Pharmaceutical Aids

and Necessities
By: Kyle Angelic Davasol
 OBJECTIVES
Identify the different pharmaceutical aids and necessities
Describe the properties of different pharmaceutical aids
Discuss the importance and application of pharmaceutical
aids and necessities to pharmaceutical preparation
 OVERVIEW

Pharmaceutical aids and necessities are agents important

for:
Preparation
Preservation
Storage of pharmaceuticals
 CLASSIFICATION
Acids and bases
Buffers
Antioxidant
Water
Glass
Radiopharmaceuticals
 ACIDS, BASES AND BUFFERS
Bronsted-Lowry theory is the acid base theory we use in the
pharmacy because physiologic functions and pharmaceuticals
are often times dispensed as an aqueous solution.
General chemical expression:
HA + B = A- + HB-
Acid + Base = conjugate base + conjugate acid
 Electrolytes
Strong acids and bases are strong electrolytes
Weak acids and bases are weak electrolytes
Relation
The stronger the acid, the weaker its conjugate base, and vice versa.
The stronger the base, the weaker its conjugate acid, and vice versa.
  OFFICIAL INORGANIC ACIDS
1. Boric Acid (H3BO3)
Synonym: boracic acid, hydrogen borate, orthoboric acid
Occurrence: found in seawaters, certain plants in nearly all fruits and in some volcanic stem jets. The
native boric acid is called sassolite.
Properties: Available in three crystalline forms:
• Colorless, odorless, pearly scales
• Six-sided triclinic crystals
• White, odorless powder with a soapy feel
Uses: antiseptic because it is a weak bacteriostatic agent; in 2% w/c concentration as eyewash and as buffer
in ophthalmic solutions
the toxicity of boric acid makes it unfit to be taken orally.
Hydrochloric acid (HCl)
Synonym: chlorhydric acid, spirit of sea salt, muriatic acid
Uses: a pharmaceutical aid as an acidifying agent
 
Diluted Hydrochloric acid
Diluted HCl exists in the normal gastric juice aiding in the
conversion of pepsinogen into pepsin and of proteins into peptones
and serving as a gastric antiseptic. It is also used in management in
gastric achlorhydria, the absence if HCl in the stomach; and
hypochlohydria, the deficiency of HCl production of the stomach.
Nitric acid (HNO3)
 Synonyms: spirit of nitre, aquafortis, aqua fuerte
 Properties: nitric acid will produce a yellow stain on animal tissue due to the
nitration of the aromatic amino acid, phenylamine, tyrosine and tryptophan
found in the proteins of skin
 This reaction is known as xanthoproteic test It oxidizes common metals except
gold and platinum to produce the nitrate salt of the metal
 Uses: the manufacture of sulfuric acid, coal tar dyes and explosive, a nitrating
agent in pyroxylin USP XVIII; a source of nitrate ion in the preparation of milk
of bismuth, externally, the elimination of chancres and warts.
Phosphoric acid (H3PO4)
 Synonym: orthophosphoric acid, acido orthofosforico
 Use: acidifying agent
 
Diluted phosphoric acid
 Uses: a tonic and stimulant to the gastric mucous membranes; a synergestic substance to pepsin
and acids to the formulation of peptones
 
Sulfuric acid (H2SO4)
 Synonym: oil of vitriol, vitriolic acid, aceite de vitriole
 Preparation: there are two ways to prepare sulfuric acid:
 Contact of catalytic process
 Lead chamber process
 Both have the same principle, that is, the oxidation of the sulfur dioxide to sulfur trioxide by
adding enough water to form sulfuric acid.
 In the catalytic process, vanadium and platinized silica gels are catalyst.
 Use: dehydrating agent in the preparation of pyroxylin USP XX
 
