll, carotene.
• Diluents: peppermint oil,peanut oil, sesame oil, glucose, lactose, cinnamon water, corn oil.
• Flavors: nutmeg, orange peel, cardamom, cocoa, lemon, oil.
• Disintegrants: Starch, psyllum husk, CMC, microcrystalline cellulose
• Sweetening agents: Glycyrrhiza, honey, sorbitol agents
• Ointment bases: Beeswax, lanolin, polyethylene glycol, paraffin, petroleum jelly,
spermaceti, wool fat
• Emulsifying and suspending agents: Acacia, agar, alginic acid, betonte, methyl cellulose,
gelatin, tragacanth, gum.
• Lubricants: Talc, cocoa butter, magnesium stearate
• Solvents: alcohol, glycerine.
• Perfumery agents: Sandal wood oil, rose oil, lavender oil, rosemary oil, musk
• Flavouring agents: cardamom oil, orange oil, fennel oil, Peppermint oil
SWEETENERS
Sweetening agent excipients are substances that sweeten and mask the taste of food,
beverages and medications to make them palatable to the consumer.
Recently the demand greatly increased for natural sweetening agents, especially for
non-caloric sweetening agents, because they are highly potent, useful, safe and
low-calorie sugar alternatives.

Ideal Properties of Sweetening Agents:

• They are required to be effective when used in small concentration.
• They must be stable at a wide range of temperature to which the formulations to be
exposed.
• They should be non-toxic and non-hygroscopic in nature.
• Prolonged use should not produce any carcinogenic effects in the formulations.
• They should have very low or non-calorific value.
• They should be compatible with other ingredients in formulations.
• They should not show batch to batch variations.
• They should be readily available and inexpensive.
Aspartame,
Saccharin sodium,
sucralose, Alitame
 • SACCHARIDE SWEETENERS:
• Saccharide sweeteners include sucrose, glucose, fructose and honey, and these
have high calorific value. The regular use of these sweeteners enhances the
prevalence of diseases like CVS, obesity, diabetes and dental caries.
1. Sucrose: It is a disaccharide obtained from cane juice of Saccharum
officinarum Graminae) and the roots of Beta vulgaris (Chenopodiaceae).
Sucrose is used in many pharmaceutical preparations like syrups and
lozenges. It gives viscosity and consistency to solutions.
2. Honey: Honey is sugar secretion deposited in the honeycombs of Bees Apis
mellifera or A, indica (Apidae). It is solution of dextrose, laevulose and
sucrose. It is used as demulcent, sweetener, nutrient, antiseptic and
ingredient of cough mixture.
3. Sorbitol: It is polyhydric alcohol isolated from the Ash berries (Sorbus
aucupaira, Rosaceae). It is prepared synthetically by catalytic hydrogenation
of glucose. It is used as sweetening agent and vehicle in elixirs, linctuses and
mixtures.
 Binders
• Binders are the agents that impart cohesiveness to the granules. They
are generally added to the formulation to impart plasticity and
increases inter particulate bonding strength mechanically, chemically
or by adhesive to form a cohesive whole, because they promote
cohesiveness, they ae also called adhesives.
• Polymer binders require strong disintegrate and also creates problems
such as rapid over granulation, increase in tablet hardness and
dissolution concert diminish.
• Therefore, natural binders are more applicable for any cosmetic
formulations.
• Plant sources natural binders are like acacia, tragacanth etc.
• Animal sources are chitin, chitosan.
• Marine sources are agar, alginic acid, and microbial sources of binders are xanthan and dextran.
 Advantages of Natural Binder:
(a) They are used for variation of the drug release and thereby influence the
absorption and bioavailability of the integrated drugs.
(b) They are broadly used in the pharmaceutical and food industry as
excipients and additives due to their low toxicity, biodegradable, accessibility
and inexpensive.
(c) They act as vehicles which convey the integrated drug to the absorption
site and are expected to swear the stability of the incorporated drug.
(d) They give precision and accuracy of the dosage, and also improve the
organoleptic properties of the drugs.
