Here it contains explanation about different excipients

1. EXCIPIENTS OF INTEREST
Presented By
M SREEKANTH
20031S0402
A SEMINAR ON

2. An Excipent is a pharmacologically inactive
substance formulated alongside of the Active
Pharmaceutical Ingredient (API) of Medication
Drug products contain both drug substance (commonly
referred to as active pharmaceutical ingredient or API)
and excipients. Formulation of API with excipients is
primarily to ensure an efficacious drug product with
desired properties and a robust manufacturing process

3. The resultant biological, chemical and physical
properties of the drug product are directly affected by
the excipients chosen, their concentration and
interactions with the API:
•Consistency of drug release and bioavailability
•Stability including protection from degradation
•Ease of administration to the target patient
population(s) by the intended route

4. •Excipients determine the bulk of the final product in
dosage forms such as tablet, capsule, etc., the speed of
disintegration, rate of dissolution,release of drug,
protection against moisture, stability during storage,
and compatibility .
Ideal properties of excipient
•No interaction with drug
•Cost effective
•Pharmacologically inert
•Stable for handling
•Feasible

5. Excipients are inactive ingredients used as carriers for the
active ingredients in a pharmaceutical product.
These may be classified into the following categories:
•Antiadherents
•Binders
•Coatings
•Disintegrants
•Fillers and Diluents
•Coloring Agents
•Glidants & Emulsifiers
•Lubricants
•Preservatives
•Sorbents & Sweeteners

6. DISINTEGRANTS AGENTS
These are the substances Which are added to a tablet
formulation to facilitate its breaking or
disintegration when it contact in water in the GIT
Such Tablet fragmentation Plays an important role
in subsequent Dissolution of the tablet and which
inturn governs the Bioavailability Of the Drug

7. MECHANISM
They Draws Water into the Tablet
This results in Swelling of the Tablet
Then the Tablet Bursts A part

8. Examples;-
1)Starch and It's Derivatives
2) Cellulose & it's Derivatives
3)Clays
4)Alginates
5)PVP,Cross linked

9. STARCH & ITS DERIVATIVES
Starch USP and various Starch Derivatives are the
most commonly used Disintegrating Agents
•Concentration range :5-10%
•Low cost
• Starch Derivatives and other modified Polymers can
increase in volume by 200 -500% in presence of
Water

10. STARCHES CONCENTRATION RANGE
STARCH USP
Carboxymethyl Starches
Primogel
Explotab
Pregelatinised Starches
5-20%
1-8%
4% Optimum
5%
Examples of Various Starches

11. CLAYS
•Veegum HV & Bentonite are used Disintegrants
• Concentration Range of 10%
Demerits
• Less Effective
• Clay produce an off-white appearance

12. MICRO CRYSTALLINE CELLULOSE
Trade Name : Avicel
•It is a Direct Compression Material
• Produces Cohesive impacts & also acts as
Disintegranting agent
Avicel grades -PH 101 ( powder) PH102
(granules)

13. Ac- Di-Sol
•Ac-Di-Sol is internally cross linked form of
sodium corboxymethyl cellulose
•It is effective in low concentration levels
•Cross linked PVP are also used as disintegranting
agent

14. BINDERS
Binders hold the ingredients in a tablet together. Binders ensure that
tablets and granules can be formed by increasing cohesive state of the
drug powder, with required mechanical strength. In other word
according to WHO binders act as an adhesive to ‘bind together’
powders, granules and tablets to result in the necessary mechanical
strength.
Binders can be added to a powder in different ways: As a dry powder
which is mixed with the other ingredients before wet agglomeration.
During the agglomeration procedure the binder might thus dissolve
partly or completely in the agglomeration liquid; As a solution which
is used as agglomeration liquid during wet agglomeration. The binder
is here often referred to as a solution binder.

