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Pharmaceutical Chemistry 1 (Lecture Notes)

Acids and Bases- Used in the conversion of drugs to chemical forms


convenient to their product formulation.
Official Inorganic Acids
1. Boric Acid
Synonyms: Agua Boricada, Boric Acid.
Occurrence: Native boric acid is called Sassolite, its largest source is in the
combinations of:
Na2B4O7. 4H2O (Rasorite or Kernite)
Na2B4O7. 10H2O (Borax)
CaB4O7. 4H2O (Borocalcite)
Ca3B6O10. 5H2O (Colemanite)
H3BO3. Na2B4O7. 2CaB4O7. 18H2O (Tincal).
Properties: It is available in 3 forms,
1. Colorless, odorless, pearly scales.
2. Six-scaled triclinic crystals.
3. White, odorless powder that is unctuous to touch (soapy texture).
-Not absorbed through intact skin but highly toxic when ingested orally.
-Clear solutions are obtained when 1 gram is dissolved in 25 ml water,
addition of HCL decreases its solubility in water.
Uses:
-It must contain not less than 95% and not more than 100.5%, calculated as
anhydrous form, also a weak bacteriostatic.
- Antiseptic solutions, ointments and powders.
- 2.5% to 4.5% for use an eyewash.
-Used as a buffer in ophthalmic solutions like:
Aluminum Acetate USP Solution XVIII and Aluminum Subacetate Solution USP
XVIII.
- Reaction of Boric Acid with equimolar quantities of Glycerin at 140-150
degrees Celsius, produces Boroglycerin Glycerite which is being used as a
base for suppositories.
2. Hydrochloric Acid
Synonyms: Muriatic Acid, Spirit of Sea Salt, Marine Acid and Espiritu de Sal
Marina.
Occurrence: An aqueous solution of hydrogen chloride gas containing not
less than 35% and not more than 36% per HCL weight.
Properties: It is color yellow in solution due to the absorption of unknown
impurities.
Uses:
- Used as a pharmaceutical aid or as an acidifying agent.
- Capable of reacting with organic molecules to form water-soluble
hydrochloride salts.
- Suitable for incorporation into a solid dosage form.
- Disadvantage of usage, is that it is hygroscopic (absorb moisture,
staying dry).
Diluted Hydrochloric Acid
It contains not more than 9.5 g and not more than 10.5 g per 100 mL.
- It exists in the normal gastric juice (containing about 0.2%).
- Aids the conversion of pepsinogen into pepsin & proteids into peptones
and as gastric antiseptic.
- Valuable in some forms of indigestion; achlorhydria (absence) and
hypochlorhydria (deficiency).
- Diluted in water and transmitted through a straw, since it can cause
the solvent action in the enamel of the teeth.
- Glutamic Acid Hydrochloride and Betaine Hydrochloride-
available forms.

3. Nitric Acid
Synonyms: Spirit of Nitre, Aqua Fortis, Agua Fuerte and Azotic Acid.
Properties:
- An aqueous solution containing not less than 68% and not more than
71% per weight of HNO3.
- Corrosive, fuming liquid with a characteristic highly irritating odor.
- Produces a yellow stain on animal tissue due to nitration of aromatic
amino acids, phenylamine, tyrosine and tryptophan found on
skin.
- It is a strong monoprotic acid that is also an oxidizing and nitrating
agent.
- Its nitrating properties are used in organic chemistry, it also used in the
manufacture of trinitrotoluene (TNT).
Uses:
- An acidifying agent with bases.
- Nitrating agent in Pyroxylin USP XVIII as a source of nitrate ion in
creating Milk of Bismuth.
- Destroys chancres and warts.
4. Phosphoric Acid
Synonyms: Orthophosphoric Acid.
Properties:
- A non-volatile and has no oxidizing properties, thus enabling its use
whenever a non-oxidizing acid is required.
Uses:
- As an acidifying agent.
- Can be used to treat Sodium Hydroxide at particular concentrations to
produce mixtures of HPO4 (2-) and H2PO4- that serves as the basic
and acidic species of the buffer system.
- Used as a solvent in the preparation of Anileridine Injection NF XV.

Diluted Phosphoric Acid


- Not less than 9.5 g and not more than 10.5 g in 100 ml solution.
- As a tonic and stimulant to the gastric system, acts as a synergistic
that aids to form peptones.
- Also used for some pharmaceutical preparations.
5. Sulfuric Acid
Synonyms: Oil of Vitriol
Properties:
- Has an oily consistency containing not less than 94% and not more
than 98% of H2SO4.
- When heated strongly, it becomes vaporized and gives off white and
dense fumes of Sulfur Trioxide.
- 10% dissolved of Sulfur Trioxide is also called as Oleum, fuming
Sulfuric Acid, Pyrosulfuric Acid, Disulfuric Acid or Nordhausen Acid are
its variants.
Preparation:
Contact Process Lead Chamber Process
Used mostly by commercial Most concentrated product that
industries and has an advantage contains only 76% by weight of
to obtain a product with various H2SO4, used this process to
strength, Vanadium and create Primary Calcium
Platinized Silica gels are used as Phosphate or Superphosphate
catalysts. and Fertilizer.
Uses:
- Used to form salts of basic organic drug molecules.
- Used as a dehydrating agent in the preparation of Pyroxylin USP 26.