Acetic acid (CH3COOH)
 Synonym: glacial acetic acid
 Use: irrigation solution with some bacteriostatic properties
 Official Inorganic Bases
Strong Ammonia Solution Sodium Carbonate
Diluted Ammonia Solution Soda Lime
Calcium Hydroxide Potassium Bicarbonate
Potassium Hydroxide Sodium Bicarbonate
Sodium Hydroxide
 Strong Ammonia Solution (NH4OH)
Other Names:
USP38/NF33
 Ammonium Hydroxide
 Stronger Ammonia Water
Precautions:
 Use care in handling (Caustic nature and irritating properties of its vapor)
 Cool the container well before opening
 Cover the closure with cloth while opening
 Do not waste or inhale the vapors
 Bronsted base
 Manufacture of nitric acid and sodium bicarbonate
 Preparation of aromatic spirit
 Preparation of ammoniacal silver nitrate solution 
Tollens’ reagent is an alkaline solution of ammonia cal silver nitrate and is used to test for aldehydes
 Diluted Ammonia Solution (NH4OH)
USP38/NF33
Prepared from strong ammonia solution
Known as ammonia water or household ammonia
Employed as circulatory stimulant through inhalation of vapors
USES
When used externally, it is counter-irritant
 Calcium Hydroxide Ca(OH)2 USP38/NF33
Other Names
Slaked lime
Calcium hydrate
Preparation: Manufacture from lime or Calcium Oxide by slaking process

Medicinally used as fluid electrolyte and topical astringent

Utilized for its high hydroxide ion concentration in pharmaceutical preparations
Its alkalinity reacts with free fatty acids in various oils to form calcium soaps which have emulsifying properties.
Due to its ability to absorb CO2 from expired air, it is combined with NaOH or KOH in a mixture known as soda
lime
Potassium Hydroxide (KOH) USP38/NF33
Other names:
• Caustic potash
• Potassa
Properties:
• Deliquescent
• Very strong base with caustic/ corrosive effect on tissues (handle carefully)
Uses:
• As a caustic in veterinary practice
• As a saponifying agent to hydrolyze esters of fatty acids into their constituent alcohols and potassium salt
Sodium Hydroxide (NaOH) USP38/NF33
Other Names:
• Caustic soda
• Soda lye
Properties
• It attacks soft glass (containers should be made of hard glass with rubber stoppers)
• Glass-stoppered bottles can be used if a little petroleum or paraffin is spread around the stopper
• Not borosilicate, a soft glass has high coefficients of thermal expansion, thus it does not require a high
temperature to make them soft.
Uses:
• Same as potassium hydroxide but has advantage since it less deliquescent, milder, and cheaper.
Sodium Carbonate (Na2CO3.H2O) USP38/NF33
Other Names:
 Monohydrate sodium carbonate
Use:
 In pharmaceutical preparations, its basicity forms sodium salts of acidic
drugs
 
Soda Lime USP38/NF33
Uses:
 A mixture of Ca(OH)2 and NaOH or KOH or both intended for
metabolism test, anesthesia, and O2 therapy
Potassium Bicarbonate USP38/NF33
Other Names:
 Potassium Hydrogen Carbonate
 Potassium Acid Carbonate
Use:
 Buffering agent for pharmaceutical preparations
 
Sodium Bicarbonate USP38/NF33
Other Names:
 Sodium Hydrogen Carbonate
Use:
 Preferred in preparation of effervescent mixtures containing sodium
bicarbonate and organic acids such as tartaric or citric.
 These additives react to liberate CO2 that acts as a disintegrator
producing effervescent when in water.
 BUFFERS
A buffer is a solution of a weak acid and its salt or the salt of its conjugate base or a weak base and its salt or the
salt of its conjugate acid that resist drastic changes in pH when small amounts of acid or base are added to it.
Buffers control the pH of pharmaceutical products within certain specified limits for these reasons:
A. Chemical Stability
B. Solubility of the drug
C. Patient’s comfort
 
Some factors which can produce alterations in pH include:
D. Alkali in certain inexpensive containers
E. Gases present in air such as CO2 and NH3
 MECHANISM OF ACTION
When small amounts of hydrogen ion are introduced into the medium, they will react with the conjugate base and basic members of
the buffer to form a weak acid.
Similarly, when small amounts of hydroxide ion are introduced into the medium, they will react with the weak acid or acidic member
of the buffer pair and form water and the conjugate base.
Hence, each component of the buffer pair will react with either acid or base to form the other component.
 
