SOLUTIONS

SOLUTIONS
A

solution is a homogenous one-phase system

consisting of two or more components.
Solution consists of two phases:
- Solvent phase;
determine the phase of the solution and usually
constitutes the largest proportion of the system,
but there are some exceptions e.g. syrup.
- Solute phase;
dispersed as molecules or ions throughout the
solvent i.e. they are said to be dissolved in the
solvent.

Solutions
Gas in gas (air)

solid in solid (alloys)

Gas in liquid (cokes)

liquid in liquid (alcohol in water)

solid in liquid (sugar in water)

Solutions
Well-mixed (uniform) single phase
homogenous
transparent
cannot be separated by filter
sugar in water

do not separate on standing

Definitions

SOLUBILITY
- It is the number of parts of solvent (by
volume) that will dissolve one part of solute
(by weight of a solid or liquid).
- It also can be defined as the amount of a
solute that passes into solution
- A solute will dissolve best in a solvent that
has a similar polarity to itself.
MISCIBILITY
when the two components forming a solution
are either both gases, solids or liquids it is
more usual to talk in terms of miscibility
rather than solubility.

Solutions
Solvent: greater quantity (water)
Solute: smaller quantity (sugar)

Immiscible: two liquids do not mix

miscible: two liquids can mix

(in any quantities)

e.g. alcohol in water

ADVANTAGES OF SOLUTIONS
Liquids

are easier to swallow, and so more

acceptable by paediatric and geriatric use.
Faster therapeutic response.
Uniform distribution of drug throughout
the preparation, compared to suspension
and emulsion.
Reduced irritation to the gastric mucosa,
compared to solid dosage forms, due to
immediate dilution by gastric contents.

DISADVANTAGES OF SOLUTIONS
Bulky,

so inconvenient to transport and

store
If the container breaks, the whole product is
lost.
Poor stability.
Microbial contamination is more likely.
In-accurate dosing.
Difficult to mask the bitter taste of some
drugs.

 Most

solutions prepared in the pharmacy are

straightforward; others have special problems
associated with them.

All

require some knowledge of the solubility

characteristics of the drug(s) being dissolved (These
may be found in Remington's Pharmaceutical
Sciences, dispensing textbooks, Merck's Index).

Pharmaceutical

solutions can be (1) simple or (2)

complex.
In addition that one may find multiple solids (drugs,
stabilizers, buffers, colors, etc.) mixed with multiple
liquids (water, flavors, alcohol, propylene glycol).

 Solutions

are sometimes classified as:

simple solutions
solutions prepared by chemical reaction.
There is no fundamental differences
between them, these terms refer to the
method required to prepare them.
As an example, salt dissolved in water is a
simple solution.
In contrast, one can prepare Calcium
Hydroxide solution (sometimes called Lime
Water) by adding Calcium Oxide to water.
That

which went in is not that which comes

out; a chemical reaction has taken place.

 Strong

Iodine Solution U.S.P. (Lugols

solution)

R/

Iodine
50 gm
Potassium iodide 100 gm
purified water ad 1000 ml
Iodine dissolves in potassium iodide
to form the water soluble I3 complex

FORMULATION OF
SOLUTIONS
A. Aqueous solution
B. Non aqueous solution

AQUEOUS SOLUTION

A. Aqueous solution

Water is the most widely used solvent.

Advantages
Lack of toxicity
non-expensive
physiological compatibility
Disadvantages
Some hydrolysable drugs such as glycosides
and esters form unstable solutions when
dissolved in water.

TYPES OF WATER
1.

Potable Water:
Water freshly drawn from the public water
supply (main system) and suitable for
drinking.

2.

Pharmacopeal Purified Water BP:

- Freshly boiled and cooled immediately before
use to destroy micro-organism.
- Must be used when the presence of salts is
undesirable.
- Prepared by distillation or deionization.

TYPES OF WATER
3.

Water For Injections

Sterilized (pyrogen-free) distilled water
used for parenteral solutions.
CO2-free

water: For formulation of

solutions of some drugs (e.g.
aminophylline), it must be free from
carbon dioxide. This is obtained by
boiling distilled water for 10 minutes,
cooled and sealed in their containers and
then sterilized.

TYPES OF WATER
Aromatic waters

Aromatic waters
Aromatic

waters are saturated solutions of

aromatic or volatile substances in water.
They possess an odor similar to the plant
or volatile substance from which they are
made
Due to their pleasant odor, they used as
flavoring or perfuming vehicles in certain
pharmaceutical preparations.
Mostly they exert no therapeutic action.
Examples: peppermint water, chloroform
water, camphor water,..

Concentrated Aromatic Water

(Spirits)
These

are strong stock solution of aromatic

materials in alcohol.
Fresh aromatic water are prepared by
dilution of the strong one; 1 part of strong
solution to 39 parts of water (freshly boiled
and cooled).
On dilution they yield a fine precipitate. In
the finally divided form, the precipitated
substance is more easily dissolved in water.

IMPROVEMENT OF AQUEOUS
SOLUBILITY

(1) COSOLVENCY
The

solubility of poorly soluble drugs can be

improved by the addition of water miscible
solvent in which the compound is soluble.
Vehicles used in combination to increase the
solubility of a drug are called COSOLVENTS.
Most commonly used blends is water/ethanol
blend, other suitable solvents are glycerol,
propylene glycol.

