Antioxidants

- compound that function chemically as reducing agents
-used in pharmaceutical preparations containing easily oxidizable substances
- to maintain substances in their reduced forms
- should be physiologically inert in pharmaceutical preparations

* Mechanism of antioxidant action may be seen in two ways, both achieving the same
net results:
a.) Either the antioxidant is oxidize in place of the active constituent
b.) If the active constituent is oxidized, the antioxidant reduces it back to its normal
oxidation state
FACTORS TO BE CONSIDERED IN SELECTING SUITABLE ANTIOXIDANT:
1.) An antioxidant in a pharmaceutical preparation should be physiologically inert.
2.) Possible toxicity of both the reducing agent and its oxidized product must be assessed.
3.) Consider possible solubility problems between the reducing agent and the drug.
4.) Very strong reducing agents will form explosive mixtures when combined in dry form
or in concentrated solution with strong oxidizing agent.
o [HPH2O2]
- colorless/slightly yellow odorless liquid. 30% concentration
- pure acid is a syrupy colorless liquid, becomes solid at 17 degree celcius
- very powerful reducing agent
USES:
- Hypophosphorous acid and its salt is used as an antioxidant
-prevents the formulation of free iodine in Diluted Hydriodic Acid
- in Ferrous Iodide Syrup, preventing the formulation of both ferric ions and
molecular iodine

also used as preservatives (sodium hypophosphate, ammonium
hypophosphate)

it’s salts when used as antioxidants must never exceed 1%
concentration

Sulfurous anhydride . chlorates or permanganates o Sulfur Dioxide [SO2] .colorless.soluble in water forming sulfurous acid . Leucogen. non-flammable gas with suffocating odor characteristic of burning sulfur . strong reducing agent -hydroiodic acid is formed when passed through an aqueous solution containing iodine -when passed through potassium permanganate it is oxidized to sulfate Uses:  protects susceptible compounds from oxidation  reacts with oxygen before any other compounds do  for injectable preparations in a single-dose ampoules or multiple dose vials  bleaching wood pulps  fumigating grains   arresting fermentation fumigate houses (burning of sulfur candles) o Sodium Bisulfite [NaHSO3] -Sodium Hydrogen Sulfite.> Hypophosphites should never be triturated with oxidizing agents such as nitrates.contains sulfur +4.mixture of NaHSO3 + Na2S2O5 (sodium bisulfate&sodium metabisulfite) .white/yellowish white crystals OR granular powder with sulfur dioxide odor . giving off SO2 o Sodium Metabisulfite [Na2S2O5] . Sodium Acid Sulfite .when under pressure it condenses to a colorless liquid which boils at -10oC .unstable in air.

sold in black cylinders USES:  inert atmosphere to retard oxidation in oxidation sensitive products (Cod Liver Oil.non-flammable.. Multivitamins Preparations)  to replace containers for parenterals and topical solution  to retard oxidation for carbon monoxide .converted to bisulfite when dissolved in water -treatment of bisulfite with aqueous acid yields sulfurous acid .most commercial sodium bisulfite . Olive Oil.white crystal/white to yellowish crystalline powder -odor of sulfur dioxide . does not support combustion . odorless inert gas . neutralizes the stronger bases forming sulfite -addition of sulfites to acidic solutions result in a shift towards alkaline ph by the formation of bisulfite.acidic.which reduces the concentration of hydrogen ions USES:  found in acidic drug solutions containing phenol or catechol to prevent oxidation to quinines  in ascorbic acid injections as strong reducing agent  to prepare water soluble derivatives of normally insoluble drugs Menadione Sodium Bisulfite-for parenteral products o Nitrogen [N2] .colorless.