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PHYSICAL PHARMACY LABORATORY

(REVIEWER – THEORETICAL)

→ Class II methods – use water that


is added to the drug in a
MODULE 1: HOMEGENEOUS SYSTEMS
sufficient amount to form an
isotonic solution. The preparation
is then made up to its final
In aqueous solution, volume with an isotonic or a
- an ACID increases the buffered isotonic dilution solution.
concentration of hydronium ions These include;
[H3O+], sometimes represented as 1. White–Vincent method
hydrogen ions [H+] 2. Sprowls method.
- a BASE increases the
concentration of hydroxide ions Sodium chloride equivalent method
[OH-]. - This method is based on
calculating the E-value.
- BUFFERS are included in the - the sodium chloride equivalent or
dosage form to impart sufficient tonicity equivalent of a drug. It is
stability to enable the the amount of sodium chloride
formulation. that has the same osmotic effect
- BUFFERS are substances or a (is equivalent to) as 1 g of the
combination of substances that, drug.
by their presence in solution, resist White–Vincent method
changes in pH upon the addition - This method involves the addition
of small quantities of acid or alkali. of water to the drugs to prepare
an isotonic solution, followed by
Body fluids (blood and lacrimal fluid) the addition of an isotonic or
have an osmotic pressure corresponding isotonic-buffered diluting vehicle
to that of 0.9% (w/v) sodium chloride. to make up the solution up to the
final volume.
hydronium and hydroxide ions are Application of Tonicity
present both in pure water and in all - It is generally accepted that for
aqueous solutions, and their ophthalmic and parenteral
concentrations are inversely administration, isotonic solutions
proportional as determined by the ion are better tolerated by the
product of water. patient than those at the
extremes of hypo- or
B. Methods of Adjusting Tonicity
hypertonicity.
The methods for adjusting tonicity - Isotonic solutions cause no
subdivided into two classes: swelling or contraction of the
→ Class I methods, which employ tissues with which they come in
sodium chloride or some other contact and produce no
substance to the drug solution to discomfort when instilled in the
lower the freezing point of the eye, nasal tract, blood or other
solution to – 0.52° and thus make body tissues.
it isotonic with body fluids. Ophthalmic medication
1. Cryoscopic method - It is generally accepted that
2. Sodium chloride equivalent ophthalmic preparations
method intended for instillation into the
PHYSICAL PHARMACY LABORATORY
(REVIEWER – THEORETICAL)
cul-desac of the eye should, if The influence of substituents on the solubility
possible, be approximately of molecules in water can be due to their
isotonic to avoid irritation. The effect on the properties of the solid or
isotonic preparation duplicates liquid or to the effect of the substituent on its
interaction with water molecules.
ophthalmic tears for the comfort
of the patient.
• Polar groups such as –OH capable of
Parenteral medication
hydrogen bonding with water
- Injections that are not isotonic molecules impart high solubility.
should be administered slowly • Non-polar groups such as –CH3 and –
and in small quantities to Cl are hydrophobic and impart low
minimize tissue irritation, pain and solubility.
cell fluid imbalance.
- When parenteral solutions are
formulated, the tonicity of OTHER NOTES FOR LECTURE:
hypotonic solutions is adjusted by SOLIDS – Amorphous powder (ionic,
the addition of dextrose or covalent)
sodium chloride. This is true for LIQUIDS – Water bonds
parenterally administered GASES – Free to move around
medicines and total parenteral - Inhaler (high kinetic energy)
nutrition (TPN), which is an Polyphasic – adjusting phases
integral part of therapeutic Eutexia – absorb heat (liquefy)
options available to hospitalized
patients. SUBLIMATION – solid to gas
MELTING – solid to liquid
A. SOLUBILITY OF SOLIDS IN WATER FREEZING – liquid to solid
Liquid crystalline state – in between
- Solubility is defined liquid
in quantitative terms as
the concentration of solute in a Solvates – pseudomolymorphs
saturated solution at a certain Enantiotropic – reverse direction
temperature, and in a qualitative Monotropic – one direction only
way, it can be defined as
the spontaneous interaction of
two or more substances to form a
homogeneous molecular
dispersion.
The boiling point of liquids and the melting
point of solids both reflect the strengths of
interactions between the molecules in the
pure liquid or the solid state.

- In general, aqueous
solubility decreases with increasing
boiling point and melting point.

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