TRAGACANTH
• Synonym: gum tragacanth,
• Bio source: It consists of dried gum obtained from the plant
Astragalus gummifer belonging to the family Leguminosae.
• Chemical Constituents:
• Water soluble and is termed as ‘tragacanthin’ (60-70%) & water
insoluble and is known as ‘bassorin’ (30-40%).
• Bassorin actually gets swelled up in water to form a gel, whereas
tragacanthin forms an instant colloidal solution.
USES:
• Demulcent in cough and cold preparations
• To manage diarrhoea.
• Emollient in cosmetics, thickening, suspending agent, binding
agents, use as stabilizer for ice creams, viscosity agents.
• Used in emulsion, lotions, creams, lubricant.
 GUAR GUMS
• Synonyms: Guar gum, Jaguar gum, Guar flour and
Decorpa.

• Biological Source: Guar gum is a seed gum

produced from the powdered endosperm of the
seeds of Cyamopsis tetragonolobus Linn belonging
to family Leguminosae.

• Geographical Source: The major world suppliers

are India, Pakistan and the United States, Australia
and Africa. Rajasthan in western India is the major
guar-producing state, accounting for 70% of the
production.
•
 Chemical constituents:
• The water-soluble part of guar gum contains mainly of a high molecular weight
hydrocolloidal polysaccharide, that is, galactomannan, which is commonly known as
guaran.
• Guaran consists of linear chains of (1→4)—β—D— mannopyranosyl units with
α—D—galactopyranosyl units attached by (1→6) linkages.
• 5–7% of proteins.
 Uses:
• Guar gum is used as a protective colloid, a binding and disintegrating agent,
emulsifying agent, bulk laxative, appetite depressant and in peptic ulcer
therapy.
• Industrially, it is used in paper manufacturing, printing, polishing, textiles
and also in food and cosmetic industries.
• Used in making ointments, skin lotion coz it is cationic thus can achieve
conditioning and thickening properties.
• Skin Cosmetic and hair cosmetics.
• It is a surfactant and hence reduce liquid surface tension and applicable as
shaving creams.
• When used in shampoos it can reduce the use of conditioner.
• Used in gels, lotions, soaps, shampoos, liquid soaps, body washes
• Thickener, conditioner, surfactants, tablet manufacturer.
 ACACIA
Synonym: Gummi africanum, Gum Senegal
Bio Source: Acacia is the dried gummy exudation obtained
from the stems and branches of Acacia Senegal, A.
arabica (L.) W
family: Leguminosae
Geographical Source: drier parts of Anglo-Egyptian Sudan
and the northern Sahara, In India it is found chiefly in
Punjab, Rajasthan and Western Ghats. Sudan is the major
producer of this gum and caters for about 85% of the world
supply
Chemical constituents:
• Acacia consists principally of arabin, which is a complex mixture of
calcium, magnesium and potassium salts of arabic acid.
• Arabic acid is a branched polysaccharide that yields L-arabinose,
D-galactose, D-glucuronic acid and L-rhamnose on hydrolysis.
• Acacia contains 12–15% of water and several occluded enzymes such
as oxidases, peroxidases and pectinases
 Uses:
Demulcent, vital pharmaceutical aid for emulsification and to
serve as a thickening agent.
It finds its enormous application as a binding agent for tablets,
for example, cough lozenges.
It is used in products like skin lotions, eye lines, mascara.
It helps in solubilising oil into water without increasing viscosity.
This property helps to incorporate essential oils to low viscosity
base products such as tonners an spray.
 DILUENTS
• Diluents are known as bulking agent.
• They are the inert substances that use to make up the required bulk of tablet
when the drug dosage itself is inadequate to produce its bulk.
• They act also as fillers in pharmaceutical tablets to increase weight and
improve content uniformity.
• Diluents provide better tablet properties such as improved cohesion or to
promote flow.
• Uses of diluents are to enhance
1.Bulkiness
2. To improve cohesive property
3. To enhance flow.
4. To allow direct compression manufacturing.
Properties of dilutes are:
• They should be non-toxic, inert, biocompatible.
