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PREFORMULATION STUDIES:
PHYSICOCHEMICAL
CHARACTERIZATION
OF NEW DRUG MOLECULES
Presented By:-
BHATT BHAVIK R.
1st M- Pharm.
Department of Pharmaceutics.
NGSM IPS, Mangalore
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CONTENTS
INTRODUCTION
OBJECTIVES
PREFORMULATION STUDIES
PHYSICOCHEMICAL CHARACTERISATIONS
ANALYTICAL MEASURES
CONCLUSION
REFERENCES
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INTRODUCTION
Preformulation testing is the first step in the rational
development of dosage forms.
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OBJECTIVES
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Why is Preformulation Important ?
It describes the process of optimizing the delivery
of drug thorough determination of physical, chemical
properties of new drug molecule that affect drug
performance and development of an efficacious stable
and safe dosage form.
Crystallinity
The crystal habit describes the outer appearance of crystals
( platy, equant, needle, bladed, etc.) and internal structure
arrangement.
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Polymorphism
polymorphism is the ability of the compound to crystallize as
more than one distinct crystalline species with different internal
structure.
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Particle size
Study of particle size give an information about solubility,
dissolution rate, absorption, etc.
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SOLUBILITY ANALYSIS
1. AQUEOUS SOLUBILITY
Important goal of the preformulation effort is to devise a
method for making solutions of the drug
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2. Drug pKa / Ionization at physiological pH
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The percentage of ionization can be calculated as …
K=Co/Cw
Intrinsic dissolution
Paricular dissolution
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DRUG STABILITY
In this study includes both solutions and solid-state
experiments under various conditions for handling, formulation,
storage, and in vivo administration.
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COMPATIBILITY
Compatibility test play a very important role in the
preformulation studies of oral dosage forms.
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ANALYTICAL MEASURES
These includes:
1. Microscopy
2. Spectroscopy
3. Chromatography
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A. MICROSCOPY:
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B. SPECTROSCOPY
UV and Visible Spectrophotometry
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X-RAY DIFFRACTION
Single Crystal X-ray provides the most complete information about the
solid state.
This method is tedious, time consuming & hence unsuitable for routine
use.
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Thermal Analysis
Differential scanning calorimetry (DSC) and differential
thermal analysis(DTA) are particularly useful in
preformulation studies including purity, polymorphism,
solvation, degradation, and excipient compatibility.
Thermigravimetric analysis
Used to detect the existange and stability of solvated
drug molecule.
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C. CHROMATOGRAPHY
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REFERENCES
1) Banker GS, Rhodes CT., Modern pharmaceutics, 4th ed. New
York: Marcel Dekker; 2002. p.167-184
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Thank you
….
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