STUDY OF CONSOLIDATION PARAMETERS
DISSOLUTION PARAMETERS
PHARMACOKINETICS PARAMETERS
CONSOLIDATION
An increase in the mechanical strength of the material
resulting from particle or particle interaction. ( Increasing
in mechanical strength of the mass)
DISSOLUTION PARAMETERS
Dissolution is a process in which a solid substance solubilizes
in a given solvent i.e. mass transfer from the solid surface to
the liquid phase.
Dissolution parameters:
Effect of agitation
Effect of dissolution fluid
Influence of pH of dissolution fluid
Cont….
Effect of viscosity of the dissolution medium
Effect of the presence of unreactive and reactive additives
in the dissolution medium.
Volume of dissolution medium and sink conditions
Deaeration of the dissolution medium
Effect of temperature of the dissolution medium
EFFECT OF AGITATION
The relationship between the intensity of agitation and the
rate of dissolution varies considerably according to the
type of agitation used, the shape and design of the stirrer
and the physicochemical properties of the solid.
For the basket method, 100 rpm usually is utilized, while
for the paddle procedure, a 50 – 75 rpm is recommended.
EFFECT OF DISSOLUTION FLUID
Selection of proper medium for dissolution testing
depends largely on the physicochemical properties of the
drug.
INFLUENCE OF PH OF DISSOLUTION
FLUID
simulated gastric fluid as the test medium for tablets
containing ingredients which reacted more readily in acid
solution than in water (e.g., calcium carbonate).
EFFECT OF VISCOSITY OF THE
DISSOLUTION MEDIUM
If the interaction at the interfaces, occurs much faster than
the rate of transport, such as in the case of diffusion
controlled dissolution processes, it would be expected that
the dissolution rate decreases with an increase in viscosity.
The rate of dissolution of zinc in HCl solution containing
sucrose was inversely proportional to the viscosity of
solution.
EFFECT OF THE PRESENCE OF
UNREACTIVE AND REACTIVE ADDITIVES
IN THE DISSOLUTION MEDIUM
When neutral ionic compounds, such as sodium chloride
and sodium sulfate, or non ionic organic compounds, such
as dextrose, were added to the dissolution Medium, the
dissolution of benzoic acid was dependent linearly upon
its solubility in the particular solvent.
When certain buffers or bases were added to the aqueous
solvent , an increase in the dissolution rate was observed.
VOLUME OF DISSOLUTION MEDIUM
AND SINK CONDITIONS
The proper volume of the dissolution medium depends
mainly on the solubility of the drug in the selected fluid.
If the drug is poorly soluble in water, a relatively large
amount of fluid should be used if complete dissolution is
to be expected.
DEAERATION OF THE DISSOLUTION
MEDIUM
Presence of dissolved air or other gases in the dissolution
medium may influence the dissolution rate of certain
formulations and lead to variable and unreliable results.
Example, the dissolved air in distilled water could
significantly lower its pH and consequently affect the
dissolution rate of drugs that are sensitive to pH changes,
e.g., weak acids.
EFFECT OF TEMPERATURE OF THE
DISSOLUTION MEDIUM
Drug solubility is temperature dependent, therefore careful
temperature control during the dissolution process is
extremely important.
Generally a temperature of 37°±0.5 is maintained during
dissolution determination of oral dosage forms and
suppositories.
For topical preparations as low as 30° and 25°have been
used.
PHARMACOKINETIC
PARAMETERS
PHARMACOKINETIC PARAMETERS
Pharmacokinetics is defined as the kinetics of drug
absorption, distribution, metabolism, and excretion and
their relationship with pharmacologic, therapeutic or
toxicologic response in mans and animals.
PLASMA DRUG CONCENTRATION-
TIME PROFILE
Three important pharmacokinetic
parameters:
Peak plasma concentration (cmax)
Time of peak concentration (tmax)
Area under the curve (AUC)
PEAK PLASMA CONCENTRATION
(Cmax)
The point of maximum concentration of a drug in plasma
is called as peak and the concentration of drug at peak is
known as peak plasma concentration.
It is also called as peak height concentration and
maximum drug concentration.
Cmax is expressed in mcg/ml.
TIME OF PEAK CONCENTRATION
(tmax)
The time for drug to reach peak concentration in plasma
( after extravascular administration) is called the time of
peak concentration.
It is expressed in hours.
AREA UNDER THE CURVE (AUC)
It represents the total integrated area under the plasma
leveltime profile and expresses the total amount of drug
that comes into the systemic circulation after its
administration.
AUC is expressed in mcg/ml X HRS.
It is important for the dugs that are administered
repetitively for the treatment of chronic conditions like
asthma or epilepsy
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