Mrs.

Pradnya Wadekar Bapat 11-Jul-18 2

 Sweetening agents are the substances which are added
to a drug formulation to mask its bitter taste.
 Sugar is the most widely used natural sweetening
agents.
 Sucrose sets gold standard for sweet taste as it’s taste
is quick, short lived and clear and also abundantly
available in nature
 It imparts viscosity to drug and also even act as
preservative for liquid dosage form
 It is nutritive too

Mrs. Pradnya Wadekar Bapat 11-Jul-18 3

Mrs. Pradnya Wadekar Bapat 11-Jul-18 4
 Compatible
 sweetness even in low concentration.
 cheap and easily available
 agreeable odour
 Stability- heat stable, non hygroscopic
 non toxic
 inert
 Easy to handle in formulation- water
solubility, dissolution rate, etc
Mrs. Pradnya Wadekar Bapat 11-Jul-18 5
 CLASSIFICATION
OF sweetenerES

Nutritive Sweeteners

Non Nutritive
sweeteners

Mrs. Pradnya Wadekar Bapat 11-Jul-18 6

 Alternative nutritive sweeteners are sugar alcohol
such as Sorbitol, Mannitol, Lacitol etc.
 It is having properties like less sweet and less
calories
 FRUCTOSE- 4Kcal/gm the same as sucrose and it
doesn't cause fluctuation in blood sugar, thus better
choice for diabetic patients.
 1.5 times sweeter than sugar and cost effective for
food industry.
 Still ideal alternative for sugar does not exist?????
Mrs. Pradnya Wadekar Bapat 11-Jul-18 7
 Mostly are artificial*
 Examples include Aspartame, Saccahrin,
Clycamate, Alitame etc.
 More sweet and thus only small quantity is
required for sweetening food preparation.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 8

 Sweetness potency=

 E.g. 0.75 gm/litre solution of aspartame

matches with the sweetness of 100 gm/litre
solution of sucrose.

 Therefore aspartame is considered as 133

times sweeter than sucrose.
Mrs. Pradnya Wadekar Bapat 11-Jul-18 9
 The sweetness potency is also dependant
on taster, the pH, the viscosity of
formulation, etc

Mrs. Pradnya Wadekar Bapat 11-Jul-18 10

Mrs. Pradnya Wadekar Bapat 11-Jul-18 11
 Source: It is Steviol glycoside obtained from
leaves of the Stevia rebaudiana Berrtoni
 Family: Compositeae.
 G.S.-paraguay, Brazil, Japan, China, Taiwan,
Thailand, Malaysia.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 12

 Properties:
 It is 160- 170 times sweeter than sucrose.
 It is heat stable and pH stable and do not ferment.
 It does not induce a glycemic response.
 Natural sweetener to diabetics and carbohydrate
controlling diets.
 The dried leaves of the plant, the water extract of the
leaves and the purified ingredients of extract are used
as sweetening agents.
 It’s tainted with a bitter and undesirable after taste.
 No side effects.
 Both are diterpene Glycosides.
Mrs. Pradnya Wadekar Bapat 11-Jul-18 13
 Structure: It is made up from a diterpene
known as Steviol. Stevioside is formed by
attaching glucose molecules to the steviol
structure.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 14

 Preparation: the leaves are extracted with water/
water ethanol mix and further purified by treatment
with CaOH2/MgOH2/ carbonate. The ratio of rebaudioside
to stevioside can be increased by using methanol for
extraction of leaves
 Rebaudioside A is approximately one third higher than
stevioside and tastes better. But it is unstable and gets
decopmosed to light.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 15

 Uses- as Sweetning agent as table top
sweetner, in confectioneries, soft drinks and
fruit products.