15. Typical features of binders:
A binder should be compatible with other products of
formulation and add sufficient cohesion to the powders
Binders are classified according to their application
•Dry binders are added to the powder blend, either after a
wet granulation step, or as part of a direct powder
compression (DC) formula. e.g., Pregelatinised starch, cross-
linked PVP, cellulose, methyl cellulose,PEG and
•Solution binders are dissolved in a solvent (for example
water or alcohol can be used in wet granulation processes).
e.g., PVP, HPMC, gelatin, cellulose, cellulose derivatives,
starch, sucrose and polyethylene glycol.
• Soluble in water/ethanol Mix: PVP

16. •Acacia, Tragacanth, Gelatin, Sucrose, Starch paste are
soluble in water and are not used in water sensitive
drugs, while Na-alginate, Methyl cellulose dissolved in
alcohol and PVP, Methyl cellulose drugs, while Na-
alginate, Hydroxy Propyl cellulose dissolved both water
and alcohol.
• In case of water sensitive drugs first bender need to
dissolve on alcohol and then other excipients and active
ingredients are mixed with it.

17. Binders Used
Concentration
Required solvent
Acacia 2-5% H2O
Tragacanth 1-3% H2O
Sucrose 2-20% H2O
Gelatin 1-4% H2O
Starch paste 1-4% H2O
Na-alginate 3-5% Alcohol
Methyl cellulose 1-4% Alcohol
Pyrrolidone 2-5% H2O & Alcohol
Ethyl cellulose 0.2-.0.5% H2O & Alcohol

18. EMULSIFIERS
Emulsifying agents are those substances used in
the emulsion to reduce the interfacial tension
between the two phases i.e. aqueous phase and
oily phase thus make them miscible with each
other to form a stable emulsion.

19. Classification Emulsifying agents may be classified as
follows:
1. Natural emulsifying agents from vegetable origin
The natural emulsifying agents obtained from
vegetable sources are carbohydrates which include
gums and mucilaginous substances. They are anionic
in nature and produce O/W emulsion. Examples are a.
Acacia b. Tragacanth c. Agar d. Chondrus (Irish moss0
e. Pectin f. Starch.
2. Natural emulsifying agents from animal origin
Examples are a. Gelatin b. Egg yolk c. Wool fat
(Anhydrous lanolin)

20. 3. Semi-Synthetic polysaccharides Examples are a.
Methyl Cellulose b. Sodium carboxymetjhyl cellulose
4. Synthetic emulsifying agents This group includes
surface active agents.Examples are a. Anionic:
Various alkali soaps, metallic soaps, sulphated
alcohols and sulphonates. b. Cationic: Quaternary
ammonium compounds. c. Non-ionic: Glyceryl esters
e.g. Glyceryl monostearate.
5. Inorganic emulsifying agents Examples are a.
Magnesium oxide b. Magnesium trisilicate c.
Magnesium aluminium silicatwe d. Bentonite

21. The choice of emulsifying agents To get an emulsion of
required properties, the emulsifying agent selected must
have the following qualities
.1. It should be capable of reducing the interfacial tension
between the two immiscible liquids.
2. It should be capable of keeping the globules of
dispersed liquid distributed indefinitely throughout the
dispersion medium.
3. It should be non-toxic,4. The odour and taste should be
compatible with the preparation.
5. It should be chemically compatible with other
ingredients of the preparation.

22. VISCOSITY: Flow property of a simple liquid is
expressed in terms of viscosity. Quantitatively,
viscosity is an index of resistance of a liquid to flow. A
fluid with large viscosity resists motion because its
molecular makeup gives it a lot of internal friction. A
fluid with low viscosity flows easily because its
molecular makeup results in very little friction when
it is in motion.
VISCOSITY MODIFIERS

