herbal excipients and herbal formulations

1. Herbal excipients:
Excipients are defined as ‘the substance used as a medium for giving a medicament. The
specific application of natural polysaccharide polymers in pharmaceutical formulations
include to aid in the processing of the drug delivery system during its manufacture,
protect, support or enhance stability, bioavailability or patient acceptability, assist in
product identification, or enhance any other attribute of the overall safety, effectiveness
or delivery of the drug during storage or use . Several pharmaceutical excipients of plant
origin, like starch, agar, alginates, carrageen an, guar gum, xanthan gum, gelatin, pectin, acacia,
tragacanth, and cellulose find applications in the pharmaceutical industry as binding agents,
disintegrates, sustaining agents, protective’s, colloids, thickening agents, gelling agents, bases
in suppositories, stabilizers, and coating materials.
As plants sources are renewable and can be cultivated or harvested in sustainable manner, can
supply constant availability of raw material. Waste from food industry can be achieved as a
raw material to extract herbal excipients. These are other reasons for increase in demand of
herbal material as excipients. However, substances from plant origin also pose several potential
challenges such as being synthesized in small quantities and in mixtures that are structurally
complex, which may differ according to the location of the plants as well as other variables
such as the season. This may result in a slow and expensive isolation and purification process.
Another issue that has become increasingly.
Pharmaceutical Excipient
Pharmaceutical excipients can be defined as non-active ingredients that are mixed with
therapeutically active compounds to form medicines. The ingredient which is not an active
compound is regarded as an excipients. Excipients affect the behavior and effectivenessof
thedrug product more and more functionality and significantly. The variability of active
compounds, excipients and process are obvious components for the product variability.
Classification of Excipients
Excipients are commonly classified according to their application and function in the drug
products:
Herbal Sweetners
Binders, diluents
Disintegrants

2. Colorants
Viscosity builders
Perfumery agents and flavoring agents
Advantage of Herbal Excipients
1. Biodegradable- Naturally occurring polymer produced by all living organisms. They show
no adverse effects on the environment or human being.
2. Biocompatible and Nontoxic- Chemicallynearly all of these plant materials are
carbohydrates in nature and composed of repeating monosaccharide units. Hence they are non-
toxic.
3. Economic- They are cheaper and their production cost is less than synthetic material.
4. Safe and devoid of side effect-They are from a natural source and hence, safe and without
side effects.
5. Easy availability-In many countries they areproduced due to their application in man.
Disadvantages of Herbal Excipients
1. Microbial contamination– During production, they are exposed to external environment
and hence, there are chances of microbial contamination.
2. Variation– Synthetic manufacturing is controlled procedure with fixed quantities of
ingredients while production of natural polymers is dependent on environment and various
physical factors.
3. The uncontrolled rate of hydration—Due to differences in the collection of natural
materials at different times, as well as differences in region, species, and climate conditions the
percentage of chemical constituents present in a given material may vary.
4. Slow Process– As the production rate is depends upon the environment and many other
factors, it can’t be changed. So natural polymers have a slow rate of production.
5. Heavy metal contamination– There are chances of Heavy metal contamination often
associated with herbal excipients.

3. Colorants
Colorant/color additiveis a substance that is added or applied in order to change the Colour of
a material or surface. Colorants can be used for many purposes including printing, painting,
and for Colouring many types of materials such as foods and plastics. Colorants work by
absorbing varying amounts of light at different wavelengths (or frequencies) of its spectrum,
transmitting (if translucent) or reflecting the remaining light in straight lines or scattered.
Most colorants can be classified as dyes or pigments, or containing some combination of these.
Typical dyes are formulated as solutions; while pigments are made up of solid particles
suspended and are generally suspended in a vehicle (e.g., linseed oil). The color a colorant
imparts to a substance is mediated by other ingredients it is mixed with such as binders and
fillers are added, for example in paints and inks. In addition, some colorants impart Colour
through reactions with other substances. Colorants, or their constituent compounds may be
classified chemically as inorganic (often from a mineral source) and organic.
In India, there are more than 450 plants that can yield dyes. In addition to their dye-yielding
characteristics, some of these plants also possess medicinal value. The use of natural products
together with their therapeutic properties is as ancient as human civilization and for a long time,
mineral, plant and animal products were the main sources of drugs.
Classification
• Natural dyes obtained from plants - Berry, flower, bark, leaf, seed etc. (e.g. Catechu,
Indigofera, Myrobalan and Pomegranate).
• Natural dyes obtained from insects – Cochineal and lac.
• Natural dyes obtained from animal – Mollusk, murex snail, cuttlefish and shellfish.
• Natural dyes obtained from mineral – Clay, ochre and malachite.
7.4 Sweeteners
A sugar substitute is a food additive that provides a sweet taste like that of sugar while
containing significantly less food energy than sugar-based sweeteners, making it a zero-calorie
or low-calorie sweetener. Artificial sweeteners may be derived through manufacturing of plant
extracts or processed by chemical synthesis. Sugar alcohols such as erythritol, xylitol, and
sorbitol are derived from sugars. In 2017, sucralose was the most common sugar substitute
used in the manufacture of foods and beverages.