 DISADVANTAGE:
 Steviol has been reported to be mutagenic.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 16

 Biological Source : It is a mixed Ca & K salt of
Glycyrrhizic acid found in Glycyrrhiza glabra
 Family : Leguminosae
 Characteristics :
1. Glycirrhizin is 50x-100x sweeter than Sucrose
2. Ammonium Glycyrrhizinate is 50x sweeter than
sucrose and its salt are characterized by a
delayed sweetness onset and characteristic
liquorice taste more like flavouring agent than
sweetener
Mrs. Pradnya Wadekar Bapat 11-Jul-18 17
 Preparation:
 A crude extract of liquorice root is to be prepared
with the help of counter current extraction with
water.
 After removal of polysaccharide, Glycyrrizin can be
precipitated from crude extract with sulphuric acid.
 Ammonium glycirrhizinate is prepared by treatment
with NH3, followed by subssquent drying and
precipitation with ethanol.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 18

 Chemical Constituents : Chemical Constituents :-It is a
triterpenoids glycoside glycirrhizin.
H2O
Glycyrrhizic acid ---------> Glycyrrhetic acid (aglycone)+
2 molecules of glucuronic acid
The acid form is not particularly water-soluble, but its ammonium
salt is soluble in water at PH greater than 4.5.
It also contain liquirtin and liquiritigenin(flavonoid glycoside).
Glycyrrhizic acid is a triterpenic glycoside of β-Amyrin type
which contains two β-1,2 Glycosidic linked Glucoronic acid.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 19

 As flavoring agent and as flavor enhancing
effect in food products.
 In the treatment of peptic ulcers and as an
expectorant, produce anti-inflammatory
effects, is used in the treatment of chronic
hepatitis and cirrhosis.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 20

 CausesOedema and Hypertension. So, its
dose should be 200 mg per day or less.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 21

 Biological source: It is a flavonoid compound
present in the bitter orange Citrus aurantium Var
amara
 Family : Rutaceae
 Characteristics:
1. 330x >> Sucrose
2. It is characterized by pronounced Menthol like after
taste which limits its use.
3. It act synergistically with a number of other
sweeteners.
4. It has flavor enhancing system.
Mrs. Pradnya Wadekar Bapat 11-Jul-18 22
 Preparation: It is prepared from neohesperidin by
hydration of neohesperidin under alkaline condition.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 23

Use: It is used in confectionery, chewing gum,
beverages and dairy products

Mrs. Pradnya Wadekar Bapat 11-Jul-18 24

 Source: -It is obtained from the
arils of fruits of
Thaumatococcus danielli
 Family:- Marantaceae.
 Properties:
 It is approximately 3500 times sweeter than
sucrose
 The sweetness shows delayed onset and long
persistent taste. It loses its sweetness on
heating.
 It is highly water soluble, stable below Ph 5.5.
Mrs. Pradnya Wadekar Bapat 11-Jul-18 25
 Chemical Constituent:-It is a polypeptide
containing Thaumatin I & Thaumatin II as major
components.

 Preparation: It is extracted with water and then

purified by Ion exchange chromatography.

 Use: It is used as flavor enhancer rather than

as a sweetener.
 It is used as flavor enhancer in confectionary,
chewing gum and similar products.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 26

 The sweetness of thaumatin shows delayed
onset and long persistent liquorices like
taste.
 It loses its sweetness on heating or splitting
disulphide bridge

Mrs. Pradnya Wadekar Bapat 11-Jul-18 27

 Biological source: It is intensely sweet polypeptide
constituent present in the fruits of tropical plant
Dioscoreophyllum cumminsii Stapf Diels
(serendipity berry)
 Family: Menispermaceae
 Characteristicc:
1. 2000x >> Sucrose
2. Sweetness of the polypeptide Monellin is sensitive
to conformational changes caused by heat or
hydrolytic decomposition, so rendering it
unsuitable as normal sweetener.
Mrs. Pradnya Wadekar Bapat 11-Jul-18 28
 It is semisythetic sweetener
 Based on discovery- halogenation increases
sweetness of carbohydrates
 It is trichlorogalctosucralose

Mrs. Pradnya Wadekar Bapat 11-Jul-18 29

 It solubale in water and ethanol
 It is 600x >> sucrose
 Sweeteness is slightly delayed but persistant
for long time
 International authority limits its use*
 Evidence of benefit is lacking for long-
term weight loss with some data supporting
weight gain and heart disease risks.

