Drug Delivery System (PHM 220)

Pharmaceutical Ingredients and Excipients

(Week 3)

Maria Teresa S. Dela Cruz,RPh, M.S.Pharm.

September 2022
Outline
I. Definition of Terms
II. Use of excipients
III. Different types of Flavors
IV. Sweetening agents
V. Colorants
VI. References
Definition of Terms
• Active Pharmaceutical Ingredients – A substance used in a
finished pharmaceutical product (FPP), intended to furnish
pharmacological activity or to otherwise have direct effect in
the diagnosis, cure, mitigation, treatment or prevention of
disease, or to have direct effect in restoring, correcting or
modifying physiological functions in human beings.“(WHO definition)
• It is clear from the above that the definition of the API should
only be with respect to a single substance and should exclude
“combination of substances”.
Definition of Terms
• Excipient - substances that are included in a
pharmaceutical dosage form not for their direct
therapeutic action, but to aid the manufacturing process,
to protect, support or enhance stability, or for
bioavailability or patient acceptability.

• inactive ingredient present in dosage form

Examples: solvent, diluents, emulsifier, colorant
Use of Excipients
• Solvents – to dissolve the drug substance
• Flavors & sweeteners – to make the product more
palatable
• Colorants – to enhance appeal
• Preservatives – to prevent microbial growth
• Stabilizers – to prevent decomposition
Use of Excipients
• Diluents/fillers – to increase bulk of formulation
• Binders – to cause adhesion of powdered drug
• Lubricants/antiadherents- to assist smooth tablet formation
• Disintegrating agents – to promote tablet break up after
administration
• Tablet coatings - to improve stability, control disintegration, or
enhance appearance.
• for each dosage form, the pharmaceutical ingredients establish
the primary features of the product and contribute to the
physical form, texture, stability, taste, and overall appearance
Handbook of Pharmaceutical Excipients
• The Handbook of Pharmaceutical Excipients
presents monographs on more than 250 excipients used
in dosage form preparation.

• Each monograph includes such information as nonproprietary,

chemical, and commercial names; empirical and chemical formulas
and molecular weight; pharmaceutical specifi cations and chemical
and physical properties; incompatibilities and interactions with other
excipients and drug substances; regulatory status; and applications in
pharmaceutical formulation or technology.
 EXAMPLES OF PHARMACEUTICAL INGREDIENTS
INGREDIENT TYPE DEFINITION
Acidifying agent Used in liquid preparations to
provide acidic medium for product
stability
Alkalinizing agent Used in liquid preparations to
provide alkaline medium for
product stability
Adsorbent An agent capable of holding other
molecules onto its surface by
physical or chemical
(chemisorption) means
EXAMPLES
for product stability
Citric acid, Acetic acid, Fumaric acid
Hydrochloric acid, Nitric acid
Ammonia solution Ammonium
carbonate, Diethanolamine,
Monoethanolamine, Potassium
hydroxide, Sodium bicarbonate
Sodium borate, Sodium carbonate
Sodium hydroxide
Powdered cellulose Activated
charcoal
Different types of Flavors
• Natural – essential oil, essence or extractive which
contains the flavoring constituents derived from a spice,
fruit, vegetable juice whose function in food is flavoring
rather than nutritional
• Artificial – any substance used to impart flavor that is not
derived from a spice, fruit, vegetable juice, herb, bark..
etc
Different types of Flavors
•Spice – any aromatic vegetable substance in
whole, broken or ground form whose function is
seasoning rather that nutritional and from which
no portion of any volatile oil or other flavoring
principle has been removed
Guide in Flavor Concentration

Type Artificial Natural

Water soluble Start at 0.2% 1–2%

Oil-soluble 0.1% 0.2%

Powdered flavor 0.1% 0.75%

Sweetening agents
• Sucrose – from sugar cane, sugar beet
• Saccharin – 300 times sweeter than sucrose,
has bitter or metallic after taste, not metabolized by
the body
• Aspartame – 180-200 times sweeter than sucrose, but
broken down into phenylalanine, aspartic acid &
methanol
Aspartame
• Persons with phenylketonuria (PKU - a birth
defect that causes an amino acid called phenylalanine
to build up in your body) - should not take Aspartame
as they can not metabolize phenylalanine.
• Intake will cause increased serum levels of the amino
acid which may result in mental retardation and can
affect the fetus of a pregnant woman who has PKU
New Sweetener
• Stevia powder from the leaves of Stevia rebaudiana
bertoni
• Natural, non-toxic, safe
• 30 times sweeter than sucrose
• Can be used in both hot & cold preparations
Colorants
Shade /Color FD & C dye
Orange Yellow No. 5 or 6
Cherry Red No. 40
Lemon Yellow No. 5
Caramel Yellow No. 5
Red No. 3 , Yellow No. 6, Blue No. 1
Grape Red No. 40, Blue No. 1