4. Steviol glycosides are a gaggle of extremely sweet diterpene glycosides contained within the
leaves of stevia. Mogrosides, extracted from monk fruit are a gaggle of cucurbitane-type
triterpenoid glycosides. Glycyrrhizin is an oleanane-type triterpenoid organic compound
derived from the underground elements of Glycyrrhiza plant. Dates are wonderful sweeteners
loaded with K, copper, iron, manganese, metallic element and pyridoxal. The syrup is an
excellent sweetener enriched in manganese, Calcium, Potassium, and Zn.
Stevia
Stevia rebaudiana is a small perennial growing up to 6580 cm tall, with sessile, oppositely
arranged leaves. Different species of Stevia contain several potential sweetening compounds,
with S. rebaudiana being the sweetest of all.
Chemical constituents
Eight ent-kaurene glycosides namely dulcoside A, rebaudiosides A to E, steviolbioside, and
stevioside produce the sweet taste sensation. These glycosides are mainly compounds of the
diterpene derivative steviol.
Pharmacological actions
Stevia is used in many parts of the world as a non-caloric sweetener. Along with sweetness, a
bitter taste is also felt in humans. As an extract, this herb was found to have similar potency
with regard to sweetness as a 10% sucrose solution at either pH 3.0 or 7.0.
Uses of Stevia
• Stevia is safe for diabetics, as it does not affect blood sugar levels.
• Stevia does not have the neurological or renal side effects as other artificial sweeteners.
• Stevia possess anti-fungal and anti-bacterial properties in addition to its other versatile uses.
It can be safely used in herbal medicines, tonics for diabetic patients and also in daily usage
products such as mouthwashes and toothpastes.
• Mild Stevia leaf tea offers excellent relief for an upset stomach.
Erythritol: It is another low-calorie sweetener. It’s a sugar alcohol found naturally in certain
fruits. However, powdered erythritol available for purchase is most likely made via an
industrial process. It contains 0.24 calories per gram, or about 6% of the calories in an equal
amount of sugar, with 70% of the sweetness. Erythritol doesn't spike blood sugar or insulin
levels and has no effect on blood lipids like cholesterol or triglycerides.It’s absorbed into the
body from the intestine but eventually excreted from the kidneys unchanged.

5. 3. Glycyrrhiza glabra: Liquorice roots, which are wrinkled and brown on the outside and
yellow on the inside, contain glycyrrhizin, a compound that is 50 to 150 times as sweet as cane
sugar.
4. Thaumatin: The Thaumatins are a family of very sweet proteins present in the fruits of the
tropical plant Thaumatococcus danielli (marantaceae) a bushy plant.Thaumatin elicits a very
sweet taste that is rated to be 2000 to 10000 times sweeter than sucrose, depending on purity
and concentration.Thaumatin I and II are soluble in water and dilute alcohol.Thaumatin is
effective at masking bitter notes often associated with pharmaceuticals or vitamins.
5. Agava nector: juice of core of agava, a succulent plant native of maxico, used as honey
substitute more sweeter and thinner than honey.
5. Maple syrup: from sap of maple tree collected filtered and boiled to an extremely sweet
syrup with distintive flavour.
7.5 Binders
Binder excipients are formulated to act as an adhesive to literally “bind together” powders,
granules and other dry ingredients to impart to the product the necessary mechanical strength.
They can also give volume to low active dose tablets. Commonly used in wet granulation,
binders are added to create a more effective and predictable granule formation. Binders are
classified according to their application. For example, solution binders are dissolved in a
solvent, such as gelatin, cellulose, cellulose derivatives, polyvinylpyrrolidone, starch, sucrose
and polyethylene glycol.
Pectin: Pectins are non-starch, linear polysaccharides extracted from the plant cell walls. In
the food industry, folic acid incorporated microcapsules were prepared using alginate and
combinations of alginate and pectin polymers so as to improve stability of folic acid. The
blended alginate and pectin polymer matrix increased the folic acid encapsulation efficiency
and reduced leakage from the capsules as compared to those made with alginate alone; they
showed higher folic acid retention after freeze drying and storage.
Gums and mucilage: gum arabica (Acacia spp.), gum tragacanth (Asiatic astraglus spp),
Khaya gum (grandifoliola spp.), gum ghatti (anogeissus latifolia), locust gum (certonia siliqua)
Obtained by produced injury to plant owing unfavourable conditions, drought, by break down
of cell walls.
Guar gum: Guar gum comes from the endosperm of the seed of the legume plant Cyamopsis
tetragonolobus. Refined guar splits are obtained when the fine layer of fibrous material, which
forms the husk, is removed and separated from the endosperm halves by polishing. Strong acids