Mrs. Pradnya Wadekar Bapat 11-Jul-18 30

Mrs. Pradnya Wadekar Bapat 11-Jul-18 31
 Are mostly consumed before any normal meals to
stimulate as well as enhance the appetite.
 However, the bitter glycoside as a class do possess
almost similar activities like the bitters such as :
digestive, stomachic and febrifuge.
 Bitters increases the appetite and stimulates digestion
by acting on the mucous membranes of the mouth.
 It also increases the flow of bile, stimulate repair of gut
wall lining and regulate the secretion of insulin and
glucagons.
 They stimulate the gustatory nerves and increase the
psychic secretion of gastric juices.
 These are also used as anti-tumour and anti-malarial
agents

Mrs. Pradnya Wadekar Bapat 7/11/2018 32

 Some of the bitters belong to alkaloids

 These are not confined to the same chemical

class, but the most important ones amongst
them contain the glycosides of monoterpenes,
iridoids with pyran cyclo pentane ring.
› Monoterpenes : These are derived from C10 geranyl
phosphate and constitute important components of
volatile oils.
› Iridoids : These are monoterpenoids with pyran
cyclopentane ring.

Mrs. Pradnya Wadekar Bapat 7/11/2018 33

 Geranyl phosphate Iridoid

Mrs. Pradnya Wadekar Bapat 7/11/2018 34

 Its is the reciprocal of the dilution of a compound, a liquid
or an extract that still has a bitter taste.

 It is determined by comparison with quinine hydrochloride,

the bitterness value of which is set at 2,00,000.

 Brucin can also be used as standard for bitterness

 Amirogentin present in Gentian is considered bittermost

substance

Mrs. Pradnya Wadekar Bapat 7/11/2018 35

 Synonyms: Yellow Gentian, Gall
weed, Bitter wart, Radix Gentianae.
 Biological Source: It consist of dried rhizome and
roots of Gentiana lutea Linn.
 Family : Gentianaceae.
 CHEMICAL CONSTITUENTS: It consist of the
bitter glycoside GENTIOPICRIN as active
constituent.
› Other bitter compounds are Genticin, Amaropanin,
Amarogentin & Amaoswerin.
› It also contains Gentiin, Gentiamarin, Gentisic acid,
Tannins, Pectin and calcium oxalates.
Mrs. Pradnya Wadekar Bapat 7/11/2018 36
 USES: Potent stomachic and treats GI
problems like indigestion.
› Emmenogoggue (enhance menstrual flow)
› This bitter stem less is used to treat wounds.
› To treat arthritis, sore throat, Jaundice
› Gentian extract are used in variety of foods and
cosmetics.
Contra indications: Avoided in pregnancy and
lactation. Contra indicated in gastric and
duodenal ulcers.
Adverse effects: Raw extract may cause nausea,
vomiting and diarrhea.

Mrs. Pradnya Wadekar Bapat 7/11/2018 37

 Synonyms: Andrographis Paniculata, Kalmegh
 Biological cource: The drug consist of dried or fresh
leaves and aerial portion of the plants Andrographis
paniculata Nees.
 Family: Acanthaceae.
 Chemical Constituents • It contains a bitter
compound andrographolide up to 1 %
› It is diterpene lactone.
› Some other compounds such as neoandrographolide,
andrographosterol, andrographiside, flavonoids, phenolic
compounds and some waxy material are present.

