Principal areas of preformulation research. Key points:- 1.Physico chemical properties 2. Bulk characterisation 3.Solubility Analysis 4.Stability analysis. Uses and their Important techniques.

1. Principal areas of
Preformulation Research
Sarvesh Bari
Roll no :- 03
Ideal Institute of Pharmacy

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Principal Areas Of Preformulation Research
1. Physico –Chemical Properties
2. Bulk Characterisation
3. Solubility Analysis
4. Stability Analysis

3. Physico –Chemical Properties
• Organoleptic Properties
• Particle Size And Shape
• Purity
• Surface Area

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◇ Organoleptic Properties
Colour :- Off white , Cream yellow
Odour :- Pungent , fruity , odourless
Taste :- Acidic , Bitter , Intense sweet , Tasteless

5. Particle Size And Shape
◇ Particle size can influence variety of
important factors :
1. Dissolution rate
2. Suspendability
3. Uniform distribution
4. Lack of grittines
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* Methods to determine Particle size :
•Sieving
•Microscopy
•Sedimentation Rate Method

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# Particle shape will influence the surface area, flow of particle,
packing & compaction properties of the particles.
Particle Shape :-
Spherical
smooth
Spherical
rough
Spherical
irregular
acicular Angular

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Purity :-
• Purity studies are essential for further studies to be carried out
safely.
• Impurities may make a compound toxic .
• TLC , HPLC , GC and Paper chromatography is used.

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Surface area :-
• Particle size and surface area are inversely related to each other.
• Smaller the drug particle , greater the surface.

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Bulk Characterisation
• Crystallinity and Polymorphism
• Hygroscopicity
• Fine Particle characterization
• Thermal effects
• Powder flow Properties

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Physical Description and Bulk Charateization
Drugs can be used as
Solids (extensively)
Liquids (less extent)
Gases (less extent)
Because ease of Preparation

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The various Physical and bulk charateristics are
Crystallinity and Polymorphism :-
Solid drugs may occurs as
Amorphous ( higher solubility)
Crystalline ( higher stability)
Amorphous crystalline Characters of drugs have great importance
Ease of formulation
and handling
Chemical stability Biological Activity

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1. Amorphous Drugs :-
•A drug have randomly arranged atoms or molecules
•Amorphous forms are prepared by
Precipitation (Rapid)
Lyophilization
Rapid cooling Method
Advantages :-
Amorphous form
Higher solubility
Higher dissolution Rate

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Disadvantages :-
On storage Revert to more stable form
This instability occurs during bulk processing
Or
Within dosage form
Less stable

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Crystalline Drugs :-
Crystals are characterized by
Repetitious spacing of constituent atoms or molecules
In three dimentional array

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Crystalline forms of drugs is used because
Greater stability
For example :- Crystalline penicillin G as potassium or sodium salt
More stable and excellent therapeutic response than
amrphous form

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Polymorphism
Polymorphism is ability of compound to
Crystalline as more than one distinct crystalline species.
With different
Internal lattices
Crystal packing arrangement
Chemically identical
It depends on variation in
• Temperature
• Solvent
• Time

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Chemical stability and solubility changes due to
Polymorphism  can have impact on
Bioavailability Development program

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Setting acceptance criteria for polymorphism
Conduct polymorphism
Screening on drug
Can different
polymorphism be
formed
no No further
action
Characterize the form
Does the form have different properties
No further testes Is drug safty
efficay
Set acceptance
criteria for
polymorphism
yes
Does drug product
performance testing provide
adequate control
Monitor polymorph form
during stability of drug product
no

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Establish acceptance criteria
yes
Does a change occur which
could affect safety
Establish acceptance criteria which are
consistent with safety and efficacy
yes
No need to set acceptance
criteria for polymorph
change in drug product

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Thermal Analysis :-
1. Differential scanning colorimetry (DSC) or Differential
Thermal analysis (DTA)
Measure Heat loss or gain Due to physical or chemical changes
2. Thermo gravimetric analysis (TGA)
Measure changes in weight as
Function of time
temperature

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Uses :-
• To check purity , polymorphism, salvation , degradation and
excipient compatibility
• Used to investigate and predict
• physicochemical interaction between components.
• Used for selection of chemically compatible excipients.

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• Important technique for establishing.
• Batch to batch reproducibility of a crystal form
X Ray Diffraction :-

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Fine particle Characterization
• Size , shape and surface morphology of drug particles
Affect
Flow Property Dissolution Chemical Reactivity
Methods to evaluate Particle Size and Distribution
• sieving or Screening.
• Optical microscopy
• Sedimentation
• Stream scanning

24. Thanks!
You can find me at:
◇ Instagram @sarveshbari07
◇ sarveshbari70@gmail.com
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