6. cause hydrolysis and loss of viscosity, and alkalies in strong concentration also tend to reduce
viscosity. It is insoluble in most hydrocarbon solvents.
Khaya gum: Khaya gum is a polysaccharide obtained from the incised trunk of the tree Khaya
grandifoliola (family Meliaceae). The fact that the gum is naturally available, inexpensive and
non-toxic has also fostered the interest in developing the gum for pharmaceutical use. Further
work has also shown its potential as a directly compressible matrix system in the formulation
of 61 controlled release tablet.
Mimosa pudica:mucilage obtained from seeds of Mimosa pudica. Contains d-xylose and d-
glucoronic acid have high swelling index, used in sustained release tablets, buccal disc, good
disintegrant, good binder.
Fenugreek mucilage: obtained from trigonella foenum-graceum (leguminasae). Contains
mannose, galactose, and xylose. Provide good hardness and friability, good disintegration and
dissolution time.
Gelatin: protein obtained from partial hydrolysis of animal collagenous tissues like bone, skin,
tendon and ligaments. Used in preparation of suppositories, pastilles, pessaries and pastes, as
emulsifying agent in injections, used in capsule shell formation
Starch: multipurpose excipient applied as filler, disintegrant or binder in tablet formulation
used in granules form.
Different starches like rice, maize, corn wheat are also used a a natural binding agents. They are
added to the tablet formation to increase inter-particulate bonding strength in the tablets. The binder
is added either in dry mix or mix in granulating liquid and form matrix with fillers and drug
embedded in it.
7.6 Diluents
Diluents act as fillers in pharmaceutical tablets to increase weight and improve content
uniformity. 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. Diluents provide better tablet properties such
as improved cohesion or to promote flow. Mannitol is one of the costliest diluents, however, it
is still often used due to the sensation it provides when it is used in chewable tablets. Diluents
must be non-toxic, commercially available in acceptable grade, physiologically inert, and
physically and chemically stable by themselves as well as in combination with active
pharmaceutical ingredients (APIs).

7. Lactose: present in milk produced by cow,sheep, goat and other mammals. It’s a disaccharide
made up of glucose and galactose. Used as diluent in tablet, capsules and in dry powder
inhalations.
Mannitol: exudation from stem of Fraxinus ornus family oleaceace. Naturally occurring
alcohol found in fruits and vegetables used as osmotic diluents and bulk sweetners.
Viscosity builders
Viscosity modifiers are designed to change the thickness or texture of pharmaceutical
ingredients. Viscosity modifiers can include such products as thickeners, texturizers, gelation
agents and stiffening agents. Many viscosity modifiers can be used to convert liquids to gels,
pastes or powders to aid formulators in creating the ideal product for end users. A viscosity
modifier can decrease the thickness of a liquid to improve pour ability and ultimately make it
more palatable.
Various thickeners are found in nature or are derivatives of natural thickeners. These
ingredients are polymers that absorb water to expand and increase viscosity. Polyose
derivatives like hydroxyethylcellulose are often employed in products like shampoo or body
washes. Gum is another example of a naturally derived thickener. Others embrace algarroba
bean gum, xanthan gum, and gelatin. Plants and different gums are employed in sensible
applications primarily to thicken or gel binary compound systems and to regulate water. They
will conjointly operate as adhesives, foam stabilizers and impart different specific properties.
These thickeners will be employed in any formula that contains a high level of water. Typically,
they will be inconsistent, as a result of clear formulas to become cloudy, and feel sticky on
skin.
Xanthan gum is an associate example of high relative molecular mass additional cellular
polysaccharide produced by the fermentation of the gram negative bacteria xanthomonas genus
campestris.
Carrageenan: natural polysaccharide obtained from edible red seeweeds Chondrus crispus
family rhodophyllaceae also known as carrageenan moss or Irish moss.
Disintegrants
Disintegrants are added to oral solid dosage forms to aid in their de-aggregation. Disintegrants
are formulated to cause a rapid break-up of solids dosage forms when they come into contact
with moisture. Disintegration is typically viewed as the first step in the dissolution process.
Examples of Disintegrants include Crosslinked polymers, including crosslinked
polyvinylpyrrolidone (crospovidone), crosslinked sodium carboxymethyl cellulose