R/

Sodium Chloride 2.0 G.

Menthol .100 G.
Alcohol 10 mL.
Water q.s. ad 30 G.

Sodium chloride is more soluble in water, menthol is

more soluble in alcohol. That is the way they should
be dissolved, and then the two solutions should be
mixed
together.

IMPROVEMENT OF AQUEOUS SOLUBILITY

(2) pH Control:
If the drug is a weak acid or weak base, its solubility
in water can be controlled by the pH of the system.
(3) Particle size control:
As particle size decrease the drug solubility
increased.

(4) Chemical modification:

The drug may be chemically modified to produce a

water soluble derivative (usually salt form).
Examples;
- sodium phosphate salt of hydrocortisone

NON-AQUEOUS
SOLUTIONS

Non-aqueous solutions
If

the drug is insoluble (griseofulvin)

or unstable (e.g methylpenicillin) in
aqueous systems, it is necessary to
use alternative systems such as oils,
alcohols, liquid paraffin, glycerol.

Non-aqueous solvents
1.

Fixed oil of vegetable origin

- such as olive oil, almond oil, castor oil, ..

-

They are used mainly in preparation of

intramuscular injections e.g. Oily Phenol Injection
BP and Calciferol Injection BP, for depot therapy
Some are of suitable taste and odour for oral use
as solvent for materials as vitamin A and D.
Oils are unpleasant to use externally, unless in
emulsion.

Non-aqueous solvents
(2) Alcohols
Ethyl alcohol is a widely used solvent,
specially for external use due to its rapid
evaporation and cooling effect (e.g. paints
and liniments).
It can be used orally as cosolvent (e.g.
elixirs)
Isopropyl alcohol, has similar properties to
ethyl alcohol, but less likely to be abused if
taken orally.

Non-aqueous solvents
(3) Miscellaneous
Glycerol,
dimethylsulfoxide,
liquid paraffin,
propylene glycols,
tinctures.

Types of Preparations
Solutions

for cutaneous application;

Lotion, liniments, paints, collodions
Ear (otic) prepartions:
- Simple solution of drugs in either water,
glycerol, alcohol/water mixture for local use
- Applied as drops, sprays or washes
Eye preparations:
These are small-volume sterile liquids to be
instilled on to the eyeball for local effect

Types of Preparations
Irrigations:

- Sterile, large-volume, aqueous solutions

for cleansing of body cavities and wounds.
Mouthwashes and gargles:
- Aqueous solution for the prevention and
treatment of mouth and throat infection can
contain antiseptic and analgesic drugs
Nasal products:
- pH should be adjusted to 6.8.
- Anti-inflammatory and decongestants are
commonly used

Types of Preparations
Oral

liquids:
Elixir, linctuses, mixtures and draughts.
Parentral products:
Sterile solution for injection or infusion into
the body.
Rectal preparations:
- Aqueous or oily preparations for
cleansing, diagnosis or therapeutic
reasons (e.g.ENEMAS)

Types of Preparations
Intermediate

products:

1- Aromatic water and spirites

2- Extracts, infusion and tinctures:
Are concentrated solutions of active
principles from animal or vegetable source.
3- Syrups
-Are concentrated solution of sucrose to
which drug and flavorings are added.
e.g. Codiene Phosphate syrup (cough
suppressant)

RECOMMENDATIONS ON PREPARING
SOLUTIONS
1.

Small quantities of highly soluble materials

dissolve immediately; solution rate slows down
as more and more solute is added and may
stop as "saturation"' is reached.
2. The more rapid the stirring, the more rapidly
solution is achieved (because turbulence
reduces the width of the '"diffusion layer"
around the particles of solute).
There are some situations when vigorous
stirring is not desirable e.g. foaming agent (as
soap), or viscous solution (formation of air
bubbles which could take many, many hours
to go away.

RECOMMENDATIONS ON PREPARING SOLUTIONS

3.

Particle size reduction by grinding in a

mortar with a pestle, this is important for
"slightly soluble drug.
4. Heating usually hastens solution rate-but should be used only when necessary,
avoided in volatile materials.
5. The '"Order of Addition" may be
important. Make certain that you are
familiar with the
solubility characteristics of your solutes and
solvents.

 6.

As a general rule, non-viscous solutions

should be filtered. This rule is not followed
when the volume is small since significant
amounts of the liquid may be retained by
the filter paper.

SOLUTION
Examples of
solutions
Gas

Solute
Gas

Solid

Ethanol (common
alcohol) in water;
various hydrocarbons
in each other
(petroleum)

Sucrose (table sugar) in

water; sodium chloride
(table salt) in water;
gold in mercury,
forming an amalgam

Oxygen and other

gases in nitrogen (air)

Carbon dioxide in
Liquid water (carbonated
water)
Solvent

Solid

Liquid

Hydrogen dissolves
rather well in metals;
Hexane in paraffin
Steel, duralumin, other
platinum has been
wax, mercury in gold. metal alloys
studied as a storage
medium.