Mrs. Pradnya Wadekar Bapat 7/11/2018 38

 Uses: It is used as bitter tonic and
stomachic.
› It also known as “green chiretta” in India.
› It is used in the treatment of torpid liver (impaired
nerve impulses) and jaundice.
› The decoction of the plant is used as blood
purifier.
› The decoction of the leaves is given with spices
such as cardamom, clove or cinnamon for
stomach ailment in infants.
› It produce enzyme induction.
Mrs. Pradnya Wadekar Bapat 7/11/2018 39
 Synonyms: Chiretta, Chirayta, Bitter stick
 Biological source: It consist of the dried
entire herb of Swertia chirata
 Family: Gentianaceae
 Chemical Constituents: It contains bitter glycosides
amrogentin 0.04 % and amroswerin 0.03%.
› The other two extremely bitter principles ie chiratin and
ophelic acid also present in crude drug. • Other compound
include chiratol, mangiferin, swertianin, chiratanin, chiratenol.
 Uses: It is used as bitter tonic and stomachic.
› It is also used as antimalarial in some part of India.

Mrs. Pradnya Wadekar Bapat 7/11/2018 40

 Synonyms: Picrorhiza, Kutki
 Biological source: It consist of dried rhizomes and roots of
Picrorhiza kurroa Royle.
 Family: Scrophularelareaceae
 Chemical constituents: It contains cyclopentanopyran
monoterpenoids, a class of glycosides.
› It contains picroside I, Picroside II and kutkoside up to 3-4 % •
The drug also contains about 9 % cathartic acid.
 Uses: It is used as bitter tonic and stomachic.
› It is also used as laxatives in small doses and cathartic (produce
psychological relief) in large doses.
› It is used as hepatoprotective in Jaundice.
› It is also used as liver tonic.

Mrs. Pradnya Wadekar Bapat 7/11/2018 41

 SYNONYM :- Bitter wood, Jamaica Quassia

 BIOLOGICAL SOURCE :- It consists of the dried stem wood of

Picrasma excelsa

 Family Simarubaceae .

 CHEMICAL CONSTITUENTS :- It contains about 0.2% of the

bitter lactone i.e. quassin & its hemiacetal Neoquassin .

 USES :- 1. Bitter tonic 2. It is given as an enema in the form of

infusion to expel threadworms. 3. It possesses insecticidal
properties.

Mrs. Pradnya Wadekar Bapat 7/11/2018 42

 SYNONYM :- Gudmar , Madhunashini
 BIOLOGICAL SOURCE :- It consists of the
leaves of a perennial woody climber plant known as
Gymnema sylvestre
 Family Asclepiadaceae .

 CHEMICAL CONSTITUENTS :- It contains

pentriacontae , hentriacontane , phytin , α & β
chlorophylls. Gymnemic acids (anti-sweet compounds),
the mixture of triterpene saponins & antraquinone
derivatives.

 USES :- Stomachic, stimulant, laxative & diuretic.

Antidiabetic due to indirect stimulation of insulin
secretion from pancreas.
Mrs. Pradnya Wadekar Bapat 7/11/2018 43
 SYNONYM :- Egyptian privet, Lawsonia -alba

 BIOLOGICAL SOURCE :- It consists of fresh or dried leaves

of the plant Lawsonia – inermis
 Family: Lythraceae .

 CHEMICAL CONSTITUENT :- It contains lawsone (0.5-1%).

Lawsone , the main colouring constituent is said to be a
degradation product of primary glycoside hennoside A,B,&C.

 USES :- It is used as hair dye It shows Anti-bacterial and

anti-fungal property
Mrs. Pradnya Wadekar Bapat 7/11/2018 44
 Other examples- Nux vomica, Karela, Methi,
etc…

Mrs. Pradnya Wadekar Bapat 7/11/2018 45

 Pharmacognosy and phytochemistry by
Rangari part II
 Pharmacognosy and phytochemistry by
Gokhale, Kokate, Purohit

Mrs. Pradnya Wadekar Bapat 11-Jul-18 46