8. (croscarmellose sodium), and the modified starch sodium starch glycolate. Some of the natural
disintegrating agents are shown below-
1. Lepidus sativum
Lepidium sativum (family-Cruciferae) known as asaliyo and widely used as herbal medicine
and pharmaceutical excipient as disintegrating agent.
2. Isapghula Husk (Plantago ovata)
The seeds of Plantago ovata were soaked in distilled water for 48 hrs and then boiled for few
minutes for complete release of mucilage into water. Mucilage of Plantago ovata at a
concentration of 2 % is also a good disintegratingagent having the additional advantage of
being natural.
3. Hibiscus rosa sinesis linn.
Mucilage Hibisicus rosa-sinensis linn. Of the Malvaceae family is also known as the shoe
flower plant, China rose, Chinese hibiscus. The plant is available in Indian in large quantities
and its mucilage has been found to act as superdisintegrant. The plant contains
cyclopropanoids, methyl sterculate, methyl-2-hydroxysterculate, 2- hydroxysterculate malvate
and β-rosasterol.
4. Guar gum
5. Starch
Flavoring agents: Flavors are the mixed sensation of taste, touch, smell & sight. Nowadays,
many artificial flavors are manufactured with the help of technology in flavoring industries.
Many pharmaceutical industries use flavors in many formulations like: cough syrups,
sedatives, anti-malarial and anti-biotic. Flavors are used as taste masking agents which hides
the unpleasant taste or order of dosage form. A flavor enhances the likelihood of medicine and
makes them more compatible for patient’s administration. Due to the use of flavors in dosage
form children take medicines without any problem. Flavoring agents may be artificial or
natural. Artificial flavoring agents are synthesized in laboratories while natural flavoring agents
are extracted from plants.Sweetening agents also separated from plants and also manufactured
synthetically. Examples of dosage form in which flavoring agents are used are as follow:
Tablets, Pills, Pallets, Capsules, Pastes, Syrups, Emulsions, Suspensions, Mouth washes etc.
Examples of flavoring agents are Black pepper, Cardamom, Fennel, Ginger, Peppermint,
Nutmeg and saffron.

9. Perfumery agents: An active ingredient is a compound which imparts the aroma to the
perfume compositions or enhances the aroma of an existing perfume compostion. Perfumary
agents includes Musk, sandalwood oil, Rose oil, Jasmine oil, benzoin, Turpentine and Levender
oil.
Few flavouring and perfuming agents are:

14. Herbal formulations:
Herbal formulations means a dosage form consisting of one or more herbs or processed
herbs in specified quantities to provide specific nutritional, cosmetic benefits meant for
use to diagnose, treat, mitigate diseases of human beings or animals, alter the structure
or physiology of human beings or animals.

22. 1.Nanoparticles
A nanoparticle or ultrafine particle is usually defined as a particle of matter that is
between 1 and 100 nanometres in diameter. The term is sometimes used for larger
particles, up to 500 nm, or fibers and tubes that are less than 100 nm in only two
directions.

23. 3.Liposomes

24. -

25. Herbal syrup: Syrup is a concentrated mixture of sugar in purified water. The oral use of
liquid pharmaceutical has generally been justified on the basis of ease of administration to those
individuals who have difficulties in swallowing solid dosage forms.
Ayurvedic herbal cough syrup comprising goodness of herbs such as Tulsi, Liquorice, Ginger,
Vasaka which has been reported to provide effective relief in cough without causing adverse
effects like those associated with the use of antihistamines. Combination of these herbs with
honey is intended to provide additive benefit in relieving symptoms of acute non-productive
cough.
Preparation of Herbal Syrup: An herbal syrup is prepared by combining a concentrated
decoction with either honey or sugar, and sometimes alcohol. The base of such a syrup is a
strong herbal decoction. Mixing a decoction with honey or sugar helps to thicken and preserve
the decoction. This increases the shelf life of the decoction and often creates a soothing
application that benefits situations such as sore throat, cough, dry irritated tissues, and digestive
issues. The added sweetener can also help to increase the palatability of some herbs. Many
folks, including children, find syrups to be delicious. The basic proportions you want to use are
2 parts herbal decoction to 1 part honey or sugar. This is called a 2:1 ratio. This means that if
you start with your herbs added to 4 cups of water and simmer down the liquid to 2 cups of
decoction, then you will want to add 1 cup of honey or sugar to create and adequately preserve
your syrup. Some herbalists like to use a 1:1 ratio of decoction to honey/sugar while others find
a 1:1 ratio to result in a syrup that is too sweet. The increased amount of honey/sugar relative
to decoction in a 1:1 ratio will be better preserved and hence last longer.
Examples: raspberry syrup, cherry syrup, glycyrrhiza syrup, tolu balsam syrup, garlic syrup
Herbal Tablets: Tablets may be defined as the solid unit dosage form of medicament or
medicaments with suitable excipients and prepared either by molding or by compression. It
comprises a mixture of active substances and excipients usually in powder form, pressed or
compacted from a powder into a solid dose. The excipients can include diluents, binders,
glidants and lubricants to ensure efficient tableting. Disintegrants to promote tablet break-up
in the digestive tract; sweeteners or flavours to enhance taste; and pigments to make the tablets
visually attractive or aid in visual identification of an unknown tablet. A polymer coating is
often applied to make the tablet smoother and easier to swallow, to control the release rate of
the active ingredient, to make it more resistant to the environment (extending its shelf life), or
to enhance the tablet's appearance.

