Herbal Excipients in Drugs

By
Rishika Gupta

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Contents
●
Significance of Herbals
●
Colorants
●
Sweeteners
●
Binders
●
Diluting agent

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Excipient
●
Pharmaceutical excipients can be defined as nonactive
ingredients that are mixed with therapeutically active
compound(s) to form medicines.
●
The ingredient which is not an active compound is regarded
as an excipient.
●
Excipients affect the behaviour and effectiveness of the drug
product more and more functionality and significantly.
●
The variability of active compounds, excipients and process
are obvious components for the product variability

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Significance of Natural Excipients
●
These polymers such as natural gums and mucilage are
biocompatible, cheap and easily available and are
preferred to semi synthetic and synthetic excipients
because of their lack of toxicity, low cost, availability,
soothing action and non irritant nature

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Natural Colorants
●
Highly coloured substances found in plants and animals.
●
A dye and pigment differ in respect that, dye is actually
absorbed by the material when applied to fibres to give it a
permanent colour which is resistant to the action of light,
water or soap.
●
A pigment on other hand is only applied to the surface.
●
The coloured compounds are known as chromogen and
bear chromophore group and/or auxo chrome capable of
absorbing light in the near UV regions and appears as
coloured substance.
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Natural Colorants
Source Compound Color Shade
Diaryl heptanoids
Curcuma longa Curcumin Yellow
(Turmeric)

Naphthoquinones
Lawsonia inermis Lawsone Orange
(Henna) Lawsonia alba

Juglans regia(Walnut) Juglone Brown

Juglans nigra
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Henna
●
Source: dried leaves of Lawsonia inermis (L. Alba) .
●
Family: Lythraceae
●
GS: North Africa, India, Srilanka
●
Constituents: Phenolic glycosides, Coumarins, Xanthene, Flavonoids,
Fats, Resin and Henna tannin.
●
Coloring matter: Lawesone, which can be extracted from the leaves
by NaHCO3.
●
Lawsone is 2,5-dihydroxy-1,4-naphthoquinone ■ used to dye protein
fiber in an orange shade, in conjuction with dihydroxyacetone as a
sunscreen agent .

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Turmeric
●
Source: dried rhizomes of Curcuma longa
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Family: Zingiberaceae
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GS: Subtropical regions
●
Contains a yellow natural pingment, which dissolves in alcohol to
form a deep yellow solution.
●
Alkali changes the colour to reddish orange
●
Constituents: 5% curcumins and its derivatives, which are diaryl
heptanoid compounds of dark yellow color. Curcumin,
desmethoxy curcumin and bisdesmethoxy curcumin.

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Turmeric
●
Use: principally as a constituents of curry powder. ■ It
imparts dark yellow color to food preparations.
●
A tincture is used for preparation of turmeric paper which
is used as a test for boric acid and borates
●
Curcumin is used as a yellow coloring matter but the
color is fugitive in solution.

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Natural sweeteners
●
Sweetening agents either evoke sweet taste or enhance the
perception of sweet taste. Natural sweetening agents are
preferred over synthetic sweetening agents since they do not
have any adverse impact on health.
●
Two types of sweeteners are available: natural sweeteners of
plant origin and artificial or synthetic sweeteners.
●
Non-saccharide natural sweetening agents are low calorific,
nontoxic and super sweet (100 to 10,000 times sweeter than
sugar) in nature and can overcome the problems of sucrose
and synthetic sweeteners.

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Natura sweeteners
●
Natural sweeteners are useful sugar substitutes for diabetic
patients.
●
The active sweet principles stored in plants can be grouped
under: terpenoids, steroidal saponins, dihydroisocoumarins,
dihydrochalcones, proteins, polyols, volatile oils, etc. in nature.
●
Nutritive sweeteners: sorbitol, mannitol, xylitol, lactitol, mixture of
glucosylsorbitol & glucosylmannitol, fructose
●
Non-nutritive sweeteners: Aspartame, Saccharin, cyclamate,
acesulfane-k and alitame
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Plant based natural sweeteners: Stevioside, Glycyrrhizin,
Neohesperidin, Thaumatin, Monellins, Sucralose
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Natural Sweeteners
Source
Stevia rebaudiana (Compositae) Leaf
Glycyrrhiza glabara (Leguminosae)
Citrus aurantium (Rutaceae) Bitter
orange
Thaumatococcus danielli
(Marantaceae)
Compound
Stevioside & Rebaudioside (160-170
times sweeter than sucrose)
Licorice root Glycyrrhizin (50-100
times)
Neohesperidin dihydrochalcone (330
times)
fruit aril Thaumatin (3500 times)
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Stevia
●
Source: extracted from a south American plant “Stevia rebaudiana”
●
Family: Compositae
●
GS: Paraguay, Brazil, Japan, China, Taiwan, Thailand, Malaysia
●
The dried leaves of the plants, the water extract of the leaves and
the purified ingredients of the extract are used as sweetening
agents.
●
Stevioside can be isolated from the leaves of Stevia by extraction
with water or water-ethyl alcohol mixture and further purified by
treatment with calcium or MgOH or Mg(CO3)2.

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Stevia
●
The ratio of rebaudioside A to stevioside can be increased by extraction with
methanol.
●
2 compounds isolated and purified from Aqueous extract are stevioside and
rebaudioside A.
●
Both these compounds are diterpene glycoside.
●
Stevioside is 160-170 times sweeter than sucrose.
●
Its sweetness is tainted with a bitter and undesirable after taste. But its wide
use in Japan for over 20 years did not produce any known deleterious side
effects.
●
In USA the FDA allowed the use of Stevia as a diet supplement but not as
sweetener or an ingredient of food.