23. VISCOSITY PROMOTERS:These are substances ,which
added to an aqueous mixture, increase its viscosity
without substantially modifying its other properties ,
such as taste.They provide body, increase stability ,
and improvesuspension of added ingredients. It is
desirable to increase the viscosity of liquid toprovide
or to improve palatability or pourability
•Polymers are used in suspensions, emulsions , and
other dispersions ,primarily to minimize or control
sedimentation

24. Advantages:
•High viscosity inhibits the crystal growth.
•High viscosity enhances the physical stability
•High viscosity prevents the transformation of
metastable crystal to stable crystal
Disadvantages :
•High viscosity hinders the re-dispersibility of the
sediments.
•High viscosity retards the absorption of the drug.
•High viscosity creates problems in handling of the
material during manufacturing.

25. IDEAL CHARACTERISTICS OF VISCOSITY
PROMOTERS:
Should produce a structured vehicle
Should have high viscosity at negligible shear during
storage and low viscosity at high shearing rates during
pouring
Should exhibit yield stress
Should be compatible with other excipients
Should be non-toxic
Viscosity should not be altered by temperature or on
ageing

26. CLASSIFICATION:
Natural gums
Acacia , Tragacanth
Alginic acid
Karaya , Guar gum etc.,
Cellulose derivatives
Carboxy methyl cellulose
Methyl cellulose
Ethyl cellulose
Hydroxy ethyl cellulose
Hydroxy propyl methyl cellulose

27. Microcrystalline cellulose
Chitosan
Synthetic polymers
Carbomer (poly acrylic acid)
Polyvinyl pyrrolidone
Polyvinyl alcohol
Clays
Magnesium aluminium silicate(veegum)
Bentonite
Attapulgite

28. 1) NATURAL GUMS
Natural gums are polysaccharides of natural origin ,capable
of causing a large viscosity increase in solution ,even at small
concentrations. These polymers may be either non-ionic or anionic.
Natural gums can be classified according to their origin
1. Natural gums obtained from seaweeds
Agar, alginic acid, sodium alginate, carrageenan
2. Natural gums obtained from non-marine botanical sources
Gum arabic (from the sap of acacia trees)
Gum tragacanth(from the sap of astragalus shrubs)
Karaya gum(from the sap of sterculia trees)
Guar gum(from guar beans)
Dammar gum (from the sap of dipterocarpaceae trees)

29. 3. Natural gums produced by bacterial fermentation
Gellan gum
Xanthan gum
ALGINATES
Anionic polysaccharide
Derived from brown seaweed in the form of monovalent
and divalent salts
The most widely used one is sodium alginate
Use :thickener and stabilizer

30. GUM ARABIC
Anionic polysaccharide
It is the dried exudate of trees of the genus acacia
Unlike most natural gums,acacia exhibits very low
solution viscosities
At concentration under 40% ,solutions exhibits
Newtonianflow;higher concentrations behave in a pseudo-
plastic manner
Use: suspending agent,emulsifier,adhesives and binders in
tabletting

31. GUAR GUM
Non-ionic polysaccharide derived from seeds
It exhibits pseudo-plastic flow
Disadvantage of these gels is the presence of insoluble plant
residue
Use: thickener , suspension stabilizer
XANTHAN GUM
Anionic polysaccharide
Exhibits pseudo-plastic rheology
Temperature has very little effect on the viscosity of xanthan
solutions . This temperature independence of viscosity is unique to
xanthan gum
Use : thickener , suspension stabilizer , suspending agent

32. Applications of natural gums:
Guar gum is a colon- specific drug delivery carrier is based
on its degradation by colonic bacteria.
Gum acacia used in confectionery industry and in baking
industry.
Gum tragacanth is still a preferred ingredient,particularly
used in conjunction with gum acacia.
Xanthan gum is a common suspending agent in suspension
for reconstitution.

