The document provides an extensive overview of pharmaceutical excipients, defining them as substances included in drug formulations for various purposes beyond therapeutic action. It details different types of excipients, their functions in enhancing drug stability, bioavailability, and patient acceptance, as well as specific examples such as film coatings and disintegrants. Additionally, it discusses the classification and mechanisms of agents like surfactants and provides insights into regulatory considerations for inactive ingredients in drug formulations.

1. EXCIPIENTS
(PART-II)
PREPARED BY :
ASMITA PRASAD
SEM-1 M.PHARM
(PHARMACEUTICAL TECHNOLOGY)
GUIDED BY:
Ms. Mital Patel

2. DEFINITION
 The word ‘Excipient’ is derived from the latin
word ‘Excipere’ which means ‘to except’, that is
simply understood as ‘Other than’.
Pharmaceutical excipients are basically
everything other than the API in the dosage form.
 Pharmaceutical excipients are the substances
which are included in a pharmaceutical dosage
form not for their direct therapeutic action but to
aid the manufacturing process, protect, support or
enhance stability or for bioavailability or for
patient acceptance.
 They may also assist in product identification &
enhance the overall safety of product during

3. Pharmacologically inert
Stable for handling
Cost effective
No interation with the drug
and other components
No taste, odour and colour

4. To provide essential
manufacturing technology
functions
Binders, glidants, lubricants
can be added
To enhance patient
acceptance
Flavours, colourants can
be added
To provide aid in
product identification
Colours can be added
To optimize or modify
drug release
Disintegrants,wetting
agents, biodegradable
polymers can be added
To enhance stability
Antioxidants, UV
absorbers can be added

5. TYPES OF EXCIPIENTS
SURFACE ACTIVE
AGENTS
DILUENTS LUBRICANTS FLAVOURS
COATINGS BINDERS COLOURS GLIDANTS
ANTIADHERENTS SWEETENERS ADSORBENTS PRESERVATIVE

6. 1. FILM COATING MATERIALS
■ A film coating is a thin polymer based coat applied to a solid dosage form such as a
tablet, granule or other particle.
■ The thickness of such coating is usually between 20-100 micrometers.
■ The film coating mixture usually consists of following materials:-
Film formers Plasticizers Colorants
Surfactants Flavours
Glossing
agents
Solvent

7. NON-FUNCTIONAL
(CONVENTIONAL)
TYPES OF
FILM COATING
FUNCTIONAL
These are typically done for
situations in which it is necessary
to improve:-
1. Product appearance
2. Ease of swallowing
3. Product stability
4. Taste masking
These are used when drug release
needs to be modified & represented
by:-
1. Enteric coating
2. Sustained release coating
3. Target release coating

9. DEFECT DESCRIPTION EXAMPLE REMEDY
Tablet
twinning
Tablets stick together 1. Avoid use of tablets with
large area of flat surface.
2. For capsule shaped
tablets, introduce slight
degree of curvature.
Tablet
breakage
Tablets break during pan
loading and unloading; or
while tumbling in the pan.
1. Examine pan loading and
unloading procedures to
minimize damage.
Film cracking Coating cracks due to
thermal expansion of tablet
cores and lack of film
flexibility due to overdying.
1. Reduce processing
temperature.
2. Reduce drying condition so
that moisture retention in
the tablet increases its
plasticity hence, more film

10. Logo infilling Partially spray dried
materials has
accumulated within
the logo, obstructing
the clarity of the logo
design.
1. Minimize foam
generation during
preparation of
coating suspension.
2. Reduce drying
condition to
minimize risk of
spray drying.
Rough coatings The coating deposited
on the surface of
tablet is extremely
rough; either as a
result of partial spray
drying or overwetting,
causing soft coating to
rub.
1. If caused by partial
spray drying, reduce
atomizing
conditions.
2. If caused by
overwetting, improve
the drying conditions
in the process.
Edge chipping Tablets chip on the
sharp corners.
1. Select compound
radius punches to
minimize sharpness
of edges.
2. Ensure friability

11. Disintegrants are the substances or
mixture of substances added to the drug
formulation which facilitate dispersion or
breaking up of tablet and contents of
capsules into smaller fragments for quick
dissolution while ;
Superdisintegrants are the substances
which facilitate faster disintegration with
smaller quantity in contrast to
disintegrants due to its combined effect of
swelling and water absorption and hence
promotes wettability and dispersibility of
the system thus enhancing the
disintegration and dissolution.