26. Tablet Evaluation: Before a tablet is released out into the market it has to pass a few quality
checks, which is mandatory.
Evaluation of tablet includes the assessment of tablets physical, chemical and biological
properties. To studies them the following test are formulated:
• Appearance • Size and Shape, • Organoleptic properties, • Uniformity of thickness, •
Hardness, • Friability, • Determination of pH • Specific gravity • Stability testing
Novel drug delivery system:
“Novel Drug delivery System (NDDS) refers to the formulations, systems and technologies
for transporting a pharmaceutical compound in the body as it is needed to safely achieve its
desired therapeutic effects. Drug delivery systems (DDS), are based on approaches that are
interdisciplinary and that combine pharmaceutics, bio conjugate chemistry, and molecular
biology.It is a novel approach to drug delivery that addresses the limitations of the traditional
drug delivery systems. Our country has a vast knowledge base of ayurveda whose potential is
only deing realized in the recent years.
The therapeutic benefits of these new systems include: Increased efficacy of the drug, Site
specific delivery, and decreased toxicity/side effects, increased convenience, viable treatments
for previously incurable diseases, Potential for prophylactic application, Better patient
compliance.
PHYTOSOMES
Phytosomes are also known as herbosomes, are recently added herbal formulations that are
better absorbed than extracts. Phytosomes are prepared through the attachment of individual
ingredients of herbal extracts to phosphatidyl-choline, resulting in a formulation having higher
solubility and hence better absorption leading to promoted pharmacokinetic and
pharmacodynamic properties compared to the conventional herbal extracts. Various popular
herbal extracts including Ginkgo biloba, grape seed, hawthorn, green tea, and ginseng have
been incorporated in phytosomes. The active components of these herbal extracts were
successfully bound to phosphatidyl choline. Phytosomes, also known as phospholipid
complexes, are well-known delivery systems that are closely related to liposomes in terms of
their structure and configuration. Phytosomes have a higher capacity for nutraceutical
compounds to be added to them, as they have a quite stable, chemically bound structure. Plant
extracts can bind quite easily to phosphatidylcholines due to the presence of terpenoids and
flavonoids. As delivery systems, phytosomes have proved to be superior to liposomes. The
chemical bonding ensures the stability of phytosomes, enhances the encapsulation efficiency
and stability of bioactives, generally at a stoichiometric molar ratio of 1:1 or 1:2

27. (phospholipids: phytochemicals) Phytosomes were found to improve solubility, permeability
rate and bioavailability of active compounds in various cases and inhibit or delay physical and
chemical degradation and could be implemented without generating any toxic effects. The
choline head of the phosphatidylcholine molecule binds to these compounds while the fat-
soluble phosphatidyl portion comprising the body and tail envelops the choline-bound material.
The phytosome process also intensifies the action of herbal compounds by improving
absorption, increasing biological activity, and enhancing delivery to the target tissue.
Methods of Preparation: For the preparation of Phytosomes the phytoconstituents like
bioflavonoids, flavolignan and polyphenolic compounds reacting drop by drop by the solution
of natural or synthetic phospholipids like Phosphatidycholine with vigorous stirring.
Phytosomes of ginsenoside, puerarin and kushenin are prepared in this manner. Another
example is the Curcumin phospholipids complexes which can be prepared when the ethanol
solution of the hydro-alcoholic extract of turmeric rhizomes adding the phospholipids, under
reflux and with stirring. Phytosomes which are prepared by the non solvent, freeze drying,
spray drying or vacuum drying are called the prepared complex phytosome.