• Non-hygroscopic, physically and chemically stable in formulation,
commercially easily available, colour compatible etc.
• Diluents are classified broadly based on chemical nature and
solubility.
• Natural diluents include starches, hydrolyzed starches, and partially
pre gelatinized starches.
• Common diluents include anhydrous lactose, lactose monohydrate,
and sugar alcohols such as sorbitol, xylitol and mannitol,
• Sucrose/Dextrose: It is natural disaccharide and also used as sweeting agent.
• Lactose (Milk sugar): It is natural disaccharide consisting of glucose and galactose and
obtained from the milk of most of mammals. Lactose is widely used as diluent in tablet,
capsule and to give bulk to the powders. It has no reaction with most of drugs whether
used in hydrous or anhydrous from. Lactose intolerance occurs in patients with deficiency
of the intestinal enzyme lactase.
• Starches or pre-gelatinized starches: Pre-gelatinized is a starch that has been pre-cooked,
dried and ground in to flake or powder form. These are traditional and trusted insoluble
diluents having the additional function of disintegrant.
• Microcrystalline cellulose: It is widely used as diluent / binder in tablet and capsule
formulation. MCC also reduces friction during tablet ejection and facilitate tablet
disintegration.
• Mannitol: It is natural saccharine exudation from the stem of Fraxinus ornus (Oleaceae)and
also isolated from Manna seeds (Alhagi maurorum; Fabaceae). It is chemically obtained by
reduction mannose sugar. It is frequently used as diluent in chewable and dispersible tablet.
It is comparatively less carcinogenic than sugars.
• Sorbitol: Sorbitol is hexahydric alcohol that is isomeric with mannitol. It is
found naturally in berries like Blackberry, Raspberry and Strawberry, and
other fruits like apples, apricots, avocados, peaches and plums. Sorbitol is
also commercially produced and is the most commonly used polyols in the
US. It is used as diluent in tablet and capsules, plasticizer and sweetening
agent. It is commonly used in chewable tablet because of its sweet taste and
is used as a plasticizer for gelatin in capsule formulation. It has low calorific
value than sugars.
• Xylitol: It is a polyalcohol or sugar alcohol, colorless or white solid soluble in
water. It is naturally occurring in small quantities in plums, strawberries,
cauliflower and pumpkin. Cobs of corn (Zea mays; Poaceae) are preferred
source for xylitol. It is used for its sweeting power and cooling effect in many
confectionary formulations.
 VISCOSITY BUILDERS

• They are the substances that are added to the mixture to increase its viscosity
without substantially modifying its other properties like taste.
• These are the substances that increases stability and also increase the viscosity of
the dosage forms to increase palatability or pourability.
• Hence, they are also known as stabilizers.
• Ideal properties of viscosity builders are like non-toxic, produces structured
vehicle, high viscosity during storage.
• Low viscosity at high shearing rates during pouring, exhibits yield stress,
compatible with other excipients, and viscosity should not alter with
temperature.
• Advantages:
• High viscosity inhibits the crystal growth.
• Enhance the physical stability.
• Prevents transformation of metastable crystal to stable crystals.
CARRAGEENAN (CHONDRUS EXTRACT/IRISH MASS EXTRACT)
• Biological Source: It is a sulphated polysaccharide extract of Sea weed / Irish
moss / Red algae Chondrus crispus (Rhodophyceae)]. There are three basic
types of carrageenan viz., kappa, iota and lambda. The lambda type
carrageenan produces viscous solution but is non-gelling. The kappa type
carrageenan forms a brittle gel whereas iota type produces elastic gel.
• Chemical composition: Carrageenan comprises mixture of ammonium,
calcium, magnesium, potassium and sodium sulphate esters of galactose and
3,6-anhydro-D-galactose copolymer.
• Uses: It is used as emulsifying agent, gelling agent, viscosity builder and binder
in tooth paste.
• It is also used as a dissolution rate retarding polymer in sustained release
dosage form.
XANTHAN GUM/CORN SUGAR GUM
• Biological Source: It is produced by fermentation of carbohydrates using
bacteria Xanthomonas campestris.
