Preformulation studies || objectives definition properties parameters all details preformulation || Trek Pharma

 

                                   PREFORMULATION STUDIES

Preformulation definition:

It is defined as the phase of research and development in which preformulation studies characterize physical and chemical properties of a drug molecule in order to develop safe, effective and stable dosage form.

Objectives:

To establish the physico-chemical parameters of a new drug entity

To determine its kinetics and stability

To establish its compatibility with common excipients \it provides insights into how drug products should be processed and stored to ensure their quality.

PREFORMULARION PARAMETERS OR PROPERTIES

OR PROTOCOL OF PREFORMULATION OR

PRINCIPLE AREAS PREFORMULATION

physico-chemical properties:

Organoleptic properties

Particle size and shape

Surface area

Purity

Bulk characterization:

Crystallinity and polymorphism

Hygroscopicity

Particle size characterization

Bulk density

Powder flow properties

Solubility analysis:

Ionization constant pka

pH solubility profile

Common ion effect

Thermal effect

Partition co-efficient

Solubilization

Dissolution

Stability analysis:

Solution stability

Solid state stability

Bulk stability

Compatibility

_

PHYSICO-CHEMICAL PROPERTIES

Organoleptic properties:

Colour, order, taste of the new drug must be recorded.

Colour in off-white, cream, yellow, tan, shiny

Odour in pungent, sulphorous, fruity, aromatic, odorless

Taste in acidic, bitter, bland, intense, sweet, tasteless

Particle size and shape:

Various chemical and physical properties of drug substances are affected by their particle size distribution and shapes.

Technique particle size

Technique particle size

Microscopic

1-100

Sieve

>5

Sedimentation

>1

Elutriation

1-50

Centrifugal

<50

Permeability

>1

Light scattering

0.5 - 50

The effect is not only on the physical properties of solid drugs but also on their biopharmaceutical behavior.

BULK CHARACTERIZATION

Crystallinity and polymorphism:

Crystal habit and internal structure of drug can affect bulk and physico-chemical property of molecule.

Crystal habit is description of outer appearance of crystal

Internal structure is molecular arrangement within the solid.

Compounds have several different habits, depending on the environment for polymorphs depends on solvents, temperature, pressure, rate of cooling, etc.

Polymorphic transitions can also occur during milling, granulating, drying and compressing operations.

Different polymorphs vary in physical properties such as dissolution, solid-state stability, compatibility, etc.

Bulk density:

Bulk density I defined as total mass per unit volume.

Partition coefficient:

The lipophilicity of an organic compound is usually described in terms of a partition coefficient log P.

pH solubility profile:

The solubility of acidic or basic drug will show different in solubility with changes in pH.

The relationship between solubility of the acidic drug and pH is given by the equation:

pH= pKa + log [cs]/[ca]

pKa= negative logarithm

[cs]= molar concentration of the salt form in water

[ca]= molar concentration of free acid in water

 

 

 

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