12. •Disintegrants swell when come in contact with
water and causes tablet to fall apart.SWELLING
• Tablet porosity provides pathway for the penetration of
fluid into tablets.
• Liquid is drawn up or wicked through pathways hence
tablet rupture.
POROSITY &
CAPILLARY ACTION
(WICKING)
• With the compression force involved in tableting,
starch grains are deformed more permanently.DEFORMATION
• The electric repulsive force between particles lead to
break down of particles and hence dissolution.
PARTICLE
REPULSIVE FORCES

13. XANTHA
N GUM
SODIUM
STARCH
GLYCOLAT
E
CROSS LINKED
POLYPYRROLIDON
E
(CROSPOVIDONE)
MODIFIED
CELLULOSE
(CROSCARMELLOSE
SODIUM)
SOY
POLYSACCHARID
E
CROSS-
LINKED
ALGINIC ACID
GELLAN
GUM
CALCIUM
SILICATE

14. ADVANTAGES
Remarkable tendency on wetting
causing rapid disintegraton
No lump formation on disintegration
Compatible with commonly used
therapeutic agents and excipients
Works equally effective in hydrophilic
and hydrophobic formulations
Provides mechanical strength to the
tablet for easy packaging &
transportation
Does not stick to punches & dyes

15. SUPERDISINTEGRANTS COMMERCIALLY
AVAILABLE GRADES
MECHANISM OF ACTION SPECIAL COMMENT
Crosslinked cellulose Crosscarmellose®
Ac-Di-Sol® , Nymce ZSX® ,
Primellose® , Solutab®,
Vivasol®
Swells 4-8 folds in <10
seconds.
Swelling nd wicking both.
Swells in two dimensions.
Direct compression or
granulation starch free
Crosslinked PVP Crosspovidone M®,
Kollidon ®,
Polyplasdone ®
Swells very little and returns
to original size after
compression but act by
capillary action.
Water insoluble and spongy
in nature so get porous
tablet.
Crosslinked starch Explotab ®,
Primogel ®
Swells 7-12 folds in <30
seconds.
Swells in three dimension
and high level serve as
sustained release matrix.
Crosslinked alginic acid Alginic acid NF Rapid swelling in aqueous
medium or wicking action
Promote disintegration in
both dry or wet granulation.
Soy polysaccharide Emcosoy ® Does not contain nay starch
or sugar. Used in nutritional
products.

16.  Direct compression is the tabletting of blend
of ingredients i.e., a compression mix without
any preliminary unit operation required like
granulation and agglomeration.
 The compression mix contains the API
blended with one or more excipients.
 The excipients which are used in the direct
compression process of tabletting are known to
be as Directly Compressible Excipients.

17. • Flowability
• Compressibility
• Dilution potential
• Reworkability
• Stability
• Controlled particle size

18. METHODS EXAMPLES
Chemical modification CELLULOSE DERIVATIVES:-
Ethyl cellulose, Methyl cellulose, HPMC, Sodium
carboxymethyl cellulose
STARCH DERIVATIVES :- Cyclodextrin
Laclitol
Physical modification Dextrates or compressible sugar
Sorbitol
Grinding and/or sieving α-lactose monohydrate
Dibasic dicalcium phosphate
Crystallization β- lactose
Dipac
Spray drying Spray dried lactose, EMDEX, Avicel PH, Fast Flo Lactose
Granulation/
Agglomeration
Granulated lactitol
Anhydrous α-lactose

19. EXCIPIENT BRAND NAME
Lactose Tablettose, Pharmatose, Fast flo lactose
Sucrose Dipac, Nutab
Dextrose EMDEX, Can tab
Starch Starch 1500, Era tab, Pharm DC 93000
Mannitol Mannogem 2080
Sorbitol Neosorb 60, Sorbogem, Sorbidex P
Microcrystalline cellulose/
Cellulose
Avicel PH, Emcocel, Vivacel
Alluminium hydroxide Barcroft USP 321
Calcium sulphate Delaflo

20. Surfactants (usually referred as surface active
agents) are active at the interface and possess both
hydrophilic and hydrophobic characteristics in the
same molecule.
The hydrophilic part is referred to as head group and
hydrophobic part is referred to as tail group.
In pharmaceuticals, surfactants are used to reduce
the interfacial tension between the medium and the
drug hence increasing the solubility of the drug.
It is also known as wetting agent and foam formers.