• Chemical composition: It is cream coloured powder, soluble in cold and hot
water giving highly viscous solution which is stable towards change in pH and
also to heat. It is sodium, potassium or calcium salt of high molecular weight
polysaccharides containing D-glucose, D-mannose and D- glucuronic acid,
additionally pyruvic acid is also present in side chain.
• Uses: It is used as stabilizer, viscosity enhancer and thickening agent.
MISCELLANEOUS:
• Gelatin, Acacia and Tragacanth
 DISINTEGRANTS
• Disintegrants are added to oral solid dosage forms to aid in their disaggregation.
• They are the agents that added to tablet or capsule formulations to promote the breakup of
the tablet and capsule into smaller fragments in an aqueous solution.
• This increases the available surface area and promote a rapid release of the drug substance.
Disintegration is typically viewed as the first step in the dissolution process.
• Several types of disintegrants are used for many years based on their mode of action
namely,
(a) Enhance the action of capillary forces that promote the absorption of water.
(b) Swell on contact with water and
(c) Release gases leading directly to disintegration of the tablet.
(d) Interparticulate repulsive forces.
The general purpose of incorporating one or more disintegrants in the product formulation is
to soften the binding matter that holds together the solid particles that make up the product.
Examples of disintegrants include cross linked polymers, cross linked polyvinyl pyrrolidone
(crospovidone), cross linked sodium carboxymethyl cellulose (croscarmellose sodium), and
the modified starch sodium starch glycolate.
• Recently more rapid disintegrating formulations are stimulated by the
development of "superdisintegrants".
• These derivatives are developed to have greater effectiveness even at
low concentrations.
• They are also effective intragranularly but most important drawback is
these products are hygroscopic and readily absorb moisture.
• Some of the examples are like sodium starch glycolate ( primogel) ,
crosscarmellose, alginic acid, soy polysaccharide, cross povidone
(Kollidon)etc
• Soy Polysaccharide: It is a group of high molecular weight polysaccharides
obtained from soy beans. It is natural superdisintegrants that does not contain
any starch or sugar so can be utilized in nutritional products.
• Lepidium sativum Mucilage: Lepidium sativum (Cruciferae) is commonly
known as Asaliyo. Seeds contain large amount of mucilage, dimeric imidazole
alkaloids lepidine B, C, D, E, and F. Mucilage of L. sativum has been used as
binding, disintegrating and gelling agent.
• Aegle marmelos Gum: It is obtained from the fruits of Aegle marmelos. The
ripened fruit pulp is red in color with mucilaginous and astringent taste. The
pulp contains proteins, carbohydrates, vitamin A & C, angelenine, dictamine,
marmeline, O-methyl fordinol and isopentyl halfordinal Purified Bael gum
polysaccharide contains D-galactose (71% ), D-galacturonic acid (7%), L-
rhamnose (6.5%), and L-arabinose (12.5%). It is used as thickening agent as
well as super disintegrant.
• Hibiscus rosa sinensis Mucilage: It is commonly known as Shoe flower plant,
China rose and Chinese hibiscus, and belongs to the family Malvaceae. Leaves
are rich in mucilage and composed of L-rhamnose, D-galactose, D-galacturonic
acid and D-glucuronic acid. Mucilages are utilized as suspending agent,
thickeners, disintegrants and water retention agent.
• Gellan Gum: Gellan gum is a water-soluble polysaccharide produced as a
fermentation product by bacteria Pseudomonas elodea. The disintegration
ability of Gellan gum is due to the instantaneous swelling, when it comes in
contact with water.
• Ficus indica Fruit Mucilage: Mucilage is obtained from the pulp of fruits of
Ficus indica (Cactaceae). Fruits resemble cherry and have nutritional as well as
medicinal value. Mucilage is utilized as super disintegrant.
• Miscellaneous: Guar Gum, Starch, Locust bean gum, Xanthan gum, Chitosan,
Agar and Fenugreek seed mucilage possess disintegrating property. For details
refer above sections.
 FLAVOUR

• Flavourants are also selected on the basis of the taste of the drug to be incorporated.