33. 2) CELLULOSE DERIVATIVES
Cellulose is one of the most widely used starting
material for manufacturing of modified natural polymers.
Cellulose ethers with methyl substitution generally form a gel
at a elevated temperatures. Gel formation is reversed when
temperature is reduced.
ETHYL CELLULOSE
It is a non-ionic ether derivative of cellulose
It is widely used as tablet binder ,thickening agent , coating
material for tablets , microcapsules and microparticles.
HYDROXY ETHYL CELLULOSE(HEC)
It is a non-ionic cellulose ether
Solutions of HEC exhibit pseudo-plastic flow

34. CARBOXY METHYL CELLULOSE(CMC)
Sodium CMC is an anionic polymer and is available in 3 grades-
Food , pharmaceutical and technical
It is also available with a variety of molecular weights and
degree of substitution.
CMC is more resistant to microbial attack than most natural
gums. The viscosity of CMC solution decreases reversibly with
increasing temperature.
The rheology of aqueous CMC solution depends on the degree
substitution . Low substituted CMC products exhibit thixotropy;
higher substitution leads to pseudo-plastic behaviour.
Use : suspending agent, emulsion stabilizer

35. METHYL CELLULOSE & HYDROXY PROPYL
METHYL CELLULOSE (HPMC)
Both are interesting examples , as they exhibit a
reversthermal gelation, gelling when heated and
melting when cooled.
These are the non-ionic cellulose ether derivatives.
Rheology of these solutions is pseudo-plastic , and
there is no yield point.
Use : suspension stabilizer, thickener

36. Applications of cellulose derivatives:
1. Methyl cellulose:
Used in pharmaceutical gels
High viscosity grades are used in ophthalmic
preparations
Bulk forming laxative
Lubricating jellies for surgical and medical
procedures
2. HPMC:
A 2% solution is commercially available as an
ophthalmic surgical aid.

37. 3) MICROCRYSTALLINE CELLULOSE (MCC)
Dispersions of MCC do not have viscosities that are
significantly greater than that of water. However,
combinations of CMC,MCor HPMC are used to thicken
aqueous solutions.
The colloidal dispersions of MCC blends exhibit
thixotropy rheology , also exhibit a yield point.
Viscosity is not affected by temperature
It is used as stabilizer and thickener in aqueous systems
Formulation of dry powder suspension with
MCC:alginate complexes(0.5-10%w/w of total dry
formulation)

38. 4) CHITOSAN
Chitosan is a natural biopolymer derived from the outer shell
of crustaceans. It is a weak cationic polysaccharide, biocompatible,
biodegradable, non-toxic.
Uses:
As permeation enhancer and as mucoadhesive excipient
It exhibits favourable biological behaviour , such as bioadhesion
and permeability enhancing properties , which make it a unique
material for the design of ocular drug delivery vehicles
Enhanced bone formation by transforming growth factor and
Used in tissue repair Cholesterol lowering effects

39. 5) SYNTHETIC POLYMERS
Carbomer ( polyacrylic acid )
Solutions of carbomers are very pseudo-plastic and exhibit a yield
value
It is an excellent choice as a thickener in creams and lotions
Carbomer 934P is the official name given to one member of a acrylic
polymers . Manufactured under the trade name carbopol 934P, it is
used as a thickening agent in a variety of pharmaceutical and
cosmetic products.
Polyvinyl pyrrolidone ( PVP )
Use : in ophthalmic preparations , serving as muco- mimetic agent

40. 6) CLAYS
Magnesium aluminium silicate (veegum )
The gels are formed at about 5% concentration. They
exhibit plastic flow
It functions well as a suspending agents becauseit prevent
caking without affecting pourability or spreadability of
suspension
Magnesium aluminium silicate dispersions are influenced
by heat , and the viscosity of the dispersion increases
onprolonged exposure to elevated temperatures.

41. CONCLUSION
In pharmaceutical field , the viscosity promoters
play a vital role , as they stabilize the disperse systems
and also used in various dosage forms.
Viscosity-inducing polymers should be used with
caution . They are known to form complexes with a
variety of organic and inorganic compounds.

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