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Stevia
●
Stevioside and rebaudioside A give rise to its principal
steviol which has been reported to be mutagenic.
●
Stevioside, the more important product, is used as table
top sweetener, in confectionaries, soft drinks and fruit
products.
●
The sweetness intensity of rebaudioside A is
approximately 1/3rd higher than that of stevioside and its
taste characteristics are also superior, but it is unstable
and gets decomposed to light.

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Natural Binding agents
●
Binders are agents employed to impart cohesiveness to the granules.
This ensures the tablet remains intact after compression.
●
Binders are added to tablet formulation to impart plasticity and thus
increase the interparticulate bonding strength within the tablet.
●
To hold various powders together to form a tablet is a binder, fillers
usually do not have good binding capacity, binder is either added in dry
mix or mix in granulating liquid, binder form matrix with fillers and drug
embedded in it, on drying solid binder forms glue which holds the
particles together, the wet binder is the most important ingredient in the
wet granulation process, most binders are hydrophilic & most times
soluble in water.
●

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Advantage: Natural binders
●
low toxicity, biodegradable, availability and low cost
●
can also modify the release of drug, thereby, influencing
the absorption and subsequent bioavailability of the
incorporated drug
●
Increase stability, precision and accuracy of dosage form
●
improve the organoleptic properties of the drugs where
necessary in order to enhance patient adherence

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Disadvantage: Natural binders
●
Over time they occasionally lead to tablet hardening and
a decrease in dissolution performance.
●
When polymer binders are chosen, the addition of strong
disintegtants such as super disintegrants is typically
required but these are considerably expensive and have
a negative effect on product stability as well as film
coating appearance of the finished products
●
E.g. Plant starch, pregelatinized starch, gelatin, Plant
Gums: acacia, tragacanth

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Gelatine
●
Syn: Gelfoam, Puragel, Gelatina
●
Source: A protein obtained by partial hydrolysis of animal collagenous
tissues like bone, skin, tendon and ligaments.
●
Description: faintly yellow amber coloured solid with characteristic odour.
Its available in the form of flakes, sheets, shreds, powder or granules.
●
Properties: Gelling strength:150-200
●
Solubility: practically insoluble in water, most of organic solvents, fixed
oil and volatile oils
●
Soluble in hot water, glycerol, acetic acid ■ In 5-10 times water, forms
gel below 35-40 degree C

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Gelatine
●
Constituents: Glycine (25-27%), Alanine, Glutamic acid, Proline,
Arginine, Aspartic acid and Hydroxy proline, Isoleucine, Leucine,
phenyl alanine, tryptophan
●
ChemicalTest:
●
Powder, when heated with soda lime, evolves ammonia gas
●
Powder + HgNO3 white ppt, on heating turn to red-brick red
colour (Millon’s reagent)
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Incompatibilities: Tannins and Formaldehyde
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Method of sterilization: Dry heat Sterilization

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Gelatine
●
Use: preparing suppositories, pastilles, pessaries, pastes.
●
Absorbable gelatine sponge: Haemostatic ■ Emulsifying
agent, vehicle for injection
●
Manufacture of hard and soft gelatine capsule
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Tablet binder
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Stabilizer, thickener,
●
2% mascara preparation
●
Storage: tight container in dry place

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Natural diluents
●
Diluents are often added to tablet formulations for secondary
reasons like to provide better tablet properties such as: i)To provide
improved cohesion ii)To allow direct compression manufacturing
iii)To enhance flow iv)To adjust weight of tablet as per die capacity
●
should neither support microbiological growth in the dosage form nor
contribute to any microbiological load
●
should neither adversely affect the dissolution of the product nor
interfere with the bioavailability of active pharmaceutical ingredient
●
should preferably be colourless or nearly so.

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Natural diluents
●
should not react with the drug substance and moreover it should not
have any effect on the functions of other excipients
●
should not have any physiological or pharmacological activity of its
own
●
should have consistent physical and chemical characteristics
●
should neither promote nor contribute to segregation of the
granulation or powder blend to which they are added
●
should be able to be milled (size reduced) if necessary in order to
match the particle size distribution of the active pharmaceutical
ingredient

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Lactose
●
Source: a natural disaccharide consisting of galactose and
glucose and obtained from milk of most of mammals.
●
Syn: Milk sugar, Lactin
●
Description: white crystalline powder with odourless and faintly
sweet taste. It is stable in air but readily absorbs odours
●
Several varieties of lactose are available: anhydrous alpha,
alpha monohydrate and anhydrous beta
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Hygroscopicity: absorbs insignificant amount of moisture at 25
degree at relative humidity up to about 90%

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Lactose
●
Solubility: freely soluble in water while practically insoluble in CHCl3,
ethanol and ether
●
Constituents: O-beta-D-galactopransosyl-(1-4)- alpha-D-
glucopyranose
●
Chemical test:
●
0.25 g lactose + 5 ml water + 5 ml of 10M NH3 heat in water bath at
80 degree for 10 minutes, red colour develops
●
5 ml hot saturated solution of lactose + 5 ml NaOH warm yellow
liquid, finally brownish red on adding several drops of cupric
sulphate, a red ppt of Cu(OH)2.

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Lactose
●
Incompatibilities: primary amine group
●
Method of sterilization: dried at 105 degree then sterilized by dry
heat.
●
Use: diluent in tablets, capsules, dry powder inhalations
●
Used in combination with sucrose to prepare sugar coating
solutions (Appro. 1:3)
●
Direct compression grades of lactose combined with MCC or starch
and usually requires tablet lubricant 0.5% w/w magnesium stearate.
●
Storage: well closed container in a cool dry place

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THANK YOU

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