• They are mainly of two types natural and synthetic. Natural flavouring agents are dried
and powdered forms of spices, herbs, roots and stems of plants such as ginger, coves
etc.
• Some other natural sources of flavouring agents are like essential oils from the various
aromatic plants, vanilla, peppermint, orange, lemon, garlic and onion.
• Synthetic favours are like benzyldehyde flavours from bitter almond, cherry pits,
decylaldehyde from citrus fruits like orange, and cinnamic aldehyde flavour from
cinnamon plant.
• Flavouring agents are classified according to the sources
1. Natural flavour (Van Cinnamic acid, Limonene. Menthol, Eugenol, Eucalyptol,
Camphor).
2. Microbial favour (alcohol, esters, lactones, diacetyl, methyl ketone).
3. Enzymatic flavour (esters tergan vanilla).
4. Synthetic flavour (allyl pyrazine, methoxy pyrazines).
• Salt is masked by Butterscotch, maple
• Bitter is masked by Wild cherry, walnut chocolate-mint licorice
• Sweet is masked by Fruit, berry, vanilla.
• Acid is masked by Citrus.
• Cardamom oil: It is obtained from fruits of Elettaria cardamomum
(Zingiberaceae). It contains cineole, terpineol, borneol and cinnamaldehyde. It
is used as aromatic and flavouring agent
• Orange oil: It is obtained from expression of fresh peels of Citrus aurantium
(Rutaceae). It contains citral, citronellal and limonene
• Fennel oil: It is obtained from fruits of Foeniculum vulgare (Leguminosae). It
contains anethole and fenchone.
• Ginger: it consists of rhizomes of Zingiber officinalis (Zingiberaceae). It contains
shagol as main constituent.
• Saffron: refer colorants
• Peppermint oil: it is obtained from the fresh leaves of mentha piperita
(Lamiaceae), containing menthol as chief constituents.
• Wild cherry syrup: it is obtained from the inner bark of Wild cherry tree
(Prunus serotina; Rosaceae).
 PERFUMES
• Perfumery agents are the active ingredients or enhancers which impart the aroma to
the perfume compositions.
• The word perfume derives from the Latin perfumare, meaning smoke through"
whereas perfumery is the art of making perfumes.
• They are complex combinations of natural and/or man-made substances that are
added to many consume products to give them a distinctive smell.
• Perfume is a mixture of essential oils or aroma compounds used to give the human
body "a pleasant scent.
• Perfume is derived from various sources viz.
1. Plant sources: Bark, Flowers and blossoms. Fruits, Leaves and twigs, Roots,
Rhizomes and bulbs. Seeds, Woods;
2. Animal sources: Musk, Ambergris, Civet, Hyraceum, Honey comb.
3. Other natural sources: Lichens, Seaweed.
4. Synthetic sources: Calone, a compound of synthetic origin, imparts a fresh ozonous
metallic marine scent that is widely used in contemporary perfumes.
• Many modern perfumes contain synthesized odorants. Synthetics can provide
fragrances which are not found in nature.
• Rosemary oil: It is obtained from fresh flowering tops of Rosmarinus
officinalis (Labiatae). It consists of a-pinene, limonene, camphene, borneol,
and bornyl acetate.
• Musk: It is obtained from glandular secretions from animals such as Musk
deer (Moschusmoschiferus; Moschidae). It consists of muscone.
• Civet: It is by product of anal glands of exotic civet cats (Civettictis viverra;
Viverridae). contains civetone
• Sandal wood oil: It is obtained by steam distillation of heartwood of
Santalum album (Santalaceae). It is also called chandan. It consists of
santalol (sesquiterpene alcohol).
• Rose oil: It is obtained from fresh flowers of Rosa gallica (Rosaceae). It
consists of linalool, citronellol and geraniol.
• Lavender oil: It is obtained from fresh flowering tops of Lavandula
angustifolia, L. officinalis and L. latifolia (Labiatae). It consists of a-pinene,
limonene, ocimene, camphene, borneol, linalool and lavendulyl acetate.
THANK U