If base (OH) is added, it will react with the acid to neutralize the base, forming acetate ion and water.
H2C3O2 + OH → C2H3O2 + H2O
The selected buffer should not:
Participate in oxidation-reduction reaction
Alter the solubility of other components
Form complexes with active ingredients
Examples
ACETIC ACID AND ITS CONJUGATE BASE, ACETATE ION

HC2H3O2 + H2O → H3O + C2H3O2

If acid (H3O) is added, it will react with the conjugate base to neutralize the acid, forming acetic acid and
water

C2H3O2 + H3O → HC2H3O2 + H2O

Consider the following when choosing a buffer

1. Volatile species should not be used as buffers
2. It should not have any influence on the pharmacological activity of the API
3. The use of pharmaceutical should be considered in choosing a buffer for a product. If it is to be
ingested, buffers containing borates should not be used as they are toxic systemically
TWO INORGANIC BUFFER SYSTEMS:
PHOSPHATE BUFFER SYSTEM
ADVANTAGE: it contains dihydrogen and monohydrogen phosphate ions which are found
normally in the body
DISADVANTAGE: The insolubility of the phosphate salts of such metals such as Ag, Zn and
Al support microbial growth
BORATE BUFFER SYSTEM
It contains metals that would precipitate in the presence of phosphate.
They are toxic and it is suitable in external preparations, ophthalmic, and nasal solutions but
is contraindicated in parenteral solutions.
 THREE PRIMARY BORATE BUFFER
SYSTEMS:
FELDMAN’S BUFFER SYSTEM
pH of 7.6 - 8.2
Consist of BORIC ACID, NaCl (to make it isotonic), and Sodium Borate
ATKINS AND PANTIN BUFFER SYSTEM
pH of 7.6 -11
Consist of Sodium carbonate, Boric acid, and NaCl
GIFFORD BUFFER SYSTEM:
pH of 6 - 7.6
Similar to Feldman’s Buffer System but NaCl is replaced by KCl to make it hypotonic
STANDARD BUFFER SOLUTION
Buffer system in pharmacy can be roughly categorized into:
1. Standard buffer systems - designed to provide a solution having a specific pH for analytical purposes.
2. Actual pharmaceutical buffers - designed to maintain pH limits in drug preparations.
 

STANDARD BUFFER SOLUTIONS

Standard buffer solutions having pH ranges between 1,2 and can be prepared by appropriate combinations of:
 BORIC ACID AND POTASSIUM CHLORIDE, 0.2M
 HYDROCHLORIC ACID, 0.2M
 POTASSIUM CHLORIDE, 0.2M
 POTASSIUM PHOSPHATE, MONOBASIC 0.2M
 POTASSIUM BIPTHALATE, 0.2M
 SODIUM HYDROXIDE, 0.2M
 ACETIC ACID, 2N
 BUFFER pH COMPOSITION

50ml KCl solution with a specified volume of

HYDROCHLORIC ACID 1.2 - 2
0.2 HCl and water

50 ml of potassium biphthalate solution with a

ACID PHTHALATE BUFFER 2.2 - 4.0
specified volume of 0.2 HCl and water

50 ml of potassium biphthalate with a

NEUTALIZED PHTHALATE BUFFER 4.5 - 5.8
specified volume of NaOH and water

50 ml of monobasic potassium phosphate with

PHOSPHATE BUFFER 5.8 - 8.0
NaOH and water

50ml of boric acid and KCl with NaOH and

ALKALINE BORATE 8.0 - 10.0
water

Specified amount of sodium acetate with

ACETATE BUFFER 4.1 - 5.5
acetic acid and water