PHARM CHEM 11 form or in concentrated solution with
strong oxidizing agents
6C. ANTIOXIDANTS
What are antioxidants?
OFFICIAL ANTIOXIDANTS
 Are Pharmaceutical necessity used as
efficient excipients that delay or inhibit the
oxidation process of molecules
 Are compounds which have the capability
of functioning chemically as reducing agents
Mechanism of Action of Antioxidants
 by providing electron or labile H+ which will
be accepted by any free radical to
terminate the chain reaction... the
antioxidant reduces the already oxidized
active constituent back to its normal
oxidation state.
Oxidation reactions transfer electrons from a substance
to an oxidizing agent. During this process, some free-
radicals are produced, which starts chain reactions that
damage animal cells. Antioxidants slow down these
chain reactions by removing free-radical intermediates
and eventually inhibit other oxidation reactions by
being oxidized themselves.
IMPORTANT FACTORS TO CONSIDER SELECTING A
SUITABLE ANTIOXIDANT
1. An antioxidant in a pharmaceutical
preparation should be physiologically inert
2. The possible toxicity of both the reducing
agents and its oxidized product must be
assessed
3. One should consider possible solubility
problems between the reducing agent and
the drug
4. Very strong reducing agent will form
explosive mixtures when combined in dry
1. Hypophosphorous Acid (HPH2O2)
Uses:
 The formation of free iodine is prevented in
diluted hydroiodic acid and syrup.
 Its presence in ferrous iodide syrup ensures
the non- formation of both ferric ions and
molecular iodine.
 Salts of hypophosphorus acid are
antioxidants.
o Sodium hypophosphite is a preservative
in certain foods.
o Ammonium hypophosphite is likewise a
preservative in many preparations.
2. Sulfur Dioxide (SO2)
Uses:
 It will protect many susceptible
compounds from oxidation by reducing
oxidized forms back to their original
compounds or by reacting with oxygen
before the susceptible compounds do.
 It is usually in injectable preparations in
ampules or vials
 It is used in industry to bleach wood
pulp, to fumigate grains and to arrest
fermentation
3. Sodium Bisulfite (NaHSO3) or Sodium
Metabisulfite (Na2S2O5)
Uses:
 It prevents oxidation of the compounds
of phenol or catechol nucleus to
quinones.
 It prepares water-soluble derivatives of
normally insoluble drugs.
 Metabisulfite & Bisulfite are found or
added in ascorbic acid injections as
reducing agent.
4. Nitrogen (N2)
Uses:

 As an inert atmosphere, it retards

oxidation in oxidation- sensitive
products, and replaces air in containers
for parenterals and solutions for topical
applications
 nd solutions for topical applications

5. Sodium Thiosulfate (NaSO2)2

Uses:

 Contains sulfur in two different

oxidation states.
o The oxidized sulphur atom is in a
+6 state resisting further
oxidation,
o sulphur atom in a zero oxidation
state becomes polar allowing the
compound to act as a reducing
agent.
 Acts as an antidote for cyanide
poisoning.

6. Sodium Nitrite (Na NO2)

 Nitrites can act as both a reducing
and oxidizing agent. Reduction of
compounds with sodium nitrite
results in formation of nitrates
 It is an antidote for cyanide
poisoning
 Nitrites in brine solutions are curing
ingredients of meats and fish for
they are excellent color developer,
enhance flavor production, and
prevent microbial growth. However.
Nitrite ions remain in cured meats
and react with organic amines to
form potentially carcinogenic
nitrosamines.