22. Roll-up
mechanism
• Lowers
oil/solution and
fabric/solution
interfacial
tension hence
lifting up the
stain from the
fabric
Emulsification
• Lowers the oil-
solution
interfacial
tension and
makes easy
emulsification of
oil
Solubilization
• Interaction of
micelles of
surfactant and
substance, it
spontaneously
dissolves and
form clear &
stable solution

23. Classification is based on the charged group present in
their head.
Anionic
Head is negatively
charged.
Most widely used
for preparing
shampoo
Cationic
Head is positively
charged.
Mostly used for
their disinfectant
&preservative
properties
Non-ionic
Do not have any
electrical charge,
makes them resistant
to water hardness
deactivation. Less
irritant than anionic &
cationic
Amphoteric
They can be cationic,anionic
or non-ionic; depending
upon the pH & acidity of
solution.
Used in personal care
preparations over sensitive
skin

24. As an enhancer for percutaneous
absorption
As flocculating agent
In mouth washes
In suppository bases
In contact lens cleaning

25. Surfactant as an emulsifying agent
Influencing the drug absorption
Drug absorption from rectal suppositories
In hard gelatin capsules

26. IIG consists of all the inactive ingredients present in
approved drug product which are currently marketed for
human use.
IIG is compiled by DDIR – Division of Drug
Information Resources.
PURPOSE :
Once an inactive ingredient appears in any approved
drug product for a particular route of administration, that
inactive ingredient is usually not considered to be NEW
and may require less extensive review.

27. • According to CFR 210.3 (b) 8, “inactive ingredients are defined
as any other component other than the active ingredient which
are present in the final dosage form only.”
• It does not include any processing material used which are
removed afterwards and not present in the final dosage form.
• “Inactive ingredient, which is physically or chemically
combined with the active ingredient to facilitate drug transport
are known as inactive ingredients.”
Contaminants :
• IIG does not represent any contaminant found in the approved
drug product.
Synonyms :
• Since many ingredients have synonyms, if one cannot find any
particular ingredient, one can contact drug information officer who
can assist with the dictionary maintained by the DDIR.

28. Proprietary name:
• DDIR does not always include the proprietary names
of the ingredients in IIG.
Toxics:
• If any ingredient of IIG is found to be carcinogenic or
teratogenic, it should be notified to DDIR.
DDIR draws attention of medical officers and
pharmacological reviewers towards the specific inactive
ingredient.
Structures:
Chemical structures of inactive ingredients are not
mentioned in IIG.
It can be obtained from DDIR chemist if needed for
review.

29. NAME ROUTE/
DOSAGE
FORM
CAS NO. NDA
COUNT
LAST NDA
APPROVAL
DATE
POTENCY
RANGE
 NAME
•Names are alphabetically listed starting from ACACIA to ZINC SULFATE
• After them, few excipients starting as per numerical are listed
Eg. 1,1,1-trichloroethane.
 ROUTE / DOSAGE FORM; SPECIFIC
• Route is given alphabetically i.e., Buccal, I.V., I.M.,Opthalmic,Oral,Topical.
• Dosage form is given specifically i.e., Oral; Tablet; Delayed action, Enteric coated.

30.  CAS – Chemical Abstract Service number
• It is a unique 9 digit identification number given to every individual chemical
substance.
• It is helpful in computer assisted search with the National Library of Medicine’s
Online Databases.
 NDA Count – New Drug Application
• It represents the total number of NDA filed in which inactive ingredient currently
appears.
 LAST NDA APPROVAL DATE
• It is the date of obtaining last NDA approval.
• It helps to find out the latest NDA .
 POTENCY RANGE
• It gives the minimum to maximum value of excipient used i.e. 0.5mg – 5mg.
• In many excipients, potency range is given in percentage of final product
Eg. 0.5% - 5%.

31. REFERENCE
■ Handbook of Pharmaceutical Excipients (1986) American Pharmaceutical Association,
Washington and Royal Pharmaceutical Society, London.
■ Howard C Ansel, Nicholas G Popvich, Loyd V Allen. Pharmaceutical Dosage Forms and Drug
Delivery System, First Edition, 1998, pp 78.
■ Lachman L, Liberman HA. Theory and Practice of Industrial Pharmacy, Third Edition, 1990, pp
293-294.
■ . Caramella C, Novel methods for disintegrant characterization, Part 1, Pharm. Technol. Int, 2(9),
1990, 30 – 37.
■ M.C. Gohel, Pranav D jogani, A review of co-processed directly compressible excipients, 2005,76
– 87.
■ Gohel, M. C., and Jogani, P. D., An Investigation in Direct Compression Characteristics of Co-
processed Lactose-Starch using Experimental Design, Indian J. Pharm. Sci., 65: 31-38, 2003.
■ McCUTCHEON "Detergents and Emulsifiers", McCutcheon Division Pub. Co., 175 Rock Road Glen
Rock NJ 07452 (Annuel, 3 volumes).
■ Proceedings. World Conference on Soaps and Detergents, Journal of the American Oil Chemists
Society, volume 55, Nº 1 (1978).
■ www.fda.gov