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Dissolution and Pharmacokinetics parameters

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Dissolution and Pharmacokinetics parameters

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fenilpatel082002
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DISSOLUTION PARAMETERS AND PHARMACOKINETICS PARAMETERS

DECEMBER– 2024

PRESENTED TO :
PRESENTED BY :
Mr.
FENIL N. PATEL (24024671006)
Professor of
1st SEM M.PHARM
GUNI – Faculty of Pharmacy
DEPT.OF PHARMACEUTICS

SHREE S.K PATEL COLLEGE OF PHARMACEUTICAL EDUCATION AND RESEARCH,


GANPAT UNIVERSITY,GANPAT VIDHYANAGAR-384012,KHERVA
DIST:MEHSANA(GUJARAT)
STUDY OF CONSOLIDATION PARAMETERS

 DISSOLUTION PARAMETERS
 PHARMACOKINETICS PARAMETERS
DISSOLUTION PARAMETERS

● Dissolution is the process in which a solid substance solubilizes


in a given solvent.
● 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
 Effect of surface tension of the dissolution medium
 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 temp on 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

● The selection of a proper medium for dissolution testing depends largely


on the physicochemical properties of the drug.
● The media typically used in dissolution studies include acidic solutions,
buffers, surfactants, and surfactants with acid or buffers.
● Surface active agents are used in dissolution test methods to improve the
solubility or wettability of a drug.
INFLUENCE OF PH OF DISSOLUTION FLUID

● Variations in pH exert the greatest effect in terms of drug solubility.


● For weak acids, the rate of dissolution increases with increasing pH, whereas, for weak
bases, the rate of dissolution increases with decreasing pH.
● pH of stomach is ~2. Acetylsalicylic acid pKa is 3.5.
• For tablets containing active ingredients, whose solubility is independent of pH, the
dissolution rate does not vary considerably with changes in pH of the dissolution
medium unless they contain certain excipients that are influenced by pH.
• Sodium bicarbonate, magnesium carbonate, calcium carbonate promotes disintegration
of tablet in acidic medium by producing gas.
EFFECT OF SURFACE TENSION OF THE DISSOLUTION FLUID
● Surface tension shows a significant effect on the dissolution rate of drugs and their release rate from
solid dosage forms.
● Surfactants and wetting agents lower the contact angle and, consequently, improve penetration by the
dissolution medium.
● The incorporation of surface-active agents in the dissolution medium is expected to enhance the
dissolution rate of a poorly soluble drug in solid dosage forms by decreasing the interfacial tension
and micelle formation.
● The addition of surfactant below the CMC can increase significantly the dissolution rate because of
better penetration of the solvent into the tablet resulting in greater availability of the drug surface.
● issolution data for benzocaine in different concentrations of polysorbate 80.
EFFECT OF VISCOSITY OF THE DISSOLUTION MEDIUM

If the interaction at the interfaces occurs much faster than the rate of transport, such as
in case of diffusion controlled dissolution processes, it would be expected that the
dissolution rate decreases with an increase in viscosity.
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 nonionic organic
compounds such as Dextrose were added to the dissolution medium the benzoic acid solubility was
directly dependent on its solubility in a 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 CONDITION

• The suitable 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 reasonably large amount of fluid should be
used.
• To minimize the effect of the concentration gradient and maintain sink conditions, the
concentration of the drug should not exceed 10 – 15% of its maximum solubility in
the dissolution medium selected. Volume generally 500ml, 900 ml and 1000ml used.
DEAERATION OF THE DISSOLUTION MEDIUM

● The presence of dissolved air or other gases in the dissolution medium may impact the
dissolution rate of certain formulations and lead to variable and unreliable results.
● Soluble air in distilled water can significantly lower its pH and as a result, affect the rate of
dissolution of pH-sensitive drugs.
● Another severe effect is the tendency of the dissolved air to be released from the medium in
form of a tiny air bubble.
● These bubbles collect at the surface of the dosage form thereby acting as a hydrophobic
barrier between solvent and solid surface.
● This inhibits wetting and lowers the dissolution rate.
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
● 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.

• Peak plasma concentration (Cmax)


• Time of peak concentration (tmax)
• Area under the curve (AUC)
PEAK PLASMA CONCENTRATION (CMAX)

● It is the maximum plasma drug concentration obtained after oral administration of drug.
● The point of maximum concentration of drug in plasma is known as the peak and the
concentration of drug at peak is known as peak plasma concentration.
● Cmax is expressed in µg/ml or mg/L.
● It is related with intensity of action.
● Plasma concentration time profile indicating Cmax
TIME OF PEAK CONCENTRATION (TMAX)

● It is the time required to reach maximum drug concentration in plasma after extravascular drug
administration.
● It is useful in estimating the rate of absorption.
● It is expressed in hours.
● Onset time and onset of action depends on time of peak concentration.
● Parameter is of particular importance in assessing the efficacy of drugs used to treat acute conditions
like pain and insomnia.
● Plasma concentration time profile indicating tmax
AREA UNDER CURVE (AUC)

● The area under the plasma drug concentration versus time curve.
● AUC is a measurement of the extent of drug bioavailability.
● The AUC reflects the total amount of active drug that reaches the systemic circulation.
● AUC is expressed in mcg*hour/ml.
● It is important for the drugs that are administered repetitively for the treatment of chronic
conditions like asthma or epilepsy.
● Plasma concentration time profile indicating AUC
THANK YOU

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