Official Inorganic Bases


1. Strong Ammonia Solution
Synonyms: Ammonium Hydroxide, Ammonia Water.
Properties:
- Upon exposure to air, it loses Ammonia rapidly.
- It has a pungent, characteristic odor.
- Caution: Because of the caustic nature of the solution, the irritating
properties of the vapor might be inhaled, cover its closure with a cloth
while opening to avoid inhalation.
- It possesses an unshared electrons, serves as a liquid in forming
soluble complex ions with many metal cations.
Uses:
- It is used as a Bronsted base to form ammonium salt of acids.
- Used in the manufacture of Nitric acid and Sodium Bicarbonate.
- Used in the preparation of Aromatic Ammonia Spirit, that serves as a
source of ammonia to balance ammonium carbonate against
hydrolysis.
- Used in the preparation of Ammoniacal Silver Nitrate Solution.
Diluted Ammonia Solution
- Not more than 9 g and not more than 10 g in each 100 ml solution.
- Also known as Ammonia Water or Household Ammonia.
- Used as a circulatory stimulant through inhalation, used as counter-
irritant for external use.
2. Calcium Hydroxide
Synonyms: Slaked Lime, Limewater.
Properties:
- White Powder having an alkaline and bitter taste.
- Ability to absorb Carbon Dioxide from the air, leading to the formation
of Calcium Carbonate giving its cloudy appearance of the solution.
-
Preparation:
- Slaking: It is a process of avid absorption of water by the oxide,
followed by the evolution of much heat, swelling of calcium oxide
lumps and its final disintegration into powder.
Uses:
- Used as a fluid electrolyte and as a topical astringent.
- Used in pharmaceutical preparations for its high Hydroxide ion
concentration.
- Allows to react with free Fatty Acids in various oils to form soaps.
- Useful in certain types of gas traps.
3. Potassium Hydroxide
Synonyms: Caustic Potash, Potassa.
Properties:
- Very delinquent and rapidly absorbs both moisture and Carbon Dioxide
from the air.
- Having a caustic or corrosive effect on tissues destroys tissues.
Uses:
- Used as a caustic principally in veterinary practice.
- As a saponifying agent to hydrolyze esters of fatty acids into their
constituent, alcohols and the Potassium salt.
- It is known for its widest use as a base or alkaline reagent.
4. Sodium Hydroxide
Synonyms: Caustic Soda, Soda Lye.
Properties:
- It is very delinquent and rapidly absorbs moisture and Carbon Dioxide
from the air.
- Catalyzes the hydrolysis of esters and therefore employed as a
saponifying agent, it is also a very strong base that attacks the tissues.
- Since it easily breaks the glass bottle, an amount of Paraffin or
petroleum should be placed around the stopper; or hard glass with
rubber stoppers can be used.
Uses:
- It has the same use and purpose as Potassium Hydroxide.
- It is delinquescent, also mild and cheaper.
- It is mostly used for industrial purposes.
5. Sodium Carbonate
Synonyms: Monohydrated Sodium Carbonate.
Properties:
- It absorbs small amounts of moisture from the air.
- It effloresces in dry air at 50 degrees Celsius or higher.
- Thus, becoming anhydrous at 100 degrees Celsius.
In addition to the Calcined Soda (Soda Ash), there are 3 forms:
1. Monohydrate- Na2CO3. H2O
2. Heptahydrate- Na2CO3. 7H2O
3. Decahydrate- Na2CO3. 10H2O (Sal Soda, Washing Soda)
Preparation:
- Created through the utilization of the Solvay Process:
Cooled concentrated solution of Sodium Chloride first with Ammonia
and then with Carbon Dioxide.
Uses:
- Used for basicity in pharmaceutical preparations where it would form
sodium salts of acidic drugs.
- Used in preparation of Nitromersal Solution NF XV.

6. Soda Lime
Information:
- It is a mixture of Calcium Hydroxide and Sodium or Potassium
Hydroxide or both.
- Intended for use in Metabolic Tests, Anesthesia and Oxygen Therapy.
- While in a closed system, its function is to absorb the Carbon Dioxide.
- Sodium Hydroxide is capable of sweeping/picking up Carbon Dioxide.
- Calcium Hydroxide present in the mixture will react with the
accumulated Carbon Dioxide in the form of Na2CO3 to form Calcium
Carbonate, therefore regenerating the Sodium Hydroxide.