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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.
-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
- 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
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
- 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.
- 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
- It is a strong monoprotic acid that is also an oxidizing and nitrating
- Its nitrating properties are used in organic chemistry, it also used in the
manufacture of trinitrotoluene (TNT).
- 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.
- A non-volatile and has no oxidizing properties, thus enabling its use
whenever a non-oxidizing acid is required.
- 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
- 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.
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.
- 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.
- 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.
- 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
- 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.
- 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.
- 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.
- Used as a fluid electrolyte and as a topical astringent.
- Used in pharmaceutical preparations for its high Hydroxide ion
- 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.
- Very delinquent and rapidly absorbs both moisture and Carbon Dioxide
from the air.
- Having a caustic or corrosive effect on tissues destroys tissues.
- 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.
- 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.
- 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.
- 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)
- Created through the utilization of the Solvay Process:
Cooled concentrated solution of Sodium Chloride first with Ammonia
and then with Carbon Dioxide.
- 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
- 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.